Schiff bases of isatin with aminothiazole, its N-mannich bases and Spiro isatin derivatives were synthesized. Their chemical structures were confirmed by Infrared, 1H-Nuclear Magnetic Resonance data and elemental analysis. Antimicrobial evaluation was performed by the agar diffusion method against four pathogenic bacteria and two pathogenic fungi. Anti-inflammatory activity was tested by carragenin-induced rat paw edema and compounds were evaluated for analgesic action by the acetic acid-induced writhing method; Compounds Aa, Ab and A5, A6 were found to be active against bacteria and fungi. The compounds A3, A6, Aa and Ab showed anti-inflammatory activity, having a percentage protection value of 34.69, 32.65, 38.77 and 36.73 as compared with that of indomethacin, with % protection of 46.93. Similarly, the compounds Aa, Ab and A6 showed analgesic activity, with % protection of 67.51, 64.78 and 49.81 as compared with the standard with % protection of 79.56.
The reaction of p-bromoanilino acetohydrazide(II) with aromatic aldehydes in alcohol yielded 2-[4-bromo aniline] N-substituted benzylidine hydrazides (IIIa-IIIj), which in presence of yellow mercuric oxide and iodine in DMF, yielded corresponding 4-bromo[(N-5-substituted 1,3,4 oxadiazole-2 -yl)methyl]aniline (IVa-IVj). Structures of the compounds synthesized were confirmed by IR, (1)HNMR and MASS spectroscopic analysis. The newly synthesized compounds were screened for antibacterial, antifungal and anti-inflammatory activities. Some of the compounds showed remarkable antibacterial, antifungal and anti-inflammatory activities.
The aim of this research was to investigate the effect of the duration of ultrasonication energy on the physicochemical characteristics of the nano-sized particulate drug delivery systems. For this purpose, meloxicam-loaded vitamin E d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS)-emulsified poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles were designed by using ultrasonication-solvent evaporation technique and were characterized by photon correlation spectroscopy for size and size distribution, scanning electron microscopy for surface morphology and laser Doppler anemometry for surface charge. Ultraviolet -spectrophotometer was used to measure the drug encapsulation efficiency and to obtain in vitro drug release profile. The results showed that the physicochemical properties of the prepared nanoparticles are effectively controlled by the amount of shear stress transferred from the energy source to the emulsion, which is strongly correlated to the ultrasonication time.
A three-dimensional quantitative structure-activity relationship (3D QSAR) of 44 structurally and functionally diverse series of 1- (Naphthylalkylimidazoles) as antiepileptic agents was studied using the Comparative molecular similarity indices analysis (CoMSIA) method. A training set containing 34 molecules served to establish the models. The optimum CoMSIA model obtained for the training set were all statistically significant, with cross-validated coefficients (q(2)) of 0.725 and conventional coefficients (r(2) (ncv)) of 0.998. The predictive capacities of the model were successfully validated by using a test set of 10 molecules that were not included in the training set. CoMSIA model (Model 1) obtained from the hydrophobic and Hbond acceptor field was found to have the best predictivity, with a predictive correlation coefficient (r(2) (pred)) of 0.67. The information obtained from this 3D-QSAR model can be used to guide the development of imidazoles as novel antiepileptic agents.
A series of 2-[2-(2,6-dichlorophenyl)amino]benzyl-3-(5-substituted phenyl-4,5-dihydro-1H-pyrazol-3-yl-amino)-6,8-dibromoquinazolin-4(3H) ones 6a-m have been synthesized by the reaction of 2-[2-(2,6-dichlorophenyl)amino]benzyl-3-substituted phenylacrylamido-6,8-dibromoquinazolin-4(3H) ones 5a-m with hydrazine hydrate in the presence of glacial acetic acid. The chalcones 5a-m were prepared by the condensation of 2-[2-(2,6-dichlorophenyl)amino]benzyl-3-acetamido-6,8-dibromoquinazolin-4(3H)one 4 with different substituted aromatic aldehyde. The benzoxazinone 2 was synthesized from 2-[2-(2,6-dichlorophenyl)amino]phenyl acetyl chloride 1 on treatment with 3,5-dibromoanthranilic acid in pyridine, which on reaction with hydrazine hydrate and then on acetylation reaction yielded 4. The structures of these compounds have been elucidated by elemental analyses, IR, and NMR spectral data. The title compounds pyrazolyl-quinazolin-4(3H)ones 6a-m were evaluated for their antibacterial and antifungal activities in vitro.
A journal is always judged based on the quality of papers, such as original papers, reviews, editorials, letters to the editor, being published and these articles play a most crucial role in research process. A high-quality publication is a means of science communication and collaboration of scientists in their field of expertise.  High-quality publications attract more attention of other researchers, stimulating new ideas and becoming highly cited. They boost authors’ research profile, strengthen positions of institutions supporting scientific productivity, and increase chances to get funding for future research studies. Currently, in most countries, academic promotion of an individual, recruitment, and distribution of financial sources for research are all subjected to the evaluation of a researcher/institution profile in world renowned indexing systems and catalogues, such as PubMed, Scopus, Index Copernicus, Institute for Scientific Information (ISI), etc.  .
Metformin hydrochloride is an oral antidiabetic biguinide agent, used in the management of non-insulin-dependent (type-2) diabetes mellitus. The purpose of present work was to formulate tasteless complexes of metformin hydrochloride with indion 234 and to evaluate molecular properties of drug complexes. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, mode of mixing, ratio of drug to resin, and temperature. Drug resin complexes (DRC) were evaluated for taste masking and characterized by x-ray diffraction study and infrared spectroscopy. Metformin hydrochloride release from DRC is obtained at salivary and gastric pH and in the presence of electrolytes. The efficient drug loading was evident in batch process using activated indion 234 with a pH of 3.5 and drug-resin ratio of 1:1.2, while temperature enhances the complexation process. Infrared spectroscopy revealed complexation of -NH (drug) with indion 234. DRC are amorphous in nature. Drug release from DRC in salivary pH was insufficient to impart bitter taste. Volunteers rated the complex as tasteless and agreeable. Complete drug release was observed at gastric pH in 3 h. The drug release was accelerated in the presence of electrolytes. Indion 234 is inexpensive, and the simple technique is effective for bitterness masking of metformin.
Using the water eliminated mechanism, reactions of 4-pyridinecarboxylic acid hydrazide and salicylaldehyde, benzaldehyde, cinnamaldehyde, and formaldehyde afforded the corresponding N(4)[(E)-1-(2-hydroxyphenyl) methylidene] (NHPM), N(4)-[(E)-2-phenylethylidene] (NPI), N(4)[(E,2E)-3-phenyl-2-propenylidene] (NPPI), and N(4)[(E) ethylidene] (NEI) isonicotinohydrazide, in high yields, after several minutes, as reported. These new compounds have shown antitumor activity against two kinds of cancer cells, which are K562 (human chronic myeloid leukemia) and Jurkat (human T lymphocyte carcinoma).
In the present study, five new derivatives (GG4 to GG8) of benzothiazoles were synthesized and evaluated against Staphylococcus aureus (MTCC 737), Pseudomonas aeruginosa (MTCC 424), Escherichia coli (MTCC 1687), and yeast-like fungi Candida tropicalis. p-Toluidine on treatment with ammonium thiocynate formed 2-benzothiazolamines (II), which on reaction with hydrazine hydrate formed a hydrazino derivative (III). Compounds GG4 to GG8 were synthesized by reacting the hydrazine derivative with different acetophenones. All the synthesized compounds were identified by IR and (1)H-NMR, and antimicrobial activity was performed on the synthesized compounds. Presence of NO(2), Br, OCH(3), and Cl groups to the substituted benzothiazole enhanced the antibacterial and antifungal activities.
The present study was designed to evaluate the antidepressant potential of 5-HT3 receptor antagonist N-n-propyl-3-ethoxyquinoxaline-2-carboxamide (6n). The compound '6n' with optimum log P and pA 2 value identified from a series of compounds synthesized in our laboratory was subjected to forced Swim Test (FST) (1, 2, and 4 mg/kg, i.p) and Tail Suspension Test (TST) (1, 2, and 4 mg/kg, i.p.). The compound '6n' significantly reduced the duration of immobility in mice without affecting the baseline locomotion. Moreover, '6n' (2 mg/kg, i.p.) potentiated the 5-hydroxytryptophan (5-HTP)-induced head twitch responses in mice and '6n' at tested dose (1 and 2 mg/kg, i.p.) reversed the reserpine-induced hypothermia in rats. In interaction studies of '6n' with various standard drugs/ligands using FST, '6n' (1 mg/kg, i.p.) potentiated the antidepressant effect of venlafaxine (4 and 8 mg/kg, i.p.) and fluoxetine (10 and 20 mg/kg, i.p.). Additionally, '6n' (1 and 2 mg/kg, i.p.) influenced the effect of harmane (5 mg/ kg, i.p.) as well as reversed the effect of parthenolide (1 mg/kg, i.p.) by reducing the duration of immobility in FST. Furthermore, '6n' (1 mg/kg, i.p.) potentiated the effect of bupropion (10 and 20 mg/kg, i.p.) in TST. Chronic '6n' (1 and 2 mg/kg, i.p.) treatment attenuated the behavioral abnormalities in olfactory bulbectomized rats. In conclusion, these various findings reiterated the antidepressant-like effects of '6n' in behavioral models of depression.
Metformin hydrochloride (MET) sustained-release solid dispersions (SD) were prepared by the solvent evaporation and closed melt method, using compritol 888 ATO as the polymer with five different drug-carrier ratios. Characterization of solid dispersion was carried out by Fourier Transform Infrared (FTIR) spectroscopy, ultraviolet (UV) spectroscopy, Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD). The FTIR and UV studies suggested that no bond formation had occurred between the polymer and the drug. DSC and XPRD results ruled out any interaction or complex formation between the drug and the polymer. The formulated SD had acceptable physicochemical characters and SD with a 1 : 4 drug : Polymer ratio, which released the drug over an extended period of eight-to-ten hours. The data obtained from the in vitro release studies were fitted with various kinetic models and were found to follow the Korsmeyer-Peppas equation. The prepared SD showed good stability over the studied time period. The solvent evaporation method was found to be more helpful than the closed melt method, giving the sustained release action. The SD with a 1 : 4 ratio of drug to polymer, by the solvent evaporation method, was selected as the most effective candidate for the subsequent development of a well-timed, sustained-release dosage form of the drug.
Monoamine oxidase B (MAO-B) inhibitory potential of adenosine A(2A) receptor (AA(2A)R) antagonists has raised the possibility of designing dual-target-directed drugs that may provide enhanced symptomatic relief and that may also slow the progression of Parkinson's disease (PD) by protecting against further neurodegeneration. To explain the dual inhibition of MAO-B and AA(2A)R at the molecular level, molecular docking technique was employed. Lamarckian genetic algorithm methodology was used for flexible ligand docking studies. A good correlation (R(2)= 0.524 and 0.627 for MAO-B and AA(2A)R, respectively) was established between docking predicted and experimental K(i) values, which confirms that the molecular docking approach is reliable to study the mechanism of dual interaction of caffeinyl analogs with MAO-B and AA(2A)R. Parameters for Lipinski's "Rule-of-Five" were also calculated to estimate the pharmacokinetic properties of dual-target-directed drugs where both MAO-B inhibition and AA(2A)R antagonism exhibited a positive correlation with calculated LogP having a correlation coefficient R(2) of 0.535 and 0.607, respectively. These results provide some beneficial clues in structural modification for designing new inhibitors as dual-target-directed drugs with desired pharmacokinetic properties for the treatment of PD.
The ABC and VED (vital, essential, desirable) analysis of the pharmacy store of Post Graduate Institute of Medical Education and Research (PGIMER), Chandigarh, India, was conducted to identify the categories of items needing stringent management control. The annual consumption and expenditure incurred on each item of pharmacy for the year 2007-08 was analyzed and inventory control techniques, i.e. ABC, VED and ABC-VED matrix analysis, were applied. The drug formulary of the pharmacy consisted of 421 items. The total annual drug expenditure (ADE) on items issued in 2007-08 was Rs. 40,012,612. ABC analysis revealed 13.78%, 21.85% and 64.37% items as A, B and C category items, respectively, accounting for 69.97%, 19.95% and 10.08% of ADE of the pharmacy. VED analysis showed 12.11%, 59.38% and 28.51% items as V, E, and D category items, respectively, accounting for 17.14%, 72.38% and 10.48% of ADE of the pharmacy. On ABC-VED matrix analysis, 22.09%, 54.63% and 23.28% items were found to be category I, II and III items, respectively, accounting for 74.21%, 22.23% and 3.56% of ADE of the pharmacy. The ABC and VED techniques need to be adopted as a routine practice for optimal use of resources and elimination of out-of-stock situations in the hospital pharmacy.
The aim of this study was to evaluate the influence of disintegration mechanism of various types of disintegrants on the absorption ratio (AR), wetting time (WT), and disintegration time (DT) of orodispersible tablets (ODTs). ODTs were prepared by direct compression using mannitol as filler and disintegrants selected from a range of swellable, osmotic, and porous disintegrants. Tablets formed were characterized for their water AR, WT, and DT. The porosity and mechanical strength of the tablets were also measured. Results show that the DT of formulated ODTs was directly related to the WT and was a function of the disintegration mechanism of the disintegrant used. The lowest WT and DT were observed for tablets formulated using the osmotic disintegrant sodium citrate and these tablets also showed the lowest AR and porosity. The wetting and disintegration of tablets containing the highly swellable disintegrant, sodium starch glycollate, was slowest despite their high water AR and high tablet porosity. Rapid wetting and disintegration of ODTs were therefore not necessarily related to the porosity of the tablets.
In Malaysia, there are 81 (as on February 15, 2013) higher education institutions including satellite branches of the foreign universities. In northern part of the Peninsular Malaysia, AIMST University is the first private not-for-profit university and aims to become a premier private university in the country and the region. The workshop described in this article was designed to develop and enhance the capacity of academic staff-in-leadership-role for the University. This type of workshops may be a good method to enhance the leadership qualities of the head of each unit, department, school and faculty in each university.
Statistical comparison of dissolution profiles under a variety of conditions relating to formulation characteristics, lot-to-lot, and brand-to-brand variation attracts interest of pharmaceutical scientist. The objective of this work is to apply several profile comparison approaches to the dissolution data of five-marketed aceclofenac tablet formulations. Model-independent approaches including ANOVA-based procedures, ratio test procedure, and pair wise procedure. The ratio test includes percentage, area under the curve, mean dissolution time, while the pair wise procedure includes difference factor (f(1)), similarity factor (f(2)), and Rescigno index. In the model-dependent approach, zero order, first order, Hixson-Crowell, Higuchi, and Weibull models were applied to the utilization of fit factors. All the approaches were applicable and useful. ANOVA with multiple comparison tests was found to be sensitive and discriminating for comparing the profiles. Weibull parameters were more sensitive to the difference between two release kinetic data in terms of curve shape and level.
The matrix tablets of diltiazem hydrochloride were prepared by direct compression using hydroxypropyl methyl cellulose (HPMC) and various amounts (2.5%, 5.0%, 10% and 20%) of citric acid, malic acid and succinic acid. The characterization of physical mixture of drug and organic acids was performed by Infra-red spectroscopy. An organic acid was incorporated to set up a system bringing about gradual release of this drug. The influence of organic acids on the release rate were described by the Peppas equation: M (t) /M(∞) = Kt (n) and Higuchi's equation: Q (t) = K(1)t(1/2). The addition of organic acids and the pH value of medium could notably influence the dissolution behavior and mechanism of drug-release from matrices. Increasing amounts of organic acid produced an increase in drug release rate, which showed a good linear relationship between contents of organic acid and drug accumulate release (%) in phosphate buffer, pH 7.4. The drug release increased significantly (P < 0.05) with use of succinic acid in tablet formulation. Increasing amounts of succinic acid above 10% produced decreasing values of n and increasing values of k, in a linear relationship, which indicated there was a burst release of drug from the matrix. Optimized formulations are found to be stable upon 3-month study.
Ayurvedic preparations contain toxic elements like heavy metals and other chemicals exceeding their permissible limits. Ayurvedic method of detoxification of such products involves Shodhana. Hence, in present paper it has been decided to replace Ayurvedic Shodhana process by chemical purification method and to study the benefits and/or drawbacks of the traditional Ayurvedic Shodhana process. Crude aconite root, Ayurvedic Shodhana treated aconite root and chemical Shodhana treated aconite root samples were evaluated for toxicity and changes by animal studies and thin layer chromatography (TLC) respectively. The results of the toxicity study suggest that the modified method of Shodhana is less efficient as compared to the traditional Ayurvedic Shodhana process. TLC studies have shown that pseudoaconitine and aconitine were converted into far less toxic substances like veratroyl pseudoaconine and benzoylaconine respectively only in traditional Ayurvedic Shodhana.
Extracts obtained from the leaves of various Alocasia species have been used in India as folk remedy for the treatment of various inflammatory ailments including rheumatism and bruise. The ethanolic extract of leaves of Alocasia indica Schott. was evaluated by using different in vitro antioxidant models of screening like scavenging of 1, 1-diphenyl-2-picryl hydrazyl (DPPH) radical, nitric oxide radical, superoxide anion radical, and hydroxyl radical. The antinociceptive activity was tested by acetic acid-induced writhing response, hot plate method, and tail flick method in albino rats. The anti-inflammatory potential of gels of ethanolic extract has been determined by using carrageenan-induced paw edema assay, formalin-induced paw edema assay, arachidonic acid-induced ear edema assay, and xylene-induced ear edema assay. The extract showed remarkable antioxidant activity in all models, comparable to the standard reference drug ascorbic acid. The ethanolic extract of Alocasia indica and its gels produced dose-dependent antinociceptive and anti-inflammatory activity, respectively. This finding suggests that ethanolic extract of A. indica possess potent antinociceptive and anti-inflammatory activity possibly due to its free radical scavenging properties.
Premna esculenta Roxb. (family Verbenaceae) is a shrub used by the ethnic people of Chittagong Hill Tracts of Bangladesh for the treatment of hepatocellular jaundice. The present study was done to evaluate the hepatoprotective and the in vivo antioxidant activity of ethanolic extracts of leaves of the plant in carbon tetrachloride-induced liver damage in rats. Hepatotoxicity was induced in rats by i.p. injection of CCl4 diluted with olive oil (1:1 v/v; 1 mL/kg body weight) on alternate days for 7 days. After 7 days of pretreatment of test extracts, the biochemical markers such as Serum Glutamate Oxaloacetate Transaminase (SGOT), Serum Glutamate Pyruvate Transaminase (SGPT), Alkaline Phosphatase (ALP), total protein, and albumin were estimated followed by the measurement of liver cytosolic antioxidant enzymes such as superoxide dismutase, catalase, and peroxidase. The data were analyzed using one-way analysis of variance (ANOVA) followed by Dunnett's t-test. The extract both at the doses of 200 and 400 mg/kg p.o. significantly (P < 0.001) reduced the elevated levels of SGPT, SGOT, ALP and increased the reduced levels of total protein and albumin compared to the CCl4-treated animals. The extracts also showed a significant (P < 0.001) increase in the reduced levels of superoxide dismutase (SOD), catalase, and peroxidase. The effects of the extracts on these parameters were comparable with those of the standard, silymarin. The findings of the study indicate that the leaf extract of P. esculenta showed a potential hepatoprotective activity and the protective action might have manifested by restoring the hepatic SOD, catalase, and peroxidase levels. The results justify the traditional use of this plant in liver disorders.
The aqueous fruit extract of Cucumis sativus L. was screened for free radical scavenging and analgesic activities. The extract was subjected to in vitro antioxidant studies at 250 and 500 μg/ml and analgesic study at the doses 250 and 500 mg/kg, respectively. The free radical scavenging was compared with ascorbic acid, BHA (Butylated hydroxyl anisole), whereas, the analgesic effect was compared with Diclofenac sodium (50 mg/kg). The C. sativus fruit extract showed maximum antioxidant and analgesic effect at 500 μg/ml and 500 mg/kg, respectively. The presence of flavonoids and tannins in the extract as evidenced by preliminary phytochemical screening suggests that these compounds might be responsible for free radical scavenging and analgesic effects.
Acyclovir is an antiviral drug used for the treatment of herpes simplex virus infections, with an oral bioavailability of only 10-20% [limiting absorption in gastrointestinal tract to duodenum and jejunum] and half-life of about 3 h, and is soluble only at acidic pH (pKa 2.27). Mucoadhesive polymeric nanodrug delivery systems of acyclovir have been designed and optimized using 2(3) full factorial design. Poly (lactic-co-glycolic acid) (PLGA) (50:50) was used as the polymer along with polycarbophil (Noveon AA-1) as the mucoadhesive polymer and pluronic F68 as the stabilizer. From the preliminary trials, the constraints for independent variables X(1) (amount of PLGA), X(2) (amount of pluronic F68) and X(3) (amount of polycarbophil) have been fixed. The dependent variables that were selected for study were particle size (Y(1)), % drug entrapment (Y(2)) and % drug release in 12 h (Y(3)). The derived polynomial equations were verified by check point formulation. The application of factorial design gave a statistically systematic approach for the formulation and optimization of nanoparticles with the desired particle size, % drug release and high entrapment efficiency. Drug: Polymer ratio and concentration of stabilizer were found to influence the particle size and entrapment efficiency of acyclovir-loaded PLGA nanoparticles. The release was found to follow Fickian as well as non-Fickian diffusion mechanism with zero-order drug release for all batches. In vitro intestinal mucoadhesion of nanoparticles increased with increasing concentration of polycarbophil. These preliminary results indicate that acyclovir-loaded mucoadhesive PLGA nanoparticles could be effective in sustaining drug release for a prolonged period.
I have read the article titled “Pharmacovigilance: A worldwide master key for drug safety monitoring,” and I found the topic quite informative and it also included recent updates. So first of all, I congratulate the authors for such a nice compilation. It covers almost all areas; however, I would like to add more information about pharmacovigilance in vaccines. The great challenge here is to convey a proper message to the general public as it is like a double-edged sword.  Majority of vaccines are administered to vulnerable (children) as well as healthy population that requires strict safety supervision. Therefore, the safety of a vaccination must be more than other pharmacological agents to make it acceptable in general population.  .Read more...,
Ondansetron hydrochloride, a 5 HT3 antagonist is a powerful antiemetic drug which has oral bioavailability of 60% due to hepatic first pass metabolism and has a short half-life of 5 h. To overcome the above draw back, the present study was carried out to formulate and evaluate fast dissolving films of ondansetron hydrochloride for sublingual administration. The films were prepared from polymers such as polyvinylalcohol, polyvinyl pyrrolidone, Carbopol 934P in different ratios by solvent casting method. Propylene glycol or PEG 400 as plasticizers and mannitol or sodium saccharin as sweeteners were also included. The IR spectral studies showed no interaction between drug and polymer or with other additives. Satisfactory results were obtained when subjected to physico-chemical tests such as uniformity of weight, thickness, surface pH, folding endurance, uniformity of drug content, swelling index, bioadhesive strength, and tensile strength. Films were also subjected to in vitro drug release studies by using USP dissolution apparatus. Ex vivo drug permeation studies were carried out using porcine membrane model. In vitro release studies indicated 81-96% release within 7 min and 66-80% within 7 min during ex vivo studies. Drug permeation of 66-77% was observed through porcine mucosa within 40 min. Higher percentage of drug release was observed from films containing the sweeteners. The stability studies conducted for a period of 8 weeks showed no appreciable change in drug content, surface pH, and in vitro drug release.
Hypertension is the very common chronic disease in rural, urban and semi-urban areas of today's world, which needs continuous monitoring and treatment through out the life. Lack of education, lifestyle modification, and low level of understanding on disease management in rural people will influence directly on their quality of life (QOL). The objective of this study was to know the impact of clinical pharmacist interventions on medication adherence and QOL. It was a prospective, randomized and interventional study. Fifty-six patients were enrolled; only 52 patients completed the study. Interventional group patients received patient counselling, patient information leaflets (PILS), and frequent telephonic reminding. In the baseline, first and second follow-ups, medication adherence and QOL were assessed by using Morisky Medication Adherence Scale (MMAS) and Medication Adherence Report Scale (MARS) Questionnaires and SF-12v2 Quality of life Questionnaire in both the groups. The results showed that systolic blood pressure P value in the second follow-up was 0.086+ when compared to baseline follow-up P value 0.094. The diastolic blood pressure reading of the intervention group at the second follow-up was 77.73 ± 3.63 in mmHg when compared to the baseline, i.e. 86.62 ± 11.35 in mmHg. The MMAS and MARS scores P values were 0.007(**), 1.000, <0.001(**); 0.007, 0.014 and 0.000 at the baseline, first and second follow-ups, respectively. The QOL score P values of physical component scale and mental component scale showed highly significant. This study concluded/showed that the impact of clinical pharmacist provided patient counselling had a positive impact on medication adherence and QOL.
The study is aimed to explore the perceptions and experiences of hypertensive patients toward medication use and adherence. The study was qualitative in nature conducted at Sandamen Provisional Hospital of Quetta city, Pakistan; a public hospital catering to the health needs of about 40% of the population. A qualitative approach was used to gain an in-depth knowledge of the issues. Sixteen patients were interviewed, and the saturation point was achieved after the 14(th) interview. All interviews were audio-taped, transcribed verbatim, and were then analyzed for thematic contents by the standard content analysis framework. Thematic content analysis yielded five major themes. (1) Perceived benefits and risks of medications, (2) physician's interaction with patients, (3) perception toward traditional remedies, (4) layman concept toward medications, and (5) beliefs toward hypertension and its control. The majority of the patients carried specific unrealistic beliefs regarding the long-term use of medication; yet these beliefs were heavily accepted and practiced by the society. The study indicated a number of key themes that can be used in changing the beliefs and experiences of hypertensive patients. Physician's attitude, patient's past experiences, and knowledge related to hypertension were noted as major contributing factors thus resulting in nonadherence to therapy prescribed.
In India, interruptions to highly active antiretroviral therapy (HAART) are due to adverse drug reactions. This study was aimed to assess the association between HAART adherence and adverse drug reactions (ADRs) in human immunodeficiency virus (HIV) patients. This prospective study was conducted at a Medicine department in a South Indian tertiary care teaching hospital. HIV-positive patients were interviewed for adherence using ACTG adherence questionnaire and intensively monitored for ADRs to HAART. The percentage of adherence was calculated based on missed doses, and graded as less than 80%, 80-95%, and >95%. The World Health Organization (WHO) probability scale was used for causality assessment. Logistic regression analysis as well as univariate analysis was used to assess the association (P value < 0.05). A total of 105 HIV-positive patients had been taking HAART out of whom 50 (47.6%) patients agreed for adherence assessment, and 23 (21.9%) refused due to social stigma. Upon evaluation of the patient characteristics in the reported adherence, 78% were in males (53.8%) and 22% were in females (46.2%) with the level of adherence greater than 95%. Six (12%) patients had a regular alcoholic intake with adherence less than 80% compared to 31 (62%) patients who never had any alcoholic intake (P < 0.05). A significant association between ADRs and adherence was found (P < 0.05). Causality found by the WHO scale was "probable." Clinicians must focus on education regarding the need for adherence, possible adverse effects, and early detection and prevention of ADRs to HAART.
Cancer is a malignant disease that is characterized by rapid and uncontrolled formation of abnormal cells which may mass together to form a growth or tumor, or proliferate throughout the body. Next to heart disease, cancer is a major killer of mankind. This study aims at a preliminary phytochemical screening and anticancer evaluation of Adiantum venustum Don against Ehrlich Ascites Carcinoma in animal model. The findings indicate that ethanolic extract of A. venustum Don possesses significant anticancer activity and also reduces elevated level of lipid peroxidation due to the presence of terpenoids and flavonoids. Thus, ethanolic extract of A. venustum Don could have vast therapeutic application against cancer.
To establish the Quality standards of Triticum aestivum L, seeds as per WHO guidelines. To study the antioxidant and hepatoprotective profile of T. aestivum L. seeds.
Pharmacognostic studies like morphological, microscopical, physico-chemical, phytochemical evaluation, fluorescence analysis, TLC, HPTLC, phytochemical analysis etc. of various extracts of the seeds of T. aestivum were carried out as per established methods. The ethanolic extract was evaluated for antioxidant and hepatoprotective activity using rat model.
Preliminary phytochemical analysis mainly revealed the presence of carbohydrates, phenolics, proteins, resins, lipids and flavonoids. T. aestivum at different doses, i.e. 5-45 μg/ml showed free radical scavenging activity in dose dependent manner. The amount of phenolic components was found to be 313.5 μg/mg indicating considerable antioxidant activity. The ethanolic extract of T. aestivum was administered at dose level of 100 mg/kg/day, every day for 21 days along with CCl4. Biochemical and histopathological results conclude that the seeds have hepatoprotective activity.
The compounds, 2-(methylsulfonyl)-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylic acid (DM3), 2-(phenylsulfonyl)-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylic acid (DM(4)), and 2-(p-toluenesulfonyl)-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylic acid (DM(5)) were synthesized by coupling of 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylic acid (DM(2)) with methanesulfonyl chloride, benzenesulfonyl chloride, and toluenesulfonyl chloride, which in turn, was synthesized by dissolving dilute aqueous ammonia with 2-(N-hydroxy methyl amino)-indol-3-yl-propanoic acid (DM(1)) which is the reaction product of l-tryptophan and formalin. All the intermediates and title compounds were characterized by physical, chemical, analytical, and spectral data. All the title compounds have been screened for in vivo antidiabetic activity in streptozotocin-induced diabetic rats, and serum glucose was estimated spectrophotometrically at 505 nm by glucose oxidase/peroxidase method. Compound DM(5) showed potent antidiabetic activity.
A series of novel 1[5"-(2"'-substituted phenyl)-4",5"'-dihydro isoxazole-3"-yl]-3-[(4 substituted phenyl)imino]1-3-dihydro-2H-indole-2-one were synthesized from different substituted chalconised indole-2,3-dione was prepared from the different chalconised Isatin. The structures of the compounds were elucidated by elemental and spectral (IR, (1)H NMR, and MS) analysis. The synthesized compounds were screened for their analgesic activity by the acetic acid induced Writhing method and in vitro antimicrobial activity against the Gram-positive bacteria-Staphylococcus aureus and the Gram-negative bacteria-Pseudomonas auroginosa, Pseudomonas mirabilis, and E. coli by the cup plate agar diffusion method. Compounds 6a(1), 6a(3), 6b(3), and 6b(2) were found to be active against bacteria. The compounds 6a(1), 6b(3), and 6a(3) show a significant analgesic activity. Synthesized compounds also screened for anthelmintic activity against Pheretima posthuma. Compounds 6a(1), 6b(1), and 6b(3) show significant anthelmintic activity.
Wound healing is a significant healthcare problem in today's medical practice. Despite extensive treatment modalities that are supposed to hasten the wound healing process, the outcomes of existing methods are far from optimal. One such agent that has been tried previously and found controversial in wound healing is phenytoin. In this study, the wound-healing efficacy of phenytoin was investigated in albino rats.
20 male Wistar albino rats were subjected to excisional wounds measuring 500 mm(2) on the back and then randomized to two groups (n = 10): Control group (A) and treatment group (B). The control group received no drug treatment till the end of the study. 1% Phenytoin cream was applied to the wounds of rats in the group B and continued till the 16(th) day of the study. The areas of wounds were measured on the Days 4, 8, 12, and 16 of the experiment. The percentages of the healing wounds were calculated by Walker formula after measurement of the wound area. The total number of days required for complete epithelization of wounds was noted in each group.
Statistically significant reduction (P < 0.05) in average wound area was seen in Group B (P value=0.0017, 0.0001, 0.0001, 0.0001), respectively, on Days 4, 8, 12, and 16 of the experiment in comparison to Group A. The average number of days required for complete epithelization of wound area was less in Group B as compared to Group A (P=0.0120). The difference was statically significant
In the present study, topical phenytoin accelerated healing of excisional wound in albino rats.
The aim of the present investigation was to develop sustained release ethylcellulose-coated egg albumin microspheres of diltiazem hydrochloride (DH) to improve patient compliance. The microspheres were prepared by the w/o emulsion thermal cross-linking method using different proportion of the polymer to drug ratio (1.0:1.0, 1.0:1.5 and 1.0:2.0). A 3(2) full factorial design was employed to optimize two independent variables, polymer to drug ratio (X(1)) and surfactant concentration (X(2)) on dependent variables, namely % drug loading, % drug release in 60 min (Y(60)) and the time required for 80 % drug release (t(80)) were selected as dependable variable. Optimized formulation was compared to its sustained release tablet available in market. The polymer to drug ratio was optimized to 1:1 at which a high drug entrapment efficiency 79.20% ± 0.7% and the geometric mean diameter 47.30 ± 1.5 mm were found. All batches showed a biphasic release pattern; initial burst release effect (55% DH in 1 h) and then were released completely within 6 h. In situ coating of optimized egg albumin DH microspheres using 7.5% ethylcellulose significantly reduced the burst effect and provided a slow release of DH for 8-10 h. Finally, it was concluded that ethylcellulose-coated egg albumin DH microspheres is suitable for oral SR devices in the treatment of angina pectoris, cardiac arrhythmias, and hypertension due to their size and release profile.
Parkinson's Disease (PD) is a neurodegenerative disorder in the nigrostriatal pathway of animals and humans and is responsible for most of the movement disorders, including rigidity. The present study aimed to determine the effect of chronic cigarette smoke, alcohol intake, and frequent sexual mating on 1-Methyl-4-phenyl-1,2,3,6-tertahydro pyridine (MPTP)-induced rat model of PD. After treatment, the effect of these factors was determined by biochemical and molecular evaluation. Dopamine (DA) concentration, antioxidant enzymes, and mitochondrial activity decreased after treatment with cigarette smoke, alcohol, and frequent sexual mating when compared to the values in the control group. Excessive exposure of these factors may lead to neurodegeneration, dopaminergic toxicities, and, ultimately, clinical parkinsonism. Earlier literature from different publisher suggested that nicotine and cigarette smoke can protect the dopaminergic neurons in the substantia nigra against MPTP toxicity. In this study, we assessed the effect of the above three factors on an MPTP-treated rat model and concluded that they have a neurodegenerative effect and were found to be toxic to dopaminergic neurons in the substantia nigra. Further investigation is required to understand the exact etiology of clinical parkinsonism.
The present study was designed to investigate the effects of different variables on the release profile of ibuprofen microspheres formulated using modified emulsification method. Eight batches of microspheres (F1-F8) were prepared by applying 2(3) factorial design. The amount of sodium alginate, amount of calcium chloride, and amount of magnesium stearate were selected as formulation variables. All the batches were evaluated in terms of percentage yield, percentage encapsulation efficiency and in vitro release characteristics. The batch F7 was found to be optimum batch and was further characterized via scanning electron microscopy (SEM) and particle size analysis. Multiple linear regression was applied to confirm significant effect of each variable on release characteristics. The model developed in the present study can be effectively utilized to achieve the formulation with desired release characteristics.
Allergic diseases, such as allergic asthma, are hypersensitivity reactions initiated by immunological mechanisms. Myrica esculenta (M. esculenta) is known traditionally in Ayurveda to possess anti-asthmatic activity. The present investigation was undertaken to evaluate the effect of crude extract of stem bark of M. esculenta (Family Myricaceae, commonly known as Kaiphal) on experimental allergic reactions. Experimental models studied were allergic pleurisy and vascular permeability induced by acetic acid in mice. Pretreatment with M. esculenta (75 mg/kg and 150 mg/kg, p.o.) significantly inhibited the eosinophil accumulation (P < 0.01) respectively in the pleural cavity. M. esculenta (75 and 150 mg/kg, p.o.) significantly inhibited the rise in plasma exudation (57.12% and 59.77%, P < 0.01) induced by acetic acid in mice. These findings demonstrate that the crude extract from the stem bark of M. esculenta possesses antiallergic activity. This activity may be mediated by reducing the release of mediators such as histamine, inhibition of mast cell degranulation, and inhibition of eosinophil accumulation thereby preventing the release of cytokines and chemokines.
The hypoglycemic effects of the fruit extract of C. metuliferus was investigated in normoglycemic and alloxan-induced hyperglycemic rats. The results showed that there was an insignificant (P > 0.05) decrease in the blood glucose concentration of normoglycemic rats treated with oral doses of 1000 and 1500 mg/kg of the extract. On the other hand, 500 mg/kg of the fruit extract produced an insignificant (P > 0.05) decrease in blood glucose levels of alloxan-treated rats, while 1000 and 1500 mg/kg oral dose points produced a significant (P < 0.05) decrease in the blood glucose concentration of hyperglycemic rats comparable to that produced by tolbutamide. From this study, the data suggested that the fruit extract did not alter the BGC level in normoglycemic rats, but had a potential hypoglycemic property in alloxan-induced hyperglycemic rats.
This study was carried out to investigate the effect of Aloe vera extract (AvE) on serum electrolytes, urea, and creatinine as indices of renal function in Sprague-Dawley rats. Twelve male Sprague-Dawley rats weighing between 80 and 130 g were used. Rats were divided into two groups: The control and the test groups (n=6). The test group received 1 ml of AvE daily for 28 days. Both the groups fed on standard rat chow and water ad libitum. The results showed a decrease in serum levels of sodium, and potassium, but an increase in the serum levels of bicarbonate, urea, and creatinine in the test group. The changes seen were, however, statistically insignificant, except for the serum levels of sodium and creatinine (P<0.05). It is thus concluded that AvE impairs renal handling of electrolytes with consequent hyponatremia and hypercreatinemia. However, this might be of therapeutic value in conditions associated with hypernatremia.
This study is aimed to explore the types of CAM and reasons of using CAM among elderly Malaysians.
This cross-sectional study was conducted on a sample of 256 conveniently selected elderly Malaysians who were residing in the states of Selangor and Kuala Lumpur. A pre-validated interview-administered questionnaire was used to gather information. Data was entered into PASW version 18 and analyzed.
A total of 256 questionnaires were included in the study. A response rate of 64% was achieved. Out of 256 respondents, 92 (35.9%) were male while 164 (64.1%) were female. More than half of the respondents (n = 141; 55.1%) agreed that CAM is more effective than allopathic medicine. Chinese respondents showed strong belief in the effectiveness of CAM. In terms of safety of CAM, close to three quarters of respondents (n = 178; 69.5%) believed that CAM is safer than allopathic medicine. A large majority of respondents agreed that CAM has less side effects compared to allopathic medicine (n = 201; 78.5%) and also agreed that CAM is good to maintain overall health and wellbeing (n = 212; 82.8%). A majority of the respondents expressed that they use CAM because allopathic medicine is less effective (n = 113; 44.1%).
The current study reflects the reasons of using CAM among lay public from different ethnicities. There are no reports of adverse effects related to CAM use. Future approaches should be intended for awareness campaigns for consumers, highlighting safety profile of CAM and as well as forbidding their use without the consultation of healthcare professional.
Amaranthus spinosus Linn. (Amaranthaceae) is found throughout India. This tree species has been of interest to researchers because it is a medicinal plant employed in the Indian traditional system of medicine. Pharmacognostic standardization; physico-and phytochemical evaluation of the roots of Amaranthus spinosus was carried out, to determine its macro-and microscopical characters, and also some of its quantitative standards. Microscopical studies were done by using the trinocular microscope. Total ash, water-soluble ash, acid-insoluble ash, sulfated ash values, and alcohol-and water-soluble extractive values were determined for physico-chemical evaluations. A preliminary phytochemical screening was also done to detect different phytoconstituents. Microscopically, the root showed cork, cortex, stellar region, and calcium oxalate crystals. Powder microscopy showed anamalous secondary growth in between the xylem vessels and Calcium Oxalate crystals in the cortex region. Total ash was approximately three times more than acid insoluble and water soluble ash. The ethanol soluble extractive was approximately the same as the water soluble extractive. Thin Layer Chromatography (TLC) of the Petroleum-ether extract using Benzene : Ethyl acetate (6 : 1), showed six spots. In the chloroform extract, using Benzene : Ethyl acetate (4 : 1) nine spots were seen, and in the ethanol extract, using Chloroform: Methanol (93 : 7), only four spots were observed, using Iodine vapor as a viewing medium. Phytochemically, the root exhibited terpenes, alkaloids, glycosides, and sugars. These findings might be useful to supplement information with regard to its identification parameters, which are assumed significant in the way of acceptability of herbal drugs, in the present scenario, which lacks regulatory laws to control the quality of herbal drugs.
The present study was designed to evaluate the cardioprotective effects of methanolic extract of Litsea deccanensis (MELD) against isoproterenol-induced myocardial infarction in rats by studying cardiac markers, lipid peroxidation, lipid profile, and histological changes. Male Wistar rats were treated orally with MELD (100 and 200 mg/kg) daily for a period of 21 days. After 21 days of pretreatment, isoproterenol (100 mg/kg) was injected subcutaneously to rats at an interval of 24 h for 2 days to induce myocardial infarction. Isoproterenol-induced rats showed significant (P < 0.05) increase in the levels of serum creatine kinase, lactate dehydrogenase, thiobarbituric acid reactive substances, and lipid hydro peroxides. The serum lipid levels were altered in the isoproterenol-induced myocardial infarcted rats. The histopathological findings of the myocardial tissue evidenced myocardial damage in isoproterenol-induced rats. The oral pretreatment with MELD restored the pathological alterations in the isoproterenol-induced myocardial infarcted rats. The MELD pretreatment significantly reduced the levels of biochemical markers, lipid peroxidation and regulated the lipid profile of the antioxidant system in the isoproterenol-induced rats. An inhibited myocardial necrosis was evidenced by the histopathological findings in MELD pretreated isoproterenol-induced rats. Our study shows that oral pretreatment with MELD prevents isoproterenol-induced oxidative stress in myocardial infarction. The presence of phenolic acid and flavonoid contents were confirmed by preliminary phytochemical tests. The reducing power and free radical scavenging activities of the MELD may be the possible reason for it pharmacological actions.
In our study, a series of novel 3-(4-(benzylideneamino) phenylimino) 4-fluoroindolin-2-one derivatives were synthesized and characterized by spectral (I.R, (1)H NMR, mass) and elemental analysis. The title compounds (N(1)-N(10)) were evaluated for analgesic, anti-inflammatory, and ulcerogenic index activities. Results displayed that compound N(3) exhibited significant analgesic activity. Among the title compounds studied, N(2), N(3), and N(8) exhibited significant anti- inflammatory activity comparable to reference standard diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic side effect when compared to aspirin.
The study was carried out to develop procedure for determining concentration of formaldehyde to be used for crosslinking of gelatin in the presence of drugs having amino groups. Gentamicin sulfate was used as a drug candidate due to its high content of amino acids. Gelatin crosslinking is accelerated by aldehyde-containing compounds and inhibited by amino group-containing compounds. The major modifications from already existing procedures are that the trinitrobenzenesulphonic acid (TNBS) reaction is used to detect e-amino groups of Type A gelatin in the presence of formaldehyde and further it is supported with colorimetric analysis of free formaldehyde content using a chromotropic acid regent. Since formaldehyde crosslinks amino groups, the TNBS assay can be effectively utilized for determination of complete crosslinking of gelatin with analysis of free amino acid content in crosslinked formulation. The effect of the presence of amino groups on gelatin crosslinking was estimated in the presence of gentamicin sulfate. The ε-amino content of uncrosslinked Type A gelatin was found to be 28.6 mol/gelatin molecule of 1000 residues and in case of crosslinked gelatin it varies with varying concentration of formaldehyde. The procedure stated here should be applicable to a broad range of drugs containing amino groups which are used along with gelatin or other proteinaceous materials which are applicable after crosslinking with formaldehyde.
Studies were conducted on the anthelmintic property of about 15(e-h, 1e-1h, 2d-2f and 3e-3h) synthesized aminobenzylated Mannich bases bearing N-methyl piperazine using Indian earthworms Pheritima Posthuma against piperazine citrate as standard reference. Three concentrations of each compound (0.1, 0.2, 0.3% w/v) were studied, which involved the determination of paralysis and death time of the worms. The compound 1g exhibited the most significant anthelmintic activity among all the compounds screened against the worms as compared to standard drug.
The management of cardiovascular disorders poses a dilemma for the medical fraternity. Calcium channel blockers are one of the most commonly used drugs for the management of this disorder, and it is also a well known fact that they are one of the most common group of drugs responsible for causing gingival over growth as one of their adverse effects. Amlodipine is a new generation hypertensive, which has found wide acceptance and usage due to its duration of action. Even with all its benefits as a potent hypertensive, its effect on gingival tissues is what causes concern to the patient and dental surgeon equally. The objective of this article is to create awareness regarding the adverse oral effects of amlodipine, its underlying mechanism of action in bringing about this adverse reaction, along with providing a brief review of the pharmacologic profile of this drug.
A rapid, simple and sensitive high-performance liquid chromatography (HPLC) method has been developed for quantification of olmesartan medoxomil (OLM) and amlodipine besylate (AM) in plasma. The assay enables the measurement of OLM and AM for therapeutic drug monitoring with a minimum detectable limit of 2 ng mL. The method involves a simple, one-step extraction procedure and analytical recovery was above 50%. The separation was performed on an analytical 250 × 4.6 mm Eurospher 100(-5) C18 column. The wavelength was set at 239 nm. The mobile phase was a mixture of acetonitrile:0.05 M ammonium acetate buffer: 0.1 mL triethylamine at pH 6.8 was selected at a flow rate of 1.0 mL min. The calibration curve for the determination of OLM and AM in plasma was linear over the range 2-2500 and 8-10,000 ng mL AM and OLM. The coefficients of variation for interday and intraday assay were found to be <15%. The method can be applied to a pharmacokinetic and pharmacodynamic study of OLM and AM in a combined dosage form.
Today, the use of herbal medicine for primary healthcare has increased considerably. Since local pharmacists graduate with little knowledge on herbal medicine, the majority are ill-equipped to provide pharmaceutical advice.
To develop and evaluate a herbal medicine formulary to aid healthcare professionals (HCPs) in the prescribing, dispensing and counselling responsibilities.
Monographs on all herbal substances available locally were compiled into a formulary. The formulary was then distributed to all, 216, local pharmacies. Subsequently, a questionnaire was distributed to 55 pharmacists and 10 general practitioners (GPs).
Descriptive statistical analysis.
A total of 177 herbal monographs have been compiled and 612 herbal products listed. Thirty HCPs participated in the questionnaire. The formulary was found to be useful by all participants with 19 claiming to use it frequently and 7 quite frequently. Participants (n = 30) agree that the information contained within the formulary was found to be useful (26), the formulary helped them learn which HMPs are present in the local market (29), the formulary is user friendly (27), information included is up-to-date and well referenced (29) and that there is the need for a formulary of this kind in Malta (28).
The formulary was found to be a useful tool for HCPs leading to high quality, evidence-based prescribing together with enhanced monitoring and improved patient care.