3,3'-(5,5'-methylene bis(3-mercapto-4H-1,2,4-triazole-5,4-diyl) bis (azan-1-yl-1-ylidene)diindolin-2-ones (VIIIa-t) have been synthesized by the condensation of an appropriate isatins(IIIa-t) with the intermediate 5, 51-methylene diyl bis (4-amino-4H- 1,2,4-triazole- 3-thiol)(VII). All the title compounds (VIIIa-t) were screened for Antioxidant activity and DNA Binding study, for this evaluation Ascorbic acid is employed as standard, for DNA binding Study employed DNA is Herring sperm DNA. Almost all the compounds showed free radicalscavenging activity and DNA binding to some extent. The structures of newly synthesized compounds were established on the basis of elemental analysis, IR, 1H NMR and mass spectral data.
A convenient synthesis of the 6,7,8,9 tetra hydro-5H-5-(2'-hydroxy phenyl)-2-(4'-some substituted benzylidine)-3-(4-nitrophenyl amino) thiazolo quinazoline ring system is reported. Our syntheticapproach consisted of the annelation of a 4-hydroxy phenyl 3, 4, 5, 6, 7, 8-hexahydro quinazolin-2-thione moiety using chloroacetic acid as building blocks. The procedure needs the formation of the thiazolo quinazoline derivatives by substituted benzaldehyde and p-nitro aniline.
The stem bark of Acacia nilotica is used as a powerful astringent and the decoction is used as gargle for throat troubles and stomatitis.q3 Bark contains several polyphenols such as catechin,epicatechin, dicatechin, quercetin and tannin. Gallic acid has been reported to have antidiabetic,antithrombotic, anti inflammatory and anticarcinogenic activities. A simple, precise and accuratehigh-performance thin layer chromatographic method has been established for the determination of Gallic acid in the bark powder of Acacia nilotica Linn. The acetone extract of the bark powder wasused for the experimental work. Separation was performed on Silica gel 60 F254 HPTLC plates with Toluene: Ethyl acetate: Formic acid (6:4:0.8 v/v), as mobile phase. The plate was scanned in the densitometric absorbance mode at 280 nm. Gallic acid response was linear over the range 2-7 μg ml-1. The HPTLC method was validated in terms of sensitivity, accuracy, precision and reproducibility. The concentration of gallic acid in the bark powder was found to be 0.86%.
Acne is a cutaneous pleomorphic disorder of the pilosebaceous unit involving abnormalities in sebum production and is characterized by both inflammatory (papules, pustules and nodules) and noninflammatory (comedones, open and closed) lesions. Propionibacterium acnes and Staphylococcus epidermidis are common pus-forming microbes responsible for the development of various forms of acne vulgaris. Common therapies that are used for the treatment of acne include topical, systemic,hormonal, herbal and combination therapy. Topically used agents are benzoyl peroxide, antibiotics and retinoids. Systemically used agents are antibiotics and isotretinoin. These drugs produce a number of potential side effects and development of resistance to frequently used antibiotics. Novel Drug delivery system plays a crucial role in curing ACNE. Having Optimum concentration of drug molecules and direct citation of drug to the site of action helps in curing ACNE with out side effects and there by the efficacy of the drug is increased by involvement of the Nano Particles. This review focuses on the treatment of ACNE VULGARIS using NOVEL DRUG DELIVERY SYSTEM.
In the present work, floating gastroretentive formulation of Ranitidine HCl was formulated to sustained release of Ranitidine HCl above its site of absorption. To modulate the release characteristics,HPMC (K4M) and natural swelling agent Psyllum husk are used for single-unit floating matrix tablets by a direct compression technique. The floating approach was achieved by the use of Sodium bicarbonate.The prepared floating tablets were evaluated for their floating behavior, swelling studies, in-vitro drug release studies and kinetic analysis of the release data. The optimize formulation shows floating lag time within 3 min. The effect of HPMC (K4M) and swelling agent Psyllum husk on drug release was observed.Ranitidine HCl shows drug release till 12 hrs due to gel forming property of HPMC (K4M) and swelling capacity of Psyllum husk. Form the results, it can be conclude that the prepared gastroretentive tablet of Ranitidine HCl shows desirable release profile, good floating and sustained effect in stomach. The Fourier Transform Infra Red Spectroscopy studies revealed that there is no molecular interaction which may have implications on drug release haracteristics.
A new series of dyes were synthesized from anthranilic acid derivatives by reacting p-aminobenzoic acid to HCl salt of ammonium benzoyl chloride. Then condensation of HCl salt of ammonium benzoylchloride with anthranilic acid and its derivatives at various conditions like temperature, condition of reactants and solvents were maintained for the preparation of dyes. All the dyes were screened forantibacterial activity against S.aureus and E.coli. These dyes were also shows significant anti-inflammatory activity. The structures of new synthesized dyes were established on the basis of elemental analysis, UV, IR and NMR.
N1,N3-bis(2-oxoindolin-3-ylidene)malonohydrazides (VIa-i) have been synthesized by the condensation of malonohydrazide (V) with corresponding isatin derivatives (III) in alcohol. The intermediate malonohydrazide (V) was prepared by the reaction of diethylamalonate (IV) with hydrazine hydrate. All the title compounds (VI) were screened for Acute toxicity, analgesic, anti-inflammatory and ulcerogenic activity. Ibuprofen and indomethacin were employed asstandard. The structures of newly synthesized compounds were established on the basis of elemental analysis, IR, 1H NMR and mass spectral data.
The hepatoprotective activity of methanolic extract of Solena amplexicaulis (SAME) (Lam.)Gandhi (Cucurbitaceae) at doses of 250 mg/kg and 500 mg/kg were evaluated by carbon tetrachloride(CCl4) intoxication in rats. The toxic group which received CCl4 (0.3 ml/kg of CCl4 dissolved in 1:1 ratio in olive oil by subcutaneous (s.c) alone exhibited significant increase in serum alanine aminotransferase(ALT), aspartate amino transferase (AST), alkaline phosphatase (ALP) and total bilirubin (TB) levels. It also caused significant (P<0.001) decrease in protein levels. The groups receivedpretreatment of SAME at a dose of 500 mg/kg b.w.p.o. had controlled the AST, ALT, ALP and total bilirubin levels and the effects were comparable with standard drug (silymarin 100 mg/kg b.w.p.o).The total protein (TP) and albumin (ALB) levels were significantly increased in the animals received pretreatment of the extract at the higher dose level. The animals received pretreatment of the extractshown decreased necrotic zones and hepatocellular degeneration when compared to the liver exposed to CCl4 intoxication alone. Thus the histopathalogical studies also supported the protective effect ofthe extract.
The Montelukast is a leukotrine receptor antagonist (LTRA) used for the maintenance treatment of asthma, chronic asthma attacks and to relieve symptoms of seasonal allergies. Montelukast biological half life is 2.5 to 5.5 hrs there by decreasing bioavailability upto 64%. So, in order to improve the bioavailability and efficacy, we have prepared buccal films of montelukast. In the present research work, buccal films were prepared using mucoadhesive polymers like HPMC (K4M), HPMC (50cps), HPMC (5 cps), Eudragit RL-100 and PVP K-30 by Solvent Casting technique. Buccal films were characterized for number of parameters like physical appearance and surface texture, weight uniformity, thickness, folding endurance, swelling index, surface pH, drug content uniformity, in vitro residence time, bursting strength, drug–excipients interaction study, and in vitro drug release study. All the prepared films were smooth surface and elegant texture. All the prepared films are weighing in between 26.33 to 37.66 mg. The thickness of the films was in the range of 0.246 to 0.373 mm. Folding endurance was in the range of 259 to 289. Swelling index in the range of 29.81 to 43.48 %. Surface pH was in the range of 6.00 to 6.83 pH. Drug content uniformity study showed uniform dispersion of the drug throughout the formulation in the range of 94.33 to 98.33 %. The in vitro residence time for all the films is in between 3.13 to 5.50 hrs. The bursting strength of films is in the range of 6.533 to 4.366 Kg/cm2. FT-IR studies revealed that,there was no incompatibility of the drug with the excipients used. In vitro drug release studies in the range of 67.35 to 93.62 at the end of 8th hrs.
Floating microcarriers were prepared from a sodium alginate solution containing CaCO3 and NaHCO3 as gas-forming agents. The solution was dropped to 5% CaCl2 solution containing 10% acetic acid for CO2 gas and gel formation. The effects of gas-forming agents on microcarrier size and floating ability were investigated. As concentration of gas-forming agents increased, the size and floating ability also increased. Microcarrier’s surface and cross-sectional morphology were examined with Scanning Electron Microscopy. NaHCO3 significantly increased porosity and pore diameter than CaCO3. Incorporation of CaCO3 into alginate solution resulted in smoother microcarriers than those produced with NaHCO3 as well as it showed high drug entrapment. Microcarriers incorporating CaCO3 exhibited significantly increased gel strength over control and NaHCO3-containing samples. Releasecharacteristics of Metformin hydrochloride as a model drug was studied in -vitro. Release rate of Metformin hydrochloride increased proportionally with addition of NaHCO3. However, increasingweight ratios of CaCO3 did not appreciably accelerate drug release. The results of these studies indicate that CaCO3 is superior to NaHCO3 as an effervescent agent in alginate microcarrier’s preparations. The enhanced buoyancy and sustained release properties of CaCO3-containing beads make them an excellent candidate for floating drug dosage systems (FDDS).
A series of novel 6,7,8,9 tetra hydro-5H-5-(2'-hydroxy phenyl)-2-(4'-some substituted benzylidine)-3-(4-nitrophenyl amino) thiazolo quinazoline were synthesized the reaction with appropriate aromatic aldehydes and p –nitro aniline in the presence of anhydrous sodium acetate The starting material 6,7,8,9 tetra hydro-5H-5-(2'-hydroxy phenyl) thiazolo (2, 3-b) quinazolin-3(2H)-one 3 by a new innovative route with improved yield. When tested for their in vivo H-antihistaminic activity on conscious guinea pigs, all the test compounds significantly protected the animals from histamine induced bronchospasm. The compound 5b emerged as the most active compound of the series and it is more potent (73.93% protection) when compared to the reference standard,chlorpheniramine maleate (71% protection), it showed negligible sedation (10%) when compared to chlorpheniramine maleate (30%). Therefore compound 5b will serve as prototype molecule for further development as a new class of H1-antihistamines.
The objective of the study is to isolate alkaloids having similar activity to that of strychnine and brucine from Strychnos nuxvomica and to evaluate them. Methanolic extract from the roots of S. nuxvomica after chromatography afforded stigmasterol, b-amyrin and an alkaloid 4-hydroxy-3-methoxy strychnine.The alkaloid exhibited potent central nervous system stimulant activity at lower doses (0.2 mg kg-1, i.p) but displayed depressant, convulsant and toxic effects at higher doses (1 mg kg-1, i.p). This activity is much similar to that of strychnine and indicate that the S. nuxvomica possess several such alkaloids which may be responsible for toxic activity of the drug synergistically.
Aims: To compare the possible therapeutic effects of C. igneus methanolic and aqueous extractsagainst hyperglycemic and hyperlipidemic activity in alloxan induced diabetic rats.Materials and Methods: Blood glucose level, serum lipid profile and pancreas histology as well as phytochemical investigations were estimated after administration of the both extracts at dose level of50, 100 and 200 mg/kg were comparable to that of glibenclamide (0.5mg/kg).Result: All studies in aqueous and methanolic extracts of Costus igneus have shown better effect on end of 30th day. The significantly reduce type 2 diabetes in rats and regulation of insulin secretion,islet protection as well as produce higher antidiabetic compounds by methanolic extract at dose level of 200 mg/kg.Conclusion: Our results suggest that the Costus igneus methanolic extract anti-diabetic activity is slightly higher to the aqueous extract and good agreement with the folk medicinal use of this plant.
Different doses of ethanolic fraction of stem bark of neolarckia cadamba were evaluated for hypoglycemic activity in normal and alloxan diabetic rats. The oral administration of ethanolic extractof 0.5g/kg body weight exhibited a significant antihyperglycemic activity in alloxan diabetic rats,whereas in normal rats no hypoglycemic activity was observed.
Simple first order derivative spectrophotometric method has been developed for simultaneousestimation of valsartan, amlodipine besylate and hydrochlorothiazide in combined dosage form. Themethod employed was multi-wavelength method for analysis using methanol: water (70:30) as a solvent.The three wavelengths 245, 265 and 279 nm were selected for estimation of valsartan, amlodipine besylate and hydrochlorothiazide respectively. Linearity was observed in the concentration range of 8-80 μg/ml, 1-10 μg/ml and 2-20 μg/ml for valsartan, amlodipine besylate and hydrochlorothiazide respectively. The recovery studies ascertained the accuracy of the proposed method and the results were validated as per ICH guidelines. The method can be employed for estimation of pharmaceutical formulations with no interference from any other excipients and diluents.
Eupatorium odoratum Linn is found all over tropical Asia, western Africa and in parts of Australia. It is also found in Koraput district and extensively used traditionally by the tribal people as anti-inflammatory,analgesic, antiprotozoal agent’s e.t.c. Extraction of the leaves of the plant Eupatorium Odoratum using different solvents like petroleum ether, chloroform, ethanol and their analgesic activity studies has been envisage in this present research work. All the different extracts such as petroleum ether extract, chloroform extract and ethanolic extract has been subjected to analgesic activity studies. It has been found that onlyethanolic extract (P<0.01) shows maximum analgesic activity at a dose of 300 mg/kg whereas petroleum ether extract and chloroform extract shows moderate activity at the same dose when compared with thestandard drug aspirin.
Present study involves the homology modeling of human tubulin β-1 chain(TUBB1) using known protein structure of common pig tubulin. Its 3-D structure was evaluated and validated using PROCHECK comprising 96.8% amino acid residues in favored and allowed region of Ramachandran plot. Stability of the structure was confirmed by the program ERRAT having the overall quality factor as 83.476 and Verify_3D result with 83.85% residues having 3D-1D score > 0.2. With the structure of TUBB1 generated, flexible docking was performed using GLIDE. Results indicate that among 123 colchicine analogues, CID 5370577 was found as best interacting with TUBB1 having lowest dope score of -6.45. Particularly residues TYR208, SER172 and GLU181 of TUBB1 at bond length 2.272, 1.997 and 2.249 respectively formhydrogen bonds and showed strong nonbonding interaction with analogue (CID 5370577). Further the generation of different derivatives can be made by the modification in the moieties of CID 5370577. Thesederivatives can be used to develop effective drugs against acute gouty arthritis as well as cancer.
Aims and Objective: To study the benzene, alcohol and petroleum ether extract of Senna uniflora treatment against carrageenan induced paw oedema in albino rat model.Methods: The benzene, alcohol and petroleum ether extracts of Senna uniflora was given to paw oedema induced albino rats at doses administered intraperitoneally (I.P.) ranged from 50 to 200mg/kg body weight, which comparable with indomethacin (10 mg/kg) used as a reference drug.Results: The benzene and alcohol extracts administrated orally at dose of 200 mg/kg produced significant (P < 0.05) oedema inhibition when compared with indomethacin.Conclusion: The result suggested that benzene and alcohol extracts of Senna uniflora, showed significant inhibition on paw oedema albino rats. This study reveals the possible rationale for itsfolkloric use as an anti-inflammatory agent.
The p38 protein kinase is a serine-threonine mitogen activated protein kinase, which plays an important role in inflammation and arthritis. p38 subgroup of the mitogen activated protein kinasesuper family has four isoforms: p38α, p38β, p38δ, p38γ. p38α is involved in inflammation,proliferation, differentiation and apoptosis. The biological functions of p38β, p38δ, p38γ are notunderstood completely. Many p38α inhibitors with diverse chemical structures and modes of protein interaction have been designed on the basis of their ability to compete with ATPsite or Allostericsitefor binding to p38α. In the late 1970’s and early 1980’s the initial p38 chemo type, triaryl imidazole was discovered. During the last ten years a number of novel p38 chemotypes were discovered viahigh through put screening. Among several novel p38 chemotypes developed, pyrazolyl ureas and its derivatives were identified as potent and selective p38 kinase inhibitors.
A Gastroretentive floating controlled drug delivery system containing Silymarin was prepared in the form of tablets and evaluated for its processing parameters, in vitro release in 0.1 N HCl. Eightformulations were prepared by using rate controlling polymers such as HPMC K4M and Eudragit RS100, alkalizing agent sodium bicarbonate and solubilizing agent poly vinyl Pyrrolidone (PVP K30.Floating tablets were prepared by direct compression method. The preformulation studies and tablet evaluation tests were performed and results were within the limits. Tablets remained buoyant over 20 hours in the release medium and the amount of sodium bicarbonate found to be significant for not only to remaining buoyant without causing disintegration of the tablet. The different ratios of polymers 15%and 20% showed the significant difference in the drug release with increasing in the concentration of solubilizing agent PVP K30. All the formulations exhibited diffusion dominant drug release. Stabilitystudies for all formulations were conducted for a period of 60 days at 4º±2ºC, 27º±2ºC and 45º±2ºC respectively and the formulations showed no significant changes in physical appearance, drug contentand in-vitro drug release even after 60 days. The control release of the drug from the dosage form shows the hepatoprotective activity against Isoniazid (INH) + Rifampcin (RIF) induced hepatotoxicity in rats.
Aim: To screen the various extract of leaves of Stereospermum colais for antibacterial and antifungal activity against few clinically important pathogenic bacteria and fungi.Methods: The various successive solvent extracts viz., n-hexane, chloroform, ethylacetate, ethanol and water were screened for its antimicrobial activity. The test organisms used for antibacterial study includes fresh clinical strains isolated from pathologic specimens viz., gram (+ve) Coagulase negative Staphylococcus, Entero cocci, Staphylo coccus aureus, and gram (-ve) Acinetobacter, Citrobacter,Escherichia coli, Klebsiella pneumoniae, Pseudomonas aureginosa, Salmonella typhi and Salmonella paratyphi. The antibacterial activity was assessed by Minimum Inhibitory Concentration (MIC) and agar disc diffusion method. The antifungal activity was assessed by MIC. For antifungal activity, the fungistudied were Aspergillus flavus, Aspergillus fumigatus, Aspergillus niger and Candida albicans.Results: Comparison of antibacterial activity was done with standard antibiotic ciprofloxacin (5μg/disc). The ethanol and chloroform extract showed maximum antibacterial activity followed by ethyl acetate,aqueous and n-hexane. The ethanol extract showed inhibitory effect against all fungi except Aspergillus flavus. Chloroform extract showed activity against Candida albicans. The other extracts showed significant inhibition on the growth of fungi.Conclusion: The various extracts of Stereospermum colais leaves have potential antibacterial and antifungal activity and can be used as new source for antibacterial and antifungal drugs.
Aim of study: To evaluate the root extract of Pseudarthria viscida Linn, for antidiarrhoeal activityusing standard model.Material and methods: The roots of Pseudarthria viscida Linn were collected from Kolli Hills,dried and extracted with ethanol (95%). Wistar albino rats were used for studies. Castor oil was usedto induce diarrhoea and 200, 400 mg/kg of ethanol extract of Pseudarthria viscida (EEPV) was used to test antidiarrhoeal activity. Results were calculated by student “t” test, to assess statisticalsignificance.Results and Discussion: The extract showed dose dependant inhibition of frequency of defecation aswell as reduction in number of wet feces. The percentage inhibitions of faecal with 200 and 400mg/kg doses of ethanol extract were 48.14 and 62.96 respectively. The plant roots extract contains tannins and flavonoids, which could have contribution to the antidiarrhoeal activity.Conclusion: Ethanol extract of Pseudarthria viscida (EEPV) Linn possesses significant antidiarrhoeal activity.
Xylella fastidiosa is a pathogenic bacterium that infects plants, causing a variety of diseases in over 100 plant species. Peptide fragments of antigen protein can be used to select nonamers for use in rational vaccine design and to increase the understanding of roles of the immune system in pathogenic diseases. Analysis shows MHC class II binding peptides of antigen protein from Xylella fastidiosa are important determinant for protection of host form infection. In this assay, we used PSSM and SVM algorithms for antigen design and predicted the binding affinity of antigen protein having 790 amino acids, which shows 782 nonamers.Binding ability prediction of antigen peptides to major histocompatibility complex (MHC) class I & IImolecules is important in vaccine development from Xylella fastidiosa.
Aim: To study the antimicrobial activity of aqueous, methanolic and petroleum ether extracts of leavesof Rumex vesicarius Linn.Materials and Methods: The antibacterial activity was studied by agar cup plate method using nutrient agar media. The results were compared with standard Streptomycin (100μg/ml). The antifungal activityof the extracts was investigated by agar cup plate method using Sabouraud Dextrose Agar medium and the results were compared with reference Fluconazole (100μg /ml).Result: All studied aqueous, methanolic and petroleum ether extracts have shown antimicrobial studies.The results of zone of inhibition study revealed concentration dependent nature of the extract with broad-spectrum activity against bacteria and fungi.Conclusion: The present study enlightens the potential usefulness of Rumex vesicarius in the treatment of pathogenic diseases.
The purpose of this study was to investigate the possible antioxidant effect of metformin in high fructose fed diet-induced diabetic rats. The increased level of lipidperoxidation and altered levels ofenzymatic and non enzymatic antioxidants were seen in high fructose fed consumed animals. The administration of metformin significantly normalized the altered levels of lipid peroxidation and antioxidantstatus. In conclusion, this study indicates that the administration of metformin improves antioxidant status by reducing lipidperoxidation and enhancing the antioxidant enzymes activities in liver of diabetic rats.
Oral administration of different dosage forms is the most commonly used method due to greater flexibility in design of dosage form and high patient acceptance, but the gastrointestinal tract presentsseveral formidable barriers to drug delivery. In oral colon-specific drug delivery system, colon has a large amount of lymphoma tissue (facilitates direct absorption in to the blood), negligible brushboarder membrane activity, and much less pancreatic enzymatic activity as compared with the small intestine. Colon-specific drug delivery has gained increased importance not just for the delivery of the drugs for treatment of local diseases associated with the colon but also for its potential for the delivery of proteins and therapeutic peptides. Different approaches are designed based on prodrug formulation,pH-sensitivity, time-dependency (lag time), microbial degradation and osmotic pressure etc to formulate the different dosage forms like tablets, capsules, multiparticulates, microspheres, liposomes for colon targeting. The efficiency of drug delivery system is evaluated using different in vitro and invivo release studies. This review updated the research on different approaches for formulation and evaluation of colon-specific drug delivery systems (CDDS).
The bioavailability of conventional ophthalmic solutions is very poor due to efficient protective mechanisms of the eye, blinking, reflex lachrymation and drainage which remove rapidly various foreign substances including drug from the surface of the eye. Frequent instillation of drug solution is necessary to maintain a therapeutic drug level in the tear or at the site of action but the frequent use of highly concentrated solution may induce toxic side effects due to systemic absorption of drug through nasolachrymal drainage. In recent years there has been significant efforts directed towards the development of new systems for ophthalmic drug delivery. Thisreview focuses on recent literature regarding mucoadhesive systems, vesicular systems, semisolid hydrogel and in situ gelling system. Moreover, attempt has been made to explore the applicabilityof numerous polymers for ocular drug delivery system and also includes a detailed account on various recent strategies that are developed and under development stage so far.
Aim: To evaluate nephroprotective and nephrocurative activity of rhizome of Picrorhiza kurroa.Materials and Methods: The ethanolic extract of rhizome of P. kurroa was studied for nephroprotective and nephrocurative effect in female Wistar rats against Cisplatin (5mg/kg b.w.i.p.) induced nephrotoxicity,by estimating serum creatinine and blood urea levels. One of the Ayurvedic formulations viz.Arogyawardhini, containing P. kurroa as a major ingredient was also studied for the nephroprotective and nephrocurative effects against Cisplatin induced nephrotoxicity. The formulation was standardized for thepresence of total polyphenols.Results: Treatments with the ethanolic extract of the rhizome in the dose of 600 mg/kg b.w.p.o.could significantly (P< 0.001) reduce the elevated serum levels of creatinine and blood urea.Conclusion: The formulation was found to have better activity as compared to the rhizome.
Rheumatoid arthritis (RA) is a chronic systemic inflammatory disease of unknown etiology affecting both articular tissues and extraarticular organs. The disease is often progressive and results in pain, stiffness, and swelling of joints culminating in significant morbidity and increased mortality. This chapter discusses the epidemiology, possible etiology, clinical manifestations,diagnostic approach and treatment options of RA.
Asparagus racemosus Wild, F: Aspargaceae is an ayurvedic plant with medical importance of tropical and subtropical India. Its medical usage has been reported in Indian & British Pharmacopeias and in traditional system of medicine such as Ayurveda, Unani & Siddha.Asparagus racemosus is mainly known for its phytoestrogenic properties with an increasing awareness about the harmful effects with synthetic oestrogens, the interest in plant derived oestrogens has increased tremendously making Asparagus racemosus particularly important. Its beneficial uses in correcting menstrual irregularities are mentioned in ancient literature, till date they are prescribed by ayurvedic physicians to correct menstrual irregularities with productsavailable in the markets. Asparagus racemosus has been shown to have many other properties like Antistress, Anti-diarrhoeal,Antidyspepsia, Adaptogenic action, Antiulcerogenic action, Antioxidant & Cardio protection. This article aims to evaluate the biological activities,pharmacological applications & Clinical studies of Asparagus racemosus to provide direction for further phytoestrogenic properties and unexplored areas in which Asparagus can be proved to havepotential to cure diseases like osteoporosis.
Type2 Diabetes is highly prevalent in India. Several studies on Asian Indians have shown that they are characterized by higher insulin resistance, early onset type2 diabetes and hypertension. For a given BMI Indians have a higher percentage of body fat and more visceral fat than members of other population. The tendency of Indians to have higher percentage of body fat and central adiposity compared with other races may be programmed in utero. This thin fat phenotype is present at birth. Small size at birth coupled with subsequent obesity increases risk for insulin resistance syndrome in later life.Dietary modifications play an important role in initiation of insulin resistance syndrome. This may also lead to Type2 diabetes in Indianpopulation.The oil preferred for cooking India is considerably changes the ratio of W6/W3 fatty acids. A number of free fatty acids are PPARg activators. When individual with thrifty genotype are supplied energy rich food with reduction in physical activity there will be a greater prevalence of obesity, impaired glucosetolerance and type2 diabetes. PPARg activation enhances adipocyte differentiation make the people more obese. PPARg coordinates the thrifty response and urges the need for studying PPARg in Indians. Because this could explain the heterogeneity of insulin resistance and type2 diabetes in Indians. Aim of this study is to find out PPARg polymorphisms and their association with type2 diabetes in south Indian population.With the help of PCR and Sequencing the exonic regions were screened for PPARg polymorphisms.Statistically their association with type2 diabetes was studied.
An UV spectrophotometric method using simultaneous equation was developed for the simultaneous determination of Telmisartan and Atorvastatin calcium in a binary mixture. In the proposed method, the signals were measured at 296.0 nm and 247.0 nm corresponding toabsorbance maxima of Telmisartan and Atorvastatin Calcium in methanol respectively. Linearity range was observed in the concentration range of 5-30 μg/ml for both the drugs. Concentration of each drug was obtained by using the absorptivity values calculated for both drugs at two wavelengths, 296.0 nm and 247.0 nm and solving the simultaneous equation. Developed method was applied to laboratory mixture and its pharmaceutical formulation. The method was validatedstatistically and recovery study was performed to confirm the accuracy of the method. The method was found to be rapid, simple, accurate and precise.
The purpose of this research work was to establish mucoadhesive buccal tablets of Baclofen in the forms of monolayered tablets. The tablets were prepared using Sodium methyl cellulose (NaMC ),sodium alginate and Methocel K15M as bioadhesive polymers to impart mucoadhesion. Buccal tablets were evaluated by different parameters such as weight uniformity, content uniformity, thickness,hardness, surface pH, Swelling index, ex vivo mucoadhesive strength, in vitro drug release, and in vitro drug permeation. The present study concludes that mucoadhesive buccal tablets of Baclofen canimprove the bio availability of Baclofen.
The present study is an attempt to understand the role of some highlighted vegetables like Tomato,Carrot, Onion, Cabbage, Soy bean, and Chick pea with Vitamin D3 when given together in vivo aschemopreventive agent against experimentally DAL (Dalton's ascites lymphoma cell line) induced mice carcinogenesis.The anticarcinogenic potential of this micro-nutrient rich food has been assessed by their ability to modulate certain life style in the early stages of DAL induced liver carcinogenesis in mice. Survival study of all experimental mice has a 62.5% which fed by above vegetables to cancer induced mice whereas the group fed without vegetables are showed 28.5% survival during 30 days of study period. The preliminary enzyme like SGPT and SGOT level change also observed in those mice.
The basic aim of present work was to extract the mucilage from Randia dumetorum fruit by using suitable method and to check its suitability for tablet binder. The mucilage was extracted from fruit powder bymaceration technique using water and then precipitated with alcohol in 1:2 proportion (yield 8-9 % w/w).The physicochemical properties of mucilage like moisture content, solubility, density, viscosity, pH,surface tension, swelling index, water absorption capacity and microbial load were determined. The granules were prepared by Wet Granulation technique using Paracetamol as Model drug and mucilage asbinder in concentrations 1-5 % w/w. Then tablets were punched by keeping pressure constant. The granules and tablets were evaluated as per official procedures. In vitro dissolution profiles of tablets werecarried out in Phosphate Buffer pH 5.8. All parameters were compared with standards like acacia (1-5% w/w) and starch (6, 8, 10%w/w). The evaluation data suggested that tablets prepared with Randiadumetorum fruit mucilage as binder showed good results and comparable dissolution profile as that of standards. Also the results were complied with pharmacopoeial limits. Hence, the mucilage from Randiadumetorum fruit can act as suitable binder for conventional tablets instead of synthetic polymers.
Chitosan is a weak cationic polysaccharide composed essentially of β(1→4) linked glucose amine units together with some acetyl glucose amine units. It is obtained by extensive deacetylation of chitin,a polysaccharide common in nature. Chitosan is biocompatible, biodegradable, and non toxic natural polymer that exhibits excellent film forming ability. As a result of its cationic character, chitosan is able to react with polyanions giving rise to polyelectrolyte complexes. Therefore, because of these interesting properties, it has become the subject of numerous scientific reports and patents on thepreparation of micro spheres and microcapsules. The techniques employed to microencapsulate with chitoson include, among others, ionotropic gelation, spray drying, emulsion phase separation, simpleand complex coacervation, and polymerization of vinyl monomer in the presence of chitosan. The aim of the work is to review some of the more common techniques used and to put forward the results obtained in preparing chitosan-based microcapsules: for taste masking and improving the stability of nutritional oil, the sustained release of drugs, as well as the preparation of chitosan super paramagneticmicrocapsules for immobilization of enzymes.
A reverse phase isocratic high performance liquid chromatographic method was developed for the estimation of bosentan drug in tablet formulation. The separation was achieved by C-18 hypersil250*4.6mm, 5μm and methanol: potassium dihydrogen orthophosphate buffer pH 7.8 (60:40 v/v) as mobile phase, at a flow rate of 0.8 ml/min. Detection was carried out at 220 nm. Retention time of Bosentan was found to be 8.26 +or-1. The method has been validated for linearity, accuracy and precision. Linearity of bosenatan was in the range 50-150 mcg/ml. The mean recovery obtained for was 99.1. Developed method was found to be accurate, precise, selective and rapid for estimation of bosentan in tablets.
Two simple and sensitive visible Spectrophotometric methods [I and II] have been developed for the quantitative estimation of Sparfloxacin in bulk and Pharmaceutical dosage forms. Method-Iis based on ion-pair complex formation between Sparfloxacin and Bromocresol purple, which shows yellow color and gives maximum absorption at 410.0 nm and obeys Beer’s law in the concentration range of 5-25 μg/ml. Method-II is based on ion-pair complex formation between Sparfloxacin and Bromocresol green, which shows yellow color and gives maximum absorption at 420.0 nm and obeys Beer’s law in the concentration range of 5-25 μg/ml.
A simple and sensitive spectrophotometric method has been developed for simultaneous determination of Paracetamol and Lornoxicam in a binary mixture. In the proposed method, the absorbances were measured at 257.0 nm and 287.0 nm corresponding to the absorbance maxima ofParacetamol and Lornoxicam in 0.1 N Sodium Hydroxide respectively. Linearity range was observed in the concentration range of 5-30 μg/ml for Paracetamol and 2-10 μg/ml for Lornoxicam. Concentration of each drug was obtained by using the absorptivity values calculated for both drugs at two wavelengths, 257.0 nm and 287.0 nm and solving the simultaneous equation. Developed method was applied to laboratory mixture and its marketed formulation. The method was validated statistically and recovery study was performed to confirm the accuracy of the method. The method was found to be rapid, simple, accurate and precise.
A rapid and sensitive reverse phase HPLC method is depicted for the qualitative and quantitative assay of Bupropion hydrochloride in pharmaceutical dosage form. Bupropion hydrochloride waschromatographed on a reverse phase C18 column with a mobile phase consisting of methanol:phosphate buffer (pH-6) in the ratio of 80:20% v/v.The mobile phase was pumped at a flow rate of 1ml/min. Aceclofenac was used as an internal standard and the eluents were monitored at 223 nm. The retention time of the drug was 5.7 min.With this method, linearity is observed between area under curve (AUC, expressed in mV.min) and concentration of Bupropion hydrochloride in the injected solution, in the range of 10-200 μg/ml.The method was found to be applicable for analysis of drug in tablets. The results of the analysis were validated statistically.
A term combining the words “nutrition” and “pharmaceutical,” is a food or food product that provides health and medical benefits, including the prevention and treatment of diseases. They have shownactivities like antioxidant, effect on cholesterol, anti-hormone activity and in treatment of cancer.Different species like tramates versicolor, a cancer drug called polysaccharide-k, which counter-act the immune system depressing action of common chemotherapeutic drug. Grifola frondosa has anti-cancer activity. Agaricus subrufescens shows similar effect. Agaricus bisporus shows inhibition of breastcancer development. Similarly other species like Lentinula edodes, Hericum erinaceus Flammulina velutipes shows effect.
An attempt has been made for the development of fast dissolving tablets of the carbamazepine by solid dispersion methods, using different concentrations of croscarmellose sodium as superdisintegrating agent. The major problem of this drug is very low solubility in biological fluids and poor bioavailability after oral administration. The tablets prepared were evaluated for hardness, friability,drug content, disintegrating time, wetting time and in-vitro dissolution studies. The formulations prepared with mannitol solid dispersion were showed disintegration time between the ranges of 12.83 –16.79 sec and Drug release showed between the ranges of 08 – 10 min. However the formulations prepared with PEG-6000 solid dispersion did not disintegrate in specified limit of time for fastdissolving tablet. Among all formulations SM4 showed 99.50 % drug release within 8 minutes. The prepared tablets were characterized by DSC and FTIR Studies. No chemical interaction between drug and excipient was confirmed by DSC and FTIR studies. The stability study conducted as per the ICH guidelines and the formulations were found to be stable. The results concluded that fast dissolving tablets of poorly soluble drug, carbamazepine showing enhanced dissolution, improved bioavailability,effective therapy and hence better patient compliance.
The present study was designed to evaluate the expression of estrogen and progesterone receptor as biomarkers in human benign and malignant mammary tumors. Tissue samples from tumors and adjacent uninvolved areas from fifteen breast cancer patients were analyzed. The expression of estrogen and progesterone receptors on frozen sections Her-2/neu receptor progression in breast cancer was determined immunohisto chemical. Incidence of receptor expression were significantly more among the cases with grade II malignancy (53.3 percent) than compared with grade I (6.6 percent) and grade III (40 percent) malignancy. Estrogens promote the development of mammary cancer and exert both direct and indirect proliferating effects.
A simple, fast, precise and accurate, high performance liquid chromatographic method for estimation of Cefixime in Cefixime Oral Suspension was validated using C18 [Hypersil ODS],4.6x250mm, 5 microns with mobile phase composition of Tetrabutylammonium hydroxide solution:Acetonitrile (760:240), flow rate of 2.0 ml/min and UV detection at 254 nm. Tetrabutylammonium hydroxide solution was prepared by diluting 25ml of 0.4M Tetrabutylammonium hydroxide solution with water to obtain 1000ml of solution, and pH was adjusted to 6.5 with 1.5M Phosphoric acid. The linearity of the method was observed over concentration range of 140- 260 mcg/ml. The accuracy ofthe proposed method was determined by recovery studies and found to be 99.17-101.00%. The proposed method is precise, accurate selective, reproducible and rapid for the determination cefixime in cefixime oral suspension.
Dissolution rate and dissolution efficiency of poorly soluble non-steroidal anti inflammatory drugs(NSAIDs) could be markedly enhanced by solid dispersion technology. Solid dispersions ofcelecoxib (C) are subjected to in vivo pharmacokinetic evaluation to evaluate whether these systems improve oral bio availability of the celecoxib. All the pharmacokinetic parameters of absorption,namely Ka, Cmax, Tmax, percent absorbed to various times and AUC indicated rapid absorption and higher bioavailability of celecoxib when administered as its solid dispersions. The absorption rateconstant (Ka) was found to be 3.5526hr-1 in the case of celecoxib-Croscarmellose-Poly venyl pyrrolidine (C-CC-PVP) solid dispersion. Where as in the case of celecoxib Ka was only 0.412 hr-1.An increase of 8.6 fold in Ka was observed with celecoxib-CC-PVP solid dispersion. AUC (extent of absorption) was also much higher in the case of celecoxib -CC-PVP solid dispersion when compared to celecoxib. [AUC]0-12h was increased from 91.54 ng-hr/ml for celecoxib to 587.13 nghr/ml for celecoxib-CC-PVP solid dispersion . Both Ka and AUC were markedly increased by CCPVP solid dispersion . Thus, the results of pharmacokinetic studies indicated rapid and higher oralabsorption of celecoxib when administered as CC-PVP solid dispersion.
The development and validation of an Ion chromatographic method for estimation of methane sulphonic acid in gemifloxacin mesylate drug substance was performed using acetone and buffer (1:9)as mobile phase and metrosep anion dual 2 as stationary phase at 0.5ml/min as flow rate. The analytes were monitored using suppressed conductivity detectors and linearity was obtained at the concentration range of 35.02 to 65.48 μg/ml and the correlation coefficient was found to be 0.9989.The recovery was found to be in the range of 103.53 to 116.30%w/w.
A validated, specific, stability indicating reversed-phase liquid chromatographic method has been developed for quantitative analysis of citicoline and its related substances in oral drops formulation. Forced degradation studies were performed using acidic, basic and oxidizing conditions, and thermal and photolytic stress, to show the stability indicating power of the method. The method was optimized by analysis of the samples generated during the forced degradation studies and sample solutions spiked with the impurities.Good resolution between the analyte peak and peaks corresponding to process related impurities and degradation products was achieved on a Whatman Partisil SAX C18 (250X4.6mm, 10μm) column with amobile phase constituted of phosphate buffer and acetonitrile (40:60 % v/v) and further comprises of 1gm of 1-hexane sulphonic acid sodium salt. The pH of the mobile phase was adjusted to 3.4 with ortho phosphoric acid. Detection was performed at 280 nm. Citicoline sodium was subjected to stress conditions of hydrolysis (acid, base), oxidation, photolysis and thermal degradations. The method was validated in accordance with ICH guidelines and the validation data showed that the assay is sensitive, specific and reproducible for the determination of citicoline in the presence of related substances and degradation products.
Background: The Government of India, WHO and World Bank together reviewed the NTP in the year 1992. The revised strategy was introduced in the country as a Pilot Project since 1993 in a phasedmanner as Pilot Phase I, Pilot Phase II and Pilot Phase III. By the end of 1998, only 2 per cent of the total population of India was covered by RNTCP.Objectives:1. To know the sputum conversion rate among the sputum positive tuberculosis patients.2. To find the treatment outcome of smear positive tuberculosis patients.Methodology: This Hospital based descriptive study was carried out among the out patients attending Medicine, Surgery, OBG, ENT, Dermatology, TB and Chest Department of MNR Medical College during the period of January 1st to December 2006. Oral questionnaire prepared and applied to all the individuals (377 TB suspects) those who visited for sputum examination at DMC.Results: Out of 138 TB Cases 67.3% cases were pulmonary and 32.7% were extra pulmonary. Out of 58 sputum positive cases, 49 cases returned for sputum examination at successive months and rest were transfer out. Of these 49 cases, 46 cases have converted negative at 2, 4, 6 months respectively and remaining 3 cases had sputum conversion at 3,5, 7 months. Tuberculosis prevalence increased withage i.e. above 15 years of age group and significant association was found (P< 0.001). HIV- TB Co-Infection was found in 2 cases (1.4%) of the total TB (138) cases.Conclusions: Out of 58 sputum positive cases, 4 cases (4/58) not traced and 5 cases (5/58) transferred out to neibouring districts. There is a need to increase RNTCP network to minimize the dropouts.
Pharmacoepidemiology as a discipline goes beyond epidemiologic studies of drug-related topics.Some topics receiving much attention in Pharmacoepidemiology get little in traditional epidemiology,whereas others included in traditional epidemiology without question involve some controversy about whether they should be part of Pharmacoepidemiology. Much of this occurs because Pharmacoepidemiology is what may be called a bridge science bringing together pharmacology and pharmacy, clinical specialties, epidemiology, biostatistics, demography and social sciences.Epidemiology and clinical pharmacology are the two main bridgeheads. That a significant part of the early development of Pharmacoepidemiology was within a clinical pharmacology context wouldaccount for a somewhat different perspective from traditional epidemiology. The development of more and more potent but also increasingly expensive medicines will accentuate the need for skilledpractitioners of drug administration and drug safety, of which Pharmacoepidemiology is the basic science. Strategies in education have to be developed to meet such needs. One of the most challengingareas of research in Pharmacoepidemiology is to understand why individuals respond differently to drug therapy, both in terms of beneficial and adverse effects.
b-Cyclodextrin (b-CD) and HP-b-Cyclodextrin (HP-b-CD) inclusion complexes of meloxicam (M)exhibited higher dissolution rates and dissolution efficiency values than the corresponding uncomplexeddrug. The feasibility of formulating the b-cyclodextrin and HP-b-cyclodextrin complexes of meloxicam (1:3) into tablet dosage forms is evaluated. Solid inclusion complexes of meloxicam prepared by kneading method were formulated into tablets by wet granulation anddirect compression methods. All the tablets formulated employing b-cyclodextrin and HP-b-cyclodextrin complexes of meloxicam gave rapid and higher dissolution rates of when compared tothat of meloxicam plain tablets. All the prepared tablets fulfilled the official (I.P.) disintegration time specification of uncoated tablets. Overall, tablets prepared by direct compression methoddisintegrate rapidly when compared to those prepared by wet granulation method. Analysis of dissolution data as per zero-order and first – order kinetic models indicated that the dissolution ofmeloxicam from all the tablets followed first-order kinetics. In both direct compression and wet granulation methods, tablets formulated employing cyclodextrin complexes (MT2, MT3, MT5,MT6) gave higher rates of dissolution (K1) and dissolution efficiency (DE30) values when compared to the corresponding tablets formulated with meloxicam as such (MT1, MT4). Among all the meloxicam tablets formulated, formulation MT2, which is based on M- βCD (1:3) kneadedcomplex, gave highest dissolution. A 25.66 fold increase in the dissolution rate of meloxicam was observed with MT2 when compared to its plain tablets ( MT1).