Bollettino chimico farmaceutico (Boll Chim Farm )

Publisher: Societá editoriale farmaceutica

Description

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  • Other titles
    Bollettino chimico farmaceutico
  • ISSN
    0006-6648
  • OCLC
    4055131
  • Material type
    Periodical
  • Document type
    Journal / Magazine / Newspaper

Publications in this journal

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    ABSTRACT: Chitosan hydrogel beads containing diclofanac sodium were prepared using ionotropic gelation technique in which tripolyphosphate solution was used as a counterion. Chitosan molecular weight, tripolyphosphate concentration and crosslinking time were found to have an effect on the percentage of the drug loading. The loading efficiency of diclofenac sodium was very high (more than 90%). A longer-period of contact with the counterion ions decreased the efficiency of drug loading. The beads produced all had good spherical geometry. The beads showed a narrow size distribution in which 95% of the beads prepared were in the range of 2-3 mm. Comparison of release rate-time plots of dissolution data of marketed product with the newly developed dosage form indicated the ability of the later to sustain more diclofenac sodium release. The beads were evaluated for their bioavailability in six beagle dogs relative to the commercial enteric-coated Voltaren tablets. The in vivo availability study, reveled that the prepared beads filled in hard gelatin capsules had a 126.22% bioavailability relative to that of the commercial Voltaren tablets. The beads showed comparable pharmacokinetic parameters to that of the commercial tablets. The results suggested the possibility of producing a promising sustained drug delivery system for diclofenac sodium.
    Bollettino chimico farmaceutico 01/2005; 143(10):359-64.
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    ABSTRACT: A variety of 2-substituted-4, 6-diaryl-3-pyridinecarboxylates 4 were obtained through aromatic nucleophilic substitution. reaction of secondary amines with 2-bromo-3-pyridinecarboxylate derivatives 3. The latters were obtained through bromination of 3-aryl-4-benzoyl-2-cyanobutyrates 2 in glacial acetic acid. However; reaction of primary aromatic amines with 2-bromopyridines 3 afforded 2-arylamino-3-pyridinecarboxylates 5 beside the unexpected 2-amino analogues 6. On the other hand, 3-hydroxy-1H-pyrazolo[3,4-b]pyridines 7 were isolated via reaction of 3 with hydrazine hydrate. Good to complete muscle relaxation of rabbit's jejunium, rat's uterus and rabbits aorta was observed during screening representative examples (3a, 4c, Sd, 5f and 6b) of the newly synthesized 3-pyridinecarboxylates indicating the vasodilatation and antihypertension activity for the tested compounds.
    Bollettino chimico farmaceutico 01/2005; 143(10):365-75.
  • Bollettino chimico farmaceutico 01/2005;
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    ABSTRACT: A non-bitter chloroquine suspension formulation for pediatric use was prepared in the form of an ion-pair of chloroquine with pamoic acid. Various parameters involved in the formulation of a stable and palatable suspension have been optimized. The suspension was characterized for particle size analysis, viscosity, physical and chemical stability and taste. Release of chloroquine from the ion-pair conducted as dissolution rate studies in simulated gastric media showed near to 100% release instantaneously. In-vivo bioavailability study conducted in albino rats indicated comparable bioavailability of chloroquine from the suspension with that of chloroquine phosphate syrup taken as standard. Stability study conducted over a period of 3 months showed the intactness of the ion-pair and the tasteless behavior of the suspension throughout the period of storage.
    Bollettino chimico farmaceutico 01/2005; 143(10):377-82.
  • Bollettino chimico farmaceutico 01/2005; 144:1-17.
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    ABSTRACT: Various 1,4-substituted derivatives of piperazine (I-XII) were synthesized and evaluated for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (ScMet)--induced seizures and for neurotoxicity (TOX) in the rotorod test in mice and rats. The most promising compounds seem to be 1-[(2,4,6-trimethyl)-phenoxyethyl]-4-(2-hydroxyethyl)-piperazine dihydrochloride (II) and 1,4-bis-[(4-chloro-3-methyl)-phenoxyethyl]-piperazine dihydrochloride (X) which displayed anti-MES activity with their protective index (PI) higher than that for valproate II (rats), X(mice)).
    Bollettino chimico farmaceutico 12/2004; 143(9):329-35.
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    ABSTRACT: In an attempt to design and synthesize more potent quinoline-based chemotherapeutic agents structural modifications of 5, 7-Dibromo-2-methyl-8-benzoyloxyqinoline was carried out. The replacement of the bromine atoms with the requisite alkylamino compound gave four amino-derivatives viz: bis(dipropylamino)-dipyrrolidino-, dipiperidino- and dipiperazino derivatives. The antimicrobial activities of these compounds were investigated against selected Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), Gram-negative bacteria (Escherichin coli, Pseudomonas aeruginosa and Klebsiella spp) and yeast (Candida albicans). All the compounds showed broad or significant antimicrobial activity, which varied from two to ninety times that of the parent compound. The dipyrrolidino derivative was the most effective against Gram-positive bacteria and yeast while the dipiperidino derivative was the most effective against Gram-negative bacteria. No correlation has been established between the minimum inhibitory, (MIC) concentrations of the derivatives and the structural modifications.
    Bollettino chimico farmaceutico 12/2004; 143(9):341-3.
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    ABSTRACT: The paper presents the synthesis of sulfonyl tetrahydropyrimido[4,5-d]pyrimidine derivatives as well as the antimicrobial activity of the obtained compounds. The investigations showed that the obtained sulfonyl derivatives of pyrimido[4,5-d]pyrimidines and especially the compounds with free amino group reveal interesting antibacterial and antifungal activity.
    Bollettino chimico farmaceutico 12/2004; 143(9):321-8.
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    ABSTRACT: Newly developed sildenafil citrate (SC), a selective inhibitor of cyclic guanosine monophosphate (c-GMP) specific phosphodiesterase type 5 (PDE 5) in the corpus cavernosum is used for the oral treatment of erectile dysfunction. A convenient, sensitive and simple method for the determination of sildenafil in human plasma is presented. The analytical technique was based on reversed-phase high-performance liquid chromatography coupled with UV detector set at 295 nm. Rofecoxib was used as internal standard (I.S). Liquid-liquid extraction using diethyl ether was performed to recover sildenafil and rofecoxib. The retention time of I.S and sildenafil were 5.5 minutes and 7.2 minutes respectively. The method was validated over a linear range of 10 to 1000 ng/ml from plasma. Separate stability study showed that sildenafil is stable under conditions of analysis. The extraction efficiency from plasma varied from 79.69% to 81.13 %. The minimum quantifiable concentration was set at 10 ng/ml. (%o CV<12.5%). The method was used for Bioequivalence Study of Two Brands of Sildenafil citrate 50 mg tablets in healthy human volunteers. All pharmacokinetic parameter were calculated along with statistical evaluation.
    Bollettino chimico farmaceutico 12/2004; 143(9):345-9.
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    ABSTRACT: Photooxygenation reaction of ã -terpinene (1) in the presence of tetraphenyl porphine (TPP) or Rose Bengal (RB) gave 2, 5-dihydroperoxy-1-isopropylene-4-methylene-cyclohexane (2), 3,6-dihydroperorxy-3-isopropyl-6-methyl-2,4-cyclohexadiene (3) and 1,2&4,5-diepoxy-1-isopropyl-4-methylcyclohexane (4). The epoxide 4 was also synthesised through the epoxidation reaction of ã-terpinene (1) with m-chloroperbenzoic acid (mcpba).
    Bollettino chimico farmaceutico 12/2004; 143(9):337-9.
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    ABSTRACT: The aim of the present work was to investigate the effectiveness of a dosage form approach for monitoring both the inactivation and the absorption process by targeting insulin delivery to the upper region of small intestine. The dosage form is based on the incorporation of insulin with protease inhibitor and absorption enhancer into polyacrylic polymer Eudragit L-100. Insulin microspheres were prepared by solvent evaporation technique. And also study the effect of these microspheres upon the relative hypoglycemia (RH) effect in white diabetic albino rats has been studied in comparison to that produced after subcutaneous injection of bovine insulin solution. The oral administration of formulation with aprotinin and bile salts gave significant (p< 0.01) hypoglycemia when compared with formulation with insulin alone and with insulin and bile salts. However, the duration, course and the intensity of effect were different for each formulation. It was interesting to observe that the co-administration of aprotinin and bile salts produce prolonged and significant reduction of blood glucose level. A reduction of 4.47-36.81% in plasma glucose levels and RH of about 11.7% relative to subcutaneous injection of soluble insulin solution can be achieved by encapsulation along with protease inhibitor and bile salts.
    Bollettino chimico farmaceutico 11/2004; 143(8):315-8.
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    ABSTRACT: Mesalazine, a drug of choice in the management of ulcerative colitis, was chemically modified as 5-(E)-substituted benzylideneaminosalicylic acid by condensing 5-aminosalicylic acid with selected aryl aldehydes with an intention to improve its pharmacological profile. The tests were performed to study their anti-inflammatory effect on carrageenan-induced ulcerative colitis in albino rats. The histopathological findings, serum transaminase level and lipid peroxide content in the intestine and liver were taken as indices of pharmacological activity. The azomethine derivative formed from salicylaldehyde (5-ASASB3) was found to have maximum activity and it reversed the disease symptoms in experimental animals The azomethine derivative markedly reduces the ulcerative colitis when compared with parent molecule, mesalazine.
    Bollettino chimico farmaceutico 11/2004; 143(8):309-13.
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    ABSTRACT: Cyclization of cinnamoyl isothiocyanate with nucleophilic reagents either spontaneously or with added a reagents is reported.
    Bollettino chimico farmaceutico 11/2004; 143(8):291-7.
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    ABSTRACT: Four novel series of 1,4-naphthoquinone derivatives namely 2,3-disubstiuted 4-[(benzothiazol-2-yl)hydrazono]-1,4-dihydronaphthalen-1-one 4a-c, N1-(2,3-disubstituted-4-oxo-1,4-dihydronaphthalen-1-ylidene)-N2-(benzotriazol-1-yl)acetic acid hydrazide 5a-c, 2,3-disubstituted 4-[(5-aryl-2,3-dihyrothiazol-2-ylidene)hydrazono]-1,4-dihydronaphthalen-1-one 7a-c, and 3-methyl-2-substituted carbamoyl or thiocarbamoyl-hydrazinocarbonylmethylthio-1,4-dihydronaphthalene-1,4-dione 9a-c were synthesized. Three of the new compounds were chosen by NCI to be evaluated as anticancer agents and they showed promising activity. All the prepared compounds were tested as antimicrobial agents.
    Bollettino chimico farmaceutico 11/2004; 143(8):299-307.
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    ABSTRACT: Hydrazinopyrimidine 3 was prepared and transformed into 4, 5 by the reaction with Ar-Cl and POCl3, respectively. Also 3 transformed into 6, 7 by the reaction with ArCHO and FeCl3 respectively. Compound 8 was prepared and transformed into 9, 10, 11 by the reaction with DDC, ethyl bromoacetate and Sodium ethoxide respectively.
    Bollettino chimico farmaceutico 10/2004; 143(7):275-9.
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    ABSTRACT: The objective of the current study was to determine whether homocysteine elevations precede the development of pre-eclampsia, and to examine the relationship between the occurrence of pre-eclampsia and the degree of hyperhomocysteinemia, so as to find a new prognostic parameter for women with liable to develop pre-eclampsia. The study comprised 103 pregnant females chosen of those attending the Antenatal Care Unit at Benha University Hospital and accepted to donate blood samples at the 16th week of gestation. Women, who delivered at Benha University Hospital, were retrospectively allocated into two groups: Control group (Group C): comprised 64 (71.1%) parturient, who completed their full term pregnancy without the development of pre-eclampsia. Pre-eclampsia group (Group PEc): comprised 26 (28.9%) parturient who developed pre-eclampsia throughout their course of pregnancy but had completed their full term pregnancy. Through the present study, estimated fasting plasma tHcys levels were higher than the 90th percentile of the control group (> or = 5.1 ng/dl) in 6 (9.4%) women in group C and in 9 (34.6%) in group PEc. There was a significant (P<0.05) increase of fasting plasma tHcys levels in nullipara pre-eclamptic parturient as compared to multiparous control parturient. Also, a negative significant correlation was reported between parity and the fasting plasma tHcys level in pre-eclamptic parturient. The present results showed a significant increase of fasting plasma tHcys level in obese women with a positive significant correlation between fasting plasma tHcys level and BMI in PEc group. Thus, it can be concluded that hyperhomocysteinemia is an indirect risk factor for placental vasculopathy predating clinical pre-eclampsia, and can be used as a biomarker for identifying women at risk of complications and adverse pregnancy outcomes.
    Bollettino chimico farmaceutico 10/2004; 143(7):281-7.
  • Bollettino chimico farmaceutico 07/2004; 143(5):194.

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