- Friday, December 4, 2009
- Published at:J Liposome Res. 2009 Dec 4
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The present article describes a comparative study of the performances of liposomes and ethosomes as specialized delivery systems for distamycin A (DA) and two of its derivatives. Liposomes and ethosomes were prepared by classical methods, extruded through polycarbonate filters, and characterized in terms of dimensions, morphology, and encapsulation efficiency. It was found that DA was associated with vesicles (either liposomes or ethosomes) by around 16.0%, while both derivatives of DA showed a percentage of association around 80% in the case of liposomes and around 50% in the case of ethosomes. In vitro antiproliferative activity experiments performed on cultured human and mouse leukemic cells demonstrated that vesicles were able to increase the activity of both derivatives of DA. In addition, it was demonstrated that the aging of both liposomes- and ethosomes-associated distamycin suspensions did not heavily influence the vesicle size, while all samples showed a relevant drug leakage with time. Moreover,
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- Saturday, March 1, 2008
- Published at:Not Found
- A new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives has been identified as potent A2B adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A2B, A1, A2A, and A3 adenosine receptors. N-(4-chloro-phenyl)-2-[3-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-5-methyl-pyrazol-1-yl] (11c) showed a high affinity for the human A2B adenosine receptor Ki = 7 nM and good selectivity (A1, A2A, A3/A2B > 140). Synthesis and SAR of this novel class of compounds is presented herein.
Bioorganic & Medicinal Chemistry, Volume 16, Issue 5, 1 March 2008, Pages 2419-2430
http://dx.doi.org/10.1016/j.bmc.2007.11.058
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- Tuesday, January 1, 2008
- Published at:ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH Volume: 58 Issue: 3 Pages: 149-153 Published: 2008
- The aim of this study was to compare the bioavailability, after oral administration, of the generic "Adcef (R) Suspension''(test) (125 mg/5 ml. cefdinir; CAS 91832-40-5), with that of a commercially available original preparation (reference) (125 mg/ 5 ml cefdinir). For this purpose a randomized, two-way, crossover, bioequivalence study was performed in 24 healthy, male volunteers. The Middle Eastern selected volunteers were divided into two groups of 12 subjects. One group was treated with the reference standard and the other one with the test, with a crossover after the drug washout period of 7 days. Blood samples were collected at fixed time intervals and cefdinir concentrations were determined by a validated HPLC assay method. The pharmacokinetic parameters AUC(0-24), AUC(0-infinity) C-max T-max K-e and T-1/2 were determined for both formulations and were compared statistically to evaluate the bioequivalence between the two brands of cefdinir, using the statistical model recommended by the FDA. The analys
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- Monday, January 1, 2007
- Published at:The Islamic University Journal (Series of Natural Studies and Engineering), Vol.15, No. 1, pp 13 -22 , 2007
- Purpose: The aim of this study is to develop bromhexine hydrochloride 1 %w/v oral solution for veterinary use and to evaluate its stability. Methods: Solutions of Bromhexine hydrochloride (1%w/v) were prepared by dissolving bromhexine hydrochloride in benzyl alcohol at 50 °C then alcohol 96 % v/v; Tween 80 and purified water were added. The obtained solution was filled in amber glass bottles, and the solution was stored at 25 °C/60 % relative humidity (RH) and at 40 °C /75% RH. The strengths of bromhexine hydrochloride were determined by High performance liquid chromatographic assay at 0, 2, 4, 6, 8, 10, 12, 16, 20 and 24 months. The concentrations of the drug were directly related to the peak area. pH, odor, color and crystal formation was also monitored. Results: The degradation of bromhexine hydrochloride 1% w/v oral solution was faster at 40 °C/75% RH than at 25 °C /60% RH. No significant differences were found between the initial and final pH value for the solution at the studied cond
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- Monday, January 1, 2007
- Published at:The Islamic University Journal (Series of Natural Studies and Engineering), Vol.15, No. 2, pp 83-94, 2007, ISSN 1726-6807
- Abstract:To evaluate the scientific knowledge and attitudes of health professionals in Palestine regarding the advantages of chewable tablets in comparison with other related dosage forms. Methods: Data was gathered from a questionnaire that was handed out to community pharmacists & Physicians. Pharmaceutical industry decision makers were also enrolled in this study. Data was analyzed using SPSS statistical software program version 11.0. Results: Both the 149 pharmacists and 111 physicians who participated in this study, had very close opinions with regard to the superiority of chewable tablets over the corresponding liquid dosage forms, especially when issues of palatability, stability, dose precision, ease of administration, portability and safety were mentioned. Pharmacists and physicians were uncertain about the higher effectiveness of chewable tablets in comparison with other related dosage forms, (i.e syrups and suspensions), which contain the same active ingredients. All industrial decision makers
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