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KMID : 0369819930230030139
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Jorunal of Korean Pharmaceutical Sciences
1993 Volume.23 No. 3 p.139 ~ p.144
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Biological Evaluation of Acyclovir Microcapsule Suspension Prepared by Carbopol - Gelatin Coacervation
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조진호/Cho JH
한양희/이정우/최영옥/Hahn YH/Yi JW/Choi YW
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Abstract
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Microencapsulation of acyclovir, an effective antiviral agent which acts as a specific inhibitor of herpes DNA polymerase, by carbopol-gelatin complex coacervation has been carried out to develop an oral controlled release preparation, which could improve the absorption characteristics in GI tract. After dissolving carbopol and gelatin separately in distilled water at 40?C, gelatin solution was mixed with carbopol solution while stirring at the same temperature. The pH of the mixture was lowered gradually by dropwise addition of 10% HCI with continuous stirring, and then, at pH 3.5, positively charged gelatin molecules were attracted to negatively charged carbopol. These coacervation processes were observed by optical microscopy during preparation. Plasma concentrations of acyclovir in rats after an oral administration of microcapsule suspension were assayed by HPLC, and pharmacokinetic parameters were calculated based on the model-independent analyses. Two standard formulations, oral solution and intravenous bolus injection, were used as references to compare the bioavailability. It has been revealed that Cmax, Tmax, and MRT of microcapsule suspension were greater than those of oral solution, which results in about two-fold increases in bioavailability. Therefore, in conclusion, the carbopol-gelatin microcapsule of acyclovir might be evaluated as an effective oral controlled release preparation which could increase the bioavailability of acyclovir.
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KEYWORD
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Acyclovir, Microencapsulation, Coacervation, Carbopol, Gelatin, Bioavailability, Mean residence time, Oral administration
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