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카르보폴-젤라틴의 상분리법을 이용한 Acyclovir 마이크로캅셀 현탁액의 제조 및 생물학적 평가
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  • 카르보폴-젤라틴의 상분리법을 이용한 Acyclovir 마이크로캅셀 현탁액의 제조 및 생물학적 평가
저자명
조진호,한양희,이정우,최영욱,Cho. Jin-Ho,Hahn. Yang-Hee,Yi. Jung-Woo,Choi. Young-Wook
간행물명
藥劑學會誌
권/호정보
1993년|23권 3호|pp.139-144 (6 pages)
발행정보
한국약제학회
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정기간행물|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

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 $40^{circ}C$, 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 $C_{max}$, $T_{max}$, 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.