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阿昔洛韦阴道生物黏附片的研究

Studies on vaginal bioadhesive tablets of acyclovir.

作者信息

Genç L, Oğuzlar C, Güler E

机构信息

Faculty of Pharmacy, Anadolu University, Eskişhir, Turkey.

出版信息

Pharmazie. 2000 Apr;55(4):297-9.

PMID:10798244
Abstract

Bioadhesive vaginal tablets were prepared using poly(acrylic acid) (PAA); Methylcellulose (MC), carboxymethyl cellulose (CMC), hydroxypropyl cellulose (HPC) and hydroxypropylmethyl cellulose (HPMC) as bioadhesive polymers in different concentrations and acyclovir as drug by direct compression technique (DCT) and wet granulation technique (WGT). Physical tests were applied to the tablets. The swelling behavior of vaginal tablets in distilled water, lactic solution and cow vagina, acyclovir release rate in lactic solution and bioadhesion to vaginal mucosa in cow vagina, in situ, were investigated. Swelling of the tablets containing HPC, CMC and MC was very rapid and caused disintegration of the tablets. The swelling behaviour of the tablets containing HPMC lasted 6 h in lactic solution. The force (N) necessary to detach the tablets from the vaginal tissue was found to depend on concentration and type of the bioadhesive polymer. The tablets containing HPMC needed the most detachment force.

摘要

采用聚丙烯酸(PAA)、甲基纤维素(MC)、羧甲基纤维素(CMC)、羟丙基纤维素(HPC)和羟丙基甲基纤维素(HPMC)作为生物黏附聚合物,以不同浓度,阿昔洛韦作为药物,通过直接压片技术(DCT)和湿法制粒技术(WGT)制备了生物黏附阴道片。对片剂进行了物理测试。研究了阴道片在蒸馏水、乳酸溶液和母牛阴道中的溶胀行为,阿昔洛韦在乳酸溶液中的释放速率以及在母牛阴道中原位对阴道黏膜的生物黏附性。含HPC、CMC和MC的片剂溶胀非常迅速,导致片剂崩解。含HPMC的片剂在乳酸溶液中的溶胀行为持续6小时。发现将片剂从阴道组织分离所需的力(N)取决于生物黏附聚合物的浓度和类型。含HPMC的片剂需要最大的分离力。

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