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硫酸吗啡口腔黏附片的制剂与体内外评价

Formulation and in vitro-in vivo evaluation of buccoadhesive morphine sulfate tablets.

作者信息

Anlar S, Capan Y, Güven O, Göğüş A, Dalkara T, Hincal A A

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.

出版信息

Pharm Res. 1994 Feb;11(2):231-6. doi: 10.1023/a:1018951323522.

Abstract

Buccoadhesive controlled-release systems for the delivery of morphine sulfate were prepared by compression of hydroxypropyl methylcellulose (HPMC) with carbomer (CP), which served as the bioactive adhesive compound. The release behavior of systems containing 30 mg of morphine sulfate and various amounts of the two polymers was found to be non-Fickian. The adhesion force was significantly affected by the mixing ratio of HPMC and CP in the tablet, and the weakest adhesion force was observed at a ratio of 1:1 (HPMC:CP). Interpolymer complex formation was confirmed between HPMC and CP in acidic medium by turbidity, viscosity, and FT-IR measurements. The amount absorbed (percentage of the drug loaded) of the controlled-release buccoadhesive tablets in six healthy volunteers and was 30 +/- 5%.

摘要

通过将羟丙基甲基纤维素(HPMC)与作为生物活性粘合剂化合物的卡波姆(CP)压片,制备了用于递送硫酸吗啡的口腔粘附控释系统。发现含有30mg硫酸吗啡和不同量两种聚合物的系统的释放行为是非菲克型的。片剂中HPMC和CP的混合比例对粘附力有显著影响,在1:1(HPMC:CP)的比例下观察到最弱的粘附力。通过浊度、粘度和傅里叶变换红外光谱(FT-IR)测量证实了在酸性介质中HPMC和CP之间形成了聚合物间复合物。六名健康志愿者服用控释口腔粘附片后药物的吸收量(载药量的百分比)为30±5%。

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