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[粘度对软膏剂、乳膏剂、凝胶剂和乳剂药物释放的影响]

[Influence of viscosity on drug release from ointments, creams, gels and emulsions].

作者信息

Erös I, Soósné-Csányi E, Selmeczi B

机构信息

Szent-Györgyi Albert Orvostudományi Egyetem Gyógyszertechnológiai Intézet.

出版信息

Acta Pharm Hung. 1994 Mar;64(2):57-61.

PMID:8017209
Abstract

The authors studied the drug release from high number of water-free ointments, creams, emulsions and hydrogels. They targeted to find correlation between the viscosity of these pharmaceutical forms and their drug release. Neutral oil was the lipophilic phase of emulsions, the emulsifiers were from Tween and Tagat series. The creams tested consisted of ESMA ointment, Teginacid and/or Softisan emulsifiers and water in 60-80 w/w%. The drug release from Eudispert, methyl-cellulose and hydroxy-ethylcellulose gels was studied. The applied active ingredients were as follows: griseofulvin, sulfadimidine, salicylic acid and ephedrine hydrochloride. Relevant literature suggest a reciprocal correlation between the viscosity of ointments and the quantity of the released drugs. The authors confirmed the general validity of this correlation in case of the following preconditions: if the solubility and distribution of drug do not change along with the change of viscosity there is reciprocal ratio between viscosity and the quantity of drug released. This reciprocal correlation prevails only in a small range of viscosity, that is in systems resembling Newton's liquids. In cases of ointments and gels of higher viscosity a reciprocal relationship exists between the logarithm of viscosity and the quantity of drugs released.

摘要

作者研究了大量无水软膏、乳膏、乳液和水凝胶的药物释放情况。他们旨在找出这些药物剂型的粘度与其药物释放之间的相关性。中性油是乳液的亲脂相,乳化剂来自吐温系列和塔格糖酯系列。所测试的乳膏由ESMA软膏、泰吉酸和/或Softisan乳化剂以及60 - 80 w/w%的水组成。研究了优迪思、甲基纤维素和羟乙基纤维素凝胶的药物释放情况。所应用的活性成分如下:灰黄霉素、磺胺二甲嘧啶、水杨酸和盐酸麻黄碱。相关文献表明软膏的粘度与释放药物的量之间存在反比关系。作者在以下前提下证实了这种相关性的普遍有效性:如果药物的溶解度和分布不随粘度的变化而改变,那么粘度与释放药物的量之间存在反比关系。这种反比关系仅在粘度的小范围内存在,即在类似于牛顿液体的体系中。在高粘度的软膏和凝胶情况下,粘度的对数与释放药物的量之间存在反比关系。

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