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pH对含羟丙基甲基纤维素K4M和卡波姆974的基质中盐酸普萘洛尔释放的影响。

Influence of pH on the release of propranolol hydrochloride from matrices containing hydroxypropylmethylcellulose K4M and carbopol 974.

作者信息

Perez-Marcos B, Ford J L, Armstrong D J, Elliott P N, Rostron C, Hogan J E

机构信息

School of Pharmacy and Chemistry, Liverpool John Moores University, UK.

出版信息

J Pharm Sci. 1996 Mar;85(3):330-4. doi: 10.1021/js950359z.

Abstract

The dissolution of propranolol hydrochloride from matrices containing hydroxypropylmethylcellulose K4M (HPMC K4M) and carbopol 974 has been investigated using 0.1 M hydrochloric acid or phosphate buffer at pH 4.5 or pH 7.5. In 0.1 M hydrochloric acid, HPMC K4M predominantly controlled release since carbopol has a low solubility at this pH. As the pH increased, the carbopol became increasingly ionized and interacted with propranolol hydrochloride to form an insoluble complex which retarded the release of the drug. In addition, the nature of the interaction between carbopol 974 and HPMC K4M altered. DSC and viscometric studies indicated that the two polymers contributed synergistically to the gel network at pH 7.5. Thus at pH 7.5 polymers contributed to matrix integrity and to the control of drug release.

摘要

已使用0.1 M盐酸或pH值为4.5或7.5的磷酸盐缓冲液研究了盐酸普萘洛尔从含有羟丙基甲基纤维素K4M(HPMC K4M)和卡波姆974的基质中的溶出情况。在0.1 M盐酸中,由于卡波姆在此pH值下溶解度较低,HPMC K4M主要控制药物释放。随着pH值升高,卡波姆的离子化程度越来越高,并与盐酸普萘洛尔相互作用形成不溶性复合物,从而延缓了药物的释放。此外,卡波姆974与HPMC K4M之间相互作用的性质发生了改变。差示扫描量热法(DSC)和粘度测定研究表明,在pH值为7.5时,这两种聚合物对凝胶网络具有协同作用。因此,在pH值为7.5时,聚合物有助于维持基质的完整性并控制药物释放。

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