盐酸米诺环素软膏的释放度研究

目的探讨盐酸米诺环素缓释软膏的体外释放度及释药机制。方法制备盐酸米诺环素软膏供试品溶液和盐酸米诺环素标准品溶液。释放度采用桨法（《中国药典》2010版二部附录XD第二法）,以水为释放介质,体积为500 mL,转速为100 r/min,温度为（37.0±0.5）℃,检测波长为274 nm。采用紫外分光光度法测定释放介质中盐酸米诺环素的含量。结果盐酸米诺环素检测浓度在0.99～19.87μg/mL范围内具有良好的线性关系,线性回归方程为A=0.0301C＋0.0004,相关系素r=1,平均回收率为101.6%,相对标准偏差为1.5%。在1、4、7 h的释放度分别为13.91%、29.89%、40.76%,体外释放度有良好的缓释药物行为。体外释放特征显示该软膏制剂具有复合释药的规律,一级释放机制所占比例更大一些。结论盐酸米诺环素软膏制剂具有缓释作用,释放度测定方法操作简便、快速、准确度好。

Dissolution of minocycline hydrochloride ointment in extended-release drug delivery system

Objective To study the release rate and release mechanism in vitro of minocycline hydrochloride extended-release ointment.Methods Preparation the test solution of minocycline hydrochloride ointment and standard solution of minocycline hydrochloride.And using the second method described in Chinese Pharmacopoeia（2010） as the release rate determination method.The solution medium was distilled water with volume of 500 mL.The rotational speed was100 r/min and the temperature was（37.0±0.5） ℃.The detection wavelength was 274 nm.The content of minocycline hydrochloride in solution medium was measured by UV.Results The linear range of minocycline hydrochloride was0.99-19.87 μg/mL,and linear regression equation was A=0.0301C＋0.0004（r=1）.The average recovery was 101.6%（relative standard deviation is 1.5%）.The release rate of the ointment at 1,4,7 h was 13.91%,29.89%,40.76% respectively,which showed that the preparation had a satisfying extended-release behavior.The release character in vitro demonstrated that the ointment possessed a compound drug release discipline,which preferred to satisfy the first-order release.Conclusion The extended-release drug delivery system-minocycline hydrochloride ointment displayed the extended-release function.This determination method was simple,efficient and accurate,which can be used for the quality control of minocycline hydrochloride in ointment.