盐酸青藤碱自溶性微针的制备及其体外经皮渗透性能考察

发布时间：2018-01-18 14:05

本文关键词：盐酸青藤碱自溶性微针的制备及其体外经皮渗透性能考察　出处：《中国实验方剂学杂志》2016年10期 　论文类型：期刊论文

【摘要】：目的:优选盐酸青藤碱自溶性微针的处方工艺,并考察微针对盐酸青藤碱经皮渗透性能的影响。方法:采用浇注法制备盐酸青藤碱微针,以成型性和机械性为指标筛选可达到最佳载药量的处方,并对制备出的微针进行表征。采用改良Franz扩散池考察载药凝胶和微针的经皮渗透效果。运用HPLC检测盐酸青藤碱含量,流动相甲醇-0.1%磷酸盐水溶液(18∶82),检测波长263 nm。结果:最佳处方聚乙烯吡咯烷酮、硫酸软骨素、盐酸青藤碱质量分数分别为50%,15%,35%。制得的盐酸青藤碱微针针形完整、机械强度良好,能够穿刺铝箔和离体的大鼠皮肤;载药微针组和载药凝胶组的48 h累积渗透量分别为(80 738.41±1 354.72),(15 210.02±288.57)μg·cm~(-2),渗透速率依次为(1 627.40±28.68),(321.72±15.20)μg·cm~(-2)·h~(-1)。结论:制备的载药自溶性微针机械性和成型性良好。相较于载药凝胶,盐酸青藤碱微针能够更加有效地实现经皮渗透,可改善青藤碱透皮制剂的透皮性能。
[Abstract]:Objective: to optimize the prescription process of sinomenine hydrochloride autolytic microneedle and to investigate the effect of microinjection on transdermal permeability of sinomenine hydrochloride. Methods: sinomenine hydrochloride microneedle was prepared by pouring method. The formulation of the best drug loading can be obtained by selecting the formability and mechanical property as the index. The modified Franz diffusion cell was used to investigate the transdermal permeation effect of drug-loaded gel and microneedle. The content of sinomenine hydrochloride was detected by HPLC. The mobile phase consisted of methanol-0.1% phosphate aqueous solution with a detection wavelength of 263 nm. Results: the best formulation was polyvinylpyrrolidone and chondroitin sulfate. The sinomenine hydrochloride has a fine needle shape, good mechanical strength, and can puncture aluminum foil and isolated rat skin. The cumulative osmotic capacity of microneedle loaded group and drug loaded gel group at 48 h was 80738.41 卤1 354.72). 15 210.02 卤288.57 渭 g 路cm ~ (-2) 路cm ~ (-2), and the osmotic rate was 1 627.40 卤28.68). 321.72 卤15.20 渭 g 路cm ~ (-2) 路h ~ (-1) 路h ~ (-1). Conclusion: the prepared self-soluble microneedle has good mechanical and formability, and is better than that of drug-loaded gel. The transdermal penetration of sinomenine hydrochloride microneedle is more effective and can improve the transdermal performance of sinomenine.
【作者单位】：安徽中医药大学药学院安徽省中医药科学院药物制剂研究所安徽省中药制剂工程技术研究中心;
【基金】：国家自然科学基金项目(81274099) 安徽省自然科学基金项目(11040606M219)
【分类号】：R943
【正文快照】： [网络出版时间]2016-03-31 14:50青藤碱是从青风藤中提取的异喹啉类生物碱单体,具有抗炎、免疫、镇痛、降压、抗心律失常等药理活性,临床上已有其用于治疗类风湿性关节炎及心律失常的制剂[1]。但青藤碱的生物半衰期较短,临床治疗一般需长期口服,且用药剂量偏大,易产生胃肠道刺

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