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青藤碱水凝胶软膏剂的制备及体外透皮性能评价

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目的:为提高青藤碱(Sinomenine,Sin)经皮给药的生物利用度,改善其皮肤渗透性能.方法:将Sin直接分散至卡波姆940(Cp940)基质中制得富含Sin的水凝胶软膏剂,并对其性能进行考察.首先,控制Cp940和甘油的用量,以所制备水凝胶膏剂的外观形状、累积失水率和黏度作为评价指标,合理设计实验制备水凝胶软膏剂并确定最优配方;其次,采用Franz扩散池通过体外透皮实验对不同渗透促进剂进行优化.结果:该软膏剂最优配方为1.5%Cp940,0.35%氢氧化钠,10%乙醇,20%甘油,0.2%聚乙烯丙酸钠,2%氮酮,5%1,2-丙二醇,2%药物,0.1%尼泊金乙酯,水适量,所制备凝胶膏剂呈黄色不透明半固体状,常温储存不干涸不液化,黏度适宜,易于涂布和经皮给药.体外释放实验显示,当氮酮与1,2-丙二醇联用时,Sin经皮渗透效果最佳,12 h累积释放量和累积释放率分别为347.12±3.84 μg·cm-2和22.8%,为零级释放动力学模型.结论:所制备青藤碱水凝胶软膏剂有望成为一种有效治疗类风湿性关节炎的可直接局部经皮给药的新制剂.
Preparation of Sinomenine-loaded Hydrogel Ointment and Evaluation of Its Transdermal Performance in Vitro
Objective:In order to enhance the bioavailability of Sinomenine(Sin)for transdermal administration and improve its skin permeation properties,Sin-enriched hydrogel ointment was prepared by directly dispersing Sin into Carbomer 940(Cp940)matrix,and then the transdermal performances in vitro were investigated.Methods:Firstly,the amount of Cp940 and glycerol were used as the investigating factors,and the appearance shape,cumu-lative water loss and viscosity of the prepared ointment were used as the evaluation indexes to optimize the optimal prescription of the hydrogel ointment.Secondly,in vitro transdermal experiments with different permeation enhanc-ers using a modified Franz diffusion cell.Results:The results showed that the optimal formulation of the prepared hydrogel ointment was 1.5%Cp940,0.35%NaOH,10%ethanol,20%glycerol,0.2%sodium polyvinyl propi-onate,2%azidone,5%1,2-propanediol,2%drug,0.1%ethyl p-hydrobenzoate and appropriate amount of wa-ter.And the prepared hydrogel ointment was in the form of a yellow opaque semi-solid,which was stored at room temperature with no dry-out or liquefy.Meanwhile,ointment was easy to be spread and applied by administered transdermally on account of the suitable viscosity.The in vitro release experiments indicated that the best transder-mal penetration of Sin was achieved when azidone was combined with 1,2-propanediol as transdermal accelerators,as well as the Qn and cumulative release rate in 12 h were 347.12±3.84 μg·cm-2 and 22.8%,respectively,which could be identified as a zero-level release kinetic model.Conclusion:Therefore,the prepared Sin-enriched hydrogel ointment was expected to be a novel transdermal formulation for the effective treatment of rheumatoid ar-thritis.

sinomenineCp940hydrogel ointmentformula optimizationin vitro transdermal performances

牛艳莲、刘淑兰、王文雅、王子惠、凌爱霞、吕美

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济宁医学院药学院,山东 日照 276826

青藤碱 Cp940 凝胶软膏剂 配方优化 经皮吸收

2024

南京晓庄学院学报
南京晓庄学院

南京晓庄学院学报

CHSSCD
影响因子:0.201
ISSN:1009-7902
年,卷(期):2024.40(6)