白芷香豆素黏胶分散型贴剂的制备及体外经皮渗透研究

Preparation of Drug-in Adhesive Patch of Angelica Dahurica Coumarins and Study Its in Vitro Permeability Through Excised Anthony Pig Skin

关键词:  白芷香豆素  经皮渗透  黏胶分散型  贴剂

Key words:  Angelica dahurica coumarins  transdermal permeation  drug-in adhesive  patch

摘要:

目的 制备白芷香豆素黏胶分散型贴剂，考察其离体皮肤渗透性和物理性状，筛选贴剂处方，提高白芷香豆素的透皮吸收速率。方法 将白芷香豆素分散于尤特奇压敏胶中，采用流涎工艺制备黏胶分散型贴剂。用Franz扩散池进行乳猪离体皮肤渗透实验，用HPLC测定欧前胡素的含量，考察了白芷香豆素含量、促渗剂的种类和用量、压敏胶的种类和用量、工艺参数对药物稳态透皮速率和贴剂的物理性状的影响。结果 优选出最佳处方为：药物含量1.0 mg·cm^-2，Eudragit E100 9 mg·cm^-2，油酸0.6 mg·cm^-2；固化时间为40 min，稳态透皮速率达到0.82 μg·cm^-2·h^-1。结论 制得的黏胶分散性白芷香豆素贴剂有较高的经皮渗透速率和较好的物理性状，优选出的处方及工艺稳定、可行。

Abstract:

OBJECTIVE To prepare the patch of Angelica dahurica coumarins and investigate its transdermal absorption characteristics in vitro. The foumula was chosen to improve the drug's permeation rate. METHODS Angelica dahurica coumarins was dispersed in pressure sensitive adhersive(PSA). A monolithic drug-in-adhesive transdermal patch was developed using sialorrhea technology. The experiment of percutaneous penetration of anthony pig skin in vitro was operated by Franz diffusion cells. HPLC was used to determine drug's content and permeation rate. The influence of some factors on the transdermal flux were investigated, such as the kind and the content of penetration enhancer, the kind and the content of PSA, technological parameter of the content of angelica dahurica coumarins. RESULTS The best formulation were Angelica dahurica coumarins 1.0 mg·cm^-2, Eudragit E100 9 mg·cm^-2, oleic acid 0.6 mg·cm^-2 and curing time 40 min. The permeation rate reached 0.82 μg·cm^-2·h^-1. CONCLUSION The drug-in adhesive patch of Angelica dahurica coumarins have high transdermal rate and good physico-characteristic. The optimized formula and technology is stable and feasible.