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目的:研制丹参川芎嗪鼻用温敏凝胶并对其体外释放度及粘膜渗透性进行考察。方法:以泊洛沙姆407(P407)、泊洛沙姆188(P188)、PEG-6000的用量为考察因素,胶凝温度为考察指标,通过星点设计-效应面法优选丹参川芎嗪温敏凝胶基质处方;采用Franz扩散池法考察该制剂体外释放和黏膜渗透作用。结果:最优处方中P407、P188、PEG-6000用量分别为18%、7%、1%,载药凝胶中药物12 h累积释放度为70%以上,释放曲线符合一级动力学方程。载药凝胶中盐酸川芎嗪和丹参素12 h累积渗透量分别为2 649.77和119.72μg/cm2。结论:星点设计-效应面法所建模型能较好地应用于该凝胶的处方优化,同时研制的凝胶制剂具有胶凝温度准确、缓释和较好的黏膜渗透作用。
OBJECTIVE: To develop a thermosensitive gel of ligustrazine for nasal salvia miltiorrhiza and investigate its in vitro release and mucosal permeability. Methods: The dosage of poloxamer 407 (P407), poloxamer 188 (P188) and PEG-6000 were taken as the investigation factors and the gelation temperature was taken as the index of investigation. The optimal design of Salviae miltiorrhizae ligustrazine Gum matrix prescription; using Franz diffusion cell method to investigate the preparation in vitro release and mucosal infiltration. Results: The optimum dosage of P407, P188 and PEG-6000 were 18%, 7% and 1%, respectively. The cumulative release of P407, P188 and PEG-6000 in drug-loaded gel was above 70% in 12 h. The release curve was in accordance with the first-order kinetic equation. The cumulative permeation amounts of ligustrazine hydrochloride and danshensu in drug-loaded gels for 12 h were 2 649.77 and 119.72 μg / cm2, respectively. Conclusion: The model of star-point design-response surface method can be applied to optimize the formulation of the gel. At the same time, the developed gel preparation has the advantages of accurate gelation temperature, sustained release and better mucosal infiltration.