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目的:优化胃舒原位凝胶的成型处方,并对释放度进行研究。方法:以胶凝温度和黏附力为指标,筛选了温敏型原位凝胶的成型基质配比、载药量、生物黏附材料种类及用量,确定了最优成型工艺,并考察了最佳处方的热可逆性。通过释放度试验,研究了药物的体外释放规律。结果:优选出以P40716%、P1887.5%为温敏型凝胶基质,1%HPMC为生物黏附材料,载药量为0.8 g·ml-1的成型处方。该处方在50℃以下热可逆性良好。通过释放度试验得出释放度方程为:LnQ=0.915 2Ln(t)+4.293,r=0.959。该模型符合RITGER-PEPPAS方程,证明了该温敏型原位凝胶剂在释放介质中的释药体系是通过Fick扩散和凝胶骨架溶蚀两种机制协同作用的结果。连翘苷在120 min释放度达到93.95%。结论:制成的胃舒原位凝胶具有较高的生物黏附性和良好的工艺重复性,释放性能较好。
OBJECTIVE: To optimize the forming prescription of gastric-stomach collagen in situ and study its release. Methods: Based on the gelation temperature and the adhesion, the optimum ratio of the matrix, drug loading, bioadhesive material and dosage of the thermo-sensitive in-situ gel were screened out to determine the optimal molding process and the best Prescriptions are thermoreversible. Through the release test, the drug release in vitro was studied. Results: The prescription of P40716%, P1887.5% as thermo-sensitive gel matrix, 1% HPMC as bioadhesive material and drug loading of 0.8 g · ml-1 were selected. The prescription below 50 ℃ thermal reversibility good. The release degree equation was obtained through the release test: LnQ = 0.915 2Ln (t) + 4.293, r = 0.959. The model accords with the RITGER-PEPPAS equation, which proves that the release system of the temperature-sensitive in-situ gel in the release medium is the result of the synergistic effect of Fick diffusion and gel skeleton dissolution. Forsythin released at 120 min reached 93.95%. CONCLUSION: The in situ Gelsum made gel has high bioadhesion and good reproducibility of process, and has good release properties.