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盐酸罗哌卡因多囊脂质体的制备及体外释放行为

Preparation of ropivacaine hydrochloride multivesicular liposomes and release in vitro

  • 摘要: 目的 : 制备盐酸罗哌卡因多囊脂质体(RP-MVL),并且考察其理化性质和体外释放行为。 方法 : 采用复乳化法制备盐酸罗哌卡因多囊脂质体,单因素试验考察影响多囊脂质体包封率的因素,以包封率为指标采用Box-Behnken设计法对盐酸罗哌卡因多囊脂质体的处方工艺进行优化,采用优化处方制备3批多囊脂质体,测定包封率,考察体外释放行为。 结果 : 盐酸罗哌卡因多囊脂质体粒径均一,有85%的粒径分布在7~30 μm之间,脂质药物质量比为1.328∶1,磷脂与胆固醇质量比为1.5∶1,三油酸甘油酯为6 mmol/L时,多囊脂质体的包封率最佳,包封率达90%以上,37 ℃条件下在PBS介质中释药时间可达48 h,符合一级释药规律。 结论 : 盐酸罗哌卡因多囊脂质体具有较好的缓释效果。

     

    Abstract: Aim :To prepare ropivacaine hydrochloride multivesicular liposomes,and to study the physicochemical properties and drug release behavior in vitro. Methods :Ropivacaine hydrochloride multivesicular liposomes were prepared by the multiple emulsion method.Single factor experiments were utilized to study the factors which affect the encapsulation efficiency of multivesicular liposomes.The formulation and pharmaceutical process were optimized by Box-Behnken experimental design,with the factors of encapsulation efficiency as the criteria.Three batches of the optimized multivesicular liposomes were prepared, and the encapsulation efficiency and in vitro release behavior were studied. Results :The particle size of the optimized multivesicular liposomes was uniform and 85% of them were well distributed in the range of 7-30 μm.The encapsulation efficiency was up to 90% when the ratios of lipid to drug,phospholipids to cholesterol and the amount of triolein was 1.328∶1(w/w),1.5∶1(w/w) and 6 mmol/L,respectively.The release profile in vitro fitted to a first-order kinetics with the period of release up to 48 h in PBS buffer under 37 °C. Conclusion :Ropivacaine hydrochloride multivesicular liposomes showed high encapsulation efficiency and significant sustained-release feature.

     

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