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目的 制备含有补骨脂素及醋酸地塞米松的脂质体凝胶并研究其经皮吸收后体内分布 ,为临床新制剂的开发打下基础。方法 用均匀设计优选该脂质体凝胶的处方及制备工艺 ,并用扫描电镜观测其外观、大小及分布 ,用分子筛法结合HPLC测定其包封率 ,初步考察该制剂的稳定性 ,并以家兔为试验对象研究其皮肤刺激性 ,用豚鼠研究其经皮传递后主药体内分布情况。结果 由优选出的处方及工艺制备的脂质体凝胶外观圆整 ,分布较均匀 ,包封率理想 ,稳定性良好 ,与对照品相比对家兔皮肤有明显的保护作用 ,在豚鼠皮肤内的滞留量显著增加 ,是对照品的 4.2倍 (P <0 .0 1) ,而全身吸收量明显降低 (P <0 .0 5 )。结论 含有补骨脂素及醋酸地塞米松的脂质体凝胶高效低毒 ,可望成为临床治疗白癫疯的新型外用制剂。
OBJECTIVE To prepare liposome gel containing psoralen and dexamethasone acetate and study its distribution in vivo after percutaneous absorption, and lay the foundation for the development of new clinical preparations. Methods The formulation and preparation of the liposome gel were optimized by uniform design. The appearance, size and distribution of the liposome gel were observed by scanning electron microscopy. The entrapment efficiency was determined by molecular sieve method and HPLC. The stability of the preparation was also investigated. The rabbits were used to study the skin irritation, and the guinea pigs were used to study the in vivo distribution of the drug after transdermal delivery. Results The liposome gel prepared by the optimized formulation and process showed a round and uniform appearance with good encapsulation efficiency and good stability. Compared with the control, the liposome gel has obvious protective effect on the skin of the guinea pig, (P <0. 01), while systemic absorption was significantly decreased (P <0. 05). Conclusion The liposome gel containing psoralen and dexamethasone acetate has the advantages of high efficiency and low toxicity and is expected to become a new topical preparation for the clinical treatment of epilepsy.