【摘要】 目的考察溶剂分散和挤压器联动装置制备脂质体药物制剂的工艺条件、可行性和适用范围。方法联动装置应用了溶剂分散法制备脂质体的原理,通过高压泵将溶于有机相的磷脂和脂溶性药物与水溶液在溶液混合器中高压快速混合使之形成多相多层脂质体,在高压下将脂质体连续通过挤压器,一步形成最终产品。结果新装置将高压泵、溶液混合器、脂质体粒径整合控制设备和高压超滤透析柱组成联动线,使得从投料到获得脂质体成品的整个过程一步完成,减少了不必要的中间过程。应用该装置制备的脂质体的质量可控性好,非常适合脂溶性药物脂质体制剂的大规模制备。同时用该装置制备的脂质体可以形成有效的pH梯度,适合于弱碱性药物的载药。结论实验证明,这种联动装置可应用于脂质体的工业化生产,其制备工艺简便、可控性好、实用性强。更多还原

【Abstract】 OBJECTIVE To apply the solvent dispersion technique and extruding linkage device as a feasible and suitable method for the preparation of liposomes.METHODS The linkage device applied the principle of preparing liposmes by solvent dispersion tchnique.Phospholipids and lipid-soluble drugs were transferred into solution mixer by high-pressure pump and then were mixed with water under pressure and at great speed to form multiphasic & multilamellar vesicles,which were extruded continuously by extruder under high pressure,and then the final products were produced directly.RESULTS The novel device established a linkage system with combination of high-pressure pump,solution mixer,liposomal particle size integration control equipment,and high-pressure ultra-filtered column,which developed an one-step production process from charging material to preparation of final products.The linkage production line was well-controlled and suitable for the large-scale preparation of liposomes,meanwhile gave liposomes effective pH gradient to help weak bases loaded.CONCLUSION The study shows that the linkage device can be applied in industrial production of liposomes with the advantages of convenient preparation process,good control lability and strong practicability.更多还原