利福平强化靶向新剂型研究

A Study of Enforcing the New Dosage Form of Targeting RFP

采用超微药物载体技术,将抗结核药利福平制成靶向多相脂质体,并在表面修饰强化。此新剂型具有较强的体内靶向性与病变器官滞留性,达到定向缓释药物的目的。实验表明,小鼠给药后10h肺内和福平浓度,强化靶制剂可达650.4μg/g,比同剂量溶液高9.1倍,维持时间亦更长。本文还对该制剂的稳定性、脂质体粒度分布及药物包封率进行了测定。

The microencapsulation of drug carrier was used to prepare targeting preparations of polyphase liposomes with antituberculosis drug RFP, and the surface of the liposomes was decorated. It is a new dosage form which has targeting and sustained release actions on the diseased organs. As a result, the dosage was decreased, the potency increased and the toxicity and the side effect decreased significantly. Animal experiment showed that oral administration of RFP targeting preparations achieved a concentration of 650.4 μg/g in the target side which is 9.1 times as high as that of RFP solution in the pulmonaries of rats 10 hours after administration. The stability of the preparations and the particle size distribution and the encapsulations of liposomes of drugs were investigated.