The present invention provides a composition comprising nalbuphine prodrug- Sebacoyl dinalbuphine ester and pharmaceutical biodegradable polymer PLGA. The composition is prepared as a controlled release formulation, which can be implanted in a human body, and the formulation is lozenge, capsule, soft capsule, pill, suspension, microsphere, oral implant, emulsified injection, implant or others. The controlled release formulation significantly improves the dosage of common nalbuphine injection, the composition for four times to six times daily administration is improved to once half a month or several months administration, and that is one of the characteristic and effect of the invention. By in vivo tests, the present invention confirmed the pharmacokinetic properties of controlled release formulation, and evaluated effective duration time, the controlled release formulation is used to improve the dosage of common nalbuphine injection.
本发明提供了一种由
纳布啡原药--西巴甲酰二
纳布啡酯和药用
生物可降解聚合物PLGA组成的组合物。该组合物制备成控释制剂,可植入人体,剂型有锭剂、胶囊、软胶囊、丸剂、混悬剂、微球、口服植入剂、乳化注射剂、植入剂等。控释制剂明显改善了普通
纳布啡注射液的用量,将每天给药四次至六次的组合物改善为半个月或几个月给药一次,这也是本发明的特点和效果之一。本发明通过体内试验,证实了控释制剂的药代动力学特性,并对有效持续时间进行了评价,控释制剂用于改善普通
纳布啡注射液的剂量。