The present invention features a long term controlled release formulation of the nalbuphine pro-soft drug, Sebacoyl dinalbuphine ester, in combination with commonly used pharmaceutical excipient biodegradable polymer PLGA. Said formulaion was selected from the following groups of pharmaceutical formulations including such as: tablets, capsules, soft capsules, granules, suspensions, microspheres, oral implants, implantable injections and others. Said long term controlled release formulation significantly improved the dosage and frequency for administering nalbuphine to once per half month or few months, compared to four to six times per day in the traditional way, which is one of the major features and effects of the present invention. The major improvement of this inventioncan be achieved by confirmation of the pharmacokinetic profiles and the duration time of efficacy level of drug through in vivo experiments, subsequently improved the dosage and frequency of the traditionally used nalbuphine injections.本發明係關於一種包含那布扶林(nalbuphine)前驅軟藥-癸二醯雙那布扶林酯(Sebacoyl dinalbuphine ester)、與藥學常用可降解高分子PLGA賦型劑之組成物,並將該組合物製備成可進入人體之長效控釋劑型,其中包含錠劑、膠囊、軟膠囊、丸劑、懸浮液、微球、口腔植入片、乳化針劑、植入劑或其他劑型,該控釋劑型大幅度改善那布扶林(nalbuphine)傳統習用注射劑型之使用量,原需一天投藥四次到六次改善為半個月或多個月投藥一次,此亦為本發明之特徵與功效之一。本發明主要利用體內實驗,確認本發明之控釋劑型的藥物動力學性質以及評估效期維持時間,藉以改善那布扶林(nalbuphine)傳統習用注射劑型之使用量。
