Long-acting analgesic / PLGA sustained-release agent of dinalbuphine sebacate

摘要

The present invention is a composition comprising a precursor soft drug containing nalbuphine, nalbuphine sebacate (Sebacoyl dinalbuphine ester), and a biodegradable polymer PLGA excipient often used in pharmacology. It was prepared in a sustained-release dosage form that can be administered and has a long-term effect. The dosage form includes tablets, capsules, soft capsules, pills, suspensions, microspheres, oral implants, and emulsified injections. , Including implants or other dosage forms, this sustained-release dosage form can significantly improve the dose of conventional syringe administration, requiring four to six administrations per day. It is characterized by the fact that it has been improved to a sufficient level by administration from half a month to several months. The present invention evaluates the pharmacokinetic properties of the sustained release dosage form according to the present invention and the duration of the effect through in vivo experiments, and shows that the dose of nalbuphine by conventional syringe administration can be greatly improved. confirmed. [Selection] Figure 1