Tapentadol pharmaceutical composition for transdermal administration as well as preparation method and application of pharmaceutical composition

Abstract

The invention discloses a pharmaceutical composition for transdermal administration. The pharmaceutical composition contains tapentadol or a pharmaceutically acceptable salt thereof, a polymer dispersion carrier material, a hot-melt protective agent and an optional solubilizer. A preparation method of the pharmaceutical composition includes the following steps: mixing the tapentadol or the pharmaceutically acceptable salt thereof, the polymer dispersion carrier material, the hot-melt protective agent and the optional solubilizer, performing hot-melt extrusion, and performing micronization to obtain the microparticles of the tapentadol or the pharmaceutically acceptable salt thereof. The pharmaceutical composition for the transdermal administration can make the tapentadol or the pharmaceutically acceptable salt thereof rapidly absorbed, and achieve the purpose of sedation before anesthesia without affecting breathing, thereby avoiding the adverse psychological effects of intramuscular injection or intravenous injection acupuncture on children; and at the same time, the pharmaceutical composition can also be used to prevent and / or treat and delay the development of Parkinson disease.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, more specifically to a pharmaceutical composition for transdermal administration of tapentadol, a preparation method and application thereof. Background technique [0002] Tapentadol hydrochloride is a new type of oral analgesic drug jointly developed by Johnson & Johnson Pharmaceuticals of the United States and Gruenenthal GmbH of Germany. Its sustained-release tablet was approved by the FDA in August 2012 for the treatment of adult diabetic peripheral neuropathy (DPN). associated neuropathic pain. Through oral analgesia twice a day, continuous opioid analgesia can be achieved and maintained for a period of time. [0003] Delayed formulations are generally known in the prior art for many different active ingredients. Common forms of delay include coating delay and matrix delay. Coating delay means that the core of the pharmaceutical composition comprising the active ingredient provides...

AI Technical Summary

Problems solved by technology

[0005] Chinese patent CN104434881A discloses tapentadol hydrochloride sustained-release pellets comprising an enteric-coated layer and an isolation layer, wherein the enteric-coated layer is wrapped on the outside of the isolation layer, but the preparation process of the sustained-release pellets is relatively complicated

However, it needs to be used under the guidance of professional doctors in clinical practice, and it is often accompanied by injection pain during injection, which is inconvenient for patients to use and has poor compliance.

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