Buprenorphine and its formulations: a comprehensive review.

IF 2 Q3 PSYCHOLOGY, CLINICAL Health Psychology Research Pub Date : 2022-08-20 eCollection Date: 2022-01-01 DOI:10.52965/001c.37517

Salomon Poliwoda, Nazir Noor, Jack S Jenkins, Cain W Stark, Mattie Steib, Jamal Hasoon, Giustino Varrassi, Ivan Urits, Omar Viswanath, Adam M Kaye, Alan D Kaye

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引用次数: 10

Abstract

Buprenorphine, a novel long-acting analgesic, was developed with the intention of two purposes: analgesia and opioid use disorder. Regarding its pharmacodynamics, it is a partial agonist at mu receptors, an inverse agonist at kappa receptors, and an antagonist at delta receptors. For the purpose of analgesia, three formulations of buprenorphine were developed: IV/IM injectable formulation (Buprenex®), transdermal patch formulation (Butrans®), and buccal film formulation (Belbuca®). Related to opioid dependence, the formulations developed were subcutaneous extended release (Sublocade®), subdermal implant (Probuphine®), and sublingual tablets (Subutex®). Lastly, in order to avoid misuse of buprenorphine for opioid dependence, two combination formulations paired with naloxone were developed: film formulation (Suboxone®) and tablet formulation (Zubsolv®). In this review, we present details of each formulation along with their similarities and differences between each other and clinical considerations.

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丁丙诺啡及其制剂综述。

丁丙诺啡是一种新型长效镇痛药，主要用于镇痛和阿片类药物使用障碍。就其药效学而言，它是mu受体的部分激动剂，kappa受体的逆激动剂和delta受体的拮抗剂。为了达到镇痛的目的，我们开发了三种丁丙诺啡制剂:静脉注射制剂(Buprenex®)、透皮贴剂制剂(Butrans®)和口腔膜制剂(Belbuca®)。与阿片类药物依赖相关的制剂有皮下缓释片(Sublocade®)、皮下植入片(Probuphine®)和舌下片剂(Subutex®)。最后，为了避免丁丙诺啡对阿片类药物依赖的滥用，研究人员开发了两种与纳洛酮配对的联合制剂:薄膜制剂(Suboxone®)和片剂制剂(Zubsolv®)。在这篇综述中，我们介绍了每种配方的细节，以及它们之间的异同和临床考虑。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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