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Improved medicinal compositions comprising buprenorphine and naltrexone

A composition and technology of naltrexone, applied in the field of medicinal compositions of buprenorphine, can solve problems such as limited effect

Inactive Publication Date: 2010-01-06
RB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, buprenorphine suffers from the side effects typical of opioid agonists, such as nausea and vomiting, constipation, and respiratory depression in some patients, although it has limited effect on respiratory depression as a direct consequence of its partial agonist properties

Method used

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  • Improved medicinal compositions comprising buprenorphine and naltrexone
  • Improved medicinal compositions comprising buprenorphine and naltrexone
  • Improved medicinal compositions comprising buprenorphine and naltrexone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Four healthy Caucasian participants (2 males and 2 females) aged 21 to 33 years (mean ± SEM, 26.0 ± 5.3 years) participated in the study. The mean body weight was 74 kg (± 13.3, range 57-89 kg), and the mean CPTOL at screening was 30.7 seconds (± 6.9, range 25-39 seconds). There were no significant differences between males and females with respect to age (p=0.782) or screened CPTOL (p=0.792).

[0079] Subjects were administered buprenorphine and naltrexone in a 100:1 ratio by IV infusion at a dose of 0.5 μg / kg body weight of buprenorphine. Perform a 4-hour clearing surveillance. CPTOL results such as figure 1 shown in . No adverse reactions of interest were found.

Embodiment 2

[0080] Example 2 - Comparison

[0081] As a comparative example, the same subjects in Example 1 were administered buprenorphine and saline by IV infusion on a separate day (hereinafter referred to as "administration of BUP only"). Buprenorphine was still administered at a dose of 0.5 μg / kg body weight and monitored for clearance for 4 hours. CPTOL results such as figure 1 shown in .

Embodiment 3

[0083] On a separate day, the same subjects in Example 1 were administered buprenorphine and naltrexone in a ratio of 133:1 by IV infusion at a dose of 0.5 μg / kg body weight of buprenorphine . A 4-hour clearance surveillance was performed. CPTOL results such as figure 1 shown in . No adverse reactions of interest were found.

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Abstract

An analgesic composition, in parenteral unit dosage form or in a unit dosage form suitable for delivery via the dermis or mucosa, comprises buprenorphine and an amount of naltrexone such that the ratio by weight of buprenorphine to naltrexone delivered to or reaching the plasma of a patient is in the range 100:1 to 5000:1. The analgesic action of the buprenorphine is potentiated by the low dose of naltrexone. Also provided are a method of treatment of pain and the use of buprenorphine and naltrexone for the manufacture of a medicament.

Description

technical field [0001] The present invention relates to a pharmaceutical composition containing buprenorphine in combination with naltrexone; and to the use of buprenorphine and naltrexone in the manufacture of said composition and in clinical practice as analgesics application. Background technique [0002] Although opioids are particularly effective in the management of moderate to severe pain, their use is limited by uncomfortable and potentially dangerous adverse effects. These adverse effects can include sedation, respiratory depression, nausea, and gastrointestinal problems. Therefore, efforts have been made to reduce adverse effects. [0003] There are many opioids, some of which produce more pronounced adverse effects than others. Thus, careful selection of the opioid used in the analgesic composition can itself reduce the incidence and severity of adverse reactions. A particularly suitable opioid is buprenorphine, which has been shown to possess both agonist (mo...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61P25/04
CPCA61K45/06A61K31/485A61P25/04A61P29/00A61P43/00A61K2300/00
Inventor 克利斯托弗·波恩·夏普利奥尼尔·海德
Owner RB PHARMA