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Injectable medical composition containing butorphinol and preparation method of injectable medical composition

A technology for butorphanol and a composition is applied in the field of pharmaceutical preparations, which can solve problems such as poor patient compliance, and achieve the effects of reducing the frequency of administration, reducing the volume of administration, and improving compliance

Inactive Publication Date: 2020-11-10
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Both injection and nasal spray need to be administered repeatedly at an interval of about 3-4 hours to maintain the analgesic effect. The administration frequency of the two dosage forms is relatively high, and the patient's compliance is poor. Therefore, regarding the administration frequency The development of new sustained-release dosage forms of butorphanol tartrate is very necessary

Method used

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  • Injectable medical composition containing butorphinol and preparation method of injectable medical composition
  • Injectable medical composition containing butorphinol and preparation method of injectable medical composition
  • Injectable medical composition containing butorphinol and preparation method of injectable medical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1, butorphanol free base long-acting injection prescription and rat pharmacokinetic experimental results

[0054] For butorphanol injection containing ethanol, polyethylene glycol 400, lecithin, and medium-chain triglycerides, the specific prescription composition and dosage are as follows:

[0055] Table 1 Prescription composition and dosage

[0056]

[0057] Preparation:

[0058] 1) Butorphanol free base and lecithin of recipe quantity are dissolved in ethanol;

[0059] 2) Add the prescription amount of polyethylene glycol 400 into the above system, and mix well;

[0060] 3) Add medium-chain triglycerides to the above system and adjust the volume to the target volume, and mix evenly;

[0061] 4) Filter the medicinal solution through a 0.2 μm PTFE membrane;

[0062] 5) Fill the filtered medicinal solution into 2ml vials, 0.95ml / bottle, and crimp the cap to seal.

[0063] This prescription was carried out pharmacokinetic experiment in rats, and the te...

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Abstract

The present disclosure relates to an injectable medical composition comprising butorphinol and a preparation method of the injectable medical composition. Specifically, the medical composition disclosed by the invention comprises butorphinol free alkali or a medical salt thereof, amphiphilic lipid, triglyceride and a biocompatible solvent. The medical composition provided by the invention is suitable for intramuscular injection and subcutaneous injection, is small in irritation and has the clinical advantage of long-acting slow release.

Description

technical field [0001] The present disclosure relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing butorphanol suitable for intramuscular injection or subcutaneous injection and a preparation method thereof. Background technique [0002] Butorphanol tartrate is a synthetic morphinan analgesic that acts as a mixed opioid receptor agonist-antagonist with narcotic antagonism and is very effective in the treatment of chronic and acute pain. This product and its main metabolite butorphanol stimulate κ-opioid receptors, and have dual effects on μ-receptors. It mainly interacts with these receptors in the central nervous system (CNS) to exert its pharmacological effects including analgesic effects. The analgesic potency of butorphanol is 5-8 times that of morphine, but the respiratory depression is only 1 / 5 of that of morphine. Because it mainly stimulates the κ receptor and has a partial antagonistic effect on the μ recepto...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/485A61K47/14A61P25/04
CPCA61K31/485A61K9/0019A61K47/14A61P25/04
Inventor 柴夫娟孙琼许大平李康健齐晓雪邱振均刘凯
Owner JIANGSU HENGRUI MEDICINE CO LTD