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Preparation method for alvimopan capsule

A capsule, polyethylene glycol technology, applied in the directions of capsule delivery, digestive system, active ingredients of heterocyclic compounds, etc., can solve problems such as poor content uniformity, and achieve suitable for large-scale industrial production, good dissolution gradient, and excellent uniformity. Effect

Inactive Publication Date: 2016-07-20
TIANJIN TAIPU PHARMA SCI & TECH DEV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to overcome the shortcomings and shortcomings of poor content uniformity in the preparation process of the existing Alvimopan capsules, and provide a new preparation method for Alvimopan capsules

Method used

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  • Preparation method for alvimopan capsule
  • Preparation method for alvimopan capsule
  • Preparation method for alvimopan capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] prescription:

[0075] Avimopan 12g main medicine

[0076] Monoethanolamine 6g cosolvent

[0077] Polyethylene glycol (3350) 600g dispersion medium

[0078]

[0079] 618g

[0080] Process: Melt polyethylene glycol, lower the temperature to about 70±2℃, add 12g of monoethanolamine, then add the prescription amount of aviemopan raw materials, stir evenly and clarify, reduce the temperature to about 60℃, and fill it into hard Gelatin capsules.

Embodiment 2

[0082] prescription:

[0083] Avimopan 12g main medicine

[0084] Monoethanolamine 24g cosolvent

[0085] Polyethylene glycol (4000) 480g dispersion medium

[0086]

[0087] 516g

[0088] Process: Melt polyethylene glycol, lower the temperature to about 70±2°C, add monoethanolamine, then add the prescription amount of aviemopan raw materials, stir until it is clear, and lower the temperature to about 60°C, then add hard gelatin capsule.

Embodiment 3

[0090] prescription:

[0091] Avimopan 6g main medicine

[0092] Triethanolamine 30g cosolvent

[0093] Polyethylene glycol (6000) 420g dispersion medium

[0094]

[0095] 456g

[0096] Process: Melt polyethylene glycol, lower the temperature to about 70±2°C, add triethanolamine, then add the prescription amount of aviemopan raw material, stir until it is clear, and lower the temperature to about 60°C, then add hard gelatin capsule.

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Abstract

The invention discloses a preparation method for an alvimopan capsule. The preparation method comprises the following steps: melting polyethylene glycol at first, then cooling the molten polyethylene glycol to 60 to 80 DEG C, adding an alvimopan raw material, carrying out uniform mixing under stirring, adding a proper amount of fumaric acid until an alvimopan solid is completely dissolved, and directly filling a capsule with the dissolved alvimopan solid; or carrying out cooling to room temperature for curing, subjecting polyethylene glycol containing alvimopan to crushing and sieving with a low-temperature crusher so as to obtain polyethylene glycol particles of alvimopan and filling a capsule with the particles. A weight ratio of the alvimopan raw material to polyethylene glycol is 1: 5-50; and a weight ratio of the alvimopan raw material to monoethanolamine or triethanolamine is 1: 0.5-5. The preparation method for the alvimopan capsule enables the bioavailability of the alvimopan capsule to be increased to 6%, allows the alvimopan capsule to have excellent uniformity and is more suitable for large-scale industrial production.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method of aviemopan capsules. Background technique [0002] Avimopan is an oral peripheral selective mu-opioid receptor antagonist used to treat gastrointestinal dysfunction, such as irritable bowel syndrome, spontaneous constipation and gastrointestinal side effects caused by opioid analgesia. Avimopan is a water-insoluble drug, and conventional preparations have low bioavailability. According to foreign patent literature reports, Avimopan can be made into three dosage forms: capsules, oral liquids, and freeze-dried powder injections. The foreign marketed products are hard gelatin capsules, in which avitamin is 6mg or 66mg; polyethylene glycol (molecular weight 3350) is 300mg. The preparation method is to melt polyethylene glycol and keep it in a molten state, then add aviemopan into the above-mentioned molten carrier, stir and mix uniformly, and use...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/445A61K47/34A61P1/00A61P1/10
Inventor 张殿镇周世旺赵健马克刘亚梅杨昕
Owner TIANJIN TAIPU PHARMA SCI & TECH DEV
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