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Preparation method of micro-particle-size tadalafil

A technology of tadalafil and microparticles, which is applied in the field of preparation of micro-particle tadalafil, can solve the problems of large energy, complex process, large energy consumption, etc., and achieves small particle size distribution, simple production process, and high yield high rate effect

Inactive Publication Date: 2017-06-13
NANJING ZENKOM PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This technology adopts solid dispersion technology, which can make tadalafil exist in the carrier in the form of solid solution, and then pulverize it to achieve tadalafil with fine particle size, but the process is complicated and consumes a lot Energy and not conducive to industrial production
The traditional micronization system uses a jet mill for pulverization. During the pulverization process, the loss of raw materials, high noise, high energy consumption, and large dust are the defects of the micronization technology.

Method used

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  • Preparation method of micro-particle-size tadalafil
  • Preparation method of micro-particle-size tadalafil
  • Preparation method of micro-particle-size tadalafil

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Take 10g of tadalafil with a D90 of 64.53μm, dissolve it in 10g of dimethyl sulfoxide, stir until clear, and slowly add 5g of water under stirring (propelled stirring 50rpm), stir for 10min, centrifuge, and use 5g of Washed with water three times, and air-dried to obtain 5.37 g of tadalafil with a particle size of 53.7%. As measured by a Malvern particle size analyzer, the particle size D90 of tadalafil was 21.47 μm.

Embodiment 2

[0035]Take 10 g of tadalafil with a D90 of 64.53 μm, dissolve it in 10 g of dimethyl sulfoxide, stir until clear, and slowly add 10 g of water under stirring (propelled stirring 200 rpm), stir for 10 min, centrifuge, and use 5 g of Washed with water three times, and air-dried to obtain 6.48 g of tadalafil with a particle size of 64.8%. As determined by a Malvern particle size analyzer, the particle size D90 of tadalafil was 18.14 μm.

Embodiment 3

[0037] Take 10g of tadalafil with a D90 of 64.53μm, dissolve it in 10g of dimethyl sulfoxide, stir until it becomes clear, slowly add it into 50g of water under stirring (propulsion stirring 500rpm), stir for 10min, centrifuge, and use 5g of Washed with water three times, and air-dried to obtain 8.61 g of tadalafil with a particle size of 86.1%. . As measured by a Malvern particle size analyzer, the particle size D90 of tadalafil was 14.67 μm.

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Abstract

The invention belongs to the new technical field of drug manufacturing, and particularly relates to a preparation method of micro-particle-size tadalafil. A phase conversion method is adopted to prepare tadalafil of 0.6-25um in particle size. The preparation method includes following steps: dissolving tadalafil in organic solvent; slowly adding water while being stirred; separating solid to obtain micro-particle-size tadalafil, wherein the organic solvent is one or multiple of dimethyl sulfoxide or acetone. By the preparation method, the technical defects of low micro-particle-size smashing efficiency and great loss of tadalafil are overcome.

Description

technical field [0001] The invention belongs to the field of new technology for medicine manufacture, and relates to a method for preparing tadalafil with microparticle size. Background technique [0002] Tadalafil is a selective, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase 5 (PDE5) for the treatment of erectile dysfunction in men. Chemical name: 6-(1,3-benzodioxolan-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl, (6R,12aR)-pyridine Azino[1'2':1,6]pyrido[3,4-b]indole-1,4-dione. [0003] [0004] Tadalafil is a selective and reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase 5 (PDE5). When sexual stimulation results in the local release of nitric oxide, PDE5 is inhibited by tadalafil, resulting in increased cGMP levels in the corpus cavernosum. This causes the smooth muscles to relax and blood to flow into the penile tissue, producing an erection. Tadalafil has no effect if there is no sexual s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/16A61K31/4985A61P15/10
CPCA61K9/14A61K9/16A61K31/4985
Inventor 徐卓业祁艳
Owner NANJING ZENKOM PHARMA
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