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Method for modifying dissolution of drospirenone by using grinding and drospirenone solid dispersion

A technology for drospirenone and solid preparations is applied in the field of methods and solid dispersions of drospirenone, and can solve the problems of precipitation crystallization or reduction of drug dissolution and bioavailability, easy aging of solid dispersions, easy occurrence of discoloration, and the like, Achieve the effect of improving bioavailability, facilitating promotion and easy operation

Active Publication Date: 2013-04-17
武汉九珑人福药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, drospirenone is mixed and melted with a carrier to prepare a solid dispersion. The solid dispersion prepared by this method is prone to aging, that is, the solid dispersion is prone to discoloration, increased hardness, crystallization or drug dissolution and bioavailability during storage. degree reduction etc.

Method used

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  • Method for modifying dissolution of drospirenone by using grinding and drospirenone solid dispersion
  • Method for modifying dissolution of drospirenone by using grinding and drospirenone solid dispersion
  • Method for modifying dissolution of drospirenone by using grinding and drospirenone solid dispersion

Examples

Experimental program
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Effect test

Embodiment 1

[0026] (1) Drospirenone is passed through a 100-mesh sieve, and povidone is dried through a 100-mesh sieve for subsequent use;

[0027] (2) Drospirenone 10g and 10g povidone are mixed homogeneously;

[0028] (3) The homogeneously mixed material is fully ground for more than 1 hour with a mortar, and passed through a 100-mesh sieve to obtain a solid dispersion of drospirenone.

Embodiment 2

[0030] (1) Drospirenone is passed through a 100-mesh sieve, polyethylene glycol is dried and sieved, and set aside;

[0031] (2) Drospirenone 10g and 100g polyethylene glycol are mixed homogeneously;

[0032] (3) Grind the homogeneously mixed material with a ball mill for 0.5 h, and pass through a 100-mesh sieve to obtain a solid dispersion of drospirenone.

Embodiment 3

[0034] (1) Drospirenone is passed through a 100-mesh sieve, and the hypromellose is dried and sieved for subsequent use;

[0035] (2) Drospirenone 10g and 20g hypromellose are mixed uniformly;

[0036] (3) The homogeneously mixed material was ball-milled for 0.5 h in a ball mill at 80 r / min, and passed through a 100-mesh sieve to obtain a solid dispersion of drospirenone.

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Abstract

The invention belongs to the scientific field of pharmaceutic preparations, and in particular relates to a method for modifying dissolution of drospirenone by using grinding and drospirenone solid dispersion. The method comprises the following steps: (1) the drospirenone and hydrophilic non-polymer accessories or water soluble accessories are evenly mixed by the mass ratio of 1:(1-1):30; and (2) the evenly mixed materials are fully grinded or milled, and are screened. The method has the advantages of simple operation, low cost, simplicity, practicability and convenience in promotion; the preparation produced by drospirenone dispersion which is prepared by the method is quickly dissolved out; 80 percent of drospirenone can be furthest dissolved out in 10 minutes; and 98 percent of drospirenone can be furthest dissolved out in 20 minutes; the drospirenone is quickly dissolved out; the biological utilization rate is high; no organic solvent is remained; the stability is high; and the method is suitable for preparing solid preparation.

Description

technical field [0001] The invention belongs to the scientific field of pharmaceutical preparations, and in particular relates to a method for improving the dissolution of drospirenone by grinding and a solid dispersion of drospirenone. Background technique [0002] Drospirenone is a progestin commonly used in combined oral contraceptives. Drospirenone is a substance that is slightly soluble in water and aqueous buffers of various pH values; and has poor chemical stability under acidic conditions, including the acidic environment in the stomach, and will rearrange into inactive isomers. It will be hydrolyzed under aggressive conditions. Therefore, under normal circumstances, its dissolution in vitro is not good, and its bioavailability in vivo is not high. Providing drospirenone in a rapidly dissolving form will greatly increase the bioavailability of drospirenone. [0003] For example, in patent 200580015063.3, drospirenone is dispersed in amorphous silicon dioxide. Pat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/585A61K47/38A61K47/34A61K47/32A61K47/26A61K47/10A61P15/18
Inventor 张阳洋成忠煌梁群芳
Owner 武汉九珑人福药业有限责任公司
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