Solid composition for improving content uniformity and dissolution rate of imidafenacin

A solid composition, a new technology of midana, applied in the field of pharmacy, can solve problems such as complex preparation process, unqualified content uniformity, and small specifications of the main drug

Inactive Publication Date: 2012-07-18
BEIJING D VENTUREPHARM TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Midanacin is almost insoluble in water, and the main drug is small in size. Traditional prescription technology may have low bioavailability and unqualified content uniformity. Currently, researchers may use surfactants such as sodium lauryl sulfate Solubilization, polyethylene glycol 4000 or 6000 and other methods to prepare solid dispersions to solve this problem, but there are still problems of poor stability and complicated preparation process

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1: the preparation of Midanaxin Tablets (in every 1000 tablets)

[0016] Material name Weight ratio (%) Midana 0.07 Pregelatinized starch (filler) 67.70 Hydroxypropyl cellulose (solvent) 3.00 Microcrystalline Cellulose (Filler, Disintegrant) 28.43 povidone (adhesive) 0.30 Magnesium stearate 0.50

[0017] Preparation process: Air-micronize midanacin and pregelatinized starch at a ratio of 1:10, the average particle size is 2.5um, microcrystalline cellulose passes through an 80-mesh sieve, and set aside; the prescription amount of midanacin Co-powder with pregelatinized starch, the remaining amount of pregelatinized starch, hydroxypropyl cellulose, and internally added microcrystalline cellulose are placed in a fast stirring granulator, and mixed evenly according to the principle of equal addition; start stirring, add 10 % povidone aqueous solution granulation, 18-mesh sieve granulation; ventilated drying at ...

Embodiment 2

[0029] Embodiment 2: Preparation of Midanaxin Tablets (measured per 1000 tablets)

[0030] Material name Weight ratio (%) Midana 0.05 Lactose (filler) 68.25 Hydroxypropyl cellulose (solvent) 5.00 Microcrystalline Cellulose (Filler, Disintegrant) 25.95 Hydroxypropyl Cellulose (Binder) 0.25 Magnesium Stearate (Lubricant) 0.50

[0031] Preparation process: Airflow pulverize midanacine and lactose at a ratio of 1:10, pass microcrystalline cellulose through an 80-mesh sieve, and set aside; co-powder the prescribed amount of midanacin and lactose, the remaining amount of lactose, hydroxyl Propyl cellulose and internally added microcrystalline cellulose are placed in a fast-stirring granulator, and mixed uniformly according to the principle of equal volume addition; start stirring, add 2% hydroxypropyl cellulose aqueous solution to granulate, and granulate through a 18-mesh sieve; Ventilated and dried at 50°C, the water content of...

Embodiment 2 and comparative Embodiment 2

[0039] Example 2 and comparative example 2 content uniformity inspection results (n=10):

[0040] time (min) Example 2 Comparative Example 2 1 100.6 89.7 2 101.4 99.5 3 99.3 109.8 4 98.7 94.7 5 105.4 89.7 6 103.9 100.2 7 100.4 99.5 8 99.7 100.6 9 100.1 100.4 10 97.9 94.9 Average content (%) 100.7 97.9 A 0.70 -2.10 S 2.31 5.96 A+1.80S 4.86 8.63

[0041] Table 4

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PUM

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Abstract

The invention relates to a solid composition containing imidafenacin. The solid composition can improve the dissolubility and content uniformity of main medicines effectively.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a solid composition for improving content uniformity and promoting the dissolution of midanacine. Background technique [0002] Midanacin (4-(2-methyl-1-imidazolyl)-2,2-diphenylbutyramide) is a compound with muscarinic receptor M3 and M1 antagonism, which is used as an overactive bladder Drugs for the treatment of activity disorders. [0003] Overactive bladder (symptomatic overactive lbadder, OAB) is a common chronic lower urinary tract dysfunction, which is defined by the International Anti-Urinary Incontinence Society (ICS) syndrome characterized by urinary incontinence and urge incontinence. Kyorin Corporation's overactive bladder drug "midanacin" received its first global positive approval recommendation in Japan in June 2007, and the anticholinergic side effects of this oral muscarinic M1 / M3 antagonist have been significantly improved , is an excellent drug ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/42A61K9/48A61K9/00A61K31/4174A61K47/36A61K47/38A61P13/10
Inventor 肖博郭夏宋雪梅
Owner BEIJING D VENTUREPHARM TECH DEV
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