Dutasteride self-microemulsion composition and preparation method thereof

A technology of dutasteride and composition, applied in the field of pharmaceutical preparations, can solve problems such as being unfavorable to control the particle size of emulsion droplets, complicated preparation process, etc., and achieve the effects of improving dissolution rate and simple preparation process

Inactive Publication Date: 2014-03-26
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This prescription is not conducive to controlling the particle size of milk droplets, which limits the improvement of the dissolution rate of dutasteride. The dissolution rate in the dissolution solution with surfactant is equivalent to that of Avodart on the market, and the preparation process is complicated.

Method used

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  • Dutasteride self-microemulsion composition and preparation method thereof
  • Dutasteride self-microemulsion composition and preparation method thereof
  • Dutasteride self-microemulsion composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Example 1-30 Self-microemulsion composition

[0072]

[0073]

[0074] The above-mentioned dutasteride self-microemulsion capsules (containing 0.5 mg of dutasteride / capsule) can be prepared by the following process:

[0075] Process Ⅰ: Accurately weigh the prescribed amount of dutasteride, add the prescribed amount of co-emulsifier, dissolve it in a water bath at 40°C, add the oil phase and emulsifier according to the prescribed amount, stir evenly to obtain dutasteride self-microemulsion, pour it into Dutasteride self-microemulsion hard capsules were obtained by filling them in hard capsules.

[0076] Process Ⅱ: Accurately weigh the prescription amount of oil phase, emulsifier and co-emulsifier, stir evenly to prepare a blank self-microemulsion concentrate, then weigh the prescription amount of dutasteride, stir to dissolve and mix evenly to obtain dutasteride Dutasteride hard capsules are prepared by self-microemulsion filling in hard capsules.

[0077] Pr...

Embodiment 31

[0079] Example 31 Solid Oral Capsules

[0080] prescription

Embodiment 19

[0081] Dutasteride self-microemulsion 7g of Example 19 (containing 21mg of dutasteride)

[0082] Soluble starch 35g

[0083] Preparation method: 35 g of soluble starch was added to 7 g of dutasteride self-microemulsion (containing 21 mg of dutasteride) of Example 19 under stirring, and after mixing, capsules were filled according to the content, and a total of 42 solid oral capsules were prepared.

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Abstract

The invention relates to a self-microemulsion dutasteride orally-taken preparation and a preparation method thereof. The self-microemulsion composition comprises the following components in percent by weight: 0.05%-0.3% of dutasteride, 5%-75% of oil, 20%-60% of an emulsifier and 4%-50% of a co-emulsifier. After being cured, the self-microemulsion auxiliary materials can be prepared into preparations such as tablets or capsules; after being quickly disintegrated in a stomach, the preparation can be form emulsion drops with average grain size of 10 nm-100 nm in a gastrointestinal tract after being self-microemulsified, so that solubility and dissolution rate of the dutasteride can be improved, and absorption of the dutasteride in the gastrointestinal tract can be promoted.

Description

[0001] technical field [0002] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a dutasteride self-microemulsion composition and oral preparations thereof. The composition comprises 0.05%-0.3% of dutasteride, 5%-75% of oil, emulsified Agent 20%-60%, co-emulsifier 4%-50%, the average particle size of the emulsion droplet is 10-100nm. technical background [0003] Chemical name of dutasteride: (5α,17β)-(2,5-bis(trifluoromethyl)phenyl)-3-oxo-4-aza-androst-1-ene-17-carboxamide , its chemical structure is: [0004] [0005] Dutasteride is the second generation of 5α-reductase inhibitors, researched and developed by Glaxo, and was approved by the U.S. Food and Drug Administration (FDA) on October 10, 2002. The product name is Avolve. Clinically, it is mainly used for the treatment of prostatic hypertrophy, male alopecia, seborrheic alopecia, and hereditary alopecia. It is the first and only drug that simultaneously inhibits typ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/20A61K9/48A61K31/58A61P13/08A61P17/14
Inventor 张涛丁彦吉刘翠王海屿邓杰
Owner CHONGQING PHARMA RES INST
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