Dutasteride self-microemulsion composition and preparation method thereof

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...

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.

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