Dutasteride self-microemulsion freeze-dried composition and preparation method thereof

A dutasteride, self-microemulsion technology, used in freeze-dried delivery, drug combination, pharmaceutical formulations, etc.

Active Publication Date: 2014-11-19
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention provides a kind of dutasteride self-microemulsion freeze-dried composition, and this freeze-dried composition solves the dissolution difficulty of dutasteride, Problems such as low bioavailability, narrow application range of preparations, difficulty in industrialization of solid preparations, etc.

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～22

[0087] Self-microemulsion composition

[0088] prescription:

[0089]

[0090] Preparation Process:

[0091] The aforementioned dutasteride self-microemulsion can be prepared by the following process.

[0092] Preparation of self-microemulsion: Accurately weigh the prescribed amount of dutasteride, add the prescribed amount of oil phase, dissolve it in a water bath at 40-50°C, add emulsifier and co-emulsifier according to the prescribed amount, and stir evenly to obtain dutasteride self-microemulsion milk.

Embodiment 23～44

[0094] Self-microemulsion freeze-dried product

[0095] prescription:

[0096]

[0097] Preparation of self-microemulsion lyophilized powder:

[0098] Disperse the freeze-dried excipient in purified water, and keep stirring until the excipient is completely dissolved; then add dutasteride self-microemulsion, and stir for 10 minutes to obtain an O / W type microemulsion, pour the microemulsion into cillin freeze-dried in bottles.

[0099]

[0100] Dutasteride self-microemulsion freeze-dried product results:

[0101]

[0102] The freeze-dried powders obtained from the above prescriptions are all in the form of powders, and clear and transparent liquids can be obtained after reconstitution.

Embodiment 45

[0103] Example 45 Solid Oral Capsules

[0104] Prescription Composition:

[0105] Dutasteride self-microemulsion freeze-dried product (derived from Example 26) 29g (containing 14.5mg of dutasteride)

[0106] Starch 29g

[0107] Preparation method: 29 g of soluble starch, add the lyophilized product of dutasteride self-microemulsion (29 g (containing 14.5 mg of dutasteride)) in Example 26 under stirring, mix well, and add 0.5 mg of dutasteride per grain Capsules were packed, and 29 solid oral capsules were prepared in total.

[0108] Example 45 A solid oral capsule (as a comparative example of Example 45)

[0109] Prescription Composition:

[0110] Dutasteride self-microemulsion (derived from Example 4) 29g (containing 14.5mg of dutasteride)

[0111] Starch 58g

[0112] Preparation method: 58g of starch, add the dutasteride self-microemulsion (29g (containing 14.5mg of dutasteride)) of Example 4 under stirring, after mixing, pack the capsules according to the content of 0...

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Abstract

The invention discloses a dutasteride self-microemulsion freeze-dried composition and a preparation method thereof. The dutasteride self-microemulsion freeze-dried composition disclosed by the invention comprises dutasteride self-microemulsion and a freeze-dried excipient in the weight ratio of (0.5-2):1, wherein the dutasteride self-microemulsion is mainly composed of the following components in percentage by weight: 0.05-0.3% of dutasteride, 5-75% of oil phase, 20-60% of emulsifier, and 4-50% of co-emulsifier. The dutasteride self-microemulsion freeze-dried composition disclosed by the invention is more suitable for preparing dutasteride solid preparations and is capable of increasing the bioavailability of dutasteride.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a dutasteride self-microemulsion freeze-dried composition, a preparation method thereof, and an oral solid preparation containing the freeze-dried composition. Background technique [0002] Chemical name of dutasteride: (5α,17β)-(2,5-bis(trifluoromethyl)phenyl)-3-oxo-4-aza-androst-1-ene-17-carboxamide , its chemical structure is: [0003] [0004] Dutasteride is the second-generation 5α-reductase inhibitor, researched and developed by Glaxo, and approved by the U.S. Food and Drug Administration (FDA) on October 10, 2002 for listing in the U.S., under the trade name Avodart, in the European market 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 type I and type II 5α reductase. The ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/58A61P13/08A61P17/14A61P17/08
Inventor 张涛刘翠丁彦吉王立
Owner CHONGQING PHARMA RES INST
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