Acitretin self-emulsifying transfer system and preparation method thereof

A delivery system, the technology of acitretin, which is applied in the self-emulsifying delivery system of acitretin and its preparation field, can solve the problems of undiscovered acitretin self-emulsifying delivery system in public literature reports, etc., so as to improve the bioavailability, reduce the The effect of small batch differences and reducing individual differences

Active Publication Date: 2015-02-04
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] After searching, no public literature reports o

Method used

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  • Acitretin self-emulsifying transfer system and preparation method thereof
  • Acitretin self-emulsifying transfer system and preparation method thereof
  • Acitretin self-emulsifying transfer system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Prepare raw materials by following parts by weight:

[0033] Avi A 10 servings

[0034] Labrasol 100 parts

[0035] Transcutol 400 servings

[0036] Preparation steps: Take Labrasol and Transcutol and mix them evenly; then add Acitretin to the mixture of Labrasol and Transcutol, heat in a water bath at 65°C, and stir to dissolve Acitretin to obtain the Acitretin self-emulsifying delivery system. Take 0.5g of the acitretin self-emulsifying delivery system and put it in 250mL of 37°C purified water, shake gently, the added acitretin self-emulsifying delivery system will quickly disperse and form an emulsion.

Embodiment 2

[0038] Prepare raw materials by following parts by weight:

[0039] Avi A 10 servings

[0040] Labrasol 500 servings

[0041] Transcutol 50 servings

[0042] Preparation steps: Take Labrasol and Transcutol and mix them evenly; then add Acitretin to the mixture of Labrasol and Transcutol, heat in a water bath at 40°C, and stir to dissolve the Acitretin to obtain the Acitretin self-emulsifying delivery system. Take 0.5g of the acitretin self-emulsifying delivery system and put it in 250mL of 37°C purified water, shake gently, the added acitretin self-emulsifying delivery system will quickly disperse and form an emulsion.

Embodiment 3

[0044] Prepare raw materials by following parts by weight:

[0045] Avi A 10 servings

[0046] Labrasol 500 servings

[0047] Transcutol 400 servings

[0048] Preparation steps: Take Labrasol and Transcutol and mix them evenly; then add Acitretin to the mixture of Labrasol and Transcutol, heat in a water bath at 20°C, and stir to dissolve the Acitretin to obtain the Acitretin self-emulsifying delivery system. Take 0.5g of the acitretin self-emulsifying delivery system and put it in 250mL of 37°C purified water, shake gently, the added acitretin self-emulsifying delivery system will quickly disperse and form an emulsion.

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Abstract

The invention belongs to the field of medicine preparations, and particularly relates to an acitretin self-emulsifying transfer system and a preparation method thereof. The acitretin self-emulsifying transfer system is prepared from the following components in parts by weight: 10 parts of acitretin, 100-500 parts of polyethylene glycol-8-glyceryl caprylate caprate and 50-400 parts of 2(2-ethoxyethoxy)ethanol, or a proper amount of pharmaceutically acceptable solvent. According to the self-emulsifying transfer system, acitretin with low water solubility and low bioavailability is emulsified into emulsion droplets in gastrointestinal fluid after entering gastrointestinal tracts, the absorption rate is improved, and the in-vivo bioavailability can be remarkably improved; the acitretin is dissolved in an oily medium in a molecular state, and is not influenced by crystal form and granularity distribution of the acitretin, the difference among batches can be reduced, and individual difference is reduced; and a brand-new mode is provided to acitretin preparations.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a self-emulsifying delivery system of acitretin and a preparation method thereof. Background technique [0002] Acitretin, Chinese alias: acitretin; 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonan Tetraenoic acid; English name: Etretin, its structural formula is as follows: [0003] [0004] Acitretin belongs to the second generation of retinoic acid and is a metabolite of acitretin ester. It can affect the proliferation and differentiation of cells, regulate the terminal differentiation of epidermal keratinocytes, inhibit the proliferation of lymphocytes, and produce anti-inflammatory and immune regulation effects. , can normalize the proliferation, differentiation and abnormal keratinization of epidermal cells in psoriasis and keratinization diseases. Its adverse reactions are milder than that of acitretin, and it is easy to tolerate. I...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/48A61K31/203A61K47/44A61K47/34A61P17/06A61P17/00
Inventor 程刚兰昌云朱学琳
Owner CHONGQING HUAPONT PHARMA
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