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Calcipotriol beta-cyclodextrin inclusion compound and preparation method thereof

A technology of cyclodextrin inclusion compound and calcipotriol, which is applied in the direction of drug combination, pharmaceutical formula, medical preparation of non-active ingredients, etc., can solve acid-base sensitivity, affect product stability, and calcipotriol is easy Degradation and other problems, to achieve the effect of improving the stability of the preparation, improving the stability, and improving the uniformity of the preparation content

Inactive Publication Date: 2014-04-09
JIANGSU SEMPOLL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] On the other hand: Calcipotriol is easy to degrade, especially under high temperature, high humidity, and light conditions, and is extremely sensitive to acid and alkali
The external preparations containing calcipotriol have a rapid decline in the content of the main drug during the shelf life, which affects the stability of the product

Method used

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  • Calcipotriol beta-cyclodextrin inclusion compound and preparation method thereof
  • Calcipotriol beta-cyclodextrin inclusion compound and preparation method thereof
  • Calcipotriol beta-cyclodextrin inclusion compound and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0019] Embodiment 1: the preparation method is as follows

[0020] 1. Prepare 0.3mol / L calcipotriol ethanol solution;

[0021] 2. Preparation of 0.012mol / L β-cyclodextrin aqueous solution

[0022] 3. Add 1 volume of the above ethanol solution of calcipotriol into 15 volumes of the above aqueous solution of β-cyclodextrin, and stir at 30° C. for 2 hours to perform inclusion.

[0023] 4. Cool in an ice-water bath to 0°C, stir for 4 hours, and filter out the solids. After washing with ethanol, dry under reduced pressure at 60°C for 8 hours to obtain the inclusion complex of calcipotriol β-cyclodextrin, which is a white solid.

[0024] The content and related substances of the inclusion compound of calcipotriol β-cyclodextrin were detected, the detection method is as follows, and the detection results are shown in Table 1.

[0025] 1. Calcipotriol content

[0026] Octadecylsilane bonded silica gel was used as filler, acetonitrile-water (50:50) was used as mobile phase, the flo...

Embodiment 2

[0029] Embodiment 2: the preparation method is as follows:

[0030] 1. Prepare 0.3mol / L calcipotriol ethanol solution;

[0031] 2. Preparation of 0.013mol / L β-β-cyclodextrin aqueous solution

[0032] 3. Add 1 volume of the above calcipotriol ethanol solution into 16 volumes of the above β-β-cyclodextrin aqueous solution, and stir at 35° C. for 2 hours for inclusion.

[0033] 4. Cool in an ice-water bath to 0°C, stir for 6 hours, and filter out the solids. After washing with ethanol, dry under reduced pressure at 60°C for 8 hours to obtain the inclusion complex of calcipotriol β-cyclodextrin, which is a white solid.

[0034] The content and related substances of the inclusion complex of calcipotriol β-cyclodextrin were detected, and the detection results are shown in Table 1.

Embodiment 3

[0035] Embodiment 3: the preparation method is as follows:

[0036] 1. Prepare 0.3mol / L calcipotriol ethanol solution;

[0037] 2. Preparation of 0.014mol / L β-cyclodextrin aqueous solution

[0038] 3. Add 1 volume of the above calcipotriol ethanol solution into 17 volumes of the above β-cyclodextrin aqueous solution, and stir at 35° C. for 2 hours to perform inclusion.

[0039] 4. Cool in an ice-water bath to 0°C, stir for 8 hours, and filter out the solids. After washing with ethanol, dry under reduced pressure at 60°C for 8 hours to obtain the inclusion complex of calcipotriol β-cyclodextrin, which is a white solid.

[0040] The content and related substances of the inclusion complex of calcipotriol β-cyclodextrin were detected, and the detection results are shown in Table 1.

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Abstract

The invention relates to a calcipotriol beta-cyclodextrin inclusion compound and a preparation method thereof. The inclusion compound comprises 4.5%-21% of calcipotriol. The preparation method comprises step of adding one volume of 0.3mol / L calcipotriol ethanol solution into 15-20 volumes of 0.012-0.016mol / L beta-cyclodextrin aqueous solution for clathration. The preparation method finally prepares the calcipotriol inclusion compound meeting the requirement of medicines in grain size and uniformity. The inclusion compound can be further prepared into cream, ointment and suspension solution. Compared with non-covered calcipotriol, the calcipotriol beta-cyclodextrin inclusion compound and the preparations prepared from the inclusion compound are remarkably improved in stability, and the problem of uneven content caused by trace feeding capacity is solved.

Description

Technical field: [0001] The present invention relates to β-cyclodextrin inclusion complexes of calcipotriol. The invention also relates to the preparation method of the calcipotriol inclusion compound and its preparation. Background technique: [0002] Calcipotriol is an analog of calcitriol, the active metabolite of vitamin D3 in vivo, which can inhibit the proliferation of keratinocytes and induce their differentiation. Especially suitable for the treatment of psoriasis. [0003] On the one hand: the specification of the marketed preparation is 0.005%. In the preparation process of calcipotriol preparation, due to the extremely low concentration of the specification, it is a trace amount. If it is produced by domestic conventional equipment, the phenomenon of uneven content often occurs. It is urgent to improve the content uniformity through technological means. [0004] On the other hand: Calcipotriol is easy to degrade, especially under high temperature, high humidity...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/593A61P17/06A61P37/08
Inventor 周越强汪亚萍陈玉兰
Owner JIANGSU SEMPOLL PHARMA
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