Bexarotene soft capsule and preparation method thereof

A soft capsule and soft capsule shell technology, applied in the field of medicine, can solve the problems of poor fluidity, heat generation, long mixing time, etc.

Active Publication Date: 2021-05-11
HUMANWELL PURACAP PHARM WUHAN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, the viscosity of the drug formula is greater than 5000cp, and bexarotene is a poorly soluble drug, which needs to be dispersed evenly in the formula without agglomeration. During the production process, due to the high viscosity of the formula, it takes a long time to mix, and it will generate heat when mixing the ingredients , the temperature can reach above 80 degrees Celsius, and the molecular structure of bexarotene contains carboxyl groups, and it is easy to chemically react with a large number of hydroxyl groups in polyethylene glycol 400 molecules at high temperatures; at the same time, a large number of bubbles will be generated when stirring, due to the viscosity of the formula If it is too large, it is difficult to remove the oxygen contained in it, which will cause the degradation of the drug; and because the viscosity of the formula is too high and the fluidity is poor, it will lead to poor dosage uniformity when filling capsules

Method used

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  • Bexarotene soft capsule and preparation method thereof
  • Bexarotene soft capsule and preparation method thereof
  • Bexarotene soft capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] (1) Contents composition: bexarotene 75g (D90 less than 20 microns), polyethylene glycol 400 450g, polyethylene glycol 2000 75g, polysorbate 20 60g.

[0059] (2) Preparation method: first heat polyethylene glycol 400 to 60-80 degrees Celsius, then add polyethylene glycol 2000 and polysorbate 20 to it, stir, cool to 40-45 degrees Celsius after dissolving, and then add Bexarotene was added and stirred evenly to obtain a mixed medicinal liquid. Next, the mixed medicinal liquid is kept at 30-35 degrees Celsius, and then pressed with a glue liquid (composed of gelatin, glycerol, sorbitol, water and titanium dioxide) on a soft capsule machine, dried, polished and packaged to obtain bexarotene soft capsules. capsule. The production process data are shown in Table 1.

Embodiment 2

[0061] (1) Content composition: bexarotene 75g (D90 less than 20 microns), polyethylene glycol 600-600g, polyethylene glycol 1000-75g, polysorbate 40-45g.

[0062] (2) Preparation method: first heat polyethylene glycol 600 to 60-80 degrees Celsius, then add polyethylene glycol 1000 and polysorbate 40 to it, stir, cool down to 40-45 degrees Celsius after dissolving, and then put inside Add Bexarotene and mix well. The mixed medicinal liquid is kept at 30-35 degrees Celsius, and then compressed on a soft capsule machine with a glue liquid (composed of gelatin, glycerol, sorbitol, water and titanium dioxide), dried, polished and packaged to obtain bexarotene soft capsules . The production process data are shown in Table 1.

Embodiment 3

[0064] (1) Content composition: Bexarotene 75g (D90 less than 20 microns), polyethylene glycol 400 300g, polyethylene glycol 1000 37.5g, polysorbate 40 75g.

[0065] (2) Preparation method: first heat polyethylene glycol 400 to 60-80 degrees Celsius, then add polyethylene glycol 1000 and polysorbate 40 to it, stir, cool down to 40-45 degrees Celsius after dissolving, and then put inside Add Bexarotene and mix well. The mixed medicinal liquid is kept at 30-35 degrees Celsius, and then compressed on a soft capsule machine with a glue liquid (composed of gelatin, glycerol, sorbitol, water and titanium dioxide), dried, polished and packaged to obtain bexarotene soft capsules . The production process data are shown in Table 1.

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PUM

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Abstract

The invention discloses a bexarotene soft capsule and a preparation method thereof. The bexarotene soft capsule comprises: contents and a soft capsule shell, wherein the contents include bexarotene, low molecular weight polyethylene Glycols, high molecular weight polyethylene glycols, and polysorbates. The bexarotene soft capsules composed of this formula can avoid drug degradation caused by high temperature exothermic and difficult degassing during the preparation of bexarotene soft capsules in the prior art while maintaining its drug release characteristics question.

Description

technical field [0001] The invention belongs to the field of medicine, in particular, the invention relates to bexarotene soft capsules and a preparation method thereof. Background technique [0002] Bexarotene, chemical name: 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthyl)vinyl] Benzoic acid, molecular formula: C 24 h 28 o 2 ; Molecular weight: 348.478; Chemical structural formula is as follows: [0003] [0004] Bexarotene is white to off-white crystalline powder; almost insoluble in water, slightly soluble in methanol, easily soluble in acetonitrile and dimethyl sulfoxide. Slightly hygroscopic. For the treatment of refractory and non-refractory cutaneous T-cell lymphoma (CTCL). This product can selectively activate retinoid X receptor subtypes (RXRα, RXRβ, RXRγ). RXR can form heterodimers with various receptors such as retinoic acid receptor (RAR), vitamin D receptor, thyroxine receptor, and peroxisome proliferator-activated receptor (PPAR)]. Once ac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/48A61K31/192A61K47/10A61K47/26A61P35/00
CPCA61K9/4866A61K31/192A61P35/00A61K9/4833A61K9/4825A61K47/26A61K47/02A61K47/10
Inventor 沈福星刘波丁超张九春
Owner HUMANWELL PURACAP PHARM WUHAN CO LTD
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