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Bexarotene soft capsule and preparation method thereof

A technology of soft capsules and soft capsule shells, applied in the field of medicine, can solve the problems of poor dosage uniformity, difficulty in removing oxygen, poor fluidity, etc., and achieve the effect of simple production process

Active Publication Date: 2018-08-24
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) Content 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 pour in Add bexarotene and stir evenly to obtain a mixed liquid medicine. Next, keep the mixed medicinal solution at 30-35 degrees Celsius, and then press it with the glue solution (composed of gelatin, glycerin, sorbitol, water and titanium dioxide) on a soft capsule machine, and obtain bexarotene soft capsule after drying, polishing and packaging. 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 to 40-45 degrees Celsius after dissolving, and then pour in Add the bexarotene and mix well. Keep the mixed medicinal liquid at 30-35 degrees Celsius, and then press it with the glue (composed of gelatin, glycerin, sorbitol, water and titanium dioxide) on a soft capsule machine, and obtain bexarotene soft capsules after drying, polishing and packaging . 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 to 40-45 degrees Celsius after dissolving, and then pour in Add the bexarotene and mix well. Keep the mixed medicinal liquid at 30-35 degrees Celsius, and then press it with the glue (composed of gelatin, glycerin, sorbitol, water and titanium dioxide) on a soft capsule machine, and obtain bexarotene soft capsules after drying, polishing and packaging . The production process data are shown in Table 1.

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Abstract

The invention discloses a bexarotene soft capsule and a preparation method thereof, wherein the bexarotene soft capsule comprises a content and a soft capsule shell, and the content comprises bexarotene, low molecular weight polyethylene glycol, high molecular weight polyethylene glycol and polysorbate. According to the present invention, the bexarotene soft capsule based on the formula can avoidthe drug degradation problem caused by the high temperature heat release and the difficult degassing in the preparation of the bexarotene soft capsule in the case of the maintaining of the unchanged release characteristic of the drug in the prior art.

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 Applications(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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