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Pharmaceutical composition containing difluprednate and preparation method thereof

The technology of a kind of difluprednate and composition is applied in the field of pharmaceutical composition containing difluprednate and its preparation, which can solve the problems of poor cloth delivery, poor compliance, increased side effects, etc., and achieve uniform drug distribution, foreign matter The effect of reducing sensation and reducing side effects

Inactive Publication Date: 2016-01-06
广州仁恒医药科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Yet when adopting this suspending agent technology to prepare difluprednate ophthalmic suspension, it is found that due to being limited by the existing micropowder technology, the average particle diameter of active ingredient micropowder in the suspension is only about 1-10 μ m, in There are foreign body sensation and granule sensation during use, and compliance is poor, in addition, when adopting suspension, the transfusion (intraocular transfusion) of the difluprednate of the preparation that obtains enters anterior chamber is relatively poor, thereby causes the infusion of medicine Bioavailability, in order to achieve the same efficacy, higher drug concentrations will have to be used, thus increasing the possibility of side effects

Method used

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  • Pharmaceutical composition containing difluprednate and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Purified water was heated to about 75°C, and glycerin, disodium edetate, sodium acetate, boric acid and sorbic acid were dissolved to obtain an aqueous phase. In addition, castor oil and poloxamer 407 were mixed and heated to about 75° C., and difluprednate was added to dissolve to obtain an oil phase. Then use a high-speed shearer to stir the water phase while slowly adding the oil phase to obtain colostrum, and adjust the pH to 5.5 after constant volume. The colostrum is processed by a high-pressure homogenizer, and then sterilized by moist heat to obtain an emulsion.

[0035] The particle size distribution table of difluprednate ophthalmic emulsion before the present embodiment is sterilized

[0036] particle size

Embodiment 2

100mL

[0040] Purified water was heated to about 75°C, and glycerin, disodium edetate, sodium acetate, boric acid and sorbic acid were dissolved to obtain an aqueous phase. In addition, soybean oil and egg yolk lecithin are mixed and heated to about 75° C., and difluprednate is added to dissolve to obtain an oil phase. Then use a high-speed shearer to stir the water phase while slowly adding the oil phase to obtain colostrum, and adjust the pH to 5.5 after constant volume. The colostrum is processed by a high-pressure homogenizer, and then sterilized by moist heat to obtain an emulsion.

[0041] The particle size distribution table of difluprednate ophthalmic emulsion after the present embodiment is sterilized

[0042] particle size

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Abstract

The invention discloses a pharmaceutical composition containing difluprednate. The pharmaceutical composition is O / W emulsion and contains the active components of the difluprednate, one or more kinds of oil and one or more kinds of emulsion, auxiliary materials and water which serves as solvent, and the difluprednate is dissolved in the oil and / or the emulsion, wherein the pharmaceutical composition is prepared from, 0.01%-0.1% of the difluprednate, 1%-20% of the oil, 0.01%-10% of the emulsion and the balance water and auxiliary materials. In addition, the invention further provides a preparation method of the pharmaceutical composition containing the difluprednate. Compared with the prior art, according to the pharmaceutical composition containing the difluprednate and the preparation method thereof, the pharmaceutical composition is the emulsion, the average grain diameter of oil drops of the difluprednate emulsion is smaller than one micron, the pharmaceutical composition can be subjected to moist heat sterilization, grain size variation is not large after sterilization is conducted, and the grain size does not increase after long-term storage.

Description

technical field [0001] The invention relates to the field of pharmaceutical compositions, in particular to a pharmaceutical composition containing difluprednate and a preparation method thereof. Background technique [0002] Difluprednate is a steroidal corticosteroid that suppresses inflammatory and allergic skin reactions and also suppresses reactions associated with accelerated cell regeneration leading to symptoms such as erythema, edema, thickened skin, and rough skin surface , and relieve itching, burning, and pain. Due to the introduction of 17-butyrate and 21-acetate in the molecule, the fat solubility of difluprednate is better, so that better curative effect can be achieved during external treatment. The existing external preparations are mainly 0.05% difluprednate. Fluprednate ointment and cream (trade name: MYSER, produced by Japan Tanabe Mitsubishi Pharmaceutical Co., Ltd.). [0003] Difluprednate Ophthalmic Emulsion is a glucocorticoid receptor agonist develo...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/573A61P29/00A61P37/08A61P27/02
Inventor 田元
Owner 广州仁恒医药科技股份有限公司
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