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Difluprednate Topical Preparations

A technology for difluprednate and preparations, which is applied in the field of difluprednate topical preparations, can solve problems such as affecting the bioavailability of the drug, affecting the curative effect, etc., so as to avoid the decline of transdermal absorption characteristics, avoid curative effects, and avoid particles the effect of getting bigger

Active Publication Date: 2016-01-20
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a result, the particle size of the drug micropowder becomes larger. Although the current drug standards do not provide for the situation of creams, our experiments have found that the increase in the particle size of the drug micropowder directly affects the bioavailability of the drug and thus affects the curative effect.

Method used

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  • Difluprednate Topical Preparations
  • Difluprednate Topical Preparations
  • Difluprednate Topical Preparations

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0054] Preparation of raw material preparation example 1 crystal form I

[0055] Dissolve 10 g of difluprednate in 20 mL of acetonitrile, heat until dissolved, filter off insoluble matter, then evaporate under reduced pressure, cool down after crystals appear, filter, and dry to obtain crystal form I of difluprednate.

[0056] Carry out X-ray powder diffraction measurement to crystal after drying, record characteristic peak position to be 2θ=8.9 °, 11.6 °, 17.6 °, such as figure 1 shown.

[0057] Get commercially available difluprednate crude drug and carry out X-ray powder diffraction measurement, record characteristic peak position as 2θ=6.1 °, 13.1 °, 15.4 °, 16.9 °. Such as figure 2 shown.

[0058] Get the commercially available difluorocorrone valerate cream, heat and filter to obtain the raw material micropowder wherein, measure X-ray powder diffraction 2θ=6.1 °, 13.1 °, 15.4 °, 16.9 °, such as image 3 Shown, illustrate that the crude drug that commercially availab...

Embodiment 1-1

[0060] Difluprednate 0.5g (crystal form I), white petrolatum 100g, stearyl alcohol 30g, liquid paraffin 30g,

[0061] Pingpingjia A-2050g, glycerin 50g, propylene glycol 20g, ethyl paraben 1g, citric acid (C 6 h 8 o 7 ·H 2 (0) 3g,

[0062] Sodium citrate (Na 3 C 6 h 5 o 7 2H 2 O) 6g of water for injection is added to 1000g, and the average particle diameter of difluprednate crystal form II micropowder is 8.2 μm

[0063] Accurately weighed according to the above ratio, the cream preparation process is as follows:

[0064] (1) Oil phase preparation: take white petrolatum, stearyl alcohol, liquid paraffin, and Pingpingjia A-20 in a container, heat to melt, and keep the temperature at 90°C;

[0065] (2) Water phase preparation: Dissolve citric acid and sodium citrate in water for injection, disperse the main drug evenly in glycerin and propylene glycol, add aqueous solution of citric acid and sodium citrate, ethylparaben, heat and stir The uniform temperature is maintai...

Embodiment 1-2

[0068] According to the formula and process of Example 1-1, using commercially available difluprednate raw material micropowder, the average particle size is 8.1 μm

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Abstract

Difluprednate topical external preparation comprises difluprednate micro powder used as active ingredients and one type or multiple types of pharmaceutic adjuvants, wherein the pharmaceutic adjuvants comprise water. The difluprednate topical external preparation is characterized in that the difluprednate micro powder is scattered in the pharmaceutic adjuvants in a suspended mode, the difluprednate is difluprednate crystal form I, and the X-ray powder diffraction of the difluprednate crystal form I has a characteristic peak when a diffraction angle 2theta is 8.9 degrees, 11.6 degrees and 17.6 degrees.

Description

technical field [0001] The invention relates to a local external application preparation of steroid corticosteroid, in particular to a local external application preparation of difluprednate. Background technique [0002] The molecular formula of difluprednate (CAS: 23674-86-4, difluprednate) is as follows: [0003] [0004] 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 Mitsubishi Tanabe Pharmace...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/573A61K9/10A61P29/00A61P37/08A61P17/00A61P27/02A61P11/02A61P27/16
Inventor 孙亮陈松韩昆颖
Owner TIANJIN JINYAO GRP