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Nimesulide solid dispersion micro-powder and preparation method thereof

A technology of solid dispersion and micropowder, which is applied in the field of solid dispersion micropowder of nimesulide and its preparation, which can solve the problems of low bioavailability, poor solubility of active ingredients, slow dissolution rate, etc., and achieve good dispersion and good stability , the effect of mild operating conditions

Inactive Publication Date: 2020-03-06
HAINAN HONZ PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the disadvantages of poor solubility of active ingredients, slow dissolution rate, and low bioavailability of nimesulide solid preparations in the prior art, the purpose of the present invention is to provide a solid dispersed micropowder of nimesulide, which can be used to prepare nimesulide Solubilized immediate release formulation of mesulide

Method used

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  • Nimesulide solid dispersion micro-powder and preparation method thereof
  • Nimesulide solid dispersion micro-powder and preparation method thereof
  • Nimesulide solid dispersion micro-powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] prescription:

[0029] Material composition Prescription ratio (%) Nimesulide 20 PVPK30 40 HPMC 40

[0030] Preparation:

[0031] 1) Preparation of mixed solution: Accurately weigh the mixture of 2.0g nimesulide, 4.0g PVPK30 and 4.0g HPMC and place it in a 500mL conical flask, add 200mL of dichloromethane and methanol mixed solvent (volume ratio 3:1, Containing 0.1% analytically pure hydrochloric acid by volume) to dissolve completely;

[0032] 2) CO 2 Feed: as figure 1 shown, open the CO 2 Cylinder valve, liquefied CO 2 The high-pressure pump is continuously introduced into the high-pressure crystallization kettle of the supercritical fluid crystallization equipment system through the two symmetrical channels of the kettle head (at 60° to the intermediate solution channel), and the flow rate is controlled at 100mL / min, and the inside of the kettle is regulated by the heating device and the pressure regulating valve. The temperatu...

Embodiment 2

[0036] prescription:

[0037] Material composition Prescription ratio (%) Nimesulide 20 PVPK30 30 HPMC 50

[0038] Preparation:

[0039] 1) Preparation of mixed solution: Accurately weigh the mixture of 2.0g nimesulide, 3.0g PVPK30 and 5.0g HPMC and place it in a 500mL conical flask, add 200mL of dichloromethane and methanol mixed solvent (volume ratio 1:1, Containing 0.1% analytically pure hydrochloric acid by volume) to dissolve completely;

[0040] 2) CO 2 Feed: as figure 1 shown, open the CO 2 Cylinder valve, liquefied CO 2 The high-pressure pump is continuously introduced into the high-pressure crystallization kettle of the supercritical fluid crystallization equipment system through the two symmetrical channels of the kettle head (at 60° to the intermediate solution channel), and the flow rate is controlled at 100mL / min, and the inside of the kettle is regulated by the heating device and the pressure regulating valve. The temperatu...

Embodiment 3

[0044] prescription:

[0045] Material composition Prescription ratio (%) Nimesulide 20 PVPK30 20 HPMC 60

[0046] Preparation:

[0047] 1) Preparation of mixed solution: Accurately weigh the mixture of 2.0g nimesulide, 2.0g PVPK30 and 6.0g HPMC and place it in a 500mL conical flask, add 200mL of dichloromethane and methanol mixed solvent (volume ratio 1:1, Containing 0.1% analytically pure hydrochloric acid by volume) to dissolve completely;

[0048] 2) CO 2 Feed: as figure 1 shown, open the CO 2 Cylinder valve, liquefied CO 2 The high-pressure pump is continuously introduced into the high-pressure crystallization kettle of the supercritical fluid crystallization equipment system through the two symmetrical channels of the kettle head (at 60° to the intermediate solution channel), and the flow rate is controlled at 100mL / min, and the inside of the kettle is regulated by the heating device and the pressure regulating valve. The temperatu...

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Abstract

The invention discloses nimesulide solid dispersion micro-powder. The nimesulide is prepared by using povidone and hydroxypropyl methylcellulose as dispersion carrier materials and carrying out supercritical fluid crystallization. According to the invention, the preparation method of nimesulide solid dispersion micro-powder is operated simply under mild conditions; the controllability is high; andno solvent residue is left. The obtained nimesulide solid dispersion micro-powder is small in particle size, high in dispersity and high in stability; and the saturated solubility can reach over 5 times of that of a nimesulide raw material medicine (pH = 6.8). The micro-powder can be used for preparing solubilizing quick-release particles of nimesulide; the rapid dissolving in the dissolution medium with the pH value of 6.8 is realized; and the equilibrium dissolution rate of the micro-powder is more than two times of those of bulk drugs and nimesulide particles. Besides, the micro-powder canalso be used for preparing nimesulide tablets, capsules or suspensions and the like.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a solid dispersed fine powder of nimesulide and a preparation method thereof. Background technique [0002] Nimesulide is a non-steroidal anti-inflammatory drug with good anti-inflammatory, analgesic and antipyretic effects. It is the first strong selective cyclooxygenase inhibitor listed in the world. It is used to treat rheumatoid arthritis, osteoarthritis, respiratory inflammation, postoperative pain and edema, fever and other diseases. Nimesulide, with methylsulfonyl as the active group, is a non-acid non-steroidal anti-inflammatory drug with a pKa of 6.5, almost insoluble in water and acidic media, and belongs to BCS class II (low solubility and hypertonicity) drugs , the saturation solubility in water, 0.1mol / L hydrochloric acid solution and pH 6.8 phosphate buffer solution is only 0.010, 0.007 and 0.019g / L respectively. Therefore, it is necessary to take higher doses of drugs to ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/32A61K47/38A61K31/18A61P29/00
CPCA61K9/146A61K31/18A61P29/00
Inventor 刘贵金洪江游凌日金
Owner HAINAN HONZ PHARMA
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