Nimesulide liposome solid preparation and preparation method of drug composite thereof

A technology of nimesulide and solid preparations, which is applied in the field of medicine, can solve the problems of poor dissolution of active ingredients and low bioavailability, and achieve the effects of stable product quality, reduced drug toxicity, and reduced drug side effects

Inactive Publication Date: 2010-02-10
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Aiming at the defects of poor dissolution rate of active ingredients and low bioavailability in nimesulide solid preparations in the prior art, the object of the present invention is to provide a nimesulide solid preparation with improved bioavailability, specifically, to provide A nimesulide liposome and its solid pharmaceutical composition, which solves the defects of the nimesulide solid preparation by encapsulating it with liposomes, and improves the drug efficacy and bioavailability of the preparation

Method used

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  • Nimesulide liposome solid preparation and preparation method of drug composite thereof
  • Nimesulide liposome solid preparation and preparation method of drug composite thereof
  • Nimesulide liposome solid preparation and preparation method of drug composite thereof

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Embodiment 1

[0037] The preparation of embodiment 1 nimesulide liposome

[0038] Prescription: Nimesulide 50g

[0039] Monolaurin 150g

[0040] Cholesterol 25g

[0041] Poloxamer 188 100g

[0042] Preparation Process

[0043] (1) 50g nimesulide, 150g monoglyceride laurate, 25g cholesterol and 100g poloxamer 188 were dissolved in 800ml dehydrated ethanol, mixed uniformly, decompressed and removed dehydrated alcohol on a rotary thin film evaporator, Prepare phospholipid film;

[0044](2) Add 800 ml of pH=5.5 phosphoric acid-disodium hydrogen phosphate buffer solution, shake, stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and obtain a liposome suspension;

[0045] (3) Freeze-drying the suspension to prepare nimesulide liposomes.

Embodiment 2

[0055] The preparation of embodiment 2 nimesulide liposome

[0056] Prescription: Nimesulide 100g

[0057] Monolaurin 1000g

[0058] Cholesterol 100g

[0059] Poloxamer 188 10g

[0060] Preparation Process

[0061] (1) Dissolve 100g nimesulide, 1000g monoglyceride laurate, 100g cholesterol and 10g poloxamer 188 in 2000ml dehydrated ethanol, mix well, remove dehydrated alcohol under reduced pressure on a rotary thin film evaporator, Prepare phospholipid film;

[0062] (2) Add 1000ml of acetic acid-sodium acetate buffer solution with pH=6.0, shake and stir to make the phospholipid film fully hydrated, homogeneously emulsify at a high speed, and obtain a liposome suspension;

[0063] (3) The suspension is spray-dried to prepare nimesulide liposomes.

Embodiment 3

[0073] The preparation of embodiment 3 nimesulide liposome

[0074] Prescription: Nimesulide 75g

[0075] Monolaurin 400g

[0076] Cholesterol 300g

[0077] Poloxamer 188 150g

[0078] Preparation Process

[0079] (1) 75g nimesulide, 400g monoglyceride laurate, 300g cholesterol and 150g poloxamer 188 were dissolved in 2000ml dehydrated ethanol, mixed uniformly, decompressed and removed dehydrated ethanol on a rotary thin film evaporator, Prepare phospholipid film;

[0080] (2) Add 2000ml of pH=6.5 citric acid-sodium citrate buffer solution, shake and stir to make the phospholipid film fully hydrated, and high-speed homogeneous emulsification to obtain a liposome suspension;

[0081] (3) Freeze-drying the suspension to prepare nimesulide liposomes.

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Abstract

The invention provides a Nimesulide liposome solid preparation and a preparation method of the drug composite thereof. For the Nimesulide liposome solid preparation of the invention, the active ingredient Nimesulide is prepared into liposome and then prepared into Nimesulide solid preparation with other ingredients, wherein the liposome is prepared by the following ingredients according to parts by weight: 1 part of Nimesulide, 3-10 parts of lauric acid glycerol monolaurate, 0.5-4 parts of cholesterol, and 0.1-2 parts of poloxamer188. Compared with the existing Nimesulide liposome solid preparation, the Nimesulide of the invention has high dissolution rate and improved bioavailability, and overcomes the detect that the bioavailability of the Nimesulide liposome solid preparation in the prior art is low.

Description

technical field [0001] The invention relates to a nimesulide solid preparation, specifically, the invention provides a nimesulide liposome and a solid preparation of a pharmaceutical composition thereof, and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Nimesulide, chemical name: 4-nitro-2-phenoxymethanesulfonanilide, molecular formula: C 13 h 12 N 2 o 5 S, molecular weight: 308.3, chemical structural formula: [0003] [0004] This product is a non-steroidal anti-inflammatory drug with anti-inflammatory, analgesic and antipyretic effects. Its mechanism of action is not completely clear, and it may be mainly related to the inhibition of prostaglandin synthesis, the release of leukocyte mediators and the oxidation reaction of polymorphonuclear leukocytes. According to reports, nimesulide is absorbed through oral administration, and reaches the maximum blood concentration within 1 to 2 hours after taking the d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/16A61K9/20A61K9/48A61K47/34A61K31/18A61P29/00A61K47/28
Inventor 邓菊娟
Owner HAINAN LINGKANG PHARMA CO LTD
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