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Meloxicam liposome and pharmaceutical composition thereof

A technology of loxicam lipid and meloxicam, which is applied in the field of medicine, can solve problems such as poor solubility, achieve the effects of improving stability, improving drug therapeutic index, and ensuring product quality

Inactive Publication Date: 2010-01-27
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The object of the present invention is to provide a meloxicam liposome pharmaceutical composition, which solves the problem of poor solubility by encapsulating with liposomes

Method used

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  • Meloxicam liposome and pharmaceutical composition thereof
  • Meloxicam liposome and pharmaceutical composition thereof
  • Meloxicam liposome and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Preparation of meloxicam liposome

[0037] Prescription: Meloxicam 7.5g

[0038] Egg yolk lecithin 75g

[0039] Cholesterol 22.5g

[0040] Poloxamer 188 7.5g

[0041] Preparation Process

[0042] (1) Dissolve 7.5g meloxicam, 75g egg yolk lecithin, 22.5g cholesterol and 7.5g poloxamer 188 in 500ml acetone, mix well, remove acetone under reduced pressure on a rotary thin film evaporator to obtain phospholipids membrane;

[0043] (2) Add 800 ml of pH=5.0 phosphoric acid-dipotassium hydrogen phosphate buffer solution, shake, stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and obtain a liposome suspension;

[0044] (3) freeze-drying the suspension to prepare meloxicam liposomes.

Embodiment 2

[0054] Example 2 Preparation of meloxicam liposome

[0055] Prescription: Meloxicam 30g

[0056] Egg Yolk Phosphatidylserine 45g

[0057] Cholesterol 30g

[0058] Poloxamer 188 120g

[0059] Preparation Process

[0060] (1) 30g meloxicam, 45g egg yolk phosphatidylserine, 30g cholesterol and 120g poloxamer 188 were dissolved in 1500ml ethanol, mixed uniformly, and ethanol was removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0061] (2) Add 2000ml of pH=6.0 citric acid-sodium citrate buffer solution, shake and stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and obtain a liposome suspension;

[0062] (3) freeze-drying the suspension to prepare meloxicam liposomes.

Embodiment 3

[0072] Example 3 Preparation of meloxicam liposome

[0073] Prescription: Meloxicam 15g

[0074] Hydrogenated egg yolk lecithin 90g

[0075] Cholesterol 30g

[0076] Poloxamer 188 45g

[0077] Preparation Process

[0078] (1) Dissolve 15g meloxicam, 90g hydrogenated egg yolk lecithin, 30g cholesterol and 45g poloxamer 188 in 800ml isopropanol, mix well, remove isopropanol under reduced pressure on a rotary thin film evaporator, and prepare Get phospholipid membrane;

[0079] (2) Add 1000ml of acetic acid-sodium acetate buffer solution with pH=5.6, shake and stir to make the phospholipid film fully hydrated, homogeneously emulsify at a high speed, and obtain a liposome suspension;

[0080] (3) freeze-drying the suspension to prepare meloxicam liposomes.

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PUM

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Abstract

The invention provides a meloxicam liposome and a pharmaceutical composition thereof. The meloxicam liposome consists of one part by weight of meloxicam, 1.5-10 parts by weight of phospholipid, 1-3 parts by weight of cholesterin and 1-4 parts by weight of poloxamer 188. The invention is made in a such way that the meloxicam is made into the liposome, and the liposome is made into solid pharmaceutical preparation. The preparation components and the preparation art are simple, compared with the prior meloxicam preparation, the invention can not only improve the stability of the meloxicam solid preparation, but also can improve the dissolvability and the bioavailability of the meloxicam.

Description

technical field [0001] The invention relates to a meloxicam preparation and a preparation method thereof, in particular to a meloxicam liposome and its solid pharmaceutical composition. It belongs to the field of medical technology. Background technique [0002] Meloxicam, chemical name: 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide -1,1-dioxide, molecular formula: C 14 h 13 N 3 o 4 S 2 , molecular weight: 351.42, chemical structural formula: [0003] [0004] This product is an enolic acid non-steroidal anti-inflammatory drug (NSAID), which has strong anti-inflammatory, analgesic and antipyretic effects, can inhibit the synthesis of prostaglandins, and is selective for cyclooxygenase-2 (COX-2) Sexual inhibition, more secure than other NSAIDs. It is clinically applicable to the treatment of rheumatoid arthritis and painful osteoarthritis (arthrosis, degenerative osteoarthritis). [0005] Meloxicam is poorly soluble in water, and h...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/5415A61P29/00A61P19/02A61P19/04
Inventor 陶灵刚
Owner HAINAN YONGTIAN PHARMA INST
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