Pidotimod liposome solid preparation

A solid preparation, liposome technology, applied in the field of medicine, can solve problems such as increasing drug retention time, and achieve the effects of improving bioavailability, long distribution time, and improving quality

Inactive Publication Date: 2012-07-18
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Through a large number of experiments, it was found that the liposome solid preparation made of specific excipients and Dexibuprofen effectively overcomes the problem of poor stability of the main drug, improves the dissolution rate of the drug, and increases the drug in vivo. keep time

Method used

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  • Pidotimod liposome solid preparation
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  • Pidotimod liposome solid preparation

Examples

Experimental program
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preparation example Construction

[0064] On the other hand, the present invention provides the preparation method of Dexibuprofen liposome, the method comprises the following steps:

[0065] (a) dissolve dextrobuprofen, phosphatidylinositol, cholesterol, stigmasterol and polyoxyethylene 40 hydrogenated castor oil in an organic solvent, mix well, and remove the organic solvent under reduced pressure on a rotary thin film evaporator to obtain the Lipid film;

[0066] (b) Under the protection of nitrogen, add buffer solution to the bottle, shake and stir for 30 minutes at a speed of 400-700r / min to completely hydrate the phospholipid membrane, and use a tissue masher to homogeneously emulsify at a high speed for 10-15 minutes , rotating speed 5000r / min, filter with 0.45 μm microporous membrane, make liposome suspension;

[0067] (c) Spray-drying the above-mentioned liposome suspension to obtain Dexibuprofen liposome powder.

[0068] In a preferred embodiment of the method for preparing dexibuprofen liposomes of...

Embodiment 1

[0108] The preparation of embodiment 1 Dexibuprofen liposome sheet

[0109] The raw and auxiliary materials used are as follows:

[0110]

[0111] Adopt following production process to prepare Dexibuprofen liposome tablet:

[0112] (1) 200g Dexibuprofen, 800g phosphatidylinositol, 500g cholesterol, 300g stigmasterol and 600g polyoxyethylene 40 hydrogenated castor oil are dissolved in 120000ml volume ratio of ethanol and acetone mixed solvent of 3: 1, mix Uniformly, the organic solvent is removed under reduced pressure on a rotary thin film evaporator to obtain a lipid film;

[0113] (2) Under the protection of nitrogen, add 15000ml of phosphate buffer solution with a pH value of 6.5 to the bottle, shake and stir for 30 minutes at a speed of 400-700r / min to completely hydrate the phospholipid membrane, and use a tissue masher to High-speed homogeneous emulsification for 10-15 minutes, rotating speed 5000r / min, filtering with a 0.45 μm microporous membrane to obtain a lip...

Embodiment 2

[0118] The preparation of embodiment 2 Dexibuprofen liposome tablet

[0119] The raw and auxiliary materials used are as follows:

[0120]

[0121]

[0122] Adopt following production process to prepare Dexibuprofen liposome tablet:

[0123] (1) 200g dextrobuprofen, 1200g phosphatidylinositol, 500g cholesterol, 300g stigmasterol and 700g polyoxyethylene 40 hydrogenated castor oil are dissolved in 150000ml volume ratio in ethanol and acetone mixed solvent of 3: 1, mix Uniformly, the organic solvent is removed under reduced pressure on a rotary thin film evaporator to obtain a lipid film;

[0124] (2) Under nitrogen protection, add 18000ml of phosphate buffer solution with a pH value of 6.5 to the bottle, shake and stir for 30 minutes at a speed of 400-700r / min to completely hydrate the phospholipid membrane, and use a tissue masher to High-speed homogeneous emulsification for 10-15 minutes, rotating speed 5000r / min, filtering with a 0.45 μm microporous membrane to obt...

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Abstract

The invention discloses a pidotimod liposome solid preparation and a preparation method thereof. The pidotimod liposome with excellent quality is prepared by selecting pidotimod, phosphatidylinositol, cholesterol, stigmasterol and cremophor HEL 40 in specific weight ratios and then the pidotimod liposome is prepared into the solid preparation by a common preparation method. The liposome solid preparation and preparation method provided by the invention have the following beneficial effects: the liposome solid preparation has high encapsulation efficiency and uniform grain size; the retention time of medicaments in blood circulation is long; and the preparation method is simple and practical, is beneficial to improvement of the product quality and reduction of the toxic or side effect and is suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to a liposome solid preparation, in particular to a liposome solid preparation of ibuprofen, and belongs to the technical field of medicine. Background technique [0002] Dexibuprofen (Pidotimod), first successfully developed by Gebro-Broscheh GmbH in Austria, was approved for marketing in 1994, and its chemical name is (S)-(+)-2-(4-isobutylphenyl)propionic acid , formula C 13 h 18 o 2 , the molecular weight is 206.28, and the structural formula is: [0003] [0004] Ibuprofen is a propionic acid non-steroidal anti-inflammatory drug, which has analgesic, anti-inflammatory and antipyretic effects. Tissue congestion, swelling, reduce the sensitivity of peripheral nerve pain, it plays an antipyretic effect through the hypothalamic thermoregulatory center. Although ibuprofen is a commonly used non-steroidal anti-inflammatory drug at present, its wide application is affected due to reasons such as large oral dose, poor taste an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/20A61K9/48A61K31/192A61K47/44A61K47/28A61K47/24A61P29/00
Inventor 陶灵刚李岱山
Owner HAINAN LINGKANG PHARMA CO LTD
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