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Lansoprazole vesicle type phospholipid gel slow release solid preparation

A technology of lansoprazole capsule and lansoprazole, which is applied in the field of medicine, can solve the problems of increasing drug retention time, poor stability of the main drug, etc., and achieves the enhancement of vascular permeability, enhancement of targeting, and prevention of drug metabolism inactivation. Effect

Inactive Publication Date: 2013-05-29
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present inventor has carried out research to lansoprazole vesicular phospholipid gel, finds by a large number of experiments, adopts the vesicular phospholipid gel that specific excipient and lansoprazole are made to effectively overcome main drug stability The problem of poor drug resistance, while improving the dissolution rate of the drug, increasing the retention time of the drug in the body

Method used

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  • Lansoprazole vesicle type phospholipid gel slow release solid preparation
  • Lansoprazole vesicle type phospholipid gel slow release solid preparation
  • Lansoprazole vesicle type phospholipid gel slow release solid preparation

Examples

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preparation example Construction

[0060] On the other hand, the present invention provides the preparation method of lansoprazole vesicular phospholipid gel, the method comprises the following steps:

[0061] (a) under nitrogen protection, dissolve lansoprazole, distearoylphosphatidylethanolamine and dilauroylphosphatidylcholine in an appropriate amount of organic solvent, slowly magnetically stir for 15-30 minutes at about 45°C, and then Squeeze through a cellulose ester film to obtain an organic solution

[0062] (b) freeze-drying the above solution until it is completely dry to obtain a dry solid that forms a loose spongy shape;

[0063] (c) Disperse the above solid in a buffer solution with a pH of 6.8 to 7.4 under nitrogen protection, shake and stir for 15-30 minutes, and then make the gradient homogenization of the mixture in a high-pressure homogenizer at 300 to 800 bar for 3 to 6 Go through, obtain the lansoprazole vesicular phospholipid gel of uniform paste, freeze-dry, make lansoprazole vesicular ph...

Embodiment 1

[0105] The preparation of embodiment 1 lansoprazole vesicular phospholipid gel sheet

[0106] The raw and auxiliary materials used are as follows:

[0107]

[0108] Adopt following production process to prepare lansoprazole vesicular phospholipid gel sheet:

[0109] (1) under nitrogen protection, 30g lansoprazole, 240g distearoylphosphatidylethanolamine and 48g dilauroylphosphatidylcholine were dissolved in 500ml tert-butanol, and slowly magnetically stirred for 30 minutes at about 45°C, Then squeeze through the cellulose ester film to obtain an organic solution;

[0110] (b) The above solution was pre-frozen at -60°C for 3 hours, then frozen at -50°C for 6 hours, then sublimated to 25°C for 34 hours, and finally dried at 30°C for 3 hours until it was completely dry to obtain a loose sponge-like dry solid;

[0111] (c) Disperse the above solid in 600ml of phosphate buffer with a pH value of 7.4 under nitrogen protection, shake and stir for 15 minutes, and then perform ...

Embodiment 2

[0115] The preparation of embodiment 2 lansoprazole vesicular phospholipid gel capsules

[0116] The raw and auxiliary materials used are as follows:

[0117]

[0118] Adopt following production process to prepare lansoprazole vesicular phospholipid gel sheet:

[0119] (1) under nitrogen protection, 30g lansoprazole, 180g distearoylphosphatidylethanolamine and 36g dilauroylphosphatidylcholine were dissolved in 500ml tert-butyl alcohol, and slowly magnetically stirred for 15 minutes at about 45°C, Then squeeze through the cellulose ester film to obtain an organic solution;

[0120] (2) The above solution was pre-frozen at -70°C for 2 hours, then frozen at -40°C for 8 hours, then sublimated to 20°C for 18 hours, and finally dried at 35°C for 1 hour until it was completely dry, and a loose sponge-like product was obtained. dry solid;

[0121] (3) Disperse the above-mentioned solid in 450ml of phosphate buffer with a pH value of 7.4 under nitrogen protection, shake and sti...

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Abstract

The invention discloses a lansoprazole vesicle type phospholipid gel slow release solid preparation and a preparation method thereof. The preparation method comprises the steps of: preparing good-quality lansoprazole vesicle type phospholipid gel by selecting lansoprazole, distearoyl phosphatidyl ethanolamine and dilaurin dimyristoyl phosphatidyl choline which are in a certain weight ratio; and preparing a solid preparation from the lansoprazole vesicle type phospholipid gel through a common preparation method. The lansoprazole vesicle type phospholipid gel prepared by the preparation method is uniform in tridimensional netty structure, uniform and proper in the particle diameter size, slow in medicament release and long in retention time in the blood circulation; the preparation method is simple in equipment and easy to operate and control; and by using the preparation method, the product quality is improved and the toxic side effect is reduced, thus the preparation method is suitable for industrial mass production.

Description

technical field [0001] The invention relates to a vesicular phospholipid gel solid preparation, in particular to a lansoprazole vesicular phospholipid gel solid preparation, which belongs to the technical field of medicine. Background technique [0002] Lansoprazole (Lansoprazole), chemical name: (±)-2[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl] Sulfuryl]benzimidazole, molecular formula: C 16 h 14 f 3 N 3 o 2 S, molecular weight: 369.37, structural formula: [0003] [0004] Lansoprazole was developed by Takeda Corporation of Japan and was listed in Japan in 1992. Lansoprazole is a proton pump inhibitor, which is activated under acidic conditions and binds to the proton pump (H + / K + )-ATPase base-building binding, inhibiting enzyme activity and thus inhibiting acid secretion. It is suitable for gastric ulcer, duodenal ulcer, reflux esophagitis, and Zoller-Ehrlich syndrome. [0005] Lansoprazole is insoluble in water, and its stability is relatively ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/48A61K9/00A61K31/4439A61K47/24A61P1/04
Inventor 马明廖爱国
Owner HAINAN MEIDA PHARMA