Stomach detention sustained and controlled release medicament releasing system and preparation method

A technology for controlled-release drugs and sustained-release drugs, applied in the field of medicine, can solve the problems of using many excipients, limiting flexibility, and high density of tablet cores.

Active Publication Date: 2009-02-25
北京天衡药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The use of release rate controlling excipients of less than 20% limits formulation flexibility in achieving the desired release rate while maintaining a high level of reproducibility of the release profile from batch to batch
On the other hand, excipients themselves may not be able to swell quickly and highly due to careful selection of excipients for release rate control to ensure high reproducibility of the release profile even in small amounts
The system in WO01/10417 uses the inactive phase to achieve flotation, which is realized by enclosing carbon dioxide in the inactive phase sheet to reduce the density, but the floating stability is not good
[0023] Gentamicin Gastric Floating Tablets, which are already on the market in China, use stearyl alcohol, acrylic resin, and hydroxypropyl cellulose as the tablet core matrix, and control the density of the entire tablet core at 1.1-1.2 g/cm 3 Among them, the main disadvan

Method used

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  • Stomach detention sustained and controlled release medicament releasing system and preparation method
  • Stomach detention sustained and controlled release medicament releasing system and preparation method
  • Stomach detention sustained and controlled release medicament releasing system and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] Air bag composition: Sustained release layer composition:

[0102] Capsule No. 1 1000 Rosiglitazone Tartrate 8g

[0103] Ethyl cellulose 9.0g Stearic acid 32g

[0104] Stearic acid 15.0g Ethyl cellulose 40g

[0105] Triethyl citrate 4.5g Povidone k30 16g

[0106] Talc powder 3.0g Polyethylene glycol 24g

[0107] Add absolute ethanol to 300ml Talc powder 16g

[0108] 90% ethanol solution to 1000ml

[0109] Process: Put the No. 1 capsule shell into the coating pan, spray the prepared waterproof coating solution (dissolved / dispersed by stearic acid, ethyl cellulose, triethyl citrate, talc powder) at a tablet bed temperature of 45°C Prepared in absolute ethanol), after the weight gain of the coating was 15%, the capsule was locked, and the weight gain of the coating was 15%, and placed at 45°C for 12h to obtain a waterproof air bag; Rosiglitazone tartrate, stearic acid , ethyl cellulose, povidone, polyethyle...

Embodiment 2

[0111] Air bag composition: Drug layer:

[0112] Capsule No. 1 1000 pcs Rosiglitazone Maleate 1.5g

[0113] Ethylcellulose 9.0g Eudragit RL100 4.5g

[0114] Stearic acid 15.0g Ethyl cellulose 2.0g

[0115] Triethyl citrate 4.5g Polyethylene glycol 1.0g

[0116] Talc powder 3.0g 90% ethanol solution 100ml

[0117] Add absolute ethanol to 300ml

[0118] Isolation layer: Controlled release coating:

[0119] Lactose 30g Eudragit RS100 2.5g

[0120] povidone k30 3.0g Ethylcellulose 2.0g

[0121] Absolute Ethanol 200ml Polyethylene Glycol 1.0g

[0122] Triethyl citrate 0.8g

[0123] 90% ethanol 100ml

[0124] Process: Put the No. 1 capsule shell into the coating pan, spray the prepared waterproof coating solution (dissolved / dispersed by stearic acid, ethyl cellulose, triethyl citrate, talc powder) at a tablet bed temperature of 45°C prepared in absolute ethanol), after the weight gain of coati...

Embodiment 3

[0126] Airbag Composition Eudragit RL100 4.5g

[0127] Waterproof layer: ethyl cellulose 2.0g

[0128] Eudragit L100 9.0g Polyethylene glycol 1.0g

[0129] Stearic acid 15.0g 90% ethanol solution 100ml

[0130] Triethyl citrate 4.5g

[0131] Talc powder 3.0g Controlled Release Coating:

[0132] Absolute ethanol to 300ml Eudragit RS100 2.5g

[0133] Ethylcellulose 2.0g

[0134] Composition of drug-containing layer: Polyethylene glycol 1.0g

[0135] Drug layer: Triethyl citrate 0.8g

[0136] Rosiglitazone Maleate 1.5g 90% Ethanol 100ml

[0137] Process: Put the No. 1 capsule shell into the coating pan, spray the prepared waterproof coating solution (dissolved / dispersed in stearic acid, Eudragit L100, triethyl citrate, talc powder in the water ethanol), after the weight gain of coating was 15%, the capsule was locked, and then the weight gain of the coating was 15%, and placed at 45°C for 12h to obtain a waterproof air bag;...

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Abstract

The invention provides a new air sac type gastric retention controlled-release medicine release system, including (1) an air sac which is formed by wrapping high molecular film-forming materials and hydrophobic materials outside a hollow sac; (2) a medicine containing layer which is composed of medicines and pharmaceutically acceptable excipient; the medicine containing layer covers the outside of the air sac and includes a medicine controlled release layer or a medicine slow release layer. If necessary, a quick release layer, which is composed of medicines and excipient and covers the outside of the controlled release layer or the slow release layer, can also be included. The air sac can also be internally filled with a certain amount of gas generant which includes carbonate and pharmaceutically acceptable organic acid. The average density of the whole formulation can be generally controlled below 0.6/cm<3> and is obviously superior to the present gastro-floating formulation on sale, and the floating time in the stomach is rather longer than a common gastro-floating formulation.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a novel drug release system for sustained and controlled gastric retention, in particular to an airbag type drug release system for sustained and controlled gastric retention and a preparation method thereof. Background technique [0002] Sustained and controlled release preparations for gastric retention are an important form of gastric retention controlled drug delivery system, designed and prepared according to the principle of The Hydrodynamically Balanced Sustained / Controlled Drug Delivery System (HBS), and can float in gastric juice after oral administration A special formulation that releases the drug over time. Since the density of this preparation is smaller than that of the gastric content, it usually stays in the floating state for 5-6 hours in the stomach, prolongs the release time of the drug in the stomach, and allows as much drug as possible to reach the absorption ...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K9/52A61P43/00
CPCA61K31/7036A61K9/5078G01N2013/006A61K31/4439A61K9/1676A61K31/341A61K9/5026A61K9/0065A61K31/70A61K31/4178A61K31/34A61K9/5047
Inventor 姜庆伟郑俊丽杨文斌刘全志
Owner 北京天衡药物研究院有限公司
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