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

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 ...

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 disadvantage of this preparation is that the density of the entire tablet core is high, and the pressure has a great influence on the floating ability of the tablet core. The large volume forms floating, and the tablet core volume expansion capacity is limited, so the floating effect in the stomach is not stable, and it is greatly affected by the environment in the stomach

[0024] Although the above-mentioned existing gastric retention controlled drug release systems can achieve the purpose of floating, they all have the disadvantages of complex structure, many auxiliary materials, cumbersome processing technology, high cost, and poor stability, and they cannot float immediately in the initial stage. The reason is that The initial density is high, and the volume expansion takes a certain time, and its floating capacity (generally represented by buoyancy) decreases with the decrease of the dissolution volume of the tablet core

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