A colon-targeted pH-sensitive hydrogel and its preparation method and application

A colon-targeting and hydrogel technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as poor positioning, hydrophobicity of polymer materials and reduced swelling degree , to achieve the effect of reducing toxic and side effects, alleviating noncompliance and pain, and easily obtaining materials

Active Publication Date: 2016-02-24
秦京(嘉兴)生物科技有限公司
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AI Technical Summary

Problems solved by technology

[0005] Various drug delivery systems such as pH-dependent, time-delayed drug release, pressure-controlled drug delivery system, and flora-triggered drug delivery system still have certain limitations and poor positioning
Among these five types of systems, the most promising flora-triggered drug delivery system, the key problem is how to improve the hydrophobicity of polymer materials and reduce the swelling degree

Method used

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  • A colon-targeted pH-sensitive hydrogel and its preparation method and application
  • A colon-targeted pH-sensitive hydrogel and its preparation method and application
  • A colon-targeted pH-sensitive hydrogel and its preparation method and application

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Embodiment Construction

[0053] Aiming at the problem that when the macromolecular polysaccharide material is used as the colon-targeting carrier, the drug can not be treated in advance due to the early release of the drug, it proposes a colon-targeted hydrogel that does not require coating or other cumbersome operations to avoid the destruction of the gastrointestinal tract. Glue formula and its preparation method. The hydrogel prepared by the invention inhibits the release of the water-soluble drug hydrocortisone sodium succinate in the stomach and small intestine to a large extent, and the drug reaches the colon part directionally to exert its drug effect.

[0054] Due to the similar pH environment of the small intestine and the colon, the accuracy of the colonic localization of natural polymer carbohydrate materials is reduced, leading to the early release of the drug in the small intestine, and the drug is already in the environment of the small intestine (pH=6.8 or so) before reaching the colon. ...

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Abstract

The invention discloses a colon targeting pH sensitive hydrogel, a preparation method and applications thereof. The hydrogel is prepared by the following steps: mixing konjac glucomannan and xanthan gum, then coating a layer of glycerin on the surface of the mixture, the covering the whole system with a certain amount of sodium alginate, and finally drying so as to obtain the hydrogel. By taking the in vitro drug release behavior as a reference, the affects of hydrogel preparation temperature, drug adding sequence, material ratio, glycerin amount, and drug dosage on the release behaviors of drugs which have been respectively put into an artificial gastric fluid for two hours, an artificial intestinal fluid for two hours, and an artificial colon fluid for four hours are studied, optimum hydrogel for in vitro drug release behavior is selected, and the optimum hydrogel provides the closest in-vivo pH change situation. The colon targeting pH sensitive hydrogel solves the problem that in the prior art natural polysaccharide is taken as the drug carrier, the drug is released in advance and cannot reach the colon, so the drug effect is affected in a certain degree; furthermore the operation is simple, the materials are available, the credibility of the selected screening index is high, and the amount of drugs which can reach the colon accounts for about 80%.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method and application of a colon-targeted pH-sensitive hydrogel Background technique [0002] Oral colon-specific drug delivery system (OCDDS) uses a drug delivery system to prevent the drug from being released in the upper gastrointestinal tract after oral administration, and then disintegrate or erode and release the drug after it is delivered to the ileocecal region of the human body. , and play a local or systemic therapeutic effect in the large intestine; as a new drug delivery system, colon-targeted drug delivery has become a research hotspot in recent years. A variety of targeting materials have been gradually developed and utilized. [0003] According to the drug release mechanism of different drug delivery systems, OCDDS can be divided into five categories. [0004] (1) pH-dependent OCDDS, pH-dependent OCDDS is based on the physiologica...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): A61K9/06A61K47/36A61K31/573
Inventor王珂邢建峰游翠玉许维董凯
Owner秦京(嘉兴)生物科技有限公司