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Colon-specific pH sensitive hydrogel, preparation method and application thereof

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 the problems of poor colon positioning and inability to achieve colon treatment, and reduce Toxic and side effects, reduction of early release, and the effect of easy availability of materials

Active Publication Date: 2014-07-16
吉林省派瑞斯生物技术有限公司
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Problems solved by technology

[0005] Aiming at the problem of poor colon localization of natural macromolecular polysaccharide materials and the inability to achieve colon treatment due to early release of drugs, the present invention proposes a colon-targeting pH-sensitive hydrogel and its preparation method and application without coating or other Colon-targeted hydrogels that avoid cumbersome operations such as gastrointestinal disruption are a new solution to improve water-soluble pharmaceutical agents

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  • Colon-specific pH sensitive hydrogel, preparation method and application thereof
  • Colon-specific pH sensitive hydrogel, preparation method and application thereof
  • Colon-specific pH sensitive hydrogel, preparation method and application thereof

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[0040] specific implementation plan

[0041] The present invention will be further described in detail below in conjunction with specific embodiments, which are explanations of the present invention rather than limitations.

[0042] The colon-targeted pH-sensitive hydrogel provided by the present invention is based on a combination of colon-targeted, pH-sensitive, and flora-triggered hydrogels; wherein:

[0043] Due to the pH changes in the gastrointestinal tract and colon, and the presence of high concentrations of intestinal microorganisms in the colon, the cross-linked compounds of certain polysaccharides are susceptible to colonic microbial degradation and have good colon targeting. Therefore, the present invention selects seaweed sodium bicarbonate as the gel material.

[0044] Alginic acid is a linear natural polymer compound, and its main components are D-mannuronic acid and L-guluronic acid. Because of the rigid poly-L-guluronic acid chains, alginic acid will not sel...

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Abstract

The invention discloses a colon-specific pH sensitive hydrogel, a preparation method and an application thereof. The hydrogel is prepared by mixing glycerol monostearate serving as a delayed-release material and medicines, uniformly coating the surface of the mixture with sodium alginate with a certain concentration, and baking. The in vitro drug release behavior is taken as an index to investigate the concentrations of sodium alginate and calcium chloride, the calcification time and the drug-release behavior of drug loading capacity on medicines in artificial gastric juice for 2 hours, artificial intestinal juice for 4 hours and artificial colonic juice for 4 hours, and the optimal hydrogel for the in vitro drug release behavior is screened. According to the colon-specific pH sensitive hydrogel, release of a medicine in a pH 6.8 environment can be effectively controlled by using the glycerol monostearate as a delayed-release material, and the targeting property can be further improved after the natural polysaccharide material sodium monostearate is coated, so that the glycerol monostearate is not released or little released in pH1.2, and over 90 percent of the medicine can reach the colon part.

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) refers to the use of certain pharmaceutical methods to prevent the drug from being released at the upper end of the gastrointestinal tract after oral administration, and to disintegrate after being transported to the ileum or the colon. A drug delivery system that dissolves or erodes and releases the drug, thereby exerting a local or systemic therapeutic effect. [0003] OCDDS is composed of carrier materials and target drugs, and is mainly designed according to the unique physiological characteristics and carrier characteristics of the gastrointestinal tract and colon. At present, there are six major categories of OCDDS: pH-dependent colon-targeted drug delivery system, time-dependent colon-targeted Drug...

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Application Information

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IPC IPC(8): A61K9/06A61K31/573A61K47/14A61K47/36
Inventor 王珂邢建峰许维赵桂兰闫岩董凯杨莹
Owner 吉林省派瑞斯生物技术有限公司
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