Crosslinking wrapped core slice in vivo for

A colon localization and drug delivery technology, applied in the directions of drug delivery, antitumor drugs, drug combination, etc., can solve the problems of unstable nature, difficult to popularize and use, difficult to control the degree of cross-linking, etc. stagnant release effect

Inactive Publication Date: 2008-01-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, calcium pectin is not yet a pharmaceutical excipient, the degree of cross-linking is not easy to control, and its properties are unstable, so it is difficult to popularize and use

Method used

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  • Crosslinking wrapped core slice in vivo for
  • Crosslinking wrapped core slice in vivo for
  • Crosslinking wrapped core slice in vivo for

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Indomethacin pectin / calcium chloride in vivo cross-linked pressed package chip

[0022] Tablet prescription:

[0023] Indomethacin 25mg

[0024] Microcrystalline Cellulose 20mg

[0025] Lactose 20mg

[0026] Crospovidone 5mg

[0027] Magnesium Stearate 1mg

[0028] Scale up by 1000 pieces.

[0029] Preparation process: Indomethacin is in micronized form, with an average particle size of less than 5 microns, magnesium stearate is used directly, and other auxiliary materials are passed through an 80-mesh sieve. Precisely weigh the prescribed amount of indomethacin and various auxiliary materials, mix them evenly in a small mixer, and directly compress them into tablet cores with a diameter of about 6 mm on a ZDY-1 single-punch tablet press. Check by the relevant regulations in the two appendices of the 2005 edition of the Pharmacopoeia of the People's Republic of China, the tablet weighs 71 mg, the disintegration time is less than 30 seconds, the friabili...

Embodiment 2

[0048] Example 2 Release of different pectin / calcium chloride ratio-coated chips

[0049] In order to further elucidate the in vivo cross-linking effect of calcium chloride on pectin, the release of coated chips was compared when the coating layer contained different ratios of pectin / calcium chloride.

[0050] Tablet core prescription is with embodiment 1.

[0051] The coating material prescription is shown in Table 2. Prepare according to the method for preparing the chip in Example 1. Prepared according to the prescription quantity of 1000 tablets. Check according to the relevant methods in the two appendices of the 2005 edition of the Pharmacopoeia of the People's Republic of China.

[0052] Formulation and basic properties of cake-packed tablets when the coating material contains different amounts of calcium chloride in table 2

[0053]

prescription number

Coating composition (mg)

Sheet weight

(mg)

tensile strength

(kg)

...

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Abstract

The invention pertains to the field of pharmaceutical preparation. The invention relates to a cross-linked covered tablet which is used for colon-specific drug delivery. The invention takes a drug-containing tablet as the core, the periphery of which is wrapped with a coating material, and the outer layer coating retarding material adopts the mixture of pectin of the calcium salts/calcium salts with the special amount and high parts by weight; the retarding release effect of the pectin is strengthened through the cross-linked process, so the invention is applicable to the colon-specific drug delivery, in particular to the insoluble drugs. The experimental results show that the invention can retard the release of the drug, so as to achieve the ideal colon-specific drug delivery, at the same time, the invention does not need to use more coating materials, which can significantly save the using amount of the pectin materials. The invention is applicable to the treatments of the diseases with the need of colon-specific drug delivery, such as colitis, colon cancer and other colon diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a packaged chip that can be used for colon-localized drug delivery. More precisely, the present invention relates to a colon-localized drug delivery system in the form of compressed chips, wherein the outer coating has in vivo cross-linking ability and is composed of pectin and high-weight calcium salt. Background technique [0002] The compression-packed chip is to wrap the blocking layer around the tablet core by pressing and molding, so as to delay the release of the drug and make the drug release in a single pulse. It is mainly used in situations where delayed administration is required, such as the control of cardiovascular diseases Attack in the early morning, or localized administration in the colon to treat local diseases of the colon. When used for colon-specific drug delivery, natural polysaccharides are usually used as coating blocking materials, relying on en...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/505A61K31/606A61K31/573A61P1/00A61P35/00
Inventor 吴伟魏秀莉孙宁云吴宝剑
Owner FUDAN UNIV
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