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Novel capsule colon-specific drug delivery system (CSDDS) and preparation method thereof

A technology of colon targeting and drug delivery system, which is applied in the field of medicine, can solve the problems of difficulty in ensuring accurate release of drugs to the colon, poor effect of colon targeting and controlled release, complex prescriptions, and complicated processes, and achieves convenient and controlled drug release. The effect of clear explanation principle and low production cost

Inactive Publication Date: 2011-07-27
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] For colon-targeted preparations, there are (1) double-coated colon-targeted oral preparations and preparation methods thereof (200710060577.1), (2) a controlled-release colon-targeted drug delivery preparation and preparation methods (201010106109.5) , (3) colon-targeted pellets containing vancomycin and its preparation method (200810211739.1), (4) a colon-targeted preparation of animal skin collagen polypeptide and its preparation method (200710029479.1) and other patent applications, However, they are all prepared into colon-targeting tablets or pellets, and coated with colon-targeting coating solution. The prescription and process are complicated, and the principle of controlled release is single. There are also patents such as: colon-targeted drug delivery soft capsule and its preparation method (200710031234.2), etc., but the research content is limited to coating the shell of ordinary soft capsules with pH-sensitive materials, and the effect of colon-targeted controlled release is poor

Method used

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  • Novel capsule colon-specific drug delivery system (CSDDS) and preparation method thereof
  • Novel capsule colon-specific drug delivery system (CSDDS) and preparation method thereof
  • Novel capsule colon-specific drug delivery system (CSDDS) and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Insoluble microporous membrane vesicle composition:

[0051]

[0052] Preparation process: first dissolve polyethylene glycol and poloxamer in acetone, then dissolve cellulose acetate in acetone, add an appropriate amount of titanium dioxide into it, stir well, and let stand to remove air bubbles. The insoluble microporous membrane capsule is obtained by making blanks through the dipping process, drying, shelling, cutting and finishing.

[0053] The composition of enzymolysis rubber stopper:

[0054]

[0055] Preparation process: mixing pectin, chitosan, ethyl cellulose and magnesium stearate evenly, adding them to a tablet press for tableting, and preparing a pectin sheet with a diameter of 5 mm, a hardness of 5.5 kg and a thickness of 0.9 mm, that is, Enzymatic rubber stopper.

[0056] Take epirubicin hydrochloride as the model drug, mix the drug:sodium chloride=2:1, the drug is 10mg, fill it into the capsule in the form of powder, add an enzymatic pectin plug...

Embodiment 2

[0062] Insoluble microporous membrane vesicle composition:

[0063]

[0064] Preparation process: firstly, polyethylene glycol-400 and polyethylene glycol-4000 are dissolved in a mixed solvent of acetone: anhydrous ethanol (4:1), and then cellulose acetate is dissolved in the above mixed solution, and the dipping process is the same as Example 1, drying, shelling, cutting and finishing to obtain insoluble microporous membrane capsules.

[0065] The composition of enzymolysis rubber stopper:

[0066]

[0067] Preparation process: Mix pectin, chitosan and magnesium stearate evenly, add them to a tablet press to press, and prepare a pectin sheet with a diameter of 5mm, a hardness of 5.5kg and a thickness of 0.9mm, which is an enzymatic rubber stopper .

[0068] Take indomethacin as a model drug, mix indomethacin:sodium chloride=1:2, indomethacin is 25mg, fill it into the capsule in the form of powder, add an enzymatic gel plug, and then put it in the capsule. Add a solub...

Embodiment 3

[0074] Insoluble microporous membrane vesicle composition:

[0075]

[0076] Preparation process: first dissolve cellulose acetate in acetone: anhydrous ethanol (4: 1) mixed solution, add glycerin as a plasticizer and PVP-K30 as a porogen, the preparation process is the same as Example 1, drying, and shelling , cutting and finishing to obtain insoluble microporous membrane capsules.

[0077] The composition of enzymolysis rubber stopper:

[0078] Pectin 25g

[0079] Magnesium stearate amount

[0080] Preparing Pectin Stoppers 250 Tablets

[0081] Preparation process: Mix pectin and magnesium stearate evenly, add them to a tablet press to press, and prepare a pectin sheet with a diameter of 5 mm, a hardness of 5.5 kg and a thickness of 0.9 mm, to obtain an enzymatic rubber plug.

[0082] Take verapamil hydrochloride as a model drug, mix verapamil hydrochloride:sodium chloride=1:1, verapamil hydrochloride is 60mg, fill it into the capsule in powder form, add enzymolysis p...

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Abstract

The invention relates to a novel colon-specific drug delivery system (CSDDS) and preparation method. The capsule CSDDS has the advantages that the release control principle is clear, the preparation process is simple, the drug release is precise, the scope of suitable drugs is wide, and the drug release adjustment is convenient. The capsule CSDDS provided by the invention comprises an insoluble capsule, an enzymolysis capsule, a soluble capsule cap and an enteric coating, can be used for filling chemical medicaments, traditional Chinese medicines, biological product medicines, and the like, and can be used for controlling the release of the medicaments on a colon part. The insoluble capsule of the CSDDS can be prepared by using a conventional capsule shell preparation method; the enzymolysis capsule can be prepared by using a conventional tabletting method; the enteric coating can be prepared by using a fluidized bed method; and a release test shows that the capsule shell has the advantage of controlling the medicaments to release at the colon part.

Description

technical field [0001] The invention relates to the technical field of medicine, specifically a novel colon-targeted capsule drug delivery system and a preparation method thereof. The colon-targeted capsule system of the invention can be used for filling chemical medicines, traditional Chinese medicines, biological medicines, etc., and can control the release of medicines in the colon after oral administration of medicines. Background technique [0002] Oral colon-targeted drug delivery system (OCDDS for short) refers to the use of appropriate methods to avoid the release of drugs in the stomach, duodenum, jejunum and anterior ileum after oral administration, but to release the drug after delivery to the ileocecal (or colon) , a drug delivery system that enables drugs to exert local or systemic therapeutic effects. In recent years, due to the recognition of the advantages of colon in drug absorption and local treatment, this drug delivery system has attracted more and more ...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K47/44A61K47/38A61K47/36A61K47/34A61K47/32A61K47/10
Inventor 傅红兴赵应征张福志陈密特
Owner WENZHOU MEDICAL UNIV
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