A kind of s-carboxymethyl-l-cysteine ​​inclusion compound and its enteric-coated preparation composition

A technology of cysteine ​​and enteric-coated preparations, which is applied in the direction of drug combination, drug delivery, and pill delivery, which can solve the problems of only 24 months of validity and poor stability, so as to improve bioavailability and reduce gastric irritation Symptoms, irritation-reducing effects

Active Publication Date: 2021-04-13
GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, the long-term storage stability of the common preparation of S-(carboxymethyl)-L-cysteine ​​is not good, and the validity period is only 24 months

Method used

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  • A kind of s-carboxymethyl-l-cysteine ​​inclusion compound and its enteric-coated preparation composition
  • A kind of s-carboxymethyl-l-cysteine ​​inclusion compound and its enteric-coated preparation composition
  • A kind of s-carboxymethyl-l-cysteine ​​inclusion compound and its enteric-coated preparation composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] S-carboxymethyl-L-cysteine ​​enteric-coated tablet, which contains the following substances in weight ratio:

[0028]

[0029]

[0030] Preparation method:

[0031] Preparation of S-carboxymethyl-L-cysteine ​​clathrate: Take an appropriate amount of S-carboxymethyl-L-cysteine ​​and slowly drop it into the insulated saturated aqueous solution of β-cyclodextrin, stir at a constant temperature and refrigerate. Precipitate was precipitated, filtered, washed and dried.

[0032] Weigh the S-carboxymethyl-L-cysteine ​​clathrate, microcrystalline cellulose, and sodium carboxymethyl starch of the prescribed amount, mix them evenly, pass through an 80-mesh sieve, and prepare them with hypromellose ethanol solution. Granules, 24 mesh granules, the obtained wet granules are dried, add the prescribed amount of talcum powder, mix evenly, 24 mesh granules, and tablet.

[0033] Weigh the enteric-coated layer material of the recipe amount, disperse it with purified water to obta...

Embodiment 2

[0035] S-carboxymethyl-L-cysteine ​​enteric-coated tablet, which contains the following substances in weight ratio:

[0036]

[0037] Preparation method:

[0038] Preparation of S-carboxymethyl-L-cysteine ​​inclusion compound: Dissolve appropriate amount of S-carboxymethyl-L-cysteine ​​in hot water, slowly drop into β-cyclodextrin saturated aqueous solution, 60-80°C Stir vigorously, cool to room temperature, stir at room temperature, refrigerate overnight, precipitate precipitate, filter, wash, and dry.

[0039] Weigh the prescription amount of S-carboxymethyl-L-cysteine ​​inclusion compound, lactose and mannitol mixture, sodium carboxymethyl starch, mix well, pass through 80 mesh sieve, and prepare with hydroxypropyl cellulose ethanol solution Granules, 24 mesh granules, the obtained wet granules are dried, add the prescribed amount of talcum powder, mix evenly, 24 mesh granules, and tablet.

[0040] Weigh the enteric-coated layer material of the recipe amount, disperse ...

Embodiment 3

[0042] S-carboxymethyl-L-cysteine ​​enteric-coated tablet, which contains the following substances in weight ratio:

[0043]

[0044] Preparation method:

[0045] Preparation of S-carboxymethyl-L-cysteine ​​inclusion compound: put an appropriate amount of β-cyclodextrin in a mortar, add 2 times the amount of water to grind, add an appropriate amount of S-carboxymethyl-L-cysteine Amino acid is ground into a paste and obtained after drying.

[0046] Weigh the S-carboxymethyl-L-cysteine ​​inclusion compound of the recipe, microcrystalline cellulose, lactose, mannitol mixture, sodium carboxymethyl starch, after mixing evenly, pass through an 80-mesh sieve, and use hydroxypropyl The methyl cellulose ethanol solution is granulated, granulated at 24 mesh, the obtained wet granules are dried, and the prescription amount of talcum powder is added, mixed evenly, granulated at 24 mesh, and compressed into tablets.

[0047] Weigh the enteric-coated layer material of the recipe amount, ...

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PUM

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Abstract

The invention provides an S-carboxymethyl-L-cysteine ​​inclusion compound. The S-(carboxymethyl)-L-cysteine ​​clathrate of the present invention has a good dispersion effect, can effectively reduce the stimulation of S-(carboxymethyl)-L-cysteine ​​to the digestive tract, and increase the and the stability of its formulations. The enteric-coated preparation containing the clathrate can avoid being destroyed in the acidic environment of the stomach and reduce the irritation to the stomach; it directly reaches the small intestine at the absorption site, dissolves rapidly and releases the active ingredient, increasing the S-carboxymethyl-L- Bioavailability of cysteine.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to an inclusion compound and an enteric-coated preparation thereof. Background technique [0002] S-(carboxymethyl)-L-cysteine, also known as carboxycisteine, was first developed and used clinically by the French Joullie company in 1961. It is a mucolytic drug that can affect the secretion of bronchial glands. Increase the secretion of low-viscosity salivary mucin, reduce the production of high-viscosity fucoidal mucin, and directly act on the disulfide bond of mucin to crack mucin molecules to reduce the viscosity of sputum and make it easier to spit out ; Can improve mucociliary clearance; reduce airway hyperresponsiveness. After CMC enters the body, it is easy to remove the carboxymethyl group to form cysteine, and the sulfhydryl group contained in it can interact with electrophilic groups such as reactive oxygen species (ROS) to exert a direct a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/198A61K9/30A61K9/48A61K9/16A61K47/12A61K47/34A61K47/10A61K47/14A61P11/10A61P11/00A61P11/06
CPCA61K9/1617A61K9/1641A61K9/282A61K9/2853A61K9/4858A61K9/4866A61K31/198
Inventor 王健松王玮肖颖裴泽建朱少璇
Owner GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY
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