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Sustained release tablet containing high water-soluble active ingredients and preparation method thereof

A technology for sustained-release tablets and active ingredients, applied in the field of sustained-release tablets containing highly water-soluble active ingredients and its preparation, can solve gastrointestinal mucosal irritation, lactic acidosis, high concentration of highly water-soluble active ingredients, Problems such as large differences in tablet release rates between batches, to achieve the effects of reducing the burden of medication, good drug compliance, and low cost

Active Publication Date: 2016-03-30
华益泰康药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] For highly water-soluble active ingredients, ordinary tablets have the following disadvantages: (1) Highly water-soluble active ingredients are easily soluble in water, and the drug dissolves rapidly after oral administration, and a large amount of drugs are only partially absorbed in the small intestine when they pass through the gastrointestinal tract , leading to low bioavailability; (2) The concentration of highly water-soluble active ingredients in the gastrointestinal tract is too high, which will cause obvious irritation to the gastrointestinal mucosa and adverse reactions such as lactic acidosis; (3) Ordinary tablets need daily Many times of oral administration, poor compliance, and forgetting to take the medicine will affect the effect of the medicine
Tablets produced by this manufacturing method have large variations in release rate between batches, which can affect their efficacy and safety

Method used

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  • Sustained release tablet containing high water-soluble active ingredients and preparation method thereof
  • Sustained release tablet containing high water-soluble active ingredients and preparation method thereof
  • Sustained release tablet containing high water-soluble active ingredients and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] The prescription is shown in Table 1:

[0057] Table 1: Prescription for 1000 Metformin Hydrochloride Sustained Release Tablets (750mg / tablet)

[0058]

[0059] Put the highly water-soluble active ingredient metformin hydrochloride and the first sustained-release material carboxymethylcellulose sodium in the wet mixing granulator according to the prescription amount in the above table, set the stirring speed to 200-250 rpm, and the cutting knife speed 2000-3000 rpm, after dry mixing, gradually add appropriate amount of purified water to make granules of suitable size, and then add the second slow-release material hypromellose K100MCR in a granulation pot for granulation. The prepared wet granules were moved to a fluidized bed for drying, and the material temperature was 50° C., and passed through a 1.5 mm sieve to obtain granules containing metformin hydrochloride. The lubricant in the prescribed amount is passed through a 20-mesh sieve and mixed evenly with the abo...

Embodiment 2

[0061] The prescription is as shown in Table 2:

[0062] Table 2: Prescription for 1000 niacin sustained-release tablets (750mg / tablet)

[0063]

[0064]

[0065] Sustained-release tablets were prepared by the same preparation method as in Example 1.

Embodiment 3

[0067] The prescription is shown in Table 3:

[0068] Table 3: Prescription for 1000 divalproex sodium sustained-release tablets (500mg / tablet)

[0069]

[0070] A sustained-release tablet was prepared by the same preparation method as in Example 1, except that the second sustained-release material was added together with the diluent.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations and particularly relates to a sustained release tablet containing high water-soluble active ingredients and a preparation method thereof. The sustained release tablet comprises, by weight percentage, 45%-70% of high water-soluble active ingredients, 0.3%-4% of first sustained-release material, 27%-51% of second sustained-release material, 0-18% of diluent and 0.1%-1.0% of lubricant. The first sustained-release material and the second sustained-release material can be the same or different and are selected from one or more of hydroxypropyl methylcellulose, hydroxy propyl cellulose, sodium carboxymethyl cellulose, carmellose calcium, povidone, carbomer and polyoxyethylene. Compared with the existing sustained release tablet, the sustained release tablet containing the high water-soluble active ingredients is good in compressibility, low in cost and good in quality, and the hardness cannot be reduced after long-term storage.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a slow-release tablet containing highly water-soluble active ingredients and a preparation method thereof. Background technique [0002] For highly water-soluble active ingredients, ordinary tablets have the following disadvantages: (1) Highly water-soluble active ingredients are easily soluble in water, and the drug dissolves rapidly after oral administration, and a large amount of drugs are only partially absorbed in the small intestine when they pass through the gastrointestinal tract , leading to low bioavailability; (2) The concentration of highly water-soluble active ingredients in the gastrointestinal tract is too high, which will cause obvious irritation to the gastrointestinal mucosa and adverse reactions such as lactic acidosis; (3) Ordinary tablets need daily Many times of oral administration, poor compliance, and forgetting to take the medicine wil...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/38A61K47/34A61K47/32A61K47/12A61K31/155A61K31/455A61K31/20
CPCA61K9/0002A61K9/2027A61K9/2031A61K9/2054A61K31/155A61K31/20A61K31/455
Inventor 徐国杰高春荣诸弘刚谭海松
Owner 华益泰康药业股份有限公司
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