Pharmaceutical composition containing repaglinide and preparation method thereof

A composition and drug technology, applied in the field of medicine, can solve the problems of gastrointestinal mucosal side effects, poor water solubility and dissolution stability of repaglinide, etc., and achieve the effect of improving water solubility, good dissolution stability and easy control

Active Publication Date: 2022-07-01
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The purpose of the present invention is to solve the technical problems of repaglinide in the prior art, such as poor water solubility, uneven content, poor dissolution stability, and easy to cause toxic and side effects of gastrointestinal mucosa by adding surfactants, and provide a fast dissolution, uniform content and other technical problems. , the dissolution stability is good, and the process is simple and easy to control, and the repaglinide composition and preparation method thereof suitable for industrial production

Method used

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  • Pharmaceutical composition containing repaglinide and preparation method thereof
  • Pharmaceutical composition containing repaglinide and preparation method thereof
  • Pharmaceutical composition containing repaglinide and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-8

[0033] (1) Preparation of co-micropowder

[0034]

[0035] As shown in the table above, after sieving meglumine, repaglinide was weighed according to the mass ratio and mixed with meglumine, and the micropowder parameters were set for co-micropowder to obtain co-micropowder of different particle sizes.

[0036] (2) Prescription

[0037]

[0038]

[0039] (3) Preparation method

[0040] According to the above table, weigh the co-micron powder and add the auxiliary materials. After mixing, dry granulation. Control the oil pressure of 60-70 bar, the roller speed of 9 rpm, the gap between the rollers of 0.8-1.2 mm, the granulating screen of 0.8 mm, and the speed of granulating. 250 rpm, add the adjuncts, mix well and press into tablets.

Embodiment 9

[0042] The recipe and process of Example 4 were used for scale-up production, with a scale of 100,000 / batch, and three batches were produced in parallel.

experiment example 10

[0066] Experimental Example 10: Dissolution Profile

[0067] According to the dissolution test method (the second method of four general rules of Chinese Pharmacopoeia 2020 edition), add water to 900 mL of pH5.0 citric acid / phosphate buffer (10.2 g of citric acid monohydrate and 18.16 g of disodium hydrogen phosphate dihydrate). Dissolve to 1000mL) as the dissolution medium, set the rotation speed to 75rpm, operate according to the law, take an appropriate amount of the solution at 5min, 10min, 15min and 30min respectively, filter, take the subsequent filtrate as the test solution, according to the import drug registration of repaglinide tablets Standard (JX20120236) chromatographic conditions under the content determination item, set the injection volume to 100 μL, and record the chromatogram; another about 22 mg of repaglinide reference substance, accurately weighed, placed in a 100 mL volumetric flask, dissolved in methanol and diluted to the mark , shake well, accurately m...

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Abstract

The invention provides a pharmaceutical composition containing repaglinide and a preparation method thereof. The preparation method of the repaglinide pharmaceutical composition includes: firstly co-micropowdering repaglinide and meglumine, and then dry granulating to obtain repaglinide-containing granules. The invention improves the water solubility of the poorly soluble drug repaglinide, and the prepared composition has uniform content of active components and good dissolution stability, avoids the use of surfactants, reduces the toxic and side effects of the preparation, and does not cause any problems in the preparation process. There will be the problem of sticking and pressing rollers. The co-micron powder and dry granulation process is simple and easy to control, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and mainly relates to a repaglinide-containing pharmaceutical composition and a preparation method thereof. Background technique [0002] Repaglinide (Repaglinide) is a non-sulfonylurea insulin secretagogue, also known as "meal blood sugar regulator". By binding to specific receptors on islet β cells, the ATP-dependent potassium channels in the β cell membrane are closed, the β cells are depolarized, the calcium channels are opened, and the influx of calcium ions is increased, thereby inducing insulin in the β cells. secretion. Its effect is faster than that of sulfonylureas, so the hypoglycemic effect after meals is faster, and it is the first blood sugar regulating drug to be taken with meals. Repaglinide has strong activity and small size, and each tablet contains 0.5mg, 1mg or 2mg. Repaglinide is rapidly absorbed and takes effect quickly after pre-prandial administration, stimulates insul...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/451A61K9/20A61K47/36A61K47/32A61P3/10A61P5/50A61K9/14A61K9/16A61K47/18
CPCA61K31/451A61K9/2059A61K9/2095A61K9/2027A61K9/0053A61P3/10A61P5/50A61K9/145A61K9/1652
Inventor 卢良华刘佳
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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