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Melbine crystal, medicinal composition of melbine crystal and pioglitazone and preparation method for medicinal composition

A technology of metformin and pioglitazone, which is applied in the field of medicine, can solve problems such as large differences in tablet weight, weaken patient compliance, and gastrointestinal irritation, reduce the amount and type of excipients, save preparation costs and processes, and simplify preparation processes Effect

Active Publication Date: 2013-03-13
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN101721414A improves the dissolution rate of pioglitazone by controlling the particle size of pioglitazone, but in the granulation process of this method, because the required particle size is small, large dust pollution will be generated, which will endanger the health of the staff , and pollute the environment
Moreover, the release rate of pioglitazone and metformin in the medicament prepared by this method is too fast, and there are two problems as follows: on the one hand, the high-concentration pharmaceutical active ingredient is easy to cause gastrointestinal irritation, thereby causing relatively large side effects; , in order to maintain an effective blood concentration, the patient must take the drug several times a day, thus weakening the patient's compliance
Although this method reduces the side effects of metformin by reducing the release rate of metformin, and makes the release rate of pioglitazone and metformin close, the above method needs to use multiple auxiliary materials on the one hand, thereby increasing drug costs and manufacturing processes; , the equipment requirements are too high in the preparation process of double-layer tablets, and there are often quality problems such as large differences in tablet weight and high friability, which limit the application of this type of method

Method used

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  • Melbine crystal, medicinal composition of melbine crystal and pioglitazone and preparation method for medicinal composition
  • Melbine crystal, medicinal composition of melbine crystal and pioglitazone and preparation method for medicinal composition
  • Melbine crystal, medicinal composition of melbine crystal and pioglitazone and preparation method for medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] [Example 1] Preparation of metformin crystals

[0050] 1) dissolving metformin powder in a water / ethanol mixed solution to form a metformin solution;

[0051] 2) Under stirring, add chloroform dropwise to the metformin solution prepared in step 1) until it becomes turbid;

[0052] 3) heating the turbid solution obtained in step 2) under an ultrasonic field until the solution becomes clear, and filtering;

[0053] 4) Leave the filtrate obtained in step 3) until the product precipitates, filter, wash the filter cake with anhydrous chloroform, and dry in vacuum to obtain metformin crystals.

[0054] The particle diameter of the metformin crystals obtained is 80 μm, and the X-ray powder diffraction pattern (see figure 1 ) in the characteristic peaks are displayed at 2θ of 11.2, 12.8, 14.9, 15.2, 15.3, 18.8, 22.8, 23.5, 26.6.

Embodiment 2

[0055] [Example 2] Preparation of metformin crystals

[0056] 1) Dissolve metformin powder in a water / ethanol mixed solution with a volume ratio of 1:8 to make a concentration of 10mol L -1 metformin solution;

[0057] 2) Under stirring, at 25°C, add chloroform dropwise to the metformin solution prepared in step 1) at a rate of 1ml / min until it becomes turbid;

[0058] 3) Heat the turbid solution obtained in step 2) to 40° C. under an ultrasonic field until the solution becomes clear, and filter;

[0059] 4) Stand the filtrate obtained in step 3) at 20° C. for 2 days until the product precipitates, filter, wash the filter cake with anhydrous chloroform, and dry in vacuum to obtain metformin crystals.

[0060] The obtained metformin crystals have a particle size of 60 μm, and the X-ray powder diffraction pattern measured by Cu-Kα rays is consistent with that of Example 1.

Embodiment 3

[0061] [Example 3] Preparation of metformin crystals

[0062] 1) Dissolve metformin powder in a water / ethanol mixed solution with a volume ratio of 1:3 to make a concentration of 25mol L -1 metformin solution;

[0063] 2) Under stirring, at 15°C, add chloroform dropwise to the metformin solution prepared in step 1) at a rate of 3ml / min until it becomes turbid;

[0064] 3) Heating the turbid solution obtained in step 2) to 50° C. under an ultrasonic field until the solution becomes clear, and filtering;

[0065] 4) Stand the filtrate obtained in step 3) at 25° C. for 2 days until the product precipitates, filter, wash the filter cake with anhydrous chloroform, and dry in vacuum to obtain metformin crystals.

[0066] The obtained metformin crystals have a particle size of 100 μm, and the X-ray powder diffraction pattern measured by Cu-Kα rays is consistent with that of Example 1.

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Abstract

The invention discloses a melbine crystal, a medicinal composition of the melbine crystal and pioglitazone and a preparation method for the medicinal composition. The medicinal composition consists of medicinal active ingredients and pharmaceutic adjuvants, wherein the medicinal active ingredients comprise the following components in part by weight: 5 to 30 parts of pioglitazone and 200 to 800 parts of melbine, and the melbine is the melbine crystal; and the pharmaceutic adjuvants comprise a filling agent, a disintegrating agent, an adhesion agent and a lubricating agent. The medicinal composition has the characteristics of safety, effectiveness and low cost, and particularly only ordinary matrix materials are used, so the dissolution rate of the melbine is reduced, a sustained-release effect is achieved, and the side effect of the medicinal composition is reduced; and the melbine and the pioglitazone can be released synchronously, a synergetic effect of the melbine and the pioglitazone is enhanced, and a curative effect is improved further.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a metformin crystal, a pharmaceutical composition thereof and pioglitazone, and a preparation method thereof. Background technique [0002] Pioglitazone, its chemical name is: 5-{4-[2-(5-ethyl-2-pyridine)-ethoxy]-phenyl}-2,4-thiazolidinedione hydrochloride. Molecular formula: C 19 h 20 N 2 o 3 S HCl, molecular weight: 392.90, its structural formula is as follows: [0003] [0004] Pioglitazone is a thiazolidinedione antidiabetic drug, which is an insulin sensitizer. The mechanism of action is related to the presence of insulin. It can reduce insulin resistance in peripheral tissues and liver, increase insulin-dependent glucose processing, and reduce glycogen output. Unlike sulfonylureas, its mechanism of action is a highly selective activation of peroxisome growth factor-activated receptor-γPPAR-γ1, and the activation of PPAR-γ can regulate many insulin-relat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4439
Inventor 王小树钟正明罗韬马鹰军
Owner HAINAN JINRUI PHARMA CO LTD