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Pioglitazone hydrochloride gallic acid eutectic crystal, preparation method, composition and application thereof

A technology of pioglitazone hydrochloride and gallic acid, which is applied in the field of medicine, can solve the problems of undiscovered pioglitazone hydrochloride gallic acid co-crystal patents or literature reports, low dissolution rate, low dissolution rate, etc., and achieves the advantages of good safety and significant biological The effect of absorbing advantages

Pending Publication Date: 2022-01-18
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pioglitazone hydrochloride is almost insoluble in water and belongs to insoluble drugs. At present, pioglitazone hydrochloride is mainly used as oral tablets, which have the disadvantages of low dissolution rate, low dissolution rate and low bioavailability
[0006] According to domestic and foreign patent and literature searches, no other co-crystal patents or literature reports related to pioglitazone hydrochloride gallic acid have been found

Method used

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  • Pioglitazone hydrochloride gallic acid eutectic crystal, preparation method, composition and application thereof
  • Pioglitazone hydrochloride gallic acid eutectic crystal, preparation method, composition and application thereof
  • Pioglitazone hydrochloride gallic acid eutectic crystal, preparation method, composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Preparation method 1 of pioglitazone hydrochloride and gallic acid co-crystal:

[0065] As shown in the table below, put appropriate amount of pioglitazone hydrochloride and gallic acid (molar ratio 1:1) into a mortar, add appropriate amount of organic solvent, manually grind for an appropriate time, and dry at a certain temperature. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and figure 1 Consistent, indicating that the obtained sample is a co-crystal of pioglitazone hydrochloride and gallic acid.

[0066] The experimental condition example of the preparation method 1 of table 3 pioglitazone hydrochloride and gallic acid cocrystal

[0067]

[0068] Preparation method 2 of pioglitazone hydrochloride and gallic acid co-crystal:

[0069] According to the table below, put appropriate amount of pioglitazone hydrochloride and gallic acid (molar ratio 1:1) into a ball mill jar, add an appropriate amount of organic solvent, select an appropr...

Embodiment 2

[0077] Solubility characteristics of pioglitazone hydrochloride and gallic acid co-crystal:

[0078] Pioglitazone hydrochloride belongs to the poor medicine of water solubility, uses 0.2% SDS aqueous solution to carry out experiment, solvent system has significant difference (f 2 =40.47)( Image 6 ). Refer to the solubility determination method ("Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations (First Draft)", 2012, October Center for Drug Evaluation) for determination. Using high performance liquid chromatography, using the chromatographic peak area data of the sample to calculate the concentration of the sample dissolved, taking the time as the abscissa and the solvent concentration as the ordinate to draw the solubility curve respectively, the data are shown in the following table:

[0079] The dissolution curve data of table 6 pioglitazone hydrochloride and gallic acid cocrystal and pioglitazone hydrochloride in 0.2% SDS aqueous solution

[...

Embodiment 3

[0083] Absorption characteristics and plasma concentration characteristics of pioglitazone hydrochloride and gallic acid co-crystal in rats:

[0084] The SD rats were randomly divided into groups, 5 in each group, free to drink water, and after fasting for 12 hours, the weight of the rats was weighed, according to 20 mg·kg -1 Pioglitazone hydrochloride dosage calculation, pioglitazone hydrochloride and pioglitazone hydrochloride and gallic acid eutectic samples were loaded into the solid dispenser, and the drug powder was directly placed into the stomach of rats through the oral cavity. At 15min, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 36h after administration, blood was taken from the inner canthus of the eye and placed in a heparinized tube at 4°C , centrifuge at 6500rpm for 10min, and store in a -40°C refrigerator for testing. Precisely draw 40 μL of heparin-anticoagulated plasma, place it in a 1.5 mL centrifuge tube, add 10 μL internal standard carbamaze...

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Abstract

The invention belongs to the technical field of medicines, and discloses a pioglitazone hydrochloride and gallic acid eutectic crystal, a preparation method, a pharmaceutical composition and application thereof, specifically a pioglitazone hydrochloride and gallic acid eutectic crystal solid substance state, a preparation method of a pioglitazone hydrochloride and gallic acid eutectic crystal solid substance sample, and application of the pioglitazone hydrochloride and gallic acid eutectic crystal substance as an active ingredient in preparation of drugs for reducing blood sugar and blood fat and relieving or preventing diabetic nephropathy and insulin cell degeneration.

Description

technical field [0001] The invention discloses a cocrystal of pioglitazone hydrochloride and gallic acid, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a co-crystal of pioglitazone hydrochloride and gallic acid; a preparation method of the co-crystal of pioglitazone hydrochloride and gallic acid; the co-crystal of pioglitazone hydrochloride and gallic acid is used as the active ingredient in the preparation of hypoglycemic agents, The application of the drug in reducing blood fat, alleviating or preventing diabetic nephropathy and insulin cell degeneration belongs to the field of medical technology. Background technique [0002] Drug co-crystal refers to the crystal formed by the intermolecular non-covalent interaction force between the active drug molecule and the co-crystal former in a certain ratio. By forming co-crystals, drugs can greatly enrich their crystalline forms on the one hand, and improve their ph...

Claims

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Application Information

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IPC IPC(8): C07D417/12C07C65/03C07C51/43A61K31/4439A61P3/10A61P3/06A61P13/12A61P5/50
CPCC07D417/12C07C65/03C07C51/43A61P3/10A61P3/06A61P13/12A61P5/50C07B2200/13
Inventor 吕扬杜冠华王英孔德文龚宁波杨世颖宋俊科张丽梁宇赵晓悦
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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