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Meloxicam-urea eutectic crystal and preparation method thereof

A technology of urea and co-crystal, which is applied in the field of meloxicam-urea co-crystal and its preparation, and can solve problems such as meloxicam co-crystal that has not yet been seen

Inactive Publication Date: 2020-10-09
SHANDONG FIRST MEDICAL UNIV & SHANDONG ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is no report of meloxicam co-crystal

Method used

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  • Meloxicam-urea eutectic crystal and preparation method thereof
  • Meloxicam-urea eutectic crystal and preparation method thereof
  • Meloxicam-urea eutectic crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation of embodiment 1 meloxicam-urea cocrystal

[0029] Dry grinding: Precisely weigh 0.8785g of meloxicam and 0.15g of urea (the molar ratio of meloxicam and urea is 1:1), put them in a mortar, and grind for 6 hours to obtain the dry grinding eutectic.

Embodiment 2

[0030] The preparation of embodiment 2 meloxicam-urea cocrystal

[0031] Ultrasonic reaction method: Accurately weigh 0.8785g meloxicam and 0.15g urea respectively (the molar ratio of meloxicam and urea is 1:1), add 15mL DMF, respectively, under conditions 1: 250W, 40KHz, temperature 40°C, Reaction at 60°C and 80°C for 2 hours; condition two: 250W, 40KHz, temperature at 60°C, ultrasonic reaction for 1h, 2h, and 3h; condition three: 250W, 200W, 150W, 40KH, temperature at 60°C, ultrasonic reaction for 2h; yellow Transparent solution, DMF was removed by rotary evaporation, and the ultrasonic reaction eutectic was obtained after drying.

Embodiment 3

[0032] The preparation of embodiment 3 meloxicam-urea cocrystal

[0033] Ultrasonic reaction method: Accurately weigh 0.8785g of meloxicam and 0.15g of urea (the molar ratio of meloxicam and urea is 1:1), add 15mL of DMF, and ultrasonically react for 2 hours at 60°C (250W, 40KHz) A yellow transparent solution was obtained, the DMF was removed by rotary evaporation, and the ultrasonic reaction eutectic was obtained after drying.

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Abstract

The invention relates to the field of pharmaceutical co-crystals, in particular to a meloxicam-urea eutectic crystal and a preparation method thereof. The XRD characteristic diffraction peak of the meloxicam-urea eutectic crystal appears at 8.448 + / -0.2 degrees, 13.222 degrees + / -0.2 degrees, 14.896 degrees + / -0.2 degrees, 16.344 degrees + / -0.2 degrees, 17.161 degrees + / -0.2 degrees, 22.302 degrees + / -0.2 degrees, 25.342 degrees + / -0.2 degrees, 27.016 degrees + / -0.2 degrees and 28.179 degrees + / -0.2 degrees. By forming the meloxicam-urea eutectic crystal, the in-vitro release rate of meloxicamis remarkably increased.

Description

technical field [0001] The invention relates to the field of drug co-crystals, in particular to a meloxicam-urea co-crystal and a preparation method thereof. Background technique [0002] Meloxicam is a new type of non-steroidal anti-inflammatory analgesics (NSAIDs), mainly used in the treatment of arthritis and rheumatoid arthritis, with anti-inflammatory, pain, antipyretic and other pharmacological effects, due to its gastrointestinal The adverse reactions of the tract and kidney are significantly lower than those of the same type of drugs, and meloxicam has replaced other non-steroidal anti-inflammatory drugs in most countries. However, meloxicam has poor water solubility and high permeability, so its absorption is poor and its bioavailability is low. At this stage, improving the solubility and bioavailability of poorly soluble drugs is mainly through the preparation of new drug dosage forms, such as liposomes, microemulsions, and co-crystals. [0003] Pharmaceutical co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12C07C273/02C07C273/16A61K31/5415A61P29/00
CPCA61K31/5415A61P29/00C07C273/02C07C273/16C07D417/12
Inventor 李玉琴吕宝兴张亚晴牛景梅张丽清
Owner SHANDONG FIRST MEDICAL UNIV & SHANDONG ACADEMY OF MEDICAL SCI
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