Bexarotene and ligustrazine eutectic crystal, and preparation method, composition and application thereof

A kind of technology of ligustrazine and co-crystal, applied in the field of co-crystal formed by bexarotene and ligustrazine

Active Publication Date: 2020-09-29
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

There is no report on the co-crystal of bexarotene

Method used

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  • Bexarotene and ligustrazine eutectic crystal, and preparation method, composition and application thereof
  • Bexarotene and ligustrazine eutectic crystal, and preparation method, composition and application thereof
  • Bexarotene and ligustrazine eutectic crystal, and preparation method, composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Preparation method 1 of bexarotene and ligustrazine cocrystal:

[0068] According to the table below, take appropriate amount of bexarotene and ligustrazine into a mortar, add appropriate amount of organic solvent, manually grind for an appropriate time, and dry at high temperature. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and figure 1 Consistent, indicating that the obtained sample is a cocrystal of bexarotene and ligustrazine.

[0069]

[0070]

[0071] Preparation method 2 of bexarotene and ligustrazine co-crystal:

[0072] According to the table below, take appropriate amount of bexarotene and ligustrazine into a ball mill jar, add an appropriate amount of organic solvent, select an appropriate ball-to-material ratio, set an appropriate speed, grind for an appropriate time, and dry at high temperature. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and figure 1 Consistent, indicating that the obt...

Embodiment 2

[0079] The solubility characteristics of bexarotene and ligustrazine co-crystal and bexarotene API in pure water system were investigated. Refer to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations" for determination, and the model-independent similarity factor (f2) method is used for the comparison of dissolution curves, and the samples of bexarotene and bexarotene and Ligustrazine co-crystal are compared by calculating the f2 value For the similarity of dissolution curves in two solvent systems, when the f2 value is higher than 50, the two curves are considered similar, and when the f2 value is lower than 50, the two curves are considered to be different. In the experiment, the bexarotene sample was used as a reference, and the model-independent similarity factor f2 was calculated. The dissolution percentage adopts the high performance liquid phase method to measure the content of bexarotene at a wavelength of 259nm, and calculates the dissol...

Embodiment 3

[0084] Absorption characteristics and plasma concentration characteristics of bexarotene and ligustrazine cocrystal in rats:

[0085] Twelve SD rats were randomly divided into 2 groups, 6 rats in each group, and were fasted 12 hours before administration without water. Weigh the body weight of the rat, according to 30mg·kg -1 Bexarotene dosage calculation, the bexarotene and bexarotene and Ligustrazine co-crystal samples into the solid drug delivery device, through the mouth of the powder directly into the stomach of rats. At 5min, 15min, 30min, 45min, 1h, 1.5h, 2h, 4h, 8h, 12h, 24h after administration, blood was collected from the inner canthus of the eye, placed in a heparinized tube, centrifuged at 4000rpm for 10min at 4°C, and frozen in - 40 ℃ refrigerator to be tested. Precisely draw 100 μL of plasma from experimental animals at different times, put it in a 1.5 mL centrifuge tube, add 10 μL (10ug / ml) of internal standard (ursolic acid) working solution and vortex for 5...

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Abstract

The invention discloses a bexarotene and ligustrazine eutectic crystal as well as a preparation method, a composition and application thereof. Specifically, the invention discloses a new bexarotene and ligustrazine eutectic crystal, which takes bexarotene as a medicinal active ingredient and ligustrazine as a eutectic crystal precursor. The invention discloses a preparation method of the bexarotene and ligustrazine eutectic crystal. The bexarotene and ligustrazine eutectic crystal is used as a pharmaceutical active ingredient and is applied to preparation of drugs for preventing and treating glioma, skin T-cell lymphoma, breast cancer, psoriasis, Kaposi's sarcoma, lung cancer and Cushing's disease.

Description

technical field [0001] The invention discloses a cocrystal of bexarotene and ligustrazine, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a co-crystal of bexarotene and ligustrazine; a preparation method of the co-crystal of bexarotene and ligustrazine; The application of the components in the preparation of drugs for preventing and treating glioma, skin T-cell lymphoma, breast cancer, psoriasis, Kaposi's sarcoma, lung cancer and Cushing's disease. 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 ligand in a certain ratio. By forming co-crystals, drugs can improve their physical and chemical properties and improve clinical therapeutic effects on the one hand, and on the other hand, co-crystals can enrich their crystalline forms. For chemical generic drugs, the study of co-crystals c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C63/66C07C51/42C07D241/12A61K31/192A61K31/4965A61P35/00A61P17/06A61P5/38
CPCC07C63/66C07D241/12A61K31/192A61K31/4965A61P35/00A61P17/06A61P5/38C07B2200/13A61K2300/00
Inventor 吕扬杜冠华焦凌泰杨世颖孙岚任淑月张宝喜宋俊科于浩莹王海港
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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