Bexarotene and polyvinylpyrrolidone co-amorphous substance, preparation method, composition and use thereof

A technology of polyvinylpyrrolidone and polyvinylpyrrolidone is applied in the field of co-amorphous substances, and achieves the effect of effective treatment, good safety and the advantages of finished medicine, and the effect of improving blood drug concentration

Active Publication Date: 2022-05-17
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There is no report on the co-crystal of bexarotene

Method used

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  • Bexarotene and polyvinylpyrrolidone co-amorphous substance, preparation method, composition and use thereof
  • Bexarotene and polyvinylpyrrolidone co-amorphous substance, preparation method, composition and use thereof
  • Bexarotene and polyvinylpyrrolidone co-amorphous substance, preparation method, composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Preparation method 1 of bexarotene and polyvinylpyrrolidone co-amorphous substance:

[0062] According to the table below, take an appropriate amount of bexarotene and polyvinylpyrrolidone and put them into a ball mill jar at a mass ratio of 1:1, select an appropriate ball-to-material ratio, set an appropriate speed, and grind for an appropriate time. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and figure 1 Consistent, indicating that the obtained sample is co-amorphous of bexarotene and polyvinylpyrrolidone.

[0063] Table 3 Preparation method parameters of bexarotene and polyvinylpyrrolidone co-amorphous

[0064]

[0065] Preparation method 2 of bexarotene and polyvinylpyrrolidone co-amorphous substance:

[0066] Get 3 parts of bexarodene 20g, and weigh 4g, 20g, and 100g of polyvinylpyrrolidone according to the mass ratio of 5:1, 1:1, and 1:5, respectively, and put them into a ball mill jar respectively, and select a ball-to-materia...

Embodiment 2

[0068] The solubility characteristics of bexarotene and polyvinylpyrrolidone co-amorphous substance and bexarotene API in pure water system were investigated. Refer to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations" for determination, the model-independent similarity factor (f2) method is used for the comparison of dissolution curves, and the comparison of bexarotene and bexarotene with polyvinylpyrrolidone co-amorphous When the f2 value is higher than 50, the two curves are considered to be 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 dissolution percentage by the external standard method. Take time as the ab...

Embodiment 3

[0072] Absorption characteristics and plasma concentration characteristics of bexarotene and polyvinylpyrrolidone co-amorphous substance in rats:

[0073] 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 The dose calculation of bexarotene was carried out. The sample of bexarotene and the co-amorphous substance of bexarotene and polyvinylpyrrolidone was loaded into a solid dispenser, and the powder was directly placed into the stomach of the rat through the oral cavity. 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,...

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Abstract

The invention discloses a co-amorphous product of bexarotene and polyvinylpyrrolidone, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a new co-amorphous form formed by bexarodene and polyvinylpyrrolidone; a preparation method of co-amorphous form of bexarotene and polyvinylpyrrolidone; Application of the amorphous form as an active ingredient of a drug in the preparation of drugs for the prevention and treatment of 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 co-amorphous product of bexarotene and polyvinylpyrrolidone, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a co-amorphous product formed by bexarodene and polyvinylpyrrolidone; a preparation method of a co-amorphous product of bexarodene and polyvinylpyrrolidone; a co-amorphous product of bexarodene and polyvinylpyrrolidone The application of the amorphous substance as a drug active ingredient in the preparation of drugs for the prevention and treatment of neuroglioma, skin T-cell lymphoma, breast cancer, psoriasis, Kaposi's sarcoma, lung cancer and Cushing's disease. Background technique [0002] Co-amorphous drugs refer to the amorphous substances formed by intermolecular non-covalent interaction forces between active drug molecules and co-amorphous ligands in a certain ratio. By forming a co-amorphous form of a drug, on the one hand, it can improve its physica...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C63/66A61K31/192A61K31/79A61P35/00A61P17/06A61P5/38
CPCC07C63/66A61P35/00A61P17/06A61P5/38C07B2200/13
Inventor 杜冠华吕扬孙岚任淑月杨世颖焦凌泰宋俊科张丽王景荣周启蒙
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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