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Nifedipine and rosuvastatin calcium co-amorphous drug as well as preparation method and application thereof

A technology of rosuvastatin calcium and nifedipine, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations of non-active ingredients, etc., which can solve problems such as difficult drug dissolution, difficult drug diffusion, and impact on transmembrane transport. Achieve the effects of improving solubility, strong operability, and improving bioavailability

Active Publication Date: 2020-10-09
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For nifedipine, the low solubility and strong hydrophobicity not only make it difficult for the drug to diffuse in the mucous layer and immobile water layer, affecting transmembrane transport, but most importantly, it makes it difficult for the drug to dissolve in the digestive juice of the gastrointestinal tract middle

Method used

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  • Nifedipine and rosuvastatin calcium co-amorphous drug as well as preparation method and application thereof
  • Nifedipine and rosuvastatin calcium co-amorphous drug as well as preparation method and application thereof
  • Nifedipine and rosuvastatin calcium co-amorphous drug as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Take by weighing 34.633mg (0.1mmol) of nifedipine raw material, 100.114mg (0.1mmol) of rosuvastatin calcium raw material, at room temperature, put the two kinds of weighed raw materials into the grinding bowl (volume: 10ml) Take an appropriate amount of mixed raw materials in an aluminum crucible, place the crucible on a hot stage with a temperature of 180 ° C, melt the raw materials for 2 minutes, remove the crucible from the hot stage, and place it on an iron block at room temperature On quenching, the co-amorphous drug of nifedipine and rosuvastatin calcium was obtained.

[0050] For the co-amorphous form of nifedipine-rosuvastatin calcium obtained in this embodiment, use an X-ray powder diffractometer, produced by Bruker, Germany, the model is D8 Advance, Cu-kα, tube voltage 40kV, tube current 40mA, step size 0.08, scanning range 10-50°, room temperature. The obtained diffraction pattern is as figure 1 shown. FTIR test, spectrum such as figure 2 As shown, the c...

Embodiment 2

[0055] Take nifedipine raw material 34.633mg (0.1mmol), simvastatin raw material 41.857 mg (0.1mmol), at room temperature, put the two weighed raw materials into the grinding bowl (volume: 10ml) of the mixing cryogenic grinder and mix them well, take an appropriate amount of mixed raw materials in an aluminum crucible, and place the crucible in The temperature was 180°C on a hot stage, the raw materials were melted and kept for 2 minutes, the crucible was removed from the hot stage, and placed on an iron block at room temperature for quenching to obtain the co-amorphous drug of nifedipine and simvastatin.

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Abstract

The invention provides a nifedipine and rosuvastatin calcium co-amorphous drug as well as a preparation method and application thereof, the nifedipine and rosuvastatin calcium co-amorphous drug is formed by combining nifedipine and rosuvastatin calcium according to a molar ratio of 1: 0.9-1.1, Cu-kalpha radiation is used, and an X-ray powder diffraction spectrum expressed by degree 2theta has no sharp diffraction peak; and the glass transition temperature is 89.4 + / -0.2 DEG C. The preparation method is a melting-quenching method. The amorphous drug provided by the invention effectively improves the solubility of nifedipine in an aqueous solution. The solubility of amorphous nifedipine is about six times of the solubility of crystalline nifedipine and the solubility of nifedipine after dissolution equilibrium is about three times of the solubility of crystalline nifedipine in an aqueous solution with the pH value of 6.8 at the beginning of a solubility peak moment. According to the nifedipine-rosuvastatin calcium provided by the invention, the condition of poor solubility of nifedipine can be effectively improved, and the bioavailability of the medicine is improved.

Description

technical field [0001] The invention relates to a co-amorphous drug of nifedipine and rosuvastatin calcium, a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Cardiovascular and cerebrovascular diseases are a general term for cardiovascular diseases and cerebrovascular diseases. These diseases are caused by high blood pressure, diabetes, dyslipidemia and other reasons. Among them, high blood pressure and high blood fat can not only lead to cardiovascular and cerebrovascular diseases, but also have a close relationship between the two. On the one hand, some hypertensive patients ar...

Claims

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Application Information

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IPC IPC(8): C07D211/90C07D239/42A61K31/4422A61K31/505A61K47/55A61P9/12A61P3/06
CPCC07D211/90C07D239/42A61K31/4422A61K31/505A61K47/55A61P9/12A61P3/06
Inventor 王蕾王新园陶绪堂谢冠英宋舒虹
Owner SHANDONG UNIV