Celecoxib-carbamazepine eutectic crystal, preparation method, pharmaceutical composition and application
A carbamazepine co-crystal and celecoxib technology, which is applied in the direction of drug combination, organic chemical methods, and active ingredients of heterocyclic compounds, can solve the problems of poor drug stability, low bioavailability, and large solubility differences, etc. problems, to achieve excellent drug dissolution-release properties, simple preparation method, and easy operation
Pending Publication Date: 2022-05-24
CHINA PHARM UNIV
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Problems solved by technology
[0005] Purpose of the invention: for the low bioavailability, large toxic and side effects, and poor patient compliance when carbamazepine is used as a single drug, the short half-life and poor patient compliance when celecoxib is used as a single drug, and the drugs that exist when multiple drugs are used in combination The disadvantages such as poor stability, large solubility difference, poor compatibility and the like, the present invention aims to provide a celecoxib-carbamazepine co-crystal with excellent drug synergistic dissolution-release characteristics, preparation Methods, pharmaceutical compositions and uses
Method used
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Experimental program
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Effect test
Embodiment 1
[0050] At room temperature, the raw materials of celecoxib (100 mg) and carbamazepine (62 mg) were dissolved in 10 ml of toluene solution by ultrasonic, filtered with a 0.45 μm filter, and slowly volatilized at room temperature to obtain celecoxib and carbamazepine. Cocrystal of Marzepine.
Embodiment 2
[0052] At room temperature, celecoxib (1.14g) and carbamazepine (0.71g) were dissolved by ultrasonic in 500ml toluene solution, filtered with a 0.45μm filter, and rotary evaporated at 65°C to obtain celecoxib. Cloth and carbamazepine drug co-crystal.
Embodiment 3
[0054] At room temperature, weigh 100 mg of celecoxib and 62 mg of carbamazepine, add 0.5 ml of tetrahydrofuran solution to it, form a suspension, stir for 1 day, and dry at 40 °C for 24 hours to obtain celecoxib and carbamazepine Co-crystal of zepine medicine.
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Abstract
The invention discloses a celecoxib-carbamazepine eutectic crystal, a preparation method, a pharmaceutical composition and an application of the celecoxib-carbamazepine eutectic crystal. In the eutectic crystal, the molar ratio of celecoxib to carbamazepine is (1: 2)-(2: 1). On the basis of retaining molecular structures and biological activities of celecoxib and carbamazepine, the co-crystal and the pharmaceutical composition thereof have excellent synergistic dissolution-release properties, so that the medicine has a more excellent clinical application effect, the preparation method of the co-crystal is simple and convenient and easy to operate, and the prepared co-crystal is high in purity and good in stability. And a preparation method suitable for industrial scale is developed.
Description
technical field [0001] The invention relates to a celecoxib-carbamazepine co-crystal, a preparation method, a pharmaceutical composition and an application, in particular to a celecoxib-carbamazepine with excellent dissolution-release properties, safety, effectiveness and convenient preparation Zepine co-crystal, preparation method, pharmaceutical composition and application. Background technique [0002] Epilepsy is a type of central system disease and one of the intractable diseases reported by the World Health Organization. Its specific pathogenesis is still unclear. A considerable proportion of patients develop resistance to antiepileptic drugs and are difficult to control. Carbamazepine (CBZ) is an anti-epileptic and anti-convulsant drug, and its pharmacological effects are anti-convulsant, anti-epileptic, anti-neuropathic pain, anti-mania-depression, improve the symptoms of certain psychiatric diseases, anti-central urinary collapse. Carbamazepine is a BCS class II ...
Claims
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Patent Timeline
Login to View More IPC IPC(8): C07D231/12C07D223/22A61K31/635A61K31/55A61P29/00A61P19/02A61P37/06A61P25/00A61P15/00A61P3/10A61P25/28A61P31/22A61P25/18A61P25/24A61P13/00A61P25/32A61P37/08A61P21/00
CPCC07D231/12C07D223/22A61K31/635A61K31/55A61P29/00A61P19/02A61P37/06A61P25/00A61P15/00A61P3/10A61P25/28A61P31/22A61P25/18A61P25/24A61P13/00A61P25/32A61P37/08A61P21/00C07B2200/13A61K2300/00
Inventor 蔡挺陈安崔施文蔡佩珊
Owner CHINA PHARM UNIV
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