Pinocembrin and cyclodextrin or cyclodextrin derivative inclusion compound
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A technology of cyclodextrin and pinacol, applied in the field of medicine, can solve the problems of difficulty in oral administration or injection, insolubility in water, poor oral absorption, etc., and achieves the advantages of clinical application, good safety and good dissolution. Effect
Active Publication Date: 2009-09-23
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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[0008] In order to solve the technical problems that pinoquinone is insoluble in water, has poor oral absorption, and is di...
Method used
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[0042] (1) Weigh 40g of hydroxypropyl-β-cyclodextrin, pour it into 400ml of distilled water, and stir to dissolve;
[0043] (2) Another 1 g of pinocin was weighed, dissolved in 20 ml of absolute ethanol, and poured into the above-mentioned hydroxypropyl-β-cyclodextrin solution;
[0044] (3) The mixed solution was stirred at 40-50° C. for 20 minutes by magnetic stirring method, and the solution was observed until it was clear and transparent, and the clathrate solution of pinenin hydroxypropyl-β-cyclodextrin derivative was obtained.
Embodiment 2
[0045] Example 2: Preparation of solid pinenin hydroxypropyl-β-cyclodextrin inclusion compound
[0046] (1), (2), (3) are the same as embodiment 1.
[0047] (4) Freeze-drying the clathrate solution of the pinacetin hydroxypropyl-β-cyclodextrin derivative to obtain a solid pinacetin hydroxypropyl-beta-cyclodextrin inclusion complex.
Embodiment 3
[0048] Embodiment 3: Preparation of solid pinenin hydroxypropyl-β-cyclodextrin inclusion compound
[0049] (1) Weigh 20g of hydroxypropyl-β-cyclodextrin, put it into a mortar, add 100ml of distilled water, and grind to make a paste;
[0050] (2) Another 3 g of pinocin was weighed, dissolved in 20 ml of absolute ethanol, and the solution was poured into the above-mentioned hydroxypropyl-β-cyclodextrin solution;
[0051] (3) Grinding the mixed liquid for 2 hours to obtain a uniform paste, filtering, and evaporating to dryness under reduced pressure to obtain a solid clathrate of pinasin cyclodextrin derivatives.
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Abstract
The invention discloses a pinocembrin and cyclodextrin or cyclodextrin derivative inclusion compound, wherein cyclodextrin or a cyclodextrin derivative is used to include the pinocembrin. The inclusion compound contains the pinocembrin and the cyclodextrin or cyclodextrin derivative in a molar ratio of 1:1-100. The inclusion compound can improve the water solubility of the pinocembrin and give good play of the therapeutic action of the pinocembrin. The inclusion compound is suitable for the preparation of sold dosage forms and liquid dosage forms required by clinics, including infusion solution, water injection, powder injection, oral solution, syrup, tablets, capsules, granules and dispersible tablets. The inclusion compound can be used for preparing drugs for preventing and\or treating cardiovascular and cerebrovascular diseases, particularly brain stroke, as well as drugs for preventing and\or treating bacterial and\or fungal infections.
Description
technical field [0001] The present invention relates to clathrates of pinustin cyclodextrin or cyclodextrin derivatives, a preparation method thereof, pharmaceutical compositions containing such clathrates of pinustin cyclodextrins or cyclodextrin derivatives and in the preparation of medicines the use of. It belongs to the field of medical technology. Background technique [0002] Pinocembrin, also known as pinocembrin, pinocin, chemical name 5,7-dihydroxyflavanone (5,7-Dihydroxyflavanone), 2,3-dihydro-5,7-dihydroxy-2- Phenyl-4H-1-benzopyran-4-one (2,3-Dihydro-5,7-dihydroxy-2-phenyl-4H-1-benzopyran-4-one), is a water-insoluble Dihydroflavonoids, the structure is as follows: [0003] [0004] There is a chiral center in the chemical structure of pinine, the three-dimensional structure of natural pinine is S configuration, and the specific rotation [α] D 15 It is -45.3 (c, 0.9, acetone is the solvent). [0005] (S)-pinoquinone is a natural product extracted from prop...
Claims
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