Tamibarotene cyclodextrin or cyclodextrin derivative clathrate and preparation method thereof
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A technology of tamibarotene and cyclodextrin, applied in the field of medicine, can solve the problems of poor oral absorption, difficult oral or injection administration, etc., and achieves the effects of good dissolution, good clinical application and high bioavailability
Inactive Publication Date: 2014-11-26
SHANDONG UNIV
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[0006] Aiming at the above-mentioned prior art, in order to solve the technical problems in the prior art that tamibarotene is insoluble in water, has poor oral absorption, and is difficult to be administered orally or by injection, the present invention provides tamibarotene cyclodextrin or cyclodextrin Derivative inclusion compound, its preparation method, pharmaceutical composition containing tamibarotene cyclodextrin or cyclodextrin derivative inclusion compound and its use in the preparation of medicines
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Embodiment 1
[0028] Example 1 Preparation of Liquid Tamibarotene Hydroxypropyl-β-Cyclodextrin Inclusion Complex Solution
[0029] Proceed as follows:
[0030] (1) Weigh 61 mg of hydroxypropyl-β-cyclodextrin, pour into 5 ml of distilled water, and stir to dissolve.
[0031] (2) Also known as Tamibarotene 5mg, add 5ml of absolute ethanol to dissolve, and pour this solution into the above-mentioned hydroxypropyl-β-cyclodextrin solution.
[0032] (3) The mixed solution was stirred at 45°C for 1 hour by magnetic stirring method, the ethanol was removed by rotary evaporation under reduced pressure, and the unincluded drug was removed by filtration to obtain the inclusion complex of tamibarotene hydroxypropyl-β-cyclodextrin derivative substance solution.
Embodiment 2
[0033] Example 2 Preparation of Solid Tamibarotene Hydroxypropyl-β-cyclodextrin Inclusion Compound
[0034] Proceed as follows:
[0035] (1), (2), (3) are the same as embodiment 1.
[0036] (4) Freeze-drying the inclusion compound solution of the tamibarotene hydroxypropyl-β-cyclodextrin derivative to obtain a solid tamibarotene hydroxypropyl-β-cyclodextrin inclusion compound.
Embodiment 3
[0037] Example 3 Preparation of Solid Tamibarotene Hydroxypropyl-β-cyclodextrin Inclusion Compound
[0038] Proceed as follows:
[0039] (1) Weigh 122mg of hydroxypropyl-β-cyclodextrin, put it into a mortar, add 2ml of distilled water, and grind to make a paste;
[0040] (2) Another 10 mg of tamibarotene was weighed, dissolved in 2 ml of absolute ethanol, and poured into the above-mentioned hydroxypropyl-β-cyclodextrin solution.
[0041] (3) The mixture was ground for 2 hours to obtain a uniform paste, which was filtered and evaporated to dryness under reduced pressure to obtain the inclusion compound of a solid tamibarotene cyclodextrin derivative.
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Abstract
The invention discloses a tamibarotene cyclodextrin or cyclodextrin derivative clathrate which is prepared from tamibarotene and cyclodextrin or a cyclodextrin derivative, the molar ratio of tamibarotene to cyclodextrin or cyclodextrin derivative is 1:1-1:100, and the preparation method is as follows: the cyclodextrin or cyclodextrin derivative is added to a solvent to produce a solution or suspension, and then the tamibarotene is added for stirring, grinding or ultrasonic mixing to obtain the tamibarotene cyclodextrin or cyclodextrin derivative clathrate; or the cyclodextrin or cyclodextrin derivative is put in a colloid mill or mortar, a solvent is added for stirring to make a paste, then the tamibarotene is added into the paste for grinding for 1-5 hours to obtain a homogeneous thick paste, and the tamibarotene cyclodextrin or cyclodextrin derivative clathrate is obtained by filtration, concentration or freeze drying. The invention also discloses a tamibarotene-containing composition. The tamibarotene cyclodextrin or cyclodextrin derivative clathrate improves the solubility and dissolution rate of the tamibarotene, has good water solubility, less vascular stimulation, quick disintegration, higher bioavailability and other characteristics.
Description
technical field [0001] The present invention relates to tamibarotene cyclodextrin or cyclodextrin derivative inclusion compound, its preparation method, pharmaceutical composition containing tamibarotene cyclodextrin or cyclodextrin derivative inclusion compound and its use in the preparation of medicines . It belongs to the field of medical technology. Background technique [0002] Tamibarotene (Tamibarotene, Am80), the chemical name is 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)carbamoyl] benzoic acid. It is colorless prism or white crystalline powder, easily soluble in tetrahydrofuran and dichloromethane, insoluble in water. Its structural formula is as follows: [0003] [0004] Tamibarotene is a new selective retinoic acid α receptor enhancer developed by Nippon Shinyaku, which is suitable for the treatment of relapsed or refractory acute promyelocytic leukemia. Tamibarotene tablet, listed in Japan in June 2005 (trade name: Amnolake), has the characte...
Claims
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Application Information
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