Amorphous taclolimus solid dispersion having an enhanced solubility and pharmaceutical composition comprising same
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A technology of solid dispersion and tacrolimus, which can be used in pharmaceutical combinations, organic active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as low bioavailability
Inactive Publication Date: 2008-01-30
HANMI PHARMA
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Problems solved by technology
Thus, when water-insoluble tacrolimus is orally administered, its bioavailability is inevitably low
Method used
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Embodiment 1
[0063] 400 mg of 2-hydroxypropyl-β-cyclodextrin (Aldrich, USA), 20 mg of citric acid and 20 mg of Poloxamer (Poloxamer) 188 (Lutrol F68, BASF) were added to MC (dichloromethane) and ethanol and stirred until the solution became clear. Then, 400 mg of lactose was added thereto and dispersed evenly. 100 mg of tacrolimus dissolved in ethanol was mixed with the dispersion and spray-dried while the inlet and outlet temperatures of the spray dryer (mini spray dryer B-191, Buchi, Switzerland) were maintained at 60 °C, respectively. °C and 45-50 °C to obtain a solid dispersion of tacrolimus with the ingredients listed in Table 1.
Embodiment 2
[0065] A tacrolimus solid dispersion having the ingredients listed in Table 1 was prepared by repeating the procedure of Example 1 except that 200 mg of 2-hydroxypropyl-β-cyclodextrin was used.
Embodiment 3
[0067] A tacrolimus solid dispersion having the ingredients listed in Table 1 was prepared by repeating the procedure of Example 1 except that 800 mg of 2-hydroxypropyl-β-cyclodextrin was used.
[0068] Table 1
[0069]
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Abstract
An amorphous solid dispersion of tacrolimus comprising tacrolimus, a substituted cyclodextrin derivative and an organic acid, the solid dispersion having high thermodynamic stability and solubility, providing enhanced release rate and bioavailability.
Description
technical field [0001] The present invention relates to an amorphous tacrolimus solid dispersion comprising tacrolimus, a substituted cyclodextrin derivative and an organic acid and a pharmaceutical composition comprising the dispersion, the solid dispersion exhibiting Enhanced bioavailability of tacrolimus. Background technique [0002] Molecular formula (I) is (-)-(1R, 9S, 13R, 14S, 17R, 18E, 21S, 23S, 24R, 25S, 27R)-17-allyl-1,14-dihydroxyl-12-[( E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylvinyl]-23,25-dimethoxy-13,19,21,27 -Tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0 4.9 ] Tacrolimus (or FK-506) of octacos-18-ene-2,3,10,16-tetraketone hydrate [104987-11-3] was proposed by Tanaka and Kuroda et al. (see J. Microlide-based immunosuppressive drugs discovered in Am. Chem. Soc., 109:5031 (1987) and US Pat. No. 4,894,366). [0003] [0004] The U.S. Food and Drug Administration has approved tacrolimus for the suppression of transplant rejection (Prograf) ...
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