Improvement of Dissolution Rate and Oral Bioavailability of a Sparingly Water-Soluble Drug, (.+-.)-5-((2-(2 Naphthalenylmethyl)-5-benzoxazolyl)-methyl)-2,4-thiazolidinedione, in Co-ground Mixture with D-Mannitol.

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  • Improvement of Dissolution Rate and Oral Bioavailability of a Sparingly Water-Soluble Drug,(±)-5-〔〔2-(2-Naphthalenylmethyl)-5-benzoxazolyl〕methyl〕-2,4-thiazolidinedione,in Co-ground Mixture with D-Mannitol
  • Improvement of Dissolution Rate and Ora

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We investigated the usefulness and efficiency of the co-grinding method with D-mannitol to improve the bioavailability of a sparingly water-soluble drug, (±)-5-[[2-(2-naphthalenylmethyl)-5-benzoxazolyl]methyl]-2, 4-thiazolidinedione (174), and compared it with those of the single-grinding method.The co-ground mixtures in drug/carrier weight ratios up to 1 : 5 gave fine particle sizes of less than about 3 μm, which showed a marked increase in the dissolution rate with reduction of particle size, compared with the single-ground powder, even with a similar particle size. The oral bioavailability study of co-ground powders in beagle dose exhibited a dramatic increase, as did the dissolution rate, according to finer particle size. Finally, complete bioavailability was obtained at the finest particle size of 1.2 μm (drug/carrier ratio of 1 : 5, w/w) as was a solution of the drug. Bioavailability had a good linear correlation with the dissolution rate. These findings suggested that the co-grinding method with D-mannitol dramatically increased the available surface area, caused by a reduction of particle size, which not only accelerated the dissolution rate but also resulted in greater enhancement of the bioavailability of 174.

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