Particle Design of Tolbutamide by the Spherical Crystallization Technique. V. Improvement of Dissolution and Bioavailability of Direct Compressed Tablets Prepared Using Tolbutamide Agglomerated Crystals
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概要
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Tolbutamide (TBM) agglomerated crystals were prepared by three spherical crystallization techniques, the solvent change (SC) method, neutralization (NT) method and quasi-emulsion solvent diffusion (QESD) method (SC-A, SC-B, NT and QESD) agglomerated crystals), followed by mixture with a disintegrating agent and a lubricant (physical mixtures), and then tableting by the direct compression method. Unagglomerated TBM original crystals (bulk) were treated in the same manner. The dissolution rate and bioavailability of TBM from the physical mixtures and tablets were evaluated to look for a correlation between the in vitro dissolution profile and in vivo bioavailability.The TBM dissolution rate from the physical mixtures and tablets increased in the order of bulk≦QESD<SC-A<SC-B<NT in direct proportion to an increase in the specific surface area of the agglomerated crystals and bulk. A linear relationship could be established between the specific surface area and 75% dissolution time (T_<75>).In in vivo studies in beagle dogs, the physical mixtures and tablets of the agglomerated crystals showed significantly higher values than those of the bulk in the area under the curve of plasma concentration (AUC_<0-8h>), maximum concentration in plasma (C_<max>) and absorption rate constant (k_a), especially high values were obtained with the NT physical mixtures and tablets. A linear correlation could be established between 1/T_<75> and k_a. The in vivo absorption process and bioavailability of TBM could be estimated from the in vitro dissolution profile.
- 公益社団法人日本薬学会の論文
- 1992-11-25
著者
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川島 嘉明
Gifu Pharmaceutical University
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佐野 昭光
Pharma Research & Development Division Hoechst Japan Ltd.
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竹内 洋文
Gifu Pharmaceutical University
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丹羽 敏幸
岐阜薬科大学製剤学教室
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丹羽 敏幸
Gifu Pharmaceutical University
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日野 知証
Gifu Pharmaceutical University
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栗木 武男
Pharma Research Laboratories, Hoechst Japan Limited
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栗木 武男
ヘキストジャパン(株)
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栗木 武男
Laboratory For Chemistry Hoechst Japan Limited
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栗木 武男
Pharma Research And Development Division Hoechst Japan Limited
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