• Journal of Pharmaceutical Investigation
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• v.14 no.1
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• pp.19-30
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• 1984

The pharmaceutical characteristics of solid indoprofen inclusion complex such as dissolution, permeation through a cellophane membrane, model analysis of interfacial tranesfer, absorption behaviors in rat intestine, and the plasma concentration of indoprofen after oral administrations to rabbits were examined in comparison with those indoprofen alone. The inclusion complex obtained by freeze-drying method showed the higher dissolution rate and membrane permeability among the test powders, and increased significantly the amont of indoprofen absorbed in rat intestine and the levels of plasma concentration of indoprofen after oral adminstrations to rabbits. The increase of bioavailability of $indoprofen-{\beta}-cyclodextrin$ complex was considered due to the increased solubility and dissolution rate of solid powder form.

• YAKHAK HOEJI
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• v.35 no.4
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• pp.314-318
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• 1991

A convenient method for the synthesis of indoprofen, which is a potent antiinflammatory agent, w described. Ethyl $\alpha$-(4-aminophenyl)propionate was prepared by nitration of ethyl $\alpha$-phenylpropionate, followed by reduction. Ethyl $\alpha$-[4-(1, 3-dioxo-2-iso-indolinyl)phenyl]propionate was obtained from condensation reaction of phthatic anhydride and ethyl $\alpha$-(4-aminophenyl)propionate. Indoprofen was prepared by reduction of ethyl $\alpha$-[3-(1, 3-dioxo-2-iso-indolinyl)phenyl]propionate with zinc dust-acetic acid, followed by hydrolysis of the resultant ethyl $\alpha$-[4-(1-oxo-2-iso-indolinyl)pheriyl]propionate.

• Journal of Pharmaceutical Investigation
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• v.13 no.1
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• pp.10-22
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• 1983

The interactions of ${\alpha}-cyclodextrin({\alpha}-CyD)$ and ${\beta}-cyclodextrin({\beta}-CyD)$ with several non-steroidal antiinflammatory drugs were studied on the effects of ${\alpha}-$ and ${\beta}-CyD$ on the solubility of the drugs in aqueous medium. Indoprofen, niflumic acid, alclofenac, and naproxen were chosen as representatives of antiinflammatory drugs. The solubility of all drugs studied increased with the addition of ${\beta}-CyD$, while not with glucose or ${\alpha}-CyD$. The increase of the solubility with ${\beta}-CyD$ was considered due mainly to the formation of inclusion complexes between ${\beta}-CyD$ and drugs. From the solubility data, the apparent stability constants K of the complex could be calculated. Ultraviolet absorption and circular dichroism confirmed the inclusion of indoprofen, niflumic acid and naproxen with ${\beta}-CyD$ in the molar ratio of 1 : 1. Inclusion complexes in solid powder form were obtained by the freeze-drying method and the inclusion formation was confirmed again by infrared, diffential thermal analysis, and X-ray diffraction measurements.