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PubMed · 5920679

Indomethacin.

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1966-11-05. Indomethacin.. https://pubmed.ncbi.nlm.nih.gov/5920679/

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Solid dispersion particles of amorphous indomethacin with fine porous silica particles by using spray-drying method.

The solid dispersion particles of indomethacin (IMC) were prepared with different types of silica, non-porous (Aerosil 200) or porous silica (Sylysia 350) by using spray-drying method. Powder X-ray diffraction analysis showed that IMC in solid dispersion particles is in amorphous state irrespective of the type of silica formulated. In DSC analysis, the melting peak of IMC in solid dispersion particles with Sylysia 350 shifted to lower temperature than that in solid dispersion particles with Aerosil 200 although the peak of each solid dispersion particles was much smaller than that of original IMC crystals. Dissolution property of IMC was remarkably improved by formulating the silica particles to the solid dispersion particles. In comparing the effect of the type of the silica particles, the dissolution rate of solid dispersion particles with Sylysia 350 was faster than that with Aerosil 200. The formulation amount of IMC did not affect on the amorphous state of IMC in the resultant solid dispersion particles in powder X-ray diffraction patterns. However, the area of the melting peak of IMC in the solid dispersion particles increased and an exothermic peak owing to recrystallization was observed with increasing the IMC content in the DSC patterns. The dissolution rate of IMC from the solid dispersion particles with Sylysia 350 was faster than that of Aerosil 200 irrespective of IMC content. In stability test, amorphous IMC in the solid dispersion particles with each silica particles did not crystallize under storing at severe storage conditions (40 degrees C, 75% RH) for 2 months, while amorphous IMC without silica easily crystallized under same conditions.

Indomethacin↗

[Concentration of locally applied Indometacin eyedrops for the inhibition of prostaglandin synthesis in the eye].

Indomethacin is well known as local eye drug for the prevention of cystoid macular oedema. The concentration is 50 mg/5 ml. Another inhibitor of the prostaglandin synthesis is flurbiprofen; its concentration is 1.5 mg/5 ml. Indomethacin is a suspension and available in different concentrations dependent on the shaking procedure. We measured the concentration of indomethacin in one single eyedrop from a full bottle, half full and a nearly empty bottle. After correct shaking the concentration of indomethacin was between 48 and 53 mg/5 ml.

Indomethacin↗

Solubilization of indomethacin by polysorbate 80 in mixed water-sorbitol solvents.

The effect of indomethacin on the micellar properties of the non-ionic surfactant, polysorbate 80, in water-sorbitol mixtures containing up to 25% w/v sorbitol has been investigated by light scattering, photon correlation spectroscopy and viscometric techniques. The molecular weight of polysorbate 80 micelles containing solubilized indomethacin increased linearly with increase of sorbitol concentration. Solubilization of indomethacin resulted in an increase of micellar weight due not only to the incorporation of solubilizate but also to an increase in the number of polysorbate molecules per micelle. The micelles in all systems were most satisfactorily represented as oblate ellipsoids, the asymmetry and hydration of which increased with increase of sorbitol concentration. Indomethacin solubilization caused a restructuring of the micelle to produce a more symmetrical micelle of increased hydration.

Indomethacin↗