Add time:09/10/2019         Source:sciencedirect.com

Agglomerated crystals of indomethacin and epirizole were prepared by the spherical crystallization technique. The solvent used was ethanol—water—chloroform, ethyl acetate—water, or ethyl acetate—aqueous sodium chloride. From the ethanol—chloroform—water system, we obtained agglomerated crystals of a polymorphic mixture of the β form of indomethacin (original form, γ) and amorphous epirizole. When the mole percent of epirizole loaded into the system was less than 63 and 38% for the ethyl acetate—water and ethyl acetate—aqueous sodium chloride systems, respectively, the agglomerated crystals consisted of a polymorphic mixture of the α form of indomethacin and amorphous epirizole. When the respective mole percent of epirizole loaded was more than 65 and 43% in the aforementioned systems, a new complex of indomethacin—epirizole (molecular ratio equal to 2:1) was obtained. Recovery of complex from the drugs loaded in the ethyl acetate—aqueous sodium chloride system was higher than that in the ethyl acetate—water system, as a result of a salting-out effect. The solubility of indomethacin in the agglomerated complex in a solution of 30% aqueous ethanol and in disintegration test solution no. 2 (composition, 0.05 M KH2PO4 plus 0.0236 M, NaOH, pH 6.8), specified in the Japanese Pharmacopeia X (JPX), was higher than in the physical mixture (molecular ratio of indomethacin to epirizole equal to 2:1). In the ethanol solution, indomethacin was transformed into the γ form during dissolution, and a decrease in solubility occurred. The process of dissolution of the tablet of the agglomerated complex was described by zero-order kinetics. The rate of release of indomethacin from the complex was three times more rapid than that from the physical mixture in the disintegration test solution. These agglomerated crystals can be compounded directly into pharmaceutical systems without further processing such as granulation.

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