Studies on the Method of Size Reduction of Medicinal Compounds. II. Size Reduction of Griseofulvin by Solvation and Desolvation Method using Chloroform (2)

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The mechanism of the size reduction of griseofulvin to micron grade caused by exposing to liquid or vaporous chloroform and then removing it in a vacuum at higher temperatures was investigated by the differential thermal and thermo-gravimetric analysis. The results indicate that a solvated compound having a molar composition of 1 : 1 is formed between the antibiotics and chloroform. It becomes clear that the formation and decomposition of the solvate play an important role in reducing particle size, since lattice rearrangement to the solvate and back to the original compound is occurred during these processes, and the growth of larger crystals is prevented by the difficulty of migration of the newly formed molecules to the nuclei in the solid state. The "solvation and desolvation" method of size reduction first acquired practical success in the production of finely powdered griseofulvin is thought to find application to other materials, since the processes involved are simple, effective and economical.
公益社団法人日本薬学会の論文
1964-10-25