Particle Design of Tolbutamide by the Spherical Crystallization Technique. V. Improvement of Dissolution and Bioavailability of Direct Compressed Tablets Prepared Using Tolbutamide Agglomerated Crystals

Autor:	Hirofumi Takeuchi, Akimitsu Sano, Yoshiaki Kawashima, Toshiyuki Niwa, Tomoaki Hino, Takeo Kuriki
Rok vydání:	1992
Předmět:	Chemistry Stereochemistry Diffusion General Chemistry General Medicine Dosage form law.invention Bioavailability Solvent Tableting law Specific surface area Drug Discovery Crystallization Dissolution Nuclear chemistry
Zdroj:	Chemical and Pharmaceutical Bulletin. 40:3030-3035
ISSN:	1347-5223 0009-2363
Popis:	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
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::0bcebe4a13898cfe4b26c4a75860ae95 https://doi.org/10.1248/cpb.40.3030 Zobrazit plný text záznamu