Preparation of Neurotensin Analogue-Containing Poly(dl-lactic acid) Microspheres Formed by Oil-in-Water Solvent Evaporation

Autor: Sumio Watanabe, Ichiro Yamakawa, Ryoichi Machida, Yuki Tsushima
Rok vydání: 1992
Předmět:
Zdroj: Journal of Pharmaceutical Sciences. 81:899-903
ISSN: 0022-3549
DOI: 10.1002/jps.2600810912
Popis: This report describes the preparation of injectable microspheres containing a neurotensin analogue (NA), which is a hexapeptide with neurotensin activity. NA, a hydrophilic drug, was successfully entrapped into poly( dl -lactic acid) microspheres prepared by a novel oil-in-water solvent evaporation method. The preparation method was investigated with regard to the partition of NA into the oily phase and the rapid phase separation of the polymer. Successful entrapment was achieved with the following conditions: (1) an alkaline water phase, (2) addition of fatty acid salt in the oily phase, and (3) addition of a water-miscible solvent in the oily phase. Under these conditions, NA was completely entrapped into the microspheres at poly( dl -lactic acid):NA molar ratios of >3.
Databáze: OpenAIRE