US EPA

1579960 

Journal Article 

Nanosuspensions for the formulation of poorly soluble drugs. Part 1. Preparation by a size-reduction technique 

Muller, RH; Peters, K 

1998 

Yes 

International Journal of Pharmaceutics
ISSN: 0378-5173
EISSN: 1873-3476 

IPA/99/1162228 

J 

REF 13 

229-237 

eng 

IPA COPYRIGHT: ASHP To allow the intravenous injection of poorly soluble drugs, RMKP-22 (2-propanol, 1-((2,7-bis(2,6-dimethyl-4-morpholinyl)-6-phenyl-4-pteridinyl) (2-hydroxyethyl)-amino)-2-methyl-,(cis(cis))), RMKP-23, and prednisolone were formulated as nanosuspensions by high pressure homogenization; the effect of the production parameters pressure and cycle number on the mean particle size and on the polydispersity of the nanosuspension was investigated with special attention to contamination by microparticles. Properties of the nanosuspensions increased saturation solubility and the dissolution rate. The degree of particle fineness in the nanosuspensions was found to increase with production pressure and number of cycles. Also, the achievable degree of particle fineness was a function of the nature of the drug, as were the particle shapes of the investigated drugs. Special features of the nanosuspensions known for increasing the bioavailability are discussed. It was concluded that size distribution obtained and use of an APV Gaulin homogenizer led to a product considered acceptable by regulatory authorities. 

Prednisolone; suspensions; dissolution; RMKP-22; RMKP-23; Steroids; nanosuspensions; prednisolone(Steroids; Anti-infective agents; RMKP-23(Anti-infective agents; RMKP-22(Anti-infective agents; Dissolution rates; Particle size; Solubility; (2-Propanol