xviii New Patents

4981983

DERIVATIVES OF BILIARY A C I D S , P R O C E S S F O R T H E

P R O D U C T I O N T H E R E O F A N D C O R R E S P O N D I N G

P H A R M A C E U T I C A L C O M P O S I T I O N S

Virginio Castagnola, E Giuliano Frigerio, Roberto Pellicciari, Aldo Roda, Milan, Italy as- signed to Gipharmex S p A

New derivatives of chenodeoxycholic, ur- sodeoxy cholic, cholic and ursocholic acids, bearing a methyl group in the side chain in an alfa position to the carboxylic group, the cor- responding nor- and di-nor- derivatives, and the corresponding conjugates with taurine and glycine, are described. The compounds of the in- vention are prepared by methylation of the esters with methyl iodide in the presence of lithium- dialkylamides.

composed of a pH sensitive film-forming poly- mer. The film forming polymer may be an enteric polymer containing phthalic acid with one car- boxyl group attached to the enteric polymer via an ester bond, and the second carboxyl group remaining a free acid so that the modified film forming polymer is hydrophobic at low pH and hydrophilic at higher pH. Hydrophobic stearyl side chains are attached to the enteric polymer which causes the pH controlled diffusion mem- brane to remain insoluble at high pH. Alterna- tively, the pH sensitive film forming polymer may be a polymer containing hydrophobic and free acid groups so that the modified film for- ming polymer is hydrophobic at low pH and hydrophilic but insoluble at high pH. In the pre- ferred sustained-release pharmaceutical pre- paration the film forming polymer is coated into core drug particles to produce a pH controlled diffusion membrane surrounding the core drug and form microparticles which may be admixed with free drug or time-release drug and placed in a gelatin capsule or tabletted.

4983397

P H A R M A C E U T I C A L C O M P O S I T I O N S C O N S I S T I N G O F

A C Y L A T E D P H O S P H O L I P I D S

Alan J Schroit, Raji Nayar assigned to Board of Regents University of Texas System

Liposome dispersions are prepared from (a) a synthetic phospholipid of the cephaline type in which the amino group is monoacylated with a dicarboxylic acid; (b) a synthetic phospholipid of the cephaline type; and (c) one or more com- pounds having pharmacological activity. The mixture optionally can contain phospholipids of natural sources and a pharmaceutical carrier solution buffered to pH 7.0 to 7.8.

4983586

P H A R M A C E U T I C A L F O R M U L A T I O N S F O R

P A R E N T E R A L U S E

Nicholas S Bodor assigned to University of Florida

Aqueous parenteral solutions of drugs which are insoluble or only sparingly soluble in water and/or which are unstable in water, combined with hydroxypropyl- beta-cyclodextrin, provide a means for alleviating problems associated with drug precipitation at the injection site and/or in the lungs or other organs following parenteral administration.

4983593

4983401

S U S T A I N E D R E L E A S E P H A R M A C E U T I C A L

P R E P A R A T I O N S H A V I N G P H C O N T R O L L E D M E M B R A N E

C O A T I N G S

Herman J Eichel, Brent Massmann assigned to Kinaform Technology Inc

A sustained-release pharmaceutical preparation utilizing a pH controlled diffusion membrane

P H A R M A C E U T I C A L C O M P O S I T I O N O F

D I H Y D R O P Y R I D I N E C O M P O U N D

Masahar Miyajima, Yukiya Yamaguchi, Takao Tsunematsu, Toshihisa Oda, Konan, Japan as- signed to Zeria Pharmaceutical Co; Nissan Chemical Industries L

A pharmaceutical composition comprising: a 1:1 solvate of 5-(5, 5-dimethyl-i,3 2- dioxaphosphorinane-2-yl)- 1 4-dihydro-2,6- dimethyl-4-(3- itrophenyl)-3-pyridine carboxylic