Abstract

A self-emulsifying pharmaceutical composition for delivering taxanes is disclosed. It comprises taxane, oil, surfactant and ethanol, preferably also comprises lactic acid. The surfactant is phospholipid or polyoxyethylenated castor oil. When added into the glucose injection, the self-emulsifying pharmaceutical composition immediately forms a microemulsion with a particle size of 50-300 nm. The microemulsion is stable for more than 12 hours at room temperature.

IPC Classes  ?

• A61K 9/107 - Emulsions
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61P 35/00 - Antineoplastic agents

Abstract

Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which including the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl(Cbz), t-butoxy carbonyl(Boc), or 9- fluorenyl methoxyl carbonyl(Fmoc).The present novel compounds have pharmaceutical activity and are prepared by condensation reaction of racemic, levo- or dextro- demethyl Sibutramine and racemic or D/L isoleucine under a mild condition. It is demonstrated that the present compounds have effect of losing weight to obese mode rats in different level and the effect is better than Sibutramine by the animal experiments. So the medicaments prepared by the present compounds or the medicaments prepared by the compositions of the present compounds and other pharmaceutical activity compounds may be used for treating obesity.

IPC Classes  ?

• C07C 237/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61P 3/04 - AnorexiantsAntiobesity agents
• C07C 211/26 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring