摘要:
A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
摘要:
A sustained - release pharmaceutical composition in a form of an orally deliverable tablet comprising an active pharmaceutical agent having solubility not less than about 10mg/ml, dispersed in a matrix comprising a hydrophilic polymer and a starch having a tensile strength of at least about 0.15kNcm -2 at a solid fraction representative of the tablet.
摘要:
The present invention provides a chemically modified human Growth Hormone (hGH) prepared by attaching a polyethylene glycol butyraldehyde moiety to the N-terminal phenylalanine of the protein. The chemically modified protein according to the present invention may have a much longer lasting hGH activity than that of the un-modified hGH, enabling reduced dose and scheduling opportunities. The present invention also includes methods of use for the treatment and/or prevention of diseases or disorders in which use of growth hormone is beneficial.
摘要:
The present invention provides methods for the treatment or porphylaxis of one or more aldosterone-mediated pathogenic effects in a subject suffering from or susceptible to the pathogenic effect or effects wherein the subject has one or more conditions selected from the group consisting of a sub-normal endogenous aldosterone level, salt sensitivity and an elevated dietary sodium intake. The methods comprise administering to the subject a therapeutically-effective amount of one or more epoxy-steroidal compounds that are aldosterone antagonists.
摘要:
Novel methods and combinations for the treatment and/or prophylaxis of a pathologic condition in a subject, wherein the methods comprise the administration of one or more HMG Co-A reductase inhibitors and one or more aldosterone receptor antagonists, and the combinations comprise one or more HMG Co-A reductase inhibitors and one or more of said aldosterone receptor antagonists.
摘要:
The present invention provides a therapeutic composition comprising a COX-2 selective inhibitor or a prodrug thereof and an LTB4 receptor antagonist. A method is provided for the use of such composition in the treatment, prevention, or inhibition of inflammation, an inflammation-related disorder, pain, or a pain-related disorder.
摘要:
A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a calcium channel blocker is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred calcium channel blockers are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 2O-spiroxane steroidal compounds characterized by the presence of a 9alpha,11alpha-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker verapamil HC1 (Benzenacetonitrile, (±) -alpha[3[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-3,4-dimethoxy-alpha-(1-methylethyl)hydrochloride) and the aldosterone receptor antagonist epoxymexrenone.
摘要:
The present invention relates to a novel method of treating and/or preventing psychiatric disorders in a subject by administering to the subject at last one Cox-2 inhibitor alone or in combination with one or more antidepressant agents. Compositions, pharmaceutical compositions and kits are also described.
摘要:
An article of manufacture is provided comprising a vial having (a) a first chamber that is substantially filled with an injectable pharmaceutical formulation; (b) a second chamber that is substantially empty but for a gaseous medium; (c) a septum, impermeable to the gaseous medium, separating the first and second chambers; and (d) actuating means effective to bring the formulation and the gaseous medium into contact by breach of the septum such that the gaseous medium acts as an effective headspace for agitation of the formulation. The formulation comprises an aqueous medium, a drug in solid particulate form in a therapeutically effective amount suspended in the medium, and one or more wetting and/or suspending agents in an amount effective to provide controlled flocculation of the drug, at least one ingredient of the formulation being susceptible to oxidative degradation.
摘要:
A pharmaceutical tablet is provided comprising an intraorally disintegratable core and an excipient coating adherent thereto, wherein the coating comprises gellan gum. The tablet is suitable for intraoral administration, for example for delivery of a drug contained in the core of the tablet to a subject, at least in part by absorption of the drug via oral mucosa of the subject.