摘要:
A modified release pharmaceutical composition comprises lercanidipine dissolved in a waxy substance comprising a polyalcohol fatty acid ester, the solution being contained within a pharmaceutically acceptable capsule. Preferably the polyalcohol fatty acid ester is a polyethylene glycol ester, a polypropylene glycol ester, a fatty acid glyceride or a mixture of two or more thereof. Most preferably, the polyalcohol fatty acid ester is a mixture of mono-, di- and triglycerides and polyethylene glycol mono- and diesters. Oral administration of the modified release pharmaceutical compositions to a patient has been shown to result in a mean lercanidipine plasma concentration of greater than 0.5 ng/ml for 24 hours after administration.
摘要:
The invention relates to new addition salts comprising lercanidipine and an acid counterion selected from the group consisting of: (i) inorganic acids, (ii) sulphonic acids, (iii) monocarboxylic acids, (iv) dicarboxylic acids, (v) tricarboxylic acids, and (vi) aromatic sulphonimides, with the proviso that said acid counterion is not hydrochloric acid. In particular, both amorphous and crystalline salts of lercanidipine with benzenesulphonic and naphthalene- 1,5-disulphonic acids are disclosed, as are amorphous salts of lercanidipine with several other acid counterions.
摘要:
The invention provides a substantially pure amorphous lercanidipine hydrochloride having a purity of at least 95% pure, preferably at least about 97% pure, more preferably at least about 99% pure, and still more preferably at least about 99.5% pure. The invention further relates to methods of preparing substantially pure amorphous lercanidipine, as well as methods of providing rapid relief from hypertension by administering the substantially pure amorphous lercanidipine hydrochloride of the present invention to a patient in need of such treatment.
摘要:
Antagonists that are selective for the metabotropic mGlu5 receptor over at least one of the metabotropic mGlul receptor, mGlu2 receptor and mGlu3 receptor, and preferably selective over all three thereof, are useful for the preparation of medicaments for the treatment of neuromuscular dysfunction of the lower urinary tract in mammals. A wide variety of suitable compounds is described. The medicament may contain the selective mGlu5 antagonist as the sole active agent, or may also contain one or more additional therapeutic agents for for the treatment of neuromuscular dysfunction of the lower urinary tract in mammals. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in mammals.
摘要:
N,N-Disubstituted diazocycloalkanes of the formula (I): (R = halogen, R = (C3-C8)-cycloalkyl, R = (C1-C4)-alkoxy or (C1-C4)-haloalkoxy group, m is 1 or 2, n is 1 or 2) have affinity for serotoninergic receptors. These compounds and their enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptor. 1,4-Disubstituted-piperazines (n = 1) are preferred. R is preferably F in the 2-position, R is preferably cyclohexyl, and R is preferably a methoxy or 2,2,2-trifluoroethyl group. Preferably, m = 1.
摘要:
Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the alpha1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.
摘要:
The invention provides substantially pure lercanidipine free base, having a purity of at least 95 %, preferably at least about 97 %, more preferably at least about 99 %, and still more preferably at least about 99.5 %. The lercanidipine free base of the present invention is formed as an amorphous solid that is easily handled and particularly well suited to the formulation of pharmaceutical compositions.
摘要:
A compound having 5-HT1A antagonist activity is useful for the preparation of a medicament for the treatment of neuromuscular dysfunction of the lower urinary tract in combination with the prior, concurrent or post-administration of a compound having 5-HT1B antagonist activity. Alternatively a single compound having both 5HT1A and 5-HT1B antagonist activity is useful for the preparation of a medicament for the treatment of neuromuscular dysfunction of the lower urinary tract.