Syntex (u.s.a.) Inc.

Syntex Pharmaceuticals, Ltd.

Michael J Dey

Alastair B Selkirk

Calum B MacFarlane

Calum B McFarlane

Alistair B Selkirk

John R Langridge

There is disclosed an improved long acting sustained release pharmaceutical composition for dihydropyridine calcium channel blockers wherein the calcium channel blocker and a pH-dependent binder, which are intimately admixed in essentially spherically shaped non-rugose particles of up to 1.2 mm in diameter, are provided with a coating to obtain slow, sustained release of a safe, therapeutically effective amount of the calcium channel blocker over a period of at least about 24 hours. Thus, the improved pharmaceutical composition for a dihydropyridine calcium channel blockers is suitable for once daily administration.

Long acting calcium channel blocker composition

A long acting sustained release pharmaceutical composition for dihydropyridine calcium channel blockers wherein the calcium channel blocker and a pH-dependent binder are intimately admixed in essentially spherically shaped non-rugose particles of up to 1.2 mm in diameter.

Long acting nicardipine hydrochloride formulation

There is disclosed a stable pharmaceutical composition containing nicardipine hydrochloride, a non-chloride isotonicity agent, a buffering agent and a pharmaceutically acceptable aqueous vehicle for parenteral administration.

Nicardipine pharmaceutical composition for parenteral administration

A pharmaceutical formulation suitable for parenteral (preferably intravenous) administration includes an effective amount of 1-diphenylmethyl-4-[(2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl]p iperazine and a suitable amount of an acid to generate a pharmaceutically acceptable salt having a pH above about 3.0 and a solubility above about 4.0 mg/ml. The intravenous formulation optionally includes a suitable tonicifier in a quantity sufficient to achieve isotonicity with body fluids. The salt is formed in situ during the formulation process. The salt of tartaric acid is preferred; suitable salts for lower concentration dosages are the citric acid and methane sulphonic acid salts.

Parenteral formulations of

A pharmaceutical formulation suitable for parenteral (preferably intravenous) adminstration includes an effective amount of 1-diphenylmethyl-4-[(2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl]p iperazine and a suitable amount of an acid to generate a pharmaceutically acceptable salt having a pH above about 3.0 and a solubility above about 4.0 mg/ml. The intravenous formulation optionally includes a suitable tonicifier in a quantity sufficient to achieve isotonicity with body fluids. The salt is formed in situ during the formulation process. The slat of tartaric acid is preferred; suitable salts for lower concentration dosages are the citric acid and methane sulphonic acid salts.

A long acting sustained release pharmaceutical composition for dihydropyridine calcium channel blockers wherein the calcium channel blocker and a pH-dependent binde are intimately admixed in essentially spherically shaped non-rugose particles of up to 1.2 mm in diameter.

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East Calder, United Kingdom

Michael J Dey