Pharmaceutical compositions containing non-racemic verapamil and

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

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A61K 954, A61K 924, A61K 31275

Patent

active

059555009

ABSTRACT:
Pharmaceutical compositions containing non-racemic mixtures of verapamil are described, as well as a process of making pharmaceutical compositions containing unequal amounts of R- and S-verapamil.
A process for customizing a pharmaceutical composition containing R-verapamil and S-verapamil to optimize a selected pharmaceutical activity comprises selecting a pharmaceutical activity possessed by R-verapamil or S-verapamil, alone or in combination, and then determining a target plasma level for R-verapamil and S-verapamil to achieve that activity is also described. A dosage form for administering the drug is selected. Based on dosage form, one determines the relative amounts of R- and S-verapamil to incorporate into the dosage form to achieve the targeted plasma levels. The dosage form can then be formulated.

REFERENCES:
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Overhead projection presented at Drug Information Workshop Apr. 27-29, (1992), "Generic Applications of Chiral Products".
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Karim, A., Drug Information Association Workshop, "Should Plasma Levels of Enantiomers be Determined in Evaluating the Bioavailability of Chiral Drugs?", Apr. 27-29, 1992.
McMahon, G. et al., "The Importance of Chirality to Antihypertensive Drug Effects", Current Therapeutic Research, vol. 52, pp. 89-97, 1992.
Kwon, Y. and Triggle, D.J., "Chiral Aspects of Drug Action at Ion Channels: A Commentary on the Stereoselectivity of Drug Actions at Voltage-Gated Ion Channels With Particular Reference to Verapamil Actions at the Ca.sup.2+ Channel", Chirality, 3:393-404 (1991).
Wilson, K. and Walker, J., "Chirality and Its Importance in Drug Development", Biochemical Society Transactions, vol. 19, pp. 443-475, (1991).
Eleventh draft of guidance note from European Commission, CPMP Working Party on Quality of Medicinal Products, CPMP Working Party on Safety of Medicinal Products, CPMP Working Party on Efficacy of Medical Products, Investigation of Chiral Active Substances, Oct. 1992.

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