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Amlodipine is a calcium channel blocker prescribed for the management of angina and hypertension. As a racemic mixture, amlodipine contains (R)- and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity. Based on pharmacologic research, it remains uncertain if (S)-amlodipine alone has similar efficacy and ...
Meng Qiu, Suodi Zhai
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Pharmacokinetic behaviour of R-(+)- and S-(−)-amlodipine after single enantiomer administration
Journal of Chromatography B: Biomedical Sciences and Applications, 1997Amlodipine, 3-ethyl 5-methyl-2-[(2-aminoethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methy l-3,5-pyridinedicarboxylate, is a chiral calcium antagonist, currently on the market and in therapeutic use as a racemate. The pharmacokinetic behaviour of R-(+)- and S-(-)-amlodipine after single enantiomer administration to healthy male human volunteers ...
Lukša, J +4 more
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858 THE EFFECTIVENESS OF S(-)-AMLODIPINE ON VASCULAR FUNCTION
Journal of Hypertension, 2012Objective:This study was designed to determine the effectiveness of S(-)-amlodipine on vascular function compared with racemic amlodipine in Chinese patients with mild to moderate hypertension.Methods:This was a multicenter, randomized, double-blind, placebo-controlled study with two parallel ...
Jizhen Guo, Yanchun Gong, Yan Li
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Journal of Chromatography B: Biomedical Sciences and Applications, 1997
Pharmacokinetic studies of optically pure compounds after single enantiomer administration are becoming increasingly important. The process of racemization in vivo can diminish all expected advantages of single enantiomer treatment. Amlodipine, one of the calcium channel blockers, currently used in therapy as a racemate, is one of such drugs under ...
Lukša, J +4 more
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Pharmacokinetic studies of optically pure compounds after single enantiomer administration are becoming increasingly important. The process of racemization in vivo can diminish all expected advantages of single enantiomer treatment. Amlodipine, one of the calcium channel blockers, currently used in therapy as a racemate, is one of such drugs under ...
Lukša, J +4 more
openaire +3 more sources
Technology Development for the Synthesis of S-Amlodipine Nicotinate Drug Substance
Pharmaceutical Chemistry Journal, 2017Technology for the synthesis of S-amlodipine nicotinate drug substance was developed based on an acceptable method of effective separation of the amlodipine optical isomers. A literature review suggested that the most promising methods employed 2-propanol (pure or with small additions of cosolvents) as the main solvent. However, experiments showed that
G. A. Kim +5 more
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Pharmaceutical Development and Technology, 2013
The aim of this study was to compare the specific characteristics of the S-enantiomer and the racemate of amlodipine besylate (AB) in order to design a robust and stable formulation of the active S-enantiomer which will guarantee continuous performance of the unichiral version of amlodipine.
S, Hadžidedić +3 more
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The aim of this study was to compare the specific characteristics of the S-enantiomer and the racemate of amlodipine besylate (AB) in order to design a robust and stable formulation of the active S-enantiomer which will guarantee continuous performance of the unichiral version of amlodipine.
S, Hadžidedić +3 more
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International Journal of Pharmaceutics, 2009
The objective of the present investigation was to develop and evaluate a drug-in-adhesive transdermal patch for S-amlodipine (S-AM) free base. Initial in vitro experiments were conducted to optimize the formulation parameters before transdermal delivery in rats.
Yinghua, Sun +6 more
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The objective of the present investigation was to develop and evaluate a drug-in-adhesive transdermal patch for S-amlodipine (S-AM) free base. Initial in vitro experiments were conducted to optimize the formulation parameters before transdermal delivery in rats.
Yinghua, Sun +6 more
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S-amlodipine--the 2007 clinical review.
Journal of the Indian Medical Association, 2007S-amlodipine is the only vaso-active enantiomer of amlodipine. This article reviews the published data in nearly 5000 patients. Randomised controlled trials of S-amlodipine at half the dose of racemate in the treatment of hypertension, have shown it to be as effective as racemic amlodipine.
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[Organoprotective and metabolic effects of S-amlodipine in patients with arterial hypertension].
Kardiologiia, 2014We compared effects of racemic amlodipine and S-amlodipine in 127 patients with 1-2 degree arterial hypertension (AH) on structural-functional parameters of the left ventricle and brachial artery as well as on characteristics of carbohydrate, lipid, electrolyte, and purine metabolism. Racemic amlodipine was given to 66 and S-amlodipine--to 61 patients.
B G, Iskenderov, S V, Saushkina
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Chemical Engineering Journal, 2012
Abstract A hollow fiber supported liquid membrane (HFSLM) containing the chiral selector O , O ′-dibenzoyl-(2 S ,3 S )-tartaric acid ((+)-DBTA) was characterized for the enantioseparation of ( R , S )-amlodipine. The influence of various chemical parameters, including the concentration of feed and receiving phases, as well as the carrier ...
Niti Sunsandee +3 more
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Abstract A hollow fiber supported liquid membrane (HFSLM) containing the chiral selector O , O ′-dibenzoyl-(2 S ,3 S )-tartaric acid ((+)-DBTA) was characterized for the enantioseparation of ( R , S )-amlodipine. The influence of various chemical parameters, including the concentration of feed and receiving phases, as well as the carrier ...
Niti Sunsandee +3 more
openaire +1 more source

