Drugs online research references
Chem Pharm Bull (Tokyo). 1989 Sep;37(9):2491-5.
Design of polyvinyl alcohol hydrogel as a controlled-release vehicle for rectal administration of dl-propranolol-HCl and atenolol.
Morimoto K, Fukanoki S, Morisaka K, Hyon SH, Ikada Y.
Preparations of beta-blockers, propranolol-HCl and atenolol, in poly(vinyl alcohol) (PVA) hydrogel were designed for the therapeutic treatment of hypertension by transrectal delivery. In vitro release characteristics and plasma drug concentration profiles after rectal administration in rats and dogs were examined. The PVA hydrogels containing beta-blockers were prepared by a low-temperature crystallization method. The release of beta-blockers from hydrogel preparations was consistent with Fickian diffusion (Higuchi model); the drug release versus the square root of release time profile gave a straight line over 60% of the total release process. The release of beta-blockers from hydrogel preparations increased at higher concentrations of PVA in the hydrogel preparations and was not affected by the pH of hydrogel preparations. Plasma concentrations of beta-blockers after rectal administration of hydrogels were higher than those after administration of suppositories (Witepsol H-15) in rats and dogs. The drug plasma concentrations increased at higher concentrations of PVA in hydrogel preparations. In the case of propranolol, which is a hepatic high-clearance drug, area under the blood concentration curve, 0-8 h after rectal administration of a hydrogel preparation (20% w/w PVA, pH 7.0) was 2.16 times and 5.26 times higher than those obtained with Witepsol H-15 suppository and oral administration, respectively. Rectal administration with PVA hydrogels is a favorable route for a hepatic high-clearance drug such as propranolol.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2605698&dopt=Abstract
Arzneimittelforschung. 1988 Mar;38(3):408-11.
Determination of sotalol in human body fluids for pharmacokinetic and toxicokinetic studies using high-performance liquid chromatography.
Gluth WP, Sorgel F, Gluth B, Braun J, Geldmacher-von Mallinckrodt M.
Carl-Korth-Institute for Cardiovascular Research, Division of Clinical Pharmacology, Erlangen, Fed. Rep. of Germany.
A sensitive, reliable and discriminating assay method is reported for the determination of sotalol (4-(1-hydroxy-2-isopropylaminoethyl)methanesulfonanilide) in human plasma and urine. The assay procedure has been successfully used during pharmacokinetic studies in healthy volunteers and patients as well as during toxicokinetic analysis. For sample preparation the internal standard atenolol was added to the specimen which was then extracted with n-pentanol-chloroform (1/3) at pH 9.0 followed by re-extraction into 0.05 mol/l sulfuric acid. Chromatography with fluorimetric detection was performed on Hypersil ODS 5 micron including the addition of heptanesulfonic acid and sodium dodecyl sulfate to the mobile phase of acetonitrile-water-acetic acid (20/79/1). Calibration was linear over the ranges of 0.1 to 5.0 micrograms/ml and 0.2 to 100 micrograms/ml for plasma and urine, respectively. Over these ranges coefficients of variation were below 10%. Recovery was between 82 and 98% from plasma and between 92 and 99% from urine.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3382466&dopt=Abstract
Eur J Pharmacol. 1983 Sep 2;92(3-4):285-9.
Beta 2-adrenoceptor-induced hypotension in the ganglion-blocked angiotensin II-supported rat.
Brown NL, Worcel M.
An in vivo method is described to demonstrate vascular beta 2-adrenoceptor agonist and antagonist activity. Agonist activity was shown by the ability of i.v. injected compounds to reduce blood pressure in ganglion-blocked, phenoxybenzamine-treated, angiotensin II-supported rats. Procaterol was employed to assess the relative beta 2 blocking activity of propranolol IPS 339 and atenolol. Arunlakshana and Schild analysis of the data revealed that all these compounds were competitively beta 2 antagonists, their relative potencies being 100 : 80 : 0.56 respectively.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6138268&dopt=Abstract
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