1. Fourteen healthy Swedish Caucasian subjects were given 20 mg of omeprazole orally each morning for 8 days. The subjects included five poor metabolisers (PM) of S-mephenytoin, four heterozygous extensive metabolisers (hetEM) and five subjects with a very rapid metabolism (rapidEM). 2. After the first dose, the relative mean areas under the plasma concentration vs time curve (AUC) of omeprazole in rapidEM, hetEM and PM were 1:3.7:20 (all different, P
The aim of this study was to formulate extended release compression coated core tablets of fenoterol hydrobromide, a selective beta(2) adrenergic receptor agonist, in an attempt to prevent nocturnal asthma. Two hydrophilic polymers viz Kollidon SR, Polyox WSR 303 and a hydrophobic one (Precirol ATO5) were employed. Compression coated tablets were formulated by preparing a core tablet containing 7.5 mg drug and various amounts of polymer and Emcompress then compressed coated with the same polymeric materials. For comparison purpose different matrix tablets were also prepared employing the same polymers. In-vitro release studies were carried out at different pH (1.2 and 6.8). Pharmacokinetics of extended release tablets as well as commercially available immediate release tablets (Berotec) were studied after oral administration to beagle dogs using a new developed LC-MS/MS method with a lower limit of quantification of 1 ng/ml. Fenoterol release from compression coated tablets was significantly lower than matrix tablets. The mechanism of release was changed with the nature and content of polymer. The release pattern of drug from F16 containing 40 mg Kollidon SR divided in the core tablet (15 mg) and the rest in the compressed coat (25 mg) showed a typical zero order release kinetic that could extend drug release >10 h and reasonable time for 75% to be released (t(75)) (8.92 h). When compared to immediate release Berotec tablet the MRT was significantly extended from 7.03 +/- 0.76 to 10.93 +/- 1.25 h (P
Found low compliance of admission to long-term acetylsalicylic acid (ASA) in patients with acute coronary syndrome (ACS): 74.9% of patients reported that the suspended or completely stopped taking the drug, and only 16.2% were fully committed to the long-term therapy with ASA. Patients are significantly more likely to discontinue conventional and buffered forms of ASA compared with intestinal-soluble forms of the drug (odds ratio - OR=1.81, 95% confidence interval - CI: 1.20 to 2.72; p=0,0027). The most common causes of low noncompliance were to receive ASA or the development of fear of adverse drug reactions (ADRs) - 47.1%, and the forgetfulness of the patients taking the drug regularly (25.4%). When receiving enteric forms of ASA NLR developed significantly less than in the case of buffered (OR 0.49, 95% CI, 0.35 to 0,69; p=0,00002) and "ordinary" (OR 0.21, 95 % CI 0.13 to 0,33; p=0,00001) forms of ASA. Compliance of the highest among all the drugs ASA, according to estimates by using a 10-point visual analog scale, were observed in enteric-coated forms of ASA (average score of 8.3+/-1.4). Some of the lowest noncompliance were noted to receive the "regular" aspirin tablet (6.9+/-1.4 points).