Lack of a pharmacokinetic interaction between moexipril and hydrochlorothiazide.

Objective: To investigate the potential for pharmacokinetic interactions between moexipril, a new converting enzyme inhibitor, and hydrochlorothiazide after single dose administration.

Methods: 12 healthy male volunteers were studied by an open, randomised, three-way cross-over design, in which single doses of moexipril, hydrochlorothiazide and the two drugs together were administered. Blood and urine were collected up to 48 hours for measurement of the concentrations of moexipril and its metabolite moexiprilat.

[The pharmacokinetics and bioavailability of a new mexiletine preparation in healthy volunteers].

In the course of this study, both the bioavailability and the most important pharmacokinetic parameters of a newly development mexiletine (CAS 31828-71-4) preparation (Mexiletine-ratiopharm mite, dosage 200 mg of mexiletine) were to be determined in comparison to a commercial reference preparation registered according to the AMG 1976, after single oral administration. For this purpose, the test and the reference preparation were examined in healthy male volunteers according to a randomized, 2-way crossover design. Both preparations entrained maximum plasma levels of approx.

Evaluation of the pharmacokinetics and absolute bioavailability of three isosorbide-5-mononitrate preparations in healthy volunteers.

The objective of this study was two-fold: 1. to determine the pharmacokinetic parameters and the bioavailability of two 20 mg isosorbide-5-mononitrate (CAS 16051-77-7, IS-5-MN) preparations (treatments A and B) after single oral administration and 2. to evaluate the absolute bioavailability of IS-5-MN, which was possible by the administration of a third IS-5-MN preparation (treatment C) by the intravenous route (1 mg/ml, dose 20 mg).

Bioequivalence evaluation of the metabolites 1,2 and 1,3-glyceryl dinitrate of two different glyceryl trinitrate patches after 12-h usage in healthy volunteers.

In the course of this study both the bioavailability and main pharmacokinetic parameters of the glyceryl trinitrate (GTN, CAS 55-63-0) metabolites 1,2 and 1,3-glyceryl dinitrate (1,2-GDN and 1,3-GDN) were to be determined following transdermal application of a glyceryl trinitrate test patch (Deponit 5) and an already marketed reference patch. For this purpose, both patches were examined in healthy volunteers according to a randomized two-way cross-over design, blood samples were withdrawn up to 15 h after start of patch application and the plasma concentrations of both metabolites were quantified using a GC/MS method. The investigation showed the following results: Metabolite 1,2-glyceryl dinitrate: For the area under the curve from time 0 to the last quantifiable sample (AUC(0-Tlast) arithmetic mean values of 23.

Bioequivalence evaluation of two glyceryl trinitrate patches after 12-h usage in healthy volunteers.

The study objective was to determine the bioavailability and main pharmacokinetic parameters of glyceryl trinitrate (GTN, CAS 55-63-0) following cutaneous application of two different glyceryl trinitrate patches using a randomized cross-over design. The two patches investigated were Deponit 5 (a newly developed test patch) and an already marketed reference patch. Thirty-seven healthy male volunteers were included in this study; 36 of them completed the investigation.

Bioavailability and pharmacokinetics of a fixed combination of delapril/indapamide following single and multiple dosing in healthy volunteers.

The study objective was to obtain detailed information on the bioavailability and pharmacokinetics of the new fixed combination of delapril and indapamide following single and multiple dosing. For this reason, the study was performed in two parts, separated by a medication-free period of at least 7 days. In the single dose part, one tablet, containing 30 mg delapril and 2.

Bioavailability and pharmacokinetics of a new isosorbide dinitrate spray preparation in healthy volunteers.

In the course of this study the bioavailability and pharmacokinetic profile of a newly developed 2.5 mg (per valve release) oral isosorbide dinitrate (ISDN, CAS 87-33-2) spray preparation (Isoket Spray) were determined and compared with the results for an already marketed reference spray preparation following single application. For this purpose, the test and reference spray were examined in 18 healthy volunteers according to a randomized 2-way cross-over design.

Evaluation of pharmacokinetics, bioavailability and dose linearity of diltiazem in healthy volunteers.

The objective of this randomized five-way cross-over study with healthy male volunteers was to determine, one the one hand, the bioavailability and main pharmacokinetic parameters of 4 sustained release diltiazem (Surecaps, CAS 42399-41-7) test preparations with ascending doses (180, 240, 300, 360 mg), administered as single application, versus an immediate release 60 mg diltiazem reference preparation, which was given thrice a day at 8-h intervals. On the other hand, the study also allowed the evaluation of a possible dose linearity of the test substance diltiazem. Plasma concentrations of diltiazem and its major metabolite desacetyl-diltiazem were measured by high pressure liquid chromatography (HPLC) up to 48 h after single dosing of the sustained release preparations as well as after repeated doses of the immediate release formulation.

Evaluation of bioavailability and pharmacokinetics of two isosorbide-5-mononitrate preparations in healthy volunteers.

The objective of this study was to determine both the pharmacokinetic parameters and the bioavailability of two commercial 20-mg isosorbide-5-mononitrate (IS-5-MN) preparations (test and reference preparation) after single oral administration. For this purpose, the test and the reference preparation were examined in 24 healthy male volunteers according to a randomized 2-way cross-over design, blood samples were withdrawn up to 24 hours postadministration, and plasma concentrations of IS-5-MN were quantified by a gas chromatography (GC) method. Both preparations led to peak plasma levels of approximately 360 ng/mL IS-5-MN in the mean 0.

[Plasma and urine kinetics of amitriptyline oxide and its metabolites. Comparison of intravenous infusion and oral administration in volunteers].

The study objective was to obtain detailed information on the plasma and urine kinetics of amitriptylinoxide (CAS 4317-14-0) and its metabolites. For this reason, 60 mg of amitriptylinoxide was administered to 12 subjects, both by intravenous infusion and by oral dosage, in a study performed according to a randomized two-way cross-over design. In plasma, we succeeded in analyzing the metabolites amitriptyline and nortriptyline in addition to the parent substance amitriptyloxide.

[Bioavailability and pharmacokinetics of a new nifedipine preparation in healthy volunteers].

In the course of this trial the bioavailability and the essential pharmacokinetic parameters of a newly developed 10 mg nifedipine preparation were to be determined in comparison to a marketed reference preparation after single oral administration. For this purpose, the test and the reference preparation were examined in 16 healthy volunteers according to a randomized 2-way cross-over design (latin square), blood samples were withdrawn up to 16 h p.a.

Urinary recovery and tolerability of FCE 22101 following single intravenous administration under restricted and high fluid intake.

The urinary recovery and tolerability of FCE 22101, a broad spectrum injectable penem, were investigated in a multicentre single-blind randomized crossover study of 60 healthy male volunteers. Single 1 g doses of FCE 22101 or placebo were given by intravenous bolus at weekly intervals. FCE 22101 was given either after intake of 750 ml water (treatment A) or after 8 h of water restriction (treatment B).

[Studies of the pharmacokinetics and bioavailability of a new trimethoprim/sulfamethoxazole preparation in healthy volunteers].

The objective of this study was to determine both the pharmacokinetic parameters and the bioavailability of a newly developed trimethoprim/sulfamethoxazole preparation (cotrimoxazole, Kepinol forte, 160 mg of trimethoprim/800 mg of sulfamethoxazole) in comparison with a reference preparation customary in trade and registered according to the AMG 1976, after single oral administration. For this purpose the test and the reference preparation were examined in a randomized 2-way crossover design (Latin square) in 12 volunteers each. Both dosage forms led to maximum plasma levels of approx.

[Lithogenicity and bile acid pattern in choleretic administration (3-n-butoxy-1-phenoxy-propanol: febuprol) in patients with functional right upper quadrant pain].

10 patients with right upper quadrant pain were treated with a choleretic agent (Febuprol; 3 X 200 mg t. i. d.

[Wheat bran-type roughage reduces the lithogenicity of bile].

The effect of 30 g wheat bran on the lithogenic potency of bile was studied in ten healthy males (age 25.5 +/- 0.76 years; height 182.

[Composition of VLDL, LDL and HDL lipoprotein fractions in type IIa, IIb, III, IV, and V hyperlipemia patients in comparison with healthy individuals].

The chemical composition of VLDL, LDL and HDL was studied in 82 patients with primary hyperlipoproteinaemia (37 type IIa, 7 type IIb, 3 type II, 25 type IV, 10 type V) and in ten metabolically normal individuals. Lipoprotein fractions were prepared by preparative ultracentrifugation. Each fraction was analysed for cholesterol, triglycerides, phospholipids and protein.

[Effect of beta-pyridylcarbinol on lipids and lipoprotein in primary type IIa hyperlipoproteinemia].

The effect of long-term treatment over 16 weeks with beta-pyridylcarbinol (test substance Ronicol 300) on lipids and lipoproteins was investigated in 10 patients with primary hyperlipoproteinemia type IIa. A placebo period preceded and followed the treatment period. The lipoprotein fractions VLDL, DL and HDL (very low density lipoproteins, low density lipoproteins and high density lipoproteins, respectively) were isolated by preparative ultracentrifugation.

Changes in the concentration and composition of lipids and lipoproteins in primary hyperlipoproteinemia during treatment with bezafibrate.

The effect of 2-(4-chlorobenzoyl-aminoethyl-phenoxy)-2-methylpropionic acid (bezafibrate, Cedur) at doses of 3 x 150 mg and 4 x 150 mg daily on lipids and lipoproteins in 27 patients (3 type IIa, 7 type IIb, 1 type III, 12 type IV and 4 type V) was investigated over a period of 24 weeks in a single-blind study. The lower dose was administered for the first 12 weeks and then the higher dose was given. Plasma triglycerides were reduced in all types.

[Effect of a clofibrate-inositol nicotinate combination on lipids and lipoproteins in primary hyperlipoproteinemia of types IIa, IV and V].

The effect of a combination of clofibrate and inositol nicotinate (Liporeduct forte, Liporeduct) on lipids and lipoproteins in 20 patients with primary hyperlipoproteinemia (10 type IIa, 7 type IV and 3 tyV) was investigated over a period of 16 weeks. The daily doses of clofibrate and inositol nicotinate was 1,5 g and 2,4 g in the type IIa and 1,5 g and 900 mg in the types IV and V. Placebo was given before and after the treatment period.

[Bezafibrate in primary hyperlipidemias (author's transl)].

The effect of long-term treatment over 40 weeks with Bezafibrate on lipids and lipoproteins was investigated in 27 patients with primary hyperlipoproteinemias (hlp) (12 patients with hlp type IV, 7 patients with type IIb, 3 patients with type IIa, 4 patients with type V and 1 patient with type III). Bezafibrate reduced total cholesterol by 16%, whereas HDL-cholesterol increased by 28% and 36% (p less than 0.05).