Arzneimittel Forsch
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Arzneimittel Forsch · Nov 1993
Randomized Controlled Trial Multicenter Study Comparative Study Clinical TrialObserver-blind study with metamizole versus tramadol and butylscopolamine in acute biliary colic pain.
To investigate the combined analgesic and spasmolytic effect of metamizole (dipyrone, Novalgin, CAS 68-89-3) this drug was compared with an opioid analgesic (tramadol) and a pure spasmolytic drug (butylscopolamine). In a multicentre, observer-blind, parallel-group study conducted in five German centres 74 patients suffering from "severe" or "excruciating" colic pain caused by a calculus in the bile duct were randomized to receive intravenously 2.5 g metamizole (25 patients), 100 mg tramadol (25 patients), or 20 mg butylscopolamine (24 patients). The three treatment groups were homogeneous for age, sex, height, weight and baseline pain intensity. ⋯ Metamizole was also more effective for the secondary efficacy endpoint, pain intensity on a 5-point ordinal scale. In the patient's overall assessment of treatment efficacy at the end of the trial, metamizole was rated as the most effective drug (p < 0.005). Fewer patients in the metamizole (3) and the tramadol (1) groups than in the butylscopolamine group (8) needed a second injection of the "rescue" medication (p < 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)
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Arzneimittel Forsch · Nov 1993
Comparative Study Clinical Trial Controlled Clinical Trial[Biological availability of gastric juice-resistant coated diclofenac preparations. 1. Bioavailability study following a single administration of a multiple-unit formulation in comparison with a single-unit formulation].
Bioavailability Study of Enteric Coated Diclofenac Formulations/1st Communication: Bioavailability study following single-dose administration of a multiple-unit formulation compared with a single-unit formulation Relative bioavailability of diclofenac (CAS 15307-86-5) was investigated after single-dose administration of an enteric coated multiple-unit formulation (Diclo-Puren 50, test) in comparison to a single-unit dosage form (reference). The study was carried out in a three-way changeover design with a group of 18 healthy male volunteers. Diclofenac plasma concentrations were measured using a selective and sensitive GLC-MS method after liquid-liquid extraction and subsequent derivatisation. ⋯ Mean relative bioavailability of the test formulation was calculated as 99%. Maximum plasma concentrations (mean +/- SD) were determined as 1159 +/- 632 ng/ml (test) and as 1481 +/- 637 ng/ml (reference). Maximum plasma concentrations (mean +/- SD) occurred 1.4 +/- 0.7 h (test) and 1.8 +/- 0.7 h (reference) after administration.(ABSTRACT TRUNCATED AT 250 WORDS)
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Arzneimittel Forsch · Nov 1993
In vitro effects of mistletoe extracts and mistletoe lectins. Cytotoxicity towards tumor cells due to the induction of programmed cell death (apoptosis).
The in vitro effects of therapeutically administered mistletoe extracts (ABNOBAviscum) and pure mistletoe lectins (mainly mistletoe lectin I) on a variety of human and murine tumor cell lines have been investigated. Mistletoe extracts and purified mistletoe lectins inhibited in vitro the growth of all tumor cell lines tested including B cell hybridomas, P815, EL-4, Ke37, MOLT-4 and U937. ⋯ Thus, fragmentation of genomic DNA into oligonucleosomal bands of approximately 200 base pairs in length was observed within 20 h when tumor cells were incubated with mistletoe extracts or lectins. These data point to a rational basis for the direct cytotoxic effects of mistletoe extracts and lectins apart from the postulated immunostimulatory properties of these agents.
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Arzneimittel Forsch · Oct 1993
Absorption, distribution and excretion of [carbonyl-14C]mosapride citrate after a single oral administration in rats, dogs and monkeys.
Absorption, distribution and excretion of mosapride citrate ((+/-)-4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morph oli nyl] methyl]benzamide citrate, AS-4370, CAS 112885-42-4), a novel gastric prokinetic drug, were studied with 14C-labeled drug in male and female rats mainly after a single oral administration. Plasma concentrations and excretion following oral administration of [14C]mosapride were also investigated in dogs and monkeys of both sexes. The main experimental dose was 10 mg/kg. ⋯ After oral administration in rats, about 40% of dosed radioactivity was excreted into urine and about 60% into feces via bile. Neither dose dependency nor sex differences was observed in excretion. In dogs, about 20% of dosed radioactivity was recovered in urine and about 70% in feces.(ABSTRACT TRUNCATED AT 400 WORDS)
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Arzneimittel Forsch · May 1993
Effect of a novel xanthine derivative on experimental ulcers in rats.
The effects of the novel xanthine derivative 3-ethyl-1-(6-hydroxy-6-methylheptyl)-7-propylxanthine (A90 6119, CAS 134072-58-5) on various experimentally induced ulcers was investigated in rats. A90 6119 produced a dose-dependent inhibition of gastric ulcers induced by water immersion stress and absolute ethanol with ED50- values of 2.4 and 2.8 mg/kg, p.o., respectively. The erosion induced by oral administration of 1.5% NH4OH (3 ml/rat) was significantly reduced by A90 6119 at 10 and 30 mg/kg, p.o. ⋯ Duodenal ulcer induced by cysteamine was also dose-dependently inhibited by A90 6119 with an ED50-value of 0.3 mg/kg, i.p. When doses of cimetidine (200 mg/kg) and A90 6119 (10 mg/kg), equipotent in the water immersion stress model, were orally given twice daily for 5 consecutive days before the induction of gastric ulcers by stress, the H2-receptor antagonist aggravated significantly the ulcer formation while the xanthine derivative did not show such an effect. These data suggest that the 3-ethylxanthine A90 6119 possesses pronounced anti-ulcer activity and that its repeated administration might not aggravate ulcer formation and might reduce the incidence of recurrence.