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Biomedical subjects

T Mellstrand

Publications and source records attributed to T Mellstrand.

30 records · Page 2Linked to original sources

Pharmacokinetic properties of noscapine.

Noscapine was administered to five healthy volunteers in a randomized crossover design, as an intravenous infusion of 66 mg, and as an oral 150 mg dose of either rapidly dissolving tablets or a tablet containing ion exchange resin-bound noscapine. After i.v. administration, the disposition of noscapine was bi-exponential with an elimination half-life of 2.6 h; the total plasma clearance was 22 ml/min/kg and the volume of distribution (Vdarea) was 4.7 l/kg. The absolute oral bioavailability was 30%, with a 3.6-fold interindividual variation. There was no pharmacokinetic evidence to support a prolonged action of the ion exchange resin tablet.

Administration, Oral↗

Bioavailability of theophylline from three different tablets in asthmatic patients and their bronchodilating effects in combination with terbutaline inhalation.

The bioavailability of three different theophylline tablets (microcrystallinic theophylline, Theolair, Nuelin, 3M Riker), choline theophyllinate as a new film-coated tablet (Teovent, Ferrosan, Sweden) and theophyllaminopropanol (Oxyphylline, Draco, Sweden) was investigated in eight adult asthmatics and a randomized, double-blind, cross-over study. Effects on ventilatory capacity (FEV1 and FVC), circulation (heart rate and blood pressure) and skeletal muscle tremor were followed. The theophylline concentration was determined by gas chromatography. Forty-five minutes after theophylline administration the plasma concentrations were almost the same for all four formulations. The bioavailability was also almost identical. The half-life for intravenous theophylline in these asthmatics was 7.4 +/- 0.64. The three tablet formation had equal effect on FEV1 and the effect was sustained throughout the 6-h period. Six hours after theophylline administration five terbutaline inhalations induced the same further increase in FEV1. The results indicate that theophylline alone has only a moderate acute bronchodilating effect at recommended plasma concentrations but gives a good effect when combined with inhaled beta 2-adrenostimulants.

Administration, Intranasal↗

Treatment of podophyllin poisoning with resin hemoperfusion.

1 A 43-year-old man was admitted in a coma after oral ingestion of a suspected lethal dose of podophyllin solution in alcohol. 2 Hemoperfusion with a resin filter was started 7 h after ingestion. Hemoperfusion rapidly decreased plasma concentrations of podophyllotoxin with an extraction ratio of 0.76 over the filter. The relatively low plasma concentrations of podophyllotoxin and consequently small amount removed might be explained by the rapid metabolism of the drug to an unknown derivate. 3 This metabolite was completely cleared during passage over the filter, suggesting the removal of significant amounts of podophyllotoxin metabolites. 4 No neurological deficit was observed before or after hemoperfusion. At a two-month follow-up the patient remained healthy. Hemoperfusion may possibly prevent the development of coma and neurologic deficit with loss of deep tendon reflexes.

Adult↗

Resin hemoperfusion in chloroquine poisoning.

A 46-year-old woman was admitted after ingestion of 10 g chloroquine phosphate. The patient's clinical condition deteriorated with characteristic ECG changes, low blood pressure, and respiratory depression. Resin hemoperfusion (HP) was started 4.5 h after admission at a flow of 250 mL/min for 4 h. Clearance over the resin column was 136 mL/min. Although the patient rapidly improved, a total of no more than 200 mg (2%) was removed. Total body clearance of chloroquine was increased by only 5% during HP. Treatment should therefore be directed toward aggressive supportive therapy rather than techniques to increase elimination.

Chloroquine↗

A comparison of steady state plasma theophylline concentrations with conventional and sustained release formulations.

The absorption of theophylline from a sustained release formation (Phyllocontin) in relation to drug absorption from a conventional formulation was assessed at steady state in a multiple-dose study. Seven healthy adult subjects were studied using a two 5-day period crossover design. The data from this study indicate that the sustained release tablet has acceptable sustained release characteristics and should provide both reliable and complete drug absorption, giving it advantage over conventional formulations during chronic therapy of patients with reversible airways obstruction.

Administration, Oral↗

Absorption of theophylline from conventional and sustained-release tablets.

Healthy adults were treated in periods of 4 days with fast-dissolving theophylline tablets (Oxyphyllin, Draco, Sweden) and sustained-release tablets (Theo-Dur, Draco, Sweden). To some of the volunteers a single dose of i.v. aminophyllamine was administered. The absorption of theophylline, calculated from single dose administration of uncoated tablets (Oxyphyllin) was completed within 2 hrs, whereas the absorption from sustained-release tablets (Theo-Dur) continued for 12 hrs. There was no significant difference in bioavailability between aminophylline i.v., Oxyphyllin tablets and Theo-Dur tablets. The slow-release tablet gave a stable plasma level in steady state that implies the possibility of using 12-hr dosage intervals and still achieving a stable theophylline concentration in steady state with a small difference between peak and trough concentrations. This investigation shows that it is possible to simulate the plasma concentration of theophylline in steady state by means of oral administration, using the simple one-compartment model calculated from data registered after a single i.v. dose.

Adult↗

Absorption of theophylline from conventional and sustained-release tablets.

Healthy adults were treated in periods of 4 days with fast dissolving theophylline tablets (Oxyphyllin, Draco, Sweden) and sustained-release tablets (Theo-Dur, Draco, Sweden). To some of the volunteers, a single dose of i.v. aminophyllamine was administered. The absorption of theophylline, calculated from a single dose administration, of uncoated tablets (Oxyphyllin) was completed within 2 hours, whereas the absorption of sustained-release tablets (Theo-Dur) continued during 12 hours. There was no significant difference in bioavailability between aminophylline i.v., Oxyphyllin tablets and Theo-Dur tablets. The slow release tablets gave a stable plasma level in steady state that implies the possibility of using 12-hour dosage intervals and still achieve a stable theophylline concentration in steady state with a small difference between peak and trough concentrations. This investigation shows that it is possible to simulate the plasma concentration of theophylline in steady state by means of oral administration, using the simple one-compartment model calculated from data registered after a single i.v. dose.

Aged↗