Sustained-release implants in the chemotherapy of experimental rodent malaria II

Bm, Judge; Re, Howells; Nb, Graham; Me, McNeill

doi:10.1080/00034983.1981.11687475

Cited by 7 publications

(1 citation statement)

References 4 publications

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“…were removed from the tail vein at 1, 2, 4, 6,8,10,12,24, and 26h into heparinized microhaematocrit tubes (20 pl capacity, Hawksley Lancing, UK) which were then sealed. Following centrifugation (1100g, 5 min) volumes of plasma ( 2 M 0 pl), accurately measured using a 100 p1 capacity syringe (Hamilton Ltd, Nevada, USA), were placed in microcap tubes (1-5 ml L.1.P Equipment and Services, Yorks, UK).…”

Section: Animal Studiesmentioning

confidence: 99%

The disposition of pyrimethamine base and pyrimethamine pamoate in the mouse: Effect of route of administration

Coleman

Mihaly

Edwards

et al. 1986

Biopharm & Drug Disp

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We have investigated the plasma pharmacokinetics and mass fate in mice, of pyrimethamine administered as either the base or as the poorly soluble pamoate salt, in each case by the intraperitoneal (i.p.) and subcutaneous (s.c.) routes. Following the administration of pyrimethamine base (i.p. and s.c.) and pyrimethamine pamoate (i.p.), maximum measured plasma levels of pyrimethamine were attained within 1 h, before declining monoexponentially. There was no significant difference between these three groups in the clearance (0.29 +/- 0.05, 0.30 +/- 0.03, 0.26 +/- 0.05 ml min-1), elimination half-life (4.5 +/- 0.5, 4.8 +/- 0.8, 4.9 +/- 0.5 h) and AUC (19.4 +/- 4.4, 17.3 +/- 2.2, 21.1 +/- 4.4 micrograms.h ml-1). By contrast, after s.c. dosage of pyrimethamine pamoate, drug absorption was significantly delayed, maximum plasma levels being reached after 4 h, these levels being approximately one-third of those in the other three groups. Absorption was however complete, as the values for AUC and clearance were not significantly different from the other groups. The pattern of faecal and urinary elimination of 14C radioactivity was unaffected by either dose site or formulation of pyrimethamine. The majority of the dose (44.5-64.2 per cent) was eliminated in the faeces suggesting extensive biliary excretion. Localization of 14C radioactivity in the major organs was negligible in all groups. Following each dose, between 85 and 98 per cent of the dose was accounted for. These studies indicate that of the four treatment groups only pyrimethamine pamoate on s.c. administration demonstrates a sustained release action from the dose site.(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Animal Studiesmentioning

confidence: 99%