Publication: An improved formulation of chloroquine for intramuscular administration: absorption kinetics in rabbits
Issued Date
1989-01-01
Resource Type
ISSN
20427158
00223573
00223573
Other identifier(s)
2-s2.0-0024835177
Rights
Mahidol University
Rights Holder(s)
SCOPUS
Bibliographic Citation
Journal of Pharmacy and Pharmacology. Vol.41, No.10 (1989), 726-728
Suggested Citation
S. Prakongpan, S. Sirimai, G. Edwards, C. S. Mcgrath, N. J. White An improved formulation of chloroquine for intramuscular administration: absorption kinetics in rabbits. Journal of Pharmacy and Pharmacology. Vol.41, No.10 (1989), 726-728. doi:10.1111/j.2042-7158.1989.tb06352.x Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/15882
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Title
An improved formulation of chloroquine for intramuscular administration: absorption kinetics in rabbits
Abstract
Intramuscular chloroquine is rapidly absorbed, even in severe falciparum malaria, and may cause potentially lethal hypotension. Less rapidly absorbed formulations should be safer. A chloroquine phosphate solution containing 2% methylcellulose 1500 released chloroquine 2·6 times more slowly than a commercial aqueous solution in an in‐vitro absorption simulator. There was a log linear relationship between viscosity and release rate. The absorption pharmacokinetics of the more viscous chloroquine phosphate solution were then compared with those of a commercial solution after intramuscular injection to eight rabbits in an open cross over comparison. The rate of absorption was over three times slower with the viscous solution; median time to peak whole blood concentration with the commercial aqueous solution was 10 (range 5–20) min compared with 30 (range 10–60) min for the more viscous formulation (P < 0·05). Peak whole blood concentrations were 66% (95% CI 50–82%) of those with the commercial preparation, but the acute bioavailability of the two solutions was similar. This simple new formulation may be safer than currently available chloroquine preparations and should now be evaluated in man. 1989 Royal Pharmaceutical Society of Great Britain