preliminary communication
Radioiodination and preliminary in vivo investigation of the alkaloid cryptolepine

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Abstract

In this paper we report the successful labelling of cryptolepine with 131I using the chloramine T method. Quality control by ITLC of the labelled product showed 80% labelling but when the mixture was equilibrated with some amberlite (Cl) anion resin to exchange the excess free iodide, the radiochemical purity was raised to >90%. Preliminary biodistribution in a rat did not show specific localisation of the tracer; rather, rapid clearance from the blood was indicated. It appears that its main excretory pathway is the hepatobiliary tract despite its relatively small molecular weight of 365. Also, despite i.v. administration, an appreciable 8% uptake was found in the stomach at 1 h post injection, indicating the process of enterohepatic reflux. These findings may have some bearings on the antimicrobial property of the plant.

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Cited by (3)

  • Pharmacokinetics and in vivo chemosuppressive activity studies on cryptolepine hydrochloride and cryptolepine hydrochloride-loaded gelatine nanoformulation designed for parenteral administration for the treatment of malaria

    2013, Acta Tropica
    Citation Excerpt :

    Contrary to the earlier studies; cryptolepine persisted in blood up to 10 h following administration. That observation could be due to prolonged absorption from the gastrointestinal tract as well as enterohepatic circulation as suggested by Salako et al. (1985). Although the above studies provided very useful information on the pharmacokinetics of the compound, it is important that when the compound is incorporated into a dosage form, the in vivo profile be reinvestigated.

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