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Palustop: antimalarial suppository from Cameroon for children

December 7, 2015 - 21:17 -- Pierre Lutgen

Rosine D. Chougouo NKuitchou1, Ernest Djoko1, Jonas Kouamouo1, Diane F. Domko1, Pierre Tane2, Denis Wouessidjewe1,3. 

1 Faculty of Pharmacy, Université des Montagnes »P O Box 208 Bangangte, Cameroon 2 Laboratory of Natural Products Chemistry, Faculty of Sciences, University of Dschang P O Box 67 Dschang Cameroon 3 UFR of Pharmacy, Department of Molecular Pharmacochemistry, University of Joseph Fourrier of Grenoble PO Box 53 38041 Grenoble Cedex 9.

 

Drug resistance to conventional antimalarial drugs leads to the need to develop new approaches or to better exploit medicinal herbs which according to WHO still represent 70% of the treatments in Africa. Several studies, for instance those of Chougouo and al. (Thesis, Université des Montagnes, Cameroon, 2006) showed that the infusion of Artemisia annua is more efficient than the Artemisinin-based Combination Therapy (AC) after 7 days of treatment, but hardly accepted by children mostly those under 2 years old because of the quantity to administer and the bitter taste of the preparations. Therefore, the interest of the present study with the aim to produce a more acceptable dosage form for children: suppositories made from leaves and stems powder of A. annua grown in Cameroon.

To evaluate its quality, the powder of leaves and stems of A. annua has been submitted to physicochemical analysis. The particle size has been determined by the sieve method and by laser diffraction. Artemisinin content has been determined by TLC – densitometry, total flavonoids have been titrated by aluminium chloride. The formula per unit of our suppositories has been established and suppository products have been submitted to pharmacotechnical tests (organoleptic, the average weight, desintegration time, fusion point). The powder obtained, of bitter taste, greyish-green, with characteristic odor (camphor), is homogeneous with 56,37 % of particles in the sieve of a diameter over or equal to 63 μm.

The artemisinin and entire flavonoids contents are respectively of 5 mg/g and 0,43 mg equivalent to quercetin per gram of dry matter. The suppositories contain 250 mg of active principle (1 gramm of A.annua powder for 0,72 g of the semi-synthetic glyceride Suppocire C). They are dark-green, shiny, smooth, barrel-shaped. Their average weight is 2,15 g, desintegration time 8 min 16 s, the fusion point 35,7 ˚C and the artemisinin and flavonoids contents do not change. The A. annua suppositories produced by our laboratory are in conformity with European pharmacopoeia.

They offer the potential of a better and easier treatment of malaria in small children.

Clinical trials will be run with Palustop suppositories.