สารบัญ

Category Antiprotozoal (antimalarial).

Artesunate Tablets contain not less than 90.0 per cent and not more than 110.0 per cent of the labelled amount of C₁₉H₂₈O₈.

Strength available 50 mg.

Dose Initial, 5 mg per kg of body weight on the first day. Maintenance, 2.5 mg per kg of body weight for a minimum of 4 days.
          To effect radical cure, a 3-day course of artesunate should be used in combination with a single oral dose of mefloquine 15 mg per kg of body weight (or occasionally 25 mg per kg of body weight if necessary) on the second day.

Warning See under Artesunate, p. 31.

Packaging and storage Artesunate Tablets shall be stored at a temperature not exceeding 25º.

Identification
          A. To a quantity of the powdered tablets equivalent to 50 mg of artesunate add 25 ml of acetone, shake to dissolve, and filter. Evaporate the filtrate at low temperature and dry overnight over self-indicating silica gel. The infrared absorption spectrum is concordant with the spectrum obtained from Artesunate RS (Appendix 2.1) or with the reference spectrum of Artesunate.
          B. Carry out the test as described in the “Thin-layer Chromatography” (Appendix 3.1), using silica gel GF254 as the coating substance and a mixture of 5 volumes of ethyl acetate and 95 volumes of toluene as the mobile phase. Apply separately to the plate, 2 μl of the following two solutions in toluene. For solution (A) shake a quantity of the powdered tablets equivalent to 0.1 mg of artesunate in absolute ethanol, filter and evaporate. Dissolve the residue in 1.0 ml of toluene. For solution (B) use 0.10 mg of Artesunate RS per ml. After removal of the plate, allow it to dry in air, spray with anisaldehyde TS, heat the plate to 120º for 5 minutes and examine under ultraviolet light (254 nm): the principal spot obtained from solution (A) corresponds in position, appearance and intensity to that obtained from solution (B).
          C. To a quantity of the powdered tablets equivalent to 100 mg of artesunate add 40 ml of absolute ethanol,
shake to dissolve, and filter. To half of the filtrate (keep the remaining filtrate for test D) add about 0.5 ml of hydroxylamine in ethanol (60 per cent) TS and 0.25 ml of sodium hydroxide TS. Heat the mixture in a water-bath to boiling, cool, and add 2 to 3 drops of dilute hydrochloric acid and 1 drop of iron(III) chloride TS: a light red-violet colour is produced.
          D. Evaporate the remaining filtrate from Test C on a water-bath to a volume of about 5 ml. Place a few drops of the mixture on a white porcelain dish, add one drop of vanillin-sulfuric acid TS1, and allow to stand for 30 minutes: a red colour is produced.

Related substances Carry out the test as described in the “Thin-layer Chromatography” (Appendix 3.1), using silica gel G as the coating substance.
          Reference solution 1, Reference solution 2, Mobile phase, and Procedure Proceed as directed in the Related substances under Artesunate, p. 32.
          Test solution Shake a quantity of the powdered tablets equivalent to about 10 mg of artesunate with 2 ml of dichloromethane, filter, and use the filtrate.

Assay Weigh and powder not less than 20 Artesunate Tablets. To a quantity of the powder equivalent to about 500 mg of artesunate, accurately weighed, add 50.0 ml of neutralized ethanol, shake thoroughly, filter, and discard about 10 ml of the initial filtrate. Titrate 25.0 ml of the filtrate with 0.05 M sodium hydroxide VS, using dilute phenolphthalein TS as indicator. Perform a blank determination, and make any necessary correction. Each ml of 0.05 M sodium hydroxide is equivalent to 19.22 mg of C₁₉H₂₈O₈.

Other requirements Comply with the requirements described under “Tablets” (Appendix 1.16).