Abstract: Substandard and counterfeit antimalarials is a major problem in malaria endemic areas. The availability of counterfeit/ substandard medicines is not only decreasing the efficacy in patients, but it is also one of the contributing factors for developing antimalarial drug resistance. Owing to this, a pilot study was conducted to survey quality of drugs collected from different malaria endemic areas of India. Artesunate+Sulphadoxine-Pyrimethamine (AS+SP), Artemether-Lumefantrine (AL), Chloroquine (CQ) tablets were randomly picked from public health facilities in selected states of India. The quality of antimalarial drugs from these areas was assessed by using Global Pharma Health Fund Minilab test kit. This includes physical/visual inspection and disintegration test. Thin-layer chromatography (TLC) was carried out for semi-quantitative assessment of active pharmaceutical ingredients. A total of 45 brands, out of which 21 were for CQ, 14 for AL and 10 for AS+SP were tested from Uttar Pradesh (U.P.), Mizoram, Meghalaya and Gujrat states. One out of 45 samples showed variable disintegration and retension factor. The variable disintegration and retention factor which would have been due to substandard quality or other factors including storage. However, HPLC analysis confirms standard active pharmaceutical ingredient, but may be due to humid temperature and moisture in storage may account for the observed result.
Abstract: Five crystal modifications of water insoluble
artesunate were generated by recrystallizing it from various solvents
with improved physicochemical properties. These generated crystal
forms were characterized to select the most potent and soluble form.
SEM of all the forms showed changes in external shape leading them
to be different morphologically. DSC thermograms of Form III and
Form V showed broad endotherm peaks at 83.04oC and 76.96oC prior
to melting fusion of drug respectively. Calculated weight loss in TGA
revealed that Form III and Form V are methanol and acetone solvates
respectively. However, few additional peaks were appeared in XRPD
pattern in these two solvate forms. All forms exhibit exothermic
behavior in buffer and two solvates display maximum ease of
molecular release from the lattice. Methanol and acetone solvates
were found to be most soluble forms and exhibited higher
antimalarial efficacy showing higher survival rate (83.3%) after 30
days.