Artocarpus altilis, which in Indonesia has a local name "sukun" referred to as breadfruit, is a tropical plant. The breadfruit tree produces fruit from March to September. The synonyms of A. altilis are A. communis, and A. incises. 5,6 An ethanol extract of A.altilis leaves actively inhibited the growth of P. falciparum in vitro with IC 50 values 1.32 μg/ml, and was highly active against P. berghei in vivo with ED 50 values 0.82 mg/kg body weight. While stem bark extract from A. altilis showed a very good in vivo activity against P. berghei, and weak in vitro activity against P. falciparum. 7 The previous study showed that another species of genus Artocarpus reported that prenylflavonoid compounds isolated from A. champeden stem bark extract. A. champeden stem bark extract contains artocarpones A, artocarpone B, artoindonesianin E, heteroflavanone C, artoindonesianin R, heterophyllin, artoindonesianin A-2, cycloheterophyllin, and artonin. Heteroflavanone C had the most active inhibition against P. falciparum with IC 50 values 1 nmol/L. 8 A prenylated chalcone, isolated from A. champeden stem bark extract, namely morachalcone A, was identified as a antimalarial active marker compound. 9 Leaves and stembark extract from another species, Artocarpus heterophyllus and Artocarpus camansi, also has been reported to have good antimalarial activity against P. falciparum and P. berghei. 7,8
Objective: This study aimed to compare the characteristics of acyclovir (ACV)-succinic acid (SA) cocrystal with grinding and slurry method.Methods: Cocrystals were prepared using grinding and slurry methods. Physicochemical characterizations were performed using powder X-raydiffraction (PXRD), differential scanning calorimetry, Fourier transform infrared (IR) spectroscopy, scanning electron microscope (SEM), anddissolution test.Results: The study revealed that cocrystal of ACV-SA showed a decrease in the melting temperature, i.e., 175.10°C, respectively, in comparison with themelting point of the constituent materials (ACV 253.53°C and SA 187.29°C). PXRD diffractogram showed that cocrystal with grinding method exhibitednew diffraction peaks at angle 2θ=8.92°, 16.24°, and 17.14°, while PXRD diffractogram of cocrystal with slurry method exhibit new diffraction peaksat angle 2θ=16.25°, and 19.63°. Characterization with IR spectroscopy showed the disappearance of transmission peaks at 3441cm disappearance ofC=O stretch at 1584cm and 1612cm. Dissolution efficiency of each treatment group calculated the efficiency of dissolution in 15th minutes, grindingmethod cocrystal with grinding time 15 minutes give the dissolution efficiency were 54.23%. Slurry method cocrystal with solvent concentration12 ml/g gives the high value of the dissolution efficiency is 74.36%. SEM micrographs showed that cocrystals prepared by solvent evaporation methodhave differences crystal form at magnification 5000× magnification compared to pure ACV and physical mixture.Conclusion: The study concluded that cocrystals of ACV-SA were successfully formed using grinding and slurry methods. The formed cocrystalsof ACV-SA exhibited different physicochemical characteristics as compared to the constituent materials. The formed cocrystals prepared by slurrymethod have a high intensity of diffraction peak on X-ray diffraction and highest dissolution efficiency at 15 minutes rather than grinding methodcocrystal.Keywords: Cocrystal, Acyclovir, Succinic acid, Grinding, Slurry, Powder X-ray diffraction, Fourier transform infrared, Dissolution rate.
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