A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using BSLT and MTT assay against Vero, HeLa, and MCF7 cell lines. The structures of the synthesized compounds were confirmed by FTIR, 1H-NMR, 13C-NMR, and mass spectral data. The results of the cytotoxicity evaluation showed that the synthesized compounds exhibited moderate to very high toxic activity in BSLT (LC50 value 29.80–1704.23 µM); most of the compound exhibited cytotoxic activity against HeLa cell lines, which is comparable to the activity of cisplatin (IC50 value 40.65–95.55 µM), and most of the compound tested against MCF7 cell lines exhibited moderate to very high cytotoxic activity (IC50 value 7.86–35.88 µM). However, the selectivity index (SI) of the compounds was low (<1–1.96). Among the synthesized compounds, compound 1b was the most cytotoxic and selective against MCF7 cell lines. It could be considered for further development to obtain the more active and selective chemotherapeutic agents against breast cancer.
Determination of sibutramine adulterated in herbal slimming product using thin layer chromatography (TLC) densitometric method with TLC silica gel 60 F 254 aluminium plate as stationary phase and mixture of toluen-diethylamine (10:0.3) as mobile phase has been developed. The calibration curve in the concentration range of 0.50 to 5.00µg/spot showed good linier relationship (r 2 = 0.9986). The limit of detection and quantitation (LOD and LOQ) were 217.5ng and 724.9ng/spot, respectively. The method gave satisfactory specificity, linierity, precision and accuracy validation criteria and was applied for determination of sibutramine in herbal slimming products obtained from several drugstrores in Depok City, West Java, Indonesia. Results of the determination showed that six of seven samples analyzed were detected containing sibutramine HCl w ith the concentration of 2.45-26.24mg in a single dosage of slimming herbal products.
Aim: Determination of the bioequivalence of two metformin HCl (750 mg) caplet formulations (Glucophage XR® from Bristol-Myres Squibb Company, Indonesia as a reference formulation and Glumin XR® from Ferron Par Pharmaceutical, Indonesia as a test formulation). Material and method: The study was conducted according to an open label, randomized, Two-period crossover design with a 1 week washout period. Twelve volunteers participated and all completed the study successfully. Blood samples were obtained prior to dosing and at 1.0; 1.5; 2.0; 2.5; 3.0; 3.5; 4.0; 6.0; 8.0; 10.0; 14.0; 18.0; 24.0 and 30.0 hours after drug administration. Plasma will be separated by centrifuge and stored frozen at-20 degree Celcius. Plasma concentration of metformin HCl was monitored using high performance liquid chromatography (HPLC) with photo diode array (PDA) detection over a period of 30 hours after administration. The pharmacokinetics parameter AUC 0-30 h, AUC 0-∞ and Cmax were tested for bioequivalence after log transformation of data and ratios of Tmax were evaluated non parametrically. Result: The point estimates and 90% confidence interval for AUC 0-30 h, AUC 0-∞ and Cmax were 101.88 % (94.78-109.50%), 101.50% (93.77-109.87%) and 105.93 % (97.00-115.98%), respectively, satisfying the bioequivalence criteria of the European Committee for Proprietary Medicinal Products and The US Food and Administration Guidelines. Conclusion: These results indicate that two medications of metformin HCl are bioequivalent, thus, may be prescribed interchangeably.
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