摘要：The aim of this study was to design and evaluate extended-release formulations of a model drug,nicorandil,in order to achieve the desired steady-state plasma concentration of drug in *** was employed to estimate optimum dissolution and absorption rate of *** dissolution test was employed using pH 1.2,4.0,6.8 buffer solution,or water,to measure the in vitro release behaviors of nicorandil formulations.A single dose(15 mg)of each formulation was orally administered to four beagle dogs under fasted conditions,and the pharmacokinetic parameters were *** in vitro/in vivo relationship of the extended-release formulation was confirmed using in vitro dissolution profiles and plasma concentrations of drug in beagle *** was released completely within 30 min from the immediate-release tablets and released for 24 h from the extended-release *** nicorandil plasma concentration could be modified by adjusting the drug release rate from the extended-release *** release rate of nicorandil was the rate-limiting step in the overall absorption of drug from the extendedrelease *** results highlight the potential of a nicorandil extended-release formulation in the treatment of angina pectoris.

摘要：An optimized formulation of capsules containing Lansoprazole enteric-coated pellets using D-Optimal design with a polynomial statistical model were prepared by using Eudragit?L100 as an enteric coated polymer to provide resistance to simulated gastric acid dissolution in buffer media. D-Optimal experimental design was used to determine the optimal level for three coating layers that were applied to formulate the enteric-coated pellets including a drug loading layer, a sub-coating, and an outer enteric coating. Dissolution studies were performed on the prepared Lansoprazole capsules. Less than 5 percent of Lansoprazole was released in 60 minutes in an acidic dissolution medium (pH 1.2) and greater than 90 percent of active ingredient was released in the next 60 minutes in a buffer dissolution medium (pH 6.8). The Lansoprazole capsules were stable with no observable change in physico-chemical properties in accelerated and normal storage conditions for 6 and 18 months, respectively. The pharmacokinetic parameters Cmax, Tmax, AUC0-t, and AUC0-∞ were determined after administration of the D-Optimal design optimized capsules of LPZ to healthy beagle dogs and were statistically compared to Gastevin? capsules as a reference (KRKA, Slovenia) using the non-compartmental method with the aid of WinNonlin 5.2 software. The analysis of variance showed that the two formulations did not demonstrate bioequivalence using a 90% confidence interval range (80% - 120%) of Cmax, AUC0-t, and AUC0-∞. No significant difference in Tmax was found at the 0.95 significance level using the Wilcoxon signed-rank test. D-Optimal Experimental Design provided definitive direction for an optimal formulation of capsules containing enteric-coated pellets of lansoprazole loaded within the coating of pellets that provided similar bioequivalence to Gastevin.

摘要：Objective Sulfanilamide,sulfadiazine,and dapsone were the first sulfonamides to be used to treat malaria by disrupting the folate biosynthesis process,which is essential for parasite ***,we aimed to synthesize novel N-(2-arylaminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide derivatives through a rational drug design *** All compounds were synthesized by the conventional method,and the products were characterized by spectral analysis(1 H NMR and mass spectrometry).The progression of the reaction was monitored using thin-layer chromatography(TLC).All the derivatives were analyzed for their effective binding mode in the allosteric site of the plasmodium cysteine protease *** and antifungal activities were determined using the broth dilution *** S6(N-(2-thiazol-4 yl)-acetyl-aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide and S9(N-(1 H-benzo[d]imidazol-2-yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide formed five hydrogen bonds;S8(N-(2-1 H-imidazol-2 yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide and S10(N-(1 H-benzo[d]imidazol-5-yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide formed four hydrogen bonds with the allosteric site of the *** the docking scores and formation of hydrogen bonds with the target enzyme,the novel derivatives were processed for wet lab *** the newly synthesized derivatives were subjected to in vitro antimalarial,antifungal,and antibacterial *** the derivatives exhibited sufficient sensitivity to the Plasmodium falciparum strain compared to the ***,compounds S9 and S10 showed the most potent dual antimicrobial and antimalarial *** also exhibited powerful molecular interactions in molecular docking *** Based on the above results,it was concluded that N-(2-arylaminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide derivatives have excellent biological potential to act as antimalarial,antifungal,