AIM： To compare the efficacy and safety of five days apostrophe therapy of mebendazole （MBZ） versus quinacrine （QC） on human giardiasis in children.METHODS： A clinical trial was carried out in paediatric patien...AIM： To compare the efficacy and safety of five days apostrophe therapy of mebendazole （MBZ） versus quinacrine （QC） on human giardiasis in children.METHODS： A clinical trial was carried out in paediatric patients （aged 5-15 years） with confirmed symptomatic G. duodenalis mono-infection. Patients were randomly assigned to receive either MBZ [200 mg taken three times per day GRID） （n = 61）] or QC [2 mg/kg bodyweight tid （n = 61）], both for five days. Follow-up faecal samples were obtained at 3, 5 and 7 d after the end of the treatment.RESULTS： Although the frequency of cure was higher for QC （83.6%） than for MBZ （78.7%）, the difference was not statistically significant （P 〉 0.05）. Adverse events were reported more in the QC group （P 〈 0.05）, all of them transient and self-limiting.CONCLUSION： Despite final cure rates ocurring lower than expected, the overall results of this study reconfirmed the efficacy of MBZ in giardiasis and also indicate that, although comparable to QC, at least in this setting the 5 d course of MBZ did not appear to improve the cure rates in this intestinal parasitic infection.展开更多
A new imidazolium compound, C15H17N4ClO4, was prepared from a flexible bidentate ligand of 1,3-di(imidazol-1-ylmethyl)-5-methylbenzene, and characterized by X-ray analysis. It is of orthorhombic, space group Pnma with...A new imidazolium compound, C15H17N4ClO4, was prepared from a flexible bidentate ligand of 1,3-di(imidazol-1-ylmethyl)-5-methylbenzene, and characterized by X-ray analysis. It is of orthorhombic, space group Pnma with a = 8.182(2), b = 12.874(3), c = 15.611(4) ? V = 1644.4(7) 3, Dc = 1.425 g/cm3, Z = 4, Mr = 352.78, m(MoKa) = 0.944 mm-1, F(000) = 736, S = 1.036, the final R = 0.0521 and wR = 0.1187 for 1128 observed reflections (I > 2s(I)). An infinite one-dimensional zigzag chain is formed by NH…N hydrogen bonding interactions between the imidazolium salt cations.展开更多
Abstract： The objective was to obtain solid dispersion to improve the dissolution rate, solubility and oral absorption of MB （mebendazole）, poor water-soluble drugs. The new formulation was characterized by DSC （d...Abstract： The objective was to obtain solid dispersion to improve the dissolution rate, solubility and oral absorption of MB （mebendazole）, poor water-soluble drugs. The new formulation was characterized by DSC （differential scanning calorimetry）, PXRD （powder X-ray diffraction）, FT-1R （fourier transform infrared spectroscopy） and STEM （scanning transmission electron microscopy） methods. Solid dispersions of MB with polyvinylpyrrolidone K-30 （PVP K30） were prepared by solvent evaporation method. The solubility of MB （original powder） and that of the solid dispersions was measured at 25℃ in ethanol-water. The aqueous solubility of MB was favoured by the presence of the polymer in solvent mixtures. Combination of solid dispersions with co-solvents increased the water solubility of MB in a larger extent that each method separately. Solubility parameter （o） was used to relate to solubility profiles. MB and the solid dispersions show a solubility curve with a single peak at 51 = 30.78 MPav2. Solid state characterizations indicated that the solid dispersion exist an amorphous material entrapped in polymer matrix getting highest improvement in wettability and solubility.展开更多
The compound 1,3,5-tris(benzimidazol-1-ylmethyl)-2,4,6-trimethylbenzene, crystallizes in the monoclinic system, space group P21/c, with a = 17.571(4), b = 10.860(2), c = 14.126(3) ?; ( = 92.89(3)(, V = 2692(1) ?3, Dc ...The compound 1,3,5-tris(benzimidazol-1-ylmethyl)-2,4,6-trimethylbenzene, crystallizes in the monoclinic system, space group P21/c, with a = 17.571(4), b = 10.860(2), c = 14.126(3) ?; ( = 92.89(3)(, V = 2692(1) ?3, Dc = 1.260 g/cm3, Z = 4, C33H30N6, Mr = 510.63, ((MoK() = 0.077mm-1, F (000) = 1080. The structure was refined to R = 0.0592, wR = 0.1379 for 1492 (I(2((I)) reflections. The title molecule has cis, trans, trans-conformation about the central phenyl ring. The screw-related molecules are connected by hydrogen bonds C-H(((N (x, -0.5-y, 0.5+z) and form the infinite helical chains. The polar molecular chains are antiparallelly stacked through edge-to-face C-H…πinteractions.展开更多
The title compound [ClCH2(C7H6N2)]NO3 has been prepared and characterized by elemental analysis and X-ray studies. It crystallizes in the monoclinic system, space group P21/n with a = 7.4189(3), b =15.3064(6), c = 9.2...The title compound [ClCH2(C7H6N2)]NO3 has been prepared and characterized by elemental analysis and X-ray studies. It crystallizes in the monoclinic system, space group P21/n with a = 7.4189(3), b =15.3064(6), c = 9.2657(3) ? b = 102.449(2)? C8H8ClN3O3, Mr = 229.62, V = 1027.44(7) 3, Z = 4, Dc = 1.484 g/cm3, F(000) = 472, = 0.363 mm-1, R = 0.0671 and wR = 0.1546. The crystal structure consists of discrete 2-chloromethyl-1H-benzimidazole cations and NO3- anions. The benzimidazole ring with the conjunction carbon atom C(1) is fairly planar, with the deviation from the least plane through the ring atoms is smaller than 0.010(3) ? The analytical results of crystal structure show that three different non-covalent interactions in the compound, NH…O intermolecular hydrogen bonds, CH…O interaction and p-p stacking interaction, play an important role in the crystal packing.展开更多
文摘AIM： To compare the efficacy and safety of five days apostrophe therapy of mebendazole （MBZ） versus quinacrine （QC） on human giardiasis in children.METHODS： A clinical trial was carried out in paediatric patients （aged 5-15 years） with confirmed symptomatic G. duodenalis mono-infection. Patients were randomly assigned to receive either MBZ [200 mg taken three times per day GRID） （n = 61）] or QC [2 mg/kg bodyweight tid （n = 61）], both for five days. Follow-up faecal samples were obtained at 3, 5 and 7 d after the end of the treatment.RESULTS： Although the frequency of cure was higher for QC （83.6%） than for MBZ （78.7%）, the difference was not statistically significant （P 〉 0.05）. Adverse events were reported more in the QC group （P 〈 0.05）, all of them transient and self-limiting.CONCLUSION： Despite final cure rates ocurring lower than expected, the overall results of this study reconfirmed the efficacy of MBZ in giardiasis and also indicate that, although comparable to QC, at least in this setting the 5 d course of MBZ did not appear to improve the cure rates in this intestinal parasitic infection.
基金the Natural Science Foundation of Jiangsu province (Grant No Bk2001031)
文摘A new imidazolium compound, C15H17N4ClO4, was prepared from a flexible bidentate ligand of 1,3-di(imidazol-1-ylmethyl)-5-methylbenzene, and characterized by X-ray analysis. It is of orthorhombic, space group Pnma with a = 8.182(2), b = 12.874(3), c = 15.611(4) ? V = 1644.4(7) 3, Dc = 1.425 g/cm3, Z = 4, Mr = 352.78, m(MoKa) = 0.944 mm-1, F(000) = 736, S = 1.036, the final R = 0.0521 and wR = 0.1187 for 1128 observed reflections (I > 2s(I)). An infinite one-dimensional zigzag chain is formed by NH…N hydrogen bonding interactions between the imidazolium salt cations.
文摘Abstract： The objective was to obtain solid dispersion to improve the dissolution rate, solubility and oral absorption of MB （mebendazole）, poor water-soluble drugs. The new formulation was characterized by DSC （differential scanning calorimetry）, PXRD （powder X-ray diffraction）, FT-1R （fourier transform infrared spectroscopy） and STEM （scanning transmission electron microscopy） methods. Solid dispersions of MB with polyvinylpyrrolidone K-30 （PVP K30） were prepared by solvent evaporation method. The solubility of MB （original powder） and that of the solid dispersions was measured at 25℃ in ethanol-water. The aqueous solubility of MB was favoured by the presence of the polymer in solvent mixtures. Combination of solid dispersions with co-solvents increased the water solubility of MB in a larger extent that each method separately. Solubility parameter （o） was used to relate to solubility profiles. MB and the solid dispersions show a solubility curve with a single peak at 51 = 30.78 MPav2. Solid state characterizations indicated that the solid dispersion exist an amorphous material entrapped in polymer matrix getting highest improvement in wettability and solubility.
基金the National Natural Science Foundation of China and Natural Science Foundation of Guangdong Province.
文摘The compound 1,3,5-tris(benzimidazol-1-ylmethyl)-2,4,6-trimethylbenzene, crystallizes in the monoclinic system, space group P21/c, with a = 17.571(4), b = 10.860(2), c = 14.126(3) ?; ( = 92.89(3)(, V = 2692(1) ?3, Dc = 1.260 g/cm3, Z = 4, C33H30N6, Mr = 510.63, ((MoK() = 0.077mm-1, F (000) = 1080. The structure was refined to R = 0.0592, wR = 0.1379 for 1492 (I(2((I)) reflections. The title molecule has cis, trans, trans-conformation about the central phenyl ring. The screw-related molecules are connected by hydrogen bonds C-H(((N (x, -0.5-y, 0.5+z) and form the infinite helical chains. The polar molecular chains are antiparallelly stacked through edge-to-face C-H…πinteractions.
基金the Natural Science Foundation of Shandong province (No. Y2002B06)the Outstanding Adult-Young Scientific Research Encouraging Foundation of Shandong province (No. O1BS18)
文摘The title compound [ClCH2(C7H6N2)]NO3 has been prepared and characterized by elemental analysis and X-ray studies. It crystallizes in the monoclinic system, space group P21/n with a = 7.4189(3), b =15.3064(6), c = 9.2657(3) ? b = 102.449(2)? C8H8ClN3O3, Mr = 229.62, V = 1027.44(7) 3, Z = 4, Dc = 1.484 g/cm3, F(000) = 472, = 0.363 mm-1, R = 0.0671 and wR = 0.1546. The crystal structure consists of discrete 2-chloromethyl-1H-benzimidazole cations and NO3- anions. The benzimidazole ring with the conjunction carbon atom C(1) is fairly planar, with the deviation from the least plane through the ring atoms is smaller than 0.010(3) ? The analytical results of crystal structure show that three different non-covalent interactions in the compound, NH…O intermolecular hydrogen bonds, CH…O interaction and p-p stacking interaction, play an important role in the crystal packing.
