Objective:To investigate the efficacy and effectiveness of albendazole and mebendazole in the treatment of Ascaris lumbricoides(A.lumbricoides) in the North-Western Indonesia.Methods: 229 primary school children who w...Objective:To investigate the efficacy and effectiveness of albendazole and mebendazole in the treatment of Ascaris lumbricoides(A.lumbricoides) in the North-Western Indonesia.Methods: 229 primary school children who were positive for A.lumbricoides in their stool were recruited in the study.123 children received single-dose of 400 mg albendazole and 106 children received single-dose 500 mg of mebendazole.After 1 week,their stools were examined for the cure rate (CR) and egg reduction rate(ERR).Egg culture was also performed and observation was made on week-1,-3,-4.Results:have shown a non-significant difference in CR 96.7%vs.100%:and ERR of 99.3%vs.100.0%for albendazole and mebendazole groups respectively(P】0.05).In-vitro egg culture has shown trends of decrease in the percentage of the unfertilized eggs and in≥2 cell eggs in both treatment groups(P【0.05).The embryonated eggs from the albendazole groups has shown an increase from 7.3%on week-1 to 13.8%on week-4,whilst the mebendazole group has shown a constant increase during the whole 4 weeks of culture from 7.5%to 28.3%(P【0.01). Conclusions:No evidence of drug resistance is noted so far from the area of North-Western part of Indonesia.In addition,although both drugs showed incomplete ovicidal effects,single-dose albendazole is better than mebendazole in sterilizing A.lumbricoides eggs.展开更多
Nanosizing by wet beads milling is a method to improve the solubility of poorly water soluble compounds[1,2].Mebendazole(MBZ)is a well-known anthelmintic drug in wide clinical use.There were some reports that MBZ had ...Nanosizing by wet beads milling is a method to improve the solubility of poorly water soluble compounds[1,2].Mebendazole(MBZ)is a well-known anthelmintic drug in wide clinical use.There were some reports that MBZ had the anticancer effect in preclinical study.However,the bioavailability of MEB is low(<10%)due to the poor solubility in water(0.5μg/mL).The present study aimed to develop the nanocrystal formulations of MEB to improve dissolution behavior and enhance oral absorption.展开更多
A total of 309 cases infected with ascariasis and trichuriasis were selected as subjects, of whom 177 cases received mebendazole tablet 500mg/d for the treatment of ascariasis and trichuriais,132 cases received mebend...A total of 309 cases infected with ascariasis and trichuriasis were selected as subjects, of whom 177 cases received mebendazole tablet 500mg/d for the treatment of ascariasis and trichuriais,132 cases received mebendazole tablet 200mg/d for three days, Before and after the treatment, all the patients' feces were examined with Kato's technique, the results indicated that the cure rate of ascariasis was 71. 4% (70/98) in the experiment group and 78. 6% (66/84) in the control group respectively; There was no difference between the two groups (P > 0. 05 ). The cure rate of trichuriasis infection was 87. 5% (14/16 ) in the experimental group and 93. 3% (14/15 ) in the control group;There was also no difference between the two groups (P= 0. 401 ). But the cure rate of mixed infection of ascariasis and trichuriasis was 54. 0% (34/63) and 75. 8% (25/33) respectively; The cure rate of the experimental group was apparently lower than the that of the control group (P < 0. 05 ). The average reduced rate of egg count in per gram feces (E,P, G ) for ascariasis infection was 63. 6% (14/22) in the experimental group and 93. 8% (15/16) in the control group. In conclusion, to treat ascariasis and trichuriasis infection with mebendazole tablet should be used the three-day therapy with a total dose of 600mg or 1200mg.展开更多
In the current study, hydatid cysts from livers and lungs of camels were obtained from Tambool slaughter house and protoscoleces were separated aseptically. 36-weeks-old Swiss mice (25 - 30 gram body weight males and ...In the current study, hydatid cysts from livers and lungs of camels were obtained from Tambool slaughter house and protoscoleces were separated aseptically. 36-weeks-old Swiss mice (25 - 30 gram body weight males and females) were divided into two groups of 6 each: a prophylactic group dosed with 150 ml/kg of albendazole and mebendazole was given directly after injection with 2000 protoscoleces intraperitoneally for 10 consecutive days. The treated group was given a dose of 300 ml/kg of albendazole and mebendazole for 24 days with 4 days interval separated by 2 days and after 6 months of inoculation with protoscoleces, the two groups in addition to the control group were sacrificed and necropsied. The results revealed a significant difference in the development of hydatid cyst (p < 0.01). Inside the mice, small number of cysts was noticed in the group treated with albendazole and mebendazole compared to the control group, however, albendazole was highly efficacious than the mebendazole where the efficiency of albendazole reached 97% while the mebendazole efficiency rate was almost 50% which indicates that albendazole could be considered the drug of choice in the treatment of hydatid cyst.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
Structural information on the crystalline forms of mebendazole, an anti-parasitic drug, is limited, although three polymorphic forms of this drug have been reported. The present work investigates the structures and pr...Structural information on the crystalline forms of mebendazole, an anti-parasitic drug, is limited, although three polymorphic forms of this drug have been reported. The present work investigates the structures and properties of different crystalline forms of mebendazole with a series of n-alkyl carboxylic acids, including trifluroacetic acid （1）, formic acid （2）, acetic acid （3）, propanoic acid （4）, butanoic acid （5）, valeric acid （6） and hexanoic acid （7）. These compounds were characterized by thermogravimetric analysis, IR spectra, as well as powder and single-crystal X-ray diffraction analysis. The R22（8） structural motif was detected in all the seven products, which was formed by a pair of N--H…O/O--H…N hydrogen bonds between mebendazole and carboxylic acid. Forms 3--7 were found to be neutral solvate, while in forms 1 and 2, proton transfer was observed from carboxylic acid to mebendazole.展开更多
采用静水式急性毒性试验法研究了吡喹酮、甲苯咪唑和溴氰菊酯对花鳗鲡(Anguilla marmorata)(体重为0.87±0.19 g)的急性毒性。试验结果表明,在水温28±2℃时,吡喹酮对花鳗鲡的24 h LC50、48 h LC50、72 h LC50、96 h LC50分别为...采用静水式急性毒性试验法研究了吡喹酮、甲苯咪唑和溴氰菊酯对花鳗鲡(Anguilla marmorata)(体重为0.87±0.19 g)的急性毒性。试验结果表明,在水温28±2℃时,吡喹酮对花鳗鲡的24 h LC50、48 h LC50、72 h LC50、96 h LC50分别为73.85 mg/L、66.71 mg/L、56.57 mg/L、52.72 mg/L,安全浓度为16.34 mg/L;甲苯咪唑对花鳗鲡的24 h LC50、48 h LC50、72 h LC50、96 h LC50分别为142.81mg/L、13.80 mg/L、5.19mg/L、1.74mg/L,安全浓度为0.023 mg/L;溴氰菊酯对花鳗鲡的24 h LC50、48 h LC50、72 h LC50、96 h LC50分别为9.56μg/L、9.34μg/L、7.69μg/L、7.67μg/L,安全浓度为2.68μg/L。吡喹酮、甲苯咪唑、溴氰菊酯对花鳗鲡分别属于低毒、中毒、剧毒药物。甲苯咪唑对花鳗鲡的安全浓度0.023 mg/L远低于欧洲鳗鲡(Anguilla anguilla)的常用浓度1～2 mg/L,因此在花鳗鲡养殖中使用甲苯咪唑制剂需十分谨慎。展开更多
文摘Objective:To investigate the efficacy and effectiveness of albendazole and mebendazole in the treatment of Ascaris lumbricoides(A.lumbricoides) in the North-Western Indonesia.Methods: 229 primary school children who were positive for A.lumbricoides in their stool were recruited in the study.123 children received single-dose of 400 mg albendazole and 106 children received single-dose 500 mg of mebendazole.After 1 week,their stools were examined for the cure rate (CR) and egg reduction rate(ERR).Egg culture was also performed and observation was made on week-1,-3,-4.Results:have shown a non-significant difference in CR 96.7%vs.100%:and ERR of 99.3%vs.100.0%for albendazole and mebendazole groups respectively(P】0.05).In-vitro egg culture has shown trends of decrease in the percentage of the unfertilized eggs and in≥2 cell eggs in both treatment groups(P【0.05).The embryonated eggs from the albendazole groups has shown an increase from 7.3%on week-1 to 13.8%on week-4,whilst the mebendazole group has shown a constant increase during the whole 4 weeks of culture from 7.5%to 28.3%(P【0.01). Conclusions:No evidence of drug resistance is noted so far from the area of North-Western part of Indonesia.In addition,although both drugs showed incomplete ovicidal effects,single-dose albendazole is better than mebendazole in sterilizing A.lumbricoides eggs.
文摘Nanosizing by wet beads milling is a method to improve the solubility of poorly water soluble compounds[1,2].Mebendazole(MBZ)is a well-known anthelmintic drug in wide clinical use.There were some reports that MBZ had the anticancer effect in preclinical study.However,the bioavailability of MEB is low(<10%)due to the poor solubility in water(0.5μg/mL).The present study aimed to develop the nanocrystal formulations of MEB to improve dissolution behavior and enhance oral absorption.
文摘A total of 309 cases infected with ascariasis and trichuriasis were selected as subjects, of whom 177 cases received mebendazole tablet 500mg/d for the treatment of ascariasis and trichuriais,132 cases received mebendazole tablet 200mg/d for three days, Before and after the treatment, all the patients' feces were examined with Kato's technique, the results indicated that the cure rate of ascariasis was 71. 4% (70/98) in the experiment group and 78. 6% (66/84) in the control group respectively; There was no difference between the two groups (P > 0. 05 ). The cure rate of trichuriasis infection was 87. 5% (14/16 ) in the experimental group and 93. 3% (14/15 ) in the control group;There was also no difference between the two groups (P= 0. 401 ). But the cure rate of mixed infection of ascariasis and trichuriasis was 54. 0% (34/63) and 75. 8% (25/33) respectively; The cure rate of the experimental group was apparently lower than the that of the control group (P < 0. 05 ). The average reduced rate of egg count in per gram feces (E,P, G ) for ascariasis infection was 63. 6% (14/22) in the experimental group and 93. 8% (15/16) in the control group. In conclusion, to treat ascariasis and trichuriasis infection with mebendazole tablet should be used the three-day therapy with a total dose of 600mg or 1200mg.
文摘In the current study, hydatid cysts from livers and lungs of camels were obtained from Tambool slaughter house and protoscoleces were separated aseptically. 36-weeks-old Swiss mice (25 - 30 gram body weight males and females) were divided into two groups of 6 each: a prophylactic group dosed with 150 ml/kg of albendazole and mebendazole was given directly after injection with 2000 protoscoleces intraperitoneally for 10 consecutive days. The treated group was given a dose of 300 ml/kg of albendazole and mebendazole for 24 days with 4 days interval separated by 2 days and after 6 months of inoculation with protoscoleces, the two groups in addition to the control group were sacrificed and necropsied. The results revealed a significant difference in the development of hydatid cyst (p < 0.01). Inside the mice, small number of cysts was noticed in the group treated with albendazole and mebendazole compared to the control group, however, albendazole was highly efficacious than the mebendazole where the efficiency of albendazole reached 97% while the mebendazole efficiency rate was almost 50% which indicates that albendazole could be considered the drug of choice in the treatment of hydatid cyst.
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.
文摘Structural information on the crystalline forms of mebendazole, an anti-parasitic drug, is limited, although three polymorphic forms of this drug have been reported. The present work investigates the structures and properties of different crystalline forms of mebendazole with a series of n-alkyl carboxylic acids, including trifluroacetic acid （1）, formic acid （2）, acetic acid （3）, propanoic acid （4）, butanoic acid （5）, valeric acid （6） and hexanoic acid （7）. These compounds were characterized by thermogravimetric analysis, IR spectra, as well as powder and single-crystal X-ray diffraction analysis. The R22（8） structural motif was detected in all the seven products, which was formed by a pair of N--H…O/O--H…N hydrogen bonds between mebendazole and carboxylic acid. Forms 3--7 were found to be neutral solvate, while in forms 1 and 2, proton transfer was observed from carboxylic acid to mebendazole.
文摘采用静水式急性毒性试验法研究了吡喹酮、甲苯咪唑和溴氰菊酯对花鳗鲡(Anguilla marmorata)(体重为0.87±0.19 g)的急性毒性。试验结果表明,在水温28±2℃时,吡喹酮对花鳗鲡的24 h LC50、48 h LC50、72 h LC50、96 h LC50分别为73.85 mg/L、66.71 mg/L、56.57 mg/L、52.72 mg/L,安全浓度为16.34 mg/L;甲苯咪唑对花鳗鲡的24 h LC50、48 h LC50、72 h LC50、96 h LC50分别为142.81mg/L、13.80 mg/L、5.19mg/L、1.74mg/L,安全浓度为0.023 mg/L;溴氰菊酯对花鳗鲡的24 h LC50、48 h LC50、72 h LC50、96 h LC50分别为9.56μg/L、9.34μg/L、7.69μg/L、7.67μg/L,安全浓度为2.68μg/L。吡喹酮、甲苯咪唑、溴氰菊酯对花鳗鲡分别属于低毒、中毒、剧毒药物。甲苯咪唑对花鳗鲡的安全浓度0.023 mg/L远低于欧洲鳗鲡(Anguilla anguilla)的常用浓度1～2 mg/L,因此在花鳗鲡养殖中使用甲苯咪唑制剂需十分谨慎。
