Current status of the efficacy and effectiveness of albendazole and mebendazole for the treatment of Ascaris lumbricoides in North-Western Indonesia

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.

Development of nanocrystal formulation of mebendazole with improved dissolution and pharmacokinetic behaviors

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.

THE EVALUATION OF THE EFFECT OF MEBENDAZOLE ON TREATING ASCARIS LUMBRICOIDES AND TRICHURIS TRICHURA INFECTION WITH TWO KINDS OF THERAPY

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.

Effect of Albendazole and Mebendazole on Hydatid Cyst of Mice

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.

Physicochemical Characterization and Solubility Enhancement Studies of Mebendazole Solid Dispersions in Solvent Mixtures

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.

New Crystalline Forms of Mebendazole with n-Alkyl Carboxylic Acids Neutral and Ionic Status

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.

In vitro activities of acetonic extracts from leaves of three forage legumes(Calliandra calotyrsus,Gliricidia sepium and Leucaena diversifolia) on Haemonchus contortus

Objective:To assess ovicidal activity of three acetonic extracts from the leaves of three forage legume,Calliandra calotyrsus(C.calotyrsus),Gliricidia sepium(G.sepium) and Leucaena diversifolia(L.diversifolia) in vitro on Haemonchus contortus(H.contortus).Methods:Eggs were exposed for 24 hours to five different concentrations(0.075,0.15,0.3,0.6 and 1.25 mg/mL) of acetonic extracts at room temperature(24℃).Distilled water and 0.4%Tween were used in the bioassay as negative controls.Results:The later did not affect embryonation and egg hatching of H.contortus.Conversively,significant effects were obtained with the acetonic extracts of leaves of all three plants and the maximum activity was observed with the highest concentration (1.25 mg/mL).The acetonic extract of G.sepium was found to be more active(2.9%and 0.0% for embryonation and egg hatching,respectively) than the other substances 16.5%and 33.5%, respectively for C.calothyrsus,33.7%and 33.3%,respectively for L diversifolia.Conclusions: These results suggest that the three forage legumes do possess ovicidal properties and further studies on larvae should be carried out.

Disseminated toxocariasis in an immunocompetent host

Toxocariasis is a zoonotic infection caused by Toxocara canis,or less commonly,Toxocara cati,which is one of the most common zoonotic infections worldwide.It commonly affects the pediatric and immunocompromised population;however,it has rarely been reported in the immunocompetent adults.Two of the well-recognized syndromes in children are visceral larva migrans and ocular larva migrans.Infection in adults usually ranges from asymptomatic to nonspecific symptoms which makes the diagnosis challenging.A case of 36 year-old male was presented with disseminated toxocariasis with pulmonary and hepatic involvement and striking peripheral eosinophilia.

Effect of experimental single Ancylostoma caninum and mixed infections of Trypanosoma brucei and Trypanosoma congolense on the humoural immune response to anti-rabies vaccination in dogs

Objective:To determine the effect of Ancylostoma caninum(A.caninum)and trypanosome parasites on the immune response to vaccination in dogs in endemic environments.Methods:Sixteen dogs for the experiment were grouped into 4 of 4 members each.Group I was the uninfected control one,and GPII was infected with A.caninum;GPIII was infected with A.caninum/Trypanosoma congolense(T.congolense),and GPIV was infected with Trypanosoma brucei(T.brucei)/A.caninum.The dogs were first vaccinated with antirabies vaccine before infecting GPII,GPIII and GPIV with A.caninum which were done 4 weeks after vaccination.By 2-week post-vaccination,trypanosome parasites were superimposed on both GPIII and GPIV.A secondary vaccination was given to GPI,GPII,GPIII,and GPIV by Week 12 of the experiment(4 weeks post treatment).Results:The prepatent period was(3.00±1.40)days,in the conjunct infection of T.brucei/A.caninum.It was(9.00±1.10)days,in conjunct T.congolense/A.caninum.The prepatent period of A.caninum was(14.0±2.0)days in the single A.caninum group and(13.0±1.0)days in the conjunct trypanosome/A.caninum.At the 1st week after vaccination,the antibody titer in all the vaccinated groups(GPI,GPII,GPIII,and GPIV)significantly increased(P<0.05)and peaked at the 3rd week after vaccination.Following infections,there were marked significant decreases(P<0.05)in the antibody production against rabies in GPII,GPIII and GPIV.The significant decrease(P<0.05)in antibody titer was highest in the conjunct groups(GPIII and GPIV)compared to the single infection(GPII).Treatment with diminazene aceturate and mebendazole did not significantly improve antibody response in the dogs.A secondary vaccination administered at the 12th week after the primary vaccination significantly increased(P<0.05)the antibody titer with a peak at the 3rd week after the secondary vaccination.Conclusions:It was therefore concluded that A.caninum,T.brucei and T.congolense induced immunosuppression in antirabies vaccination in dogs.