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BMC Pharmacology & Toxicology Apr 2019Parasitic diseases are the main challenge of livestock production in the world. They are mainly controlled by the use of anthelmintic drugs. To be effective, the drugs... (Comparative Study)
Comparative Study
BACKGROUND
Parasitic diseases are the main challenge of livestock production in the world. They are mainly controlled by the use of anthelmintic drugs. To be effective, the drugs should contain the appropriate amount of active pharmaceutical ingredient (API) and have the required physical characteristics. In this study, qualitative and quantitative assessments were performed to evaluate the quality of different brands of albendazole tablets legally circulating in pharmaceutical markets of Addis Ababa, Ethiopia.
METHODS
Ultraviolet-Visible Spectroscopy (UVS), Fourier Transform Infrared Spectroscopy (FTIR) and High-Performance Liquid Chromatography (HPLC) were used for identification. Quantitative analysis was performed by HPLC. United States Pharmacopeia standard was used as a control to evaluate the identity and content of the API in the samples. A total of 10 batches of albendazole tablets from six different brands were collected and evaluated.
RESULTS
All brands of albendazole tablets, except one, had acceptable physical characteristics. There was gross contamination in one batch, weight variation in 4 (40%) batches, and absence of package insert in 2 (20%) batches. All three methods of evaluation (UVS, FTIR and HPLC) confirmed that all batches passed the identity test. Quantitative analysis showed that no batch had API above the acceptable limit. However, 30% of batches from three different brands contained lower amount of API per tablet than the acceptable limit.
CONCLUSIONS
All batches of albendazole circulating in the market in Addis Ababa did not fulfil either physical or chemical quality standards. The most important finding of this research was the presence of drugs with lower level of API than the acceptable limit. This can lead to treatment failure and favour the emergence of parasites that are resistant to drugs. Therefore, there should be a thorough evaluation of drugs before approval. The study also revealed the importance of occasional assessment of drugs circulating even in the legal market.
Topics: Albendazole; Anthelmintics; Cities; Drug Labeling; Ethiopia; Quality Control; Tablets
PubMed: 31023365
DOI: 10.1186/s40360-019-0299-5 -
The Journal of the Association of... Feb 1994Based on clinical evaluation and computed tomography (CT) of the brain, 30 cases of neurocysticercosis were diagnosed. Diagnosis was supported by presence of... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
Based on clinical evaluation and computed tomography (CT) of the brain, 30 cases of neurocysticercosis were diagnosed. Diagnosis was supported by presence of histopathologically proven subcutaneous cysticerci in 12 cases. Three primary neurological syndromes were established i.e. epilepsy in 22 cases, increased intracranial tension in 6 cases and meningoencephalitis in 2 cases. Albendazole was administered orally in a dose of 15 mg/kg bodyweight/day for 30 days without prophylactic steroids. Follow up CT study at 3 months and 12 months revealed complete regression of all lesions in 2 cases, partial regressions in 14 cases and change in morphology in 4 cases. Transient appearence of fresh subcutaneous cysticerci as a side effect of therapy was noted in 4 cases. Albendazole, though acting slow, is considered a suitable alternative to praziquantel in medical management of parenchymal neurocysticercosis.
Topics: Adolescent; Adult; Albendazole; Brain Diseases; Child; Cysticercosis; Female; Follow-Up Studies; Humans; Male; Middle Aged; Tomography, X-Ray Computed
PubMed: 7860469
DOI: No ID Found -
European Journal of Clinical... 1990The pharmacokinetics of albendazole and its main metabolite, albendazole sulphoxide, have been examined after giving a single oral dose of 200 mg albendazole to 19...
The pharmacokinetics of albendazole and its main metabolite, albendazole sulphoxide, have been examined after giving a single oral dose of 200 mg albendazole to 19 patients with either Echinococcus multilocularis or E. granulosus, 5 of whom had significant extrahepatic obstruction due to the underlying disease. The AUC of albendazole sulphoxide was increased in the latter patients (mean 122 mumols.h.l-1 compared to 17 mumols.h.l-1 in the non-obstructed group). Obstructed patients had delayed absorption, ka averaging 0.39 compared to 1.41 h-1 in non-obstructed patients. The corresponding elimination rate constant, ke was also prolonged, averaging 0.041 and 0.13 h-1 in the two groups, respectively. Four patients were restudied after complete or partial resolution of the cholestasis. The pharmacokinetic parameters in them had returned towards values comparable to those in the non-obstructed patients.
Topics: Adult; Aged; Albendazole; Cholestasis; Echinococcosis; Female; Half-Life; Humans; Intestinal Absorption; Male; Middle Aged
PubMed: 2373135
DOI: 10.1007/BF00278590 -
Food Additives & Contaminants. Part A,... Jan 2018Few drugs are specifically regulated for aquaculture. Thus this study considered albendazole (ABZ) as a potential drug for use in fish, which, however, is not yet...
Few drugs are specifically regulated for aquaculture. Thus this study considered albendazole (ABZ) as a potential drug for use in fish, which, however, is not yet regulated for this application. ABZ is a broad-spectrum anthelmintic approved for farmed ruminants and recently considered for treatment of fish parasites. It is the subject of careful monitoring because of potential residues in animal products. This study evaluated the depletion of ABZ and its main known metabolites: albendazole sulfoxide - ABZSO, albendazole sulfone - ABZSO and albendazole amino sulfone - ABZ-2-NHSO, in the fillets of the Neotropical Characin pacu, Piaractus mesopotamicus, which were fed diets containing 10 mg ABZ kg body weight in a single dose. Fish were euthanised at 8, 12, 24, 48, 72, 96 and 120 hours after medication and the depletion profiles of ABZ, each metabolite and the sum of all marker residues were assessed and evaluated taking into account methodological variations regarding determination of the maximum residue limits adopted by different international regulating agencies for estimation of the withdrawal period (WP). The estimated WPs ranged from 2 to 7 days.
Topics: Albendazole; Animals; Anthelmintics; Characidae; Drug Residues; Molecular Structure; Time Factors
PubMed: 29095112
DOI: 10.1080/19440049.2017.1400186 -
Acta Dermato-venereologica Sep 1997
Topics: Albendazole; Anthelmintics; Humans; Male; Middle Aged; Stevens-Johnson Syndrome; Toxocariasis
PubMed: 9298150
DOI: 10.2340/0001555577411 -
Pharmaceutical Research Dec 1999We sought to determine whether disintegration and dissolution behavior differs among various albendazole generic formulations obtained from third world countries and to... (Comparative Study)
Comparative Study
PURPOSE
We sought to determine whether disintegration and dissolution behavior differs among various albendazole generic formulations obtained from third world countries and to compare them with the innovator's product.
METHODS
Dissolution behavior of various albendazole formulations was studied with USP Apparatus 2 in SGFsp and in a modified SGFsp which contained 0.1% of the nonionic surfactant Triton X 100. Disintegration was tested according to the European Pharmacopoeia.
RESULTS
Dissolution experiments in SGFsp showed a wide range in rate and extent of albendazole dissolution. The innovator product released 81 percent within two hours, a profile matched by only one other formulation. For other formulations 32 to 64% was released within two hours. Use of a modified SGFsp, containing 0.1% Triton X 100 to simulate the surface tension of gastric juice, resulted in less discrimination between products. The innovator product again showed the fastest and most complete dissolution, with ninety percent released within two hours. The generic formulations released between 67 and 82%, except for one formulation which achieved only 43% release. The results in SGFsp plus Triton X 100 may be more meaningful than in SGFsp since the surface tension of the medium is closer to the physiological value. All formulations passed the disintegration test according to the European Pharmacopoeia, with disintegration times ranging from 2.5 to 11 minutes.
CONCLUSIONS
Generic albendazole products vary widely in their dissolution behavior. Differences among products were greater in SGFsp than in SGFsp plus Triton X 100. These differences were not reflected in the disintegration behavior of the products.
Topics: Albendazole; Chromatography, High Pressure Liquid; Developing Countries; Octoxynol; Solubility; Solvents; Tablets; Therapeutic Equivalency
PubMed: 10644076
DOI: 10.1023/a:1018907527253 -
Journal of Chromatography. B,... Jun 2016A rapid, simple and sensitive method was developed and validated using liquid chromatography-tandem mass spectrometry (LC-MS/MS) for determination of albendazole...
A rapid, simple and sensitive method was developed and validated using liquid chromatography-tandem mass spectrometry (LC-MS/MS) for determination of albendazole sulfoxide (ABZOX) in human plasma. The plasma samples were extracted by protein precipitation using albendazole sulfoxide-d3 as internal standard (IS). The chromatographic separation was performed on Waters Xbridge C18Column (100×4.6mm, 3.5μm) with a mobile phase consisting of ammonia solution, water and methanol at a flow rate of 0.70mL/min. ABZOX was detected and identified by mass spectrometry with electrospray ionization (ESI) in positive ion and multiple-reaction monitoring (MRM) mode. The method was linear in the range of 3-1500ng/mL for ABZOX. This method was successfully applied to the bioequivalence study in human plasma samples.
Topics: Albendazole; Chromatography, Liquid; Humans; Linear Models; Reproducibility of Results; Sensitivity and Specificity; Tandem Mass Spectrometry
PubMed: 27060508
DOI: 10.1016/j.jchromb.2016.03.024 -
Experimental Parasitology Oct 2023Targeted delivery has not been achieved for anthelmintic treatment, resulting in the requirement of excess drug dose leading to side effects and therapeutic resistance....
Targeted delivery has not been achieved for anthelmintic treatment, resulting in the requirement of excess drug dose leading to side effects and therapeutic resistance. Gastrointestinal helminths take up lipid droplets from digestive fluid for energy production, egg development, and defense which inspired us to develop biocompatible and orally administrable albendazole-loaded solid lipid nanoparticles (SLN-A) that were derived from beeswax and showed drug loading efficiency of 83.3 ± 6.5 mg/g and sustained-release properties with 84.8 ± 2.5% of drug released at pH 6.4 within 24 h at 37 °C. Rhodamine B-loaded SLN showed time-dependent release and distribution of dye in-vitro in Haemonchus contortus. The sustained-release property was shown by the particles that caused enhancement of albendazole potency up to 50 folds. Therefore, this formulation has immense potential as an anthelminthic drug delivery vehicle that will be able to reduce the dose and drug-induced side effects by enhancing the bioavailability of the drug.
Topics: Animals; Haemonchus; Albendazole; Delayed-Action Preparations
PubMed: 37595879
DOI: 10.1016/j.exppara.2023.108593 -
Acta Tropica Jan 2020Neurocysticercosis is a neglected tropical disease that affects the central nervous system and is the most common cause of human epilepsy acquired in developing...
Neurocysticercosis is a neglected tropical disease that affects the central nervous system and is the most common cause of human epilepsy acquired in developing countries. Therapeutic failures attributed to medical management of neurocysticercosis with albendazole (ABZ) have been primarily linked to the poor drug absorption rate resulting in low drug level in plasma and brain tissue. The aim of the current work was to characterize and compare the brain pharmacokinetic behavior of ABZ formulated as a suspension or lipid nanocapsules (ABZ-LNCs) in healthy mice. The relative availability in brain tissue of the active metabolite ABZ sulphoxide increased 183% when ABZ was administered as LNCs, in relation to ABZ suspension. The parent drug was also detected for a short period of time. The bioavailability of ABZ in ABZ-LNCs treated mice increased more than 2 fold compared with ABZ suspension group. The enhanced drug brain exposure observed after administration of ABZ-LNCs to healthy mice has potential usefulness for the treatment of human neurocysticercosis.
Topics: Albendazole; Animals; Anthelmintics; Biological Availability; Brain; Disease Models, Animal; Humans; Lipids; Male; Mice; Nanocapsules; Neurocysticercosis
PubMed: 31600525
DOI: 10.1016/j.actatropica.2019.105215 -
Enfermedades Infecciosas Y... Apr 2019
Topics: Albendazole; Anthelmintics; Child, Preschool; Humans; Larva Migrans; Male; Ointments; Treatment Outcome
PubMed: 29907365
DOI: 10.1016/j.eimc.2018.05.001