Improvement of the Bioavailability and Anti-hepatic Alveolar Echinococcosis Effect of Albendazole-Isethionate/Hypromellose Acetate Succinate (HPMC-AS) Complex

Overview

Journal Antimicrob Agents Chemother

Publisher American Society for Microbiology

Specialty Pharmacology

Date 2021 Apr 20

PMID 33875425

Citations 4

Authors

Chunhui Hu

Fabin Zhang

Haining Fan

Affiliations

Soon will be listed here.

Abstract

Maximizing the pharmacodynamics of albendazole (ABZ), which is used to treat echinococcoses, is essential for the long-term treatment of echinococcosis patients. ABZ is a weak base whose solubility depends on the pH value of the solvent. After it has been orally administered, its solubility drops sharply from when it is in gastric juices (pH 1.4) to when it is in intestinal juices (pH 6.5) and is subsequently absorbed in the ileum and jejunum. This results in low solubility and poor bioavailability of the drug. In this study, we developed an orally administered albendazole-isethionate (ABZ-HES)/hypromellose acetate succinate (HPMC-AS) complex tablet (T) with improved solubility and bioavailability. Previous studies demonstrated that ABZ-HES has a higher intrinsic dissolution rate under pH 1.4 than the ABZ free base used in the commercial product Albenda and that HPMC-AS can effectively inhibit ABZ crystallization, which could be due to the hydrophobic interaction between ABZ and HPMC-AS in an aqueous environment. In this study, the dissolution behavior of T was studied by the two-step pH conversion method. Our results demonstrated that the oral bioavailability of T was approximately 2.6 times higher than that of ABZ. More importantly, in the rat model of secondary hepatic alveolar echinococcosis, the anti-hepatic alveolar echinococcosis effect of T was 3.4 times higher than that of a commercial product. The improved preparation with salt and polymer has proven to be a feasible method of improving the oral bioavailability and pharmacodynamics of ABZ.

Citing Articles

Combining solubilization and controlled release strategies to prepare pH-sensitive solid dispersion loaded with albendazole: and studies.

Su D, Bai M, Wei C, Long X, Liu X, Shen X Front Vet Sci. 2025; 11:1522856.

PMID: 39758610 PMC: 11695277. DOI: 10.3389/fvets.2024.1522856.

Current status of drug therapy for alveolar echinococcosis.

Jing Q, A J, Liu L, Fan H World J Hepatol. 2024; 16(11):1243-1254.

PMID: 39606163 PMC: 11586754. DOI: 10.4254/wjh.v16.i11.1243.

Ubenimex combined with Albendazole for the treatment of -induced alveolar echinococcosis in mice.

Zhou Z, Huayu M, Mu Y, Tang F, Ge R Front Vet Sci. 2024; 11:1320308.

PMID: 38585297 PMC: 10995866. DOI: 10.3389/fvets.2024.1320308.

Metabolic mechanism and pharmacological study of albendazole in secondary hepatic alveolar echinococcosis (HAE) model rats.

Li C, Zhang Y, Pang M, Zhang Y, Hu C, Fan H Antimicrob Agents Chemother. 2024; 68(5):e0144923.

PMID: 38501660 PMC: 11064478. DOI: 10.1128/aac.01449-23.

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