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核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

Enabling a novel solvent method on Albendazole solid dispersion to improve the in vivo bioavailability.

作者信息

Han Ming-Jie, Zou Zhiyang Zack

机构信息

Department of DMPK, Global Health Drug Discovery Institute, Zhongguancun Dongsheng International Science Park, Beijing, PR China.

出版信息

Eur J Pharm Sci. 2024 May 1;196:106751. doi: 10.1016/j.ejps.2024.106751. Epub 2024 Mar 18.


DOI:10.1016/j.ejps.2024.106751
PMID:38508502
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11055451/
Abstract

Albendazole, a vital medication endorsed by the World Health Organization for combating parasitic infections, encounters a challenge stemming from its low solubility, significantly impeding absorption and bioavailability. Albendazole has near-insolubility in most organic solvents, so the solid dispersions of albendazole were predominantly using the fusion method. However, the solvent method could offer the advantage of achieving molecular-level mixing homogeneity. In this investigation, we incorporated the pH adjustment to prepare albendazole solid dispersion using a solvent method, which utilizes trace amounts of HCl in methanol, yielding notably enhanced albendazole solubility. Subsequently, carriers such as PEG6000/Poloxamer 188 (PEG: polyethylene glycol) and PVP K30/Poloxamer 188 (PVP: polyvinylpyrrolidone) were employed to create albendazole solid dispersions. Comprehensive characterization through dissolution rate analysis, PXRD (Powder X-ray diffraction), SEM (Scanning electron microscopy), DSC (differential scanning calorimetry), and pharmacokinetic (PK) studies in mice and rats was conducted. The findings indicate that the solid dispersion effectively transforms the crystalline state of albendazole into an amorphous state, resulting in significantly enhanced in vivo absorption and a 5.9-fold increase in exposure. Besides, the exposure increased 1.64 times of commercial albendazole tablets. Notably, PEG6000/Poloxamer 188 and PVP K30/Poloxamer 188 solid dispersions exhibited superior dissolution rates and pharmacokinetic profiles compared to commercially available albendazole tablets.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/840a297dfbef/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/da2e37413de4/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/327ca6d9ae7a/sc1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/8a469f923d3a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/fef6d722dd7a/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/503e925a41ae/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/34e0dda92ae8/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/f89636d94326/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/d819568e5631/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/840a297dfbef/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/da2e37413de4/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/327ca6d9ae7a/sc1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/8a469f923d3a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/fef6d722dd7a/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/503e925a41ae/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/34e0dda92ae8/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/f89636d94326/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/d819568e5631/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb39/11055451/840a297dfbef/gr7.jpg

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引用本文的文献

[1]
Combining High-Throughput Screening and Machine Learning to Predict the Formation of Both Binary and Ternary Amorphous Solid Dispersion Formulations for Early Drug Discovery and Development.

Pharm Res. 2025-4

[2]
Tea Saponins: a Novel Stabilizer for Enhancing the Oral Bioavailability of Albendazole Nanocrystals.

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[3]
Combining solubilization and controlled release strategies to prepare pH-sensitive solid dispersion loaded with albendazole: and studies.

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本文引用的文献

[1]
A Comparative Evaluation of Dissolution Rate of Three Different Posterior Restorative Materials used in Pediatric Dentistry: An Study.

Int J Clin Pediatr Dent. 2023-8

[2]
Effect of pH, Ionic Strength and Agitation Rate on Dissolution Behaviour of 3D-Printed Tablets, Tablets Prepared from Ground Hot-Melt Extruded Filaments and Physical Mixtures.

Biomedicines. 2023-1-27

[3]
Current Trends on Solid Dispersions: Past, Present, and Future.

Adv Pharmacol Pharm Sci. 2022-10-22

[4]
The key new techniques in the medicinal chemist's toolkit to prioritize solubility during drug design.

Future Med Chem. 2022-10

[5]
Dissolution/Permeation of Albendazole in the Presence of Cyclodextrin and Bile Salts: A Mechanistic In Vitro Study into Factors Governing Oral Bioavailability.

J Pharm Sci. 2022-6

[6]
Effect of pH Modifiers on the Solubility, Dissolution Rate, and Stability of Telmisartan Solid Dispersions Produced by Hot-melt Extrusion Technology.

J Drug Deliv Sci Technol. 2021-10

[7]
Using Microemulsions: Formulation Based on Knowledge of Their Mesostructure.

Chem Rev. 2021-5-26

[8]
Antiparasitic Drugs in the United States-Two Roads to High Prices.

Front Sociol. 2020-10-22

[9]
Relevance of Liquid-Liquid Phase Separation of Supersaturated Solution in Oral Absorption of Albendazole from Amorphous Solid Dispersions.

Pharmaceutics. 2021-2-5

[10]
Preparation and Characterization of Solid Dispersions Composed of Curcumin, Hydroxypropyl Cellulose and/or Sodium Dodecyl Sulfate by Grinding with Vibrational Ball Milling.

Pharmaceuticals (Basel). 2020-11-12

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