Abstract
Purpose
The purpose of the present study was to investigate the effect of food viscosity on the dissolution rate of a drug. There are two types of viscosity, macroviscosity and microviscosity. Macroviscosity affects the diffusion layer thickness, whereas microviscosity affects the molecular diffusion coefficient. The mass transfer coefficient (kc) in the intrinsic dissolution rate (IDR) depends on the viscosity (η) as kc ∝ ηa (a is an exponent on η). In theory, for rotating flow over a disk, if a thickener increases only macroviscosity, a = -1/6, and if it increases both macroviscosity and microviscosity equally, a = -7/6.
Method
Benzocaine was used as a model drug. Hydroxypropyl cellulose (HPC) and methylcellulose (MC) were employed as control thickeners that increase only macroviscosity. Sucrose was employed as a control thickener for both macroviscosity and microviscosity. The FDA breakfast homogenate (BFH) was diluted with distilled water or 1 mM HCl with/without pepsin digestion. The IDR value was measured by the paddle-over-disk method.
Results
The η value of 30% BFH distilled water was 209 mPa∙s, about 300 times higher than distilled water. It was further increased by HCl (430 mPa∙s), and reduced by pepsin digestion (35 mPa∙s). The kc value was little affected by BFH (a = 0.00 to -0.09), slightly less than those in HPC (a = -0.19) and MC (a = -0.21). Sucrose decreased the kc value more significantly (a = -0.70).
Conclusion
The IDR and kc values of benzocaine were little affected by BFH, suggesting that BFH increased only macroviscosity.
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Data Availability
The data of this study are available on request from the corresponding author.
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Hirose, R., Sugano, K. Effect of Food Viscosity on Drug Dissolution. Pharm Res 41, 105–112 (2024). https://doi.org/10.1007/s11095-023-03620-y
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DOI: https://doi.org/10.1007/s11095-023-03620-y