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This paper aimed to investigate the effect of cholesterol on drug concentration and transportation from one region to another in the human body, especially to a targeted site. In this article, we performed a reformulation and incorporated constant cholesterol growth exponentially, as well as introduced the treatment in an attempt to understand the behavior of a drug administered in the human body over time. The modified models were solved using the Laplace method, where analytical results were obtained for the drug concentration in the bloodstream and that of the stomach, respectively. The Wolfram Mathematica software was used to simulate the analytical results where the entering parameters, such as the treatment parameter and the cholesterol parameter, were investigated by varying them, and the result revealed the following: (1). The cholesterol intake into the bloodstream inhibits drug diffusion from one region to another. (2). The drug concentration in the stomach steadily decreases from the initial injected concentration of 500 to 0.375998 units between 0 and 20 hours. (3). With the treatment as a control, the concentration delays attaining a peak of its activity before fading. (4). The drug concentration attains peaks in the same time frame of 0–4 hours with the rate of drug movement from the stomach to the bloodstream as 0.7448 and the rate of drug elimination from the body as 0.2213.

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