Biopharmaceutics Tools for Rational Formulation Design

Zarmpi, Panagiota; McAllister, Mark; Butler, James; Fotaki, Nikoletta

doi:10.1002/9781119678366.ch8

Cited by 1 publication

(1 citation statement)

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“…Another pKa is the pH at which the molecule is 50% protonated. This fact is important because most biologically active compounds are ionizable and also to raise their value of ionization, which can help to improve the bioavailability of medications [29] Owing to metabolism in the gut wall and following "first-pass" metabolism, oral statin medication bioavailability is quite poor. Additionally, drug permeability, inadequate water solubility, as well as drug proportionate partition all contribute to the oral bioavailability being constrained [30]…”

Section: Physicochemical Properties Of Statins Groupmentioning

confidence: 99%

Critical Appraisal of Physiochemical Characteristics of Statins and Drug Delivery Systems for Improving Their Bioavailability

Abdelghany

elbarbary²

2023

Journal of advanced Biomedical and Pharmaceutical Sciences

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Statins have cholesterol and non-cholesterol (pleiotropic) action. They play a crucial role in preventing cardiac disease brought on by elevated blood cholesterol levels and atherosclerotic plaques, which decrease cholesterol levels by restricting the enzyme HMG-CoA reductase. In recent decades, several kinds of research have been published to discuss several physicochemical properties of statins. They have low solubility and bioavailability for several of their members. They have a similar chemical structure and molecular weight. Meanwhile, lipid-soluble or lipophilic statins (atorvastatin, simvastatin, fluvastatin, lovastatin, cerivastatin) undergo hepatic and enteric metabolism via cytochrome P450. Nowadays Statins have a proven decrease in heart disease death rates and a very favorable safety record. Long-term statin therapy for at-risk individuals significantly reduces illness and death from cardiac disease. The neurological system, kidney, and liver have all been impacted negatively by statin use. Long-term use of statins causes rhabdomyolysis, which is among the most commonly reported side effects of it. Simvastatin is a weakly water-soluble medication (liquid solubility of 0.03 g/L) with a low half-life of around two hours plus a low bioavailability of 5%. Due to its sluggish dissolving rate in the digestive system and substantial first-pass impact. This review focused on different techniques used to improve the solubility and bioavailability of the statins group. Keywordsstatins, physicochemical properties, solid lipid nanoparticles, pleiotropic effect statins' elevations in elevated-density lipoprotein cholesterol percentage (HDL-C) and reduction in triglyceride percentage were seen on other lipid parameters [6, 7].

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Section: Physicochemical Properties Of Statins Groupmentioning

confidence: 99%