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Book ChapterDOI

Selection of Excipients Based on the Biopharmaceutics Classification System of Drugs

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TLDR
This chapter focuses primarily on the factors determining and influencing bioavailability as well as the selection of excipients for formulating new dosage forms with enhanced therapeutic efficacy, based on the physicochemical properties of drugs.
Abstract
Active agents have been considered the main ingredients of any therapeutic product since the early ages of formulation technology. However, the importance of the inactive ingredients has been realized during the last three decades. With the development and manufacturing of more intelligent and multifunction excipients, new ways became available for formulation technologists to increase the beneficial effects of drugs on human body. Many modern active agents have internal characteristics that significantly decrease their potential and theoretical bioavailability; however, today we have the widest variety of inactive ingredients that we can utilize in order to change these properties. The careful and educated selection of excipients might significantly influence the effect of the drugs, including hastening or delaying their onset of action, increasing their bioavailability by changing their physicochemical characteristics, and increasing their stability. In this chapter, we focus primarily on the factors determining and influencing bioavailability as well as the selection of excipients for formulating new dosage forms with enhanced therapeutic efficacy, based on the physicochemical properties of drugs. We will provide some examples from the scientific literature to demonstrate the achievements in this multidisciplinary area.

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Citations
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Pharmaceutical nanococrystal synthesis: a novel grinding approach

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Pharmaceutical nanococrystal synthesis: a novel grinding approach

- 01 Jan 2022 - 
TL;DR: Nanococrystals as discussed by the authors are a green in situ surfactant-assisted mechanochemical synthesis, which can be used to synthesize new green fluorescent light-emitting diode (LED) sensors.
References
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Journal ArticleDOI

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

TL;DR: Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described in this article, where the rule of 5 is used to predict poor absorption or permeability when there are more than 5 H-bond donors, 10 Hbond acceptors, and the calculated Log P (CLogP) is greater than 5 (or MlogP > 415).
Journal ArticleDOI

A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability

TL;DR: A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption.
Journal ArticleDOI

Drug-like properties and the causes of poor solubility and poor permeability

TL;DR: There are currently about 10000 drug-like compounds, and true diversity does not exist in experimental combinatorial chemistry screening libraries because current ADME experimental screens are multi-mechanisms, and predictions get worse as more data accumulates.
Journal ArticleDOI

Improving drug solubility for oral delivery using solid dispersions.

TL;DR: The historical background and definitions of the various systems including eutectic mixtures, solid dispersions and solid solutions, as well as the production, the different carriers and the methods used for the characterization of solid dispersion are outlined.

Phase solubility techniques

T K Higuchi, +1 more
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