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Related Concept Videos

Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems01:22

Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems

Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug absorption...
Preclinical Development: Overview01:28

Preclinical Development: Overview

Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...

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Related Experiment Video

Updated: May 27, 2026

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
05:08

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

Bridging solubility between drug discovery and development.

Li Di1, Paul V Fish, Takashi Mano

  • 1Pharmacokinetics Dynamics and Metabolism, Pfizer Inc., Eastern Point Road, Groton, CT 06340, USA. Li.Di@Pfizer.com

Drug Discovery Today
|December 6, 2011
PubMed
Summary
This summary is machine-generated.

Drug candidate solubility is critical for development success. Different screening methods address the distinct needs of drug discovery and drug development stages to overcome solubility challenges.

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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
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Last Updated: May 27, 2026

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
05:08

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
06:26

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

Area of Science:

  • Pharmacology and Pharmaceutical Sciences
  • Medicinal Chemistry

Background:

  • Drug solubility significantly impacts the success of pharmaceutical candidates.
  • Poor solubility presents challenges in both in vitro and in vivo studies, increasing drug development costs.
  • Specialized screening requirements exist for different phases of drug development.

Purpose of the Study:

  • To highlight the critical role of solubility in drug candidate progression.
  • To differentiate solubility screening needs between drug discovery and drug development.
  • To introduce the concept of tailored methodologies for solubility assessment.

Main Methods:

  • Review of existing literature on drug solubility screening.
  • Analysis of methodologies employed in early-stage drug discovery.
  • Examination of techniques used in later-stage drug development.

Main Results:

  • Solubility is a key determinant of drug efficacy and safety.
  • Early drug discovery requires rapid solubility assessments.
  • Drug development necessitates more rigorous and varied solubility testing protocols.

Conclusions:

  • Effective drug development hinges on addressing solubility early and consistently.
  • Tailored solubility screening approaches are essential for efficient progression from discovery to market.
  • Methodologies must be adapted to the specific requirements of each developmental stage to mitigate risks associated with poor solubility.