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Bioavailability Enhancement: Drug Permeability Enhancement

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 Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...

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Amorphous azithromycin with improved aqueous solubility and intestinal membrane permeability.

Marique Aucamp¹, Roelf Odendaal, Wilna Liebenberg

¹Center of Excellence for Pharmaceutical Sciences, North-West University , Potchefstroom , South Africa.

Drug Development and Industrial Pharmacy

|July 2, 2014

Summary

Amorphous azithromycin (AZM-A) significantly enhances solubility and membrane permeability compared to crystalline AZM-DH. This amorphous form improves oral bioavailability of the poorly soluble macrolide antibacterial agent.

Keywords:

Amorphous apparent permeability coefficient azithromycin dissolution solubility vapor sorption

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Area of Science:

Pharmaceutical Sciences
Drug Delivery
Materials Science

Background:

Azithromycin (AZM) is a macrolide antibacterial with poor water solubility, limiting its oral bioavailability.
Low solubility is a key challenge for effective oral drug delivery of Azithromycin.

Purpose of the Study:

To enhance Azithromycin's solubility and membrane permeability by preparing an amorphous form.
To investigate the impact of improved solubility on the permeability of Azithromycin.

Main Methods:

Preparation of amorphous azithromycin (AZM-A) via melt quench cooling.
Comparison of water solubility between AZM-A and crystalline azithromycin dihydrate (AZM-DH).
Assessment of apparent permeability coefficient (Papp) across excised intestinal tissue at physiological pH.

Main Results:

Amorphous azithromycin (AZM-A) demonstrated significantly increased water solubility versus crystalline AZM-DH.
AZM-A exhibited statistically significant higher Papp values (p < 0.05) than AZM-DH at pH 6.8 and 7.2.
Improved solubility of amorphous Azithromycin correlated with enhanced membrane permeability.

Conclusions:

Preparing amorphous azithromycin by melt quench cooling effectively improves its solubility.
The enhanced solubility of amorphous azithromycin leads to significantly improved membrane permeability at physiological pH.
Amorphous azithromycin holds potential for improving the oral bioavailability of this antibacterial agent.