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Development of Itraconazole Tablets Containing Viscous KinetiSol Solid Dispersions: In Vitro and In Vivo Analysis in
Justin M Keen1,2, Justin S LaFountaine3, Justin R Hughey4
1Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, A1920, Austin, Texas, 78712, USA. justin.keen@dispersoltech.com.
AAPS Pharmscitech
|December 2, 2017
Summary
Developing amorphous solid dispersions for poorly soluble drugs requires understanding formulation factors. This study explored itraconazole amorphous solid dispersions in hydroxypropyl methylcellulose for immediate and controlled release tablets, showing potential for prolonged absorption.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Amorphous solid dispersions (ASDs) are crucial for enhancing the bioavailability of poorly soluble drugs.
- Current research often focuses on ASD particulates, necessitating further formulation into final dosage forms.
- Understanding formulation factors for ASDs in immediate and controlled-release tablets remains a challenge.
Purpose of the Study:
- To investigate formulation factors for developing immediate and controlled-release tablets using itraconazole amorphous solid dispersions.
- To evaluate the impact of formulation on the gelling tendency of hydroxypropyl methylcellulose (HPMC).
- To assess the in vivo performance of developed dosage forms.
Main Methods:
- Preparation of itraconazole amorphous solid dispersions using KinetiSol® Dispersing technology.
- Formulation of tablets for immediate and controlled drug release.
- Evaluation using non-sink dissolution methodologies.
- Pharmacokinetic assessment in beagle dogs.
Main Results:
- Successful development of immediate and controlled-release itraconazole tablets from amorphous solid dispersions.
- Identification of key formulation properties influencing HPMC gelling.
- Exploratory pharmacokinetic study indicated a prolonged absorption phase compared to a commercial control.
Conclusions:
- Amorphous solid dispersions offer a viable approach for formulating poorly soluble drugs like itraconazole into diverse release profiles.
- Formulation strategies can mitigate challenges associated with polymer gelling in ASDs.
- The developed dosage forms demonstrate potential for improved pharmacokinetic profiles.
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