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Amorphous Solid Dispersions or Prodrugs: Complementary Strategies to Increase Drug Absorption
Alfred C F Rumondor1, Sundeep S Dhareshwar2, Filippos Kesisoglou3
1Formulation Sciences, Merck Research Laboratories, Merck & Co., Inc., Kenilworth, New Jersey 07033.
Amorphous solid dispersions (ASDs) and prodrugs enhance oral drug bioavailability. These complementary strategies address solubility and absorption challenges, improving drug delivery for pharmaceutical candidates.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Biopharmaceutics
Background:
- Maximizing oral bioavailability is a key challenge in drug development.
- Amorphous solid dispersions (ASDs) are increasingly used to improve drug solubility and dissolution rates.
- However, ASDs may not overcome solubility limitations at high doses, necessitating alternative strategies.
Purpose of the Study:
- To discuss amorphous solid dispersions (ASDs) and prodrugs as complementary approaches for enhancing oral bioavailability.
- To review the fundamental principles of drug absorption and bioavailability.
- To summarize the literature and successful applications of ASDs and prodrugs in drug development.
Main Methods:
- Review of scientific literature on amorphous solid dispersions and prodrugs.
- Discussion of biopharmaceutical evaluation aspects for these drug delivery strategies.
- Analysis of fundamental principles of drug absorption and bioavailability.
Main Results:
- ASDs improve drug solubility and dissolution, with many marketed formulations.
- Prodrugs can increase drug solubility beyond formulation approaches, complementing ASDs.
- Both ASDs and prodrugs are valuable tools for improving oral absorption.
Conclusions:
- ASDs and prodrugs represent complementary strategies to enhance oral bioavailability.
- Understanding biopharmaceutical principles is crucial for effective application of these approaches.
- Further research and application of ASDs and prodrugs can overcome drug delivery challenges.
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