Solid dispersions, Part I: recent evolutions and future opportunities in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs
- 11 August 2011
- journal article
- review article
- Published by Informa Healthcare in Expert Opinion on Drug Delivery
- Vol. 8 (11), 1501-1519
- https://doi.org/10.1517/17425247.2011.618181
Abstract
Introduction: In recent years, the number of active pharmaceutical ingredients with high therapeutic impact, but very low water solubility, has increased significantly. Thus, a great challenge for pharmaceutical technology is to create new formulations and efficient drug-delivery systems to overcome these dissolution problems. Areas covered: Drug formulation in solid dispersions (SDs) is one of the most commonly used techniques for the dissolution rate enhancement of poorly water-soluble drugs. Generally, SDs can be defined as a dispersion of active ingredients in molecular, amorphous and/or microcrystalline forms into an inert carrier. This review covers literature which states that the dissolution enhancement of SDs is based on the fact that drugs in the nanoscale range, or in amorphous phase, dissolve faster and to a greater extent than micronized drug particles. This is in accordance to the Noyes–Whitney equation, while the wetting properties of the used polymer may also play an important role. Expert opinion: The main factors why SD-based pharmaceutical products on the market are steadily increasing over the last few years are: the recent progress in various methods used for the preparation of SDs, the effect of evolved interactions in physical state of the drug and formulation stability during storage, the characterization of the physical state of the drug and the mechanism of dissolution rate enhancement.Keywords
This publication has 86 references indexed in Scilit:
- Enhanced dissolution of megestrol acetate microcrystals prepared by antisolvent precipitation process using hydrophilic additivesInternational Journal of Pharmaceutics, 2010
- Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugsDrug Discovery Today, 2007
- When poor solubility becomes an issue: From early stage to proof of conceptEuropean Journal of Pharmaceutical Sciences, 2007
- Nanosizing — Oral formulation development and biopharmaceutical evaluationAdvanced Drug Delivery Reviews, 2007
- Nanosizing: a formulation approach for poorly-water-soluble compoundsEuropean Journal of Pharmaceutical Sciences, 2003
- Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract1PII of original article: S0169-409X(96)00487-5. The article was originally published in Advanced Drug Delivery Reviews 25 (1997) 3–14.1Advanced Drug Delivery Reviews, 2001
- What is the True Solubility Advantage for Amorphous Pharmaceuticals?Pharmaceutical Research, 2000
- The effect of dry mixing on the apparent solubility of hydrophobic, sparingly soluble drugsEuropean Journal of Pharmaceutical Sciences, 1999
- A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo BioavailabilityPharmaceutical Research, 1995
- Pharmaceutical Applications of Solid Dispersion SystemsJournal of Pharmaceutical Sciences, 1971