Abstract
The oral solid dosage forms are extremely relevant to drug therapy and responsible for much of the pharmaceutical industry turnover worldwide. However, the development of medicines in solid form involves significant challenges, including obtaining formulations with appropriate bioavailability for low aqueous solubility drugs (classes II and IV of the Biopharmaceutics Classification System). One of the most effective strategies to overcome poor dissolution rate and low absorption of drugs is the solid dispersion technique, however, although it has been the focus of much research in recent decades, there are relatively few commercially available products based on such technology. This is mainly due to problems related to production scale-up and physicochemical instability and creates opportunities for new studies to explore the full potential of the technology. This review presents an overall approach to the factors affecting the dissolution rate and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology. Keywords: oral delivery, drug solubility, drug dissolution, solid dispersion.
Highlights
The oral route is the most commonly used for drug administration due to significant inherent advantages compared to other routes, such as safety, non-invasive nature, convenience and comfort to the patient, possibility of self-administration and systemic distribution of the drug
Recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling the rate and the extent of drug absorption grounded the proposition of the Biopharmaceutical Classification System (BCS) for correlating drug product in vitro dissolution and in vivo bioavailability, in which classes II and IV encompass drugs with low solubility [5, 6, 7]
This review presents an overall approach to the factors affecting the dissolution and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology
Summary
The oral route is the most commonly used for drug administration due to significant inherent advantages compared to other routes, such as safety, non-invasive nature, convenience and comfort to the patient, possibility of self-administration and systemic distribution of the drug. A major obstacle to the development and large-scale production of oral solid dosage forms is the low solubility of many drugs, given the negative effect that this property has on drug absorption and bioavailability. This review presents an overall approach to the factors affecting the dissolution and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology. Factors and characteristics related to the dosage form itself may interfere with drug release, for example, the manufacturing process, the nature of the excipients, the disintegration time and the drug release rate [20, 21, 22, 23]. Using water-soluble and swellable excipients favors the disintegration of the dosage form and drug release, and, on the contrary, the use of insoluble excipients may hinder the disintegration and dissolution steps [20, 21, 22, 23]
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