Amorphous drug substances

Q11 Development and Manufacture of Drug Substances

Co-amorphous drug-amino acid formulations

Poorly water soluble drugs are considered a major challenge within development of drug formulations for oral delivery. Several formulations strategies exist to overcome this issue including salt formation and solid dispersions to name a few. Recently, a new formulation approach was introduced combining two drug molecules or a drug and an amino acid to form a so-called co-amorphous system. Sever...

Amorphous metal-organic frameworks for drug delivery.

We report the encapsulation of the hydrophilic model molecule calcein in the Zr-based MOF UiO-66, followed by amorphization of the framework by ball-milling. We show controlled release of calcein over more than 30 days, compared with the 2 day release period from crystalline UiO-66.

Environmental risk assessment of pharmaceutical drug substances--conceptual considerations.

Drugs, i.e. active ingredients of human medicinal products, may be introduced into the environment after use in patients by sewage effluent pathways and consequently are detected at low concentrations in sewage effluents and in surface waters. Legal requirements in a number of geographical regions (Europe, US, and intended in Canada) demand environmental risk assessments (ERA) for new drug subs...

Influence of dietary substances on intestinal drug metabolism and transport.

Successful delivery of promising new chemical entities via the oral route is rife with challenges, some of which cannot be explained or foreseen during drug development. Further complicating an already multifaceted problem is the obvious, yet often overlooked, effect of dietary substances on drug disposition and response. Some dietary substances, particularly fruit juices, have been shown to in...