In this paper, we explore the strategy
increasingly used to improve
the bioavailability of poorly water-soluble crystalline drugs by formulating
their amorphous solid dispersions. We focus on the potential application
of a low molecular weight excipient octaacetyl-maltose (acMAL) to
prepare physically stable amorphous solid dispersions with ibuprofen
(IBU) aimed at enhancing water solubility of the drug compared to
that of its crystalline counterpart. We thoroughly investigate global
and local molecular dynamics, thermal properties, and physical stability
of the IBU+acMAL binary systems by using broadband dielectric spectroscopy
and differential scanning calorimetry as well as test their water
solubility and dissolution rate. The obtained results are extensively
discussed by analyzing several factors considered to affect the physical
stability of amorphous systems, including those related to the global
mobility, such as plasticization/antiplasticization effects, the activation
energy, fragility parameter, and the number of dynamically correlated
molecules as well as specific intermolecular interactions like hydrogen
bonds, supporting the latter by density functional theory calculations.
The observations made for the IBU+acMAL binary systems and drawn recommendations
give a better insight into our understanding of molecular mechanisms
governing the physical stability of amorphous solid dispersions.
The 2019 CPhI Annual Report describing rankings, innovations and key trends in pharma industry is summarized. Pharmaceutical markets were assessed based on the following indicators: growth potential, API manufacturing, innovation, competitiveness and finished product. The top three markets are USA, Germany and Japan, while China has made the largest overall improvement. Interestingly, UK demonstrated the largest growth decrease among all the markets reported. The fact is attributed to Brexit. The winner of CPhI Award was PolarDry® Electrostatic Spray Dryer. Thanks electrostatic induction applied in spraying nozzle, polar solvent is moved to the surface and non-polar ingredients into center of droplets. The most promising recent drug delivery devices were drug patches, smart dose injectors, multidose delivery injectable caps and smart dry powder inhalers. The most anticipated drug delivery devices are needle-free devices, wearable delivery devices, pre-filled syringes and dual chamber products as well as autoinjectors and pens. A few preselected articles were briefly summarized. Bikash Chatterjee from Pharmatech Associates described evolution of industry called Pharma 4.0. The key assumptions are gathering of data from across the global supply chain by smart sensors and devices referred to Internet of Things, the data evaluation by applying Artificial Intelligence tools and finally complete integration of databases. Mr. Girish Malhotra presented trends in global quality assurance. The following worth to be highlighted: necessity of technological improvements in manufacturing oriented on costs optimization and the highest possible drug products quality, standardization of requirements for drug products quality assessment. The regulatory agencies are oriented to enforce changes implementation by hesitant companies. D.M. Ecker and P.Seymur from BioProcess Technology Group presented "Mammalian Biomanufacutring Industry Overview". Vicky Qing Xia described rapidly growing biotechnological market of China. M.E.Ultee paid attention on developing gene therapies market in US.
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