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Natural deep eutectic solvents (NADES) are pharmaceutically accepted systems not only because they typically offer a serious enhancement of active pharmaceutical ingredient (API) solubility, but also due to their non-toxicity. This fortunate conjuncture allows for designing new media for escalation and controlled release of APIs. For example, composition optimisation of a series of NADES comprising choline chloride with multi-hydroxyl compounds was successfully performed for a set of sulphonamide-based drugs. These results confirmed that NADES in general, and the ones based on choline chloride and glycerol particularly, are an attractive alternative to traditional solvents for sulphonamide dissolution. Experiments augmented with in silico modelling can offer deeper insights into the thermodynamic characteristics of these systems and an explanation for the origin of the observed solubility enhancement. Research of this type offers universal resolutions to the problem of low solubility issues for many types of drugs. Of particular interest is that such screening is not restricted to artificial in vitro environments but can be also easily adopted for the study of modelled in vivo situations. One of very important and interesting examples is a new curcumin–NADES formulation preserving its beneficial properties even after dilution with FaSSIF solution, which mimicks intestinal absorption.

Research & information: general --- deep eutectic solvents --- molecularly imprinted polymers --- extraction --- phenolic compounds --- antioxidant activity --- spruce bark --- phytomass --- valorization --- deep eutectic solvent --- composite resins --- hydrogen bond --- eutectic solvents --- natural deep eutectic solvents --- nanostructured ionic solvents --- neoteric solvents --- ionic liquids --- ionic liquid --- hybrid solvent --- CO2 solubility --- Henry’s constant --- viscosity

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The development of paediatric medicines can be challenging since this is a different patient population with specific needs. A medicine designed for use in paediatric patients must consider the following aspects: patient population variability; the need for dose flexibility; route of administration; patient compliance; excipient tolerability. For example, the toxicity of excipients may differ in children compared to adults and children have different taste preferences. Globally, about 75% of drugs do not carry regulatory approval for use in children; worldwide, many medications prescribed for the treatment of paediatric diseases are used off-label, and less than 20% of package inserts have sufficient information for treating children. This book provides an update on both state-of-the-art methodology and operational challenges in paediatric formulation design and development. It aims at re-evaluating what is needed for more progress in the design and development of age-appropriate treatments for paediatric diseases, focusing on: formulation development; drug delivery design; efficacy, safety, and tolerability of drugs and excipients.

Medicine --- dasatinib --- Duchenne muscular dystrophy --- cyclodextrin inclusion complex --- phase solubility studies --- paediatric age --- liquid formulation --- tumorspheres --- retinoblastoma --- topotecan --- penetration --- confocal microscopy --- poorly water soluble drug --- solubility enhancement --- grinding --- spray congealing --- neglected tropical diseases --- polymorph --- Norvir® --- ritonavir --- poorly soluble compound --- pediatric --- palatability assessment --- bioavailability --- flavor profile --- Interleukin-1 --- anakinra --- canakinumab --- innovative biotechnologies --- autoinflammatory disease --- Kawasaki disease --- systemic juvenile idiopathic arthritis --- personalized medicine --- child --- pediatrics --- neonates --- formulation --- product development --- formulation development --- oral --- parenteral --- topical --- inhaled --- intra nasal --- biopharmaceutics --- administration --- excipient --- NICU --- device --- medication error --- dosage form --- modified release --- drug delivery --- paediatric formulation development --- paediatric dosage forms --- chronic myeloid leukemia --- tyrosine kinase inhibitors --- pediatric age --- imatinib --- nilotinb --- ponatinib --- Orodispersible formulation --- pyrazinamide --- pediatric drug delivery --- tuberculosis --- design of experiments --- children --- edible films --- development --- design --- paediatric --- age-related --- palatable --- taste-masking --- acceptable --- dasatinib --- Duchenne muscular dystrophy --- cyclodextrin inclusion complex --- phase solubility studies --- paediatric age --- liquid formulation --- tumorspheres --- retinoblastoma --- topotecan --- penetration --- confocal microscopy --- poorly water soluble drug --- solubility enhancement --- grinding --- spray congealing --- neglected tropical diseases --- polymorph --- Norvir® --- ritonavir --- poorly soluble compound --- pediatric --- palatability assessment --- bioavailability --- flavor profile --- Interleukin-1 --- anakinra --- canakinumab --- innovative biotechnologies --- autoinflammatory disease --- Kawasaki disease --- systemic juvenile idiopathic arthritis --- personalized medicine --- child --- pediatrics --- neonates --- formulation --- product development --- formulation development --- oral --- parenteral --- topical --- inhaled --- intra nasal --- biopharmaceutics --- administration --- excipient --- NICU --- device --- medication error --- dosage form --- modified release --- drug delivery --- paediatric formulation development --- paediatric dosage forms --- chronic myeloid leukemia --- tyrosine kinase inhibitors --- pediatric age --- imatinib --- nilotinb --- ponatinib --- Orodispersible formulation --- pyrazinamide --- pediatric drug delivery --- tuberculosis --- design of experiments --- children --- edible films --- development --- design --- paediatric --- age-related --- palatable --- taste-masking --- acceptable

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This Book serves to highlight the mechanisms related to the low intestinal drug absorption, the strategies to overcome the obstacles or intestinal drug absorption, and in situ, in vitro, and in silico methodologies to predict to intestinal drug absorption. This Book presents a series of drug absorption studies and related technologies that predict intestinal permeation of drugs that govern the pharmacokinetic features of therapeutic drugs. It also contains the mechanistic understanding regarding the first-pass metabolism and intestinal efflux that modulate the pharmacokinetics of drug and suggest the formulation strategies to enhance the bioavailability of investigated drugs.

rebamipide --- nanocrystals --- oral mucositis --- hydrogel --- endocytosis --- enoxaparin --- lipid–polymer hybrid nanoparticles --- oral --- intestinal absorption --- naftidrofuryl oxalate --- solubility --- permeability --- dissolution profiles --- pharmaceutical availability --- BCS drug classification --- non-sink condition --- solubility–permeability interplay --- unstirred water layer --- poorly soluble drugs --- solubilizer additive --- phenylketonuria --- l-phenylalanine ammonia-lyase --- enzyme --- kinetics --- catabolism disorder --- biomedical drug --- P-glycoprotein --- breast cancer resistance protein --- LY335979 --- WK-X-34 --- in vivo–in vitro correlation --- lipolysis-permeation --- lipid-based drug delivery system --- PermeaPad --- cinnarizine --- lipolysis --- amorphous solid dispersion --- candesartan Cilexetil --- PVPK30 --- pH-modulation --- spray drying --- bioavailability --- nasal administration --- spray-drying --- chitosan --- microsphere --- meloxicam --- silymarin --- D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) --- liver distribution --- acetaminophen-induced hepatotoxicity --- extra virgin olive oil --- secoiridoids --- metabolism --- phenolic compounds --- intestinal permeability --- drug-phytochemical interaction --- hepatic metabolism --- mixed inhibition --- quercetin --- repaglinide

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In 2015, the first pharmaceutical cocrystal was approved by the FDA. Since then, the number of cocrystals on the market and in the development pipeline has been slowly but steadily growing. It is now well established that cocrystals are a versatile new approach to oral drug formulation. This Reprint Book is a collection of articles that show the utility of pharmaceutical cocrystals and various aspects of cocrystal research: • Cocrystals as a strategy to modify the physicochemical properties of a drug such as dissolution behaviour, tabletability, and melting point; • Development of new coformers; • Screening studies for multiple cocrystal forms; • Cocrystals in nano-sized drug delivery.

Research & information: general --- nitazoxanide --- cocrystals --- multicomponent crystals --- dissolution behavior --- supersaturated formulations --- crystallization inhibitors --- drug-polymer interactions --- nano co-crystals --- crystal engineering --- polydispersity index --- zeta potential --- particle size --- zidovudine --- lamivudine --- HIV/AIDS --- sonochemistry --- imidazole N-oxides --- barbituric acid --- thiobarbituric acid --- pharmaceutical cocrystals --- mechanochemistry --- solid state NMR --- X-ray Diffraction --- design of experiments --- Quality by Design --- cocrystal --- compaction --- nanoindentation --- slip plane --- tabletability --- surface topology --- interparticulate bonding area --- interparticulate bonding strength --- nefiracetam --- solid state --- solubility --- dissolution rate --- stability --- formulation --- diclofenac sodium --- L-proline --- salt cocrystal --- multicomponent crystal --- monohydrate --- tetrahydrate --- dissolution --- itraconazole --- terephthalic acid --- crystal structure --- solid-state --- thermal analysis --- wettability --- n/a

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In 2015, the first pharmaceutical cocrystal was approved by the FDA. Since then, the number of cocrystals on the market and in the development pipeline has been slowly but steadily growing. It is now well established that cocrystals are a versatile new approach to oral drug formulation. This Reprint Book is a collection of articles that show the utility of pharmaceutical cocrystals and various aspects of cocrystal research: • Cocrystals as a strategy to modify the physicochemical properties of a drug such as dissolution behaviour, tabletability, and melting point; • Development of new coformers; • Screening studies for multiple cocrystal forms; • Cocrystals in nano-sized drug delivery.

nitazoxanide --- cocrystals --- multicomponent crystals --- dissolution behavior --- supersaturated formulations --- crystallization inhibitors --- drug-polymer interactions --- nano co-crystals --- crystal engineering --- polydispersity index --- zeta potential --- particle size --- zidovudine --- lamivudine --- HIV/AIDS --- sonochemistry --- imidazole N-oxides --- barbituric acid --- thiobarbituric acid --- pharmaceutical cocrystals --- mechanochemistry --- solid state NMR --- X-ray Diffraction --- design of experiments --- Quality by Design --- cocrystal --- compaction --- nanoindentation --- slip plane --- tabletability --- surface topology --- interparticulate bonding area --- interparticulate bonding strength --- nefiracetam --- solid state --- solubility --- dissolution rate --- stability --- formulation --- diclofenac sodium --- L-proline --- salt cocrystal --- multicomponent crystal --- monohydrate --- tetrahydrate --- dissolution --- itraconazole --- terephthalic acid --- crystal structure --- solid-state --- thermal analysis --- wettability --- n/a