Re-visitation of Two Models for Predicting Mechanically-Induced Disordering after Cryogenic Impact Milling
ConclusionsPrediction accuracy of the ρcrit model decreased with dataset expansion, relative to previously published results. Overall, the ρcrit model was considerably less accurate relative to the bivariate empirical model, which retained very high prediction accuracy for the expanded dataset. Although the empirical model does not imply a mechanism, model robustness suggests the importance of glass transition temperature (Tg) and molar volume (Mv) on formation and persistence of amorphous materials following extensive cryomilling. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 31, 2023 Category: Drugs & Pharmacology Source Type: research
A Perspective on Model-Informed IVIVC for Development of Subcutaneous Injectables
AbstractSubcutaneously administered drugs are growing in popularity for both large and small molecule drugs. However, development of these systems – particularly generics – is slowed due to a lack of formal guidance regarding preclinical testing andin vitro–in vivo correlations (IVIVC). Many of these methods, while appropriate for oral drugs, may not be optimized for the complex injection site physiologies, and release rate and absorption mechanisms of subcutaneous drugs. Current limitations for formulation design and IVIVC can be supported by implementing mechanistic, computational methods. These methods can help to...
Source: Pharmaceutical Research - July 31, 2023 Category: Drugs & Pharmacology Source Type: research
Coformer-Dependent Physical Stability in a Series of Naringenin-Based Coamorphous Materials with Caffeine, Theophylline, and Theobromine
ConclusionFive naringenin-based multi-component solids were generated in this study: 3 new CAMs, 1 new cocrystal, and 1 previously reported cocrystal. Destabilization of CAMs was found to be exposure specific and coformer dependent. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 28, 2023 Category: Drugs & Pharmacology Source Type: research
Single-dose pharmacokinetics and lung function of nebulized niclosamide ethanolamine in sheep
ConclusionsSingle local pulmonary administration of niclosamide via nebulization was well tolerated in sheep and resulted in substantially higher peak ELF concentration compared to the human equivalent oral 2 g dose. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 27, 2023 Category: Drugs & Pharmacology Source Type: research
A Physiology-Based Mathematical Model to Understand Drug Delivery from Contact Lenses to the Back of the Eye
ConclusionsThe model constitutes a first step towards the possibility of predicting the ocular drug distribution and the treatment efficacy in the early stage of contact lens development, and it may help reduce both the need forin vivo tests (with ethical and economic advantages) and the gap between the lens design and clinical application. It also allows for an improved understanding of drug transport in the eye.Graphical abstract (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 27, 2023 Category: Drugs & Pharmacology Source Type: research
The Critical Role of Equilibrative Nucleoside Transporter-2 in Modulating Cerebral Damage and Vascular Dysfunction in Mice with Brain Ischemia-Reperfusion
ConclusionsEnt2 plays a critical role in modulating cerebral collateral circulation and ameliorating pathological events of brain ischemia and reperfusion injury. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 27, 2023 Category: Drugs & Pharmacology Source Type: research
Single-dose pharmacokinetics and lung function of nebulized niclosamide ethanolamine in sheep
ConclusionsSingle local pulmonary administration of niclosamide via nebulization was well tolerated in sheep and resulted in substantially higher peak ELF concentration compared to the human equivalent oral 2 g dose. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 27, 2023 Category: Drugs & Pharmacology Source Type: research
A Physiology-Based Mathematical Model to Understand Drug Delivery from Contact Lenses to the Back of the Eye
ConclusionsThe model constitutes a first step towards the possibility of predicting the ocular drug distribution and the treatment efficacy in the early stage of contact lens development, and it may help reduce both the need forin vivo tests (with ethical and economic advantages) and the gap between the lens design and clinical application. It also allows for an improved understanding of drug transport in the eye.Graphical abstract (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 27, 2023 Category: Drugs & Pharmacology Source Type: research
The Critical Role of Equilibrative Nucleoside Transporter-2 in Modulating Cerebral Damage and Vascular Dysfunction in Mice with Brain Ischemia-Reperfusion
ConclusionsEnt2 plays a critical role in modulating cerebral collateral circulation and ameliorating pathological events of brain ischemia and reperfusion injury. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 27, 2023 Category: Drugs & Pharmacology Source Type: research
Selection of Silica Type and Amount for Flowability Enhancements via Dry Coating: Contact Mechanics Based Predictive Approach
ConclusionSignificant flow enhancements were achieved at 50% SAC, validating previous models. Most uncoatedvery cohesive powders improved by two flow categories, attainingeasy flow. Flowability could not be predicted for both the uncoated and dry coated powders via particle size alone. Prediction was significantly better using Bond number computed via the mechanistic multi-asperity particle contact model accounting for the particle size, surface energy, roughness, and the amount and type of silica. The widely accepted 200 nm surface roughness was not valid for most pharmaceutical powders. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 20, 2023 Category: Drugs & Pharmacology Source Type: research
Using the LeiCNS-PK3.0 Physiologically-Based Pharmacokinetic Model to Predict Brain Extracellular Fluid Pharmacokinetics in Mice
ConclusionThe current version of the mouse LeiCNS-PK3.0 model seems to reasonably predict available information on brainECF from healthy mice for most drugs. This brings the translation between mouse and human brain PK one step further. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 13, 2023 Category: Drugs & Pharmacology Source Type: research
Impact of Primary Container Closure System on PS80 Oxidation and the Mechanistic Understanding
ConclusionsPrimary containers of drug products play a significant role in the rate of PS80 oxidation. This study revealed a new major contributor to PS80 oxidation and potential mitigation strategy for biological drug products. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 11, 2023 Category: Drugs & Pharmacology Source Type: research
