Physiological Dynamics in the Upper Gastrointestinal Tract and the Development of Gastrointestinal Absorption Models for the Immediate-Release Oral Dosage Forms in Healthy Adult Human
AbstractThis review is a revisit of various oral drug absorption models developed in the past decades, focusing on how to incorporate the physiological dynamics in the upper gastrointestinal (GI) tract. For immediate-release oral drugs, GI absorption is a critical input of drug exposure and subsequent human body response, yet difficult to model largely due to the complex GI environment. One of the biggest hurdles lies at capturing the high within-subject variability (WSV) of bioavailability measures, which can be mechanistically explained by the GI physiological dynamics. A thorough summary of how GI dynamics is handled in...
Source: Pharmaceutical Research - October 3, 2023 Category: Drugs & Pharmacology Source Type: research
Development and Validation of Discriminatory In-vitro Release Method for Intramammary Drug Product
ConclusionThe developedin-vitro release methods can be used as a potential tool forin-vitro comparability evaluations for IMM formulations. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - October 3, 2023 Category: Drugs & Pharmacology Source Type: research
Physiological Dynamics in the Upper Gastrointestinal Tract and the Development of Gastrointestinal Absorption Models for the Immediate-Release Oral Dosage Forms in Healthy Adult Human
AbstractThis review is a revisit of various oral drug absorption models developed in the past decades, focusing on how to incorporate the physiological dynamics in the upper gastrointestinal (GI) tract. For immediate-release oral drugs, GI absorption is a critical input of drug exposure and subsequent human body response, yet difficult to model largely due to the complex GI environment. One of the biggest hurdles lies at capturing the high within-subject variability (WSV) of bioavailability measures, which can be mechanistically explained by the GI physiological dynamics. A thorough summary of how GI dynamics is handled in...
Source: Pharmaceutical Research - October 3, 2023 Category: Drugs & Pharmacology Source Type: research
Practical Advice on Scientific Design of Freeze-Drying Process: 2023 Update
ConclusionsThe authors revisited advice from a seminal paper by Tang and Pikal (Pharm Res. 21(2):191-200, 2004) on selecting freeze-drying process conditions and found that the majority of recommendations are still applicable today. There have been a number of advancements, including methods to promote ice nucleation and computer modeling for all steps of freeze-drying process. The authors created a database for primary drying and provided examples of complete freeze-drying cycles design. The paper may supplement the knowledge of scientists and formulators and serve as a user-friendly tool for quickly estimating the design...
Source: Pharmaceutical Research - October 2, 2023 Category: Drugs & Pharmacology Source Type: research
Modeling Gasotransmitter Availability to Brain Capillary Endothelial Cells with Ultrasound-sensitive Microbubbles
ConclusionsThis computational study demonstrates feasibility of the CO / MB strategy, and that controlled delivery is important for viability of this strategy. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - October 2, 2023 Category: Drugs & Pharmacology Source Type: research
In vivo Pharmacokinetic/Pharmacodynamic Analysis of the Efficacy of the Cefepime/Nacubactam Combination Against β-Lactamase-Producing Enterobacterales based on the Instantaneous MIC Concept
ConclusionsOur results indicate thatfT > MICi is a PK/PD parameter is suitable for monitoring the CFPM/NAC combination. The minimum target value for achieving a static effect against β-lactamase-producing Enterobacterales is 30%. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - October 2, 2023 Category: Drugs & Pharmacology Source Type: research
Practical Advice on Scientific Design of Freeze-Drying Process: 2023 Update
ConclusionsThe authors revisited advice from a seminal paper by Tang and Pikal (Pharm Res. 21(2):191-200, 2004) on selecting freeze-drying process conditions and found that the majority of recommendations are still applicable today. There have been a number of advancements, including methods to promote ice nucleation and computer modeling for all steps of freeze-drying process. The authors created a database for primary drying and provided examples of complete freeze-drying cycles design. The paper may supplement the knowledge of scientists and formulators and serve as a user-friendly tool for quickly estimating the design...
Source: Pharmaceutical Research - October 2, 2023 Category: Drugs & Pharmacology Source Type: research
Modeling Gasotransmitter Availability to Brain Capillary Endothelial Cells with Ultrasound-sensitive Microbubbles
ConclusionsThis computational study demonstrates feasibility of the CO / MB strategy, and that controlled delivery is important for viability of this strategy. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - October 2, 2023 Category: Drugs & Pharmacology Source Type: research
In vivo Pharmacokinetic/Pharmacodynamic Analysis of the Efficacy of the Cefepime/Nacubactam Combination Against β-Lactamase-Producing Enterobacterales based on the Instantaneous MIC Concept
ConclusionsOur results indicate thatfT > MICi is a PK/PD parameter is suitable for monitoring the CFPM/NAC combination. The minimum target value for achieving a static effect against β-lactamase-producing Enterobacterales is 30%. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - October 2, 2023 Category: Drugs & Pharmacology Source Type: research
Investigation of Dispersion Kinetics of Particulate Lubricants and their Effect on the Mechanical Strength of MCC Tablets
ConclusionsThe lubricant particle size controls the tensile strength reduction if short mixing times are applied. For extended mixing times, the investigated lubricants can be divided into two groups in terms of dispersion kinetics. Possible underlying reasons are discussed in detail in order to enhance the general understanding of lubricant dispersions in tablet formulations. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - September 26, 2023 Category: Drugs & Pharmacology Source Type: research
Investigating the Impact of Co-processed Excipients on the Formulation of Bromhexine Hydrochloride Orally Disintegrating Tablets (ODTs)
ConclusionsWe proved that the active ingredient cannot be absorbed in oral cavity and its dissolution profiles in media representing upper part of gastrointestinal tract are similar to marketed immediate release drug product. In our opinion, the developed formula is suitable for registration within the well-established use procedure without necessity of bioequivalence testing. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - September 19, 2023 Category: Drugs & Pharmacology Source Type: research
An Update on Potential Molecular Biomarkers of Dietary Phytochemicals Targeting Lung Cancer Interception and Prevention
AbstractSince ancient times, dietary phytochemicals are known for their medicinal properties. They are broadly classified into polyphenols, terpenoids, alkaloids, phytosterols, and organosulfur compounds. Currently, there is considerable interest in their potential health effects against various diseases, including lung cancer. Lung cancer is the leading cause of cancer deaths with an average of five-year survival rate of lung cancer patients limited to just 14%. Identifying potential early molecular biomarkers of pre-malignant lung cancer cells may provide a strong basis to develop early cancer detection and interception ...
Source: Pharmaceutical Research - September 19, 2023 Category: Drugs & Pharmacology Source Type: research
Population Pharmacokinetics and Pharmacogenetics Analyses of Dasatinib in Chinese Patients with Chronic Myeloid Leukemia
ConclusionsThis study ’s findings suggested that low-dose dasatinib would be better suited for Chinese patients, and the dosage can be appropriately reduced according to the increase of age, especially for the elderly. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - September 19, 2023 Category: Drugs & Pharmacology Source Type: research
Investigating the Impact of Co-processed Excipients on the Formulation of Bromhexine Hydrochloride Orally Disintegrating Tablets (ODTs)
ConclusionsWe proved that the active ingredient cannot be absorbed in oral cavity and its dissolution profiles in media representing upper part of gastrointestinal tract are similar to marketed immediate release drug product. In our opinion, the developed formula is suitable for registration within the well-established use procedure without necessity of bioequivalence testing. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - September 19, 2023 Category: Drugs & Pharmacology Source Type: research
