Article
Pharmacology & Pharmacy
Bai Lv, Guobao Yang, Yejuan Wei, Yaran Lei, Yaning Ding, Wei Gong, Yuli Wang, Chunsheng Gao, Cuiyan Han
Summary: This study developed colchicine sustained-release pellets using fluidized-bed technology to prevent acute gout attacks. The pellets showed a smooth surface and spherical shape, and the release of colchicine from the pellets was similar under different pH conditions. Pharmacokinetic and pharmacodynamic studies demonstrated that the sustained-release pellets had a longer mean residence time, higher tmax, and exhibited a more optimal preventive potential against acute gout attack compared to commercial colchicine tablets. The study suggests that these sustained-release pellets provide a powerful alternative to commercial tablets.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Pharmacology & Pharmacy
Daniel J. Blackwell, Abigail N. Smith, Tri Do, Aaron Gochman, Jeffrey Schmeckpeper, Corey R. Hopkins, Wendell S. Akers, Jeffrey N. Johnston, Bjorn C. Knollmann
Summary: This study developed a bioassay to measure the concentrations of nat-verticilide and ent-verticilide in murine plasma and correlated plasma concentrations with antiarrhythmic efficacy. The results showed that ent-verticilide has favorable pharmacokinetic properties and reduces ventricular arrhythmias in the nanomolar range, warranting further drug development.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2023)
Article
Veterinary Sciences
Jeff D. Olivarez, Pierre-Yves Mulon, Lisa S. Ebner, Haley Cremerius, Channing Cantrell, Rebecca Rahn, Windy Soto-Gonzalez, Joan Bergman, Sherry Cox, Jonathan P. Mochel, Amanda J. Kreuder, Joe S. Smith
Summary: The objective of this study was to estimate the pharmacokinetic parameters of pantoprazole in neonatal calves and investigate its effect on abomasal pH. The results showed that the pharmacokinetic parameters of pantoprazole in neonatal calves were similar to previous reports. Additionally, pantoprazole significantly increased abomasal pH. These findings suggest that pantoprazole may be a potential treatment/preventative for abomasal ulcers.
FRONTIERS IN VETERINARY SCIENCE
(2023)
Article
Chemistry, Applied
Heejun Park, Eun-Sol Ha, Min-Soo Kim
Summary: This study evaluated the effects of various cyclodextrins on stabilizing exenatide and on the pharmaceutical properties of PLGA microsphere. The results showed that 8-CyD had the best stabilizing effect on exenatide and improved the drug properties of the microspheres.
CARBOHYDRATE POLYMERS
(2021)
Article
Pharmacology & Pharmacy
Han Liu, Suohui Zhang, Zequan Zhou, Mengzhen Xing, Yunhua Gao
Summary: In this study, two-layer sustained-release microneedles (TS-MNs) were successfully fabricated for the sustained delivery of exenatide (EXT). The TS-MNs showed good mechanical strength and could penetrate the skin for drug release. Moreover, the TS-MNs retained high drug activity during storage and had high relative bioavailability.
Article
Pharmacology & Pharmacy
D. N. Venkatesh, S. N. Meyyanathan, R. Shanmugam, S. S. Kamatham, J. R. Campos, J. Dias-Ferreira, E. Sanchez-Lopez, J. C. Cardoso, P. Severino, E. B. Souto
Summary: Isradipine sustained release tablets composed of hydroxypropylmethyl cellulose showed a 24-hour controlled release profile and higher absorption in vivo compared to immediate release tablets. The findings suggest that the sustained release tablets provide an efficient solid dosage form to overcome the limitations of conventional immediate release tablets.
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
(2021)
Review
Infectious Diseases
Gauri G. Rao, Cornelia B. Landersdorfer
Summary: The use of pharmacokinetic/pharmacodynamic approaches is crucial in optimizing dosage regimens of anti-infectives to maximize efficacy, minimize toxicity and resistance, and ensure a high likelihood of therapeutic success. This involves well-designed preclinical studies, mathematical-model-based analysis, in-silico simulations, and the integration with population pharmacokinetic modelling to consider interindividual variability and predict treatment outcomes in patients. The importance of this approach is highlighted through the example of Polymyxin B, showcasing the necessity of pharmacokinetic/pharmacodynamic modelling in conjunction with experimentation for successful translation to clinical practice.
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
(2021)
Review
Veterinary Sciences
Longfei Zhang, Hongbing Xie, Yongqiang Wang, Hongjuan Wang, Jianhe Hu, Gaiping Zhang
Summary: Pharmacokinetic/pharmacodynamic (PK/PD) integration models are used to investigate the antimicrobial activity characteristics of drugs targeting pathogenic bacteria through comprehensive analysis of the interactions between PK and PD parameters. PK/PD models have been widely applied in the development of new drugs, optimization of the dosage regimen, and prevention and treatment of drug-resistant bacteria.
FRONTIERS IN VETERINARY SCIENCE
(2022)
Article
Medicine, Research & Experimental
Haofan Liu, Bingwen Zhang, Yanna Chen, Zhe Cui, Liandong Hu
Summary: The objective of this study was to explore an innovative sustained release technology and design a new microporous resin-based polymer device (RPD) for controlled release of glipizide (GZ). The results showed that the resin layer prepared by photocurable resin can effectively control the release of GZ and exhibit excellent in vitro release and in vivo pharmacokinetic properties.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Chemistry, Medicinal
Duanduan Cong, Wenyuan Qi, Xiaohui Liu, Xiaoyu Xu, Lingyun Dong, Wei Xue, Kexin Li
Summary: This study aimed to compare the pharmacokinetic characteristics of enteric-coated sustained-release (EcSr) aspirin tablets with enteric-coated (Ec) aspirin tablets in healthy Chinese participants. The results showed that EcSr aspirin tablets had less inter-individual variation in release and absorption, and meals had no significant effect on their pharmacokinetics.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2023)
Review
Biochemistry & Molecular Biology
Giuseppina Ioele, Martina Chieffallo, Maria Antonietta Occhiuzzi, Michele De Luca, Antonio Garofalo, Gaetano Ragno, Fedora Grande
Summary: Despite the remarkable progress in anticancer research, there are still challenges in terms of high toxicity and stability of the approved drugs. Therefore, developing tissue-specific targeted drug formulations and improving stability are crucial. Prodrug development and the use of nanocarriers have shown promise in enhancing solubility, pharmacokinetics, cellular absorption, and stability of anticancer drugs.
Review
Pharmacology & Pharmacy
Karine Rodriguez-Fernandez, Victor Mangas-Sanjuan, Matilde Merino-Sanjuan, Antonio Martorell-Calatayud, Almudena Mateu-Puchades, Monica Climente-Marti, Elena Gras-Colomer
Summary: The emergence of biological therapies has revolutionized the treatment of psoriasis. However, the complex pharmacokinetic properties of monoclonal antibodies (mAb) have posed challenges for dosage determination. This study reviewed population pharmacokinetic/pharmacodynamic (PK/PD) models of different types of mAb used in psoriasis treatment. The results showed that body weight and immunogenicity significantly influenced drug clearance. The lack of consensus on PK/PD relationships emphasizes the importance of therapeutic drug monitoring (TDM) in psoriasis treatment.
Review
Biochemistry & Molecular Biology
Romain Pelletier, Brendan Le Dare, Diane Le Bouedec, Angeline Kernalleguen, Pierre-Jean Ferron, Isabelle Morel, Thomas Gicquel
Summary: Since the 2000s, there has been an increase in the availability of new psychoactive substances (NPS) on the drug market. Arylcyclohexylamine (ACH) compounds, such as ketamine and its derivatives, have raised concerns due to their growing use and lack of detailed toxicity information. Initially used for anesthesia, these compounds are now increasingly used recreationally. ACH derivatives exhibit antagonistic activity against the N-methyl-D-aspartate receptor, resulting in dissociative effects. Synthetic ketamine derivatives from Asia are making their way to Europe, where they are often not classified as narcotics and therefore legal. This article discusses the pharmacology, epidemiology, chemistry, metabolism, and case reports of intoxication related to ACH derivatives.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Carmen Flores-Perez, Luis Alfonso Moreno-Rocha, Juan Luis Chavez-Pacheco, Norma Angelica Noguez-Mendez, Janett Flores-Perez, Delfina Ortiz-Marmolejo, Lina Andrea Sarmiento-Arguello
Summary: This study proposes a pharmacokinetic-pharmacodynamic (PK-PD) population model for the use of midazolam in pediatric patients undergoing minor surgery. The results demonstrate that adequate sedation without adverse effects can be achieved at half the usual dose. Further research is needed to optimize dosing schedules and prevent potential adverse effects.
Article
Chemistry, Multidisciplinary
Lieby Zborovsky, Leonardo Kleebauer, Maria Seidel, Arseni Kostenko, Leonard von Eckardstein, Frank Otto Gombert, John Weston, Roderich D. Suessmuth
Summary: The study reported the design and synthesis of new albicidins with N-atoms, showing enhanced antibacterial activity and spectrum, particularly against Gram-positive bacteria. Density functional theory calculations were used to find the most stable conformation of each derivative. In vivo experiments with an albicidin analogue demonstrated promising pharmacokinetics, lack of toxicity, and efficacy in reducing bacterial titers in an E. coli infection model with fluoroquinolone-resistant strains, highlighting the potential of albicidins as active antibacterial agents.