The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3(2) full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion). The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.
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http://dx.doi.org/10.4103/0250-474X.42974 | DOI Listing |
Mol Pharm
January 2025
Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, Georgia 30341, United States.
This investigation aimed to enhance transdermal methotrexate delivery through human skin by employing Dr. Pen microneedles and poly(d,l-lactide--glycolide) acid microparticles formulated from eight polymer grades (Expansorb DLG 95-4A, DLG 75-5A, DLG 50-2A, DLG 50-5A, DLG 50-8A, DLG 50-6P, DLG 50-7P, and DLL 10-15A). A comprehensive characterization of the microparticles was performed, encompassing various parameters such as size, charge, morphology, microencapsulation efficiency, yield, release kinetics, and chemical composition.
View Article and Find Full Text PDFSci Adv
January 2025
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China.
Acute alcohol intoxication could cause multiorgan damage, including nervous, digestive, and cardiovascular systems, and in particular, irreversible damage to the brain and liver. Emerging studies have revealed that the endogenous multienzymatic antioxidant defense system (MEAODS) plays a central role in preventing oxidative stress and other toxicological compounds produced by alcohol. However, few available drugs could quickly regulate MEAODS.
View Article and Find Full Text PDFJ Med Chem
January 2025
Department of Medicinal Chemistry, University of Minnesota, 308 Harvard Street SE, Minneapolis, Minnesota 55455, United States.
The antibacterial agent Bio-AMS is metabolized in vivo through hydrolysis of the central acyl-sulfamide linker leading to high clearance and release of a moderately cytotoxic metabolite . Herein, we disclose analogues designed to prevent the metabolism of the central acyl-sulfamide moiety through steric hindrance or attenuation of the acyl-sulfamide electrophilicity. was identified as a metabolically stable analogue with a single-digit nanomolar dissociation constant for biotin protein ligase (BPL) and minimum inhibitory concentrations (MICs) against and ranging from 0.
View Article and Find Full Text PDFAdv Healthc Mater
January 2025
School of Pharmacy, Queen's University Belfast, Lisburn Road 97, Belfast, BT9 7BL, UK.
Implantable drug delivery systems are crucial for achieving sustained delivery of active compounds to specific sites or systemic circulation. In this study, a novel reservoir-type implant combining a biodegradable rate-controlling membrane with a drug-containing core prepared using direct compression techniques is developed. The membrane is composed of poly(caprolactone) (PCL), and risperidone (RIS) served as the model drug.
View Article and Find Full Text PDFPeerJ
January 2025
Department of Entomology, The Pennsylvania State University, University Park, PA, United States of America.
Background: Preventative pesticide seed treatments (hereafter preventative pest management or PPM) are common corn and soybean treatments, and often include both fungicides and neonicotinoid insecticides. While PPM is intended to protect crops from soil-borne pathogens and early season insect pests, these seed treatments may have detrimental effects on biological control of weed seeds by insects.
Methods: Here, in two 3-year corn-soy rotations in Pennsylvania USA, we investigated a PPM approach to insect management compared to an integrated pest management approach (IPM) and a "no (insect) pest management" (NPM) control.
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