Paracetamol, a frequently used antipyretic and analgesic drug, has poor compression moldability owing to its low plasticity. In this study, new co-crystals of paracetamol (PCM) with caffeine (as a co-former) were prepared and delineated. Co-crystals exhibited improved compaction and mechanical behavior. A screening study was performed by utilizing a number of methods namely dry grinding, liquid assisted grinding (LAG), solvent evaporation (SE), and anti-solvent addition using various weight ratios of starting materials. LAG and SE were found successful in the screening study. Powders at 1:1 and 2:1 weight ratio of PCM/CAF by LAG and SE, respectively, resulted in the formation of co-crystals. Samples were characterized by PXRD, DSC, and ATR-FTIR techniques. Compressional properties of PCM and developed co-crystals were analyzed by in-die heckle model. Mean yield pressure (Py), an inverse measure of plasticity, obtained from the heckle plots decreased significantly (p < .05) for co-crystals than pure drug. Intrinsic dissolution profile of co-crystals showed up to 2.84-fold faster dissolution than PCM and physical mixtures in phosphate buffer pH 6.8 at 37 °C. In addition, co-crystals formulated into tablets by direct compression method showed better mechanical properties like hardness and tensile strength. In vitro dissolution studies on tablets also showed enhanced dissolution profiles (∼90-97%) in comparison to the tablets of PCM prepared by direct compression (∼55%) and wet granulation (∼85%) methods. In a single dose sheep model study, co-crystals showed up to twofold increase in AUC and C. A significant (p < .05) decrease in clearance as compared to pure drug was also recorded. In conclusion, new co-crystals of PCM were successfully prepared with improved tabletability in vitro and in vivo profile. Enhancement in AUC and C of PCM by co-crystallization might suggest the dose reduction and avoidance of side effects.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1080/03639045.2018.1435687 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Analysis of hollow visceral injuries admitted to a level one intensive care unit in South Africa.
S Afr J Surg
December 2024
Division of Surgery, Tygerberg Hospital, Stellenbosch University, South Africa.
Background: Bowel trauma, encompassing injuries to the small and large intestine, represents a significant medical challenge due to its potential for morbidity and mortality. Management of bowel injuries remains surgical, but multiple factors influence the outcome in these patients. This study provides an in-depth analysis of the high-risk features of hollow visceral trauma in the ICU setting and the corresponding mortality rates, shedding light on the critical factors that influence outcomes in these cases.
View Article and Find Full Text PDFEpidemiology and anatomic distribution of colorectal cancer in South Africa.
S Afr J Surg
December 2024
Centre for Global Surgery, Department of Global Health, Stellenbosch University, South Africa.
Background: Colorectal cancer (CRC) is the fifth most common cancer in sub-Saharan Africa (SSA) and the third most common in South Africa (SA). CRC characteristics in SSA are not well described. The aim is to describe patient characteristics and anatomic location of colorectal adenocarcinoma (CRC-AC) in SA.
View Article and Find Full Text PDFExperience of a tertiary/quaternary unit with surgery for endocrine hypertension.
S Afr J Surg
December 2024
Department of Surgery, School of Clinical Medicine, Chris Hani Baragwanath Academic Hospital, University of the Witwatersrand, South Africa.
Background: Endocrine hypertension is believed to be underestimated worldwide especially in the developing countries. There is a scarcity of publications on endocrine hypertension in sub-Saharan Africa. The aim of this study was to reflect the profile of patients with endocrine hypertension of adrenal/paraganglioma origin at Chris Hani Baragwanath Academic Hospital (CHBAH).
View Article and Find Full Text PDFIsolation, screening, and characterization of heavy metal-resistant bacteria from solid waste dumping sites in Central Gondar, Northwest, Ethiopia.
Sci Prog
January 2025
Department of Environmental and Industrial Biotechnology, Institute of Biotechnology, University of Gondar, Gondar, Ethiopia.
Objective: Heavy metal pollution is one of the more recent problems of environmental degradation caused by rapid industrialization and human activity. The objective of this study was to isolate, screen, and characterize heavy metal-resistant bacteria from solid waste disposal sites.
Methods: In this study, a total of 18 soil samples were randomly selected from mechanical sites, metal workshops, and agricultural land that received wastewater irrigation.
Au-In Alloy for Excellent Ohmic Contact in GeSe Devices with Enhanced Photodetector Properties.
ACS Appl Mater Interfaces
January 2025
Key Laboratory of MEMS of Ministry of Education, School of Integrated Circuits, Southeast University, Nanjing 210096, China.
Metal-semiconductor contact plays a significant role in devices such as transistors, photoemitters, and photodetectors. Here, the AuIn alloy contact gives a state-of-the-art low (contact resistance) in GeSe devices. The of GeSe-AuIn is measured to be 25 kΩ μm under channel carrier concentration around = 2.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!