Journal of Pharmaceutical Sciences and Research

Abstract

The limited bioavailability observed in many contemporary pharmaceuticals can often be attributed to their poor oral solubility. A significant proportion of new chemical entities (NCEs) and recently approved active pharmaceutical ingredients (APIs) fall into Biopharmaceutics Classification System (BCS) Class II and Class IV, characterized by low solubility in aqueous environments. This challenge has led to an increased demand for effective strategies to enhance solubility and, consequently, bioavailability. Since its serendipitous discovery in 1783, the use of cocrystals has been explored to address various physicochemical issues associated with suboptimal performance in both oral and other delivery routes. Cocrystals offer benefits beyond mere dissolution enhancement; they also improve tabletability, flow properties, and physicochemical stability against environmental factors such as light. The versatility of cocrystals extends to the formulation of fixed-dose combinations, enabling the concurrent delivery of multiple drugs. This review aims to elucidate the critical factors in selecting appropriate coformers, suitable preparation methods, and the analysis of cocrystals formed from APIs and coformers. Additionally, the review discusses the advantages that cocrystal technology offers within the pharmaceutical industry.

Keywords: Cocrystals, dissolution enhancement, improved physicochemical properties, methods of synthesis, Applications of cocrystals.

Abstract

Objective: The aim of this study was to compare esmolol to nitroglycerine in terms of effectiveness in controlling hypotension during nasal surgery. Materials and Methods: After approval by our institutional Ethics Committee, 40 patients were recruited and randomized into two drug groups: esmolol (Group E) and nitroglycerine (Group N). In group E, a bolus dose of 500 μg/kg esmolol was administered over 30 sec followed by continuous administration at a dose of 25-300 μg/ kg/min to maintain systolic arterial pressure at 80 mmHg. In group N, nitroglycerine was administered at a dose of 0.5-2 μg/kg/min. Results: During the hypotensive period, systolic arterial pressure, di- astolic arterial pressure, mean arterial pressure, and heart rate were decreased 24%, 33%, 27% and 35%, respectively, in group E (p<0.001, p<0.001, p<0.001, p<0.001) and were decreased 30%, 33%, 34% and 23%, respectively, in group N (p<0.001, p<0.001, p<0.001, p<0.001). The decrease in heart rate was higher in group E during the hypotensive period (p=0.048). During the recovery period, diastolic arterial pressure and heart rate were decreased 9% and 18%, respectively, in group E (p=0.044, p<0.001). Systolic arterial pressure, diastolic arterial pressure, and mean arterial pressure were decreased 7%, 3% and 7%, respectively, in group N (p=0.049, p=0.451, p=0.045). Conclusion: Esmolol provides hemodynamic stability and good sur- gical field visibility and should be considered as an alternative to nitroglycerine.

Keywords: Anesthesia, Controlled hypotension, Esmolol hydrochloride, Nitroglycerin

Abstract

Nonclinical studies play a crucial role in the drug development pathway, providing essential insights into the safety and potential effectiveness of drugs, biologics, and devices. These studies, which include both in vitro and in vivo experiments, are conducted in compliance with Good Laboratory Practices (GLP) and non-GLP standards, and are designed to define the relevant efficacy and/or safety characteristics of the products under development. Nonclinical development experts, such as those at ProPharma Group, provide critical guidance to sponsors, helping to ensure that nonclinical studies are appropriately designed and conducted to support the intended indication, route of administration, and duration of treatment. Nonclinical studies play a crucial role in the development of drugs, biologics, and devices by providing valuable insights into their safety profile and potential effectiveness. Conducting nonclinical evaluations throughout the product development process enables informed decision-making, risk assessment, and enhances confidence in the ultimate success of the clinical evaluations and regulatory approval. Nonclinical studies include pharmacology, pharmacokinetic, and toxicology programs that are appropriate to support the intended indication, route of administration and duration of treatment for the product. The nonclinical development program can help assure that time and resources are not spent on studies that fail to meet regulatory expectations.