Synthesis of glibenclamide cocrystals through grinding methods
Abstract
The pharmaceutical industry has been struggling against problems related with drugs with low solubility as this is a very limiting factor in the development of drug products. Co-crystals are solid forms known for a very long time although they have not been fully explored in their potentialities. Co-crystals can be defined as crystalline homogenous structures composed of two or more compounds, held together by noncovalent bonds, usually hydrogen bonds, and solid at room temperature. These structures can change the physicochemical properties of drugs, like solubility, dissolution rate, stability and particle properties, which could be interesting for the drug development process. It is still difficult to identify the optimal co-crystallization method for each situation and typically this process is evaluated on a case-by-case basis. Reported studies show that the most commonly used method is solvent evaporation. However, the main drawback of solvent evaporation is the scale-up difficulty. Therefore, this work explored milling as an alternative method. This method can more easily be scaled-up. This work is based on the co-crystallization of glibenclamide, a sulfonylurea used in the treatment of non-insulin-dependent diabetes mellitus. Glibenclamide is categorized as a class II drug (low solubility, high permeability) by the Biopharmaceutical Classification System. The formation of co-crystals was attempted with six different co-formers – adenine (ADE), nicotinamide (NICO),…
Read the paper
Related studies
- Improving sleep quality leads to better mental health: A meta-analysis of randomised controlled trials
- Tocilizumab in patients with severe COVID-19: a retrospective cohort study
- A new aging measure captures morbidity and mortality risk across diverse subpopulations from NHANES IV: A cohort study
- Fruit, vegetable, and legume intake, and cardiovascular disease and deaths in 18 countries (PURE): a prospective cohort study
- Are noise and air pollution related to the incidence of dementia? A cohort study in London, England
- Long COVID symptoms and duration in SARS-CoV-2 positive children — a nationwide cohort study
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.