The bigger a pill is, the harder it is to swallow. The pill sizes They do not depend on the whim of the manufacturer but on technical limitations that prevent the drug from being concentrated further without making it more difficult for the body to absorb it.
About 60 percent of the drugs on the market, including many of the most widely used, have hydrophobic substances as active ingredients. It is estimated that about 90 percent of the drugs being developed now are also hydrophobic.
Currently, to create hydrophobic drug tablets, pharmaceutical companies use a process that requires grinding the active compound into nanocrystals, which are easier for human cells to absorb. These crystals are then mixed with excipients, compounds that help stabilize the drug and control its release in the body. An excipient that is often mixed with hydrophobic drugs is methylcellulose, a compound derived from cellulose. Methylcellulose dissolves easily in water, which helps drugs release more quickly in the body.
This method is widely used, but it has many inefficiencies. The milling step requires a lot of time and energy, and the final concentration of the drug is not so high that the entire dose can be put into a small tablet in all cases.
Chemical engineers at the Massachusetts Institute of Technology (MIT) in the United States have now devised a simpler process for incorporating hydrophobic drugs into tablets or other forms such as capsules. His technique, which consists of creating an emulsion of the drug and then crystallizing it, allows to put more drug load in a pill of equal size.
Chemical engineers at MIT have devised a new way of making tablets that allows more of the active substance to be concentrated without compromising the effectiveness of the drug, thus making it possible for the tablets to be smaller, like the ones in the photograph. stored in the vials. (Photo: Felice Frankel. CC BY-NC-ND 3.0)
Using their technique with fenofibrate, a drug used to help lower cholesterol, the team of Liang-Hsun Chen, Patrick Doyle and others have achieved a drug load of about 60 percent. In contrast, the currently available forms of fenofibrate have a drug concentration of approximately 25 percent.
Chen, Doyle and their colleagues have published the details of their new technique in the academic journal Advanced Materials, under the title “Design and Use of a Thermogelling Methylcellulose Nanoemulsion to Formulate Nanocrystalline Oral Dosage Forms.” (Source: NCYT from Amazings)