3
RUDN University Scientists in Pharmaceutical Technology Proved Effectiveness of New Dosage Form

RUDN University Scientists in Pharmaceutical Technology Proved Effectiveness of New Dosage Form

RUDN University scientists together with colleagues from Switzerland proved in a clinical trial the effectiveness of a new dosage form — amorphous solid dispersion. This is the first such study in humans to show the mechanism of action of this form of drug release. In the future, it will help to increase the effectiveness of drugs and use new active substances for treatment.

One of the main reasons for the dropout of new oral drugs at the preclinical and clinical stages of development is low bioavailability. The drug itself can be effective, but it is poorly absorbed in the body because of its low solubility. Amorphous solid dispersion (ASD) is a new form of drug release that has the potential to solve this problem. ASD consists of a drug substance and a polymer framework that “binds” the drug and improves its solubility, thus increasing bioavailability. RUDN University scientists in the field of pharmaceutical technology, together with colleagues from Switzerland, conducted a clinical study and proved the effectiveness of ASD. This is the first such human trial.

“Despite the research effort on mechanisms of increased bioavailability through ASDs during the last decades, these mechanisms are far from being understood in every detail. Furthermore, the translation from preclinical studies to clinical outcomes in humans has not been validated. This clinical study aimed to investigate the mechanisms and effects of a particle forming ASD on bioavailability in humans to understand the complex absorption from ASDs in humans. To our best knowledge, there are currently neither documented data nor methods providing such insights”, Rimma Abramovich, Doctor of Pharmaceutical, Director of the Shared Research and Education Center of the RUDN University

The clinical study involved 16 volunteers; healthy men aged 20 to 38 years. As a model medicine, doctors used the antiviral drug efavirenz, which is used in the treatment of HIV infection. Participants in the study took efavirenz orally in three different forms in three interventions — 50 mg in the form of solid ASD, 50 mg in the form of dissolved ASD, and 3 mg of a molecular solution of efavirenz. To avoid distortion of the results, doctors maintain a washout period of 14 to 21 days. After each intervention, the doctors took a blood test and measured the pharmacokinetic profile — the dynamics of efavirenz concentration in blood plasma over time.

It turned out that ASD in solid form works in the same way as a regular efavirenz tablet — the maximum concentration of about 6.5 nanograms per milliliter is reached in two hours. And the dissolved ASD acts as a molecular solution of the drug — the concentration of the drug in the blood reached approximately the same value after the same time — about 10 nanograms per milliliter after 50-60 minutes. However, given that the molecular solution is absorbed from the intestine into the blood passively (that is, without additional chemical reactions), the scientists calculated that the actual concentration of the drug in the intestine in the case of dissolved ASD is 16.7 times higher than in the case of conventional efavirenz. This means that the dissolved ASD behaves like a so-called supersaturated solution; meaning that it contains 10 times more dissolved matter than it can dissolve under normal conditions.

“We could show that drug absorption from drug-rich particles, formed upon the dissolution of the ASD, was fast and complete in humans”, Rimma Abramovich, Doctor of Pharmaceutical, Director of the Shared Research and Education Center of the RUDN University.

Student's Scientific Initiatives View all
03 Nov 2017
June 22 - 26, 2017 in Barnaul, Altai State University, took place the Summer Academy of the BRICS Youth Assembly, an international event that brought together representatives of different countries
1012
International scientific cooperation View all
03 Nov 2017
The main goal of the RUDN University and UNISDR Office for Northeast Asia and Global Education and Training Institute for Disaster Risk Reduction at Incheon (UNISDR ONEA-GETI) cooperation is to obtain knowledge about disaster risk reduction and international experience in this area for creating training courses for basic and additional professional education in RUDN
974
Similar newsletter View all
31 Mar
RUDN University awards for specific areas of science and technology based on the results of 2021

Every year, RUDN University selects the best of the best in the field of science and innovation and encourages with a special reward. Since 2009, the Academic Council of the University has been awarding one reward in natural and technical sciences and the other one in social and humanitarian sciences. Both individual researchers and groups of authors can become laureates.

46
31 Mar
International Day of Women and Girls in Science: women scientists of the RUDN talk about their path to science

“Science is the basis of all progress that facilitates the life of mankind and reduces its suffering,” — Marie Sklodowska—Curie. A symbol of a woman’s success in science. The first scientist in the world — twice winner of the Nobel Prize.

290
31 Mar
RUDN University Mathematicians Create a Model for Queue Organizing with Self-Sustained Servers

RUDN University mathematicians proposed a model for optimizing the operation of queuing systems (from computer networks to stores). Unlike analogues, the servers in it are self-sustained. They can determine when to start and stop working themselves. Such a model can be useful, for example, for online taxi services and other systems where workers choose their own operating hours.

57
Similar newsletter View all