A breakthrough in the treatment of anxiety and insomnia. Polish scientists have developed a new form of a popular drug.

• Polish scientists from three universities in Gdańsk have developed a new, more soluble and ecological form of chlordiazepoxide – a drug for anxiety and insomnia
• The new drug salt with saccharin significantly improves its bioavailability, which may enable reduced doses and reduce side effects
• The invention responds to the growing problem of mental disorders and pharmaceutical challenges related to the poor solubility of many active substances
• A simple and environmentally friendly production method makes the new form of the drug attractive to the pharmaceutical industry, although its market implementation requires long and expensive research.

Research on the innovative solution was conducted by scientists from three universities: the Medical University of Gdańsk (GUMed), the University of Gdańsk (UG) and the Gdańsk University of Technology (PG) .

The University of Gdańsk Technology Transfer Centre announced that the invention was created in connection with the growing problem of mental disorders in societies .

Chlordiazepoxide is a drug belonging to the benzodiazepine group, which is used to treat ailments such as:

• depression,
• anxiety disorders,
• neurosis,
• insomnia,
• illnesses resulting from the abuse of psychoactive substances.

Chlordiazepoxide was discovered in the 1950s by Leon Sternbach, a Polish-American chemist and pharmacist, a graduate of the Jagiellonian University.

Its effectiveness has not been fully exploited so far because chlordiazepoxide does not dissolve well in water , and therefore the rate and extent of absorption of the drug in the body are low.

Scientists have created a new salt of chlordiazepoxide with saccharin, which will allow for much better and faster absorption of the drug in the body.

Prof. Wesołowski from the Department of Analytical Chemistry of the Medical University of Gdańsk told PAP that the basic problem in pharmacy is that most active pharmaceutical substances are very poorly or practically insoluble in water, which significantly limits their bioavailability.

- Available literature data show that approximately 40% of active substances are classified as practically insoluble in water, while up to 70% of active substances being studied as potential drugs are characterized by poor solubility in water - he said.

He added that this situation is particularly unfavourable because poor water solubility and the low dissolution rate of the active substance result in limited bioavailability, i.e. a small amount of the active substance that enters the bloodstream.

- The biological activity of a drug substance in the human body is proportional to the amount of the active ingredient that dissolves in water. Therefore, if the solubility of the drug substance in water is poor, the dose of the drug should be increased to obtain the same therapeutic effect. However, a large dose of the drug may cause increased toxicity of the active substance to the human body, and in addition, it adversely affects the production process of a pharmaceutical preparation with a large dose of the substance and generates higher costs of the production process - said the scientist.

He noted that currently, the most common method of administering drugs is oral.

- In order to induce the therapeutic effect of a medicinal substance taken orally in the form of a solid form of the drug (e.g. a tablet), it is necessary to dissolve it, which is a key factor determining the action of the drug in the body, because only a dissolved medicinal substance can be absorbed by the human body - he added.

The scientist emphasized that the desired direction of research - especially from the point of view of the pharmaceutical industry - is to find an optimal solid form of a given active substance that would be characterized by greater solubility in water.

Prof. Wesołowski said that the invention is aimed at pharmaceutical industry plants.

- The new salt of chlordiazepoxide with saccharin is characterized by better solubility in water compared to pure chlordiazepoxide - an active substance with very low solubility, with anxiolytic and sedative effects. A significant improvement in the solubility of chlordiazepoxide in water may result in an increase in its bioavailability, which creates the possibility of reducing the drug dose and limiting side effects - he noted.

As he added, another advantage is the simple and eco-friendly way of obtaining salt , which does not require advanced equipment or expensive or toxic reagents.

- These advantages of the newly obtained salt can be used by pharmaceutical companies to obtain a new form of the drug with chlordiazepoxide, e.g. tablets with controlled release of the active substance - he said.

- Research related to introducing a new product to the pharmaceutical market is long-term and very expensive, and includes many stages of research, including several phases of clinical trials involving humans - he emphasized.

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