How to Make Hard-to-Absorb Medicines Easier for the Body to Use
A method for mixing specific chemical compounds with surfactants to help the body absorb them more effectively.
Patent Number
US 5002952
Status
Active
Filing Date
July 27, 1989
Grant Date
March 26, 1991
Expiration
~July 2009 (estimated)
Claims
14
Assignee
Green Cross Corp Japan
Inventors
Nobuo Kondo, Kazumasa Yokoyama, Nobutoshi Yamada, Tsunetaka Nakajima, Masahiro Watanabe, Hideo Sugi, Takahiro Haga, Toru Koyanagi
Citations
16 forward · 9 backward
What it covers
This patent describes a way to improve how the body absorbs a class of chemicals called benzoyl urea compounds. These compounds are often difficult for the body to process because they do not dissolve well in water. By mixing these compounds with specific nonionic surfactants—substances that help bridge the gap between water and oil—and grinding them into tiny particles (0.2 to 10 micrometers), the inventors created a formula that is much easier for the body to take up. The process involves wet-milling the mixture, often using glass beads, to ensure the particles are small enough to be effective.
What it doesn't cover
- —Does not cover benzoyl urea compounds outside the specific chemical structure defined in claim 1.
- —Does not cover the use of ionic surfactants, which have a different chemical charge profile.
- —Does not cover methods of administration that do not rely on this specific particle-size reduction process.
- —Does not cover the synthesis of the benzoyl urea compound itself, only the composition and its preparation.
The clever bit
The innovation lies in the combination of mechanical wet-milling with specific nonionic surfactants to stabilize the resulting micro-particles, preventing them from clumping back together and ensuring consistent absorption.
Why it matters
Many potent drugs fail in clinical trials simply because the body cannot absorb them efficiently. This patent addresses the 'bioavailability' problem, which is a major hurdle in pharmaceutical development. By providing a standardized way to formulate these compounds, it allows researchers to turn promising chemical candidates into viable, usable medicines.
Real-world examples
- 1.Formulations for agricultural pesticides
- 2.Experimental drug delivery systems for poorly soluble compounds
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