Activery The amorphization specialist
Activery believes that amorphous drugs provide new and innovative routes to final dosage forms with differentiated pharmacokinetics
| Nanoparticle Processing in the Solid State Dramatically Increases the Cell Membrane Permeation of a Cholesterol-Lowering Drug, Probucol |
 |
 |
 |
|
Nanoparticle Processing in the Solid State Dramatically Increases the Cell Membrane Permeation of a Cholesterol-Lowering Drug, Probucol
High cholesterol levels (or hypercholesterolemia) are linked with many diseases, particularly with the risk of coronary heart diseases. Probucol is commonly used to reduce cholesterol in blood. While the effectiveness of this drug highly depends on its solubility, unfortunately, it is nearly insoluble (solubility is 5 ng/mL in water). Therefore, it is essential to develop approaches to increase its solubility and bioavailability and to enhance the efficiency of the drug. Here we show that a new method increases the solubility of probucol in water and its ability to permeate cell membranes. This new method of processing the drug in a nanoparticle utilizes the grinding of PBC probucol together with sodium dodecylsulfate and methacrylic copolymer. Solid-state NMR experiments reveal the polymorphic state of probucol and the conversion of this drug from crystalline to the amorphous state, and determine its nearness to the copolymer due to the grinding process that enables the formation of nanoparticles.
|
Pharma Notes
- New study on Inhaled Drug Delivery Market
- Particles that deliver larger and more effective doses of drugs to cancers
- The global protein therapeutics market will be worth $77bn by 2011 with biogenerics playing an increasingly important rol
- A federal jury in Texas Monday upheld the patent on Johnson & Johnson's arthritis treatment Remicade and ordered Abbott Laboratories to pay its rival $1.67 billion for infringing on the patent
- Transdermal delivery represents an attractive alternative to oral delivery of drugs and is poised to provide an alternative to hypodermic injection tool
Differentiated Generics
- Teva may lose patent challenge
- Labopharm receives notice of ANDA submission with paragraph IV certification for generic of Ryzolt
- Depomed (DEPO) Receives Paragraph IV Notice from Lupin Limited Over Patent Filing for Generic Glumetza Tablets
- The rate and number of successful Paragraph IV challenges is reducing the average effective patent life for innovator drugs
- Teva Sues Mylan Over Multiple Sclerosis Drug COPAXONE
Nanoparticles world
- Nanoparticle created to attack cardiovascular plaque
- Nanoparticle lung threat blocked
- Newly-developed nanoparticle to build therapies for treating individuals with cardiovascular disease.
- Nanoparticle Processing in the Solid State Dramatically Increases the Cell Membrane Permeation of a Cholesterol-Lowering Drug, Probucol
- Erectile dysfunction could be treated by a nanoparticle formulation applied directly to the penis