Tranilast-loaded amorphous solid dispersion prepared with fine droplet drying process for improvement of oral absorption and anti-inflammatory effects on chemically-induced colitis was written by Moritani, Tatsuru;Kaneko, Yuuki;Morinaga, Tadahiko;Ohtake, Hiroto;Seto, Yoshiki;Sato, Hideyuki;Onoue, Satomi. And the article was included in Journal of Drug Delivery Science and Technology in 2021.Product Details of 53902-12-8 This article mentions the following:
The aim of the present study was to evaluate the applicability of a tranilast (TL)-loaded amorphous solid dispersion prepared with a fine droplet drying (FDD) process for the treatment of inflammatory bowel diseases. The FDD process, a novel powderization technol. using an inkjet head, was employed to produce an amorphous solid dispersion of tranilast (ASD/TL). The physicochem. properties of ASD/TL were evaluated in terms of the morphol., particle size, crystallinity, drug-polymer interaction, and dissolution behavior. The oral absorption behavior of TL and anti-inflammatory effect on a chem.-induced colitis model were evaluated after oral administration of TL samples. The particle size of ASD/TL was 4 μm, and the span factor, one of the parameters to present the uniformity of particle size distribution, was calculated to be 0.28. In each ASD/TL particle, TL was dispersed in an amorphous state in the carrier polymer, and ASD/TL showed improved dissolution behavior of TL, as evidenced by a 2-times higher dissolution than the equilibrium solubility of crystalline TL even under acidic conditions. Orally-dosed ASD/TL exhibited rapid and improved oral absorption with 16-fold higher bioavailability than crystalline TL. ASD/TL could significantly attenuate the inflammatory symptoms in the colon tissues of colitis model rats based on the results of histol. analyses and measurement of biomarkers. ASD/TL might contribute to the development of effective treatment for inflammatory bowel diseases due to its enhanced biopharmaceutical properties. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Product Details of 53902-12-8).
2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Product Details of 53902-12-8
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics