Troxerutin can be prepared using starch as a filler and 95% ethanol as a wetting agent to form a suitable soft mass. After granulation and drying, the granules are sized using a nylon sieve. The mixture is then uniformly mixed with magnesium stearate and talc as lubricants before compression into tablets. The resulting tablets have a smooth and delicate appearance, good tablet hardness, stable tablet weight variation, and qualified content. This process improves the flowability and outflow rate of troxrutin powder, resulting in a fast and uniform granule flow rate, thus ensuring stable tablet weight variation. Granulation also reduces the amount of fine powder, minimizing contact between the powder and the punch, and preventing die pulling. This process requires no drying, consumes little energy, and is low-cost, making it suitable for industrial production.
Used in the treatment of venous disorders
Troxerutin, a derivative of the naturally occurring bioflavonoid rutin, is thought to inhibit red cell and platelet aggregation, improve erythrocyte deformability, and improve plasma viscosity retinal microcirculation. A double-blind randomized clinical trial compared troxerutin with placebo in 27 patients with CRVO. The limitations of the study included a small number of patients and short follow-up time.
In a nitrogen atmosphere 120 g of caustic soda (3 moles) in solution are
added to 610 g of rutin (1 mol) suspended in 2 litres of water, the mixture
being vigorously agitated by a mechanical stirrer, 241.5 g of ethylene
chlorohydrin being then introduced at 55°C for 10 min. When all the
chlorohydrin has been thus added the temperature is progressively raised to
75°C and maintained at this level for 2 hours. After cooling, in a nitrogen
atmosphere, the pH value adjusted to 5 by the addition of dilute hydrochloric
acid. The solution is kept in an ice box for 24 hours and then filtered to
remove any impurities. At reduced pressure the solution is evaporated until
dry, the residue taken up in 3 litres of boning methanol which dissolves the
tri-(β-hydroxyethyl)rutin formed and leaves the sparingly soluble sodium
chloride behind. The tri-(β-hydroxyethyl)rutin is recovered from its methanolic
solution either by evaporation and refrigeration, or by evaporation
precipitation with absolute ethanol. In either case tri-(β-hydroxyethyl)rutin
obtained is in the form of small very hygroscopic crystals which contain
alcohol of crystallization.These crystals are quickly shaken washed in a little
cold absolute ethanol and then dried in vacuum at 100°C. 680 g of anhydrous
tri-(β-hydroxyethyl)rutin are thus obtained in the form of a yellow powder
which melts at 156°C.GB Patent No. 833,174; April 21, 1960; Assigned to Zyma S.A., a Swiss
Corporation, of Route Etraz, Nyon Canton of Vaud, Switzerland
Troxerutin is a brain penetrant, vasoprotective flavonol isolated from Sophora japonica, which is present in many other plants including grains, fruits, and vegetables. Troxerutin exhibits multiple biological activities including anti-oxidative, anti-radiation, and anti-inflammatory. Recent study indicates th at troxerutin improves the synaptic failure induced by Aβ peptide. It appears th at Troxerutin could promote radioprotection by stimulating NEAT1 to upregulate PDPK1 expression by suppressing miR-147.
VEGFR | Wnt/β-catenin | NF-kB | SOD | PI3K | Akt
[1] Patent: CN104478972, 2017, B. Location in patent: Paragraph 0018; 0019; 0020; 0021; 0022; 0023; 0024-0031
[2] Patent: CN106892950, 2017, A. Location in patent: Paragraph 0018-0026
[3] Chinese Chemical Letters, 2013, vol. 24, # 3, p. 223 - 226
[4] Patent: CN103601772, 2016, B. Location in patent: Paragraph 0011-0014
[5] Patent: CN104447914, 2017, B. Location in patent: Paragraph 0013; 0014
