Active constituents: baicalin, and baicalein.
There is an increasing amount of evidence demonstrating baicalein and baicalin’s anti-cancer potential.
Metabolic Interaction between Ammonia and Baicalein {study} "In conclusion, this study confirmed that baicalein, a flavonoid with a vic-trihydroxyl structure on the A-ring, has the potential to detoxify ammonia and treat ammonia-associated chronic diseases."
Baicalein inhibits 5-LOX
Baicalein is an iron chelator {ref}
Synergy
Safety, tolerability, and pharmacokinetics of a single ascending dose of baicalein chewable tablets in healthy subjects {study} "Single oral doses of 100-2800 mg of baicalein were safe and well tolerated by healthy subjects. Clinical laboratory assessments showed no signs of toxicity in the liver or kidney."
References & Sources
- Anti-cancer effects of baicalein in non-small cell lung cancer in-vitro and in-vivo
- (2015) Baicalin induces apoptosis in hepatic cancer cells in vitro and suppresses tumor growth in vivo
- The Fascinating Effects of Baicalein on Cancer: A Review
Preparation of baicalin suspension,
Baicalin Magnesium salt
https://data.epo.org/publication-server/document?iDocId=6289731&iFormat=2
[0030] Adding baicalin powder to purified water at a weight (g)-volume (ml) ratio of 1: 20-100 of the baicalin to the purified water ; and uniformly mixing the same to obtain a baicalin suspension.
[0031] The baicalin is used as a raw material, which is commercially available.
[0032] According to the present invention, when the ratio of the baicalin to the purified water is greater than 1:20, the concentration of the baicalin suspension is too high to bring about many impurities due to incomplete reaction; however, when the ratio of the baicalin to the purified water is less than 1:100, the reaction rate of magnesium ion-containing baicalin suspension is slow, bringing about many impurities due to incomplete reaction. Therefore, the ratio of the baicalin to the purified water is 1:20-100, preferably 1:30-70, and more preferably 1:32-36.
B. Preparation of magnesium ion-containing baicalin suspension
[0033] Adding a magnesium compound in the baicalin suspension obtained in step A at a molar ratio of baicalin to magnesium of 0.5-3.0:1; and uniformly mixing the same to obtain a magnesium ion-containing baicalin suspension.
[0034] The magnesium compound is selected from the group consisting of magnesium hydroxide, magnesium oxide, basic magnesium carbonate, magnesium acetate, magnesium sulfate, magnesium nitrate and magnesium chloride, which are commercially available.
[0035] Preferably, the magnesium compound is magnesium hydroxide, magnesium oxide or basic magnesium carbonate.
[0036] More preferably, the magnesium compound is magnesium hydroxide.
[0037] According to the present invention, When the molar ratio of baicalin to magnesium is less than 0.5:1, there will be many remaining magnesium ions in the reaction, which form impurities in the resulting product; however, when the molar ratio of baicalin to magnesium is greater than 3.0:1, the amount of the baicalin is too high resulting in lower reaction rate, and thus it is difficult to filter the magnesium ion-containing baicalin suspension due to many impurities. Therefore, the molar ratio of baicalin to magnesium is 0.5-3.0:1; preferably 0.8-2.6:1; and more preferably 1.8-2.2:1.
C. Reaction
[0038] Reacting the magnesium ion-containing baicalin suspension obtained in step B at 20-70°C under stirring until the reaction becomes clear; and then filtering the magnesium ion-containing baicalin suspension to obtain a filtrate.
[0039] In this step, the baicalin is reacted with the magnesium compound in the magnesium ion-containing baicalin suspension to generate baicalin magnesium, that is in a reaction medium, Mg2+ from the magnesium compound is bonded to COO- from the baicalin to generate the baicalin magnesium.
[0040] A temperature at which the baicalin reacts with the magnesium compound is 20-70°C, and when the temperature is lower than 20°C, the reaction is too slow, resulting in too many impurities; however, when the temperature is higher than 70°C, the baicalin will be decomposed. Preferably, the reaction temperature is 40-65°C, and more preferably 50-60°C.
[0041] In the present invention, the reaction progress is determined by whether the reaction system becomes clear and transparent, because the reaction is a precipitation reaction producing a precipitate and a resulting product which is dissolved in the reaction system. The reaction is completed when it becomes clear.
[0042] In this step, filtration is to remove residues that are not completely reacted in the reaction system, or other impurities without participating in the reaction.
[0043] In this step, a filter unit for the filtration may be various filter units which are usually used in pharmaceuticals and chemical industries; for example, a vacuum filter, a plate-and-frame filter press and the like.
D. Drying
[0044] Drying the filtrate obtained in step C to produce the baicalin magnesium compound.
[0045] In the present invention, the drying process is heating to evaporate, spray drying or freeze drying.
[0046] In the present invention, the heating to evaporate should be interpreted as heating to evaporate the moisture in the filtrate obtained in step C to produce a baicalin magnesium compound having a moisture content of 1.0% or less by weight.
[0047] In the present invention, the moisture content is determined by oven drying.
[0048] The spray drying should be interpreted as dispersing the filtrate obtained in step C into particles by a spray drying device and bringing the particles into contact with hot air to instantly remove moisture so as to obtain the baicalin magnesium compound having a moisture content of 1.0% or less by weight. The spray drying device is commercially available, for example, a product under the trade name QZR-5 (Linzhou Drying Machine Company, Xishan, Jiangsu).
[0049] The freeze drying should be interpreted as freezing the filtrate obtained in step C to 0°C or less by a freeze-drying device and sublimating moisture from solid to vapor by heating under high vacuum to remove the moisture so as to obtain the baicalin magnesium compound having a moisture content of 1.0% or less by weight. The freeze-drying device is commercially available, for example, a product under the trade name LGJ-22D (Beijing Four-Ring Scientific Instrument Co., Ltd.).
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