Valproate and protoberberine compounds, preparation method and application
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A technology of original berberine and compounds, applied in the field of medicine, to achieve high water solubility, low hygroscopicity, and the effect of facilitating oral absorption
Inactive Publication Date: 2015-08-26
HUNAN PROVINCE CHINESE MEDICINE RES INST OF TRADITIONAL CHINESE MEDICINE +1
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But so far no ideal preparations such as berberine and new derivatives have entered the market
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Embodiment 1
[0020] Preparation of berberine valproate compound
[0021] Dissolve 4 grams of berberine sulfate in 90 ml of warm water, and dissolve 4 grams of sodium valproate in 10 ml of water, mix and stir the above two solutions, filter, put the filtrate in the refrigerator, and precipitate chrysanthemum cluster crystals , filtered, washed with a small amount of ice water and dried, and dried at 60°C.
[0022] The berberine valproate compound is orange-yellow needle-like crystal, with a melting point of about 103°C and no hygroscopicity, which improves the defect of hygroscopicity of sodium valproate.
[0023] The water solubility of berberine valproate compound is large (1:20), which is about 50 times higher than that of berberine hydrochloride (1:1000). Utilization.
[0024] The UV absorption spectrum of the berberine valproate compound that present embodiment 1 obtains: λ 水 max nm 228 244 263 422, consistent with berberine.
[0025] HR-MS (m / s) positive ion mode 336.12275[M Ber...
Embodiment 2
[0033] The mensuration of the fat-water partition coefficient of the berberine valproate compound that present embodiment 1 obtains
[0034]Using the shake flask method and ultraviolet spectrophotometry to measure the content, the n-octanol / water partition coefficient of 2-propylvaleric acid was measured with water and pH3.0, 7.0, and 11.0 buffer solutions, and the lgP was 0.800, 1.014, and 0.668 and 0.608.
[0035] The measured lipid-water partition coefficient values show that berberine valproate not only has high solubility, but also has good permeability, and has a good balance between permeability and solubility.
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Abstract
The invention belongs to the technical field of medicine, and particularly relates to valproate and protoberberine compounds, a preparation method and an application. The valproate and protoberberine compounds have the general structural formula represented by the specification, wherein A <+> represents berberine, coptisine, palmatine, jatrorrhizine or sanguinarine. The valproate and protoberberine compounds have high water solubility and low hygroscopicity and facilitate oral absorption and improve bioavailability, berberine and valproate have the anticancer effect, and berberine further has the functions of delaying epileptic seizure time and relieving the degree of epileptic seizure and can cooperate with valproate for synergy and attenuation.
Description
technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a proberberine compound of valproic acid, a preparation method and an application. Background technique [0002] Original berberine includes Berberine, CAS No. 2086-83-1, Coptisine, CAS No. 6020-18-4, Palmatine, CAS No. 3486-67- 7. Jatrorrhizine, CAS No. 3621-38-3, Sanguinarine, CAS No. 2447-54-3. [0003] Berberine is the main active ingredient widely present in many Chinese herbal medicines such as Coptis chinensis. Berberine hydrochloride (also known as berberine hydrochloride) is a legal over-the-counter drug in my country. It is mainly used for diarrhea and intestinal infection. It is safe and effective and has a long history of use. In recent years, studies have found that berberine has many important pharmacological activities and clinical application values, such as anti-arrhythmia, anti-heart failure, anti-platelet aggregation, anti-rheumatoid arthritis, h...
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