1、 Pharmacopoeia standard of Fangji
Fangji
Fangji
STEPHANIAE TETRANDRAE RADIX
This product is the dried root of Stephania tetrandra S.moore, a plant powder of tetrandriaceae. Excavate in autumn, wash, remove the coarse skin, sun dry until semi dry, cut into sections, and then cut into longitudinal sections for drying.Fangji
STEPHANIAE TETRANDRAE RADIX
[properties] the product is irregular cylindrical, semi cylindrical or massive, with many bends, 5-10cm long and 1-5cm in diameter. The surface is grayish yellow, and there are often nodular tumor like deep transverse grooves at the bends. It is heavy, solid, flat section, gray white, rich in powder, with sparse radial texture. The breath is slight and the taste is bitter.
[identification] (1) cross section of this product: sometimes the cork layer remains. There are scattered stone cell groups in the inner layer of the plug, which are often arranged tangentially. Phloem is wider. The cambium forms a ring. The xylem accounts for the majority, and the ray is wide; ; There are wood fibers beside the catheter. Parenchyma cells were filled with starch granules, and fine rod-shaped calcium oxalate crystals could be seen.
(2) Take 1g of this product powder, add 15ml of ethanol, heat and reflux for 1 hour, cool, filter, evaporate the filtrate, add 5ml of ethanol to dissolve the residue, and use it as the test solution. In addition, take tetrandrine reference substance and tetrandrine reference substance, add chloroform to make a mixed solution containing 1mg per 1ml as the reference solution. . In the chromatogram of the test sample, spots with the same color appear at the corresponding position of the chromatogram of the control sample.
[check] moisture Not more than 12.0% (the second method of general rule 0832).
Total ash Not more than 4.0% (general rule 2302).
[extract] according to the hot leaching method under the determination method of alcohol soluble extract (general rule 2201), using methanol as solvent, it shall not be less than 5.0%.
[content determination] determine according to HPLC (general rule 0512).
; Octadecylsilane bonded silica gel was used as filler; The mobile phase was acetonitrile methanol water glacial acetic acid (40:30:30:1) (containing 0.41g sodium dodecyl sulfonate per 100ml); The detection wavelength is 280nm. The number of theoretical plates should not be less than 4000 according to the tetrandrine peak.
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Preparation of test solution Take about 0.5g of this product powder (passing through No. 3 screen), accurately weigh it, precisely add 25ml of 2% hydrochloric acid methanol solution, weigh it, heat and reflux for 30 minutes, cool it, then weigh it, use 2% hydrochloric acid methanol solution to make up for the lost weight, shake it well, filter it, accurately measure 5ml of continuous filtrate, put it in a 10ml measuring bottle, add mobile phase to the scale, shake it well, and get it.
Assay Precisely suck 10 µ l of the control solution and 10 µ l of the test solution respectively, inject them into the liquid chromatograph, and determine.
The total amount of tetrandrine (c38h42n2o6) and tetrandrine (c37h40n2o6) in this product shall not be less than 1.6% according to the dry product.
Decoction pieces
[processing] remove impurities, soak slightly, wash, moisten thoroughly, cut into thick pieces, and dry.
This product is a thick piece of quasi-circular or semi-circular shape. The outer skin is light grayish yellow. The cut surface is gray white, powdery, with sparse radial texture. The breath is slight and the taste is bitter.
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[identification] (except the cross-sectional surface) [inspection] [extract] is the same as that of medicinal materials.
. It belongs to bladder and lung meridian.
[functions and indications] dispel wind, relieve pain, promote diuresis and reduce swelling. It is used for rheumatism, arthralgia, edema, beriberi, adverse urination, eczema and sores.
[usage and dosage] 5 ~ 10g.
[storage] put it in a dry place to prevent mold and moth.
2、
① Sinomenine, tetrandrine, a phenolic alkaloid, MENICINE, menidine, and rhynchophylline.
The alkaloids of tetrandra tetrandra had various synonyms,SinomenineIt was once known as tetrandrine, tetrandrine, nortetrandrine, tetrandrine B, and tetrandrine, a phenolic alkaloid. Menonisine was originally called tetrandrine a, and menidine was originally called tetrandrine B, which are isomers of tetrandrine and nortetrandrine, respectively.
Fenfangji root still contains flavone glycosides, phenols, organic acids, volatile oils, etc.
② The root of tetrandrine contains tetrandrine, IsotetrandrineMagnoliane, tetrandrine, tetrandrine, mephenisine, normephenisine and other alkaloids
3、 Pharmacological action of Radix stephaniae tetrandrae
① Tetrandra tetrandra: an analgesic effect
The analgesic effects of tetrandrine, tetrandrine a, tetrandrine B and tetrandrine C were measured by hot plate method in mice. The total base has the strongest effect, with an effective dose of 50 mg / kg and a median lethal dose of 241-251 mg / kg. Tetrandrine has stronger analgesic effect than a and B, but it is also toxic, so it has no practical value. The method of electrically stimulating mouse tail also proved that a, B and tetrandrine extract or fried wattle all have certain analgesic effects. The effect of a is stronger than that of B, and its effective dose is 10 ~ 20 times greater than that of morphine. If the analgesic efficacy of morphine is 100, the total alkaloids of tetrandrine and Corydalis are about 13 and 40, respectively. When the latter two are combined, the analgesic efficacy is not increased, but weakened. Diphenhydramine, an anti histamine drug, can significantly enhance the analgesic effect of a and B without affecting their toxicity. It has been reported that the analgesic effect of tetrandrine was weakened or even disappeared after a certain dose was exceeded, which may be due to the fact that a larger dose of tetrandrine can excite the central nervous system, thus weakening the analgesic effect. However, according to foreign reports, 100-250 mg / kg of α - adrenergic acid is required for mice to increase the pain threshold by 7-10%. Clinically, 30 mg oral or subcutaneous injection has no significant analgesic effect.
II. Anti inflammatory and anti allergic effects
Tetrandrine and tetrandrine B have certain anti-inflammatory effects on formaldehyde induced arthritis in rats; The effect of a is stronger than that of B. In this regard, the effect of a is similar to that of cortisone, stronger than sodium salicylate and weaker than that of butazone. After adrenalectomy, the effect disappeared. It can reduce the content of vitamin C in rat adrenal gland and eosinophils in peripheral blood; It still has this effect when given again 7 days after the removal of the pituitary gland, so it acts directly on the adrenal gland. In normal rats, the vitamin C content in the adrenal gland did not decrease, and there was no hypertrophy in the bilateral adrenal glands. The excretion of 17 hydroxysterols in urine did not increase, indicating that its role in exciting the adrenal cortex is nonspecific. ; In rat skin trypan blue test, it can reduce vascular permeability. For anaphylactic shock in rabbits caused by whole egg white, it can significantly reduce the incidence of severe shock symptoms, but has no obvious effect on mortality, and has no effect on histamine shock in guinea pigs. In addition, it can inhibit immune hemolysis. It has also been reported that, like antigenic substances, it can activate lymph nodes, increase the weight and concentration of RNA in plasmablasts and plasma cells, and cause the increase of such cells. Because it has mild analgesic, anti-inflammatory, antipyretic, anti anaphylactic shock and other effects, it should belong to antipyretic analgesic.
Three effects on the circulation system
Tetrandrine has a significant antihypertensive effect on anesthetized cats. 3-6 mg / kg can reduce blood pressure by 50-65% for more than 1 hour. It can be administered intravenously, intramuscularly or orally. During hypotension, cardiac contractility was only temporarily weakened, and heart rate and conduction had no significant changes. The dilation of blood vessels was stronger and longer than that of papaverine in both isolated and rabbit ear specimens. . Atropine can partially cancel the hypotensive effect of A. For the asystole heart, it can also significantly increase the coronary flow. For guinea pigs
Effects of four pairs of striated muscles
Tetrandrine and some of its analogues have the effect of relaxing striated muscles.
Five effects on smooth muscle
It was reported earlier that tetrandrine could inhibit the uterine smooth muscle of guinea pigs or rabbits in isolated small intestine of rabbits. In fact, this is dose-dependent. The isolated rabbit intestine was excited first and then inhibited. A larger dose could partially inhibit the spastic contraction caused by pilocarpine and barium chloride. . It causes contraction of bronchial smooth muscle in guinea pigs and cats, which is caused by the release of histamine. The tension of isolated rabbit, guinea pig small intestine and in vivo rabbit intestinal smooth muscle was increased, and the contraction amplitude was decreased.
Vi. antibacterial, antigenic and antitumor effects
Tetrandra tetrandra has some antibacterial (Shigella) and antifungal effects in test tubes, but the variety has not been identified, and the concentration is relatively high. Tetrandrine can inhibit or kill amoeba histolytica in vitro and in vivo (mouse cecum method), and its intensity is 1 / 22 of that of emetine, but more than that of berberine At 1:4000, a can kill cancer cells in vitro. 30-50 mg / kg intraperitoneal injection or 100 mg / kg subcutaneous injection (the median lethal dose is 950 mg / kg) can inhibit Ehrlich ascites cancer cells in mice and ascites liver cancer cells in rats.
VII. Other functions
Tetrandrine had hypnotic effect on dogs, but had no antagonistic effect with apomorphine; The neutrophils in rabbits were significantly increased while lymphocytes were decreased. Tetrandrine a, tetrandrine B and tetrandrine can make pigeons vomit. Tetrandrine can excite the central nervous system, and a small dose can cause respiratory excitation and hyperreflexia; The toxic dose caused clonic convulsion in mice and died of respiratory failure. Phenobarbital had antagonistic effect, and had antipyretic effect on rats with fever caused by injection of E. coli broth; It does not cause vomiting of animals.
② Tetrandrine: tetrandrine has a cooling effect on febrile rabbits, which can reduce rabbit blood pressure and vasoconstrict; Paralyze the frog's myocardium and skeletal muscles. . It has no obvious effect on nitrogen metabolism in rabbits and can enhance lymphogenesis in dogs; It can paralyze Paramecium. It has some protective effects on the lethal effects of tetanus, diphtheria, botulinum toxin and tetrodotoxin on mice. The minimum lethal dose for rabbits is 0.05 g / kg for intravenous injection and 0.15 g / kg for subcutaneous injection. The minimum lethal dose of subcutaneous injection to frogs and mice is 0.5 ~ 1.0 g / kg, which can cause paralysis and occasional convulsion of animals, and die of respiratory failure.
The non alkaloid component tetrandrine 50 mg / kg or B 200 mg / kg has no antipyretic effect on rats (fever caused by E. coli broth injection). The hot plate method in mice proved that a and B had no analgesic effect. The median lethal dose of intravenous injection of a to mice is 76 mg / kg, and the toxicity of B is very low. For the effect of magnoliane, see the green wood incense stick.