Flos Daturae
1、 Pharmacopoeia standard of Flos Daturae       This product is the dried flower of Datura metel. From April to November, the flowers are harvested at the beginning of bloom, dried in the sun or at low temperature.
      [character] this product is mostly shrunk into strips, and the complete one is 9 ~ 15cm long. The calyx is tubular, 2/5 of the corolla, grayish green or grayish yellow, the apex is 5-lobed, the base has 5 longitudinal veins, and the surface is slightly hairy; The Corolla is trumpet shaped, light yellow or yellowish brown, the apex is 5-lobed, the lobes have short tips, there are 3 obvious longitudinal veins under the short tips, and the two lobes are slightly concave; Stamens 5, filaments adnate to corolla tube, 3/4 of corolla length; . The drying quality is flexible and the air is special; Dried in the sun, it has crisp quality, slight air and bitter taste.
      . The pollen grains are spherical or oblong, with a diameter of 42 ～ 65 μ m, and there are striated carvings on the surface. Calyx non glandular hairs 1-3 cells, wall with warty process; Glandular hair has 1-5 cells in the head and 1-5 cells in the stalk. The margin of corolla lobes is 1-10 cell non glandular hairs, and the wall is slightly warty. The non glandular hairs at the base of the filament are thick, 1-5 cells, the diameter of the base is about 128 μ m, and the top is blunt. There are calcium oxalate sand crystals, square crystals and cluster crystals in the thin-walled cells of calyx and corolla.
      (2) Take 1g of this product powder, add 1ml of concentrated ammonia test solution, mix well, add 25ml of trichloromethane, shake well, place overnight, filter, evaporate the filtrate, add 1ml of trichloromethane to dissolve the residue as the test solution. . Test according to thin-layer chromatography (general rule 0502), suck 10 μ l each of the above two solutions, dot them on the same silica gel G thin-layer plate, use ethyl acetate methanol concentrated ammonia test solution (17:2:1) as the developing agent, develop, take out, dry, and spray with dilute bismuth potassium iodide test 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.
      [inspection] the moisture content shall not exceed 11.0% (the second method of general rule 0832).  
        The total ash content shall not exceed 11.0% (general rule 2302).
      Acid insoluble ash content shall not exceed 2.0% (general rule 2302).
      [extract] according to the hot leaching method under the determination method of alcohol soluble extract (general rule 2201), the use of ethanol as solvent shall not be less than 9.0%.
      [content determination] determine according to HPLC (general rule 0512).
      Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; The mobile phase was acetonitrile-0.07mol/l sodium phosphate solution (containing 0.0175mol/l sodium dodecyl sulfate, adjusting the pH value to 6.0 with phosphoric acid) (50:100); The detection wavelength was 216nm. The number of theoretical plates should not be less than 3000 according to the peak of scopolamine hydrobromide.
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      Preparation of test solution take about 1g of powder (passing through No. 3 screen), weigh accurately, place in a conical flask, add 10ml of 2mol/l hydrochloric acid solution, sonicate (power 250W, frequency 40KHz) for 30 minutes, cool, filter, wash the filter residue and filter with 10ml of 2mol/l hydrochloric acid solution for several times, combine the filtrate and washing solution, adjust the pH value to 9 with concentrated ammonia test solution, extract 4 times with trichloromethane, 10ml each time, combine the trichloromethane solution, recover the solvent to dryness, dissolve the residue with mobile phase, transfer to a 5ml volumetric flask, add mobile phase to the scale, shake well, filter, and take the filtrate is obtained.
      The determination method is to precisely suck 10 μ l of the reference solution and 10 μ l of the test solution, inject them into the liquid chromatograph, and determine.
      The content of scopolamine (C17H21NO4) shall not be less than 0.15% according to the dry product.
      [nature, taste and meridian tropism] pungent, warm; Toxic. Return to lung and liver channels.
      [functions and indications] relieve asthma and cough, relieve spasm and relieve pain. It is used for asthma and cough, cold pain in the abdomen, rheumatism and arthralgia, and slow shock in children; .
      [usage and dosage] 0.3 ～ 0.6g, Yiru pill powder; It can also be used for cigarette smoking in several times (the daily volume is not more than 1.5g). .
      [note] it is forbidden for pregnant women, patients with exogenous diseases, phlegm heat cough and asthma, glaucoma, hypertension and tachycardia.
      [storage] put it in a dry place to prevent mold and moth.


2、
1. the flower of Datura stramonium contains 0.12% - 0.82% of hyoscine alkaloids, among which hyoscine isScopolamine(scopola mine) is 0.11% - 015%, and hyoscyamine is also known asHyoscyamine0.01% - 0.37% [1, 2]. It also contains atropine [3].
2. Datura stramonium flower contains alkaloids of 0.19% - 0.53%, including the alkaloids of 0.19% - 0.53% in the flower...................The content of the alkaloids in the flower of Datura stramoniScopolamine0.17% - 0.53%,Hyoscyamine0.01% - 0.49% [1, 2]. It also contains atropine [3], tyramine,Scopolamine Apocynum(aposcopolamine) is apohyoscine [4].
The flowers of the same genus mameru contain alkaloids from 0.14% to 0.33%, of whichScopolamine0.03% - 0.09%,HyoscyamineIt is 0.08% - 0.28% [1, 5], and also contains atropine [3]. Scopolamine, up to 0.4%, plusHyoscyamine[1,5] and trace atropine [3].

3、 Pharmacological effects of Flos Daturae
1. effects on the central nervous system: 1.1. effects on behavior: when scopolamine 6mg/kg was injected into the lateral ventricle of rabbits, the eye closure, lateral recumbency, righting reflex disappeared, and recovered after about 40 minutes, but the activity was still less. Scopolamine Combined with hibernation mixture can produce general anesthesia in humans, monkeys and dogs. Scopolamine Combined with pentobarbital or meperidone can also significantly reduce the activity of mice, showing a synergistic effect with central inhibitors. Low dose scopolamine (0.1-0.2mg/kg) increased the spontaneous activity of mice. Intraperitoneal injection of scopolamine 4mg/kg in mice can enhance the activity increase caused by central stimulants (amphetamine, methamphetamine, caffeine, etc.), and can resist the activity reduction caused by reserpine and chlorpromazine, showing the central excitatory effect. Therefore, the effect of scopolamine on the central nervous system is bidirectional.
1.2. effect on EEG: awake cats with buried electrodes were intraperitoneally injected with scopolamine hydrobromide 0.05-0.1mg/kg. After 5 minutes, EEG changed from low amplitude fast wave to irregular high amplitude slow wave. But at this time, the wake-up reaction still existed, and the animals were quiet. When the dose was increased to 0.25-0.50mg/kg, the EEG activity showed highly synchronized and irregular high amplitude slow waves, and the EEG wake-up response also disappeared; The animals showed excitement and mania. For monkeys, dogs, rabbits, rats and other animals, scopolamine induced EEG responses are very similar, and can block the wake-up response caused by a variety of physiological stimuli.
1.3. effects on conditioned reflex: scopolamine 0.05-100mg/kg subcutaneously injected into rats can block avoidant conditioned reflex and secondary conditioned reflex to varying degrees, and the blocking rate is in parallel with the dose. Scopolamine had the strongest effect on the secondary and conditioned reflexes, while atropine had a weaker effect on the avoidance conditioning in rats.
1.4. effect on pain perception: Rabbit potassium ion penetration method and mouse hot plate method proved that scopolamine has certain analgesic effect, and can strengthen the analgesic effect of dolantin, and resist the reduction of pain threshold caused by norepinephrine lateral ventricular injection and the attenuation of dolantin analgesic effect. Mice were intraperitoneally injected with 0.2mg of total alkaloids of Flos Daturae. After 15 minutes, the pain threshold of radiant heat could be increased by 54.7%. It has also been reported that scopolamine has a stronger central analgesic effect on tremor than atropine.
1.5. interaction with neurotransmitters: 1/100000 scopolamine for lateral ventricle perfusion in cats can increase the release of acetylcholine. During perfusion, intravenous injection of scopolamine 1mg/kg can not further increase the release of acetylcholine. However, intraperitoneal injection of scopolamine 0.63mg/kg in rats can reduce the content of acetylcholine in the brain by 31%. The effect is strongest 60 minutes after administration, and returns to normal at 120 minutes, indicating that non lateral ventricle administration can still promote the release of acetylcholine in the brain. . Intravenous injection of reserpine 0.5-1.0mg/kg or intracerebroventricular injection of p-chlorophenylalanine (PCPA) 5.0mg/kg each could prolong the anesthesia caused by intracerebroventricular injection of scopolamine 2-3mg/kg, but intracerebroventricular injection of 5-HT 250mg each and intravenous injection of youjiangning 50mg/kg could significantly shorten the anesthesia time; However, intracerebroventricular injection of norepinephrine 20O μ g per animal had no significant effect on the duration of scopolamine anesthesia.
Therefore, scopolamine mainly has inhibitory effects on some parts of the cerebral cortex and subcortical, such as disappearing consciousness and producing anesthesia. It is believed that this is related to its blocking of m-choline receptors in the cerebral cortex and brainstem reticular structure, and may also be related to its anti noradrenalin effect in the central nervous system. But it has different degrees of excitatory effect on medulla oblongata and spinal cord, especially on the respiratory center of medulla oblongata. For this reason, scopolamine can increase the respiratory rate of awake dogs, thus counteracting the effect of hibernating drugs (dolantin and chlorpromazine) to slow down breathing.
2. effects on the circulatory system: 2.1. effects on the cardiovascular system: scopolamine can relieve the inhibition of the vagus nerve on the heart, making sympathetic nerve dominant, so the heart rate increases. Atropine has similar and stronger effects. . In vitro rabbit ear vascular perfusion showed that scopolamine 20mg could antagonize the vasoconstriction induced by norepinephrine 20 μ g/0.1mg, but this effect was much weaker than that of atropine.
2.2. effects on hemodynamics: the cardiac output of hemorrhagic shock dogs was not increased after intravenous injection of total alkaloids of Flos Daturae, but after blood transfusion to supplement blood volume, total alkaloids of Flos Daturae could increase cardiac output. It is suggested that the effect of Flos Daturae on cardiac output is related to blood volume. Scopolamine 10-20mg/kg intravenously injected into anesthetized rabbits can antagonize the pressor effect of intravenous injection of 5 μ g/kg epinephrine or norepinephrine. .
3. effects on respiratory system and smooth muscle organs: low dose of Flos Daturae injection can completely antagonize the contraction of isolated guinea pig tracheal smooth muscle caused by acetylcholine. . Scopolamine can reduce the peristalsis and tension of gastrointestinal tract, block the function of cholinergic nerve, relax bladder detrusor, contract urethral sphincter, and cause urinary retention.
4. other effects: when the total alkaloid of Flos Daturae or scopolamine is used as an anesthetic, it can dilate the blood vessels around the patient, increase the body surface temperature, and decrease the body temperature. . After the application of Flos Daturae anesthesia to psychiatric patients, the average value of blood cholinesterase activity was significantly increased by intravenous administration, but not by intramuscular injection.