CN1557824A - Silkworm excrement total alkaloid and its preparation method - Google Patents
Silkworm excrement total alkaloid and its preparation method Download PDFInfo
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Abstract
The present invention discloses one kind of total silkworm excrement alkaloid and its preparation process, medicine composition with the compound as active component, and the application of the medicine composition in preparing medicine for preventing and treating diabetes, obesity, hyperlipemia and viral infectious disease. The preparation process of total silkworm excrement alkaloid includes extracting silkworm excrement with solvent, decompression concentrating the concentrate, depositing with methanol or ethanol, cationic exchange resin purifying the supernatant, ammonia water washing, decolorizing with active carbon, drying and forming. All the total silkworm excrement and the composition adopts natural component as alpha-glycosidase inhibitor and has the features of clear mechanism, determined curative effect, low cost, etc.
Description
Technical field
The present invention relates to a kind of Chinese medicine total alkaloids, its preparation method and be the pharmaceutical composition of activeconstituents, and their application in the medicine of preparation prophylactic treatment diabetes, obesity, hyperlipidemia and disease of viral infection with this alkaloid.
Background technology
Silkworm excrement claims late silkworm excrement, silkworm dung, horse ring liver, late silkworm excrement, two silkworm excrements etc. again as traditional Chinese medicine, is the dry ight soil of Bombycidae insect bombyx mori (Bombyx mon L.) larva.The exsiccant silkworm excrement is the cylinder shape granule, and little have green grass gas, and look black, solid, evenly.Silkworm property is dry, nontoxic, the dry wind that can win dries, so silkworm excrement cures mainly the disease of rheumatism, therefore has the function of the analgesic therapy of dispelling rheumatism, invigorate blood circulation clinically, diseases such as dispelling the wind and dampness pathogens numbness pain, rubella itch, a wind headache, munbness, unsuccessful, the rapid vomiting and diarrhoea convulsion in joint, waist pin be cold gushes, marginal blepharitis eye.In addition, silkworm excrement also contains tannin and vitamins C, as astringent matter, diarrhoea, nosebleed, gingival hemorrhage and hemorrhoid hemorrhage etc. is all had good curative effect pharmaceutically; Pectin activity in the silkworm excrement is higher than other plant pectin (as apple pectin, citrus pectin etc.), and various pathogenic bacterium are had strong the inhibition and killing action, can prevent and treat the not normal disease of enteron aisle, and constipation is had significant curative effect.
Remove in the silkworm excrement after air-dry and contain 9.9% moisture content, 90.1% dry-matter (crude protein 13.6%, crude fat 3.7%, robust fibre 12.5%, nitrogen-free extract 48.7%, ash 12.6%) outside, also contain rich nutrient substances, wherein copper, iron, phosphorus, zinc and other micronutrient levelss are all higher; Contain 18 seed amino acids, comprise 8 kinds of needed by human, also contain abundant chlorophyll and derivative thereof, β-Hu Luobusu, pohytol, low-methoxy pectin and flavonoid compound in addition.
Part protein, carbohydrate and the lipoid material in the mulberry leaf of having nibbled the mulberry leaf post consumption, and most of effective ingredient with defecate to external, so the main component of silkworm excrement comes from mulberry leaf.The crude protein that contains in the silkworm excrement is higher than cereal grass, and chlorophyll, carotene are other green plants several times, even tens of times.
Chinese patent application numbers 99109111.6 disclose a kind of employing continuously or intermittently extraction method extract silkworm excrement, remove insolubles after filtration, filtrate merging further is condensed into paste and carries out the method for preparations shaping, be used for the treatment of and prevent diabetes.In addition, contain in the mulberry leaf 1-S-GI (deoxynojirimycin, DNJ), its chemistry 2R by name, 3R, 4R, 5S-2-methylol-3,4,5-trihydroxy-piperidines, this alkaloid is a kind of analog of natural sugar, has the inhibition activity of very high alpha-glucosidase, can be used for treating diseases such as diabetes, obesity, virus infection.Chinese patent application number 01113191.8 discloses " a kind of Chinese medical extract, Preparation Method And The Use with alpha-glucosidase inhibitor activity ", and this invention has related to by Chinese medicine White Mulberry Root-bark, mulberry leaf and mulberry fruit and prepared total alkaloids.
Summary of the invention
The purpose of this invention is to provide a kind of silkworm excrement total alkaloid with alpha-glucosidase inhibitor activity.
Second purpose of the present invention provides a kind of preparation method with silkworm excrement total alkaloid of alpha-glucosidase inhibitor activity.
The 3rd purpose of the present invention provides a kind of pharmaceutical composition that is used to prevent and treat diabetes, obesity, hyperlipidemia and disease of viral infection.
The 4th purpose of the present invention provides the application of a kind of silkworm excrement total alkaloid aspect the medicine of preparation prevention and treatment diabetes, obesity, hyperlipidemia and disease of viral infection.
Technical scheme of the present invention is summarized as follows:
A kind of preparation method of silkworm excrement total alkaloid, it comprises the steps:
(1) serve as to extract solvent with water or methyl alcohol or ethanol or aqueous alcohols, silkworm excrement is carried out cold soaking extracts or heating is extracted or refluxing extraction, the consumption of described extraction solvent is 5～15 times of silkworm excrement weight; Extraction time is 1～4 time, and united extraction liquid filters, and removes the dregs of a decoction;
(2) heating concentrating under reduced pressure extracting solution is to 1～2 times of silkworm shit volume;
(3) the adding volumn concentration is 75%～100% methyl alcohol or ethanol, and the amount of adding is 3～5 times of concentrated extracting solution, carries out the alcohol precipitation at 4 ℃～30 ℃; Centrifugal or filter, remove residue and insolubles;
(4) supernatant liquor of getting pure post precipitation carries out purifying through cation exchange resin column, with the non-adsorbable impurity of deionized water flush away, uses 0.2～1N ammoniacal liquor wash-out again, and elutriant is removed ammoniacal liquor through concentrating under reduced pressure;
(5) be that 1/10～1/100 gac of silkworm excrement weight decolours with consumption, collect destainer,, maybe will collect the direct spray drying forming of liquid and make dry powder, promptly get flaxen silkworm excrement total alkaloid through concentrating, becoming dry powder through vacuum-drying or lyophilize.
Extracting solvent is that 25～75% aqueous alcohols is good with volumn concentration.
Extracting method preferably heats extraction or refluxing extraction, and extracting temperature is 60～100 ℃.
The consumption that extracts solvent is that 10 times of silkworm excrement weight are advisable.
Extraction time preferably 2 times.
The concentration of elutriant ammoniacal liquor is 0.5N preferably.
Zeo-karb is the strong acid type resin of crosslinked polystyrene system preferably, and its model is 001 * 1.1 or 001 * 4 or 001 * 7 or 001 * 14.5 or Amberlite IR120 or Dowex 50 or Zerolit 225.
A kind of silkworm excrement total alkaloid, it prepares with following method:
(1) serve as to extract solvent with water or methyl alcohol or ethanol or aqueous alcohols, silkworm excrement is carried out cold soaking extracts or heating is extracted or refluxing extraction, the volumetric usage of described extraction solvent is 5～15 times of silkworm excrement weight; Extraction time is 1～4 time, and united extraction liquid filters, and removes the dregs of a decoction;
(2) heating concentrating under reduced pressure extracting solution is to 1～2 times of silkworm shit volume;
(3) the adding volumn concentration is 75%～100% methyl alcohol or ethanol, and the amount of adding is 3～5 times of concentrated extracting solution, carries out the alcohol precipitation at 4 ℃～30 ℃; Centrifugal or filter, remove residue and insolubles;
(4) supernatant liquor of getting pure post precipitation carries out purifying through cation exchange resin column, with the non-adsorbable impurity of deionized water flush away, uses 0.2～1N ammoniacal liquor wash-out again, and elutriant is removed ammoniacal liquor through concentrating under reduced pressure;
(5) be that 1/10～1/100 gac of silkworm excrement weight decolours with consumption, collect destainer, through concentrate, vacuum-drying or lyophilize become dry powder, maybe will collect the direct spray drying forming of liquid and make dry powder, promptly gets flaxen silkworm excrement total alkaloid.
Extracting solvent is that 25～75% aqueous alcohols is good with volumn concentration.
Extracting method preferably heats extraction or refluxing extraction, and extracting temperature is 60～100 ℃.
The consumption that extracts solvent is that 10 times of silkworm excrement weight are advisable.
Extraction time preferably 2 times.
The concentration of elutriant ammoniacal liquor is 0.5N preferably.
Zeo-karb is the strong acid type resin of crosslinked polystyrene system preferably, and its model is 001 * 1.1 or 001 * 4 or 001 * 7 or 001 * 14.5 or Amberlite IR120 or Dowex 50 or Zerolit 225.
Be used to prevent and treat diabetes, obesity, hyperlipidemia, and the pharmaceutical composition of disease of viral infection, wherein contain the treatment effective amount of actives, and contain one or more pharmaceutically acceptable carriers.
A kind of silkworm excrement total alkaloid of the present invention and pharmaceutical composition can be used for preparing in the medicine of prevention and treatment diabetes, obesity, hyperlipidemia and disease of viral infection.
Above described pharmaceutically acceptable carrier be meant the pharmaceutical carrier of pharmaceutical field routine, for example: thinner such as lactose, starch, dextrin, microcrystalline cellulose; Weighting agent such as starch; Tackiness agent such as derivatived cellulose, gelatin and polyvinylpyrrolidone; Wetting agent such as glycerine; Disintegrating agent such as dry starch, sodium starch glycolate, sodium alginate, sodium bicarbonate and carbide of calcium etc.; Correctives such as lactose, sweet Stevia element, D-wood sugar, Xylitol etc.; Lubricant such as talcum powder, calcium stearate and Magnesium Stearate etc.; Sanitas such as phenylformic acid, phenylcarbinol etc.
A kind of silkworm excrement total alkaloid of the present invention can composition the mode of form by oral administration be applied to the patient who needs this treatment.Composition can be made conventional solid preparation such as tablet, powder, capsule, pill etc., make liquid preparation such as syrup.
The various formulations of pharmaceutical composition of the present invention can be according to the conventional production method preparation of pharmaceutical field.For example a kind of silkworm excrement total alkaloid is mixed with one or more pharmaceutical carriers, be made into required formulation then.
It is a kind of silkworm excrement total alkaloid of 1～99% that pharmaceutical composition of the present invention preferably contains weight ratio, most preferably contains weight ratio and be a kind of silkworm excrement total alkaloid of 10～80%.
The usage quantity of a kind of silkworm excrement total alkaloid of the present invention can be according to the type and the severity situation of patient age, body weight, the disease of being treated, and its 24 hours dosage can be 0.1～10mg/kg body weight.
A kind of silkworm excrement total alkaloid of the present invention extracts from silkworm excrement, some effective ingredients in the mulberry leaf have been concentrated after nibbling mulberry leaf, the particle diameter of silkworm excrement is in the most suitable particle size range of extraction process, therefore, can be easily raw material extracts to extracting, separation and purifying, and obtain the various effective ingredients in the mulberry leaf; Silkworm excrement cheap, wherein total alkaloid contents is higher, is mainly the DNJ Alkaloid with alpha-glucosidase inhibitor activity.Silkworm excrement total alkaloid and composition thereof, all adopt natural component as alpha-glucosidase inhibitor, have that the mechanism of action is clear, characteristics such as determined curative effect, cost are low, can be used for prevention and treatment of diseases such as diabetes, obesity, hyperlipidemia and virus infection.
Description of drawings
Fig. 1 suppresses graphic representation for a kind of silkworm excrement total alkaloid of the present invention;
Fig. 2 is the high-efficient liquid phase chromatogram of a kind of silkworm excrement total alkaloid of the present invention.
Embodiment
The present invention is further illustrated below in conjunction with specific embodiment, but do not limit the present invention in any way.
A kind of preparation method of silkworm excrement total alkaloid: (1) gets silkworm excrement 1kg, adds volumn concentration and be 50% ethanol 10L, and 75 ℃ of insulations 5 hours are filtered, and filter residue adds 50% ethanol 10L again, and 75 ℃ of insulations 5 hours are filtered, and merge filtrate twice, the centrifugal dregs of a decoction of removing; (2) heating concentrating under reduced pressure extracting solution is to 2L; (3) the adding volumn concentration is 95% methyl alcohol, and the amount 6L of adding carries out alcohol precipitation, suction filtration at 4 ℃～10 ℃; (4) get the strong acid type resin of the supernatant liquor of pure post precipitation through cation exchange resin column crosslinked polystyrene system, its model is 001 * 1.1 to carry out purifying, with the non-adsorbable impurity of deionized water flush away, with 0.5N ammonia soln wash-out, the positive part elution peak of collection of biological alkali, decolour through the 10g charcoal absorption again, concentrating under reduced pressure, centrifugal, lyophilize, get the faint yellow extract powder of 7.86g, adopting the determination of acid-basetitration total alkaloid content is 64%.
Alkaloidal acid base titration: getting above-mentioned dry powder 0.5 gram, be dissolved in the 20ml glacial acetic acid, is titrating solution with 0.1N perchloric acid, is indicator with Viola crystallina, records wherein N atom equivalents.Getting above-mentioned dry powder 0.5 gram again, be dissolved in the 20ml water, is titrating solution with 0.1N NaOH, records wherein carboxylate radical equivalents.N atom equivalents deducts the carboxylate radical equivalents and should be alkaloidal mole number, and the alkaloid molecular weight is in 180, and the alkaloid weight of calculating should be not less than 30% of gross weight.
Formula: alkaloid=[perchloric acid volume (mL)-NaOH volume (mL)] * 0.036 * 100%
A kind of preparation method of silkworm excrement total alkaloid: (1) gets silkworm excrement 1kg, and adding volumn concentration is 75% ethanol 10L, 100 ℃ of reflux 2 hours, filter, filter residue adds 75% ethanol 10L again, continues to reflux 2 hours, filter, merge filtrate twice, the centrifugal dregs of a decoction of removing; (2) heating concentrating under reduced pressure extracting solution is to 2L; (3) adding 8L volumn concentration is 75% ethanol, carries out the alcohol precipitation at 20 ℃～30 ℃; Centrifugal or filter, remove residue and insolubles; (4) get the strong acid type resin of the supernatant liquor of pure post precipitation through cation exchange resin column crosslinked polystyrene system, its model 001 * 7 is carried out purifying, with the non-adsorbable impurity of deionized water flush away, uses 0.5N ammoniacal liquor wash-out again, and elutriant is removed ammoniacal liquor through concentrating under reduced pressure; (5) decolour with the 20g gac, will collect the liquid spray drying forming and make dry powder, promptly get flaxen silkworm excrement total alkaloid.
A kind of preparation method of silkworm excrement total alkaloid: (1) gets silkworm excrement 1kg, and adding volumn concentration is 25% methyl alcohol 25L, and 60 ℃ are incubated 5 hours, filter, and filter residue repeats to extract 2 times again, filters merging filtrate, the centrifugal dregs of a decoction of removing; (2) heating concentrating under reduced pressure extracting solution is to 2L; (3) ethanol of adding 10L carries out the alcohol precipitation at 25 ℃～30 ℃; Centrifugal or filter, remove residue and insolubles; (4) supernatant liquor of getting pure post precipitation carries out purifying through the resin Dowex 50 of cation exchange resin column polystyrene, with the non-adsorbable impurity of deionized water flush away, uses 1N ammoniacal liquor wash-out again, and elutriant is removed ammoniacal liquor through concentrating under reduced pressure; (5) decolour with the 50g gac,, promptly get flaxen silkworm excrement total alkaloid through concentrating, becoming dry powder through lyophilize.
Embodiment 4
A kind of preparation side of silkworm excrement total alkaloid: (1) gets silkworm excrement 1kg, adds 13L water, and soak at room temperature extracts 2 times, each 24 hours, filters merging filtrate, the centrifugal dregs of a decoction of removing; (2) heating concentrating under reduced pressure extracting solution is to 3L; (3) 12L methyl alcohol carries out the alcohol precipitation at 25 ℃～28 ℃; Centrifugal or filter, remove residue and insolubles; (4) supernatant liquor of getting pure post precipitation is through the strong acid type resin of cation exchange resin column crosslinked polystyrene system, and its model is 001 * 4 to carry out purifying, with the non-adsorbable impurity of deionized water flush away, uses 0.5N ammoniacal liquor wash-out again, and elutriant is removed ammoniacal liquor through concentrating under reduced pressure; (5) decolour with the 10g gac,, promptly get flaxen silkworm excrement total alkaloid through concentrating, becoming dry powder through lyophilize.
A kind of preparation method of silkworm excrement total alkaloid: (1) gets silkworm excrement 1kg, adds 5L methyl alcohol, and 80 ℃ of heating and refluxing extraction 4 times each 5 hours, are filtered merging filtrate, the centrifugal dregs of a decoction of removing; (2) heating concentrating under reduced pressure extracting solution is to 3L; Centrifugal or filter, remove residue and insolubles; (3) get the strong acid type resin of supernatant liquor through cation exchange resin column crosslinked polystyrene system, Amberlite IR120 carries out purifying, with the non-adsorbable impurity of deionized water flush away, uses 0.5N ammoniacal liquor wash-out again, and elutriant is removed ammoniacal liquor through concentrating under reduced pressure; (5) gac with 100g decolours, and through concentrating, becoming dry powder through lyophilize, promptly gets flaxen silkworm excrement total alkaloid.
A kind of preparation method of silkworm excrement total alkaloid: implementation step is with embodiment 5, and resin column wherein is the strong acid type resin of crosslinked polystyrene system, and its model is 001 * 14.5.
Embodiment 7
A kind of preparation method of silkworm excrement total alkaloid: implementation step is with embodiment 5, and resin column wherein is the strong acid type resin of crosslinked polystyrene system, and its model is Zerolit 225.
Embodiment 8
A kind of alpha-glycosidase of silkworm excrement total alkaloid suppresses experiment:
Get the male Wister rat (1) of body weight 120～140g, get small intestine after the execution, peel off mesentery, with content in physiological buffer (PBS) the flushing intestines of precooling.Shred the back as in the homogenizer, add 30ml PBS and grind, 4 ℃, 10,000 rev/mins, centrifugal 10 minutes, get supernatant liquor and get rat small intestine alpha-glycosidase crude enzyme liquid.
Get the acarbose, DNJ standard substance of 10ng～1mg/ml different concns respectively and by each 200 μ l of PBS solution of the prepared silkworm excrement total alkaloid of experimental example 1, add above-mentioned alpha-glycosidase crude enzyme liquid 100 μ l, 10mg/ml maltose solution 100 μ l, be mixed, 37 ℃ of incubations 20 minutes, 2 minutes termination reactions of boiling water bath.The cooling back burst size of determination of glucose oxidase glucose.With sample concentration (mg/ml) is X-coordinate, the absorbancy (OD of 490nm
490nm) draw the inhibition curve of Glycosylase for ordinate zou mapping.As shown in Figure 1, with the alpha-glucoside inhibiting activity IC of the silkworm excrement total alkaloid of this method preparation
50Be 10～30 μ g/ml.
The content determination of glucose (glucose oxidase method): get testing sample 10 μ l and use (glucose oxidase enzyme reagent kit, time spent preparation) in the working fluid in 200 μ l glucose assays, 37 ℃ were reacted 15 minutes, measured its absorbancy in the 490nm place.(under the effect of glucose oxidase, glucose at first is oxidized to gluconic acid and H
2O
2, H
2O
2The catalysis peroxidase synthesizes red quinonimine with 4-aminoantipyrene and phenol, and at the 490nm place maximum absorption is arranged.)
Embodiment 9
With the mensuration of high performance liquid chromatography to a kind of silkworm excrement total alkaloid:
Get a kind of silkworm excrement total alkaloid 1mg that DNJ standard substance or embodiment produce, be dissolved in respectively in the 20mmol/L NaOH solution, adopt Tianjin, island LC-10AT high performance liquid chromatograph to analyze.Chromatographic condition: CarboPac PAl (250 * 4mm) posts; Moving phase, 20mmol/L NaOH; Flow velocity, 0.5ml/ minute; Adopt the ED40 detector; Sample size 10 μ l.Analytical results shows, silkworm excrement total alkaloid elution peak occurs with DNJ standard substance in identical retention time 3.3 minutes, proves and contains DNJ composition (Fig. 2) in the silkworm excrement total alkaloid.
Embodiment 10:
A kind of silkworm excrement total alkaloid is to the influence of normal mouse postprandial blood sugar
Choose 18～22g male mice in kunming, it is divided into positive control group (acarbose), blank group (physiological saline) and administration group (silkworm excrement total alkaloid) at random by body weight, and every group each 9, (24 ± 1 ℃) feed under the constant temperature, raise with standard feed, freely drink water.Water is can't help in the 16h fasting before the test, gets certain density silkworm excrement total alkaloid, acarbose respectively, and physiological saline irritates stomach to normal mouse, irritates stomach starch (3g/kg) simultaneously.After administration 0,30,60,90,120 minutes tail vein bloods, and be collected in the centrifuge tube that contains a certain amount of heparin sodium centrifugal 10 minutes of 3000rpm, get supernatant,, investigate the influence of silkworm excrement total alkaloid the normal mouse sugar tolerance with the determination of glucose oxidase plasma glucose levels.The result is as shown in table 1, and silkworm excrement total alkaloid can obviously reduce the level of postprandial blood sugar of normal mouse on the level of 0.5～2.0mg/kg, and can delay the time on blood sugar peak.Administration is in the time of 30,60 minutes, and the administration group is compared with control group, and there were significant differences for blood glucose value (p＜0.01).
Table 1 silkworm excrement total alkaloid is to the influence of normal mouse sugar tolerance
(unit: mmol/L)
| Administration time | ????min | 0??????????????30?????????????60?????????????90????????????120 |
| Dosage | ????mg/kg | |
| Blank group acarbose silkworm excrement total alkaloid | ????0.0 ????3.0 ????2.0 ????1.0 ????0.5 | 8.20±1.75?????14.07±1.89????13.51±3.13????11.62±2.3????9.86±2.23 6.90±2.15?????9.86±1.68 **??10.32±3.12 **?8.17±1.56 **?6.93±2.14 **7.00±l.25?????9.464±2.20 **?8.19±1.96 **??7.85±1.24 **?6.58±1.09 **7.79±0.93?????10.50±2.35 **?9.76±2.80 **??8.44±1.05 **?7.55±0.79 **8.13±1.79?????11.50±3.06 **?11.40±3.00 **?9.87±1.68 *??8.32±1.58 * |
Compare with negative control group,
*, p＜0.05;
*, p＜0.01; (n=9)
Embodiment 11
A kind of silkworm excrement total alkaloid is to the influence of tissue of experimental diabetic mice postprandial blood sugar
Choose 18～22g male mice in kunming, (24 ± 1 ℃) raise with standard feed under the constant temperature, freely drink water.After water is can't help in the 18h fasting, press 200mg/kg body weight abdominal injection tetraoxypyrimidine (2.5% normal saline solution), the control group intraperitoneal injection of saline.The tail vein is got blood behind the 48h, and the plasma glucose levels behind the mensuration fasting 12h is decided to be the diabetes model mouse with the mouse of blood glucose value more than 11mmol/L.Diabetic mice is divided into 3 groups at random, and every group each 7, the difference of each treated animal average blood sugar value is not more than 0.5mmol/L, establishes negative control group, positive controls (acarbose), the experimental group of diabetes model respectively.Other gets 7 of normal mouses, is made as normal blank group.Water is can't help in the 16h fasting before the test, gets acarbose contrast solution (3mg/kg) or silkworm excrement alkaloid (2mg/kg) and a certain amount of starch (3g/kg) and irritates stomach for simultaneously tetraoxypyrimidine inductive tissue of experimental diabetic mice.After administration 0,30,60,90,120 minutes tail vein bloods with the determination of glucose oxidase plasma glucose levels, are investigated the influence of silkworm excrement alkaloid to the diabetic mice sugar tolerance respectively.The result is as shown in table 2, and silkworm excrement total alkaloid can significantly delay the time on blood sugar peak, and reduces the postprandial hyperglycemia level of diabetic mice, and administration is after 30 minutes, and the administration group is compared with the diabetes negative control group, and there were significant differences for blood glucose value (p＜0.01).
Table 2 silkworm excrement total alkaloid is to the influence of tissue of experimental diabetic mice postprandial blood sugar
(unit: mmol/L)
| Administration time | ????min | ?0????????????30?????????????60???????????90???????????120 |
| Dosage | ????mg/kg | |
| Blank group negative control group acarbose silkworm excrement total alkaloid | ????0.0 ????0.0 ????3.0 ????2.0 | ?8.20±1.75???14.07±1.89????13.51±3.13??11.62±2.3???9.86±2.23 ?14.52±3.39??23.41±4.17????19.53±3.34??16.60±2.28??15.12±2.89 ?13.99±3.53??17.31±3.38 **?20.48±4.14??16.52±3.48??15.60±2.95 ?14.49±2.93??17.93±4.43 **?21.34±3.37??17.52±3.53??15.61±3.72 |
Compare with negative control group,
*, p＜0.05;
*, p＜0.01; (n=7)
Embodiment 12
Tablet: a kind of silkworm excrement total alkaloid 100mg
Lactose 1800mg
W-Gum 580mg
Magnesium Stearate 20mg
The preparation method: a kind of silkworm excrement total alkaloid, lactose and starch are mixed, and water is evenly moistening, the mixture after moistening sieve, drying, after sieve, add Magnesium Stearate, then with the mixture compressing tablet, the heavy 250mg of sheet, active component content is 10mg.
Embodiment 13
Capsule: a kind of silkworm excrement total alkaloid 100mg
Lactose 1870mg
Magnesium Stearate 30mg
The preparation method: a kind of silkworm excrement total alkaloid, lactose and Magnesium Stearate are mixed, sieve, the mixture hard gelatin capsule of packing into, the heavy 200mg of each capsule, active component content is 10mg.
Claims (10)
1, a kind of preparation method of silkworm excrement total alkaloid is characterized in that it comprises the steps:
(1) serve as to extract solvent with water or methyl alcohol or ethanol or aqueous alcohols, silkworm excrement is carried out cold soaking extracts or heating is extracted or refluxing extraction, the volume of described extraction solvent is 5～15 times of silkworm excrement weight; Extraction time is 1～4 time, and united extraction liquid filters, and removes the dregs of a decoction;
(2) heating concentrating under reduced pressure extracting solution is to 1～2 times of silkworm shit volume;
(3) the adding volumn concentration is 75%～100% methyl alcohol or ethanol, and the amount of adding is 3～5 times of concentrated extracting solution, carries out the alcohol precipitation at 4 ℃～30 ℃; Centrifugal or filter, remove residue and insolubles;
(4) supernatant liquor of getting pure post precipitation carries out purifying through cation exchange resin column, with the non-adsorbable impurity of deionized water flush away, uses 0.2～1N ammoniacal liquor wash-out again, and elutriant is removed ammoniacal liquor through concentrating under reduced pressure;
(5) be that 1/10～1/100 gac of silkworm excrement weight decolours with consumption, collect destainer,, maybe will collect the direct spray drying forming of liquid and make dry powder, promptly get flaxen silkworm excrement total alkaloid through concentrating, becoming dry powder through vacuum-drying or lyophilize.
2. the preparation method of a kind of silkworm excrement total alkaloid according to claim 1 is characterized in that described extraction solvent is the aqueous alcohols of volumn concentration 25～75%.
3. the preparation method of a kind of silkworm excrement total alkaloid according to claim 1 is characterized in that extracting method is that heating is extracted or refluxing extraction, and extracting temperature is 60～100 ℃.
4. the preparation method of a kind of silkworm excrement total alkaloid according to claim 1, the volume that it is characterized in that described extraction solvent is 10 times of silkworm excrement weight.
5. the preparation method of a kind of silkworm excrement total alkaloid according to claim 1 is characterized in that described extraction time is 2 times.
6. the preparation method of a kind of silkworm excrement total alkaloid according to claim 1, the concentration that it is characterized in that described elutriant ammoniacal liquor is 0.5N.
7. the preparation method of a kind of silkworm excrement total alkaloid according to claim 1, it is characterized in that described Zeo-karb is the strong acid type resin of crosslinked polystyrene system, its model is 001 * 1.1 or 001 * 4 or 001 * 7 or 001 * 14.5 or Amberlite IR120 or Dowex 50 or Zerolit 225.
8. silkworm excrement total alkaloid is characterized in that through the preparation method of a kind of silkworm excrement total alkaloid of one of claim 1 to 7 prepared.
9. be used to prevent and treat diabetes, obesity, hyperlipidemia, and the pharmaceutical composition of disease of viral infection, wherein contain a kind of silkworm excrement total alkaloid and the pharmaceutically acceptable carrier of the claim 8 for the treatment of significant quantity.
10. the application of a kind of silkworm excrement total alkaloid of claim 8 in the medicine of preparation prevention and treatment diabetes, obesity, hyperlipidemia and disease of viral infection.
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| CNA2004100186581A CN1557824A (en) | 2004-02-13 | 2004-02-13 | Silkworm excrement total alkaloid and its preparation method |
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| CN1557824A true CN1557824A (en) | 2004-12-29 |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100372544C (en) * | 2005-12-09 | 2008-03-05 | 南开大学 | Silkworm sand total alkaloid and preparation thereof |
| WO2009100605A1 (en) * | 2008-01-30 | 2009-08-20 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd | A pharmaceutical composition for treating diabetes and preparation methods thereof |
| CN103536649A (en) * | 2013-10-17 | 2014-01-29 | 漳州片仔癀药业股份有限公司 | Preparation method of Jintangning capsules |
| CN105769923A (en) * | 2016-05-27 | 2016-07-20 | 厦门市医药研究所 | Bombyx mori extract and extraction method and application thereof |
| CN109007145A (en) * | 2018-07-26 | 2018-12-18 | 佛山科学技术学院 | A kind of preparation method of multiple-effect health-care black tea beverage |
-
2004
- 2004-02-13 CN CNA2004100186581A patent/CN1557824A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100372544C (en) * | 2005-12-09 | 2008-03-05 | 南开大学 | Silkworm sand total alkaloid and preparation thereof |
| WO2009100605A1 (en) * | 2008-01-30 | 2009-08-20 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd | A pharmaceutical composition for treating diabetes and preparation methods thereof |
| GB2469220A (en) * | 2008-01-30 | 2010-10-06 | Zhangzhou Pien Tze Huang Pharm | A pharmaceutical composition for treating diabetes and preparation methods thereof |
| GB2469220B (en) * | 2008-01-30 | 2012-10-24 | Zhangzhou Pien Tze Huang Pharm | Pharmaceutical composition for treating diabetes and preparation method thereof |
| CN103536649A (en) * | 2013-10-17 | 2014-01-29 | 漳州片仔癀药业股份有限公司 | Preparation method of Jintangning capsules |
| CN105769923A (en) * | 2016-05-27 | 2016-07-20 | 厦门市医药研究所 | Bombyx mori extract and extraction method and application thereof |
| CN109007145A (en) * | 2018-07-26 | 2018-12-18 | 佛山科学技术学院 | A kind of preparation method of multiple-effect health-care black tea beverage |
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