CN100577159C - Myricetin dispersion tablets for treating cardio-cerebral blood vessel diseases and preparation method thereof - Google Patents
Myricetin dispersion tablets for treating cardio-cerebral blood vessel diseases and preparation method thereof Download PDFInfo
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- CN100577159C CN100577159C CN200710034611A CN200710034611A CN100577159C CN 100577159 C CN100577159 C CN 100577159C CN 200710034611 A CN200710034611 A CN 200710034611A CN 200710034611 A CN200710034611 A CN 200710034611A CN 100577159 C CN100577159 C CN 100577159C
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Abstract
The present invention discloses a myricetin dispersion tablet for curing angiocardiopathy and cerebrovascular disease. Its composition contains (by weight portion) 100-200 portions of myricetin or myricetin containing 2% of borneol, 10-35 portions of cross-linked polyvinylpyrrolidone, 40-150 portions of microcrystal cellulose, 40-80 portions of alpha-lactose or 50-150 portions of pregelled starch, 10-35 portions of polyvinylpyrrolidone, 1-10 portions of sodium lauryl sulfate and 1-5 portions of magnesium stearate. Said invention also provides the preparation method of said dispersion tablet.
Description
Technical field
The present invention relates to a kind of medicine that is used to prevent and treat cardiovascular and cerebrovascular disease, also relate to the described preparation method that is used to prevent and treat the medicine of cardiovascular and cerebrovascular disease.
Background technology
The heart, cerebrovascular disease are the diseases of serious harm human health.(platelet activatingfactor is platelet aggregation activator the strongest known to so far and important inflammatory mediator PAF) to platelet activating factor, and it can act on the various kinds of cell receptor, produces biological effect widely.PAF participates in many pathophysiological change, and is closely related with all pathogenic processes oversensitive, cerebrovascular disease such as ischemia-reperfusion, inflammatory reaction, atherosclerosiss; The effect of antagonism PAF is to suppress thrombosis at present, improves multiple disturbance of blood circulation, the important channel of all oversensitive, cerebrovascular disease such as prevention and treatment coronary heart disease, atherosclerosis etc.Discover, rabbit platelet gathering, 5-HT that ampelopsin can suppress the PAF mediation discharge and the interior calcium ion concentration rising of platelet, thereby play the cardiovascular effect of protection, and experimental result shows that its anti-PAF effect is stronger than the effective ingredient S-A Hydroxysafflor yellow A effect of traditional blood-activating and stasis-removing Flos Carthami; Its mechanism of action is similar to the paf receptor antagonists Ginkgo total lactones, be a kind of new paf receptor antagonists, so ampelopsin can be used for preventing and treat coronary blood supply insufficiency due to arteriosclerosis and the hypertension, angina cordis, myocardial infarction, cerebral embolism, cerebral vasospasm and because of bad caused other illness of arteries blood supply.Since the sixties in last century, domestic and international many scholars have done a large amount of further investigations to ampelopsin extracting method and pharmacology, drug effect, the main at present extracting method that adopts has water or organic solvent extraction method, or the reuse adsorbent resin is made with extra care and is obtained behind water or organic solvent extraction, or extract and get with high-speed countercurrent chromatography, the ampelopsin product that obtains through enzyme process, alkali conversion method in addition in addition.
Medicine or health food that the external at present ampelopsin extract of producing is made are mainly conventional tablet, but because of the water solublity and the fat-soluble homogeneous phase of ampelopsin are on duty, absorb slowly in the body, bioavailability is very low, thereby onset is not ideal enough after the medication, has influenced the curative effect of existing tablet.Also have and once attempted ampelopsin is made drop pill, to improve infiltration rate in its dissolution rate and the body; But this dosage form is stable inadequately, and the long-term back of placing easily produces the medicine crystallize, catabiosis such as dissolution reduction, thus influenced the absorption of principal agent composition, its bioavailability is reduced.
Summary of the invention
The object of the present invention is to provide a kind of good absorbing, rapid-action, stay-in-grade, as to can be used for preventing or treating cardiovascular and cerebrovascular disease ampelopsin dispersible tablet.
Solution of the present invention is based on Chinese medicine to cardiovascular and cerebrovascular disease and pathogenetic understanding of complication and Therapeutic Principle, the invention of tracking modern pharmacological research, from plant class Chinese herbal medicine, extract ampelopsin with better anti thrombotic action, be equipped with special adjuvants such as crospolyvinylpyrrolidone, microcrystalline Cellulose, make the tablet formulation that is beneficial to absorption especially.
Another object of the present invention is to provide the preparation method of this ampelopsin dispersible tablet.
The ampelopsin dispersible tablet that is used for the treatment of cardiovascular and cerebrovascular disease provided by the invention, the parts by weight of forming are: the ampelopsin ampelopsin of 2% Borneolum Syntheticum (or contain) 100-200, crospolyvinylpyrrolidone 10-35, microcrystalline Cellulose 40-150, alpha-lactose 40-80 or pregelatinized Starch 50-150, polyvinylpyrrolidone 10-35, sodium lauryl sulphate 1-10, magnesium stearate 1-5, essence is an amount of.
Its preparation process comprises the step of following order:
(1) earlier ampelopsin and each adjuvant are crossed 100 mesh sieves respectively, take by weighing in ampelopsin and each by the prescription amount and add adjuvant, fully mixing.
(2) polyvinylpyrrolidone is made into 10% aqueous solution and makes wetting agent system soft material, 50 mesh sieves are granulated, and wet grain was in 50-80 ℃ of drying 2 hours.
(3) with 50 mesh sieve granulate, add the magnesium stearate that adds adjuvant and cross 80 mesh sieves, an amount of essence, mixing, tabletting promptly gets ampelopsin dispersible tablet of the present invention.
The preparation method that is used for the treatment of the ampelopsin dispersible tablet of cardiovascular and cerebrovascular disease provided by the invention, the adding method of microcrystalline Cellulose, alpha-lactose, pregelatinized Starch among its preparation technology adds in being, the adding method of crospolyvinylpyrrolidone adds 60%-90% in being, adds 10%-40%; The adding method of sodium lauryl sulphate, magnesium stearate and essence is for adding.
Ampelopsin dispersible tablet of the present invention is characterized in that every amount that contains principal agent composition ampelopsin is 100-200mg.
The principal agent composition of ampelopsin dispersible tablet of the present invention can be ampelopsin or the ampelopsin that contains 2% Borneolum Syntheticum.
The principal agent composition ampelopsin of ampelopsin dispersible tablet of the present invention can obtain like this:
Get Ampelopsis grossedentata or other Fructus Vitis viniferae material ampelopsis raw medicinal material water or alcohol-water boiling and extraction or reflux, extract,, extract one or many, filtered while hot; Merge extractive liquid, adds alkaline assistants such as sodium bicarbonate, sodium carbonate, through heated and boiled, conversion, concentrate, the crystallize process, again through alcohol-water recrystallization, purity is ampelopsin crystal more than 95%.
The advantage of ampelopsin dispersible tablet of the present invention has been to select for use and has helped ampelopsin and disperse fast and the specific quick-acting disintegrating agents of stripping and good excipient, making behind the product oral of making rapidly, disintegrate becomes homodisperse fine particle, thereby improve the principal agent dissolubility, the water solublity of solution ampelopsin and fat-soluble poor, absorb in the body slowly, the difficult problem that bioavailability is low, infiltration rate in the dissolution rate of raising principal agent ampelopsin and the body plays quick-acting effects efficiently; And this product taking convenience, rapid-action, stable quality after long time storage, the bioavailability height, its therapeutic effect is better than conventional tablet and drop pill, and diseases such as thromboembolia type cardio-cerebrovascular disorder and hyperlipidemia, coronary heart disease are had excellent prevention and therapeutic effect.
The specific embodiment
The present invention is further illustrated below in conjunction with the experiment of embodiment and main pharmacodynamics, but should be appreciated that these embodiment just illustrate the present invention, rather than in office where face limits the scope of the invention.
Embodiment 1
Ampelopsin 100g
Crospolyvinylpyrrolidone 13g (in add)
4g (adding)
Polyvinylpyrrolidone 15g
Microcrystalline Cellulose 57g
Alpha-lactose 57g
Sodium lauryl sulphate 5g (adding)
Magnesium stearate 1.3g (adding)
Essence an amount of (adding)
Make 1000 altogether
Took by weighing medicine and each adjuvant behind 100 mesh sieves by the prescription amount, with equivalent progressively increase method with medicine with in add the abundant mixing of adjuvant, grind.Add 10% the polyvinylpyrrolidone aqueous solution prepare, fully grind the system soft material.After the soft material that makes crossed the wet grain of 50 mesh sieve systems,, take out the back and cross 50 mesh sieves, add the magnesium stearate that adds adjuvant and cross 80 mesh sieves with granulate in 60 ℃ of baking oven inner dryings 2 hours, mixing, tabletting, quality inspection, packing, promptly.Every nearly weighs 250mg, contains ampelopsin 100mg/ sheet.
This product outward appearance yellow green, color and luster is even, and every index all meets " Chinese pharmacopoeia version pertinent regulations in 2005.
Usage and consumption: oral, each 1-2 sheet, 3 times on the one.
Storage: sealing, put shady and cool dry place.
Embodiment 2
Ampelopsin 100g
Borneolum Syntheticum 2g
Crospolyvinylpyrrolidone 12g (in add)
4g (adding)
Polyvinylpyrrolidone 15g
Microcrystalline Cellulose 58g
Pregelatinized Starch 57g
Sodium lauryl sulphate 4g (adding)
Magnesium stearate 1.2g (adding)
Essence an amount of (adding)
Make 1000 altogether
Its preparation process and method are with embodiment 1.
Every of this product nearly weighs 250mg, contains ampelopsin 100mg/ sheet, contains Borneolum Syntheticum 2mg/ sheet.The outward appearance yellow green, color and luster is even, and every index all meets " Chinese pharmacopoeia version pertinent regulations in 2005.
Usage and consumption: oral, each 1-2 sheet, 3 times on the one.
Storage: sealing, put shady and cool dry place.
Embodiment 3
Ampelopsin 200g
Polyvinylpyrrolidone 35g
Microcrystalline Cellulose 150g
Pregelatinized Starch 130g
Sodium lauryl sulphate 10g (adding)
Magnesium stearate 2.5g (adding)
Essence an amount of (adding)
Make 1000 altogether
Its preparation process and method are with embodiment 1.
Every of this product nearly weighs 0.5g, contains ampelopsin 200mg/ sheet.The outward appearance yellow green, color and luster is even, and every index all meets " Chinese pharmacopoeia version pertinent regulations in 2005.
Usage and consumption: oral, each 1,3 times on the one.
Storage: sealing, put shady and cool dry place.
Relevant pharmacodynamic experiment result is as follows for the principal agent composition of ampelopsin dispersible tablet of the present invention:
Laboratory animal: Kunming kind white mice, 18-22g; Wistar kind rat, body weight 100-135g.SPF level animal is provided credit number by Guangxi Medical University's Experimental Animal Center: SCXK osmanthus 2003-0003.Animal is indoor in air-conditioned laboratory animal by the sex sub-cage rearing, 22 ± 1 ℃ of room temperatures, 60 ± 5 ℃ of relative humiditys.Freely drink water and feed the standard particle feedstuff.
(1) ampelopsin dispersible tablet principal agent composition brings out the influence of chmice acute pulmonary infarction to ADP
Get 60 of mices, be divided into blank group (1%CMC 20ml/kg) at random, 1 group of ampelopsin and ampelopsin 2 groups (containing 2% Borneolum Syntheticum in the ampelopsin) divide large, medium and small dosage group (78.0mg/kg, 156.0mg/kg, 312mg/kg, addend drips and adds 1%CMC after tween 80 grinds to be made into suspension standby during preparation), aspirin (500mg/kg) group, 10 every group.Each group is all irritated the corresponding medicinal liquid of stomach.Every day 1 time, continuous 7d, 1h after the last administration, tail vein injection ADP normal saline solution 200mg/kg causes that platelet aggregation forms acute pulmonary embolism in the body respectively, and mice breathes dyspnea with rapid and short breath immediately, and hemiplegia is stiff.Recover the time of autonomic activities behind the record injection derivant to mice.
Table 1 ampelopsin dispersible tablet principal agent composition to ADP bring out the chmice acute pulmonary infarction influence (X ± S, N=10)
Annotate: compare with matched group: * P＜0.05; * P＜0.01; * * P＜0.001.
Experimental result shows, compare with matched group, on this model, 2 groups of 1 group of ampelopsin and ampelopsin and aspirin group all can obviously shorten the caused breathing dyspnea with rapid and short breath persistent period of the inductive platelet aggregation pulmonary infarction of ADP, the result shows, ampelopsin and the ampelopsin that contains 2% Borneolum Syntheticum demonstrate the stronger inductive platelet aggregation pulmonary infarction of inhibition ADP effect when little, middle dosage.
(2) ampelopsin dispersible tablet principal agent composition is to the thrombotic influence experiment of rat body angular vein
Get 70 of rats, male and female half and half, body weight 200-250g, be divided into blank group (1%CMC 20ml/kg) at random, 1 group of ampelopsin and ampelopsin 2 groups (containing 2% Borneolum Syntheticum in the ampelopsin) divide large, medium and small dosage group (78.0mg/kg, 156.0mg/kg, 312mg/kg, addend drips and adds 1%CMC after tween 80 grinds to be made into suspension standby during preparation), aspirin (500mg/kg) group, 8 every group.Each group is all irritated the corresponding medicinal liquid of stomach.Every day 1 time, continuous 7d, 1h after the last administration, rat is anaesthetized with 3% pentobarbital sodium intraperitoneal administration, cuts the about 3cm of skin in ventrimeson, separates postcava, in left renal vein below thick line ligation postcava, stitching stomach wall.Behind the 4h, reopen the abdominal cavity, folder stopped pipe chamber, 2cm place exhausts this section tube chamber inner blood below ligation, cuts tube chamber open, and removal of thromboses is placed on the filter paper, blots blood, takes by weighing wet weight of thrombus (mg) with micro-electronics Libra.With the thrombus weight is evaluation index, measures the influence of each administration group to venous thrombosis.
Table 2 ampelopsin dispersible tablet principal agent composition to the thrombotic influence of rat body angular vein (X ± S, N=8)
Annotate: compare with matched group: * P＜0.05; * P＜0.01; * * P＜0.001.
Experimental result shows, with matched group relatively, on this model, 2 groups of 1 group of ampelopsin and ampelopsin and aspirin group all can obviously reduce the rat suppository weight in wet base, wherein 2 groups of 1 group of ampelopsin and ampelopsin little, in, effect is all obvious when heavy dose of.
Above pharmacodynamic result shows, the effective ingredient ampelopsin of ampelopsin dispersible tablet of the present invention and the ampelopsin of 2% Borneolum Syntheticum in little, in, heavy dose of (78.0mg/kg, 156.0mg/kg, 312mg/kg) Shi Junneng obviously suppresses the inductive mouse platelets of ADP and assembles formed pulmonary infarction, obviously shortens the caused breathing dyspnea with rapid and short breath persistent period of the inductive platelet aggregation pulmonary infarction of ADP; The thrombotic pharmacodynamic experiment result of rat body angular vein shows that the effective ingredient of ampelopsin dispersible tablet of the present invention has the antibody angular vein thrombotic effect similar to aspirin.
Claims (7)
1. ampelopsin dispersible tablet, it is characterized in that the parts by weight of forming are: ampelopsin or contain the ampelopsin 100-200 of 2% Borneolum Syntheticum, crospolyvinylpyrrolidone 10-35, microcrystalline Cellulose 40-150, pregelatinized Starch 50-150, polyvinylpyrrolidone 10-35, sodium lauryl sulphate 1-10, magnesium stearate 1-5, essence is an amount of.
2. ampelopsin dispersible tablet as claimed in claim 1 is characterized in that: pregelatinized Starch 50-150 replaces with alpha-lactose 40-80.
3. ampelopsin dispersible tablet as claimed in claim 1 is characterized in that: every amount that contains principal agent composition ampelopsin is 100-200mg.
4. the preparation method of ampelopsin dispersible tablet as claimed in claim 1 is characterized in that adopting the step of following order:
(1) earlier ampelopsin and each adjuvant are crossed 100 mesh sieves respectively, take by weighing ampelopsin and 60-90% crospolyvinylpyrrolidone, microcrystalline Cellulose, alpha-lactose or pregelatinized Starch by the prescription amount, fully mixing;
(2) polyvinylpyrrolidone is made into 10% aqueous solution and makes wetting agent system soft material, 50 mesh sieves are granulated, and wet grain was in 50-80 ℃ of drying 2 hours;
(3) with 50 mesh sieve granulate, add 10-40% crospolyvinylpyrrolidone, sodium lauryl sulphate, reached the magnesium stearate of 80 mesh sieves, an amount of essence, mixing, tabletting promptly gets the ampelopsin dispersible tablet.
5. the preparation method of ampelopsin dispersible tablet as claimed in claim 4 is characterized in that the adding method of crospolyvinylpyrrolidone and amount are: in add 60%-90%, add 10%-40%.
6. the preparation method of ampelopsin dispersible tablet as claimed in claim 4 is characterized in that the adding method of microcrystalline Cellulose, alpha-lactose or pregelatinized Starch is: in add.
7. the preparation method of ampelopsin dispersible tablet as claimed in claim 4 is characterized in that the adding method of sodium lauryl sulphate, magnesium stearate and essence is: add.
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| CN200710034611A CN100577159C (en) | 2007-03-20 | 2007-03-20 | Myricetin dispersion tablets for treating cardio-cerebral blood vessel diseases and preparation method thereof |
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| CN102633762A (en) * | 2012-04-06 | 2012-08-15 | 昆明龙津药业股份有限公司 | Myricetin sulfonic acid compound and salt compound thereof and application of myricetin sulfonic acid and salt compound |
| CN103381152A (en) * | 2013-02-05 | 2013-11-06 | 吉林省金梓源生物科技有限公司 | Application of myricetin used as cathepsin K inhibitor |
| CN104127404A (en) * | 2014-07-08 | 2014-11-05 | 华侨大学 | Anti-depression drug and preparation method thereof |
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| Title |
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| 杨梅中活性成分杨梅素的研究进展. 唐霖等.中成药，第28卷第1期. 2006 |
| 杨梅中活性成分杨梅素的研究进展. 唐霖等.中成药，第28卷第1期. 2006 * |
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