CN1562060A - Haw leaf total flavone oral disintegration tablet and its preparing method - Google Patents
Haw leaf total flavone oral disintegration tablet and its preparing method Download PDFInfo
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- CN1562060A CN1562060A CN 200410022336 CN200410022336A CN1562060A CN 1562060 A CN1562060 A CN 1562060A CN 200410022336 CN200410022336 CN 200410022336 CN 200410022336 A CN200410022336 A CN 200410022336A CN 1562060 A CN1562060 A CN 1562060A
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- total flavones
- folium crataegi
- oral cavity
- ethanol
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- 229930003944 flavone Natural products 0.000 title claims abstract description 77
- 235000011949 flavones Nutrition 0.000 title claims abstract description 77
- GAMYVSCDDLXAQW-AOIWZFSPSA-N Thermopsosid Natural products O(C)c1c(O)ccc(C=2Oc3c(c(O)cc(O[C@H]4[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O4)c3)C(=O)C=2)c1 GAMYVSCDDLXAQW-AOIWZFSPSA-N 0.000 title claims abstract description 22
- VHBFFQKBGNRLFZ-UHFFFAOYSA-N vitamin p Natural products O1C2=CC=CC=C2C(=O)C=C1C1=CC=CC=C1 VHBFFQKBGNRLFZ-UHFFFAOYSA-N 0.000 title claims abstract description 22
- 150000002212 flavone derivatives Chemical class 0.000 title claims abstract description 20
- 238000000034 method Methods 0.000 title claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 24
- 239000000945 filler Substances 0.000 claims abstract description 8
- 238000002156 mixing Methods 0.000 claims abstract description 7
- 239000000314 lubricant Substances 0.000 claims abstract description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 72
- 150000002213 flavones Chemical class 0.000 claims description 55
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 36
- 210000000214 mouth Anatomy 0.000 claims description 25
- 239000000203 mixture Substances 0.000 claims description 23
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- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 18
- 238000005303 weighing Methods 0.000 claims description 18
- 239000002671 adjuvant Substances 0.000 claims description 17
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- 238000002360 preparation method Methods 0.000 claims description 16
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical group [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 12
- 239000000284 extract Substances 0.000 claims description 12
- 238000001914 filtration Methods 0.000 claims description 12
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 12
- 239000000243 solution Substances 0.000 claims description 12
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- 238000005325 percolation Methods 0.000 claims description 8
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- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical group OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 6
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- HIXDQWDOVZUNNA-UHFFFAOYSA-N 2-(3,4-dimethoxyphenyl)-5-hydroxy-7-methoxychromen-4-one Chemical compound C=1C(OC)=CC(O)=C(C(C=2)=O)C=1OC=2C1=CC=C(OC)C(OC)=C1 HIXDQWDOVZUNNA-UHFFFAOYSA-N 0.000 claims description 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 3
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 3
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- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 3
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- 229960002675 xylitol Drugs 0.000 claims description 3
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 2
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 claims description 2
- 241000167854 Bourreria succulenta Species 0.000 claims description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- 239000005434 MCC/mannitol excipient Substances 0.000 claims description 2
- 239000004952 Polyamide Substances 0.000 claims description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- 239000004376 Sucralose Substances 0.000 claims description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims description 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 2
- 235000010358 acesulfame potassium Nutrition 0.000 claims description 2
- 229960004998 acesulfame potassium Drugs 0.000 claims description 2
- 239000000619 acesulfame-K Substances 0.000 claims description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 2
- 235000019693 cherries Nutrition 0.000 claims description 2
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- 238000004132 cross linking Methods 0.000 claims description 2
- XMGQYMWWDOXHJM-UHFFFAOYSA-N limonene Chemical compound CC(=C)C1CCC(C)=CC1 XMGQYMWWDOXHJM-UHFFFAOYSA-N 0.000 claims description 2
- 239000007968 orange flavor Substances 0.000 claims description 2
- 229920002647 polyamide Polymers 0.000 claims description 2
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- 229940085605 saccharin sodium Drugs 0.000 claims description 2
- 239000000741 silica gel Substances 0.000 claims description 2
- 229910002027 silica gel Inorganic materials 0.000 claims description 2
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- 235000019408 sucralose Nutrition 0.000 claims description 2
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 2
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- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 5
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- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
An oral disintegrating tablet of the common flavone of haw leaf is prepared from said common flavone, filler, disintegrant, effervescent agent, lubricant and flavouring through proportionally mixing, and die pressing.
Description
Technical field:
The present invention relates to a kind of can be in the oral cavity rapidly disintegrate discharge the blood circulation promoting and blood stasis dispelling that has of medicine, the logical heart arteries and veins of a surname, the Folium Crataegi total flavones oral cavity disintegration tablet of network effect of relaxing of regulating the flow of vital energy, the present invention relates to the preparation method of said preparation simultaneously.
Background technology:
The Folium Crataegi of different cultivars all contains abundant flavonoid and other biological active component.The flavone compound general name Folium Crataegi total flavones that from the leaf of Fructus Crataegi, extracts, therefrom isolate 30 surplus kind of monomer, its preparation claims " Yixintong ".Studies show that for many years the flavone compound in the Folium Crataegi has many-sided pharmacological action, anti-angiocardiopathy is had good prospects for application.
At present, the oral Pharmaceutical dosage forms of Folium Crataegi total flavones extract has tablet, capsule, drop pill etc., and cardiovascular and cerebrovascular disease is had extensively definite therapeutical effect.This medicine reduces myocardial oxygen consumption on the one hand, and coronary blood flow increasing, blood viscosity lowering increase the myocardial nutrition blood supply on the one hand, and heart diseases due to myocardial ischemia and anoxia is had significant curative effect; Product are the cerebral blood flow increasing amount significantly, reduces the generation of lipid peroxide; Take Yixintong for a long time and can produce positive prevention and therapeutical effect, be subjected to extensive patients and medical worker's welcome coronary heart disease, angina pectoris, arrhythmia, cerebral arteriosclerosis, cerebral blood supply insufficiency, cerebral thrombosis, alzheimer disease and various brain injury sequela.
At present, although the existing various oral Pharmaceutical dosage forms of Folium Crataegi total flavones extract, existing dosage form is used concerning the old man that swallows certain difficulty and child neither be very convenient.For example: with regard to the tablet and capsule that are commonly used for oral formulations, old people that many swallows are more weak and child just are unwilling to take these solid dosage formss, and the complaint medicine is difficult to swallow or esophageall obstruetion.With regard to granule, except that its dysphagia, they also easily are stranded in the oral cavity, thereby in mouth, produce unhappy sensation, when taking above-mentioned oral formulations, also need drink water simultaneously, especially old man and child need take the problem that a large amount of water is just overcome dysphagia again, and still, too much drinking-water can influence old people and child's night's rest again.Therefore, up to the present, above-mentioned these conventional peroral dosage forms can't be considered to old man and the optimal dosage form of child.
In addition, the technology of existing Folium Crataegi total flavones preparation is comparatively backward, and the main active in the Folium Crataegi total flavones extract is embarrassed water-soluble total flavones, so these preparation ubiquity strippings are slow, and the phenomenon that bioavailability is low.
Summary of the invention:
It is slow that purpose of the present invention is intended to solve above-mentioned peroral dosage form stripping, bioavailability is low, the problem that is difficult for swallowing, the Folium Crataegi total flavones oral cavity disintegration tablet and the preparation method of disagreeable taste a kind of disintegrate rapidly are provided, discharge and covered, thereby the ease for use of raising Folium Crataegi total flavones oral formulations and the purpose of convenience reached.
Technical scheme of the present invention is as follows:
A kind of Folium Crataegi total flavones oral cavity disintegration tablet, it comprises the principal agent Folium Crataegi total flavones and the adjuvant for the treatment of effective dose, and wherein: the principal agent Folium Crataegi total flavones consumption for the treatment of effective dose is 20%～50% of prescription gross weight; The adjuvant of surplus be can be in the oral cavity rapidly disintegrate discharge the pharmaceutically acceptable excipient of medicine.
Described Folium Crataegi total flavones is obtained by percolation, decoction and alcohol sedimentation technique or resin absorption extraction method, wherein:
The specific embodiment of A, percolation is as follows:
Get Folium Crataegi, be ground into coarse powder, after the even moistening and airtight placement of adding ethanol, reinstall in the percolator, add ethanol, flood after 2～3 hours to soaking the medical material face, carry out percolation, collect the liquid of filtering, decompression recycling ethanol is to finite concentration, after the water gaging dilution such as adding, add petroleum ether and remove pigment, divide water-yielding stratum, extract with the ethyl acetate jolting, extracting solution reclaim under reduced pressure ethyl acetate and be concentrated into dried, total flavones.General flavone content is greater than 80%.
The specific embodiment of B, decoction and alcohol sedimentation technique is as follows:
Get Folium Crataegi, pulverize, add the water of 5 times of amounts, 0.4～0.6% aqueous slkali, 70～90 ℃ of heating are also slowly stirred, and extract 3 times.Merge extractive liquid,, concentrating under reduced pressure.After the concentrated solution cooling, adding 95% ethanol is 60～80% to containing the alcohol amount, and after-filtration is left standstill in cold preservation, after ethanol is reclaimed in the filtrate distillation, add the hot water dilution, leave standstill filtration, filtrate is extracted with the ethyl acetate jolting, extracting solution reclaim under reduced pressure ethyl acetate and be concentrated into dried, total flavones.General flavone content is greater than 80%.
The specific embodiment of C, resin absorption extraction method is as follows:
Get Folium Crataegi, be ground into coarse powder, with hot water or ethanol extraction, extracting solution is evaporated to dried, add water and stir, leave standstill filtration, filtrate is crossed macroporous adsorptive resins, with ethanol elution, behind the decompression recycling ethanol, be concentrated into dried, total flavones.Or be further purified with polyamide column, total flavones.General flavone content is greater than 90%.
Described pharmaceutically acceptable excipient comprises filler, disintegrating agent, effervescent, lubricant and correctives, and wherein filler is selected from microcrystalline Cellulose and mannitol or lactose, sorbitol, xylitol, sucrose, and its consumption is 30～60% of the prescription gross weight; Disintegrating agent is selected from carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone and low-substituted hydroxypropyl cellulose, and its consumption is 5%～15% of the prescription gross weight; Effervescent is selected from sodium bicarbonate or sodium carbonate and citric acid or tartaric acid, and its consumption is 0.1～5% of the prescription gross weight; Lubricant is magnesium stearate or micropowder silica gel, and its consumption is 0.5～2% of the prescription gross weight; Correctives is sweeting agent and essence, and consumption is 0.1～2% of the prescription gross weight.
Wherein the filler microcrystalline Cellulose also has the effect of disintegrating agent and binding agent concurrently.
Described sweeting agent is selected from aspartame, Sucralose, acesulfame potassium, saccharin sodium.
Described essence is selected from Herba Menthae essence, cherry essence, Fructus Citri tangerinae essence, orange flavor.
The preparation method of Folium Crataegi total flavones oral cavity disintegration tablet of the present invention, concrete processing step comprises raw material pulverizing, weighing mixing, granulation, tabletting or two kinds of approach of direct compression after raw material pulverizing, weighing, mixing:
Wherein: the 1st kind to make the preparation concrete steps of finished product through raw material pulverizing, weighing mixing, granulation, tabletting as follows:
Step 1: with Folium Crataegi total flavones and various adjuvant pulverize separately, cross 50～100 mesh sieves then, preserve standby respectively;
Step 2: take by weighing Folium Crataegi total flavones by recipe quantity, take by weighing filler and the disintegrating agent of partly measuring by accessory formula, and with its abundant mix homogeneously;
Step 3: with above-mentioned mixed uniformly component, granulate, then at oven dry below 60 ℃, granulate;
Step 4: in above-mentioned granule, add the disintegrating agent of surplus and other adjuvants in the accessory formula, fully mix homogeneously;
Step 5: the granule of above-mentioned mix homogeneously is sent into tablet machine, carry out tabletting.
The ratio that adds in the described disintegrating agent and add is 20%～80%.
The 2nd kind after raw material pulverizing, weighing, mixing direct compression to make the preparation concrete steps of finished product as follows:
Step 1: with Folium Crataegi total flavones and various adjuvant pulverize separately, cross 50～100 mesh sieves then, preserve standby respectively;
Step 2: take by weighing Folium Crataegi total flavones by recipe quantity, take by weighing various adjuvants by the prescription in the accessory formula, and with its abundant mix homogeneously;
Step 3: the component of above-mentioned mix homogeneously is sent into tablet machine, carry out tabletting and make finished product.
The hardness of Folium Crataegi total flavones oral cavity disintegration tablet finished product of the present invention is 15～40N.
The invention has the advantages that:
1, the present invention has overcome the shortcoming of disintegrating agent and the single effect of effervescent, has given full play to the synergy of the two, thereby obtains the good oral cavity disintegration tablet of disintegrating property.
Can not need the water assisting deglutition when 2, the present invention takes, just can become fine grained at intraorally rapidly disintegrating, only several swallowing acts can be finished drug administration process, have the patient of obstacle and the patient of old people or water intaking inconvenience to provide convenience to some medicines of swallowing.
3, enter gastrointestinal tract after the disintegrate of the present invention and disperse, extensively cover gastrointestinal mucosa rapidly, absorb soon, mouthfeel is good, bioavailability height, and taking convenience.
4, the present invention fills a prescription rationally, disintegrating property is good, inlet no grittiness and uncomfortable taste, preparation technology are easy, and utilizes conventional tablet production equipment in the pharmaceuticals industry to get final product economy and produce high-quality oral cavity disintegration tablet easily in enormous quantities.
The present invention has blood circulation promoting and blood stasis dispelling, the logical heart arteries and veins of a surname, the effect of the easypro network of regulating the flow of vital energy.
The specific embodiment
Embodiment one: percolation prepares the Folium Crataegi total flavones thing
Get Folium Crataegi, be ground into coarse powder, after the even moistening and airtight placement of adding ethanol, reinstall in the percolator, add ethanol, flood after 2～3 hours to soaking the medical material face, carry out percolation, collect the liquid of filtering, decompression recycling ethanol is to finite concentration, after the water gaging dilution such as adding, add petroleum ether and remove pigment, divide water-yielding stratum, extract with the ethyl acetate jolting, extracting solution reclaim under reduced pressure ethyl acetate and be concentrated into dried, total flavones.General flavone content is greater than 80%.
Embodiment two: decoction and alcohol sedimentation technique prepares the Folium Crataegi total flavones extract
Get Folium Crataegi, pulverize, add the water of 5 times of amounts, 0.4～0.6% aqueous slkali, 70～90 ℃ of heating are also slowly stirred, and extract 3 times.Merge extractive liquid,, concentrating under reduced pressure.After the concentrated solution cooling, adding 95% ethanol is 60～80% to containing the alcohol amount, and after-filtration is left standstill in cold preservation, after ethanol is reclaimed in the filtrate distillation, add the hot water dilution, leave standstill filtration, filtrate is extracted with the ethyl acetate jolting, extracting solution reclaim under reduced pressure ethyl acetate and be concentrated into dried, total flavones.General flavone content is greater than 80%.
Embodiment three: the resin absorption extraction method prepares the Folium Crataegi total flavones extract
Get Folium Crataegi, be ground into coarse powder, with hot water or ethanol extraction, extracting solution is evaporated to dried, add water and stir, leave standstill filtration, filtrate is crossed macroporous adsorptive resins, with ethanol elution, behind the decompression recycling ethanol, be concentrated into dried, total flavones.General flavone content is greater than 90%.
Embodiment four: the prescription test
Folium Crataegi total flavones 32.0g (general flavone content restrains greater than 80mg/)
Lactose 25.0g
Mannitol 10.0g
Microcrystalline Cellulose 20.0g
Low-substituted hydroxypropyl cellulose 3.0g
Crospolyvinylpyrrolidone 5.0g
Magnesium stearate 1.0g
Sodium bicarbonate 1.0g
Citric acid 1.0g
Aspartame 1.0g
Herba Menthae essence 1.0g
Make 1000 altogether
Preparation method: get above-mentioned each component, pulverize, cross 100 mesh sieves, take by weighing each component by above-mentioned recipe quantity, mix homogeneously is sent powder into conventional tablet machine then, carries out tabletting, and getting sheet heavily is the Folium Crataegi total flavones oral cavity disintegration tablet of 100mg.
Result of the test: tablet hardness: 15～40N
Disintegration: 20～50 seconds
Mouthfeel: no grittiness and uncomfortable taste, no foreign body sensation.
General flavone content: 25.9mg/ sheet.
[usage and consumption] is oral, one time 2～3
Embodiment five: the prescription test
Folium Crataegi total flavones 50.0g (general flavone content restrains greater than 80mg/)
Mannitol 10.0g
Microcrystalline Cellulose 20.0g
Low-substituted hydroxypropyl cellulose 3.0g
Crospolyvinylpyrrolidone 10.0g
Magnesium stearate 1.0g
Sodium bicarbonate 2.0g
Citric acid 2.0g
Aspartame 1.0g
Herba Menthae essence 1.0g
Make 1000 altogether
Preparation method:
Step 1: with Folium Crataegi total flavones and various adjuvant pulverize separately, cross 100 mesh sieves then, preserve standby respectively;
Step 2: take by weighing Folium Crataegi total flavones, mannitol and 75% recipe quantity microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone by recipe quantity, and with its abundant mix homogeneously;
Step 3: will add an amount of dehydrated alcohol in the component of above-mentioned mix homogeneously, and stir, make suitable soft material, granulate, under 50 ℃ temperature, dry granulate then;
Step 4: the disintegrating agent and other adjuvants in the prescription, the fully mix homogeneously that in above-mentioned granule, add surplus;
Step 5: the granule of above-mentioned mix homogeneously is sent into tablet machine, carry out tabletting.Getting sheet heavily is the Folium Crataegi total flavones oral cavity disintegration tablet of 100mg.
Result of the test: tablet hardness: 15～40N
Disintegration: 20～50 seconds
Mouthfeel: no grittiness and uncomfortable taste, no foreign body sensation.
General flavone content: 41.5mg/ sheet.
[usage and consumption] is oral, one time 2
Embodiment six: the prescription test
Folium Crataegi total flavones 64.0g (general flavone content restrains greater than 80mg/)
Lactose 70.0g
Xylitol 20.0g
Microcrystalline Cellulose 26.0g
Low-substituted hydroxypropyl cellulose 3.0g
Crospolyvinylpyrrolidone 7.0g
Sodium bicarbonate 2.0g
Citric acid 2.0g
Aspartame 2.0g
Herba Menthae essence 2.0g
Magnesium stearate 2.0g
Make 1000 altogether
Preparation method: step 1: with Folium Crataegi total flavones and various adjuvant pulverize separately, cross 100 mesh sieves then, preserve standby respectively;
Step 2: take by weighing Folium Crataegi total flavones, lactose, mannitol and 75% recipe quantity microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone by recipe quantity, and with its abundant mix homogeneously;
Step 3: will add an amount of water in the component of above-mentioned mix homogeneously, and stir, make suitable soft material, granulate, under 50 ℃ temperature, dry granulate then;
Step 4: the disintegrating agent and other adjuvants in the prescription, the fully mix homogeneously that in above-mentioned granule, add surplus;
Step 5: the granule of above-mentioned mix homogeneously is sent into tablet machine, carry out tabletting.Getting sheet heavily is the Folium Crataegi total flavones oral cavity disintegration tablet of 200mg.
Result of the test: tablet hardness: 15～40N
Disintegration: 20～50 seconds
Mouthfeel: no grittiness and uncomfortable taste, no foreign body sensation.
General flavone content: 53.6mg/ sheet.
[usage and consumption] is oral, one time 1
Embodiment seven: the prescription test
Folium Crataegi total flavones 32.0g (general flavone content restrains greater than 80mg/)
Lactose 58.0g
Mannitol 20.0g
Microcrystalline Cellulose 30.0g
Low-substituted hydroxypropyl cellulose 4.0g
Crospolyvinylpyrrolidone 8.0g
Magnesium stearate 2.0g
Sodium bicarbonate 1.5g
Citric acid 1.5g
Aspartame 1.5g
Herba Menthae essence 1.5g
Make 1000 altogether
Preparation method: take by weighing each component by above-mentioned recipe quantity, pulverize, mix homogeneously is crossed 100 mesh sieves then, and powder is sent into conventional tablet machine, carries out tabletting, and getting sheet heavily is the Folium Crataegi total flavones oral cavity disintegration tablet of 160mg.
Result of the test: tablet hardness: 15～40N
Disintegration: 10～40 seconds
Mouthfeel: no grittiness and uncomfortable taste, no foreign body sensation.
General flavone content: 26.7mg/ sheet
Claims (8)
1, a kind of Folium Crataegi total flavones oral cavity disintegration tablet, it comprises the principal agent Folium Crataegi total flavones and the adjuvant for the treatment of effective dose, and wherein: the principal agent Folium Crataegi total flavones consumption of treatment effective dose is 20%～50% of the prescription gross weight; The adjuvant of surplus be can be in the oral cavity rapidly disintegrate discharge the pharmaceutically acceptable excipient of medicine.
2, oral cavity disintegration tablet as claimed in claim 1 is characterized in that: described Folium Crataegi total flavones is obtained by percolation, decoction and alcohol sedimentation technique or resin absorption extraction method, wherein:
The specific embodiment of A, percolation is as follows:
Get Folium Crataegi, be ground into coarse powder, after the even moistening and airtight placement of adding ethanol, reinstall in the percolator, add ethanol, flood after 2～3 hours to soaking the medical material face, carry out percolation, collect the liquid of filtering, decompression recycling ethanol is to finite concentration, after the water gaging dilution such as adding, add petroleum ether and remove pigment, divide water-yielding stratum, extract with the ethyl acetate jolting, extracting solution reclaim under reduced pressure ethyl acetate and be concentrated into dried, total flavones.General flavone content is greater than 80%.
The specific embodiment of B, decoction and alcohol sedimentation technique is as follows:
Get Folium Crataegi, pulverize, add the water of 5 times of amounts, 0.4～0.6% aqueous slkali, 70～90 ℃ of heating are also slowly stirred, and extract 3 times.Merge extractive liquid,, concentrating under reduced pressure.After the concentrated solution cooling, adding 95% ethanol is 40～60% to containing the alcohol amount, and after-filtration is left standstill in cold preservation, after ethanol is reclaimed in the filtrate distillation, add the hot water dilution, leave standstill filtration, filtrate is extracted with the ethyl acetate jolting, extracting solution reclaim under reduced pressure ethyl acetate and be concentrated into dried, total flavones.General flavone content is greater than 80%.
The specific embodiment of C, resin absorption extraction method is as follows:
Get Folium Crataegi, be ground into coarse powder, with hot water or ethanol extraction, extracting solution is evaporated to dried, add water and stir, leave standstill filtration, filtrate is crossed macroporous adsorptive resins, with ethanol elution, behind the decompression recycling ethanol, be concentrated into dried, total flavones.Or be further purified with polyamide column, total flavones.General flavone content is greater than 90%.
3, oral cavity disintegration tablet as claimed in claim 1, it is characterized in that: described pharmaceutically acceptable excipient comprises filler, disintegrating agent, effervescent, lubricant and correctives, wherein filler is selected from microcrystalline Cellulose and mannitol or lactose, sorbitol, xylitol, sucrose, and its consumption is 30～60% of the prescription gross weight; Disintegrating agent is selected from carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone and low-substituted hydroxypropyl cellulose, and its consumption is 5%～25% of the prescription gross weight; Effervescent is selected from sodium bicarbonate or sodium carbonate and citric acid or tartaric acid, and its consumption is 0.1～5% of the prescription gross weight; Lubricant is magnesium stearate or micropowder silica gel, and its consumption is 0.5～2% of the prescription gross weight; Correctives is sweeting agent and essence, and consumption is 0.1～2% of the prescription gross weight.
4, as claim 1 or 3 described oral cavity disintegration tablets, it is characterized in that: described sweeting agent is selected from aspartame, Sucralose, acesulfame potassium, saccharin sodium.
5, as claim 1 or 3 described oral cavity disintegration tablets, it is characterized in that: described essence is selected from Herba Menthae essence, cherry essence, Fructus Citri tangerinae essence, orange flavor.
6, as claim 1 or 3 described oral cavity disintegration tablets, it is that direct compression makes finished product after the pulverizing of principal agent, adjuvant, weighing, mixing, and concrete processing step is as follows:
Step 1: with Folium Crataegi total flavones and various adjuvant pulverize separately, cross 50～100 mesh sieves then, preserve standby respectively;
Step 2: take by weighing Folium Crataegi total flavones by recipe quantity, take by weighing various adjuvants by the prescription in the accessory formula, and with its abundant mix homogeneously;
Step 3: the component of above-mentioned mix homogeneously is sent into tablet machine, carry out tabletting and make finished product.
7, as claim 1 or 3 described oral cavity disintegration tablets, comprise raw material pulverizing, weighing mixing, granulation, sheeting process, it is characterized in that: concrete processing step is as follows:
Step 1: with Folium Crataegi total flavones and various adjuvant pulverize separately, cross 50～100 mesh sieves then, preserve standby respectively;
Step 2: take by weighing Folium Crataegi total flavones by recipe quantity, take by weighing filler and the disintegrating agent of partly measuring by accessory formula, and with its abundant mix homogeneously;
Step 3: with above-mentioned mixed uniformly component, granulate, then at oven dry below 60 ℃, granulate;
Step 4: in above-mentioned granule, add the disintegrating agent of surplus and other adjuvants in the accessory formula, fully mix homogeneously;
Step 5: the granule of above-mentioned mix homogeneously is sent into tablet machine, carry out tabletting.
8, the preparation method of Folium Crataegi total flavones oral cavity disintegration tablet according to claim 7 is characterized in that: add in the described disintegrating agent and the ratio that adds is 20%～80%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410022336 CN1562060A (en) | 2004-04-19 | 2004-04-19 | Haw leaf total flavone oral disintegration tablet and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410022336 CN1562060A (en) | 2004-04-19 | 2004-04-19 | Haw leaf total flavone oral disintegration tablet and its preparing method |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103735667A (en) * | 2014-02-12 | 2014-04-23 | 沈阳药科大学 | Method for preparing total triterpenoid saponin and total flavonoids from Chinese hawthorn leaves |
| CN106923023A (en) * | 2017-04-21 | 2017-07-07 | 安徽省领航动物保健品有限责任公司 | A kind of optimization processing acorn nut powder prepares hog grower feed auxiliary material |
| CN110063398A (en) * | 2019-04-24 | 2019-07-30 | 河北科技师范学院 | A kind of hawthorn polyphenol tabletting and preparation method thereof of anti-UVB radiation |
-
2004
- 2004-04-19 CN CN 200410022336 patent/CN1562060A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103735667A (en) * | 2014-02-12 | 2014-04-23 | 沈阳药科大学 | Method for preparing total triterpenoid saponin and total flavonoids from Chinese hawthorn leaves |
| CN103735667B (en) * | 2014-02-12 | 2016-03-23 | 沈阳药科大学 | A kind of method preparing total triterpene saponins and total flavones from Folium Crataegi |
| CN106923023A (en) * | 2017-04-21 | 2017-07-07 | 安徽省领航动物保健品有限责任公司 | A kind of optimization processing acorn nut powder prepares hog grower feed auxiliary material |
| CN110063398A (en) * | 2019-04-24 | 2019-07-30 | 河北科技师范学院 | A kind of hawthorn polyphenol tabletting and preparation method thereof of anti-UVB radiation |
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