CN1586589A - Ginseng stem and leaf total saponin oral disintegration tablet and its preparing method - Google Patents

Ginseng stem and leaf total saponin oral disintegration tablet and its preparing method Download PDF

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Publication number
CN1586589A
CN1586589A CN 200410069353 CN200410069353A CN1586589A CN 1586589 A CN1586589 A CN 1586589A CN 200410069353 CN200410069353 CN 200410069353 CN 200410069353 A CN200410069353 A CN 200410069353A CN 1586589 A CN1586589 A CN 1586589A
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Prior art keywords
stem
leaf
radix ginseng
total saponins
essence
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CN 200410069353
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Chinese (zh)
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CN1283267C (en
Inventor
蒋海松
王红喜
王锦刚
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Beijing Kexin Bicheng Medicine Technology Development Co Ltd
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Beijing Kexin Bicheng Medicine Technology Development Co Ltd
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Publication of CN1283267C publication Critical patent/CN1283267C/en
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Abstract

The present invention relates to oral disintegrated tablet of ginseng stem and leaf total ginsenoside for invigorating spleen and nourishing vital energy and its preparation process. Ginseng stem and leaf total ginsenoside as main material as well as stuffing, disintegrating agent, corrective, flow assistant, lubricant and other supplementary material are prepared into the oral disintegrated tablet. Into the supplementary material, adhesive, coating material and/or effervescent agent may be added, if necessary. The oral disintegrated tablet of the present invention has excellent crushing degree, fast disintegration, good taste and low cost, and may be taken with no water and high curative effect.

Description

The Ginseng Caulis and Folium all saponin orally disintegrating tablet preparation and its preparation method
[technical field]
The present invention relates to a kind of can the spleen invigorating QI invigorating, be used for the cardiopalmus that the deficiency of vital energy causes, breathe hard fatigue and weak, the indigestion and loss of appetite ginseng stem and leaf total saponin oral disintegration tablet that waits card.
[background technology]
Clinical research shows that stem and leaf of Radix Ginseng total saponins has the adjusting cardiac function, strengthens the heart power that contracts, coronary blood flow increasing and myocardial flow, thereby increase the supply of flesh blood oxygen, the reduction peripheral vascular resistance is arranged, lightening heart load, thereby the effect of depressor muscle oxygen consumption again.Coronary artery dilator reduces blood viscosity, repairs col arterial blood cannon born endotheliocyte, ischemia and anoxybiotic cardiac muscle are improved and protects.
Stem and leaf of Radix Ginseng total saponins can strengthen myocardial contraction, improves the heart blood discharge amount, improves the heart, cerebral blood supply, prevents the caused ischemical reperfusion injury in the logical again back of the heart, cerebrovascular.Has the human body immunity improving function, endocrine regulation and autonomic nervous dysfunction, strengthening by means of tonics, the Fructus Alpiniae Oxyphyllae of calming the nerves, enhancing body stress ability, antifatigue effect.Be used for coronary heart disease, cerebral thrombosis and sequela, climacteric syndrome, latent diabetes and antineoplastic auxiliary treatment.
[summary of the invention]
The objective of the invention is to improve existing stem and leaf of Radix Ginseng total saponins aspect peroral dosage form deficiency, provide a kind of taking convenience, absorption is rapid-action, bioavailability is high ginseng stem and leaf total saponin oral disintegration tablet to extensive patients and medical personnel.Needn't drink water when the present invention relates to take, in the oral cavity, only need tens seconds can rapid disintegrate or dissolving, the ginseng stem and leaf total saponin oral disintegrating tablet and the preparation technology thereof that can finish to take medicine with saliva hypopharynx.
One, prescription
The ginseng stem and leaf total saponin oral disintegrating tablet that reaches of the present invention comprises the material medicine stem and leaf of Radix Ginseng total saponins, needs following former, the auxiliary material of 9 classes altogether, wherein: when not making Cotton seeds, then do not use coating material, effervescent also can for selecting adjuvant for use as one sees fit.Stem and leaf of Radix Ginseng total saponins (5-50) %, binding agent (0-5) %, filler (10-80) %, disintegrating agent (2-35) %, correctives (1-40) %, coating material (0-40) %, effervescent (0-30) %, fluidizer (0.01-5) %, lubricant (0.3-3) %.
Wherein:
Binding agent includes but are not limited to starch, pregelatinized Starch, dextrin, maltodextrin, sucrose, arabic gum, gelatin, methylcellulose, carboxymethyl cellulose, ethyl cellulose, polyvinyl alcohol, Polyethylene Glycol, polyvinylpyrrolidone (PVP), alginic acid and alginate, xanthan gum, hydroxypropyl cellulose and hydroxypropyl emthylcellulose (HPMC), can use use also capable of being combined separately.
Filler includes but are not limited to mannitol (granular or powdery), xylitol, sorbitol, maltose, erithritol, microcrystalline Cellulose, PROSOLV SMCC, polymerization sugar (EMDEX), coupling sugar, glucose, lactose, sucrose, dextrin and starch etc., can use separately, also can applied in any combination, consumption is generally (10-80) %.
Disintegrating agent includes but are not limited to crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), low substituted hydroxy-propyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa) and soybean polysaccharide (EMCOSOY) etc., can use use also capable of being combined separately.
Correctives includes but are not limited to mannitol, xylitol, stevioside, lactose, fructose, sucrose, protein sugar, maltose alcohol, glycyrrhizin, Sodium Cyclamate, gelatin, aspartame, flavoring banana essence, flavoring pineapple essence, vanillin, fragrant citrus essence, flavoring orange essence, Herba Menthae essence, ginseng essence, strawberry essence, citric acid, citric acid etc., can use use also capable of being combined separately.
Coating material includes but are not limited to gelatin, arabic gum, alginate, chitosan, carboxymethyl cellulose salt, cellulose acetate phthalate ester, ethyl cellulose, methylcellulose, hypromellose, crylic acid resin (homemade acrylic resin I, II, III, IV, Eudragit series), polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol etc., can use use also capable of being combined separately.
Fluidizer includes but are not limited to micropowder silica gel, Pulvis Talci, Cab-O-sil, Arosil, hydrated sodium aluminosilicate etc., can use use also capable of being combined separately.
Lubricant includes but are not limited to magnesium stearate, calcium stearate, zinc stearate, glyceryl monostearate, Polyethylene Glycol, hydrogenated vegetable oil, sodium stearyl fumarate, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium laurylsulfate, magnesium laurylsulfate, Stepanol MG and Pulvis Talci etc., can use use also capable of being combined separately.
Effervescent includes but are not limited to the mixture of malic acid, citric acid or citric acid and sodium bicarbonate or sodium carbonate.
Two, preparation method
The ginseng stem and leaf total saponin oral disintegrating tablet that reaches of the present invention, its preparation method is a direct compression process, the manufacturer with preparation conventional tablet all can adopt.
The stem and leaf of Radix Ginseng total saponins bitter in the mouth, the present invention can adopt two kinds of distinct methods to carry out flavoring or taste masking: 1. adopt the direct flavoring of correctives; 2. in advance stem and leaf of Radix Ginseng total saponins is carried out powder coating with taste masking.
Concrete preparation method is as follows:
The preprocess method of first step stem and leaf of Radix Ginseng total saponins:
1. directly the flavoring method---this law is granulated to the stem and leaf of Radix Ginseng total saponins raw material or is not dealt with, and directly enters for second step;
2. powder coating taste masking---get selected coating material, with the dissolving of the solvent that adapts with it and to be diluted to debita spissitudo standby, getting stem and leaf of Radix Ginseng total saponins again places ebullated bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get stem and leaf of Radix Ginseng total saponins powder coating granule, dry back sieving for standby;
Second step took by weighing correctives and stem and leaf of Radix Ginseng total saponins or the feed particles after first step taste masking processing according to quantity, and mix homogeneously is standby;
The 3rd step took by weighing filler, disintegrating agent, effervescent, fluidizer and mix homogeneously according to quantity, made evenly again with through second mixing of materials that goes on foot gained, and adding lubricant mixing is standby;
The 4th step gained material detects through intermediate, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
[beneficial effect]
Tablet is a kind of conventional dosage forms, because of its steady quality, dosage accurately, take, easy to carry, mechanization degree is high, low one of the at present the most frequently used dosage form that becomes of production cost, but because of the tablet extrusion forming, disintegrate is slow, bioavailability is lower, and part patient swallows comparatively difficult, thereby promoting the use of to a certain extent of tablet is restricted.The oral administration solid quick releasing formulation becomes a focus, particularly oral cavity disintegration tablet of new drug development in recent years for this reason, because of its taking convenience, rapid-action, bioavailability is high, the good emphasis that becomes tablet exploitation of mouthfeel.
Oral cavity disintegration tablet is meant not to be needed water or only needs low amounts of water, need not to chew, and tablet places lingual surface, meets after saliva separates rapidly or collapse, and borrows and swallows power, and medicine can be gone into the tablet of stomach onset.The characteristics of oral cavity disintegration tablet are that absorption is fast, bioavailability is high, and intestinal is residual few, and side effect is low, avoids liver first-pass effect etc.
According to the requirement of " formulation characteristic of oral cavity disintegration tablet and quality control meeting summary ", oral cavity disintegration tablet has essential leap than the disintegration rate of drop pill and ordinary tablet, and the disintegrate of oral cavity disintegration tablet generally in 30 seconds, is no more than 1 minute at most.
[specific embodiment]
For the preparation method of ginseng stem and leaf total saponin oral disintegrating tablet of the present invention better is described, in conjunction with directly flavoring method and powder coating taste masking method are as follows for an embodiment respectively:
Embodiment one direct flavoring method
One. prescription
1. raw material---stem and leaf of Radix Ginseng total saponins 25.0g;
2. binding agent---polyvinylpyrrolidone K-30 0.5g;
3. filler---mannitol 53.5g;
PROSOLV?SMCC?5.0g;
4. correctives---aspartame 1.0g;
Ginseng essence 1.0g;
5. disintegrating agent---crospolyvinylpyrrolidone 8.0g;
L-HPC?4.0g;
6. fluidizer---micropowder silica gel 1.0g;
7. lubricant---sodium stearyl fumarate 1.0g.
Gross weight 100g makes 1000 altogether.
Two. preparation method
1) get the stem and leaf of Radix Ginseng total saponins raw material pulverizing, granulate, cross 26 mesh sieves with polyvinylpyrrolidone K-30, standby;
2) with micropowder silica gel, ginseng essence, PROSOLV SMCC and aspartame, cross 40 mesh sieves respectively, mix homogeneously adds the stem and leaf of Radix Ginseng total saponins granule of having granulated again, and mix homogeneously is standby;
3) get mannitol, L-HPC and crospolyvinylpyrrolidone and cross 40 mesh sieves respectively, mix homogeneously will add and mix homogeneously through the raw material of flavoring again, adds sodium stearyl fumarate and mix homogeneously at last;
4) intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment two powder coating taste masking methods
One. prescription
1. raw material---stem and leaf of Radix Ginseng total saponins 25.0g;
2. coating material---Eudragit E100 3.5g;
Eudragit NE30D (doing) 1.5g;
3. filler---mannitol 50.5g;
Microcrystalline Cellulose 5.0g;
4. correctives---aspartame 1.0g;
Ginseng essence 1.0g;
5. disintegrating agent---crospolyvinylpyrrolidone 6.0g;
L-HPC?4.0g;
6. fluidizer---micropowder silica gel 1.5g;
7. lubricant---sodium stearyl fumarate 1.0g.
Gross weight 100g makes 1000 altogether.
Two. preparation method
1) gets Eudragit E100 and Eudragit NE30D Eudragit NE30D with the dissolving of the medicinal industrial alcohol more than 95% and to be diluted to finite concentration standby;
2) get stem and leaf of Radix Ginseng total saponins and place ebullated bed to seethe with excitement, spray into above-mentioned solution by certain speed and carry out powder coating, make stem and leaf of Radix Ginseng total saponins powder coating granule, dry back is standby;
3) with mannitol, microcrystalline Cellulose, micropowder silica gel, PVPP, L-HPC, aspartame, sodium stearyl fumarate and ginseng essence mix homogeneously, again and sieve after the coated granule mixing standby;
4) intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment three effervescent flavoring methods
One. prescription
1. raw material---stem and leaf of Radix Ginseng total saponins 25.0g;
2. binding agent---polyvinylpyrrolidone K-30 0.5g;
3. effervescent---citric acid 12.5g;
Sodium bicarbonate 10.0g;
4. filler---mannitol 28.0g;
PROSOLV SMCC?5.0g;
5. correctives---aspartame 1.0g;
Fragrant citrus essence 1.0g;
6. disintegrating agent---crospolyvinylpyrrolidone 10.0g;
L-HPC?5.0g;
7. fluidizer---micropowder silica gel 1.0g;
8. lubricant---sodium stearyl fumarate 1.0g.
Gross weight 100g makes 1000 altogether.
Two. preparation method
1) get stem and leaf of Radix Ginseng total saponins and citric acid raw material and mix the back pulverizing, granulate, cross 26 mesh sieves with polyvinylpyrrolidone K-30, standby;
2) get sodium bicarbonate and pulverize, granulate, cross 26 mesh sieves with polyvinylpyrrolidone K-30, standby;
3) adjuvant that all the other are all is crossed mix homogeneously behind 40 mesh sieves respectively, adds the granule of having granulated again, and mix homogeneously is standby;
4) intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Disintegration that the sample of the foregoing description is measured and slice, thin piece hardness are as follows:
Embodiment disintegration (second) slice, thin piece hardness (newton)
1 11-22 18-26
2 13-29 15-24
3 15-28 16-25

Claims (8)

  1. One kind can the spleen invigorating QI invigorating, be used for the cardiopalmus that the deficiency of vital energy causes, breathe hard, fatigue and weak, the indigestion and loss of appetite ginseng stem and leaf total saponin oral disintegrating tablet that waits card, by stem and leaf of Radix Ginseng total saponins, filler, disintegrating agent, correctives, fluidizer, supplementary materials such as lubricant, according to circumstances can also add binding agent, effervescent or coating material, with suitable proportioning, form through specific method for preparing, it is characterized in that its prescription is composed as follows: stem and leaf of Radix Ginseng total saponins (5-50) %, binding agent (0-5) %, filler (10-80) %, disintegrating agent (2-35) %, correctives (1-40) %, coating material (0-40) %, effervescent (0-30) %, fluidizer (0.01-5) %, lubricant (0.3-3) %.
  2. 2. various adjuvants of addressing according to claim 1 of being addressed is characterized in that selection kind separately is as follows:
    Binding agent---include but are not limited to starch, pregelatinized Starch, dextrin, maltodextrin, sucrose, arabic gum, gelatin, methylcellulose, carboxymethyl cellulose, ethyl cellulose, polyvinyl alcohol, Polyethylene Glycol, polyvinylpyrrolidone (PVP), alginic acid and alginate, xanthan gum, hydroxypropyl cellulose and hydroxypropyl emthylcellulose (HPMC), can use use also capable of being combined separately.
    Filler---include but are not limited to mannitol (granular or powdery), xylitol, sorbitol, maltose, Chi ?alcohol, microcrystalline Cellulose, PROSOLV SMCC, polymerization sugar (EMDEX ), coupling sugar, glucose, lactose, sucrose, dextrin and starch etc., can use separately, also can applied in any combination, consumption is generally (10-80) %.
    Disintegrating agent---include but are not limited to crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), low substituted hydroxy-propyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa) and soybean polysaccharide (EMCOSOY ) etc., can use use also capable of being combined separately.
    Correctives---include but are not limited to mannitol, xylitol, stevioside, lactose, fructose, sucrose, protein sugar, maltose alcohol, glycyrrhizin, Sodium Cyclamate, gelatin, aspartame, flavoring banana essence, flavoring pineapple essence, vanillin, fragrant citrus essence, flavoring orange essence, Herba Menthae essence, ginseng essence, strawberry essence, citric acid, citric acid etc., can use use also capable of being combined separately.
    Coating material---include but are not limited to gelatin, arabic gum, alginate, chitosan, carboxymethyl cellulose salt, cellulose acetate phthalate ester, ethyl cellulose, methylcellulose, hypromellose, crylic acid resin (homemade acrylic resin I, II, III, IV, Eudragit Series), polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol etc., can use use also capable of being combined separately.
    Fluidizer---include but are not limited to micropowder silica gel, Pulvis Talci, Cab-O-sil, Arosil, hydrated sodium aluminosilicate etc., can use use also capable of being combined separately.
    Lubricant---include but are not limited to magnesium stearate, calcium stearate, zinc stearate, glyceryl monostearate, Polyethylene Glycol, hydrogenated vegetable oil, sodium stearyl fumarate, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium laurylsulfate, magnesium laurylsulfate, Stepanol MG and Pulvis Talci etc., can use use also capable of being combined separately.
  3. 3. preparation method that is used for the ginseng stem and leaf total saponin oral disintegrating tablet that claim 1 addresses is characterized in that being made up of following steps:
    The pretreatment of first step stem and leaf of Radix Ginseng total saponins:
    (1) directly flavoring---this law is granulated to the stem and leaf of Radix Ginseng total saponins raw material or is not dealt with, and directly enters for second step;
    (2) powder coating taste masking---get selected coating material, with the dissolving of the solvent that adapts with it and to be diluted to debita spissitudo standby, getting stem and leaf of Radix Ginseng total saponins again places ebullated bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get stem and leaf of Radix Ginseng total saponins powder coating granule, dry back sieving for standby;
    Second step took by weighing correctives and stem and leaf of Radix Ginseng total saponins or the feed particles after first step taste masking processing according to quantity, and mix homogeneously is standby;
    The 3rd step took by weighing filler, disintegrating agent, effervescent, fluidizer and mix homogeneously according to quantity, made evenly again with through second mixing of materials that goes on foot gained, and adding lubricant mixing is standby;
    The 4th step gained material detects through intermediate, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
  4. 4. the preparation method of addressing according to claim 3 is characterized in that: the method for the first step (2) need be used coating material that stem and leaf of Radix Ginseng total saponins is carried out taste masking in advance and handle.
  5. 5. the preparation method of addressing according to claim 4, it is characterized in that: be used for coating material that taste masking handles and be any one or two or more mixture such as gelatin, arabic gum, alginate, chitosan, carboxymethyl cellulose salt, cellulose acetate phthalate ester, ethyl cellulose, methylcellulose, hypromellose, crylic acid resin (homemade acrylic resin I, II, III, IV, Eudragit series), polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol.
  6. 6. any preparation method of addressing according to claim 3 is characterized in that: according to circumstances also can add the adjuvant effervescent.
  7. 7. the effervescent of addressing according to claim 6, it is characterized in that: this adjuvant is the mixture of malic acid, citric acid or citric acid and sodium bicarbonate or sodium carbonate.
  8. 8. preparation method that is used for the ginseng stem and leaf total saponin oral disintegrating tablet that claim 1 addresses, the hardness that it is characterized in that the tablet that obtains are between 10 to 45 newton, and disintegration time is at 1-60 in second.
CN 200410069353 2004-07-19 2004-07-19 Ginseng stem and leaf total saponin oral disintegration tablet and its preparing method Expired - Fee Related CN1283267C (en)

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007006208A1 (en) * 2005-07-14 2007-01-18 National Institute Of Pharmaceutical R & D Co., Ltd. Medicinal composition containing ginseng secondary glycosides, its preparation method and application
CN100387226C (en) * 2005-03-18 2008-05-14 北京科信必成医药科技发展有限公司 Cepharanthine oral disintegration tablet and its preparing method
CN102948418A (en) * 2011-08-26 2013-03-06 浙江海洋学院 Tea saponin tablet and preparation method thereof
CN106943440A (en) * 2017-04-10 2017-07-14 高其品 The sorbefacient of polyose medicament bioavilability can be improved

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100387226C (en) * 2005-03-18 2008-05-14 北京科信必成医药科技发展有限公司 Cepharanthine oral disintegration tablet and its preparing method
WO2007006208A1 (en) * 2005-07-14 2007-01-18 National Institute Of Pharmaceutical R & D Co., Ltd. Medicinal composition containing ginseng secondary glycosides, its preparation method and application
US7973014B2 (en) 2005-07-14 2011-07-05 National Institute Of Pharmaceutical R&D Co., Ltd. Medicinal composition containing ginseng secondary glycosides, its preparation method and application
CN102948418A (en) * 2011-08-26 2013-03-06 浙江海洋学院 Tea saponin tablet and preparation method thereof
CN102948418B (en) * 2011-08-26 2015-10-21 浙江海洋学院 A kind of tea saponin tablet and preparation method thereof
CN106943440A (en) * 2017-04-10 2017-07-14 高其品 The sorbefacient of polyose medicament bioavilability can be improved

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Correction item: Denomination of Invention

Correct: Ginseng stem and leaf total saponin oral disintegrating tablet preparation and preparation process thereof

False: Ginseng stem and leaf total saponin oral disintegrating tablet preparation and preparation method thereof

Number: 45

Page: 920

Volume: 22

CI03 Correction of invention patent

Correction item: Denomination of Invention

Correct: Ginseng stem and leaf total saponin oral disintegrating tablet preparation and preparation process thereof

False: Ginseng stem and leaf total saponin oral disintegrating tablet preparation and preparation method thereof

Number: 45

Page: The title page

Volume: 22

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Address after: 100083 Haidian District, Xueyuan Road, No. 30, A building, room No. 15, room, room 15

Patentee after: COSCI MED-TECH Co.,Ltd.

Address before: 100080, Haidian District satellite building, No. 63, Zhichun Road, Beijing, room 1410, Beijing

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Granted publication date: 20061108