CN1628655A - Andrographolide dispersed tablet and preparation method thereof - Google Patents
Andrographolide dispersed tablet and preparation method thereof Download PDFInfo
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- CN1628655A CN1628655A CNA2004100745311A CN200410074531A CN1628655A CN 1628655 A CN1628655 A CN 1628655A CN A2004100745311 A CNA2004100745311 A CN A2004100745311A CN 200410074531 A CN200410074531 A CN 200410074531A CN 1628655 A CN1628655 A CN 1628655A
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- andrographolide
- dispersible tablet
- lactose
- tablet
- microcrystalline cellulose
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Abstract
The invention discloses an andrographolide dispersed tablet and preparation method, wherein the tablet is prepared from andrographolide and pharmaceutical carrier, the prescription for each 1000 dispersed tablets includes, andrographolide 50-100g, lactose 50-200g, crystalline cellulose 50-250g, low substituted methylcellulose propylene glycol ether 20-150g, crosslinked povidone 20-150g, stevioside 2-20g, right amount of 95% ethanol, silica gel powder 2-20g, magnesium stearate 2-10, the invention has the advantages of good taste, convenient in use, quick action, and can be used for treating diseases including respiratory tract infection and bacteria dysentery.
Description
[technical field]
The present invention relates to the new pharmaceutical preparation of Chinese medicine andrographolide and prescription composition, particularly andrographolide dispersed tablet and preparation method thereof.
[background technology]
The andrographolide sheet has recorded in the 19 in Chinese traditional patent formulation preparation, is the ordinary tablet that andrographolide is made, and this ordinary tablet is longer disintegration, and stripping is slower, and stripping in 120 minutes just reaches 80%, so that onset is slower.The present invention is by making andrographolide a kind of new dosage form tablet formulation, make the quick disintegrate of active constituents of medicine andrographolide and reach homogeneously dispersed state, effective ingredient stripping fast, by having improved mouthfeel with flavoring agent, can be placed on and disperse the back oral in the water, be fit to the old people and the children taking of dysphagia.The present invention chooses dispersion technology, the andrographolide sheet is made the andrographolide dispersed tablet of quick acting, the complete disintegrate in 3 minutes of this dispersible tablet reaches finely dispersed state, and its effective ingredient andrographolide cumulative leaching rate in the time of 10 minutes reaches more than 60%, improves bioavailability.
[summary of the invention]
The invention provides a kind of andrographolide dispersed tablet, this dispersible tablet is made by physiology effective amount of actives andrographolide and the pharmaceutical carrier that can be made into dispersible tablet.
Dispersible tablet of the present invention, described pharmaceutical carrier is selected from: lactose, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, steviosin, ethanol, micropowder silica gel, magnesium stearate, calcium hydrogen phosphate.
Dispersible tablet of the present invention, per 1000 active component andrographolide and pharmaceutical carriers by following proportioning are made, andrographolide 25-100g wherein, lactose 50-200g, microcrystalline Cellulose 50-250g, disintegrating agent is selected from low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose.Their amount is defined as low-substituted hydroxypropyl cellulose 20-150g, polyvinylpolypyrrolidone 20-150g, carboxymethyl starch sodium 20-150g, cross-linking sodium carboxymethyl cellulose 20-150g, add steviosin 2-20g in addition, ethanol 40-200ml, micropowder silica gel 2-20g, magnesium stearate 2-10g.
Dispersible tablet of the present invention, lactose wherein, microcrystalline Cellulose is a diluent, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose are disintegrating agent, the disintegrating agent total amount be not less than total sheet heavy 5%, be not more than 40%.
Dispersible tablet of the present invention, described dispersible tablet can be in 3 minutes disintegrate and reach homogeneously dispersed state fully, its effective ingredient andrographolide cumulative leaching rate in the time of 10 minutes is more than 60%.
Dispersible tablet of the present invention, most preferably per 1000 active component andrographolide and pharmaceutical carriers by following proportioning are made,
Andrographolide 50g
Lactose 170g
Microcrystalline Cellulose 150g
Low-substituted hydroxypropyl cellulose 60g
Polyvinylpolypyrrolidone 50g
Steviosin 10g
95% ethanol 80ml
Micropowder silica gel 6g
Magnesium stearate 3g
Make 1000
The present invention also provides the preparation method of dispersible tablet of the present invention: this method is through following steps, supplementary material is crossed 100 mesh sieves respectively, take by weighing andrographolide, lactose, microcrystalline Cellulose, steviosin and disintegrating agent, mix homogeneously by recipe quantity, with 95% ethanol system soft material, the 16-24 mesh sieve, 50 ℃ of dryings, dry back 16-24 mesh sieve granulate, add micropowder silica gel, magnesium stearate, mixing, tabletting, promptly.
Preferred prescription screening process of the present invention is as follows:
The andrographolide sheet is that andrographolide adds the tablet that an amount of excipient is made, and records in the 19 in national standard Chinese traditional patent formulation preparation, and specification is 50mg, and consumption is a 0.1-0.15g, 3-4 time on the one.This product dosage form is selected dispersible tablet, can be oral because of dispersible tablet, also can be scattered in wet suit usefulness, and especially convenient to the child and the old man of dysphagia, be added with sweeting agent, liked by the child.Specification is elected the 25-100mg/ sheet as, can once obey 1 to 3, and is more convenient.
The selection of adjuvant
The selection of diluent:
Every andrographolide 25-100mg/ of this product sheet is so must add diluent.Diluent commonly used has two classes, and a class is water-soluble diluent, and as lactose, sucrose, mannitol, sorbitol etc., a class is the water-insoluble diluent, as starch, pregelatinized Starch, microcrystalline Cellulose, dextrin, calcium hydrogen phosphate etc.The water-soluble back of andrographolide viscosity is bigger, for overcoming this problem, selected lactose and microcrystalline Cellulose as diluent, lactose is very stable in air, is difficult for suction, inoperative with most drug, and compressibility is better, does not produce viscosity after water-soluble, and easy operating is grasped in the tablet manufacturing process, tablet is bright and clean attractive in appearance, and good dissolution rate is arranged.Microcrystalline Cellulose has dilution, bonding, disintegrate triple role, compressibility is better, suction is expanded at once, speeding up disintegration of tablet, microcrystalline Cellulose is combined with lactose and can better overcome the above problems, for this reason, we have passed through a large amount of experiments, and selected at last lactose and microcrystalline Cellulose are diluent.
The selection of disintegrating agent:
This product specification is the 25-100mg/ sheet, makes dispersible tablet again, and adjuvant need be added, so sheet is heavy bigger.Adjuvant is more, need be with disintegrating agent, make the rapid disintegrate of tablet, improve dissolution rate and bioavailability.The disintegrating agent that the present invention selects is: carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, sodium carboxymethyl cellulose etc., and these several disintegrating agents can be used separately, but also combination in any is used.Carboxymethyl starch sodium has and stronger draws moistly, and water absorbing capacity is big, can absorb 30 times of its dry bulk, but not exclusively water-soluble, thus tablet there is better disintegration, but improper with it, will prolong disintegration time.Low-substituted hydroxypropyl cellulose is difficult for dissolving in water, but good hygroscopicity and water absorption are arranged, and having bonding and closing the double effect of disintegrate, so can promote the tablet molding and increase hardness, also can quicken dispersive fineness after the disintegrate, thus the dissolution rate of quickening medicine.Do not produce viscosity after the polyvinylpolypyrrolidone imbibition, be fit to do disintegrating agent of the present invention.It is the most preferred disintegrating agent scheme of the present invention that low-substituted hydroxypropyl cellulose and polyvinylpolypyrrolidone share.
Selection of lubricants is selected micropowder silica gel and magnesium stearate, because of micropowder silica gel lubricate not only, can also promote disintegration of tablet; Though Pulvis Talci is a hydrophilic lubricant, does not influence disintegration of tablet, the frictional force of slice, thin piece and mould circle is relatively poor when reducing slice, makes the slice, thin piece edge vestige that rubs out easily; Though and magnesium stearate is a hydrophobic lubricant, consumption is suitable, generally not too influences disintegrate, significantly reduces the frictional force of slice, thin piece and mould circle, makes slice, thin piece bright and clean attractive in appearance.By the preferable adjuvant of experiment sieving.
Determining of supplementary product kind and amount
(1) prescription design: according to the physicochemical property of andrographolide, the optimization formula of selection is: lactose, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, steviosin, ethanol, micropowder silica gel, magnesium stearate.
(2) recipe quantity: according to the requirement of sheet weight and the quantitative limitation of adjuvant, the scope of determining preferred amount is: lactose 50-200g, microcrystalline Cellulose 50-250g, low-substituted hydroxypropyl cellulose 20-150g, polyvinylpolypyrrolidone 20-150g, steviosin 2-20g, ethanol 40-200ml, micropowder silica gel 2-20g, magnesium stearate 2-10g.
(3) most preferred prescription is selected:
Above recipe design is become six prescriptions (seeing Table 12-1);
Six prescriptions of table 12-1 design
Method for making: supplementary material was pulverized 100 mesh sieves, press recipe quantity weighting raw materials andrographolide, lactose, microcrystalline Cellulose, hyprolose (the low replacement), polyvinylpolypyrrolidone, steviosin, mix homogeneously adds 95% ethanol system soft material, and soft material is granulated with 18 mesh sieves, wet grain is in 50 ℃ of dryings, dry back adds micropowder silica gel, magnesium stearate, mix homogeneously with 18 mesh sieve granulate, with the oval special-shaped punch die tabletting of 16.8 * 8.2mm, sheet heavily is 0.5g.
Investigate the index and the method for inspection thereof:
Dispersing uniformity: the dispersible tablet dispersing uniformity of pressing under two appendix A tablets of Chinese Pharmacopoeia version in 2000 item is checked, gets 2 of this product, puts jolting in the 100ml water, in 20 ℃ ± 1 ℃ water, and all disintegrates and sieve in 3 minutes by No. 2.
Disintegration: getting this product by the inspection of an appendix XII of Chinese Pharmacopoeia version in 2000 A disintegration time mensuration method, is the disintegrate medium with water.
Dissolution: get this product according to dissolution method (two appendix XC first methods of Chinese Pharmacopoeia version in 2000), 900ml is a solvent with simulated gastric fluid-95% ethanol, and rotating speed is that per minute 100 changes, operation in accordance with the law, in 10 minutes sampling 10ml, filter, get subsequent filtrate as need testing solution.Other gets the andrographolide reference substance and is made into reference substance solution.Measure absorption value at 224nm respectively according to spectrophotography, calculate dissolution.
Prescription is investigated the result: by the above-mentioned investigation index and the method for inspection thereof.Six prescriptions to design are investigated, and the results are shown in Table 12-2.
The investigation result of six prescriptions of table 12-2
Conclusion: investigate the result according to six prescriptions, prescription six is comparatively desirable, and disintegration is short, and dispersing uniformity is better.So main adjuvant is selected lactose 170g, microcrystalline Cellulose 150g, hyprolose 60g, polyvinylpolypyrrolidone 50g in the most preferred prescription.
Dispersible tablet of the present invention, the dispersible tablet that particularly preferred prescription is made, mouthfeel is good, and taking convenience is rapid-action, can be used for treating diseases such as upper respiratory tract infection and bacillary dysentery and has good effect.
[specific embodiment]
Embodiment 1
One, the preparation of andrographolide dispersed tablet
Andrographolide 50g
Lactose 170g
Microcrystalline Cellulose 150g
Hyprolose (the low replacement) 60g
Polyvinylpolypyrrolidone 50g
Steviosin 10g
95% ethanol 80ml
Micropowder silica gel 6g
Magnesium stearate 3g
Make 1000
Two, preparation technology
1, method for making: supplementary material was pulverized 100 mesh sieves, take by weighing crude drug andrographolide, lactose, microcrystalline Cellulose, hyprolose (the low replacement), polyvinylpolypyrrolidone, the steviosin of purchase by recipe quantity, mix homogeneously, add 95% ethanol system soft material, soft material is granulated with 18 mesh sieves, wet grain is in 50 ℃ of dryings, dry back with 18 mesh sieve granulate, add micropowder silica gel, magnesium stearate, mix homogeneously, semi-finished product are surveyed content, qualified back oval special-shaped punch die tabletting with 16.8 * 8.2mm, check, qualified back packing promptly.
Embodiment 2
One, the preparation of andrographolide dispersed tablet
Andrographolide 25g
Lactose 50g
Microcrystalline Cellulose 50g
Hyprolose (the low replacement) 20g
Polyvinylpolypyrrolidone 20g
Steviosin 20g
95% ethanol 40ml
Micropowder silica gel 2g
Magnesium stearate 2g
Make 1000
Two, preparation technology
1, method for making: supplementary material was pulverized 100 mesh sieves, take by weighing crude drug andrographolide, lactose, microcrystalline Cellulose, hyprolose (the low replacement), polyvinylpolypyrrolidone, the steviosin of purchase by recipe quantity, mix homogeneously, add 95% ethanol system soft material, soft material is granulated with 18 mesh sieves, wet grain is in 50 ℃ of dryings, dry back with 18 mesh sieve granulate, add micropowder silica gel, magnesium stearate, mix homogeneously, semi-finished product are surveyed content, qualified back oval special-shaped punch die tabletting with 16.8 * 8.2mm, check, qualified back packing promptly.
Embodiment 3
One, the preparation of andrographolide dispersed tablet
Andrographolide 100g
Lactose 200g
Microcrystalline Cellulose 250g
Hyprolose (the low replacement) 150g
Polyvinylpolypyrrolidone 150g
Steviosin 20g
95% ethanol 200ml
Micropowder silica gel 20g
Magnesium stearate 10g
Make 1000
Two, preparation technology
1, method for making: supplementary material was pulverized 100 mesh sieves, take by weighing crude drug andrographolide, lactose, microcrystalline Cellulose, hyprolose (the low replacement), polyvinylpolypyrrolidone, the steviosin of purchase by recipe quantity, mix homogeneously, add 95% ethanol system soft material, soft material is granulated with 18 mesh sieves, wet grain is in 50 ℃ of dryings, dry back with 18 mesh sieve granulate, add micropowder silica gel, magnesium stearate, mix homogeneously, semi-finished product are surveyed content, qualified back oval special-shaped punch die tabletting with 16.8 * 8.2mm, check, qualified back packing promptly.
Embodiment 4
Get andrographolide, heavily add 8% carboxymethyl starch sodium and 10% polyvinylpolypyrrolidone by sheet, add an amount of lactose again, microcrystalline Cellulose, steviosin, mix homogeneously, with 95% ethanol system soft material, the 16-24 mesh sieve is granulated, 50 ℃ of dryings, dry back 16-24 mesh sieve granulate adds micropowder silica gel, magnesium stearate, mixing, tabletting, by the requirement check of two appendix of Chinese Pharmacopoeia version in 2000 relevant " dispersible tablet ", disintegration was less than 3 minutes, other check items also meet " dispersible tablet " requirement, and its effective ingredient andrographolide cumulative leaching rate in the time of 10 minutes reaches more than 60%.
Claims (7)
1, a kind of andrographolide dispersed tablet is characterized in that, this dispersible tablet is made by physiology effective amount of actives andrographolide and the pharmaceutical carrier that can be made into dispersible tablet.
2, the dispersible tablet of claim 1, described pharmaceutical carrier is selected from: lactose, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, steviosin, ethanol, micropowder silica gel, magnesium stearate, calcium hydrogen phosphate.
3, the dispersible tablet of claim 2, per 1000 active component andrographolide and pharmaceutical carriers by following proportioning are made, andrographolide 25-100g, lactose 50-200g, microcrystalline Cellulose 50-250g, low-substituted hydroxypropyl cellulose 20-150g, polyvinylpolypyrrolidone 20-150g, steviosin 2-20g, ethanol 40-200ml, micropowder silica gel 2-20g, magnesium stearate 2-10g.
4, the dispersible tablet of claim 3 is characterized in that, lactose wherein, microcrystalline Cellulose is a diluent, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone are disintegrating agent, the disintegrating agent total amount be not less than total sheet heavy 5%, be not more than total sheet heavy 40%.
5, the dispersible tablet of claim 4 is characterized in that, described dispersible tablet can be in 3 minutes disintegrate and reach homogeneously dispersed state fully, its effective ingredient andrographolide cumulative leaching rate in the time of 10 minutes is more than 60%.
6, the dispersible tablet of claim 3, per 1000 active component andrographolide and pharmaceutical carriers by following proportioning are made,
Andrographolide 50g
Lactose 170g
Microcrystalline Cellulose 150g
Low-substituted hydroxypropyl cellulose 60g
Polyvinylpolypyrrolidone 50g
Steviosin 10g
95% ethanol 80ml
Micropowder silica gel 6g
Magnesium stearate 3g
7, the preparation method of any one dispersible tablet of claim 1-6: it is characterized in that,, supplementary material is crossed 100 mesh sieves respectively through following steps, take by weighing andrographolide, lactose, microcrystalline Cellulose, steviosin and disintegrating agent by recipe quantity, mix homogeneously is with 95% ethanol system soft material, 16-24 mesh sieve, 50 ℃ of dryings, dry back 16-24 mesh sieve granulate adds micropowder silica gel, magnesium stearate, mixing, tabletting, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100745311A CN1628655A (en) | 2004-09-07 | 2004-09-07 | Andrographolide dispersed tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100745311A CN1628655A (en) | 2004-09-07 | 2004-09-07 | Andrographolide dispersed tablet and preparation method thereof |
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| CN1628655A true CN1628655A (en) | 2005-06-22 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102552193A (en) * | 2011-11-08 | 2012-07-11 | 天圣制药集团股份有限公司 | Andrographolide tablet and preparation method thereof |
| CN104138361A (en) * | 2014-07-31 | 2014-11-12 | 南京正科制药有限公司 | Andrographolide dispersible tablet and preparation method thereof |
| CN104274440A (en) * | 2013-07-11 | 2015-01-14 | 成都中医药大学 | Andrographolide composite particles and preparation method thereof |
| CN107184558A (en) * | 2017-05-25 | 2017-09-22 | 南京正科医药股份有限公司 | A kind of andrographolide dispersed tablet |
-
2004
- 2004-09-07 CN CNA2004100745311A patent/CN1628655A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102552193A (en) * | 2011-11-08 | 2012-07-11 | 天圣制药集团股份有限公司 | Andrographolide tablet and preparation method thereof |
| CN104274440A (en) * | 2013-07-11 | 2015-01-14 | 成都中医药大学 | Andrographolide composite particles and preparation method thereof |
| CN104274440B (en) * | 2013-07-11 | 2017-04-26 | 成都中医药大学 | Andrographolide composite particles and preparation method thereof |
| CN104138361A (en) * | 2014-07-31 | 2014-11-12 | 南京正科制药有限公司 | Andrographolide dispersible tablet and preparation method thereof |
| CN107184558A (en) * | 2017-05-25 | 2017-09-22 | 南京正科医药股份有限公司 | A kind of andrographolide dispersed tablet |
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