CN1267094C - Orally disintegrating tablet of safflor yellow and its preparation process - Google Patents
Orally disintegrating tablet of safflor yellow and its preparation process Download PDFInfo
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- CN1267094C CN1267094C CN 200410070379 CN200410070379A CN1267094C CN 1267094 C CN1267094 C CN 1267094C CN 200410070379 CN200410070379 CN 200410070379 CN 200410070379 A CN200410070379 A CN 200410070379A CN 1267094 C CN1267094 C CN 1267094C
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- disintegrating tablet
- orally disintegrating
- yellow
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- essence
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Abstract
The present invention relates to a safflower yellow orally disintegrating tablet and a preparation process thereof. The safflower yellow orally disintegrating tablet has the effects of coronary arteriae dilation, antioxidation, myocardium protection, blood pressure decrease, immunodepression and brain protection, etc. The present invention aims at making up for the preparation insufficiency of existing safflower yellow preparation and providing a safflower yellow orally disintegrating tablet and a preparation process thereof for all patients and medical workers; the safflower yellow orally disintegrating tablet has the advantages of convenient use and rapid absorption and effect-taking. Safflower yellow is used as raw material; filling agents, disintegrating agents, corrigents, flow aid, lubricating agents, etc. are used as auxiliary materials; adhesives or coating materials can also be used according to different situations; appropriate quantity of effervescent agents can be added on specific situation; the orally disintegrating tablet is prepared by a specific preparation method and obtained after tabletting by tabletting machines. The orally disintegrating tablet of the present invention has the characteristics of good friability, rapid disintegration, good taste, no gravel feel, no need of specific production condition, low production cost, convenient carry, storage, transportation and use, etc.; most of all, the orally disintegrating tablet can be taken without water and takes effect quickly, and therefore, the present invention improves the patient's compliance and enhances the curative effect of the medicine.
Description
[technical field]
The present invention relates to a kind of Orally disintegrating tablet of safflor yellow with effects such as coronary artery dilating, antioxidation, protection cardiac muscle, blood pressure lowering, immunosuppressant and brain protections.
[background technology]
Flos Carthami is a drug for invigorating blood circulation and eliminating stasis commonly used, can be used for many disturbance of blood circulation treatment of diseases such as coronary heart disease, angina pectoris.Carthamus yellow is the effective site of extracting from Chinese medicine safflower (being commonly called as Flos Carthami), is the main water soluble ingredient of Flos Carthami, is a mixing chalcone derivative glycosides.Can treat or prevent disturbance of blood circulation illness such as multiple cardiovascular and cerebrovascular disease.The Carthamus yellow crude product is the food colour that a country allows use, has gone on the market year surplus in the of ten.Carthamus yellow has many-sided cardiovascular pharmacological effect, but anticoagulant, and antithrombotic forms, and resists myocardial ischemia antiplatelet activity factor, free radical resisting etc.
The dosage form of existing Carthamus yellow preparation has: tablet, capsule and injection.
Because dosage form needs a large amount of water to send down when most of oral formulations are taken, this makes the patient of many old peoples, infant or dysphagia, water intaking inconvenience be difficult to take.Injection often is easy to generate anaphylaxis or untoward reaction etc. again, and it is big that the while injection also exists operation easier, and the patient suffering is also big, makes and medical treatment cost high the shortcoming that patient economy burden is heavy.Therefore, be necessary to prepare and take convenient dosage form to satisfy the multiple needs that clinical treatment and family use.
[summary of the invention]
The objective of the invention is to improve the deficiency of existing Carthamus yellow aspect peroral dosage form, provide a kind of taking convenience, absorption is rapid-action, bioavailability is high Orally disintegrating tablet of safflor yellow preparation to extensive patients and medical personnel.Needn't drink water when the present invention relates to take, in the oral cavity, only need get final product rapid disintegrate or dissolving in tens seconds, can finish Orally disintegrating tablet of safflor yellow of taking medicine and preparation method thereof with saliva hypopharynx.
One, prescription
The Orally disintegrating tablet of safflor yellow that reaches of the present invention comprises the material medicine Carthamus yellow, needs following former, the auxiliary material of 9 classes altogether, and wherein: when not making Cotton seeds, then do not use coating material, effervescent also can for selecting adjuvant for use as one sees fit.
Carthamus yellow (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 Orally disintegrating tablet of safflor yellow that reaches of the present invention, its preparation method is a direct compression process, the manufacturer with preparation conventional tablet all can adopt.
The Carthamus yellow 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 Carthamus yellow is carried out powder coating with taste masking.
Concrete preparation method is as follows:
The preprocess method of first step Carthamus yellow:
1. directly the flavoring method---this law is granulated to the Carthamus yellow 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 Carthamus yellow again places ebullated bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get Carthamus yellow powder coating granule, dry back sieving for standby;
Second step took by weighing correctives and Carthamus yellow 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, disintegrate rapidly after the chance saliva, or borrow and swallow power, 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 Orally disintegrating tablet of safflor yellow 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---Carthamus yellow 30.0g;
2. binding agent---polyvinylpyrrolidone K-30 0.5g;
3. filler---mannitol 48.5g;
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 Carthamus yellow raw material pulverizing, granulate, cross 26 mesh sieves with polyvinylpyrrolidone K-30, standby;
2) with micropowder silica gel, ginseng essence, PROSOLV
SMCC and aspartame are crossed 40 mesh sieves respectively, and mix homogeneously adds the Carthamus yellow 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---Carthamus yellow 30.0g;
2. coating material---Eudragit
E100 3.5g;
Eudragit
NE30D (doing) 1.5g;
3. filler---mannitol 55.5g;
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 110g makes 1000 altogether.
Two. preparation method
1) gets Eudragit
E100 and Eudragit
NE30D Eudragit
NE30D is with the dissolving of the medicinal industrial alcohol more than 95% and to be diluted to finite concentration standby;
2) get Carthamus yellow and place ebullated bed to seethe with excitement, spray into above-mentioned solution by certain speed and carry out powder coating, make Carthamus yellow 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---Carthamus yellow 30.0g;
2. binding agent---polyvinylpyrrolidone K-30 0.5g;
3. effervescent---citric acid 12.5g;
Sodium bicarbonate 10.0g;
4. filler---mannitol 43.0g;
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 120g makes 1000 altogether.
Two. preparation method
1) get Carthamus yellow 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 2 3 | 11-22 13-29 15-28 | 18-26 15-24 16-25 |
Claims (7)
1. Orally disintegrating tablet of safflor yellow, it is characterized in that its weight consists of Carthamus yellow 5～50%, clothing sheet material polyacrylic resin 4.55～40%, disintegrating agent crospolyvinylpyrrolidone and low-substituted hydroxypropyl methylcellulose amount to 2～35%, filler 10-80%, correctives 1～40%, fluidizer 0.01～5%, lubricant 0.3～3% is formed, wherein filler is selected from mannitol, microcrystalline Cellulose, dextrin, lactose, starch, in maltodextrin and the pregelatinized Starch one or more, correctives is selected from mannitol, lactose, stevioside, gelatin, aspartame, cyclamate, glycyrrhizin, fragrant citrus essence, flavoring orange essence, Herba Menthae essence, ginseng essence, strawberry essence, citric acid, in the citric acid one or more, fluidizer is selected from micropowder silica gel, Pulvis Talci, Cab-O-sil, Arosil, in the hydrated sodium aluminosilicate one or more, lubricant is selected from magnesium stearate, glyceryl monostearate, Stepanol MG, in the Pulvis Talci, in the sodium stearyl fumarate one or more; After wherein Carthamus yellow being carried out powder coating with coating material, the gained granule is pressed into disintegrating tablet with other adjuvant.
2. Orally disintegrating tablet of safflor yellow as claimed in claim 1, wherein filler is mannitol and/or microcrystalline Cellulose.
3. Orally disintegrating tablet of safflor yellow as claimed in claim 1, wherein correctives is aspartame and/or ginseng essence.
4. Orally disintegrating tablet of safflor yellow as claimed in claim 1, wherein lubricant is a sodium stearyl fumarate.
5. Orally disintegrating tablet of safflor yellow as claimed in claim 1, wherein fluidizer is micropowder silica gel.
6. Orally disintegrating tablet of safflor yellow as claimed in claim 1, it is characterized in that its weight consists of: 30 parts of Carthamus yellows, 5 parts of polyacrylic resins, 55.5 parts in mannitol, 5 parts of microcrystalline Cellulose, 1 part of aspartame, 1 part of ginseng essence, 6 parts of crospolyvinylpyrrolidone, 4 parts of low-substituted hydroxypropyl methylcellulose, 1.5 parts of micropowder silica gels, 1 part of sodium stearyl fumarate.
7.., it is characterized in that forming by following steps as the preparation method of any described Orally disintegrating tablet of safflor yellow of claim 1-6:
The pretreatment of first step Carthamus yellow; Get selected coating material, with the dissolving of the solvent that adapts with it and to be diluted to debita spissitudo standby, get Carthamus yellow again and place fluid bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get Carthamus yellow powder coating granule, dry back sieving for standby;
Second step took by weighing correctives and Carthamus yellow granule 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, fluidizer and mix homogeneously according to quantity, made evenly again with through second mixing of materials that goes on foot gained, added the lubricant mixing, and is standby;
The 4th step gained material detects through intermediate, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410070379 CN1267094C (en) | 2004-08-03 | 2004-08-03 | Orally disintegrating tablet of safflor yellow and its preparation process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410070379 CN1267094C (en) | 2004-08-03 | 2004-08-03 | Orally disintegrating tablet of safflor yellow and its preparation process |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1602857A CN1602857A (en) | 2005-04-06 |
| CN1267094C true CN1267094C (en) | 2006-08-02 |
Family
ID=34666796
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410070379 Expired - Fee Related CN1267094C (en) | 2004-08-03 | 2004-08-03 | Orally disintegrating tablet of safflor yellow and its preparation process |
Country Status (1)
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|---|---|
| CN (1) | CN1267094C (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101327208B (en) * | 2008-04-30 | 2010-04-21 | 北京市心肺血管疾病研究所 | Use of Carthamus tinctorius yellow colour in preparing medicament for treating and/or preventing lung damnification |
| CN103127009B (en) * | 2011-12-02 | 2014-12-24 | 浙江永宁药业股份有限公司 | Carthamin yellow sublingual tablet and preparation method and application thereof |
| CN102961357A (en) * | 2012-11-09 | 2013-03-13 | 新疆农业大学 | Safflower carthamus uranidin effervescent tablets and preparation technology thereof |
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2004
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
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Address after: 100083 A building, block 15, Tiangong building, No. 30, Haidian District, Beijing, Xueyuan Road Patentee after: COSCI MED-TECH Co.,Ltd. Address before: 100080, Haidian District satellite building, No. 63, Zhichun Road, Beijing, room 1410, Beijing Patentee before: COSCI MED-TECH Co.,Ltd. |
|
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20060802 |
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| CF01 | Termination of patent right due to non-payment of annual fee |