CN1660078A - Oral disintegration tablet of bergenin and compound bergenin and preparation method - Google Patents
Oral disintegration tablet of bergenin and compound bergenin and preparation method Download PDFInfo
- Publication number
- CN1660078A CN1660078A CN 200410093147 CN200410093147A CN1660078A CN 1660078 A CN1660078 A CN 1660078A CN 200410093147 CN200410093147 CN 200410093147 CN 200410093147 A CN200410093147 A CN 200410093147A CN 1660078 A CN1660078 A CN 1660078A
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- CN
- China
- Prior art keywords
- bergeninum
- preparation
- sodium
- lactose
- essence
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 238000002360 preparation method Methods 0.000 title claims description 21
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- 229920001282 polysaccharide Polymers 0.000 claims description 2
- 239000005017 polysaccharide Substances 0.000 claims description 2
- 150000004804 polysaccharides Chemical class 0.000 claims description 2
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 2
- 230000008569 process Effects 0.000 claims description 2
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- 238000007873 sieving Methods 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 239000000429 sodium aluminium silicate Substances 0.000 claims description 2
- 235000012217 sodium aluminium silicate Nutrition 0.000 claims description 2
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 claims description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 2
- 235000017550 sodium carbonate Nutrition 0.000 claims description 2
- 229960001462 sodium cyclamate Drugs 0.000 claims description 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 2
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims description 2
- 229940013618 stevioside Drugs 0.000 claims description 2
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 claims description 2
- 235000019202 steviosides Nutrition 0.000 claims description 2
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- ZKLPARSLTMPFCP-UHFFFAOYSA-N Cetirizine Chemical compound C1CN(CCOCC(=O)O)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZKLPARSLTMPFCP-UHFFFAOYSA-N 0.000 claims 1
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 claims 1
- PVLJETXTTWAYEW-UHFFFAOYSA-N Mizolastine Chemical compound N=1C=CC(=O)NC=1N(C)C(CC1)CCN1C1=NC2=CC=CC=C2N1CC1=CC=C(F)C=C1 PVLJETXTTWAYEW-UHFFFAOYSA-N 0.000 claims 1
- JAUOIFJMECXRGI-UHFFFAOYSA-N Neoclaritin Chemical compound C=1C(Cl)=CC=C2C=1CCC1=CC=CN=C1C2=C1CCNCC1 JAUOIFJMECXRGI-UHFFFAOYSA-N 0.000 claims 1
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- UFLGIAIHIAPJJC-UHFFFAOYSA-N Tripelennamine Chemical compound C=1C=CC=NC=1N(CCN(C)C)CC1=CC=CC=C1 UFLGIAIHIAPJJC-UHFFFAOYSA-N 0.000 claims 1
- GXDALQBWZGODGZ-UHFFFAOYSA-N astemizole Chemical compound C1=CC(OC)=CC=C1CCN1CCC(NC=2N(C3=CC=CC=C3N=2)CC=2C=CC(F)=CC=2)CC1 GXDALQBWZGODGZ-UHFFFAOYSA-N 0.000 claims 1
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- YNNUSGIPVFPVBX-NHCUHLMSSA-N clemastine Chemical compound CN1CCC[C@@H]1CCO[C@@](C)(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 YNNUSGIPVFPVBX-NHCUHLMSSA-N 0.000 claims 1
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- 229960001271 desloratadine Drugs 0.000 claims 1
- VLARUOGDXDTHEH-UHFFFAOYSA-L disodium cromoglycate Chemical compound [Na+].[Na+].O1C(C([O-])=O)=CC(=O)C2=C1C=CC=C2OCC(O)COC1=CC=CC2=C1C(=O)C=C(C([O-])=O)O2 VLARUOGDXDTHEH-UHFFFAOYSA-L 0.000 claims 1
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- MJJALKDDGIKVBE-UHFFFAOYSA-N ebastine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(=O)CCCN1CCC(OC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 MJJALKDDGIKVBE-UHFFFAOYSA-N 0.000 claims 1
- 229960000325 emedastine Drugs 0.000 claims 1
- KBUZBQVCBVDWKX-UHFFFAOYSA-N emedastine Chemical compound N=1C2=CC=CC=C2N(CCOCC)C=1N1CCCN(C)CC1 KBUZBQVCBVDWKX-UHFFFAOYSA-N 0.000 claims 1
- 229960003592 fexofenadine Drugs 0.000 claims 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
- 229960001375 lactose Drugs 0.000 claims 1
- 229960001120 levocabastine Drugs 0.000 claims 1
- ZCGOMHNNNFPNMX-KYTRFIICSA-N levocabastine Chemical compound C1([C@@]2(C(O)=O)CCN(C[C@H]2C)[C@@H]2CC[C@@](CC2)(C#N)C=2C=CC(F)=CC=2)=CC=CC=C1 ZCGOMHNNNFPNMX-KYTRFIICSA-N 0.000 claims 1
- 229960003088 loratadine Drugs 0.000 claims 1
- JCCNYMKQOSZNPW-UHFFFAOYSA-N loratadine Chemical compound C1CN(C(=O)OCC)CCC1=C1C2=NC=CC=C2CCC2=CC(Cl)=CC=C21 JCCNYMKQOSZNPW-UHFFFAOYSA-N 0.000 claims 1
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- 229920001542 oligosaccharide Polymers 0.000 claims 1
- 150000002482 oligosaccharides Chemical class 0.000 claims 1
- 229960003910 promethazine Drugs 0.000 claims 1
- 229960004793 sucrose Drugs 0.000 claims 1
- 229960000351 terfenadine Drugs 0.000 claims 1
- 229960003223 tripelennamine Drugs 0.000 claims 1
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- 206010008631 Cholera Diseases 0.000 description 2
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- 238000010521 absorption reaction Methods 0.000 description 2
- 229960004543 anhydrous citric acid Drugs 0.000 description 2
- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 description 2
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Landscapes
- Medicinal Preparation (AREA)
Abstract
An orally-disintegrating tablet of bergenin for treating cough, chronic trachetitis and other inflammations is prepared from bergenin, filler, disintegrant, flavouring, flow aid, lubricant, and optional adhesive or coating and effervescent agent.
Description
Technical field
The present invention relates to a kind ofly have antitussive, eliminate the phlegm, effects such as antiinflammatory, analgesic, antiviral, and the Bergeninum that can comprehensive treatment chronic tracheitis and the oral cavity disintegration tablet and the preparation technology thereof of bergenini compositae tabellae.
Background technology
Bergeninum is the isocoumarin compounds that obtains from Xinjiang saxifragaceae plant Rhizoma Seu Herba Bergeniae refining refinement, studies show that Bergeninum has following effect:
1. potent antitussive: antitussive intensity is equivalent to 1/4th of codeine approximately, cough-relieving rapidly.And to the selective inhibitory action of coughing centre, and other maincenter there is not the obvious suppression effect, the side effect of having avoided morphine class cough medicine maincenter to suppress.
2. potent eliminating the phlegm: the Radix Platycodonis of its action intensity and Isodose is suitable, drives away bronchus pathology secretions, keeps respiratory passage unblocked.Eliminate the parasitic environment of pathogenic microorganism.
3. antiinflammatory action: hyperfunction to the vascular permeability that inflammation is early stage, ooze out with edema remarkable inhibitory action is arranged, and propagation phase inflammation is also had the good restraining effect.Help the bronchitic clinical symptoms of relieve chronic.
Refrigeration function: rabbit is injected cholera, typhoid fever, paratyphoid fever, first by auricular vein recall the heating that vaccine, cholera and Typhoid-Paratyphoid A and B Vaccine and Tetanus Toxoid Complex cause stronger refrigeration function is arranged.
4. antivirus action: but can not only go out DNA viruses, and can suppress RNA viruses.Cell behind the inactivation of viruses still can continue division and go down to posterity, but illustrate that the Bergeninum virus of going out effectively and not injures viral cell of being lodged.
5. promote the pathological tissues restitution: with titanium dioxide stove drying gas manufactured rat chronic tracheitis model, with Bergeninum treatment 10 days, the result shows that the goblet cell of treatment group rat trachea reduces (showing the phlegm-dispelling functions that the sticking amount of name reduces), cell infiltration alleviates, emphysema and pulmonary collapse degree also alleviate, and have solved the treatment problem of the Histological change of chronic bronchitis.
Bergeninum has significant potent antitussive, eliminates the phlegm, antiinflammatory, analgesic, antiviral biological activity, promotes compound actions such as pathological tissues recovery, the effect with comprehensive chronic tracheitis.Succeeding in developing of Bergeninum is the important achievement that traditional Chinese medicine is excavated by China.Antiallergic agent has stronger histamine H1-receptor blocking effect, can alleviate other symptoms of respiratory tract that allergy causes, two medicines cooperate the common outstanding prescription of forming the treatment cough illness.Solved current treatment chronic bronchitis medicine and the single problem of curative effect, promoted therapeutic effect, chronic bronchitis has been had good antitussive, phlegm-dispelling functions
The dosage form of existing Bergeninum and bergenini compositae tabellae preparation mainly is an ordinary tablet.Need a large amount of water to send down when ordinary tablet is taken, this makes many old peoples, infant or dysphagia, fetch water inconvenient patient and cough and asthmatic patient be difficult to take.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 existing Bergeninum and the deficiency of bergenini compositae tabellae aspect peroral dosage form, provide a kind of taking convenience, absorption is rapid-action, bioavailability is high Bergeninum and bergenini compositae tabellae orally disintegrating tablet preparation 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 Bergeninum that can finish to take medicine with saliva hypopharynx and bergenini compositae tabellae oral cavity disintegration tablet and preparation method thereof.
One, prescription
The Bergeninum that reaches of the present invention and the oral cavity disintegration tablet of bergenini compositae tabellae comprise medicine material, need 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.
Supplementary materials such as the compound recipe that Bergeninum or bergenini compositae tabellae and antiallergic agent are formed, filler, disintegrating agent, correctives, fluidizer, lubricant, according to circumstances can also add binding agent, effervescent or coating material, proportioning with suitable forms through specific method for preparing.It is characterized in that its prescription is composed as follows: the compound recipe that Bergeninum or Bergeninum and antiallergic agent are formed (5-70) %, 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 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 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, lactose, fructose, sucrose, protein sugar, maltose alcohol, sorbitol, mannitol, reduction starch sugar, xylitol, reduction BATANG, erithritol, isomerized lactose (lactulose), reduction lactose (lactose), gelatin, glycyrrhizin, Sodium Cyclamate, aspartame, stevioside, cyclamate, 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 bergenini compositae tabellae oral cavity disintegration 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 Bergeninum 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 Bergeninum is carried out powder coating with taste masking.
Concrete preparation method is as follows:
The preprocess method of first step bergenini compositae tabellae:
1. direct flavoring method---this law is granulated to raw material and/or partial supplementary material or is not dealt with, and directly enters for second step;
2. coating taste masking method---get selected coating material, with the dissolving of the solvent that adapts with it and to be diluted to debita spissitudo standby, place ebullated bed to make boiling raw material again, spray into above-mentioned solution with suitable speed then and carry out coating, get coated granule, dry back sieving for standby;
Second step took by weighing correctives and the feed particles after the first step is handled 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.
The specific embodiment
For the better preparation method of explanation bergenini compositae tabellae oral cavity disintegration tablet of the present invention, in conjunction with direct flavoring method, powder coating taste masking method and effervescent flavoring method respectively for an embodiment.For embodiment be in order to further specify the present invention, but limit the present invention never in any form.
Embodiment one direct flavoring method---Bergeninum oral cavity disintegration tablet
One. prescription
1. raw material---Bergeninum 125.0g;
2. binding agent---hydroxypropyl emthylcellulose 2.0g;
3. filler---mannitol 168.0g;
Microcrystalline Cellulose 20.0g;
4. correctives---aspartame 3.5g;
Herba Menthae essence 3.5g;
5. disintegrating agent---crospolyvinylpyrrolidone 10.5g;
Cross-linking sodium carboxymethyl cellulose 10.5g;
6. fluidizer---micropowder silica gel 3.5g;
7. lubricant---magnesium stearate 3.5g.
Amount to 350g, make 1000 altogether.
Two. preparation method
1) get Bergeninum raw material and part mannitol powder and mix the back pulverizing, standby;
2) hydroxypropyl emthylcellulose (preferred 3 to 50 centipoises) is standby with the dissolving of adequate amount of ethanol solution;
3) with step 2) binder solution prepared granulates to the material of step 1), and drying is crossed 26 mesh sieves, and is standby;
4) with micropowder silica gel, Herba Menthae essence, microcrystalline Cellulose and aspartame, sieve, mix homogeneously adds the granule of step 3) again, and mix homogeneously is standby;
5) get mannitol (granular), crospolyvinylpyrrolidone and the cross-linking sodium carboxymethyl cellulose mix homogeneously of surplus, add the material of step 4) again, mix homogeneously adds the magnesium stearate mix homogeneously at last;
6) intermediate detects, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment two coating taste masking method---bergenini compositae tabellae oral cavity disintegration tablets
One. prescription
1. raw material---Bergeninum 125.0g;
Chlorphenamine maleate 2.0g;
2. coating material---ethyl cellulose 18.7g;
Methylcellulose 6.3g;
3. filler---mannitol 147.0g;
Microcrystalline Cellulose 17.5g;
4. correctives---aspartame 2.0g;
Herba Menthae essence 3.5g;
5. disintegrating agent---crospolyvinylpyrrolidone 9.0g;
Cross-linking sodium carboxymethyl cellulose 9.0g;
6. fluidizer---micropowder silica gel 6.5g;
7. lubricant---magnesium stearate 3.5g.
Amount to 350g, make 1000 altogether.
Two. preparation method
1) get chlorphenamine maleate, mix with progressively increase dilution method and Bergeninum, standby;
2) ethyl cellulose and methylcellulose are dissolved with adequate amount of ethanol solution, standby;
3) material with step 1) places fluid bed, with step 2) binder solution prepared carries out coating, and drying is crossed 26 mesh sieves, and is standby;
4) with micropowder silica gel, Herba Menthae essence, microcrystalline Cellulose and aspartame, sieve, mix homogeneously adds the granule of step 3) again, and mix homogeneously is standby;
5) get mannitol (granular), crospolyvinylpyrrolidone and cross-linking sodium carboxymethyl cellulose mix homogeneously, add the material of step 4) again, mix homogeneously adds the magnesium stearate mix homogeneously at last;
6) intermediate detects, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment three effervescent flavoring method---bergenini compositae tabellae oral cavity disintegration tablets
One. prescription
1. raw material---Bergeninum 125.0g;
Chlorphenamine maleate 2.0g;
2. binding agent---hydroxypropyl emthylcellulose 5.0g;
3. effervescent---anhydrous citric acid 33.0g;
Sodium bicarbonate 30.0g;
4. filler---mannitol 148.0g;
PROSOLV
SMCC 16.5g;
5. correctives---aspartame 2.0g;
Fragrant citrus essence 3.5g;
6. disintegrating agent---cross-linking sodium carboxymethyl cellulose 15.0g;
Low-substituted hydroxypropyl cellulose 12.0g;
7. fluidizer---micropowder silica gel 4.0g;
8. lubricant---magnesium stearate 4.0g.
Amount to 400g, make 1000 altogether.
Two. preparation method
1) get chlorphenamine maleate, mix with progressively increase dilution method and Bergeninum, standby;
2) hydroxypropyl emthylcellulose (preferred 3 to 50 centipoises) is dissolved with adequate amount of ethanol solution, standby;
3) get anhydrous citric acid, material and the part mannitol powder of pulverizing back and step 1) mix back step 2) part binder solution fluidized bed granulation, sieve after the drying, standby;
4) get sodium bicarbonate and pulverize back and remaining mannitol powder mix homogeneously,, sieve with remaining binder solution fluidized bed granulation, standby;
5) 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;
6) intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Claims (10)
- One kind have antitussive, eliminate the phlegm, effect such as antiinflammatory, analgesic, antiviral, and the Bergeninum of the comprehensive treatment chronic tracheitis of energy and the oral cavity disintegration tablet of bergenini compositae tabellae, supplementary materials such as the compound recipe raw material of forming by Bergeninum or Bergeninum and antiallergic agent, filler, disintegrating agent, correctives, fluidizer, lubricant, according to circumstances can also add binding agent, effervescent or coating material, proportioning with suitable forms through specific method for preparing.It is characterized in that its prescription is composed as follows: compound recipe raw material (5-70) % that Bergeninum or Bergeninum and antiallergic agent are formed, 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. the antiallergic agent of addressing according to claim 1 of being addressed, include but are not limited to promethazine, chlorphenamine, sodium cromoglicate, tripelennamine, terfenadine, astemizole, azelastine, cetirizine, ebastine, levocabastine, emedastine, mizolastine, clemastine, fexofenadine, loratadine, Desloratadine etc. and various forms of salt thereof, can use use also capable of being combined separately; The preferred chlorphenamine maleate that uses.
- 3. 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 microcrystalline Cellulose, PROSOLV SMCC, mannitol (granular or powdery), xylitol, sorbitol, maltose (pure), Chi ?alcohol, polymerization sugar (EMDEX ), coupling sugar, glucose, sucrose, fructose, oligosaccharide, levulose, lactose, isomerized lactose (lactulose), reduction lactose (lactose), dextrin, reduction starch sugar, reduction BATANG 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, lactose, fructose, sucrose, protein sugar, maltose alcohol, sorbitol, mannitol, reduction starch sugar, xylitol, reduction BATANG, erithritol, isomerized lactose (lactulose), reduction lactose (lactose), gelatin, glycyrrhizin, Sodium Cyclamate, aspartame, stevioside, cyclamate, 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.
- 4. one kind is used for the Bergeninum that claim 1 addresses or the preparation method of bergenini compositae tabellae oral cavity disintegration tablet, it is characterized in that being made up of following steps:The pretreatment of first step raw material, can take following two kinds of methods:(1) direct flavoring method---this law can be granulated or do not deal with raw material, directly enters for second step;(2) coating taste masking method---get selected coating material, with the dissolving of the solvent that adapts with it and to be diluted to debita spissitudo standby, get raw material again and place ebullated bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get coated granule, dry back sieving for standby;Second step took by weighing correctives and the feed particles after first step taste masking is handled 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.
- 5. the preparation method of addressing according to claim 4 is characterized in that: the method for the first step (2) need be used coating material that raw material is carried out taste masking in advance and handle.
- 6. the preparation method of addressing according to claim 5, it is characterized in that: the coating material that is used for the taste masking processing is 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), any one or two or more mixture such as polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol.
- 7. the method for granulating of addressing according to claim 4 is characterized in that using dry granulation mechanism to be equipped with, and also can use the high-speed stirred mixer-granulator, wave granulator and the preparation of fluid bed one-step-granulating method; The preferred fluid bed marumerization that uses.
- 8. any preparation method of addressing according to claim 4 is characterized in that: according to circumstances also can add the adjuvant effervescent.
- 9. the effervescent of addressing according to claim 7, it is characterized in that: this adjuvant is the mixture of malic acid, citric acid or citric acid and sodium bicarbonate or sodium carbonate.
- 10. one kind is used for the Bergeninum that claim 1 addresses and the preparation method of bergenini compositae tabellae oral cavity disintegration tablet, it is characterized in that it adopts direct compression process preparation technology, and the hardness of tablet is between 10 to 45 newton, and disintegration time is at 1-60 in second.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410093147 CN1660078A (en) | 2004-12-17 | 2004-12-17 | Oral disintegration tablet of bergenin and compound bergenin and preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410093147 CN1660078A (en) | 2004-12-17 | 2004-12-17 | Oral disintegration tablet of bergenin and compound bergenin and preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1660078A true CN1660078A (en) | 2005-08-31 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410093147 Pending CN1660078A (en) | 2004-12-17 | 2004-12-17 | Oral disintegration tablet of bergenin and compound bergenin and preparation method |
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| Country | Link |
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| CN (1) | CN1660078A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101797253A (en) * | 2010-03-18 | 2010-08-11 | 四川大学 | Bergenin and cetirizine dihydrochloride compound oral administration preparation |
| CN103610713A (en) * | 2013-12-12 | 2014-03-05 | 昆明振华制药厂有限公司 | Compound bergenin tablet and preparation method thereof |
| CN106562957A (en) * | 2015-10-08 | 2017-04-19 | 中国科学院微生物研究所 | Application of Compound AJ-2 in the Preparation of Medicines for Treating or Preventing Influenza Viruses |
| WO2019077620A1 (en) * | 2017-10-16 | 2019-04-25 | Council Of Scientific & Industrial Research | Gastroretentive sustained release formulations of bergenia ciliata |
| CN110403910A (en) * | 2019-09-02 | 2019-11-05 | 广东九明制药有限公司 | Desloratadine piece and preparation method thereof |
-
2004
- 2004-12-17 CN CN 200410093147 patent/CN1660078A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101797253A (en) * | 2010-03-18 | 2010-08-11 | 四川大学 | Bergenin and cetirizine dihydrochloride compound oral administration preparation |
| CN103610713A (en) * | 2013-12-12 | 2014-03-05 | 昆明振华制药厂有限公司 | Compound bergenin tablet and preparation method thereof |
| CN103610713B (en) * | 2013-12-12 | 2016-01-20 | 昆明振华制药厂有限公司 | A kind of compound bergenin pills and preparation method |
| CN106562957A (en) * | 2015-10-08 | 2017-04-19 | 中国科学院微生物研究所 | Application of Compound AJ-2 in the Preparation of Medicines for Treating or Preventing Influenza Viruses |
| CN106562957B (en) * | 2015-10-08 | 2019-02-12 | 中国科学院微生物研究所 | Application of compound AJ-2 in preparing medicine for treating or preventing influenza virus |
| WO2019077620A1 (en) * | 2017-10-16 | 2019-04-25 | Council Of Scientific & Industrial Research | Gastroretentive sustained release formulations of bergenia ciliata |
| US11446346B2 (en) * | 2017-10-16 | 2022-09-20 | Council Of Scientific & Industrial Research | Gastroretentive sustained release formulations of Bergenia ciliata |
| CN110403910A (en) * | 2019-09-02 | 2019-11-05 | 广东九明制药有限公司 | Desloratadine piece and preparation method thereof |
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Open date: 20050831 |