CN1247203C - Helicidum oral disintegation tablet and its preparing method - Google Patents
Helicidum oral disintegation tablet and its preparing method Download PDFInfo
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- CN1247203C CN1247203C CN 200410062280 CN200410062280A CN1247203C CN 1247203 C CN1247203 C CN 1247203C CN 200410062280 CN200410062280 CN 200410062280 CN 200410062280 A CN200410062280 A CN 200410062280A CN 1247203 C CN1247203 C CN 1247203C
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Abstract
The present invention discloses a helicidum oral disintegration tablet which is suitable for relieving neurotic headache, dizziness and sleep disorder and assists in treating constitutional headache. The helicidum oral disintegration tablet aims to make up for the shortages of the existing helicidum preparation and provide a helicidum oral disintegration tablet with convenient taking, rapid absorption and high biological availability and a preparation method thereof for extensive patients and medical workers. Helicidum is used as a raw material, a filling agent, a disintegrating agent, a flavoring agent, a flow aid, a lubricating agent, and the like are used as auxiliary materials, an adhesive or a coating material can also be used according to different situations, a proper quantity of effervescent agents can be added according to the circumstances, and then the oral disintegration tablet is prepared by a specific preparation method. The preparation has the characteristics of simple preparation process, short disintegration time and rapid effect taking, and the helicidum oral disintegration tablet can be directly and completely disintegrated in an oral cavity with 60 seconds without water, and be favorable to the dissolution and absorption of medicaments.
Description
[technical field] the present invention relates to a kind of being applicable to and alleviates neurosal headache, giddy and sleep disorder, a kind of oral cavity disintegration tablet of diseases such as auxiliary treatment primary headache.
[background technology] this strain oral tablet that effective component extracting is made from the fruit of Proteaceae radish plant tree Helicid Hilgirica Beed.This product chemical constitution have similar monomer glucosides to Rhizoma Gastrodiae.Prove through pharmacology and clinical research, this product is similar to gastrodine to central nervous system's effect, but its calmness, sleep peacefully, the analgesic effect is strong than gastrodine, the therapeutical effect produce effects of the headache that neurosis is caused, giddy, sleep disorder is fast, general 3～7 days produce effects of medication.This product has certain curative effect to primary headache.
Three, the problem of Cun Zaiing
The dosage form of existing helicide preparation has: drop pill, hard capsule, soft capsule, injection, dispersible tablet and ordinary tablet.
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 remedy the deficiency of existing helicide dosage form, provide to extensive patients and medical personnel that a kind of absorption is fast, bioavailability is high, intestinal is residual few, side effect is low, avoid liver first-pass effect, and needn't drink water, in the oral cavity, only need tens seconds to get final product rapid disintegrate or dissolving, can finish Helicidum oral disintegation tablet of taking medicine and preparation method thereof with saliva hypopharynx.
One, prescription
The Helicidum oral disintegation tablet that reaches of the present invention comprises the material medicine helicide, 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.
1. helicide (10～50) %, 2. binding agent (0.5～5) %,
3. filler (10～80) %, 4. coating material (0～50) %,
5. disintegrating agent (2～30) %, 6. correctives (1～40) %,
7. fluidizer (0.01～5) %, 8. lubricant (0.3～3) %,
9. effervescent (0～30) %.
Wherein:
Binding agent---include but are not limited to starch, pregelatinized Starch, dextrin, maltodextrin, sucrose, arabic gum, methylcellulose, carboxymethyl cellulose, ethyl cellulose, polyvinyl alcohol, Polyethylene Glycol, polyvinylpyrrolidone (PVP), alginic acid and alginate, xanthan gum and hydroxypropyl emthylcellulose (HPMC), can use use also capable of being combined separately.
Coating material---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.
Filler---mannitol, microcrystalline Cellulose, dextrin, lactose, starch, maltodextrin and pregelatinized Starch etc. can be used use also capable of being combined separately.
Disintegrating agent---crospolyvinylpyrrolidone (PPVP), carboxymethyl starch sodium (CMS-Na), low substituted hydroxy-propyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa) etc. can use use also capable of being combined separately.
Correctives---mannitol, lactose, stevioside, gelatin, aspartame, cyclamate, glycyrrhizin, 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.
The mixture of effervescent---malic acid, citric acid or citric acid and sodium bicarbonate or sodium carbonate.Fluidizer---micropowder silica gel, Pulvis Talci, Cab-O-sil, Arosil, hydrated sodium aluminosilicate etc. can use use also capable of being combined separately.
Lubricant---magnesium stearate, glyceryl monostearate, Stepanol MG, Pulvis Talci etc. can use use also capable of being combined separately.
Two, preparation method
The Helicidum oral disintegation tablet that reaches of the present invention, its preparation method are to adopt common press device and direct compression process technology, and the manufacturer with preparation conventional tablet all can adopt.Adopt the oral cavity disintegration tablet of this method preparation to have enough hardness (intensity), can satisfy the requirement of production, packing, accumulating, have good mouthfeel and short disintegration time simultaneously again.
In view of the helicide mildly bitter flavor, the present invention can adopt two kinds of distinct methods to carry out flavoring or taste masking: adopt the direct flavoring of correctives 1.; 2. in advance helicide is carried out powder coating with taste masking, concrete preparation method is as follows: the preprocess method of first step helicide:
1. directly the flavoring method---this law is granulated to the helicide 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 lyase that adapts with it and to be diluted to debita spissitudo standby, getting helicide again places ebullated bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get helicide powder coating 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, meets after saliva separates rapidly or collapse, and borrows and swallows power, and medicine can be gone into the tablet of stomach onset.Oral cavity disintegration tablet needn't be used water delivery service, and saliva can make its disintegrate or dissolving, both can swallow by conventional tablet, can be placed in the water again to take after the disintegrate, also can not need to take medicine with water swallow.Especially provide convenience for old man, children's, dysphagia or the inconvenient person that fetches water take medicine,, then can improve the drug compliance of child patient greatly, solved the problem that it is difficult that infant is taken medicine if adopt certain method to improve its mouthfeel in the preparation.The characteristics of oral cavity disintegration tablet are that absorption is fast, bioavailability is high, intestinal is residual few, side effect is low, avoid liver first-pass effect etc., therefore, oral cavity disintegration tablet is applicable to onset rapidly, and valid density and poisoning concentration differ bigger medicine, and some war wound emergency treatment medicines, NSAID (non-steroidal anti-inflammatory drug), spasmolytic Bendectin and analgesic etc. all relatively are fit to make oral cavity disintegration tablet.Other medicine such as blood drug level are in for a long time than plateau, then easily produce drug resistance, make oral cavity disintegration tablet and then can overcome this problem, produce excellent curative.
According to the disclosed description introduction of No. 03148531.6 patent " FUFANG DANSHEN KOUQIANG BENGJIEPIAN and preparation method ", oral cavity disintegration tablet has the leap of essence than the disintegration rate of drop pill and ordinary tablet, the disintegrate of oral cavity disintegration tablet generally in 30 seconds, is no more than 1 minute at most.And the dissolve scattered time limit of drop pill Chinese Pharmacopoeia regulation is in 30 minutes, and be all molten loosing about 5 minutes the disintegration of conventional tablet Chinese Pharmacopoeia regulation.
The principal indication of helicide is the road stasis of blood resistance of treatment treatment brain, apoplectic hemiplegia, heart arteries and veins stasis of blood the moon, obstruction of qi in the chest and cardialgia; Apoplexy sequela, diseases such as angina pectoris, Most patients is an old group, even there wherein have quite a few patient to swallow food to be not very convenient, and that other most of oral formulations also exist dissolve scattered time limit is long, dissolution is low, absorb relatively poor, problems such as liver sausage first pass effect and bioavailability are lower, add injection again and often be easy to generate anaphylaxis or untoward reaction etc. again, it is big simultaneously yet to exist operation easier, the patient suffering is also big, make and the medical treatment cost height, the shortcoming that patient economy burden is heavy, the helicide Orally-disintegrating tablet that reaches therefore of the present invention, it is more outstanding that its advantage just seems.
[specific embodiment] is in order better to illustrate the preparation method of Helicidum oral disintegation tablet of the present invention, in conjunction with directly flavoring method and powder coating taste masking method are as follows for an embodiment respectively:
Embodiment 1 direct flavoring method
One, prescription
1. raw material---helicide 250.0g;
2. binding agent---PVP-K30 5.0g;
3. filler---lactose 150.0g;
Mannitol 922.0g;
4. fluidizer---micropowder silica gel 15.0g;
5. disintegrating agent---crospolyvinylpyrrolidone 40.0g;
L-HPC?80.0g；
6. correctives---aspartame 8.0g;
Ginseng essence 15.0g;
7. lubricant---magnesium stearate 15.0g;
Gross weight 1500.0g makes 10000, the 150mg/ sheet altogether.
Two, preparation method
The first step is got helicide, does binding agent with PVP-K30, and wet granulation is crossed 20 mesh sieve granulate, and 30 mesh sieve granulate are crossed in oven dry, make the helicide granule, and are standby;
Second step was got the residue adjuvant mix homogeneously except that magnesium stearate, and the helicide granule that will make again adds and mix homogeneously, adds magnesium stearate and mix homogeneously at last;
The 3rd step intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment 2 contains effervescent flavoring method
One, prescription
1. raw material---helicide 250.0g;
2 filleies---mannitol 762.0g;
3. effervescent---citric acid 160.0g;
Sodium bicarbonate 140.0g;
4. fluidizer---micropowder silica gel 15.0g;
5. disintegrating agent---crospolyvinylpyrrolidone 120.0g;
6. correctives---aspartame 8.0g;
Fructus Citri tangerinae essence 30.0g;
7. lubricant---magnesium stearate 15.0g;
Gross weight 1500.0g makes 10000, the 150mg/ sheet altogether.
Two, preparation method
The first step is got citric acid and sodium bicarbonate pulverize separately, sifts out 20 order to 60 purpose granules, and is standby;
Second step was got the residue supplementary material mix homogeneously except that magnesium stearate, and citric acid that will make and sodium bicarbonate particle add and mix homogeneously again, add magnesium stearate and mix homogeneously at last;
The 3rd step intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Embodiment 3 powder coating taste masking methods
One, prescription
1. raw material---helicide 250.0g;
2 filleies---mannitol 1019.5g;
3. coating material---Eudragit E100 40.0g;
Eudragit NE30D (doing) 10.0g;
4. fluidizer---micropowder silica gel 22.5g;
5. disintegrating agent---crospolyvinylpyrrolidone 120.0g;
6. correctives---aspartame 8.0g;
Ginseng essence 15.0g;
7. lubricant---magnesium stearate 15.0g;
Gross weight 1500.0g makes 10000, the 150mg/ sheet altogether.
Two, preparation method
The first step is got Eudragit E100 and Eudragit NE30D with the medicinal industrial alcohol dissolving more than 95% and to be diluted to finite concentration standby;
Second step got helicide and places ebullated bed to seethe with excitement, and sprayed into above-mentioned solution by certain speed and carried out powder coating, made helicide powder coating granule, and the 0.6mm sieve is crossed in dry back, and is standby.
The 3rd the step with mannitol, micropowder silica gel, crospolyvinylpyrrolidone, aspartame and ginseng essence mix homogeneously, again and sieve after the coated granule mixing, add magnesium stearate at last, mixing,
The 4th step intermediate content detection, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
Disintegration of the foregoing description and slice, thin piece hardness numerical value are as follows:
| Embodiment | Disintegration (second) | Slice, thin piece hardness (newton) |
| 1 2 3 | ＜43 seconds＜50 seconds＜38 seconds | 17-35 20-33 18-28 |
Claims (2)
1 one kinds of Helicidum oral disintegation tablets, it is characterized in that its weight consists of helicide 10-50%, coating material polypropylene acid resin 3.3-50%, disintegrating agent crospolyvinylpyrrolidone 2-30%, filler 10-80%, correctives 1-40%, fluidizer 0.01-5% and lubricant 0.3-3% form, 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 one or more; After wherein helicide being carried out powder coating with coating material, the gained granule is pressed into disintegrating tablet with other adjuvant.
The preparation method of 2 Helicidum oral disintegation tablets that reach according to claim 1 is characterized in that being made up of following steps:
(1) pretreatment of helicide; Get selected coating material, with the dissolving of the solvent that adapts with it and to be diluted to debita spissitudo standby, get helicide again and place fluid bed to make boiling, spray into above-mentioned solution with suitable speed then and carry out powder coating, get helicide powder coating granule, dry back sieving for standby;
(2) correctives and the feed particles after first step taste masking is handled are taken by weighing according to quantity, and mix homogeneously is standby;
(3) filler, disintegrating agent, fluidizer are taken by weighing according to quantity also mix homogeneously, make evenly again with through second mixing of materials that goes on foot gained, add the lubricant mixing, standby;
(4) the gained material detects through intermediate, determine that sheet is heavy after, send into the tablet machine tabletting promptly.
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| CN 200410062280 CN1247203C (en) | 2004-07-05 | 2004-07-05 | Helicidum oral disintegation tablet and its preparing method |
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| CN 200410062280 CN1247203C (en) | 2004-07-05 | 2004-07-05 | Helicidum oral disintegation tablet and its preparing method |
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| CN1247203C true CN1247203C (en) | 2006-03-29 |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102198160B (en) * | 2010-05-06 | 2012-10-03 | 成都科尔医药技术有限公司 | Medicine composition for treating headache or insomnia as well as preparation method and purpose thereof |
| CN102824353B (en) * | 2011-06-14 | 2015-11-25 | 上海现代药物制剂工程研究中心有限公司 | A kind of helicide oral formulations and its preparation method and application |
| CN103169716A (en) * | 2011-12-26 | 2013-06-26 | 昆明贝克诺顿制药有限公司 | Compound medicinal composition for treating pain |
| CN104069119B (en) * | 2013-03-29 | 2016-05-18 | 昆明制药集团股份有限公司 | A kind of application of helicidum and preparation |
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