CN1273115C - Quick acting and heart resurrecting oral disintegrating tablet and its preparation process - Google Patents
Quick acting and heart resurrecting oral disintegrating tablet and its preparation process Download PDFInfo
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- CN1273115C CN1273115C CN 200410019985 CN200410019985A CN1273115C CN 1273115 C CN1273115 C CN 1273115C CN 200410019985 CN200410019985 CN 200410019985 CN 200410019985 A CN200410019985 A CN 200410019985A CN 1273115 C CN1273115 C CN 1273115C
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- borneolum syntheticum
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Abstract
The present invention relates to a quick acting and heart resurrecting oral disintegrating tablet and a preparation process thereof, which belongs to an oral disintegrating type traditional Chinese medicine preparation containing easily subliming medicinal components and a preparation technology thereof. The problems are solved that an effective constituent, namely borneol is easy to sublime to make medicinal effect content unstable in the process of producing and storing quick acting and heart resurrecting medicines at present, and comatose patients and patients with serious diseases can not take the medicines conveniently. In the present invention, the borneol is prepared into solid microcapsules (ball) or dispersive bodies which are uniformly mixed with szechwan lovage rhizome, a corrective, a bulking agent, a disintegrating agent, a lubricating agent and glidant and then processed through sieving and tabletting so as to obtain the oral disintegrating tablet through a modern package technology. The preparation can be taken conveniently and sufficiently disintegrated without taking water in the mouth cavity, and the operation of disintegration can be completed within 10 to 50 seconds so as to rapidly obtain the effects of efficiently releasing the medicine, rapidly taking effects and early peaking. Accordingly, the oral disintegrating tablet is especially suitable for partial patients with dysphagia or narcose patients to take with conspicuous curative effects. The present invention has the advantages of simple and direct preparation processes, optimized working environment and obtained economic benefit and social benefit.
Description
Technical field
The invention belongs to a kind of Chinese patent medicine mouth and collapse type preparation and preparation method, relate to a kind of fast-acting heart disease curing oral cavity disintegration tablet that the drug effect stable content contains Borneolum Syntheticum medicine carrying microcapsule or solid dispersion medicine carrying microgranule and preparation method thereof that makes; Be particularly related to and have coronary blood flow increasing, allevating angina pectoris, cure mainly coronary heart disease, uncomfortable in chest, feel suffocated, precordialgia, taking convenience, rapid-action to indication, fast-acting heart disease curing oral cavity disintegration tablet and preparation method thereof.
Background technology
SUXIAO JIUXIN WAN is a kind of Chinese patent medicine of classics, effect such as have calmness, ease pain, resist myocardial ischemia.Be used for coronary heart disease, uncomfortable in chest, feel suffocated, treatment of conditions such as precordialgia.But traditional pill often has absorption not exclusively, has shortcomings such as slow curative effect, and takes inconvenience for the stupor critically ill patient.As fast-acting heart disease curing drop pill, containing needs about 5 minutes, and onset is slow, influences first aid.Though liquid preparation has been avoided containing process, it is not easy to store and carry, and to dysphagia person, often easily medicinal liquid is choked into trachea.
Oral cavity disintegration tablet (orally disiuteg rating tablet) is the novel form of developing in recent years.Compare this dosage form with conventional tablet and need not water and also need not to chew, medicine places on the tongue, and meeting saliva can rapid disintegrate, borrows the swallowing act onset.Also can put the Sublingual, medicine passes through the mucosa absorption onset after the disintegrate rapidly.Current many Western medicine are made oral cavity disintegration tablet, and effect is fine, but traditional Chinese medicine mouth disintegrating tablet there be limited evidence currently of particularly to Chinese medicine volatile, the distillation composition, is not seen the report of making oral cavity disintegration tablet as yet on the market.
Existing commercially available fast-acting heart disease curing preparation also exists drug effect content problem of unstable.Its reason is the main component Borneolum Syntheticum of this medicine, and easily distillation institute extremely.Borneolum Syntheticum as the medicine of having one's ideas straightened out, plays the effect of " fragrance is walked to scurry, and priming is up " in the fast-acting heart disease curing medicament in homeland pharmacy, be to alleviate one of main component uncomfortable in chest.Because this medicine exists the physical property of easy distillation, cause it to have many difficult problems all the time in the routine production of China's Chinese formulated products with in storing; As since the distillation of Borneolum Syntheticum make its in production technology for the content that guarantees it have to high limit feed intake, not only waste herb resource but also make production environment abominable, the workman is difficult to stand; Because the Borneolum Syntheticum distillation causes effective content constantly to run off in patent medicine, unstable before the deadline to messenger drug with content, through accelerated test and keep sample see bright some the annual before the deadline Borneolum Syntheticum composition distillation of the Chinese patent medicine number of dropouts that contains Borneolum Syntheticum of verification unexpectedly can be up to 30% about, be one of technical barrier of the current obstacle modernization of Chinese medicine; The medicinal content standard of stable and controllable has for want of limited it and has obtained the international market access smoothly again; Because Borneolum Syntheticum distils and causes a lot of difficulties to the preparation packing that contains Borneolum Syntheticum, outward appearance, often, the Borneolum Syntheticum sublimate returns goods because of polluting as the transparent plastic packaging of modern patent medicine " bubble eye " packing.Above problem needs to be resolved hurrily.The novel form of developing this medicine is imperative.
In sum, adopting modern medicinal agents technology and novel medicinal auxiliary material, seek to be suitable for parcel drug delivery technologies volatile, the distillation medicine, is the key of the modernization of Chinese medicine; Preparation fast-acting heart disease curing novel form one oral cavity disintegration tablet is the task of top priority.
Summary of the invention
The problem that solves:
At above-mentioned situation, easily distil in order to solve Borneolum Syntheticum, cause SUXIAO JIUXIN WAN drug effect content instability and stupor, critically ill patient are taken inconvenient problem.A kind of modernization parcel drug delivery technologies is provided and take conveniently, rapid-action to indication, reach the peak early, fast-acting heart disease curing oral cavity disintegration tablet evident in efficacy.Thereby for this medicine has increased novel form.
Technical scheme:
Fast-acting heart disease curing oral cavity disintegration tablet, medicinal ingredient are Rhizoma Chuanxiong and Borneolum Syntheticum, and its each composition pharmaceutical dosage is according to the common dose of ministry standard WS3-B-3484-98 regulation, and the quality of two flavor Chinese medicines is 40%～60% than Rhizoma Chuanxiong, and Borneolum Syntheticum is 60%～40%.
The oral cavity disintegration tablet prescription is by weight percentage:
Medicinal ingredient 3.8～18.9%
Filler 48.0～71.0%
Disintegrating agent 9.0～27.8%
Correctives 0.5～1.1%
Lubricant 0.9～2.1%
Fluidizer 0.9～2.1%
Need to prove:
The volatile oil that the form of being used as medicine of medicinal ingredient Rhizoma Chuanxiong is that the water of this medical material is carried, alcohol extraction, ether are carried, a kind of method in the supercritical extraction, vapor extraction method obtains, or parcel medicine carrying microcapsule, the microsphere of volatile oil, or the direct ground product of medical material, the form of being used as medicine of medicinal ingredient Borneolum Syntheticum is its solid dispersion, parcel medicine carrying microcapsule, microsphere.
Borneolum Syntheticum is that fast-acting heart disease curing is alleviated one of main component uncomfortable in chest.Pharmacy procedure of the present invention is made Borneolum Syntheticum solid dispersion or is wrapped up medicine carrying microcapsule, microsphere, runs off in order to the distillation of restriction Borneolum Syntheticum.Because of Borneolum Syntheticum has been dispersed on the solid dispersion soluble in water, has improved this water-fast medicine of Borneolum Syntheticum and in water, dissolved and dispersibility again.
Above-mentioned filler is selected from one or both in microcrystalline Cellulose, dextrin, lactose, starch or the mannitol.
Disintegrating agent is selected from one or both in low substituent group hydroxypropyl methylcellulose (L-HPC), crospolyvinylpyrrolidone (PVPP), crosslinked carboxymethyl fecula sodium (CCMS-Na) or the cross-linking sodium carboxymethyl cellulose (CMC-Na).
Above-mentioned solid dispersion carrier is selected from Polyethylene Glycol, and (being PEG-6000, PEG-4000, PEG-12000, PEG-60000), polyvinylpyrrolidone (are PVP-K
15, K
30, K
60, K
90) and beta-schardinger dextrin-and derivant thereof in one or both.
Correctives is selected from one or both in Mentholum, Oleum menthae, stevioside or the aspartame.
Lubricant is selected from one or both in magnesium stearate, Stepanol MG, the Pulvis Talci.
Fluidizer is selected from one or both in micropowder silica gel, the Pulvis Talci.
The concrete steps of oral cavity disintegration tablet preparation are as follows:
(1) selection of medicinal ingredient and pretreatment
The selection of medicinal ingredient:
The volatile oil that the form of being used as medicine of medicinal ingredient Rhizoma Chuanxiong is that the water of this medical material is carried, alcohol extraction, ether are carried, a kind of method in the supercritical extraction, vapor extraction method obtains, or parcel medicine carrying microcapsule, the microsphere of volatile oil, or the direct ground product of medical material.
The form of being used as medicine of medicinal ingredient Borneolum Syntheticum is its solid dispersion, parcel medicine carrying microcapsule, microsphere.
The pretreatment of medicinal ingredient:
The volatile oil of above-mentioned medical material, the ground product of medical material are all by the pharmacopeia predetermined processing.
The preparation method of above-mentioned parcel medicine carrying microcapsule or microsphere is:
Adopt coacervation or interfacial polymerization; Medicinal ingredient and capsule material are dissolved in the pharmacopeia regulation can be used in the organic solvent of pharmacy, form organic facies; Water intaking in addition, the surfactant of adding 2～3% disperses, and forms water; Water is fully stirred or ultrasound condition under, organic facies is at the uniform velocity splashed into aqueous phase, under the cross-linking agent effect, carry out crosslinked and solidify, obtain medicinal parcel medicine carrying microcapsule or microsphere; The water extraction organic solvent that reuse is excessive, just can obtain discharging medicinal ingredient, runny parcel medicine carrying microcapsule or microsphere powder.Above-mentioned stirring or ultrasonic time 0.5～2 hour; Be not less than 2 hours crosslinked and hardening time.It is pointed out that above-mentionedly in preparation parcel medicine carrying microcapsule, capsule material concentration is 1～10% in the organic facies.
Wherein the capsule material is selected from natural and the synthetic high polymer pharmaceutic adjuvant, and natural polymer medical adjuvant comprises gelatin, arabic gum, sodium alginate, cellulose and cellulosic derivant, chitosan; The synthetic high polymer pharmaceutic adjuvant comprises the copolymer of poly-methyl-prop diluted acid, polymethyl acrylate, poly-methyl-prop diluted acid and poly-methyl-prop diluted acid ester, Youteqi E-100, Youteqi EPO, polyvinyl alcohol, the 1-3 kind in polyvinylpyrrolidone and the Polyethylene Glycol.Organic solvent is selected from the organic solvent of approval usefulness in the pharmacopeia, as ethanol, ethyl acetate, Ethyl formate and chloroform.Surfactant is selected from tween, class of department, sodium lauryl sulphate, polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol.Plasticizer such as citric acid, triethyl citrate, Polyethylene Glycol, cross-linking agent such as formaldehyde and glutaraldehyde.
Rhizoma Chuanxiong is handled through said method, promptly obtains drug loading and be 60～90% solid Rhizoma Chuanxiong microcapsule or microsphere, and its particle diameter is 1～100um;
Borneolum Syntheticum is handled through said method, promptly obtains drug loading and be 50～30% Borneolum Syntheticum medicine carrying microcapsule, microsphere or solid dispersion microparticle, and its particle diameter is 1～100um;
(2) film-making
All mixed tabletting:
Medicinal ingredient and correctives pulverize separately are crossed 80 mesh sieves, take by weighing respectively by above-mentioned formula ratio, mix homogeneously, in addition filler, disintegrating agent, fluidizer, lubricant are crossed 80 mesh sieves respectively, by formula ratio take by weighing respectively, mix homogeneously, all mix with the ingredient that is mixed with correctives again, sieve, tabletting; Tabletting adopts conventional tablet pharmaceutical equipment and pressing process can make oral cavity disintegration tablet.
Beneficial effect:
The invention provides a kind of modernized drug delivery technologies of easy distillation Chinese medicine and a kind of taking convenience, the fast-acting heart disease curing oral cavity disintegration tablet rapid-action, evident in efficacy to indication.It uses modern solid dispersion technology and novel medicinal auxiliary material, utilizes the strongly hydrophilic carrier, increases the dissolubility and the dissolution rate of insoluble medicine, improves bioavailability of medicament.Use technique for packing and Rhizoma Chuanxiong and Borneolum Syntheticum can be prepared into solid parcel medicine carrying microcapsule, microsphere or dispersion, to guarantee that oral cavity disintegration tablet is in the loss that can not distil of the lay up period Borneolum Syntheticum of medicine, effective ingredient has rhythm and pace of moving things ground to discharge, and guarantees pharmaceutical effectiveness and the stable content of storage period; Solved currently in producing and storing, effective ingredient-Borneolum Syntheticums such as SUXIAO JIUXIN WAN easily distil, the drug effect content problem of unstable of bringing.Synergism by parcel medicine carrying dispersion technology and disintegrating agent, reach drug oral after, need be not moisture in the oral cavity, just fully disintegrate.The preparation disintegration time can be finished in 10～50 seconds, and did not have sand type.Drug effect is fast, reach the peak early, have no side effect, avirulence, be the old man or swallowed the ideal administering mode of impaired patients.It can promptly alleviate uncomfortable in chest, distressed, is convenient to coronary heart disease patient's first aid and prevention; Thereby solved stupor, critically ill patient and taken inconvenience, the slow problem of onset, and utilized carrier can also cover the bad smell of medicine.The present invention has not only increased novel form for traditional fast-acting heart disease curing medicine, and its preparation method is simple and direct, preparation process resistance is little, use conventional tablet pharmaceutical equipment, i.e. directly compressible production.In addition,, optimized production environment, improved drug quality, both had an economic benefit, social benefit has been arranged again owing to controlled the easily problem of distillation of Borneolum Syntheticum.
Below in conjunction with specific embodiment, the present invention will be further described.Its specific embodiments only is construed as to illustrating, but not any way limits the scope of the invention.
The specific embodiment
Embodiment 1:
The selection of medicinal ingredient and pretreatment
Get 1 kilogram of Rhizoma Chuanxiong, ethanol 10 rises up in the retort, heats back gold-plating, extracts 10 hours, concentrating under reduced pressure reclaims ethanol and volatile oil, merges volatile oil and concentrate.Get above-mentioned volatile oil 10g, join among the alcoholic solution 50g that contains the strange E-100 of 6% You Te, make oil phase.Other 1000ml that fetches water adds Polyethylene Glycol 30g and disperses, and forms water; Water is being carried out under the stirring condition organic facies is at the uniform velocity splashed into aqueous phase, obtaining medicinal Rhizoma Chuanxiong parcel medicine carrying microcapsule through crosslinked, curing; The excessive water 1000ml of reuse extracts organic solvent, more after filtration, drying, obtains discharging medicinal ingredient, runny parcel Rhizoma Chuanxiong medicine carrying microcapsule.Drug loading is 80% solid Rhizoma Chuanxiong microcapsule or microsphere, and its particle diameter is 1～100um.
Get Borneolum Syntheticum 10g, be dissolved in the 50ml ethanol, add polyvinylpyrrolidone and each 0.5g of ethyl cellulose, form oil phase, other 1000ml that fetches water adds 30g sodium lauryl sulphate and 0.5g Polyethylene Glycol, disperses the formation water; Water is being carried out under the stirring condition organic facies is at the uniform velocity splashed into aqueous phase, obtaining medicinal Borneolum Syntheticum parcel medicine carrying microcapsule through crosslinked, curing; With excessive water extraction organic solvent, more after filtration, drying, obtain to discharge medicinal ingredient, runny parcel Borneolum Syntheticum medicine carrying microcapsule.
The Chinese medicine Borneolum Syntheticum is handled through said method, promptly obtains drug loading and be 30% Borneolum Syntheticum medicine carrying microcapsule, and its particle diameter is 1～100um.
Film-making
Prescription (by weight) component is:
Medicinal ingredient medicine carrying Rhizoma Chuanxiong 4.40g
Medicine carrying Borneolum Syntheticum 5.60g
Microcrystalline Cellulose 14.6g
Mannitol 22g
Cross-linking sodium carboxymethyl cellulose 12.00g
Aspartame 0.15g
Herba Menthae 0.15g
Magnesium stearate 0.55g
Micropowder silica gel 0.55g
It makes 1000
Concrete preparation method is:
Cross 80 mesh sieves with giving first medicine carrying Rhizoma Chuanxiong for preparing and Borneolum Syntheticum medicinal ingredient and aspartame, Herba Menthae pulverize separately, mix homogeneously takes by weighing cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose, mannitol, micropowder silica gel, magnesium stearate again and crosses 80 mesh sieves respectively.Take by weighing respectively by recipe quantity, mix homogeneously mixes with the medicinal ingredient that is mixed with correctives aspartame, Herba Menthae, crosses 80 mesh sieves respectively, uses conventional tablet pharmaceutical equipment and pressing process tabletting, can make oral cavity disintegration tablet.This oral cavity disintegration tablet disintegration in 37 ℃ of aqueous mediums is 20～30 seconds.
Embodiment 2:
The selection of medicinal ingredient and pretreatment and film-maker send out with embodiment 1.
Film-making prescription (by weight) component is:
Medicinal ingredient medicine carrying Rhizoma Chuanxiong 4.40g
Medicine carrying Borneolum Syntheticum 5.60g
Microcrystalline Cellulose 19.0g
Mannitol 14.4g
Carboxymethyl starch sodium 15.0g
Herba Menthae 0.25g
Stevioside 0.05g
Magnesium stearate 0.65g
Micropowder silica gel 0.65g
Make 1000 altogether
Film-making: concrete preparation method is:
With stevioside, Herba Menthae and medicine carrying Rhizoma Chuanxiong, Borneolum Syntheticum, pulverize separately, mix homogeneously is crossed 80 mesh sieves.Press recipe quantity and in addition carboxymethyl starch sodium, microcrystalline Cellulose, mannitol, micropowder silica gel, magnesium stearate crossed 80 mesh sieves respectively, mix homogeneously, again be mixed with stevioside and mix, sieve with the medicinal ingredient of Herba Menthae, tabletting makes oral cavity disintegration tablet.This oral cavity disintegration tablet disintegration in 37 ℃ of water is 20～30 seconds.
Embodiment 3:
The selection of medicinal ingredient and pretreatment and film-maker send out with embodiment 1.
Prescription (by weight) component is:
Medicinal ingredient medicine carrying Rhizoma Chuanxiong 4.40g
Medicine carrying Borneolum Syntheticum 5.60g
Microcrystalline Cellulose 21.00g
Mannitol 15.60g
Crospolyvinylpyrrolidone 12.00g
Stevioside 0.05g
Herba Menthae 0.25g
Magnesium stearate 0.55g
Micropowder silica gel 0.55g
Make 1000 altogether
Concrete preparation method is:
With stevioside and medicine carrying Rhizoma Chuanxiong, Borneolum Syntheticum pulverize separately, cross 80 mesh sieves, take by weighing mix homogeneously by recipe quantity.With cross-linked pvp, microcrystalline Cellulose, mannitol, micropowder silica gel, magnesium stearate are crossed 80 mesh sieves respectively, take by weighing mix homogeneously by recipe quantity in addition.With the medicinal ingredient that the is mixed with stevioside mix homogeneously that sieves, tabletting promptly gets oral cavity disintegration tablet again, and this oral cavity disintegration tablet disintegration in 37 ℃ of aqueous mediums is 40～50 seconds.
Embodiment 4:
The selection of medicinal ingredient and pretreatment:
Get 1 kilogram of Rhizoma Chuanxiong, ethanol 10 rises up in the retort, heats back gold-plating, extracts 10 hours, concentrating under reduced pressure reclaims ethanol and volatile oil, merges volatile oil and concentrate.Get above-mentioned volatile oil 10g, join and contain 4% gelatin, among the water-soluble 40ml of 4% arabic gum, add fine little plain stirring of 1g ethoxy again it is fully mixed, form organic facies.Other 1000ml that fetches water adds the 30g Polyethylene Glycol, disperses, and forms water; Under to water stirring or ultrasound condition, organic facies at the uniform velocity is added drop-wise to aqueous phase, add 20% formaldehyde and 50% glutaraldehyde 5ml again, adjusting pH value to 8～9 are crosslinked, curing obtained medicinal Rhizoma Chuanxiong parcel medicine carrying microcapsule in 2 hours; Again after filtration, drying, obtain discharging medicinal ingredient, runny parcel Rhizoma Chuanxiong medicine carrying microcapsule.
Get Borneolum Syntheticum 10g, be dissolved in the 50ml ethanol, add 3g polyvinylpyrrolidone and 1g ethyl cellulose, form oil phase, other 1000ml that fetches water adds the sodium lauryl sulphate and the Polyethylene Glycol of 10g of 10g, disperses the formation water; Water is being carried out under the stirring condition organic facies is at the uniform velocity splashed into aqueous phase, obtaining medicinal Borneolum Syntheticum parcel medicine carrying microcapsule through crosslinked, curing; The water extraction organic solvent that reuse is excessive more after filtration, drying, obtains discharging medicinal ingredient, runny parcel Borneolum Syntheticum medicine carrying microcapsule.
Film-making: prescription (by weight) component is:
Medicinal ingredient medicine carrying Rhizoma Chuanxiong 4.40g
Medicine carrying Borneolum Syntheticum 5.60g
Lactose 10.7g
Starch 24.2g
Crospolyvinylpyrrolidone 13.7g
Aspartame 0.15g
Herba Menthae 0.15g
Stepanol MG 0.55g
Micropowder silica gel 0.55g
It makes 1000
Concrete preparation method is:
Cross 80 mesh sieves, mix homogeneously with giving first medicine carrying Rhizoma Chuanxiong for preparing and Borneolum Syntheticum medicinal ingredient and aspartame, Herba Menthae pulverize separately; Take by weighing crospolyvinylpyrrolidone, lactose, starch, micropowder silica gel, Stepanol MG again, cross 80 mesh sieves respectively.Take by weighing respectively by recipe quantity, mix homogeneously mixes with the medicinal ingredient that is mixed with correctives aspartame, Herba Menthae, crosses 80 mesh sieves respectively, uses conventional tablet pharmaceutical equipment and pressing process tabletting, can make oral cavity disintegration tablet.This oral cavity disintegration tablet is in 37 ℃ of aqueous mediums, and be 20～30 seconds disintegration.
Embodiment 5:
The selection of medicinal ingredient and pretreatment and film-maker send out with embodiment 1.
Film-making prescription (by weight) component is:
Medicinal ingredient medicine carrying Rhizoma Chuanxiong 6g
Medicine carrying Borneolum Syntheticum 4g
Dextrin 20g
Lactose 13.4g
Carboxymethyl starch sodium 15.0g
Herba Menthae 0.25g
Stevioside 0.05g
Magnesium stearate 0.65g
Micropowder silica gel 0.65g
Make 1000 altogether
Cross 80 mesh sieves, mix homogeneously with giving first medicine carrying Rhizoma Chuanxiong for preparing and Borneolum Syntheticum medicinal ingredient and stevioside, Herba Menthae pulverize separately; Take by weighing carboxymethyl starch sodium, lactose, dextrin, micropowder silica gel, magnesium stearate again, cross 80 mesh sieves respectively.Take by weighing respectively by recipe quantity, mix homogeneously mixes with the medicinal ingredient that is mixed with correctives stevioside, Herba Menthae, crosses 80 mesh sieves respectively, uses conventional tablet pharmaceutical equipment and pressing process tabletting, can make oral cavity disintegration tablet.This sheet disintegration in 37 ℃ of aqueous mediums is 30～40 seconds.
Embodiment 6:
The selection of medicinal ingredient and pretreatment and film-maker send out with embodiment 1.
Its film-making prescription (by weight) component is:
Medicinal ingredient medicine carrying Rhizoma Chuanxiong 4.4g
Borneolum Syntheticum 5.6g
Microcrystalline Cellulose 21g
Mannitol 15g
Crospolyvinylpyrrolidone 11.4g
Stevioside 0.15g
Herba Menthae 0.25g
Magnesium stearate 1.1g
Pulvis Talci 1.1g
Cross 80 mesh sieves, mix homogeneously with giving first medicine carrying Rhizoma Chuanxiong for preparing and Borneolum Syntheticum medicinal ingredient and stevioside, Herba Menthae pulverize separately; Take by weighing crospolyvinylpyrrolidone, microcrystalline Cellulose, mannitol, Pulvis Talci and magnesium stearate again, cross 80 mesh sieves respectively.Take by weighing respectively by recipe quantity, mix homogeneously mixes with the medicinal ingredient that is mixed with flavoring stevioside and Herba Menthae, crosses 80 mesh sieves respectively, uses conventional tablet pharmaceutical equipment and pressing process tabletting, can make oral cavity disintegration tablet.This sheet disintegration in 37 ℃ of aqueous mediums is 30～40 seconds.
Claims (9)
1. fast-acting heart disease curing oral cavity disintegration tablet, medicinal ingredient is Chinese medicine Rhizoma Chuanxiong, Borneolum Syntheticum, its pharmaceutical dosage is by ministry standard WS
3The common dose of-B-3484-98 regulation, the mass ratio of two flavor Chinese medicines is a Rhizoma Chuanxiong 40%～60%, Borneolum Syntheticum is 60%～40%, it is characterized in that, the volatile oil that the form of being used as medicine of medicinal ingredient Rhizoma Chuanxiong is that the water of this medical material is carried, alcohol extraction, ether are carried, a kind of method in the supercritical extraction, vapor extraction method obtains and parcel medicine carrying microcapsule, the microsphere of concentrate, or the solid ground product of medical material; The form of being used as medicine of medicinal ingredient Borneolum Syntheticum is solid dispersion, parcel medicine carrying microcapsule, the microsphere of Borneolum Syntheticum; This fast-acting heart disease curing oral cavity disintegration tablet is in mentioned component and ratio uniform mixing, crosses 80 mesh sieves, and as the medicinal ingredient of oral cavity disintegration tablet, with the correctives uniform mixing, the homogeneous mixture with filler, disintegrating agent, lubricant, fluidizer all mixes, sieves again, tabletting makes;
The oral cavity disintegration tablet prescription is by weight percentage:
Medicinal ingredient 3.8～18.9%
Filler 48.0～71.0%
Disintegrating agent 9.0～27.8%
Correctives 0.5～1.1%
Lubricant 0.9～2.1%
Fluidizer 0.9～2.1%.
2. according to the described fast-acting heart disease curing oral cavity disintegration tablet of claim 1, it is characterized in that filler is selected from one or both in microcrystalline Cellulose, dextrin, lactose, starch or the mannitol.
3. according to right 1 described fast-acting heart disease curing oral cavity disintegration tablet, it is characterized in that disintegrating agent is selected from one or both among low substituent group hydroxypropyl methylcellulose L-HPC, crospolyvinylpyrrolidone PVPP, crosslinked carboxymethyl fecula sodium CCMS-Na or the cross-linking sodium carboxymethyl cellulose CMC-Na.
4. according to the described fast-acting heart disease curing oral cavity disintegration tablet of claim 1, it is characterized in that the solid dispersion carrier is selected from Polyethylene Glycol, promptly PEG-6000, PEG-4000, PEG-12000, PEG-60000, polyvinylpyrrolidone are PVP-K
15, PVP-K
30, PVP-K
60, PVP-K
90With in beta-schardinger dextrin-and the derivant thereof one or both.
5. according to the described fast-acting heart disease curing oral cavity disintegration tablet of claim 1, it is characterized in that correctives is selected from one or both in Mentholum, Oleum menthae, stevioside or the aspartame.
6. according to the described fast-acting heart disease curing oral cavity disintegration tablet of claim 1, it is characterized in that lubricant is selected from one or both in magnesium stearate, Stepanol MG, the Pulvis Talci.
7. according to the described fast-acting heart disease curing oral cavity disintegration tablet of claim 1, it is characterized in that fluidizer is selected from one or both in micropowder silica gel, the Pulvis Talci.
8. the preparation method of the described fast-acting heart disease curing oral cavity disintegration tablet of claim 1, medicinal ingredient is Rhizoma Chuanxiong, Borneolum Syntheticum, its pharmaceutical dosage is by ministry standard WS
3The common dose of-B-3484-98 regulation, the ratio of two flavor Chinese medicines is a Rhizoma Chuanxiong 40%～60%, Borneolum Syntheticum is 60%～40%, it is characterized in that the fast-acting heart disease curing oral cavity disintegration tablet is in mentioned component and ratio uniform mixing, cross 80 mesh sieves, as the medicinal active ingredient of oral cavity disintegration tablet, mix with correctives, filler, disintegrating agent, lubricant, fluidizer respectively, sieve, tabletting makes;
The oral cavity disintegration tablet prescription is by weight percentage:
Medicinal ingredient 3.8～18.9%
Filler 48.0～71.0%
Disintegrating agent 9.0～27.8%
Correctives 0.5～1.1%
Lubricant 0.9～2.1%
Fluidizer 0.9～2.1%
The concrete steps of oral cavity disintegration tablet preparation are as follows:
(1) selection of medicinal ingredient and pretreatment
The selection of medicinal ingredient:
The volatile oil that the form of being used as medicine of medicinal ingredient Rhizoma Chuanxiong is that the water of this medical material is carried, alcohol extraction, ether are carried, a kind of method in the supercritical extraction, vapor extraction method obtains, or parcel medicine carrying microcapsule, the microsphere of this volatile oil, or the direct ground product of medical material; The form of being used as medicine of medicinal ingredient Borneolum Syntheticum is solid dispersion, parcel medicine carrying microcapsule, the microsphere of Borneolum Syntheticum;
The pretreatment of medicinal ingredient:
The volatile oil of above-mentioned medical material, the ground product of medical material are all handled by the conventional method of pharmacopeia regulation;
The preparation method of parcel medicine carrying microcapsule or microsphere is:
Adopt coacervation or interfacial polymerization, medicinal ingredient and capsule material are dissolved in the pharmacopeia regulation, can be used in the organic solvent of pharmacy the formation organic facies; Water intaking adds 2～3% surfactant in addition, disperses, and forms water; Under to water stirring or ultrasound condition, organic facies at the uniform velocity is added drop-wise to aqueous phase, make its dispersion, add plasticizer or cross-linking agent or regulate pH value to 4～10, carry out crosslinked and curing, obtain medicinal parcel medicine carrying microcapsule or microsphere; With excessive water extraction organic solvent, more after filtration, drying, obtain discharging medicinal ingredient, runny parcel medicine carrying microcapsule or microsphere; Stirring or ultrasonic time 0.5～2 hour; Be not less than 2 hours crosslinked and hardening time;
Wherein the capsule material is selected from natural and the synthetic high polymer pharmaceutic adjuvant, and natural polymer medical adjuvant comprises gelatin, arabic gum, sodium alginate, cellulose and cellulosic derivant, chitosan; The synthetic high polymer pharmaceutic adjuvant comprises the copolymer of poly-methyl-prop diluted acid, polymethyl acrylate, poly-methyl-prop diluted acid and poly-methyl-prop diluted acid ester, Youteqi E-100, Youteqi EPO, polyvinyl alcohol, the 1-3 kind in polyvinylpyrrolidone and the Polyethylene Glycol; Organic solvent is selected from organic solvent ethanol, ethyl acetate, Ethyl formate and the chloroform of approval usefulness in the pharmacopeia; Surfactant is selected from tween, class of department, sodium lauryl sulphate, polyvinyl alcohol, polyvinylpyrrolidone, Polyethylene Glycol; Plasticizer is selected from citric acid, triethyl citrate, Polyethylene Glycol, and cross-linking agent is selected from formaldehyde and glutaraldehyde; Above-mentioned stirring or ultrasonic time are 0.5～2 hour; Be not less than 2 hours crosslinked and hardening time;
The Chinese medicine Rhizoma Chuanxiong is handled through said method, promptly obtains drug loading and be 60%～90% solid Rhizoma Chuanxiong microcapsule or microsphere, and its particle diameter is 1～100 μ m;
The Chinese medicine Borneolum Syntheticum is handled through said method, promptly obtains drug loading and be 50～30% Borneolum Syntheticum medicine carrying microcapsule or solid dispersion medicine carrying microgranule, and its particle diameter is 1～100 μ m;
(2) film-making
Medicinal ingredient and correctives pulverize separately are crossed 80 mesh sieves, take by weighing respectively by above-mentioned formula ratio, mix homogeneously, in addition filler, disintegrating agent, fluidizer, lubricant are crossed 80 mesh sieves respectively, by formula ratio take by weighing respectively, mix homogeneously, all mix with the ingredient that is mixed with correctives again, sieve, tabletting; Tabletting adopts conventional tablet pharmaceutical equipment and pressing process can make oral cavity disintegration tablet.
9. according to the preparation method of the described fast-acting heart disease curing oral cavity disintegration tablet of claim 9, it is characterized in that capsule material concentration is 1～10% in the organic facies in preparation parcel medicine carrying microcapsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410019985 CN1273115C (en) | 2004-07-15 | 2004-07-15 | Quick acting and heart resurrecting oral disintegrating tablet and its preparation process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410019985 CN1273115C (en) | 2004-07-15 | 2004-07-15 | Quick acting and heart resurrecting oral disintegrating tablet and its preparation process |
Publications (2)
| Publication Number | Publication Date |
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| CN1593505A CN1593505A (en) | 2005-03-16 |
| CN1273115C true CN1273115C (en) | 2006-09-06 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN 200410019985 Expired - Fee Related CN1273115C (en) | 2004-07-15 | 2004-07-15 | Quick acting and heart resurrecting oral disintegrating tablet and its preparation process |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105362320B (en) * | 2015-12-02 | 2019-06-07 | 广东药科大学 | A kind of method that 3D printing prepares fast-acting heart disease curing oral disnitegration tablet |
| CN109044990A (en) * | 2018-08-02 | 2018-12-21 | 合肥中科力科技有限公司 | A kind of drug package preparation process |
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