CN106176963A - A kind of Plumula Nelumbinis oral cavity disintegration tablet and preparation method thereof - Google Patents

A kind of Plumula Nelumbinis oral cavity disintegration tablet and preparation method thereof Download PDF

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CN106176963A
CN106176963A CN201610580095.8A CN201610580095A CN106176963A CN 106176963 A CN106176963 A CN 106176963A CN 201610580095 A CN201610580095 A CN 201610580095A CN 106176963 A CN106176963 A CN 106176963A
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plumula nelumbinis
oral cavity
cavity disintegration
active component
disintegration tablet
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薛中峰
高华宏
汪杰
陈明聪
钟莹
张影
黄祖光
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
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    • A61K36/185Magnoliopsida (dicotyledons)
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
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    • A61K9/2022Organic macromolecular compounds
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    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/33Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/331Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation or decoction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/33Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/333Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/39Complex extraction schemes, e.g. fractionation or repeated extraction steps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/50Methods involving additional extraction steps
    • A61K2236/51Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/50Methods involving additional extraction steps
    • A61K2236/53Liquid-solid separation, e.g. centrifugation, sedimentation or crystallization

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Abstract

The present invention relates to a kind of Plumula Nelumbinis oral cavity disintegration tablet and preparation method thereof, it is with Plumula Nelumbinis as crude drug, and its preparation method is: take the active component of Plumula Nelumbinis, it is dried, beat powder, add beta cyclodextrin, mannitol by weight, low-substituted hydroxypropyl cellulose, pregelatinized Starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, and after granulate, disintegrating tablet made by tabletting.

Description

A kind of Plumula Nelumbinis oral cavity disintegration tablet and preparation method thereof
Technical field
The present invention relates to drug world, be specifically related to a kind of Plumula Nelumbinis oral cavity disintegration tablet and preparation method thereof.
Background technology
Arrhythmia refers to tachycardia that the abnormal or exciting conductive impairment of the self-disciplining of heart causes, the most slow, and the rhythm of the heart is not A neat or class disease of ectopic cardiac rhythm.Its clinical manifestation is paroxysmal cardiopalmus, chest pain, dizziness, pareordia sense of discomfort, feel oppressed, Out of breath, hands and feet coolness and fainting, the even symptom such as obnubilation.There is the small part arrhythmic patients can be asymptomatic, only electrocardio Figure changes.Its sickness rate and case fatality rate are the highest, constitute about the 11% of natural death number.According to statistics, China there are about 60 every year Ten thousand people die from sudden cardiac death, and wherein 90% is to be caused by malignant arrhythmia, therefore becomes for ARR treatment Numerous medical personal focus of attention all the time.
Clinically ARR western medicine is had the features such as rapid, the determined curative effect of effect, but side effect is relatively big, and And in place of several equal Shortcomings of class antiarrhythmic drug used clinically at present, during such as treatment arrhythmia, lure the most again Sending out arrhythmia, incidence rate is up to more than 10%;The most easily induce conduction block and drug induccd heart failure simultaneously, and to some intractable Arrhythmia is invalid.
The traditional Chinese medical science is the most on the books as far back as Huangdi's Internal Classics one book to ARR understanding, such as " a Plain Questions normal person meteorology opinion piece " Have: " people one exhales arteries and veins one to move, and one inhales arteries and veins one moves, and says few gas.... people one exhales arteries and veins four to move above saying extremely ", the contained arteries and veins of Pulse Classic comes again " first the least, irregularity in frequency of pulse beat " " such as fiber crops bean hitter " etc., depict ARR pulse condition the most visually.Later age, doctor, passed through Clinical practice, is described as pulse condition knot, generation, promotees, count, slow etc. is all.
Motherland's medical science is thought, if suffering from the disease such as the thoracic obstruction, pained, gastral cavity is vexed, cough with asthma, the obstruction of heart-QI for a long time, all can cause yang-energy virtual loss heart arteries and veins and losing In Wen Yun, deficiency of YIN-blood, it is flourish and be disease that heart arteries and veins loses network, thus cause occurring slow, count, promote, tie, generation, the most serious is exhausted The abnormal pulse such as arteries and veins, these pulse conditions all can reflect arrhythmia.Differentiation of tcm, with vigorate qi and replenish the blood, tranquilizing by nourishing the heart is primary disease Therapeutic Principle.
In recent years, research finds the phenol biology total alkali extracted from prepared slices of Chinese crude drugs Plumula Nelumbinis, such as liensinine, methyl Plumula Nelumbinis Alkali, isoliensinine etc. have significant antiarrhythmic effect.Therefore, bioavailability and Plumula Nelumbinis in order to improve medicine are steady Qualitative, in conjunction with the compliance of patients with arrhythmia treatment, facilitate patient to take simultaneously, Plumula Nelumbinis is prepared as solid immediate release agent Type oral instant-dissolving tablet.
Summary of the invention
It is an object of the invention to provide a kind of Plumula Nelumbinis oral cavity disintegration tablet;
It is a further object of the present invention to provide the preparation method of a kind of Plumula Nelumbinis oral cavity disintegration tablet.
It is an object of the invention to by following technical scheme realization:
Plumula Nelumbinis oral cavity disintegration tablet of the present invention, it is to be prepared from by the raw material of following weight portion:
Plumula Nelumbinis 5-50 part, beta-schardinger dextrin-2-20 part, mannitol 5-25 part, low-substituted hydroxypropyl cellulose 5-30 part, in advance Gelling starch 5-15 part, magnesium stearate 0.1-3 part, coloring agent 0.1-1 part, correctives 0.1-1 part.
Preferably, it is to be prepared from by the raw material of following weight portion:
Plumula Nelumbinis 15-30 part, beta-schardinger dextrin-5-15 part, mannitol 15-25 part, low-substituted hydroxypropyl cellulose 20-30 part, Pregelatinized Starch 10-15 part, magnesium stearate 0.1-1 part, coloring agent 0.3-0.8 part, correctives 0.3-0.8 part.
The following is primary efficacy and the pharmacological action of Plumula Nelumbinis of the present invention:
Plumula Nelumbinis, for the green embryo in the middle of the mature seed of nymphaeaceae plant lotus Nelumbo nucifera Gaertn. Root, i.e. Plumula Nelumbinis.Nature and flavor are bitter, cold, are included into the heart, kidney channel.Plumula Nelumbinis has clearing away heart-fire for tranquillization, restoring normal coordination between the heart and kidney, effect of unsmoothing the sperm and stopping bleeding, uses In heat attacking the pericardium, unconsciousness and delirium, disarmony between the heart and kidney, the diseases such as seminal emission, heat in blood haematemesis of having a sleepless night.Recording according to " book on Chinese herbal medicine is the newest ", Plumula Nelumbinis is " clear Heart-fire, suppressing the hyperactive liver fire, purgation of spleen excess fire, drop lung-fire, relieving restlessness of relieving summer heat, promoting the production of body fluid to quench thirst, control mesh red and swollen ".Plumula Nelumbinis is " Chinese Pharmacopoeia " 2015 Version is recorded, main product Hunan, Hubei, Fujian, Jiangsu, zhejiang and other places.
Containing multiple alkaloid in Plumula Nelumbinis: liensinine (liensinine), isoliensinine (isoliensinine), methyl Liensinine (neferine), C19H23NO3 (lotusine), methyl-corypalline alkali (methye-corypalline), Folium Nelumbinis Alkali (Nuciferine), pronuciferine (+)-Pronuciferine (Pronuciferine) and demethyl coclaurine (demethylcoclaurine), Cornu Bovis seu Bubali Florigen (Lotusine), also gets amorphism alkaloid Nn-9, again containing galuteolin from separation liensinine mother solution (Galuteolin), the flavonoid such as hyperin (Hyperin), globulariacitrin (Rutin).In addition, in Plumula Nelumbinis possibly together with The trace element such as water soluble polysaccharide composition and zinc, copper, ferrum, calcium, magnesium, sodium, potassium, nickel, manganese, cadmium.
Modern plants chemical research shows in Plumula Nelumbinis that phenol alkaloid position is mainly containing liensinine, (-)-Neferine, different Liensinine.Modern pharmacological research shows, Plumula Nelumbinis total alkaloids and monomer all have have widely arrhythmia, resist myocardial ischemia With the effect of blood pressure lowering, it is primarily adapted for use in treatment arrhythmia and myocardial ischemia.Its antiarrhythmic effect is better than conventional medicament Kui Nining, function of resisting myocardial ischemia and diltiazem are suitable, additionally, also have blood pressure lowering, antioxidation and for glycosuria The preventing and treating of disease syndrome.
Plumula Nelumbinis alkaloid main component liensinine, isoliensinine, (-)-Neferine, the pharmacological action of C19H23NO3 and Its mechanism is as follows:
1, liensinine (Lien) has preferable antiarrhythmic effect, and its mechanism of action may be with retardance Na+, Ca2+, K+ Transmembrane transport relevant.
2, (-)-Neferine (Nef) can suppress the self-disciplining of sinuatrial node slow reacting cell and delay Atrioventricular Conduction, has maincenter Property antiarrhythmic effect.For Ia class antiarrhythmic drug, its antiarrhythmic mechanism and quinidine or procaine acyl Amine is similar.
3, C19H23NO3 (lotus, lotusine) is water-soluble alkaloid in Plumula Nelumbinis.Lot dose-dependently increases The contractility of isolated myocardium and effect are better than amrinone (Am) and papaverine (Pa).But not there is antiarrhythmic effect.Lot Similar to phosphodiesterase III inhibitor to the feature of hemodynamic effects.
4, α receptor is had more obvious blocking effect interior calcium that this receptor can be suppressed to cause to release by isoliensinine (Iso) Put and extrinsic AGB stars.Pulse dependent calcium channel is also had retardation.Transient slight blood pressure lowering and the not normal effect of the anti-heart of Iso can Can be the most relevant with these.
Present invention also offers the preparation method of the active component of Plumula Nelumbinis, the method is to use water to carry or lower alcohol extract Extraction is prepared from.Concrete preparation method is as follows:
Scheme one: take Plumula Nelumbinis, extracting in water 2-3 time, each amount of water is equivalent to 5-12 times of medical material gross weight, every time Extraction time is 1-3 hour, united extraction liquid, filters, and when filtrate is concentrated into 25 DEG C, relative density is the thick paste of 1.20-1.40, Obtain described active component.
Scheme two: take Plumula Nelumbinis, extracting in water 2-3 time, each amount of water is equivalent to 5-12 times of medical material gross weight, every time Extraction time is 1-3 hour, united extraction liquid, filters, takes supernatant after standing, and when filtrate is concentrated into 25 DEG C, relative density is The clear paste of 1.05-1.20, adds ethanol, and making alcohol content is 40%-70%, stands 6-24 hour, filters, and filtrate is concentrated into 25 DEG C Time relative density be the thick paste of 1.20-1.40, obtain described active component.
Scheme three: take Plumula Nelumbinis, adds alcohol extraction 2-3 time, and each alcohol adding amount is equivalent to 5-12 times of medical material gross weight, every time Extraction time is 1-3 hour, united extraction liquid, filters, and when filtrate is concentrated into 25 DEG C, relative density is the thick paste of 1.20-1.40, Obtain described active component.
Scheme four: take Plumula Nelumbinis, adds alcohol extraction 2-3 time, and each alcohol adding amount is equivalent to 5-12 times of medical material gross weight, every time Extraction time is 1-3 hour, united extraction liquid, filters, and when filtrate is concentrated into 25 DEG C, relative density is the clear paste of 1.05-1.20, Adding water, making water content is 40%-70%, stands 6-24 hour, filters, and when filtrate is concentrated into 25 DEG C, relative density is 1.20- The thick paste of 1.40, obtains described active component.
Described lower alcohol extract is methanol, ethanol, normal propyl alcohol, isopropanol, 1-propenol-3, n-butyl alcohol, isobutanol, two grades of fourths One or more mixing in alcohol, tertiary butyl alcohol.
The coloring agent told and correctives include but not limited to following:
Coloring agent: amaranth, carmine, erythrosine, the reddest, lemon yellow, sunset yellow, indigo, light blue, beet red, lac Red, red pigment of cowberry, capsanthin, red rice are red.
Correctives: sucrose, simple syrup, syrupus aromaticus, stevioside, glycerol, sorbitol, mannitol, saccharin sodium, A Sipa Smooth.
Present invention also offers the preparation method of a kind of Plumula Nelumbinis oral cavity disintegration tablet:
Method 1: take the active component of the Plumula Nelumbinis of above-mentioned gained, adds beta-schardinger dextrin-, mannitol, low replacement by weight Hydroxypropyl cellulose, pregelatinized Starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, After granulate, disintegrating tablet made by tabletting.
Method 2: take the active component of the Plumula Nelumbinis of above-mentioned gained, is dried, beats powder, add beta-schardinger dextrin-by weight, sweet Dew alcohol, low-substituted hydroxypropyl cellulose, pregelatinized Starch, magnesium stearate, coloring agent, correctives, routinely granule preparation side Method makes granule, and after granulate, disintegrating tablet made by tabletting.
Plumula Nelumbinis oral cavity disintegration tablet of the present invention is effective ingredient in Chinese preparation, and principle active component physicochemical property is clear Chu, the mechanism of action is clear and definite, and taking dose is little, and active component content is high, and safety range is wide, meets and prepares dosage form novel, efficient Primary condition.Plumula Nelumbinis oral cavity disintegration tablet is rapid due to release, and medicine is directly entered body is followed by oral cavity, sublingual mucosal absorption Ring, decreases the gastrointestinal tract destruction to medicine, decreases liver first-pass effect, therefore the most rapid-action compared with conventional tablet, raw Thing availability is also remarkably improved, and meets tcm emergency ARR clinical application requirement.Compared with injection, this dosage form has Having volume little, good stability, drug absorption is fast, takes and the advantage such as easy to carry.
The present invention is directed to arrhythmia clinical treatment present situation, overcome the deficiency of existing treatment antiarrhythmic medicament preparation, Under guidance of traditional Chinese medicine theory, actively use modern Chinese medicine pharmaceutical technology, on existing Research foundation, both designed and developed into further Meet tcm clinical practice Therapy characteristics, there is again the pure Chinese medicinal preparation quick-acting, efficient of Modern preparations feature.The rhythm of the heart is lost by the present invention Normal treatment and oral cavity disintegration tablet technology of preparing produce important and active influence, will produce huge social benefit and warp simultaneously Ji interests.
A kind of Plumula Nelumbinis oral cavity disintegration tablet that the present invention provides has the advantage that
1, the Plumula Nelumbinis oral cavity disintegration tablet that the present invention provides is not required to water delivery service, is put in oral cavity disintegrate or melt in about 15~30 seconds Changing, bad for some function of deglutition and water intaking inconvenience patient is especially suitable.
2, the Plumula Nelumbinis oral cavity disintegration tablet onset that the present invention provides is rapid, can reduce medicine " first pass effect " simultaneously.
3, oral cavity disintegration tablet is a kind of new oral solid preparation occurred in drugs consumption market in recent years, unique with it Superiority increasingly liked by patient, the present invention provide Plumula Nelumbinis oral cavity disintegration tablet there is wide market prospect.
Detailed description of the invention
The present invention is further illustrated below by embodiment.It should be understood that embodiments of the invention are for illustrating The present invention rather than limitation of the present invention.The simple modifications that the present invention is carried out by the essence according to the present invention broadly falls into the present invention Claimed scope.Except as otherwise noted, the percent of the amount of alcohol in the present invention is percentage by volume, and v/v represents solution Volume ratio.
Embodiment 1
Plumula Nelumbinis 50g, beta-schardinger dextrin-2g, mannitol 5g, low-substituted hydroxypropyl cellulose 30g, pregelatinized Starch 5g, stearic Acid magnesium 3g, coloring agent 1g, correctives 1g.
Taking Plumula Nelumbinis, crushed after being dried becomes coarse powder, extracting in water 3 times, and three amount of water are the most respectively when in medical material gross weight 12 times, 8 times, 5 times, each extraction time is respectively 3 hours, 2 hours, 1 hour, united extraction liquid, filter, filtrate is concentrated into When 25 DEG C, relative density is the thick paste of 1.40, obtains the active component of Plumula Nelumbinis.
Take the active component of Plumula Nelumbinis, add beta-schardinger dextrin-, mannitol, low-substituted hydroxypropyl cellulose, pre-glue by weight Changing starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, and after granulate, disintegrate made by tabletting Sheet.
Embodiment 2
Plumula Nelumbinis 5g, beta-schardinger dextrin-20g, mannitol 25g, low-substituted hydroxypropyl cellulose 5g, pregelatinized Starch 15g, firmly Fatty acid magnesium 0.1g, coloring agent 0.1g, correctives 0.1g.
Taking Plumula Nelumbinis, crushed after being dried becomes coarse powder, and extracting in water 2 times, each amount of water is respectively equivalent to medical material gross weight 10 times, 6 times, each extraction time is 2 hours, united extraction liquid, filter, take supernatant after standing, filtrate is concentrated into 25 DEG C Time relative density be the clear paste of 1.05, add ethanol, making alcohol content is 40%, stands 24 hours, filtration, filtrate is concentrated into 25 DEG C Time relative density be the thick paste of 1.20, obtain the active component of Plumula Nelumbinis.
Taking the active component of Plumula Nelumbinis, be dried, beat powder, add beta-schardinger dextrin-, mannitol by weight, low substituted hydroxy-propyl is fine Dimension element, pregelatinized Starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, presses after granulate Sheet makes disintegrating tablet.
Embodiment 3
Plumula Nelumbinis 15g, beta-schardinger dextrin-15g, mannitol 15g, low-substituted hydroxypropyl cellulose 20g, pregelatinized Starch 10g, Magnesium stearate 1g, coloring agent 0.3g, correctives 0.3g.
Taking Plumula Nelumbinis, crushed after being dried becomes coarse powder, and extracting in water 3 times, each amount of water is respectively equivalent to medical material gross weight 12 times, 8 times, 6 times, each extraction time is respectively 3 hours, 2 hours, 1 hour, united extraction liquid, filter, take after standing Clear liquid, when filtrate is concentrated into 25 DEG C, relative density is the clear paste of 1.20, adds ethanol, and making alcohol content is 70%, stands 6 hours, Filtering, when filtrate is concentrated into 25 DEG C, relative density is the thick paste of 1.40, obtains the active component of Plumula Nelumbinis.
Taking the active component of Plumula Nelumbinis, be dried, beat powder, add beta-schardinger dextrin-, mannitol by weight, low substituted hydroxy-propyl is fine Dimension element, pregelatinized Starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, presses after granulate Sheet makes disintegrating tablet.
Embodiment 4
Plumula Nelumbinis 20g, beta-schardinger dextrin-10g, mannitol 20g, low-substituted hydroxypropyl cellulose 25g, pregelatinized Starch 15g, Magnesium stearate 1g, coloring agent 0.8g, correctives 0.8g.
Taking Plumula Nelumbinis, crushed after being dried becomes coarse powder, adds alcohol extraction 3 times, and each alcohol adding amount is equivalent to the 12 of medical material gross weight Times, 10 times, 6 times, each extraction time is 3 hours, 2 hours, 1 hour, united extraction liquid, filter, when filtrate is concentrated into 25 DEG C Relative density is the thick paste of 1.30, obtains the active component of Plumula Nelumbinis.
Take the active component of Plumula Nelumbinis, add beta-schardinger dextrin-, mannitol, low-substituted hydroxypropyl cellulose, pre-glue by weight Changing starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, and after granulate, disintegrate made by tabletting Sheet.
Embodiment 5
Plumula Nelumbinis 40g, beta-schardinger dextrin-5g, mannitol 10g, low-substituted hydroxypropyl cellulose 20g, pregelatinized Starch 8g, firmly Fatty acid magnesium 2g, coloring agent 0.5g, correctives 0.5g.
Taking Plumula Nelumbinis, crushed after being dried becomes coarse powder, adds alcohol extraction 2 times, and each alcohol adding amount is equivalent to the 10 of medical material gross weight Times, 8 times, each extraction time is 2 hours, united extraction liquid, filter, when filtrate is concentrated into 25 DEG C relative density be 1.40 thick Cream, obtains the active component of Plumula Nelumbinis.
Taking the active component of Plumula Nelumbinis, be dried, beat powder, add beta-schardinger dextrin-, mannitol by weight, low substituted hydroxy-propyl is fine Dimension element, pregelatinized Starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, presses after granulate Sheet makes disintegrating tablet.
Embodiment 6
Plumula Nelumbinis 10g, beta-schardinger dextrin-8g, mannitol 20g, low-substituted hydroxypropyl cellulose 25g, pregelatinized Starch 12g, firmly Fatty acid magnesium 1.5g, coloring agent 0.5g, correctives 0.8g.
Taking Plumula Nelumbinis, crushed after being dried becomes coarse powder, adds alcohol extraction 2 times, and each alcohol adding amount is equivalent to the 8 of medical material gross weight Times, each extraction time is 2 hours, united extraction liquid, filters, and when filtrate is concentrated into 25 DEG C, relative density is the clear paste of 1.20, Adding water, making water content is 40%, stands 24 hours, filters, and when filtrate is concentrated into 25 DEG C, relative density is the thick paste of 1.40, i.e. Obtain the active component of Plumula Nelumbinis.
Taking the active component of Plumula Nelumbinis, be dried, beat powder, add beta-schardinger dextrin-, mannitol by weight, low substituted hydroxy-propyl is fine Dimension element, pregelatinized Starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, presses after granulate Sheet makes disintegrating tablet.
Embodiment 7
Plumula Nelumbinis 20g, beta-schardinger dextrin-10g, mannitol 15g, low-substituted hydroxypropyl cellulose 10g, pregelatinized Starch 15g, Magnesium stearate 2.5g, coloring agent 0.3g, correctives 0.5g.
Taking Plumula Nelumbinis, crushed after being dried becomes coarse powder, adds alcohol extraction 3 times, and each alcohol adding amount is equivalent to the 12 of medical material gross weight Times, 10 times, 5 times, each extraction time is 3 hours, 2 hours, 1 hour, united extraction liquid, filter, when filtrate is concentrated into 25 DEG C Relative density is the clear paste of 1.05, adds water, and making water content is 70%, stands 6 hours, filters, and filtrate is concentrated into 25 DEG C of phases It is the thick paste of 1.20 to density, obtains the active component of Plumula Nelumbinis.
Take the active component of Plumula Nelumbinis, add beta-schardinger dextrin-, mannitol, low-substituted hydroxypropyl cellulose, pre-glue by weight Changing starch, magnesium stearate, coloring agent, correctives, process for producing granula makes granule routinely, and after granulate, disintegrate made by tabletting Sheet.Pharmacodynamic experiment
1 experimental example Plumula Nelumbinis oral cavity disintegration tablet antiarrhythmic experimentation
1.1 laboratory animal
SD rat, Mus age 8~12 weeks, body weight 280 ± 10g, Guangdong Medical Lab Animal Center provide, male and female divide cage Freely raise, be randomly divided into 6 groups: negative control group, mexiletine group and 3 dosage Plumula Nelumbinis oral cavity disintegration tablet groups.
1.2 medicines and dosage
(1) test medicine: Plumula Nelumbinis oral cavity disintegration tablet described in the embodiment of the present invention 5, is prepared from by Plumula Nelumbinis medical material, makes It is configured to desired concn with front drinking water.Basic, normal, high dosage is respectively: 0.4g/kg, 0.8g/kg, 1.6g/kg.
(2) positive drug: mexiletine, each dosage is 50mg/kg.
(3) negative medicine: the auxiliaries removing Plumula Nelumbinis in substrate instant component forms.
Administering mode: gastric infusion, every day 2 times, the upper and lower noon is each once.Continue 7 days.
1.3 statistical analysis
Data result is usedRepresent, use the ANOVA variance analysis of SPSS17.0 statistical software to carry out significance of difference inspection Test.1.4 experimental techniques and result
1.4.1 laboratory animal modeling and administration
Aconitine induced rat arrhythmia is tested.Negative control group gavage (ig) gives equal-volume bare substrate 0.6g/ Kg, Plumula Nelumbinis oral cavity disintegration tablet basic, normal, high dosage group respectively organize ig respectively give 0.4,0.8,1.6g/kg, positive group ig give U.S. West rule 50mg/kg, is administered 7 days.After last is administered 30 minutes, lumbar injection (ip) urethane 1.2g/kg anaesthetizes, and faces upward position and fixes, Lead physiological signal record analysis system with six to monitor continuously, and record electrocardiogram (ECG) II and lead ECG.After electrocardiogram is stable, Quickly Lingual vessels injection (iv) aconitine 200 μ g/kg (having noted in 0.01%, 0.2ml/100g, 3s), occurs ventricular premature contraction in succession (Ventricular prem ature beat, VP), ventricular tachycardia (Vent ricular tachycardia, VT), and Develop into stable biphasic or bipolar type arrhythmia, to ventricular fibrillation (Vent ricular fibrillation, VF) and heart occur Stop fight (Cardiac arrest, CA), following experimental index in recording 60 minutes: not normal time of occurrence, the not normal persistent period, extensive Multiple time of occurrence, normal duration (initial time, by injection, calculates each section of merging summation occurred).
1.4.2 Plumula Nelumbinis oral cavity disintegration tablet anti-aconitine induction SD rat ventricular result
Table 1 aconitine each group of SD rat ventricular experimental result of induction
Compared with negative control group, P < 0.05
1.5 conclusion
The arrhythmia of Aconitine Induced is likely due to the most excited cardiac muscle, makes Myocardial Na+Channel opener, accelerates cardiac muscle Cell Na+Caused by interior stream, it is chiefly to facilitate membrane depolarization, accelerates pacemaker self-disciplining, shorten refractory stage, thus cause room Property and the arrhythmia such as supraventricular ectopic rhythm and ventricular tachycardia.Test result indicate that, Plumula Nelumbinis oral cavity disintegration tablet is permissible Extending arrhythmia time of occurrence, shorten the not normal persistent period, extend normal duration, Plumula Nelumbinis oral cavity disintegration tablet has one Fixed Antiarrhythmic Effect.
Although, used general explanation, detailed description of the invention and test, the present invention made detailed retouching Stating, but on the basis of the present invention, can make some modifications or improvements it, this is apparent to those skilled in the art 's.Therefore, these modifications or improvements without departing from theon the basis of the spirit of the present invention, belong to claimed Scope.

Claims (10)

1. a Plumula Nelumbinis oral cavity disintegration tablet, it is characterised in that it is to be prepared from by the raw material of following weight portion:
Plumula Nelumbinis 5-50 part, beta-schardinger dextrin-2-20 part, mannitol 5-25 part, low-substituted hydroxypropyl cellulose 5-30 part, pregelatinated Starch 5-15 part, magnesium stearate 0.1-3 part, coloring agent 0.1-1 part, correctives 0.1-1 part.
2. Plumula Nelumbinis oral cavity disintegration tablet as claimed in claim 1, it is characterised in that it is to be prepared by the raw material of following weight portion : Plumula Nelumbinis 15-30 part, beta-schardinger dextrin-5-15 part, mannitol 15-25 part, low-substituted hydroxypropyl cellulose 20-30 part, Pregelatinized Starch 10-15 part, magnesium stearate 0.1-1 part, coloring agent 0.3-0.8 part, correctives 0.3-0.8 part.
3. Plumula Nelumbinis oral cavity disintegration tablet as claimed in claim 1 or 2, it is characterised in that the active component of Plumula Nelumbinis is to use water Carry or lower alcohol extract extracts and is prepared from.
4. Plumula Nelumbinis oral cavity disintegration tablet as claimed in claim 3, it is characterised in that the active component of Plumula Nelumbinis is by following Method is prepared from: take Plumula Nelumbinis, extracting in water 2-3 time, and each amount of water is equivalent to 5-12 times of medical material gross weight, every time Extraction time is 1-3 hour, united extraction liquid, filters, and when filtrate is concentrated into 25 DEG C, relative density is the thick paste of 1.20-1.40, Obtain described active component.
5. Plumula Nelumbinis oral cavity disintegration tablet as claimed in claim 3, it is characterised in that the active component of Plumula Nelumbinis is by following Method is prepared from: take Plumula Nelumbinis, extracting in water 2-3 time, and each amount of water is equivalent to 5-12 times of medical material gross weight, every time Extraction time is 1-3 hour, united extraction liquid, filters, takes supernatant after standing, and when filtrate is concentrated into 25 DEG C, relative density is The clear paste of 1.05-1.20, adds ethanol, and making alcohol content is 40%-70%, stands 6-24 hour, filters, when filtrate is concentrated into 25 DEG C Relative density is the thick paste of 1.20-1.40, obtains described active component.
6. Plumula Nelumbinis oral cavity disintegration tablet as claimed in claim 3, it is characterised in that the active component of Plumula Nelumbinis is by following Method is prepared from: take Plumula Nelumbinis, adds alcohol extraction 2-3 time, and each alcohol adding amount is equivalent to 5-12 times of medical material gross weight, every time Extraction time is 1-3 hour, united extraction liquid, filters, and when filtrate is concentrated into 25 DEG C, relative density is the thick paste of 1.20-1.40, Obtain described active component.
7. Plumula Nelumbinis oral cavity disintegration tablet as claimed in claim 3, it is characterised in that the active component of Plumula Nelumbinis is by following Method is prepared from: take Plumula Nelumbinis, adds alcohol extraction 2-3 time, and each alcohol adding amount is equivalent to 5-12 times of medical material gross weight, every time Extraction time is 1-3 hour, united extraction liquid, filters, and when filtrate is concentrated into 25 DEG C, relative density is the clear paste of 1.05-1.20, Adding water, making water content is 40%-70%, stands 6-24 hour, filters, and when filtrate is concentrated into 25 DEG C, relative density is 1.20- 1.40 thick paste, obtain described active component.
8. Plumula Nelumbinis oral cavity disintegration tablet as claimed in claim 3, it is characterised in that described lower alcohol extract is methanol, second One or more in alcohol, normal propyl alcohol, isopropanol, 1-propenol-3, n-butyl alcohol, isobutanol, secondary butanol, tertiary butyl alcohol mix Close.
9. the preparation method of a Plumula Nelumbinis oral cavity disintegration tablet, it is characterised in that take the activity of Plumula Nelumbinis described in claim 3 Composition, adds beta-schardinger dextrin-, mannitol, low-substituted hydroxypropyl cellulose, pregelatinized Starch, magnesium stearate, coloring by weight Agent, correctives, process for producing granula makes granule routinely, and after granulate, disintegrating tablet made by tabletting.
10. the preparation method of a Plumula Nelumbinis oral cavity disintegration tablet, it is characterised in that take the work of Plumula Nelumbinis described in claim 3 Property composition, be dried, beat powder, add beta-schardinger dextrin-by weight, mannitol, low-substituted hydroxypropyl cellulose, pregelatinized Starch, firmly Fatty acid magnesium, coloring agent, correctives, process for producing granula makes granule routinely, and after granulate, disintegrating tablet made by tabletting.
CN201610580095.8A 2016-07-22 2016-07-22 A kind of Plumula Nelumbinis oral cavity disintegration tablet and preparation method thereof Pending CN106176963A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110353073A (en) * 2019-08-27 2019-10-22 广东工业大学 A kind of decompression hard candy and preparation method thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
朱珠: "莲心含片制备工艺研究", 《中国优秀硕士学位论文全文数据库 工程科技Ⅰ辑》 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110353073A (en) * 2019-08-27 2019-10-22 广东工业大学 A kind of decompression hard candy and preparation method thereof

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