CN101543526A - Kudzu root total aglycone sustained-release pellet as well as preparation method and application thereof - Google Patents
Kudzu root total aglycone sustained-release pellet as well as preparation method and application thereof Download PDFInfo
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- CN101543526A CN101543526A CN200810102635A CN200810102635A CN101543526A CN 101543526 A CN101543526 A CN 101543526A CN 200810102635 A CN200810102635 A CN 200810102635A CN 200810102635 A CN200810102635 A CN 200810102635A CN 101543526 A CN101543526 A CN 101543526A
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Abstract
The invention discloses a kudzu root total aglycone sustained-release pellet as well as a preparation method and an application thereof, belonging to the field of traditional Chinese medicines. The sustained-release pellet consists of a pellet core and a coating layer, wherein the pellet core is prepared by kudzu root total aglycone and pharmaceutic adjuvant which are respectively 5-80 percent and 20-95 percent of the weight of the pellet core in proportion; and the weight of the coating layer is 1-20 percent of that of the pellet core. The preparation can effectively control the releasing speed of the kudzu root total aglycone in the body, improve the utilization rate of the pellet and have obvious curative effect in the aspect of curing diseases such as angiocardiopathy, high blood pressure, cerebral thrombosis, cephalalgia, sugar diabetes, menopause syndrome, tumor, and the like.
Description
Technical field
The present invention relates to the preparation method and the application of a kind of kudzuvine root total aglycon slow-release micro-pill and this slow-release micro-pill, belong to the field of Chinese medicines.
Background technology
Radix Puerariae is the dry root of legume pueraria lobata Pueraria labata (Willd.) Ohwi, contain many clocks flavones ingredient in the Radix Puerariae, as puerarin, daiazi, 4,7 glucosulfone daiazi, 3 ' methoxy puerarin, 7-xylose-puerarin, daidzein etc., its major part exists with the glycoside form.Total flavonoid glycoside constituents in the Radix Puerariae has curative effect preferably in diseases such as treatment cardiovascular disease, hypertension, cerebral thrombosis, headache, diabetes, climacteric syndrome and tumor.
The slow-release micro-pill technology can be wrapped up with smaller units ingredient by the release-controlled film clothing, make clinical other required solid dosage formss again, can obtain rate of releasing drug in the comparatively ideal body.This technology has following advantage: medicine is big at the area of gastrointestinal tract surface distributed, has improved bioavailability when reducing GI irritation; Seldom be subjected to digestive tract to carry the influence of the food rhythm and pace of moving things; The junior unit of several different release rules can be formed into multiple unit system to obtain ideal rate of releasing drug, obtain the blood drug level of expection; Drug release kinetics can obtain predicting more accurately and favorable reproducibility.
Contain a large amount of glycoside compositions in the Radix Puerariae, it is mainly flavonoid glycoside, and Radix Puerariae total glycosides and aglycon just draw attention in the application of field of medicaments.Owing to be subjected to the influence of Chinese medicine compound preparation technology, the preparation of present kudzu vine root also stays in relatively backward state, and make the preparation of the most suitable performance drug effect with the Chinese medicine ingredients that suitable technology will have a special efficacy, cause the extensive concern of field of traditional Chinese medicine pharmacy, representing the new development direction of the modern preparation of Chinese medicine.Kudzuvine root total aglycon being made slow releasing pellet, not only can be for extensive patients provide safety, Chinese medicine preparation efficiently, the preparation modernization of more middle pharmaceutically active ingredient provides extremely beneficial reference.
Summary of the invention
It is the slow-release micro-pill of active component with the kudzuvine root total aglycon that first purpose of the present invention is to provide a kind of.
Second purpose provides the preparation method of this slow-release micro-pill.
The object of the invention first purpose is achieved in that
The inventor provides a kind of kudzuvine root total aglycon slow-release micro-pill, and it is made up of ball and coatings, and wherein the ball core is to be made by kudzuvine root total aglycon and pharmaceutic adjuvant, its ratio be respectively the ball core heavy 5%～80% and 20%～95%; The weight of coatings be the ball core heavy 1～20%.
Kudzuvine root total aglycon is to extract from the Radix Puerariae medical material by prior art to obtain the Radix Puerariae total glycosides, and this effective site is hydrolyzed, and makes glycoside material wherein slough glycosyl, generates to have more bioactive aglycon.The inventor confirms that after deliberation glycoside material gained aglycon after hydrolysis has not had glycosyl, and its lipotropy strengthens greatly, thereby aglycon is absorbed than the easier intestinal mucosa that sees through of glycosides; Simultaneously, the molecule of medicine is more little also easy more to be absorbed, the glycosides hydrolysis fall with glycan molecule become aglycon after, molecular change gets littler, also can easier absorption.In addition, directly as medical substance, overcome in the past glycoside material long operational time, factor such as transformation efficiency is low, conversion results is uncertain in vivo, improved the bioavailability of medicine greatly, saved drug resource with aglycon.
Pharmaceutic adjuvant is meant used adjuvant in the preparation micropill process, as: microcrystalline Cellulose, starch, dextrin, lactose, cyclodextrin, EudragitRS, EudragitRL etc.
Coatings is an emphasis of the present invention, slow-release micro-pill has that blood drug level is steady, toxic and side effects is little, take number of times few, can take together with liquid, characteristics such as relative low price, and these advantages reach its slow release purpose by coatings.Coatings is made up of sustained release coating material, plasticizer, porogen, and wherein the sustained release coating material accounts for 60～90%; Plasticizer-containing accounts for 5～35%; Contain porogen and account for 0.1～10%.Wherein said sustained release coating material can be one or two or more kinds a mixture of acrylic resin aqueous dispersion, Aquacoat, ethyl cellulose powder, Hydroxypropyl Methylcellulose Phathalate, cellulose acetate-phthalate; Plasticizer can be one or two or more kinds the mixture in diethyl phthalate, triethyl citrate, triacetin, dibutyl sebacate, glycerol, propylene glycol, the Polyethylene Glycol; Porogen can be one or two or more kinds the mixture in lactose, hypromellose, hydroxypropyl cellulose, Polyethylene Glycol, polyvinylpyrrolidone, sucrose, the mannitol.
In the coating process, can be more smooth in order to make coatings, the some other adjuvant that may use such as Pulvis Talci, dodecyl sodium sulfate, dimethyl-silicon wet goods should be considered as extension of the present invention, should be subjected to protection of the present invention.
Second purpose of the present invention provides the preparation method of above-mentioned kudzuvine root total aglycon slow-release micro-pill.Concrete step is divided into following 2 steps:
(1) preparation of pastille micropill, below two kinds of methods all can
A. with the pharmaceutic adjuvant mix homogeneously; add binding agent; play female also pill-rolling to required order number with comminutor (or coating pan); oven dry; make the blank micropill of smooth ball; blank micropill is placed fluid bed (or coating pan), and kudzuvine root total aglycon and polymeric membrane clothing material are with water or water and alcohol mixeding liquid, and the skin that is coated on the ball celphere is made the pastille micropill.
B. pharmaceutic adjuvant and medicament mixed is even, add binding agent, play female also pill-rolling to required order number with comminutor (or coating pan), oven dry makes smooth ball-shaped pastille micropill.
(2) coating of slow release layer
The pastille micropill is placed fluid bed (or coating pan), sustained release coating material, porogen, plasticizer are mixed with solution or suspension with water or water and alcohol mixeding liquid, the skin that is sprayed at the pastille micropill is made slow-release micro-pill, the scope that its weightening finish is needed.
With in can incapsulating after the gained slow-release micro-pill drying or be pressed into tablet, make slow releasing preparation.
Beneficial effect
Kudzuvine root total aglycon slow-release micro-pill of the present invention also has the following advantages except the characteristics with common pellets:
(1) surface area that can be different according to the ball core is adjusted the size of drug loading, to reach required drug release rate; Also can reach required dissolution rate by mixed proportion and the spraying consumption of adjusting polymer; Perhaps can be mixed, to reach required release with the pastille micropill of different rates of release.In the design of formulation and technology, has flexible and changeable advantage.
(2) because the flowability of spheroidal micropill better, in the process of coating medicine and polymer, can obtain higher productive rate and repeatability, be easy to industrialization.
The specific embodiment
Enumerate embodiment below, further specify the present invention, each embodiment only is used to illustrate the present invention, does not limit the present invention:
Embodiment 1
Get Radix Puerariae 4kg, coarse pulverization, add 80% alcohol reflux three times, each 1.5 hours, filter merging filtrate, decompression recycling ethanol, water liquid extracts three times with water-saturated n-butanol, n-butyl alcohol liquid evaporate to dryness, and dry thing is dissolved in water, 115 ℃ of sterilization 20min, with lactic acid bacteria culturers hydrolysis fermentation 72 hours, hydrolyzed solution was added on the AB-8 type macroporous adsorptive resins, respectively with water, 30% ethanol, 80% ethanol elution, collect 80% ethanol elution, decompression recycling ethanol, drying under reduced pressure obtains kudzuvine root total aglycon 175g.
Embodiment 2
Get Radix Puerariae medical material 5kg, pulverize, add 10 times of water gagings and decoct 3 times, each 1 hour, filter, merging filtrate concentrates, 70% ethanol precipitation, reclaim ethanol, n-butyl alcohol liquid is reclaimed in n-butanol extraction 3 times of water liquid, 115 ℃ of sterilizations of surplus water liquid 15-20min, the escherichia coli strain is mixed with every milliliter with sterilized water and contains 10
8Individual conidial suspension is that the ratio of 3-10% inserts culture medium with the form of spore suspension in V/W,, shakes incubation time 72-96h under the condition of shaking speed 140-220rpm in 26-30 ℃; After stopping fermentation, filter, filter cake is measured 80% alcohol reflux 2 times with 5 times, each 30 minutes, merging filtrate, decompression recycling ethanol, surplus water liquid is crossed the D101 macroporous resin column, difference water, 70% ethanol elution, collect 70% ethanol elution, reclaim ethanol, concentrate, drying obtains kudzuvine root total aglycon 190g.
Embodiment 3
Get Radix Puerariae medical material 9kg, pulverize, add 60% alcohol reflux 3 times, each 1 hour, filter, merging filtrate reclaims ethanol, and surplus water liquid is crossed the D101 macroporous resin column, water, 70% ethanol elution are collected 70% ethanol elution respectively, reclaim ethanol, water liquid adds hydrochloric acid 300ml, heating hydrolysis 4 hours, the neutralization of hydrolyzed solution hydro-oxidation sodium, cross the AB-8 macroporous resin column, water, 70% ethanol elution are collected 70% ethanol elution respectively, reclaim ethanol, spray drying obtains kudzuvine root total aglycon 245g.
Embodiment 4
At first preparing 40-60 purpose parent nucleus, is adjuvant with microcrystalline Cellulose 150g, lactose 100g.Technological parameter is as follows: engine speed 200rpm, air blast flux is 25L/min, jet flow is 25L/min, and whiff pressure is 0.4mPa, and the spray pump rotating speed is 50rpm, 2% HPMC is a binding agent, the whitewashing time is 40min, and polishing time is 15min, keeps spouting velocity 7rpm in the polishing process, the back 50 ℃ of oven dry that take the dish out of the pot, screening is got 40-60 order granule as parent nucleus.Prepare the kudzuvine root total aglycon slow-release micro-pill then; take by weighing 40-60 order parent nucleus 100g; the material of putting centrifugal coating pelletizing machine is indoor; embodiment 1 gained kudzuvine root total aglycon is mixed with microcrystalline Cellulose 50g and lactose 20g, cross 100 mesh sieves, put into solid feed hopper then; start centrifugal coating pelletizing machine by following parameter; machine rotating speed 300rpm, polishing time are 10min, the same molding of all the other parameters.Treat to take the dish out of the pot after material adds, 50 ℃ of oven dry promptly get the pastille micropill, and pastille micropill particle diameter is controlled at the 14-26 order.Take by weighing 18-24 order kudzuvine root total aglycon pastille micropill 300g, put in the centrifugal coating pelletizing machine.Other gets Aquacoat 100g, mannitol 10g, and propylene glycol 10g adds Pulvis Talci 10g, and dodecyl sodium sulfate 1g adds water to 600ml, stirs to make coating solution.Spray pump rotating speed 15rpm, the same molding of other parameter, after coating finished, 40 ℃ got final product in aging 24 hours.At last, behind above-mentioned coating pastille micropill mensuration content, pack conventional capsule into promptly.
Embodiment 5
At first preparing 44-60 purpose parent nucleus, is adjuvant with microcrystalline Cellulose, starch, and operation is with embodiment 4.Prepare the kudzuvine root total aglycon slow-release micro-pill then, to test example 2 gained kudzuvine root total aglycons is dissolved among the 60% ethanol 300ml, in 500ml acetone, add Pulvis Talci 10g, Fructus Citri Limoniae triethylenetetraminehexaacetic acid vinegar 20g, dimethicone 5g, mix with 60% ethanol liquid of kudzuvine root total aglycon after stirring, stirring is spent the night and is promptly got medicine carrying liquid, 40-60 purpose parent nucleus 200g is dropped into 30 ℃ of preheating 2-3min in the fluid bed, and adjusting the fluidisation air quantity is 80m
3/ h makes the ball core be in good fluidized state, and regulating inlet temperature is 40 ℃, and outlet temperature is 35 ℃, with the spray rate of 10ml/min medicine carrying liquid is sprayed into fluidising chamber until spray, and the adjustment inlet temperature is 60 ℃, promptly gets the pastille micropill behind the heat treatment 20min.Get the coating material of Hydroxypropyl Methylcellulose Phathalate 50g, cellulose acetate-phthalate 50g, be dissolved in the 1000mL acetone, stir, wait to dissolve the back and add Pulvis Talci 10g, Fructus Citri Limoniae triethylenetetraminehexaacetic acid vinegar 20g and dimethicone 5g mixing.30-60 purpose pastille micropill 400g is dropped into 30 ℃ of preheating 5min in the fluid bed, and adjusting the boiling air quantity is 80m
3/ h makes the pastille micropill be in good fluidized state, regulating best inlet temperature is 35 ℃, outlet temperature is 30 ℃, by certain spray rate coating solution is sprayed into fluidising chamber with 15ml/min, adjusting inlet temperature is 60 ℃, heat treatment takes out screening after 24 hours, get the 18-32 order and promptly get the pastille coated micropill, packs conventional capsule into promptly.
Embodiment 6
To test example 3 kudzuvine root total aglycons and starch 200g, lactose 50g, cross 100 mesh sieve mixings, and add suitable quantity of water and make soft material, granulate, round as a ball in the spheronizator, take out micropill in 50 ℃ of dry 3-4h, after the screening, get 18-24 purpose pastille micropill and carry out coating.The sustained release coating material is acrylic resin aqueous dispersion 100g, diethyl phthalate 5g, triethyl citrate 5g, triacetin 5g, lactose 2g, hypromellose 3g, Pulvis Talci 5g, dimethicone 5g composition.Can in centrifugal granulator or fluid bed, carry out during coating.Operation is test example 5 together, with the pastille coated micropill that makes, and tabletting, promptly.
Claims (8)
1, a kind of kudzuvine root total aglycon slow-release micro-pill, it is made up of ball core and coatings, it is characterized in that the ball core is to be made by kudzuvine root total aglycon and pharmaceutic adjuvant, its ratio be respectively the ball core heavy 5%～80% and 20%～95%; The weight of coatings be the ball heart heavy 1～20%.
2, slow-release micro-pill according to claim 1 is characterized in that described kudzuvine root total aglycon is by the hydrolysis of Radix Puerariae total glycosides.
3, slow-release micro-pill according to claim 1 is characterized in that described pharmaceutic adjuvant is microcrystalline Cellulose, starch, dextrin, lactose, cyclodextrin, Eudragit RS, the mixture of one or two or more kinds among the Eudragit RL.
4, slow-release micro-pill according to claim 1 is characterized in that described coatings is to be made by the material of following weight ratio: sustained release coating material 60～90%, plasticizer 5～35%, porogen 0.1～10%.
5, slow-release micro-pill according to claim 4 is characterized in that described sustained release coating material can be any or the mixture more than two kinds in acrylic resin aqueous dispersion, Aquacoat, ethyl cellulose powder, Hydroxypropyl Methylcellulose Phathalate, the cellulose acetate-phthalate; Plasticizer can be any or the mixture more than two kinds in diethyl phthalate, triethyl citrate, triacetin, dibutyl sebacate, glycerol, propylene glycol, the Polyethylene Glycol; Porogen can be any or the mixture more than two kinds in lactose, hypromellose, hydroxypropyl cellulose, Polyethylene Glycol, polyvinylpyrrolidone, sucrose, the mannitol.
6, the method for preparing arbitrary described slow-release micro-pill in the claim 1 to 5 comprises preparation ball core and coating steps, the method that it is characterized in that preparing the ball core can be following any:
A. with the pharmaceutic adjuvant mix homogeneously, add binding agent, with comminutor molding and pill-rolling to required order number, oven dry, make the blank micropill of smooth ball, blank micropill is placed fluid bed, and kudzuvine root total aglycon and polymeric membrane clothing material are with water or water and alcohol mixeding liquid, and the skin that is coated on the ball celphere is made the pastille micropill;
B. pharmaceutic adjuvant and medicament mixed is even, add binding agent, use comminutor molding and pill-rolling to required order number, oven dry makes smooth ball-shaped pastille micropill.
7, slow-release micro-pill preparation method according to claim 6, it is characterized in that coating method is: the pastille micropill is placed fluid bed, sustained release coating material, porogen, plasticizer are mixed with solution or suspension with water or water and alcohol mixeding liquid, the skin that is sprayed at the pastille micropill is made slow-release micro-pill, the scope that its weightening finish is needed, drying, promptly.
8, arbitrary described kudzuvine root total aglycon slow-release micro-pill is used for the treatment of application in the medicine of cardiovascular disease, hypertension, cerebral thrombosis, headache, diabetes, climacteric syndrome or tumor in preparation in the claim 1 to 5.
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| Application Number | Priority Date | Filing Date | Title |
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| CN200810102635A CN101543526A (en) | 2008-03-24 | 2008-03-24 | Kudzu root total aglycone sustained-release pellet as well as preparation method and application thereof |
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| CN200810102635A CN101543526A (en) | 2008-03-24 | 2008-03-24 | Kudzu root total aglycone sustained-release pellet as well as preparation method and application thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103800428A (en) * | 2012-11-15 | 2014-05-21 | 吉林吉春制药股份有限公司 | Medicine for treating yin deficiency and yang excess syndrome of hypertension and coronary heart disease and preparation method thereof |
| CN110381971A (en) * | 2017-03-07 | 2019-10-25 | 株式会社Lg生活健康 | Composition is used in the improvement of Menopause symptom |
-
2008
- 2008-03-24 CN CN200810102635A patent/CN101543526A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103800428A (en) * | 2012-11-15 | 2014-05-21 | 吉林吉春制药股份有限公司 | Medicine for treating yin deficiency and yang excess syndrome of hypertension and coronary heart disease and preparation method thereof |
| CN110381971A (en) * | 2017-03-07 | 2019-10-25 | 株式会社Lg生活健康 | Composition is used in the improvement of Menopause symptom |
| US11026987B2 (en) | 2017-03-07 | 2021-06-08 | Lg Household & Health Care Ltd. | Composition for remedying female climacteric syndrome symptoms |
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Open date: 20090930 |