CN1212113C - Total emodin anthraquinone granule and its prepn and the prepn of dispersive Sanhuang tablet - Google Patents
Total emodin anthraquinone granule and its prepn and the prepn of dispersive Sanhuang tablet Download PDFInfo
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- CN1212113C CN1212113C CN 03107177 CN03107177A CN1212113C CN 1212113 C CN1212113 C CN 1212113C CN 03107177 CN03107177 CN 03107177 CN 03107177 A CN03107177 A CN 03107177A CN 1212113 C CN1212113 C CN 1212113C
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Abstract
The present invention provides rhubarb total anthraquinone granules and a fabrication process for dispersive Sanhuang tablets, which aims to solve the problems that the rhubarb total anthraquinone granules in dispersive Sanhuang tablets produced by the ordinary adhesive agents in the prior art almost have no purgative effect. The present invention provides rhubarb total anthraquinone granules which have the characteristic of releasing drug effect when the granules arrive at the large intestine, the process for preparing the rhubarb total anthraquinone granules, and the process for preparing the dispersive Sanhuang tablets based on the preparation of the granules. The process comprises the steps: preparing adhesive agents with enteric solubility, preparing auxiliary materials of the dispersive Sanhuang tablets, preparing the rhubarb total anthraquinone granules by using the adhesive agents, the auxiliary materials and rhubarb total anthraquinone; preparing baicalin granules and berberine hydrochloride granules by using the auxiliary materials, baicalin and berberine hydrochloride; synthesizing the dispersive Sanhuang tablets by using the two kinds of granules, etc. The rhubarb total anthraquinone granules and the dispersive Sanhuang tablets have the advantages of purgative effect, and also have superior pharmacodynamics index than that of the medicine in the prior art, and the rhubarb total anthraquinone granules can be used singly.
Description
Technical field: the invention belongs to the Chinese medicine preparation technical field, relate in particular to the preparation technology who utilizes method and three-yellow dispersed tablet of total Radix Et Rhizoma Rhei anthraquinone.
Background technology: Chinese patent CZ1335293A disclosed " effective rhubarb component extraction process and SANHUANG quick releasing formulation and preparation method thereof " relates to the extraction of total Radix Et Rhizoma Rhei anthraquinone and utilizes total Radix Et Rhizoma Rhei anthraquinone to prepare the method for three-yellow dispersed tablet.Wherein the extraction of total Radix Et Rhizoma Rhei anthraquinone comprises and uses anion exchange method; The preparation of three-yellow dispersed tablet comprises according to prescription granulates total Radix Et Rhizoma Rhei anthraquinone and baicalin, berberine hydrochloride together with ground and mixed such as sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, stirring, perhaps " SANHUANG " added in the PEG-6000 fused solution of recipe quantity, mix steps such as making drop pill.Further experiment studies show that the total Radix Et Rhizoma Rhei anthraquinone that obtains with anion exchange method almost is dissociated anthraquinone entirely.And introduce according to " CHINA JOURNAL OF CHINESE MATERIA MEDICA " calendar year 2001 the 27th (1) phase 72-74 page or leaf " my opinion about the Radix Et Rhizoma Rhei cathartic large intestine target administration " a literary composition: " because of what play discharge function in the Radix Et Rhizoma Rhei mainly is the combined anthraquinone constituents; the combined anthraquinone constituents mostly be that β-glycoside bond is in conjunction with sugar; after oral not by upper gastrointestinal α-glycoside bond enzyme hydrolysis; after it enters large intestine by enteral β-glycoside bond enzyme hydrolysis; discharge glycoside unit and the performance discharge function; sugar has the function that transhipment glycoside unit arrives site of action-large intestine, and dissociated anthraquinone is the final material that combined anthraquinone produces discharge function in vivo "." medicinal herb components chemistry " the 238th page of record of publishing again according to People's Press 1986: " when oral anthracene derivant class cathartic; must arrive large intestine could produce effects; but before dissociated anthraquinone arrived large intestine, the overwhelming majority had been absorbed or has destroyed, so the diarrhea inducing effect of playing is very weak." so in this patented technology, the total Radix Et Rhizoma Rhei anthraquinone that the Radix Et Rhizoma Rhei of recipe quantity extracts with ion exchange is produced the discharge function that three-yellow dispersed tablet does not reach former SANHUANG PIAN with its disclosed preparation method.
Summary of the invention:
The objective of the invention is,, provide a kind of pharmaceutics means that adopt to make total Radix Et Rhizoma Rhei anthraquinone arrive the method that large intestine discharges again for the total Radix Et Rhizoma Rhei anthraquinone that recipe quantity Radix Et Rhizoma Rhei in the three-yellow dispersed tablet is extracted produces the discharge function of former SANHUANG PIAN.The mentality of designing of this method comprises three partial contents, and first provides a kind of total Radix Et Rhizoma Rhei anthraquinone granule, and this granule has the characteristic that the arrival large intestine discharges again; Second portion provides the particulate process of preparation total Radix Et Rhizoma Rhei anthraquinone; Third part provides with the total Radix Et Rhizoma Rhei anthraquinone granule and prepares the process of three-yellow dispersed tablet with other " Erhuang ", can produce and the same discharge function of former SANHUANG PIAN with the three-yellow dispersed tablet of this process preparation.
Technical solution of the present invention is:
A kind of total Radix Et Rhizoma Rhei anthraquinone granule, it is characterized in that: it contains total Radix Et Rhizoma Rhei anthraquinone 12g, three-yellow dispersed tablet adjuvant 34g, be bonded with 10ml enteric solubility binding agent, wherein, so-called enteric solubility adhesive component comprises polyacrylic resin II number, polyacrylic resin III number and PEG-6000, and this three's content proportioning is: 0~4g: 4~16g: 4~20g; So-called three-yellow dispersed tablet adjuvant component comprises microcrystalline Cellulose, sodium carboxymethyl cellulose and low-substituted hydroxypropyl cellulose, and this three's content proportioning is: 95~155g: 10~40g: 10~40g.
The particulate preparation method of a kind of total Radix Et Rhizoma Rhei anthraquinone is characterized in that being finished by following steps:
(1) preparation enteric solubility binding agent is got polyacrylic resin II number 0~4g, and polyacrylic resin III number 4~16g adds 4~20gPEG-6000, stirs evenly with 100ml 50~95% dissolve with ethanols;
(2) preparation three-yellow dispersed tablet adjuvant is got microcrystalline Cellulose 95~155g, sodium carboxymethyl cellulose 10~40g, low-substituted hydroxypropyl cellulose 10~40g, mix homogeneously;
(3) granulate, get the 12g total Radix Et Rhizoma Rhei anthraquinone and add 34g three-yellow dispersed tablet adjuvant, mix homogeneously adds enteric solubility binding agent 10ml then, and high-speed stirred is granulated, 50 ℃ of dryings, and 50 eye mesh screen granulate are promptly.
A kind of preparation technology of three-yellow dispersed tablet is a raw material with total Radix Et Rhizoma Rhei anthraquinone, baicalin and berberine hydrochloride, it is characterized in that being finished by following steps:
(1) preparation enteric solubility binding agent is got polyacrylic resin II number 0~4g, and polyacrylic resin III number 4~16g adds 4~20gPEG-6000, stirs evenly with 100ml 50~95% dissolve with ethanols;
(2) preparation three-yellow dispersed tablet adjuvant is got microcrystalline Cellulose 95~155g, sodium carboxymethyl cellulose 10~40g, low-substituted hydroxypropyl cellulose 10~40g, mix homogeneously;
(3) preparation total Radix Et Rhizoma Rhei anthraquinone granule is got the 12g total Radix Et Rhizoma Rhei anthraquinone and is added 34g three-yellow dispersed tablet adjuvant, and mix homogeneously adds enteric solubility binding agent 10ml then, and high-speed stirred is granulated, 50 ℃ of dryings, 50 eye mesh screen granulate.
(4) preparation baicalin and berberine hydrochloride granule are got 42g baicalin and 10g berberine hydrochloride and are added aforementioned three-yellow dispersed tablet adjuvant 200g, and mix homogeneously is done binding agent with the aqueous solution of HPMC, and high-speed stirred is granulated, 50 ℃ of dryings, 40 eye mesh screen granulate;
(5) film-making, it is even that the above-mentioned total Radix Et Rhizoma Rhei anthraquinone granule that makes and baicalin and berberine hydrochloride granule are added mix lubricant, tabletting, the bag film-coat, promptly.
Theoretical foundation of the present invention and experimental basis are: generally the pH of gastric juice is 0.9~1.5 in digestive tract, and small intestinal is 6.0~6.8, is 6.5~7.5 at colon.According to gastral pH characteristics, do binding agent with water miscible solid dispersion carrier material and enteric solubility material mixing, enteric solubility material wherein can make total Radix Et Rhizoma Rhei anthraquinone arrival large intestine discharge again, thereby and water miscible solid dispersion carrier material can make total Radix Et Rhizoma Rhei anthraquinone produce enough discharge functions at the large intestine rapid release.Here, the decision of adhesive therefor amount arrives the amount that the large intestine total Radix Et Rhizoma Rhei anthraquinone discharges, and remaining total Radix Et Rhizoma Rhei anthraquinone discharges other effect in SANHUANG PIAN of performance Radix Et Rhizoma Rhei under one's belt with in the small intestinal.The present invention is an index with the discharge function of mice, selects the consumption and the ratio of solid dispersion carrier material and enteric solubility material.
Compare with the disclosed technology of CZ1335293A, because this patent has adopted the technical measures of making binding agent of water miscible solid dispersion carrier material and enteric solubility material mixing, therefore the three-yellow dispersed tablet that makes with this method, the discharge function of people and mice is better than the SANHUANG coated tablet.Certainly, compare with the SANHUANG coated tablet, owing to be to feed intake in this product prescription with total Radix Et Rhizoma Rhei anthraquinone, thus eliminated the difference between crude drug source and the extraction process, so this product steady quality not only, and other pharmacodynamic index all is better than coated tablet.In addition, total Radix Et Rhizoma Rhei anthraquinone granule provided by the invention not only can be used as the raw material goods of preparation three-yellow dispersed tablet, and can be used as the preparation that the Radix Et Rhizoma Rhei single medicinal material is used for the medicine of discharge function, can certainly be as the preparation of using the medicine of Radix Et Rhizoma Rhei discharge function in the compound medicine that Radix Et Rhizoma Rhei is arranged.
The specific embodiment: the present invention is elaborated below in conjunction with embodiment.
Embodiment 1, the total Radix Et Rhizoma Rhei anthraquinone granule.The invention provides the total Radix Et Rhizoma Rhei anthraquinone granule and comprise following constituent content: total Radix Et Rhizoma Rhei anthraquinone 12g, three-yellow dispersed tablet adjuvant 34g is bonded with 10ml enteric solubility binding agent.Enteric solubility adhesive component content wherein comprises polyacrylic resin II number 0~4g, polyacrylic resin III number 4~16g, PEG-6000 4~20g; Three-yellow dispersed tablet adjuvant constituent content wherein comprises microcrystalline Cellulose 95~155g, sodium carboxymethyl cellulose 10~40g, low-substituted hydroxypropyl cellulose 10~40g.
The PEG-6000 here is a water-soluble solid dispersion carrier material, and polyacrylic resin II number, III number are the enteric solubility material.Water-soluble solid dispersion carrier material wherein can also be: the polyvidone class, surfactant such as poloxamer, organic acid such as citric acid, tartaric acid, succinic acid, cholic acid, deoxycholic acid etc., saccharide and alcohols such as dextrose, galactose, sucrose, mannitol, sorbitol, xylitol etc.; Enteric solubility material wherein can also be: cellulose acetate phthalate ester (CAP), Lac, hypromellose phthalate ester (HPMCP) etc.
Embodiment 2, preparation total Radix Et Rhizoma Rhei anthraquinone granule method.This method is finished by following steps:
(1) preparation enteric solubility binding agent is got polyacrylic resin II number 0~4g, and polyacrylic resin III number 4~16g adds 4~20gPEG-6000, stirs evenly with 100ml 50~95% dissolve with ethanols;
(2) preparation three-yellow dispersed tablet adjuvant is got microcrystalline Cellulose 95~155g, sodium carboxymethyl cellulose 10~40g, low-substituted hydroxypropyl cellulose 10~40g, mix homogeneously;
(3) granulate, get the 12g total Radix Et Rhizoma Rhei anthraquinone and add 34g three-yellow dispersed tablet adjuvant, mix homogeneously adds enteric solubility binding agent 10ml then, and high-speed stirred is granulated, 50 ℃ of dryings, and 50 eye mesh screen granulate are promptly.
Embodiment 3, preparation three-yellow dispersed tablet technology.This technology is finished by following steps:
(1) preparation enteric solubility binding agent is got polyacrylic resin II number 0~4g, and polyacrylic resin III number 4~16g adds 4~20gPEG-6000, stirs evenly with 100ml 50~95% dissolve with ethanols;
(2) preparation three-yellow dispersed tablet adjuvant is got microcrystalline Cellulose 95~155g, sodium carboxymethyl cellulose 10~40g, low-substituted hydroxypropyl cellulose 10~40g, mix homogeneously;
(3) preparation total Radix Et Rhizoma Rhei anthraquinone granule is got the 12g total Radix Et Rhizoma Rhei anthraquinone and is added 34g three-yellow dispersed tablet adjuvant, and mix homogeneously adds enteric solubility binding agent 10ml then, and high-speed stirred is granulated, 50 ℃ of dryings, 50 eye mesh screen granulate.
(4) preparation baicalin and berberine hydrochloride granule are got 42g baicalin and 10g berberine hydrochloride and are added aforementioned three-yellow dispersed tablet adjuvant 200g, and mix homogeneously is done binding agent with the aqueous solution of HPMC, and high-speed stirred is granulated, 50 ℃ of dryings, 40 eye mesh screen granulate;
(5) film-making, it is even that the above-mentioned total Radix Et Rhizoma Rhei anthraquinone granule that makes and baicalin and berberine hydrochloride granule are added mix lubricant, tabletting, the bag film-coat, promptly.
Claims (3)
1, a kind of total Radix Et Rhizoma Rhei anthraquinone granule, it is characterized in that: it contains total Radix Et Rhizoma Rhei anthraquinone 12g, the auxilliary 34g that annotates of three-yellow dispersed tablet, be bonded with 10ml enteric solubility binding agent, wherein so-called enteric solubility adhesive component comprises polyacrylic resin II number, polyacrylic resin III number and PEG-6000, and this three's content proportioning is: 0~4g: 4~16g: 4~20g; So-called three-yellow dispersed tablet adjuvant component comprises microcrystalline Cellulose, sodium carboxymethyl cellulose and low-substituted hydroxypropyl cellulose, and this three's content proportioning is: 95~155g: 10~408: 10~40g.
2, the particulate preparation method of a kind of total Radix Et Rhizoma Rhei anthraquinone is characterized in that being finished by following steps:
(1) preparation enteric solubility binding agent is got polyacrylic resin II number 0~4g, and polyacrylic resin III number 4~16g adds 4~20gPEG-6000, stirs evenly with 100ml 50~95% dissolve with ethanols;
(2) preparation three-yellow dispersed tablet adjuvant is got microcrystalline Cellulose 95~155g, sodium carboxymethyl cellulose 10~40g, low-substituted hydroxypropyl cellulose 10~40g, mix homogeneously;
(3) granulate, get the 12g total Radix Et Rhizoma Rhei anthraquinone and add 34g three-yellow dispersed tablet adjuvant, mix homogeneously adds enteric solubility binding agent 10ml then, and high-speed stirred is granulated, 50 ℃ of dryings, and 50 eye mesh screen granulate are promptly.
3, a kind of preparation technology of three-yellow dispersed tablet is a raw material with total Radix Et Rhizoma Rhei anthraquinone, baicalin and berberine hydrochloride, it is characterized in that being finished by following steps:
(1) preparation enteric solubility binding agent is got polyacrylic resin II number 0~4g, and polyacrylic resin III number 4~16g adds 4~20gPEG-6000, stirs evenly with 100ml 50~95% dissolve with ethanols;
(2) preparation three-yellow dispersed tablet adjuvant is got microcrystalline Cellulose 95~155g, sodium carboxymethyl cellulose 10~40g, low-substituted hydroxypropyl cellulose 10~40g, mix homogeneously;
(3) preparation total Radix Et Rhizoma Rhei anthraquinone granule is got the 12g total Radix Et Rhizoma Rhei anthraquinone and is added 34g three-yellow dispersed tablet adjuvant, and mix homogeneously adds enteric solubility binding agent 10ml then, and high-speed stirred is granulated, 50 ℃ of dryings, 50 eye mesh screen granulate.
(4) preparation baicalin and berberine hydrochloride granule are got 42g baicalin and 10g berberine hydrochloride and are added aforementioned three-yellow dispersed tablet adjuvant 200g, and mix homogeneously is done binding agent with the aqueous solution of HPMC, and high-speed stirred is granulated, 50 ℃ of dryings, 40 eye mesh screen granulate;
(5) film-making, it is even that the above-mentioned total Radix Et Rhizoma Rhei anthraquinone granule that makes and baicalin and berberine hydrochloride granule are added mix lubricant, tabletting, the bag film-coat, promptly.
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CN 03107177 CN1212113C (en) | 2003-03-06 | 2003-03-06 | Total emodin anthraquinone granule and its prepn and the prepn of dispersive Sanhuang tablet |
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CN107184563A (en) * | 2017-05-31 | 2017-09-22 | 潘小平 | Micro-capsule, the preparation method and use of Physcion and its derivative |
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