CN1278722C - Orally disintegrating tablet of 'Baibaodan' and its preparation - Google Patents
Orally disintegrating tablet of 'Baibaodan' and its preparation Download PDFInfo
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Abstract
The present invention discloses a 'Baibaodan' orally disintegrating tablet and a preparation method thereof. The present invention is characterized in that the 'Baibaodan' orally disintegrating tablet is prepared from effective components extracted from notoginseng, processed Yunnan aconitum kusnezoffii, psammosilene tunicoides root and paris root, and pharmaceutical adjuvant; a composite disintegrating agent containing erythritol is also used; erythritol and chitin or low-substituted hydroxypropyl cellulose or sodium carboxymethyl starch or crosslinked sodium carboxymethyl starch or non-soluble crosslinked polyvinyl pyrrolidone are combined with raw materials according to a certain proportion to prepare a composite disintegrating agent. Since erythritol has the effect of corrigents simultaneously, the dosage of pharmaceutical adjuvant of the preparation is reduced; pharmacological experiments show that the 'Baibaodan' orally disintegrating tablet of the present invention has the characteristics of quick disintegration, rapid effect-taking and excellent pharmacological action.
Description
Technical field
The invention belongs to technical field of traditional Chinese medicine pharmacy, be specifically related to a kind of cure-all oral cavity disintegration tablet and preparation method thereof.
Background technology
Oral cavity disintegration tablet is a kind of new pharmaceutical preparation, and it can absorb through hypoglossis mucous membrane, directly enters blood, has avoided first pass effect effectively, so taking dose is little, and safety is good, and effect rapidly.Though be oral formulations, can reach the effect of ejection preparation.Therefore just progressively become the focus that pharmaceutical manufacturer and research and development field are paid close attention to.This dosage form mainly is to select suitable fast disintegrant, by the existing certain rigidity of its tablet of making, certain sedimentation is arranged again.Can not need the water assisting deglutition when taking, can rapid disintegrate become fine grained in the oral cavity, only several swallowing acts can be finished drug administration process.Its more common solid orally ingestible absorbs fast, bioavailability height, and taking convenience.
The preparation oral cavity disintegration tablet will be considered the problem of following critical aspects: 1, the advantage of oral cavity disintegration tablet just is rapid disintegrate, and it is fast to discharge medicine, reaches rapid-action effect, seeks suitable disintegrants, to guarantee oral cavity disintegration tablet disintegrate rapidly in the oral cavity; 2, seek relatively inexpensive pharmaceutic adjuvant, to reduce production cost; 3, only need the just disintegrate fully of water of minute quantity owing to disintegrating tablet, therefore must consider stability, prolongation shelf life and the shelf-life of humidity environment oral cavity disintegration tablet higher relatively in the process of storage, significant to medical manufacturing enterprise.
Disintegrating agent is commonly used in the oral cavity disintegration tablet adjuvant have low-substituted hydroxypropyl cellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa), crospolyvinylpyrrolidone (PVPP), crosslinked carboxymethylstach sodium (CCMS-Na) etc. [He Jianchang, etc.New oral solid quick releasing formulation-oral cavity quick disintegrating slice.The pharmacy practice magazine, 2000,18 (3): 151].These adjuvants are all water insoluble, but a common characteristic is all arranged, and have hygroscopicity [pharmaceutical preparation portion of Shanghai Institute of Pharmaceutical Industry, Pharmaceutical National Engineering Research Center exactly.Pharmaceutic adjuvant application technology (second edition), Chinese Medicine science and technology publishing house, 2002,73～75].In the higher environment of humidity, oral cavity disintegration tablet is the moisture absorption especially easily, and cracked trend is arranged.So relatively harsher to environment requirement in production, storage and transportation with the oral cavity disintegration tablet that these adjuvants are made, must adopt special packing, seal cover, desiccant bag etc., all can produce considerable influence to production cost.And above-mentioned disintegrating agent all is synthetic through chemical process, and price is higher, for the more relatively oral cavity disintegration tablet of adjuvant content, can cause production cost to increase, and and then can increase patient's financial burden.Therefore, seek disintegrating agent functional, that price is suitable, make that the disintegration time of oral cavity disintegration tablet is shorter, price is more cheap, stability better becomes one of key problem in technology of exploitation oral cavity disintegration tablet.
Application number is 99802175 patent application bibliographical information, and during as disintegrating agent, the hardness of making oral cavity disintegration tablet is identical with disintegration time at the erythritol that uses separately equivalent or low-substituted hydroxypropyl cellulose (L-HPC).The erythritol sweet taste is pure, after eating nice and cool mouthfeel characteristic is arranged, and also can make correctives and use, and reduces the weight of oral cavity disintegration tablet.Erythritol can not influence normal carbohydrate metabolism, is fit to diabetes patient; And be sweet taste material low in calories, be suitable for obese patients, simultaneously caries prevention is also had positive role.
Chitin is the relatively low natural pharmaceutic adjuvant of a kind of price, and it has another name called chitin, chitin, is a kind of biological polysaccharide polymer material, extensively is present in the carapace in the unicellular lower eukaryote.This material can be degraded by lyase, has excellent biological compatibility, avirulence, chemical property quite stable.
Standard No. WS-11350 (ZD-1350)-2002 has write down the standard of BAIBAODAN JIAONANG, this standard is simply pulverized four flavor Chinese medicines, just incapsulates, and is prepared into BAIBAODAN JIAONANG, this method is not extracted purification to each flavor Chinese medicine, has strengthened patient's dose; Do not retrieve relevant cure-all oral cavity disintegration tablet Patent data.
Summary of the invention
For these reasons, in the selection course that disintegrating agent uses in oral cavity disintegration tablet, we discover that erythritol and disintegrating agent commonly used at present mix by a certain percentage, form a kind of compound disintegrating agent and have more performance, the oral cavity disintegration tablet made from it compares with the simple oral cavity disintegration tablet that uses erythritol or disintegrating agent commonly used at present to make, the disintegration time of oral cavity disintegration tablet was shortened, and because erythritol does not have hygroscopicity, the stability of the feasible oral cavity disintegration tablet of making significantly improves.In the compound disintegrating agent, erythritol is in the amount ranges of 30%-70%, and along with the increase of content, the disintegration time of oral cavity disintegration tablet shortens, and stability strengthens.
We find that in experiment chitin disintegrating agent effect with commonly used at present aspect the disintegrate effect is suitable, even are better than disintegrating agent commonly used.
We have studied compound disintegrating agent in experiment, select the mixture of use erythritol and chitin, disintegrating agent commonly used, are based on many-sided consideration.When making disintegrating agent with single erythritol, though erythritol does not have hygroscopicity, the tablet stability of making is good, and the swelling degree after the single erythritol suction is less, influences the disintegrating property of oral cavity disintegration tablet, and disintegration time is prolonged.Add a certain amount of disintegrating agent commonly used, utilize rapid expansible character after their moisture absorptions, neither influence the stability of oral cavity disintegration tablet, also kept the characteristic of its rapid disintegrate, reached reasonable effect.
The present invention carries out alcohol extraction to Radix Notoginseng in the cure-all and obtains effective site, Radix Aconiti Kusnezoffii (system) water is carried purification with macroreticular resin obtain effective site, Rhizoma Paridis is carried out ethanol percolate extraction obtain effective site, Radix Psammosilenes is carried out water extract-alcohol precipitation to be obtained effective site and mixes with disintegrating agent of the present invention, add filler, granulate, add lubricant, tabletting, obtain the cure-all disintegrating tablet, The pharmacological results shows, cure-all oral cavity disintegration tablet of the present invention has that disintegrate is fast, onset is rapid, the better characteristics of pharmacological action.
The present invention is achieved through the following technical solutions.
One. process recipes
(1) crude drug of the present invention consists of:
Radix Notoginseng 7.5 weight portions, Radix Aconiti Kusnezoffii (system) 80 weight portions, Rhizoma Paridis 62.5 weight portions, trivial 100 weight portions of aufe
(2) get notoginseng decoction piece and pulverize, cross the 10-15 mesh sieve, get the Radix Notoginseng of pulverizing, add that 5-8 doubly measures, the ethanol extraction of 60%-80% 2-4 time, each 2-4 hour, filtration, filtrate recycling ethanol is extremely most, and the vacuum concentration drying obtains Sanchi effective-component;
(3) get Radix Aconiti Kusnezoffii (system) decoction pieces, pulverize, soaked 0.5-1 hour, add 10-20 times of decocting again and boil 2 times, each 1-2 hour, filter, relative density was 1.05-1.10 when merging filtrate, filtrate were concentrated to 50 ℃, last AB-8 type macroporous adsorptive resins, carry out eluting with 6-8 times of water, discard water lotion, reuse 8-10 doubly, the ethanol elution of 75%-85%, merge eluent, reclaim ethanol to the greatest extent, the vacuum concentration drying obtains the effective site of Radix Aconiti Kusnezoffii (system);
(4) get Rhizoma Paridis, with 6-10 doubly, soak with ethanol 24-36 hour of 60%-70%, filter, filtrate recycling ethanol is to the greatest extent, the vacuum concentration drying obtains Rhizoma Paridis effective site;
(5) get Radix Psammosilenes, add 10-20 times of decocting and boil 2-5 time, each 2-5 hour, filter, merging filtrate, relative density is the extractum of 1.20-1.30 when being concentrated into 60 ℃, adds ethanol and makes and contain the alcohol amount and be 50%-80%, leaves standstill 24 hours, filter, filtrate recycling ethanol is to most, and the vacuum concentration drying obtains Radix Psammosilenes effective site; (6) with Sanchi effective-component 0.7-1.5 weight portion,, Radix Aconiti Kusnezoffii (system) effective site is the 8-16 weight portion, Rhizoma Paridis effective site 6-13 weight portion, Radix Psammosilenes effective site is that the 10-20 weight portion mixes with disintegrating agent 44-52 weight portion of the present invention, add filler 100.2-117.5 weight portion, granulate, add lubricant 5.3-5.8 weight portion, tabletting obtains the cure-all disintegrating tablet.
The compound disintegrating agent of the present invention is by erythritol and chitin or low-substituted hydroxypropyl methylcellulose or carboxymethyl
Starch Sodium or crosslinked carboxymethyl fecula sodium or insoluble crospolyvinylpyrrolidone are formed, both compound disintegrate
The percentage by weight of agent mesoerythrit is 30%-70%.
A kind of for in the microcrystalline Cellulose, nano micro crystal cellulose of filler.
Lubricant is a kind of in magnesium stearate, Pulvis Talci, the Stepanol MG.
Two. the disintegrating agent performance is investigated experiment
Experimental raw: erythritol, chitin, low-substituted hydroxypropyl methylcellulose, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, insoluble crospolyvinylpyrrolidone, buy by market.
Experimental technique:
(1) solubility experiment: the saturated aqueous solution at 37 ℃ of preparation samples, utilize membrane filter to filter, obtain filtrate, the filtrate of predetermined of accurately weighing is utilized the freeze-drying drying, thereby is obtained the content of water, calculate water-soluble on the water content basis that obtains thus again, the results are shown in Table 1.
(2) viscosity experiment: the saturated aqueous solutions at 37 ℃ of different disintegrating agents of preparation, utilize membrane filter to filter, obtain filtrate, utilize viscometer to obtain filtrate 37 ℃ viscosity, the results are shown in Table 1.
(3) measurement of wettability: precision takes by weighing above-mentioned disintegrating agent, dry weighs fully, is put into 1 week under 25 ℃ and 75% the damp condition, takes by weighing weight, and calculating wettability (%) sees Table 1.
(4) volume increases percent: the volume of moisture absorption fore-and-aft survey disintegrating agent, calculate the percent (%) of the volume increase of disintegrating agent, and see Table 1.
Table 1 disintegrating agent performance is investigated relatively
| Disintegrating agent | Dissolubility (37 ℃) W/V | Viscosity (37 ℃) mpa.s | Wettability % | Volume increases percent % |
| The insoluble crospolyvinylpyrrolidone of erythritol chitin low-substituted hydroxypropyl methylcellulose carboxymethyl starch sodium crosslinked carboxymethyl fecula sodium | 45 - - - - - | 3.5 - - - - - | 0.03 11.29 14.09 21.07 22.18 22.64 | 0.02 16.57 20.36 22.89 28.14 27.62 |
Conclusion: the characteristics of investigating experiment and oral cavity disintegration tablet by above-mentioned performance, we can analyze, erythritol has very big advantage as disintegrating agent in wettability, but because its moisture pick-up properties is very little, volume increase degree is also very little, therefore, in disintegrating procedue volumetric expansion slow, can not reach the requirement of the rapid disintegrate of oral cavity disintegration tablet; Erythritol is again good correctives simultaneously, not only can be used as disintegrating agent but also can be used as correctives if choose suitable weight, can significantly reduce consumption, the operation in the formulation preparation process and the cost of preparation of pharmaceutic adjuvant; Other disintegrating agent hygroscopicity are too big, cause oral cavity disintegration tablet very poor aspect stable; By analyzing, erythritol is carried out mixing of proper proportion with other disintegrating agent, the compound disintegrating agent as oral cavity disintegration tablet has good advantages.
Three. the selection of compound disintegrating agent
Experimental raw: choose crosslinked carboxymethyl fecula sodium and carry out different proportion with erythritol and mix, mixed proportion is respectively erythritol: crosslinked carboxymethyl fecula sodium=1: 9 or 2: 8 or 3: 7 or 4: 6 or 5: 5 or 6: 4 or 7: 3 or 8: 2 or 9: 1, totally 9 groups, be respectively experimental group 1-9, with experimental group 1-9 and same filler (in microcrystalline Cellulose, the nano micro crystal cellulose a kind of) and lubricant (in magnesium stearate, Pulvis Talci, the Stepanol MG a kind of), carry out tabletting; Change above-mentioned disintegrating agent into chitin,, be experimental group 10, carry out tabletting with same filler, mix lubricant with weight; Change above-mentioned disintegrating agent into weight crosslinked carboxymethyl fecula sodium, with same filler, mix lubricant, experimental group 11 carries out tabletting.
Experimental technique:
(1) hardness of mensuration tablet: utilize the tablet hardness tester to measure the hardness of tablet, the results are shown in Table 2.
(2) stability experiment: tablet is put into 12 weeks under 25 ℃ and 75% the damp condition, observes the tablet spoilage, the results are shown in Table 2.
(3) disintegrate experiment: according to the disintegration of tablet method of testing of stipulating in the Pharmacopoeia of People's Republic of China, utilize the disintegrate tester to measure, the results are shown in Table 2.
(4) disintegrate test in the oral cavity, disintegration time, grittiness, taste to three health adults have tested experimental group the results are shown in Table 2.
The selection of table 2 experimental group disintegrating agent
| Experimental group | Hardness (kg) | Spoilage (%) | Disintegration time (s) | The Orally disintegrating time (s) | Grittiness | Taste |
| 1 2 3 4 | 4.1 3.9 2.1 2.2 | 22.1 21.6 9.3. 8.6 | 42.1 43.6 26.3 25.2 | 51.2 52.9 32.9 28.3 | Have seldom | Bad generally carefully |
| 5 6 7 8 9 10 11 | 2.2 2.1 2.0 1.9 1.8 4.6 4.8 | 8.1 8.6 9.3 9.6 10.2 33.9 36.5 | 26.1 26.9 26.8 35.9 35.6 54.1 55.6 | 26.7 27.4 27.3 38.6 39.1 62.9 62.8 | Seldom having much has a lot | Good very poor carefully carefully |
Change above-mentioned chitin, crosslinked carboxymethyl fecula sodium into chitosan, low-substituted hydroxypropyl methylcellulose, crosslinked carboxymethyl fecula sodium, crosslinked insoluble polyvinylpyrrolidone (PH-J), experimentize, the result of experiment conclusion and table 2 is close.
Conclusion: experimental result shows, erythritol is mixed with into the mixing disintegrating agent with other disintegrating agent, has good effect, simultaneously because erythritol has sweet taste, so can reduce or replace correctives to use, by experiment erythritol: the suitable ratio of other disintegrating agent be 3-7: 7-3.
Four. check and analysis
The method of [assay] detects in the standard according to standard No. WS-11350 (ZD-1350)-2002, the results are shown in 3.
Table 3 content relatively
| The medicine group | Radix Notoginseng is in the ginsenoside Rg1 |
| BAIBAODAN JIAONANG cure-all oral cavity disintegration tablet of the present invention | 0.1164mg/ grain 0.1359mg/ sheet |
Conclusion: by the check and analysis experiment, the active constituent content of oral cavity disintegration tablet of the present invention significantly improves, and proves absolutely that technology of the present invention has remarkable meaning.
Five. the preparation disintegration time mensuration
In order to prove absolutely that the employed compound disintegrating agent of cure-all oral cavity disintegration tablet of the present invention has disintegrate characteristics rapidly than single disintegrating agent, we have carried out following experiment: disintegrating agent is selected in the design by table 4 for use, make into oral cavity disintegration tablet with effective ingredient at identical pressure lower sheeting, place the beaker of the 10ml that fills 5ml37 ℃ of water, stir with 30 rev/mins speed, measure the disintegration of the oral cavity disintegration tablet that contains different disintegrating agents.
The disintegration time mensuration of the different disintegrating agents of table 4
| The experiment number | Disintegrating agent | Disintegration (s) | |
| Form | Consumption (g: g) | ||
| 1 2 3 4 5 6 7 8 9 10 | Chitin antierythrite: chitin low-substituted hydroxypropyl methylcellulose antierythrite: low-substituted hydroxypropyl methylcellulose sodium carboxymethyl starch antierythrite: sodium carboxymethyl starch crosslinked carboxymethyl fecula sodium antierythrite: the insoluble PVPP antierythrite of crosslinked carboxymethyl fecula sodium: insoluble PVPP | - (3∶7) - (4∶6) - (5∶5) - (6∶4) - (7∶3) | 30.8 17.7 27.4 16.3 38.5 15.6 40.1 14.3 33.5 13.5 |
The result: the oral cavity disintegration tablet that uses compound disintegrating agent is in 13.5-17.7 all disintegrates and by No. 2 sieves in second; The oral cavity disintegration tablet that uses single disintegrating agent is in 27.4-40.1 all disintegrates and by No. 2 sieves in second.Illustrate that compound disintegrating agent of the present invention has disintegrate characteristics rapidly really.
Six. the disintegration experiment
Get cure-all oral cavity disintegration tablet of the present invention, place the beaker of the 10ml that fills 5ml37 ℃ of water, stir with 30 rev/mins speed.Oral cavity disintegration tablet of the present invention whole disintegrates in 20 seconds are also sieved by No. 2.
Seven. the dissolution experiment
1. instrument and reagent: the full-automatic digestion instrument of SR-6 type (U.S. Hanson company); Distilled water (self-control) BAIBAODAN JIAONANG (Kunming Chinese Medicine Factory Co., Ltd.); Cure-all oral cavity disintegration tablet (Qianluchun Science and Technology Co., Ltd., Beijing's laboratory provides).
2. experimental technique: second method of pressing in the dissolution method (" 2000 editions two appendix XC of Chinese pharmacopoeia) is measured.Each container fills the distilled water through degassing processing of 100ml, and heating makes water temperature remain on 37 ℃ ± 0.5 ℃, and rotating speed of agitator is 50 rev/mins.Put into 1 of cure-all oral cavity disintegration tablet of the present invention, in the time of 20 minutes, get 2ml solution, centrifugal 10 minutes (12000rpm), supernatant is as need testing solution.Measure with ginsenoside Rg1's assay method with above-mentioned check and analysis Radix Notoginseng.The results are shown in Table 5.
The dissolution of two kinds of medicines of table 5 relatively
| The medicine group | Sample time, (min) Radix Notoginseng was with ginsenoside Rg1 (mg) | |||||||
| 0.5 | 1 | 2 | 4 | 8 | 12 | 16 | 20 | |
| BAIBAODAN JIAONANG cure-all oral cavity disintegration tablet | 0.0245 0.0681 | 0.0357 0.0712 | 0.0412 0.9812 | 0.0512 0.1104 | 0.0635 0.1357 | 0.0834 0.1358 | 0.9472 0.1359 | 0.1041 0.1359 |
Conclusion: strippings in 30 seconds of cure-all oral cavity disintegration tablet of the present invention were dissolved almost completely in the time of 50%, 8 minute.
Seven. pharmacology embodiment
The influence of Dichlorodiphenyl Acetate induced mice writhing response
Laboratory animal: Kunming mouse, body weight 20 ± 2g.Provide by Peking University's Experimental Animal Center.
Experiment medicine: BAIBAODAN JIAONANG (Kunming Chinese Medicine Factory Co., Ltd.); Cure-all oral cavity disintegration tablet (Qianluchun Science and Technology Co., Ltd., Beijing's laboratory provides);
Experimental technique: with 60 rats, be divided into 3 groups at random, 20 every group.1 group is the blank group, gavages the 0.5%CMC-Na with volume; 2 groups is the BAIBAODAN JIAONANG group; 3 groups is cure-all oral cavity disintegration tablet group.Successive administration 5 days, last administration are after 1 hour, and every Mus lumbar injection 0.6% acetum 0.2ml/10g observes and writes down in the mice 15min and turn round the body number of times.Experimental result sees Table 6.
The influence of table 6 cure-all preparation Dichlorodiphenyl Acetate induced mice writhing response
| Group | n | Turn round body number of times (inferior) |
| Blank group BAIBAODAN JIAONANG group cure-all oral cavity disintegration tablet | 20 20 20 | 39.24±9.76 28.93±8.66 ** 19.64±6.58 **[ *] |
Annotate: compare with the blank group
*P＜0.01, compare with positive controls [
*] P＜0.05
Conclusion: show that by pharmacological evaluation cure-all oral cavity disintegration tablet of the present invention has better pharmacological action.
Eight. preparation embodiment
Embodiment 1
(1) crude drug of the present invention consists of:
Radix Notoginseng 7.5 grams, Radix Aconiti Kusnezoffii (system) 80 grams, Rhizoma Paridis 62.5 grams, trivial 100 grams of aufe;
(2) get notoginseng decoction piece and pulverize, cross 10 mesh sieves, get the Radix Notoginseng of pulverizing, add 5 times of amounts, 60% ethanol extraction 2 times, each 2 hours, filter, filtrate recycling ethanol is extremely most, and the vacuum concentration drying obtains Sanchi effective-component 0.7 and restrains;
(3) get Radix Aconiti Kusnezoffii (system) decoction pieces, pulverize, soaked 0.5 hour, add 10 times of decoctings again and boil 2 times, each 1 hour, filter, relative density was 1.05 when merging filtrate, filtrate were concentrated to 50 ℃, last AB-8 type macroporous adsorptive resins, carry out eluting with 6 times of water, discard water lotion, 8 times of reuse, 75% ethanol elution, merge eluent, reclaim ethanol to most, the vacuum concentration drying, the effective site 8 that obtains Radix Aconiti Kusnezoffii (system) restrains;
(4) get Rhizoma Paridis, with 6 times, 60% soak with ethanol 24 hours, filter, filtrate recycling ethanol is to the greatest extent, and the vacuum concentration drying obtains Rhizoma Paridis effective site 6 grams;
(5) get Radix Psammosilenes, add 10 times of decoctings and boil 2 times, each 2 hours, filter, merging filtrate, relative density is 1.20 extractum when being concentrated into 60 ℃, adds ethanol and makes that to contain the alcohol amount be 50%, leaves standstill 24 hours, filter, filtrate recycling ethanol is to most, and the vacuum concentration drying obtains Radix Psammosilenes effective site 10 grams;
(6) with Sanchi effective-component 0.7 gram,, Radix Aconiti Kusnezoffii (system) effective site be 8 the gram, Rhizoma Paridis effective site 6 grams, Radix Psammosilenes effective site is that 10 grams mix with disintegrating agent 52 grams of the present invention, add filler microcrystalline Cellulose 117.5 grams, granulate, add magnesium stearate lubricant 5.8 grams, tabletting obtains 1000 of cure-all disintegrating tablets.
The compound disintegrating agent of the present invention is made up of erythritol and chitin or low-substituted hydroxypropyl methylcellulose or carboxymethyl starch sodium or crosslinked carboxymethyl fecula sodium or insoluble crospolyvinylpyrrolidone, and the percentage by weight of both compound disintegrating agent mesoerythrit is 30%-70%.
Embodiment 2
(1) crude drug of the present invention consists of:
Radix Notoginseng 7.5 grams, Radix Aconiti Kusnezoffii (system) 80 grams, Rhizoma Paridis 62.5 grams, trivial 100 grams of aufe;
(2) get notoginseng decoction piece and pulverize, cross 15 mesh sieves, get the Radix Notoginseng of pulverizing, add 8 times of amounts, 80% ethanol extraction 4 times, each 4 hours, filter, filtrate recycling ethanol is extremely most, and the vacuum concentration drying obtains Sanchi effective-component 1.5 and restrains;
(3) get Radix Aconiti Kusnezoffii (system) decoction pieces, pulverize, soaked 1 hour, add 20 times of decoctings again and boil 2 times, each 2 hours, filter, relative density was 1.10 when merging filtrate, filtrate were concentrated to 50 ℃, last AB-8 type macroporous adsorptive resins, carry out eluting with 8 times of water, discard water lotion, 10 times of reuse, 85% ethanol elution, merge eluent, reclaim ethanol to most, the vacuum concentration drying, the effective site 16 that obtains Radix Aconiti Kusnezoffii (system) restrains;
(4) get Rhizoma Paridis, with 10 times, 70% soak with ethanol 36 hours, filter, filtrate recycling ethanol is to the greatest extent, and the vacuum concentration drying obtains Rhizoma Paridis effective site 13 grams;
(5) get Radix Psammosilenes, add 20 times of decoctings and boil 5 times, each 5 hours, filter, merging filtrate, relative density is 1.30 extractum when being concentrated into 60 ℃, adds ethanol and makes that to contain the alcohol amount be 80%, leaves standstill 24 hours, filter, filtrate recycling ethanol is to most, and the vacuum concentration drying obtains Radix Psammosilenes effective site 20 grams;
(6) with Sanchi effective-component 1.5 grams,, Radix Aconiti Kusnezoffii (system) effective site be 16 the gram, Rhizoma Paridis effective site 13 grams, Radix Psammosilenes effective site is 20 grams and disintegrating agent 44 grams of the present invention, add filler nano micro crystal cellulose 100.2 grams, granulate, add lubricant Pulvis Talci 5.3 grams, tabletting obtains 1000 of cure-all disintegrating tablets.
The compound disintegrating agent of the present invention is made up of erythritol and chitin or low-substituted hydroxypropyl methylcellulose or carboxymethyl starch sodium or crosslinked carboxymethyl fecula sodium or insoluble crospolyvinylpyrrolidone, and the percentage by weight of both compound disintegrating agent mesoerythrit is 30%-70%.
Embodiment 3
(1) crude drug of the present invention consists of:
Radix Notoginseng 7.5 grams, Radix Aconiti Kusnezoffii (system) 80 grams, Rhizoma Paridis 62.5 grams, trivial 100 grams of aufe;
(2) get notoginseng decoction piece and pulverize, cross 10 mesh sieves, get the Radix Notoginseng of pulverizing, add 6 times of amounts, 65% ethanol extraction 3 times, each 3 hours, filter, filtrate recycling ethanol is extremely most, and the vacuum concentration drying obtains Sanchi effective-component 0.8 and restrains;
(3) get Radix Aconiti Kusnezoffii (system) decoction pieces, pulverize, soaked 0.6 hour, add 12 times of decoctings again and boil 2 times, each 1.5 hours, filter, relative density was 1.06 when merging filtrate, filtrate were concentrated to 50 ℃, last AB-8 type macroporous adsorptive resins, carry out eluting with 7 times of water, discard water lotion, 9 times of reuse, 80% ethanol elution, merge eluent, reclaim ethanol to most, the vacuum concentration drying, the effective site 9 that obtains Radix Aconiti Kusnezoffii (system) restrains;
(4) get Rhizoma Paridis, with 7 times, 65% soak with ethanol 28 hours, filter, filtrate recycling ethanol is to the greatest extent, and the vacuum concentration drying obtains Rhizoma Paridis effective site 8 grams;
(5) get Radix Psammosilenes, add 12 times of decoctings and boil 3 times, each 3 hours, filter, merging filtrate, relative density is 1.25 extractum when being concentrated into 60 ℃, adds ethanol and makes that to contain the alcohol amount be 55%, leaves standstill 24 hours, filter, filtrate recycling ethanol is to most, and the vacuum concentration drying obtains Radix Psammosilenes effective site 14 grams;
(6) with Sanchi effective-component 0.8 gram, Radix Aconiti Kusnezoffii (system) effective site is 9 grams, Rhizoma Paridis effective site 8 grams, Radix Psammosilenes effective site is that 14 grams mix with disintegrating agent 50.5 grams of the present invention, add filler microcrystalline Cellulose 112.3 grams, granulate, add lubricant Stepanol MG 5.4 grams, tabletting obtains 1000 of cure-all disintegrating tablets.
The compound disintegrating agent of the present invention is made up of erythritol and chitin or low-substituted hydroxypropyl methylcellulose or carboxymethyl starch sodium or crosslinked carboxymethyl fecula sodium or insoluble crospolyvinylpyrrolidone, and the percentage by weight of both compound disintegrating agent mesoerythrit is 30%-70%.
Embodiment 4
(1) crude drug of the present invention consists of:
Radix Notoginseng 7.5 grams, Radix Aconiti Kusnezoffii (system) 80 grams, Rhizoma Paridis 62.5 grams, trivial 100 grams of aufe;
(2) get notoginseng decoction piece and pulverize, cross 15 mesh sieves, get the Radix Notoginseng of pulverizing, add 7 times of amounts, 70% ethanol extraction 3 times, each 2 hours, filter, filtrate recycling ethanol is extremely most, and the vacuum concentration drying obtains Sanchi effective-component 1.2 and restrains;
(3) get Radix Aconiti Kusnezoffii (system) decoction pieces, pulverize, soaked 0.8 hour, add 16 times of decoctings again and boil 2 times, each 2 hours, filter, relative density was 1.09 when merging filtrate, filtrate were concentrated to 50 ℃, last AB-8 type macroporous adsorptive resins, carry out eluting with 6 times of water, discard water lotion, 10 times of reuse, 85% ethanol elution, merge eluent, reclaim ethanol to most, the vacuum concentration drying, the effective site 15 that obtains Radix Aconiti Kusnezoffii (system) restrains;
(4) get Rhizoma Paridis, with 9 times, 70% soak with ethanol 30 hours, filter, filtrate recycling ethanol is to the greatest extent, and the vacuum concentration drying obtains Rhizoma Paridis effective site 12 grams;
(5) get Radix Psammosilenes, add 18 times of decoctings and boil 4 times, each 4 hours, filter, merging filtrate, relative density is 1.28 extractum when being concentrated into 60 ℃, adds ethanol and makes that to contain the alcohol amount be 70%, leaves standstill 24 hours, filter, filtrate recycling ethanol is to most, and the vacuum concentration drying obtains Radix Psammosilenes effective site 18 grams;
(6) with Sanchi effective-component 1.2 grams,, Radix Aconiti Kusnezoffii (system) effective site be 15 the gram, Rhizoma Paridis effective site 12 grams, Radix Psammosilenes effective site is that 18 grams mix with disintegrating agent 46.1 grams of the present invention, add filler microcrystalline Cellulose 102.1 grams, granulate, add magnesium stearate lubricant 5.6 grams, tabletting obtains 1000 of cure-all disintegrating tablets.
The compound disintegrating agent of the present invention is made up of erythritol and chitin or low-substituted hydroxypropyl methylcellulose or carboxymethyl starch sodium or crosslinked carboxymethyl fecula sodium or insoluble crospolyvinylpyrrolidone, and the percentage by weight of both compound disintegrating agent mesoerythrit is 30%-70%.
Embodiment 5
(1) crude drug of the present invention consists of:
Radix Notoginseng 75 grams, Radix Aconiti Kusnezoffii (system) 800 grams, Rhizoma Paridis 625 grams, trivial 1000 grams of aufe
(2) get notoginseng decoction piece and pulverize, cross 10 mesh sieves, get the Radix Notoginseng of pulverizing, add 6 times of amounts, 75% ethanol extraction 2 times, each 4 hours, filter, filtrate recycling ethanol is extremely most, and the vacuum concentration drying obtains Sanchi effective-component 14.2 and restrains;
(3) get Radix Aconiti Kusnezoffii (system) decoction pieces, pulverize, soaked 0.5 hour, add 20 times of decoctings again and boil 2 times, each 1 hour, filter, relative density was 1.07 when merging filtrate, filtrate were concentrated to 50 ℃, last AB-8 type macroporous adsorptive resins, carry out eluting with 6 times of water, discard water lotion, 10 times of reuse, 75% ethanol elution, merge eluent, reclaim ethanol to most, the vacuum concentration drying, the effective site 146 that obtains Radix Aconiti Kusnezoffii (system) restrains;
(4) get Rhizoma Paridis, with 8 times, 65% soak with ethanol 32 hours, filter, filtrate recycling ethanol is to the greatest extent, and the vacuum concentration drying obtains Rhizoma Paridis effective site 124 grams;
(5) get Radix Psammosilenes, add 18 times of decoctings and boil 4 times, each 3 hours, filter, merging filtrate, relative density is 1.28 extractum when being concentrated into 60 ℃, adds ethanol and makes that to contain the alcohol amount be 75%, leaves standstill 24 hours, filter, filtrate recycling ethanol is to most, and the vacuum concentration drying obtains Radix Psammosilenes effective site 182 grams;
(6) with Sanchi effective-component 14.2 grams,, Radix Aconiti Kusnezoffii (system) effective site be 146 the gram, Rhizoma Paridis effective site 124 grams, Radix Psammosilenes effective site is that 182 grams mix with disintegrating agent 460 grams of the present invention, add filler nano micro crystal cellulose 1016.6 grams, granulate, add lubricant Stepanol MG 57.2 grams, tabletting obtains 10000 of cure-all disintegrating tablets.
The compound disintegrating agent of the present invention is made up of erythritol and chitin or low-substituted hydroxypropyl methylcellulose or carboxymethyl starch sodium or crosslinked carboxymethyl fecula sodium or insoluble crospolyvinylpyrrolidone, and the percentage by weight of both compound disintegrating agent mesoerythrit is 30%-70%.
Embodiment 6
(1) crude drug of the present invention consists of:
Radix Notoginseng 15 grams, Radix Aconiti Kusnezoffii (system) 160 grams, Rhizoma Paridis 125 grams, trivial 200 grams of aufe;
(2) get notoginseng decoction piece and pulverize, cross 15 mesh sieves, get the Radix Notoginseng of pulverizing, add 7 times of amounts, 65% ethanol extraction 3 times, each 4 hours, filter, filtrate recycling ethanol is extremely most, and the vacuum concentration drying obtains Sanchi effective-component 2.6 and restrains;
(3) get Radix Aconiti Kusnezoffii (system) decoction pieces, pulverize, soaked 0.5 hour, add 19 times of decoctings again and boil 2 times, each 2 hours, filter, relative density was 1.08 when merging filtrate, filtrate were concentrated to 50 ℃, last AB-8 type macroporous adsorptive resins, carry out eluting with 7 times of water, discard water lotion, 9 times of reuse, 80% ethanol elution, merge eluent, reclaim ethanol to most, the vacuum concentration drying, the effective site 29.8 that obtains Radix Aconiti Kusnezoffii (system) restrains;
(4) get Rhizoma Paridis, with 8 times, 65% soak with ethanol 24 hours, filter, filtrate recycling ethanol is to the greatest extent, and the vacuum concentration drying obtains Rhizoma Paridis effective site 24.5 grams;
(5) get Radix Psammosilenes, add 15 times of decoctings and boil 3 times, each 3 hours, filter, merging filtrate, relative density is 1.25 extractum when being concentrated into 60 ℃, adds ethanol and makes that to contain the alcohol amount be 60%, leaves standstill 24 hours, filter, filtrate recycling ethanol is to most, and the vacuum concentration drying obtains Radix Psammosilenes effective site 34.6 grams;
(6) with Sanchi effective-component 2.6 grams,, Radix Aconiti Kusnezoffii (system) effective site be 29.8 the gram, Rhizoma Paridis effective site 24.5 grams, Radix Psammosilenes effective site is that 34.6 grams mix with disintegrating agent 92.6 grams of the present invention, add filler microcrystalline Cellulose 204.8 grams, granulate, add lubricant Pulvis Talci 11.1 grams, tabletting obtains the cure-all disintegrating tablet.
The compound disintegrating agent of the present invention is made up of erythritol and chitin or low-substituted hydroxypropyl methylcellulose or carboxymethyl starch sodium or crosslinked carboxymethyl fecula sodium or insoluble crospolyvinylpyrrolidone, and the percentage by weight of both compound disintegrating agent mesoerythrit is 30%-70%.
Claims (4)
1. cure-all oral cavity disintegration tablet, it is characterized in that obtaining Sanchi effective-component 0.7-1.5 weight portion by the 60%-80% ethanol extraction, the water logging bubble, water extraction, the system Radix Aconiti Kusnezoffii effective site that the ethanol elution of AB-8 type macroporous adsorptive resins 75%-85% obtains is the 8-16 weight portion, the Rhizoma Paridis effective site 6-13 weight portion that the 60%-70% ethanol extraction obtains, water extraction, it is the 10-20 weight portion that ethanol precipitation obtains Radix Psammosilenes effective site, compound disintegrating agent is the 44-52 weight portion, filler 100.2-117.5 weight portion, lubricant is prepared from for the 5.3-5.8 weight portion, compound disintegrating agent is by erythritol and chitin, the low-substituted hydroxypropyl methylcellulose, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, a kind of composition in the insoluble crospolyvinylpyrrolidone, the weight percentage of compound disintegrating agent mesoerythrit are 30%-70%.
2. a kind of cure-all oral cavity disintegration tablet according to claim 1, wherein the pharmaceutic adjuvant filler is a kind of in microcrystalline Cellulose, the nano micro crystal cellulose.
3. a kind of cure-all oral cavity disintegration tablet according to claim 1, wherein lubricant is a kind of in magnesium stearate, Pulvis Talci, the Stepanol MG.
4. according to the preparation method of any described a kind of cure-all oral cavity disintegration tablet of claim 1-3, it is characterized by:
(1) crude drug is: Radix Notoginseng 7.5 weight portions, system Radix Aconiti Kusnezoffii 80 weight portions, Rhizoma Paridis 62.5 weight portions, trivial 100 weight portions of aufe;
(2) get notoginseng decoction piece and pulverize, cross the 10-15 mesh sieve, get the Radix Notoginseng of pulverizing, add that 5-8 doubly measures, the ethanol extraction of 60%-80% 2-4 time, each 2-4 hour, filtration, filtrate recycling ethanol is extremely most, and the vacuum concentration drying obtains Sanchi effective-component;
(3) produce the Radix Aconiti Kusnezoffii decoction pieces, pulverize, soaked 0.5-1 hour, add 10-20 times of decocting again and boil 2 times, each 1-2 hour, filter, relative density was 1.05-1.10 when merging filtrate, filtrate were concentrated to 50 ℃, last AB-8 type macroporous adsorptive resins, carry out eluting with 6-8 times of water, discard water lotion, reuse 8-10 doubly, the ethanol elution of 75%-85%, merge eluent and reclaim ethanol to the greatest extent, the vacuum concentration drying obtains making the effective site of Radix Aconiti Kusnezoffii;
(4) get Rhizoma Paridis, with 6-10 doubly, soak with ethanol 24-36 hour of 60%-70%, filter, filtrate recycling ethanol is to the greatest extent, the vacuum concentration drying obtains Rhizoma Paridis effective site;
(5) get Radix Psammosilenes, add 10-20 times of decocting and boil 2-5 time, each 2-5 hour, filter, merging filtrate, relative density is the extractum of 1.20-1.30 when being concentrated into 60 ℃, adds ethanol and makes and contain the alcohol amount and be 50%-80%, leaves standstill 24 hours, filter, filtrate recycling ethanol is to most, and the vacuum concentration drying obtains Radix Psammosilenes effective site;
(6) Sanchi effective-component 0.7-1.5 weight portion, system Radix Aconiti Kusnezoffii effective site 8-16 weight portion, Rhizoma Paridis effective site 6-13 weight portion, Radix Psammosilenes effective site 10-20 weight portion are mixed with compound disintegrating agent 44-52 weight portion, add filler 100.2-117.5 weight portion, granulate, add lubricant 5.3-5.8 weight portion, tabletting obtains the cure-all disintegrating tablet.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200410049619 CN1278722C (en) | 2004-06-22 | 2004-06-22 | Orally disintegrating tablet of 'Baibaodan' and its preparation |
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| CN 200410049619 CN1278722C (en) | 2004-06-22 | 2004-06-22 | Orally disintegrating tablet of 'Baibaodan' and its preparation |
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| CN1278722C true CN1278722C (en) | 2006-10-11 |
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