CN100444845C - Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract - Google Patents
Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract Download PDFInfo
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- CN100444845C CN100444845C CNB2005100732744A CN200510073274A CN100444845C CN 100444845 C CN100444845 C CN 100444845C CN B2005100732744 A CNB2005100732744 A CN B2005100732744A CN 200510073274 A CN200510073274 A CN 200510073274A CN 100444845 C CN100444845 C CN 100444845C
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Abstract
The present invention discloses a gstrointestinal tract bioadhesion preparation of panax notoginseng saponin and a preparation method of the gstrointestinal tract bioadhesion preparation. The preparation is composed of 30 to 120 parts by weight of panax notoginseng saponin, 25 to 150 parts by weight of adhesive 25-150 and/or 25 to 150 parts by weight of a bleaching assisting agent, wherein the adhesive is any kind of carbomer, sodium alginate, chitosan, CMC-Na, HPMC K100M, HPMC K15M, HPMC K4M and HPMC 15Lcp or the mixture of sever kinds of carbomer, sodium alginate, chitosan, CMC-Na, HPMC K100M, HPMC K15M, HPMC K4M and HPMC 15Lcp; the bleaching assisting agent is any kind of sodium alginate, CMC-Na, HPMC K100M, HPMC K15M, HPMC K4M, HPMC RT15 and chitosan or the mixture of several kinds of sodium alginate, CMC-Na, HPMC K100M, HPMC K15M, HPMC K4M, HPMC RT15 and chitosan. The gstrointestinal tract bioadhesion preparation of the present invention can obviously enhance the bioavailability of panax notoginseng saponin.
Description
Technical field
The present invention relates to gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins and preparation method thereof, belong to the Chinese medicine extract formulation art.
Background technology
Radix Notoginseng is traditional Chinese medicine, is the root of Araliaceae Panax notoginseng (Burk.) F.H.Chen.Radix Notoginseng really is familiar with by common people and is able to extensive use is that medicine scholar Li Shizhen (1518-1593 A.D.) in greatness records it in Compendium of Material Medica (1578) afterwards.Over more than 400 year, the medical scholar of China has continued to study the unique effects of Radix Notoginseng, has obtained a large amount of scientific achievements, confirms that the main effect of Radix Notoginseng is: " hemostasia and dissipation blood stasis, subduing swelling and relieving pain ".Over nearly 30 years, the scientist of countries such as China and Japan, the U.S. utilizes modern physics, chemical technology and modern medicine and pharmacology theory that Radix Notoginseng has been carried out comparatively systematic research, and people have had understanding comparatively comprehensive, system to Radix Notoginseng.
So far, people have obtained 28 kinds of monomer saponins to the different parts separation of Radix Notoginseng.Wherein, 13 kinds of Protopanaxatriol's type saponin, 15 kinds of protopanoxadiol type saponin, triol type saponin is 3: 1 (1.MasayukiYoshikawa with the content ratio of diol type saponin, et al.Bioactive Saponins and Glycosides.VIII.Notoginseng (1): NewDammarane-TriterpeneOligoglycosides, Notoginsenosides-A,-B,-C, and-D, from the DriedRoot of Panax notoginseng (Burk.) .Chem Pharm Bull, 1997,45 (6): 1039.2.MasayukiYoshikawa，et al.Bioactive Saponins and Glycosides.IX.Notoginseng(2)：Structure of Five NewDammarane-Type Triterpere Oligoglycosides，Notoginsenosides-E，-G，-H，-Iand-J，and a NovelAcetylenic Fatty Acid Glycoside，Notoginsenic Acid β-Sophoroside，from the Dried Root ofPanax notoginseng(Burk.).Chem Pharm Bull，1997，45(6)：1056)。Other also have chemical constituents such as flavone, dencichine.The result of these composition comprehensive functions has good physiological regulatory action to blood system, cardio-cerebrovascular, central nervous system, metabolic system etc.Based on this, developed kind surplus medicine that YUNNAN BAIYAO, Qiyeshen an sheet, Radix Notoginseng total arasaponins preparation (XUESAITONG), Pien Tze Huang, FUFANG DANSHEN PIAN, pseudo-ginseng toothpaste etc. are primary raw material with the Radix Notoginseng, health product, the cosmetics 200.
Radix Notoginseng contains ginsenoside Rb1, Rb2, Rc, Rd, Re, Rf, Rg1, Rg2, Rh1, more than 20 kind of saponin constituents such as arasaponin R1, R2, R3, R4, R6, and wherein with ginsenoside Rb1, Rg1, arasaponin R1 content is the highest.Radix Notoginseng total arasaponins has expansion artery, brings high blood pressure down, and the cerebral blood flow increasing amount, microcirculation improvement prevents the liver organization fibrosis, fatigue-resisting function is mainly used in: 1, prevention and treatment diseases of cardiovascular and cerebrovascular systems.Be applicable to coronary heart disease, angina pectoris, arrhythmia, hypertension, arteriosclerosis, apoplexy (cerebral hemorrhage), diseases such as the headache that apoplexy sequela and cerebral blood supply insufficiency cause is dizzy, senile dementia.2, adjusting, enhancing body adaptability and resistance.Be applicable to the fatigue syndrome that fatigue or excessive thinking cause, mountain sickness, after being ill, deficiency of both QI and blood after puerperal, operation, after the radiotherapy, chemotherapy, physical weakness etc.3, the liver protecting.Be used to prevent and treat the hepatic injury that causes because of excessive drinking, obesity, various hepatitis, liver tissue fibrosis (alcoholic liver, fatty liver).
The present oral medication of Radix Notoginseng total arasaponins has only the tablet and the capsule of regular dosage form.Do not have biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract, particularly do not have the preparation of high bioavailability.
Technical scheme
An object of the present invention is to disclose a kind of biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract with high bioavailability, another object of the present invention is to disclose a kind of preparation method with biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract of high bioavailability, and said preparation can reach the effect of control drug release simultaneously.
The influence of principal agent and adjuvant is mutual in the pharmaceutical preparation, briefly, is exactly the selection of the characteristic decision adjuvant of principal agent, the drug effect of the characteristic decision principal agent of adjuvant.This interactional relation is present in pharmaceutical preparation always and studies in the whole process of clinical use.Though those skilled in the art know: the characteristic according to principal agent is determined adjuvant, but, for principal agent is effective ingredient in Chinese, because effective ingredient in Chinese complicated component, wherein physicochemical properties such as the dissolubility of reactive compound, stability, pH value have nothing in common with each other, be difficult to select the adjuvant that adapts with it, and for the adjuvant that can be used as adhesion preparation, filter out and to improve the prescription that bioavailability has the control drug release effect simultaneously and must could realize through creative work.
Through experimentation, Radix Notoginseng total arasaponins mainly adds the raising bioavailability that gastrointestinal tract biologic adhesion preparation that other conventional adjuvants make can be given prominence to adhesive agent and/or bleach activator, and their ratio is Radix Notoginseng total arasaponins 30-120 weight portion, adhesive agent 25-150 weight portion and/or bleach activator 25-150 weight portion; Wherein adhesive agent be among carbomer, sodium alginate, chitosan, sodium carboxymethyl cellulose (CMC-Na), hydroxypropyl emthylcellulose (HPMC), HPMC K100M, HPMC K15M, HPMC K4M, the HPMC 15Lcp any or several; Bleach activator be in sodium alginate, CMC-Na, HPMC K100M, HPMC K15M, HPMCK4M, HPMC RT15, the chitosan any or several.
Described the object of the invention can be realized by following technical scheme 1,2 or 3:
Technical scheme 1:
Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract of the present invention is mainly made by following compositions: Radix Notoginseng total arasaponins 30-120 weight portion, carbomer (Carbopol is called for short CP) 25-150 weight portion, Polyethylene Glycol (being called for short PEG) 12.5-75 weight portion are formed; Said composition can add adjuvants such as filler, lubricant, fluidizer and make dosage forms such as tablet, capsule, granule; Wherein filler can be selected from lactose, starch, glucose, microcrystalline Cellulose any or several, lubricant can be selected from magnesium stearate or sodium lauryl sulphate;
As follows at technical scheme 1 preferred scheme for comprising:
Consisting of of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet:
Radix Notoginseng total arasaponins 30-140 weight portion, CP25-150 weight portion, Polyethylene Glycol 12.5-75 weight portion, lactose 50-200 weight portion, magnesium stearate 1.25-12.5 weight portion, micropowder silica gel 0.25-1.5 weight portion;
Wherein the composition of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet can be more preferably:
Radix Notoginseng total arasaponins 55-100 weight portion, CP50-100 weight portion Polyethylene Glycol 30-70 weight portion, lactose 60-150 weight portion magnesium stearate 1.25-9 weight portion, micropowder silica gel 0.25-1.5 weight portion;
Through experiment screening, the preferred CP974P NF of compositions carbomer, CP971P NF and CP934P in the technical scheme 1; The wherein preferred PEG 4000 of Polyethylene Glycol, EG6000, and available glucose substitutes;
The preparation method of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet is in the technical scheme 1:
The auxilliary 95% ethanol system soft material that adopts is crossed 20 mesh sieves and is granulated, and 60 ℃ of dry 1h add lubricant mixing tabletting behind the 24 order granulate; Perhaps dry granulation perhaps adds direct compression behind the lubricant mixing.Preferred direct compression and dry granulation tabletting.
Technical scheme 2:
Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract of the present invention is mainly made by following compositions: Radix Notoginseng total arasaponins 30-120 weight portion, chitosan 37.5-130 weight portion, Polyethylene Glycol 25-75 weight portion are formed; Said composition can add adjuvants such as filler, lubricant, fluidizer and make dosage forms such as tablet, capsule, granule; Wherein filler can be selected from polyvinylpyrrolidone (be called for short: any of PVP) lactose, pregelatinized Starch, glucose, microcrystalline Cellulose, lubricant can be selected from magnesium stearate or sodium lauryl sulphate.
As follows at technical scheme 2 optimized technical scheme for comprising:
Consisting of of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet:
Radix Notoginseng total arasaponins 30-140 weight portion, chitosan 25-130 weight portion PVP0-50 weight portion, Polyethylene Glycol 25-75 weight portion magnesium stearate 1.25-12.5 weight portion, micropowder silica gel 0.25-2.5 weight portion lactose 30-200 weight portion.
Wherein the composition of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet can be more preferably:
Radix Notoginseng total arasaponins 55-100 weight portion, chitosan 40-80 weight portion PVP K3020-40 weight portion, Polyethylene Glycol 35-60 weight portion, magnesium stearate 2-7.5 weight portion, micropowder silica gel 1-1.4 weight portion lactose 45-180 weight portion.
The preferred PEG 4000 of Polyethylene Glycol, PEG6000 or available hydroxypropyl emthylcellulose among the compositions in the technical scheme 2 (be called for short: HPMC), glucose any substitute.
The preparation method of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet is in the technical scheme 2: can adopt wet granulation, medicine and auxiliary materials and mixing, a part adopt 95% ethanol to make soft material, cross 20 mesh sieves, 60 ℃ of dry 1h add lubricant mixing tabletting behind the 24 mesh sieve granulate; Perhaps dry granulation also can add direct compression behind the lubricant.Preferred direct compression of preparation method and dry granulation tabletting.
Technical scheme 3:
Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract of the present invention is mainly made by following compositions: Radix Notoginseng total arasaponins 30-120 weight portion, CP 25-75 weight portion, hydroxypropyl emthylcellulose 25-250 weight portion, Macrogol 4000 (PEG 4000) 12.5-75 weight portion are formed; Said composition can also add adjuvants such as filler, lubricant, fluidizer and make tablet; The wherein preferred HPMC K100M of hydroxypropyl emthylcellulose, HPMC K15M, HPMC K4M, HPMC 15Lcp, perhaps any substitutes with octadecanol or hydrogenated vegetable oil, and PEG 4000 can any substitutes with PEG6000, glucose; Wherein filler can be selected from any of lactose, starch, glucose, microcrystalline Cellulose, and lubricant can be selected from magnesium stearate or sodium lauryl sulphate, and fluidizer can be used micropowder silica gel.
Comprise as follows at technical scheme 3 optimized technical scheme:
(1), consisting of of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet:
Radix Notoginseng total arasaponins 30-140 weight portion, CP 15-75 weight portion HPMC K100M 25-150 weight portion, PEG 400012.5-75 weight portion, polyvinylpyrrolidone (PVP) 0-75 weight portion, lactose 15-200 weight portion, magnesium stearate, 1.25-12.5 weight portion, micropowder silica gel 0.25-3 weight portion
Wherein the composition of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet can be more preferably:
Radix Notoginseng total arasaponins 55-100 weight portion, CP 25-60 weight portion, HPMC K100M 40-100 weight portion, PEG 400030-55 weight portion, PVP 15-55 weight portion, lactose 25-160 weight portion, magnesium stearate 2-5.5 weight portion, micropowder silica gel 1-1.5 weight portion
(2), the composition of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet can also for:
Arasaponin 30-140 weight portion
Ka Baimu 12.5-50 weight portion
HPMC 100KM 25-125 weight portion
HPMC 4KM (or HPMC15Lcp) 25-100 weight portion
PEG 4000 12.5-25 weight portions
Lactose 15-100 weight portion
Wherein the composition of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet can be more preferably:
Arasaponin 55-100 weight portion
Ka Baimu 20-40 weight portion
HPMC 100KM 40-80 weight portion
HPMC 4KM (or HPMC15Lcp) 40-90 weight portion
PEG 4000 15-25 weight portions
Lactose 20-80 weight portion
The preparation method of total saponin of notoginseng for gastrointestinal tract bioadhesion tablet is in the technical scheme 3: earlier
CP934P principal agent and adjuvant in addition ground the mixing that sieves, cross 60 mesh sieves, adding CP 934P mixing once more sieves, and adds magnesium stearate, tabletting after the micropowder silica gel mixing sieves, and the pressure limit of tabletting is 35-45N.
Among the technique scheme compositions each form in used carbomer (CP) preferred CP974P NF, CP971P NF and CP934P.
The biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract function cures mainly identical with its oral ordinary preparation: blood vessel alluvial, blood vessel embolism, interior wound congestion, cerebral blood flow deficiency, paralysis, hemiplegia, wound inflammation, surgical wound inflammation, gastritis, skin infection pain, anemia, puerperal congestion, dysmenorrhea, health is weak, physical function is old and feeble, neurasthenia, hepatic injury, liver tissue fibrosis, alcoholic liver, fatty liver, anoxia symptom, hypomnesis, oncosis.
Through test, the employed active component Radix Notoginseng total arasaponins of each technical scheme of the present invention is taken from commercially available product and Radix Notoginseng total arasaponins that extracts from Radix Notoginseng root or leaf portion by art methods and monomer saponin ginsenoside Rb1, the Rg1 that wherein contains, and arasaponin R1 all can reach purpose of the present invention.
Technical scheme 1,2 of the present invention or 3 is tested through bioavailability, has very high bioavailability, this be in the prior art various preparations can't compare, each technical scheme gained gastrointestinal tract biologic adhesion preparation of the present invention is compared the dosage that can save Radix Notoginseng total arasaponins greatly with existing Radix Notoginseng total arasaponins preparation, improve curative effect, and each each preparation of technical scheme gained of the present invention there is the effect of better controlled drug release.
Following experimental example further specifies the present invention.
Following experimental example is made the total saponin of notoginseng for gastrointestinal tract biological adhesive tablet by each technical scheme is described by direct compression, and specification is the 250mg/ sheet.
Experimental example 1 technical scheme 1 adhesion, release, bioavailability experiment
1. adhesion experiment
Experimental technique: adopt accompanying drawing 1 shown device, A fixes with line with test tablet, with buffer moistening 10 minutes, after applying the mucosa of 100g pressure on making it and being fixed on stainless steel substrates and closely contacting 5 minutes, in container D, inject tap water with the speed of 5ml/min by peristaltic pump C, with the gross mass (gram) of balance weighing container and water, represent the size of adhesion as minimum peeling force when mucosa and tablet are peeled off, each 6 tablets of tablets of measuring, averaging compares.
The result: commercially available ordinary tablet adhesion is 0 gram, and adhesion tablet is 18.44 grams.Illustrate that the present invention more can promote the absorption of medicine.
2. release experiment
Release investigation method: with reference to " 2000 editions two appendix XD first methods of Chinese pharmacopoeia, measure the release of commercially available ordinary tablet and adhesion tablet, concrete operations are dissolution medium with the distilled water, rotating speed is 100r/min, and interior at interval at the fixed time sampling 5ml filters, and in time add blank medium, subsequent filtrate carries out assay, and the drug accumulation of measuring different time points discharges percent, gets cumulative release percent and the data of time.
The result:
From adhesion tablet release in vitro data as can be seen, discharged closely 30% in 3 hours, do not have the prominent phenomenon of releasing, 9 hours cumulative release continue to discharge 12 hours more than 70%, discharge fully, meet the standard of design, and control drug release helps the absorption of medicine effectively.And commercially available ordinary tablet does not have this effect, discharges (discharging percentage rate is 90%) at 3 hours fully with interior.
3. bioavailability experiment
Administration and blood-sampling method: three beasle dog random number are No. 1 dog, No. 2 dogs, No. 3 dogs, fasting is 12 hours before the test, take commercially available ordinary tablet (reference preparation) and adhesion tablet (test formulation) for respectively No. 1 dog, No. 2 dogs, No. 3 dogs early morning, press arasaponin 90mg/kg dosed administration.Get blank blood before taking medicine, commercially available ordinary tablet in the back 0.5,1,2,3,4 of taking medicine,, 6,8,10,12,16h, 24h, 36h get foreleg venous blood 3ml, adhesion tablet is got foreleg venous blood 3ml in the back 0,0.5,1,2,3,4,6,8,10,12,16 of taking medicine, 24h, 36h, anticoagulant heparin, in the centrifugal 5min of 3000rpm, it is standby in-20 ℃ of preservations to isolate blood plasma immediately.
The plasma sample processing method: precision is measured blood plasma 0.5ml (activatory solid phase extraction column), after adopting 20% methanol 2ml drip washing respectively, with the 2ml methanol-eluted fractions, eluent dries up in 60 ℃ of following water-bath nitrogen, behind 100 μ l, 50% dissolve with methanol vortex high speed centrifugation, sample introduction is measured, and sampling volume 20 μ l measure the ginsenoside Rg according to the condition of following analysis system
1, ginsenoside Rb
1, Panax Notoginseng saponin R
1The peak area of each composition and internal standard substance peak area ratio, substitution standard curve equation calculates drug plasma concentration.
High performance liquid chromatogram-mass spectrometry analytical system condition:
The ginsenoside Rg
1Molecular ion peak 875------chooser ion 423
Mass spectrum condition: CE:28-30; OP:80-87
Ginsenoside Rb
1Molecular ion peak 1183------chooser ion 487.2
Mass spectrum condition: CE:35V OP:110V
FP：250V EP：-10V
CXP：25V
Panax Notoginseng saponin R
1Molecular ion peak 1007------chooser ion 423.5
Mass spectrum condition: CE:36-30 OP:80-87
Internal standard substance: glipizide 50 (μ l)
Mobile phase is formed:
Time (min) flow velocity (ml/min) methanol 10mMNH
4OAc
0 0.250 50％ 50％
4 0.250 50％ 50％
4.1 0.250 90％ 10％
14.0 0.250 90％ 10％
25 0.250 50％ 50％
Date processing and relative bioavailability evaluation:
With lower area of blood concentration-time curve AUC
0 → ∞Data are calculated according to the following equation.
Fr wherein: relative bioavailability
AUC
0 → ∞ (test): the area under the drug-time curve of test formulation
AUC
0 → ∞ (standard): the area under the drug-time curve of reference preparation
D
Standard: the dosage of test formulation
D
Test: the dosage of reference preparation
Evaluation result:
Compare with commercially available conventional tablet, adhere to the interior AUC of lamellar body and improved 1.1-11.2 doubly, wherein Rg
1: 1.9 times of Rb
1: 1.1 times: Panax Notoginseng saponin R
1: 11.2 times.Illustrate that the technical program has outstanding effect on bioavailability.
Experimental example 2 technical schemes 2 releases, bioavailability, adhesion experiment
1. release experiment: with reference to " 2000 editions two appendix XD first methods of Chinese pharmacopoeia, measure the release of commercially available ordinary tablet and adhesion tablet, concrete operations are dissolution medium with the distilled water, rotating speed is 100r/min, and interior at interval at the fixed time sampling 5ml filters, and in time add blank medium, subsequent filtrate carries out assay, and the drug accumulation of measuring different time points discharges percent, gets cumulative release percent-time data.
The result:
| Time (hour) | 0 | 3 | 6 | 9 | 12 |
| Cumulative release percent (%) | 0 | 39.04494 | 61.79775 | 80.05618 | 101.01 |
From adhesion tablet release in vitro data as can be seen, discharged 39% in 3 hours, do not have the prominent phenomenon of releasing, 9 hours cumulative release continue to discharge 12 hours more than 75%, discharge fully, meet the standard of design, and control drug release helps the absorption of medicine effectively.And commercially available ordinary tablet does not have this effect, discharges (discharging percentage rate is 92%) at 3 hours fully with interior.
2. bioavailability experiment
Bioavailability experimental technique in the same experimental example 1 of method.
Result of the test compares with conventional tablet, adheres to the interior AUC of lamellar body and has improved 1.2-10.6 doubly, wherein Rg
1: 2.1 times; Rb
1: 1.2 times; Panax Notoginseng saponin R
1: 10.6 times.
3. adhesion experiment
Adhesion experimental technique in the same experimental example 1 of method.
The result is: meansigma methods is 22.21 grams
Having suitable adhesion is the essential condition that produces adhesive attraction in the body, promotes absorption, control drug release.
Experimental example 3 technical schemes 3 releases, bioavailability, floating, adhesion experiment
1. release experiment
With reference to " 2000 editions two appendix XD first methods of Chinese pharmacopoeia, measure the release of commercially available ordinary tablet and adhesion tablet, concrete operations are dissolution medium with the distilled water, rotating speed is 100r/min, and interior at interval at the fixed time sampling 5ml filters, and in time add blank medium, subsequent filtrate carries out assay (adopting the determination of color total saponin content), and the drug accumulation of measuring different time points discharges percent, gets cumulative release percent-time data.
The result is as follows:
| Time (hour) | 0 | 3 | 6 | 9 | 12 |
| Cumulative release percent (%) | 0 | 27.85 | 49.94 | 63.10 | 72.97 |
From adhesion tablet release in vitro data as can be seen, discharged closely 30% in 3 hours, do not have the prominent phenomenon of releasing, 9 hours cumulative release are nearly 70%, continue to discharge 12 hours, discharge fully, meet the standard of design, and control drug release helps the absorption of medicine effectively.And commercially available ordinary tablet does not have this effect, discharges (discharging percentage rate is 95%) at 3 hours fully with interior.
2. the determination experiment of flotation time
(1) tablet material adopts the determination experiment of the following scheme flotation time in the technical scheme 3:
Radix Notoginseng total arasaponins 30-140 weight portion, CP15-75 weight portion HPMC K100M 25-150 weight portion, PEG 400012.5-75 weight portion, polyvinylpyrrolidone (PVP) 0-75 weight portion, lactose 15-200 weight portion, magnesium stearate, 1.25-12.5 weight portion, micropowder silica gel 0.25-3 weight portion.
Embodiment method by corresponding composition is made tablet.
Experimental technique:
Adopting the slurry method, is medium with simulated gastric fluid 750ml, 37 ℃ of constant temperature, and 75 rev/mins, write down the buoyant time of ordinary preparation and adhesion preparation respectively, measure the result of 6 tablets of tablets, the comparison of averaging.
The result: the average flotation time of adhesion tablet is 7.0 ± 1.04 hours, and ordinary tablet is 0 hour, and flotation time length helps increasing medicine in the gastrointestinal time of staying, thereby promotes to absorb.
(2) tablet material adopts the determination experiment of the flotation time of the following scheme in the technical scheme 3:
Arasaponin 30-140 weight portion
Ka Baimu 12.5-50 weight portion
HPMC 100KM 25-125 weight portion
HPMC 4KM (or HPMC15Lcp) 25-100 weight portion
PEG 4000 12.5-25 weight portions
Lactose 15-100 weight portion
Embodiment method by corresponding composition is made tablet.
Adopting the slurry method, is medium with simulated gastric fluid 750ml, 37 ℃ of constant temperature, and 75 rev/mins, write down the buoyant time of ordinary preparation and adhesion preparation respectively, measure the result of 6 tablets of tablets, the comparison of averaging.
Flotation time (n=6)
17.5 17.5 15 21.5 18 18
17.9 hours average times
3. bioavailability experiment
Method is with the bioavailability experimental technique in the experimental example 1.
The result:
Compare with commercially available conventional tablet, adhere to the interior AUC of lamellar body and improved 1.2-2.3 doubly, wherein panoxadiol's type saponin is 1.2 times, 2.3 times on panaxatriol's type.
4. adhesion experiment
Experimental technique: adopt accompanying drawing 1 shown device, A fixes with line with test tablet, with buffer moistening 10 minutes, after applying the mucosa of 100g pressure on making it and being fixed on stainless steel substrates and closely contacting 5 minutes, in container D, inject tap water with the speed of 5ml/min by peristaltic pump C, with the gross mass (gram) of balance weighing container and water, represent the size of adhesion as minimum peeling force when mucosa and tablet are peeled off, each 6 tablets of tablets of measuring, averaging compares.Each sheet adhesion values is respectively: 24.693,22.475,23.05,21.964,26.421,24.867 grams.The adhesion tablet meansigma methods is 23.91 grams.
Following examples all can corresponding each technical scheme of realization experiment effect.
Embodiment 1
Radix Notoginseng total arasaponins 75g;
CP 934P 60g
PEG 4000 45g
Lactose 66.25g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
According to aforementioned proportion, the principal agent beyond the CP 934P and the mix homogeneously of adjuvant are crossed 60 mesh sieves, add
After CP 934P ground and mixed is even, add magnesium stearate, tabletting after the micropowder silica gel mixing sieves, tabletting pressure is made 1000 greater than 40N.Oral, one time two, a twice-daily.
Embodiment 2
Radix Notoginseng total arasaponins 75g;
CP971P NF 60g
PEG6000 45g
Lactose 66.25g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
The mixture of medicine and adjuvant in advance with special big briquetting equipment extruding 2-3 time, is pressed into the suitable thin slice of hardness, pulverizes, tabletting again behind the granulate is made 1000.Oral, one time two, a twice-daily.
Embodiment 3
Radix Notoginseng total arasaponins 75g;
CP974P NF 60g
PEG 4000 45g
Glucose 65g
Microcrystalline Cellulose 51.25g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
With medicine and adjuvant in proportion behind the mixing, wet granulation is crossed the 12-14 mesh sieve and is gone out big particle, and the hard capsule case of packing into is made 1000 capsules.Oral, one time two, a twice-daily.
Embodiment 4
Radix Notoginseng total arasaponins 75g;
CP 934P 60g
PEG 4000 45g
Lactose 65g
Starch 55g
With medicine and adjuvant mix homogeneously, behind wet granulation, cross the 12-14 mesh sieve and go out big particle, cross 60 mesh sieves then and go out fine powder, make uniform particles, packing then, every bag 0.6 gram.Oral, one time one bag, a twice-daily.
Embodiment 5
Radix Notoginseng total arasaponins 75g;
CP974P NF 60g
PEG 4000 45g
Starch 67.5g
Sodium lauryl sulphate 2.5g
In above ratio with adjuvant and medicament mixed evenly after, adopt 95% ethanol system soft material, cross the granulation of 20 mesh sieves, 60 ℃ of dry 1h, 24 order granulate, tabletting is made 1000.Oral, one time two, a twice-daily.
Embodiment 6
Radix Notoginseng total arasaponins 90g;
CP 934P 90g
PEG 4000 40g
Lactose 50g
Magnesium stearate 4g
Micropowder silica gel 1g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, an a slice, a twice-daily.
Embodiment 7
Radix Notoginseng total arasaponins 75g;
CP971P NF 96g
PEG6000 60g
Lactose 80g
Magnesium stearate 2g
Micropowder silica gel 1g
According to aforementioned proportion, the principal agent beyond the CP971P NF and the mix homogeneously of adjuvant are crossed 60 mesh sieves, add
Go into CP971P NF ground and mixed evenly after, add magnesium stearate, the micropowder silica gel mixing back tabletting that sieves, tabletting pressure is made 1000 greater than 40N.Oral, one time two, a twice-daily.
Embodiment 8
Radix Notoginseng total arasaponins 65g;
CP974P NF 80g
PEG 4000 55g
Glucose 45g
Microcrystalline Cellulose 2.3g
Magnesium stearate 1.5g
Micropowder silica gel 1.2g
According to aforementioned proportion, the principal agent beyond the CP974P NF and the mix homogeneously of adjuvant are crossed 60 mesh sieves,
After adding CP974P NF ground and mixed is even, add magnesium stearate, tabletting after the micropowder silica gel mixing sieves, tabletting pressure is made 1000 greater than 40N.Oral, one time two, a twice-daily.
Embodiment 9
Radix Notoginseng total arasaponins 75g;
CP 934P 55g
PEG 4000 65g
Lactose 65g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, one time two, a twice-daily.
Embodiment 10
Radix Notoginseng total arasaponins 95g;
CP974P NF 60g
PEG 4000 55g
Sodium lauryl sulphate 1.5g
The mixture of medicine and adjuvant in advance with special big briquetting equipment extruding 2-3 time, is pressed into the suitable thin slice of hardness, pulverizes, tabletting again behind the granulate is made 1000.Oral, an a slice, a twice-daily.
Embodiment 11
Radix Notoginseng total arasaponins 75g
Chitosan 50g
PVP K30 30g
PEG 4000 37.5g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
Lactose 50g
With medicine and auxiliary materials and mixing, make soft material with 95% ethanol, cross 20 mesh sieves, 60 ℃ of dry 1h add magnesium stearate mixing tabletting behind the 24 mesh sieve granulate, make 1000.Oral, one time two, a twice-daily.
Embodiment 12
Radix Notoginseng total arasaponins 75g
Chitosan 50g
PVP K30 30g
PEG 4000 37.5g
Magnesium stearate 2.5g
With medicine and adjuvant in proportion behind the mixing, wet granulation is crossed the 12-14 mesh sieve and is gone out big particle, and the hard capsule case of packing into is made 1000 capsules.Oral, one time two, a twice-daily.
Embodiment 13
Radix Notoginseng total arasaponins 75g
Chitosan 50g
PVP K30 30g
PEG 4000 37.5g
After using PVP K30 solution with wet granulations such as chitosans earlier, add the medicine mixing, tabletting is made 1000.Oral, one time two, a twice-daily.
Embodiment 14
Radix Notoginseng total arasaponins 75g
Chitosan 50g
PVP K30 55g
PEG 6000 37.5g
Lactose 82.5g
With medicine and adjuvant mix homogeneously, behind wet granulation, cross the 12-14 mesh sieve and go out big particle, cross 60 mesh sieves then and go out fine powder, make uniform particles, packing granule, every bag 0.6 gram.Oral, one time one bag, a twice-daily.
Embodiment 15
Radix Notoginseng total arasaponins 75g
Chitosan 50g
PVP K30 30g
HPMC 15Lcp 37.5g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
Microcrystalline Cellulose 50g
With medicine and the adjuvant mixing that sieves, add direct compression behind the magnesium stearate mixing.Make 1000.Oral, one time two, a twice-daily.
Embodiment 16
Radix Notoginseng total arasaponins 65g
Chitosan 45g
PVP K30 35g
PEG 4000 55g
Magnesium stearate 5g
Micropowder silica gel 1.25g
Lactose 60g
The mixture of medicine and adjuvant in advance with special big briquetting equipment extruding 2-3 time, is pressed into the suitable thin slice of hardness, pulverizes, tabletting again behind the granulate is made 1000.Oral, an a slice, a twice-daily.
Embodiment 17
Radix Notoginseng total arasaponins 75g
Chitosan 50g
PVP K30 30g
PEG 40003 7.5g
Magnesium stearate 2.5g
The mixture of medicine and adjuvant in advance with special big briquetting equipment extruding 2-3 time, is pressed into the suitable thin slice of hardness, pulverizes, tabletting again behind the granulate is made 1000.Oral, an a slice, a twice-daily.
Embodiment 18
Radix Notoginseng total arasaponins 85g
Chitosan 80g
PVP K30 40g
PEG 4000 65g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, an a slice, a twice-daily.
Embodiment 19
Radix Notoginseng total arasaponins 65g
Chitosan 50g
PVP K30 25g
PEG 6000 30g
Lactose 40g
With medicine and adjuvant mix homogeneously, behind wet granulation, cross the 12-14 mesh sieve and go out big particle, cross 60 mesh sieves then and go out fine powder, make uniform particles, packing granule, every bag 0.6 gram.Oral, one time one bag, a twice-daily.
Embodiment 20
Radix Notoginseng total arasaponins 95g
Chitosan 70g
PVP K30 50g
HPMC 15Lcp 37.5g
Magnesium stearate 2g
Micropowder silica gel 1.25g
Microcrystalline Cellulose 50g
The mixture of medicine and adjuvant in advance with special big briquetting equipment such as the extruding of open-type rubber mixing machine 2-3 time, is pressed into the suitable thin slice of hardness, pulverizes again, tabletting again behind the granulate.Make 1000, oral, an a slice, a twice-daily.
Embodiment 21
Radix Notoginseng total arasaponins 75g;
CP 934P 30g
HPMC K100M 50g
PEG 4000 37.5g
PVP 25g
Lactose 25g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
The mixing that in proportion medicine and adjuvant sieved adds direct compression behind magnesium stearate and the micropowder silica gel mixing.Make 1000.Oral, one time two, a twice-daily.
Embodiment 22
Radix Notoginseng total arasaponins 95g;
CP 934P 40g
HPMC K100M 50g
PEG 4000 37.5g
PVP 25g
The mixture of medicine and adjuvant in advance with special big briquetting equipment such as the extruding of open-type rubber mixing machine 2-3 time, is pressed into the suitable thin slice of hardness, pulverizes again, tabletting again behind the granulate.Make 1000, oral, an a slice, a twice-daily.
Embodiment 23
Radix Notoginseng total arasaponins 85g;
CP 934P 30g
HPMC K100M 50g
PEG 4000 37.5g
PVP 25g
Starch 25g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, an a slice, a twice-daily.
Embodiment 24
Radix Notoginseng total arasaponins 75g;
CP 934P 35g
HPMC K100M 50g
Glucose 35g
PVP 25g
Micropowder silica gel 1.25g
The mixing that in proportion medicine and adjuvant sieved adds direct compression behind the micropowder silica gel mixing.Make 1000.Oral, one time two, a twice-daily.
Embodiment 25
Radix Notoginseng total arasaponins 75g;
CP 934P 36g
HPMC K100M 55g
PEG 4000 37.5g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, one time two, a twice-daily.
Embodiment 26
Radix Notoginseng total arasaponins 65g;
CP 934P 20g
HPMC K100M 50g
PEG 4000 30.5g
PVP 35g
Lactose 25g
Magnesium stearate 3.5g
Micropowder silica gel 1.25g
The mixing that in proportion medicine and adjuvant sieved adds direct compression behind the magnesium stearate mixing.Make 1000.Oral, one time two, a twice-daily.
Embodiment 27
Radix Notoginseng total arasaponins 110g;
CP 934P 60g
HPMC K100M 60g
PEG 4000 50g
PVP 25g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, an a slice, a twice-daily.
Embodiment 28
Radix Notoginseng total arasaponins 70g;
CP 934P 40g
HPMC K100M 60g
PEG 4000 45g
PVP 45g
Starch 25g
The mixture of medicine and adjuvant in advance with special big briquetting equipment such as the extruding of open-type rubber mixing machine 2-3 time, is pressed into the suitable thin slice of hardness, pulverizes again, tabletting again behind the granulate.Make 1000, oral, one time two, a twice-daily.
Embodiment 29
Radix Notoginseng total arasaponins 65g;
CP 934P 30g
HPMC K100M 60g
Glucose 37.5g
PVP 45g
Micropowder silica gel 1g
The mixing that in proportion medicine and adjuvant sieved adds direct compression behind the micropowder silica gel mixing.Make 1000.Oral, one time two, a twice-daily.
Embodiment 30
Radix Notoginseng total arasaponins 95g;
CP 934P 65g
HPMC K100M 80g
PEG 4000 55g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, an a slice, a twice-daily.
Embodiment 31
Radix Notoginseng total arasaponins 75g
Octadecanol 50g
Carbomer 75g
Microcrystalline Cellulose 25g
With the octadecanol heating and melting, add adjuvants such as principal agent, microcrystalline Cellulose, ground 40 mesh sieves after the cooling, add the carbomer mixing, direct compression, pressure is greater than 30N; Also can adopt direct compression that each adjuvant is ground the 60 order mixings that sieve, direct compression is made 1000.Oral, one time two, a twice-daily.
Embodiment 32
Arasaponin 75g
Ka Baimu 100g
Octadecanol 37.5g
Microcrystalline Cellulose 12.5g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
With the octadecanol heating and melting, add adjuvants such as principal agent, microcrystalline Cellulose, ground 40 mesh sieves after the cooling, add the carbomer mixing, direct compression, pressure is greater than 30N; Also can adopt direct compression that each adjuvant is ground the 60 order mixings that sieve, direct compression is made 1000.Oral, one time two, a twice-daily.
Embodiment 33
Arasaponin 75g
Ka Baimu 25g
HPMC 100KM 50g
HPMC 4KM 75g
PEG 4000 20g
Lactose 20g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, one time three, once-a-day.
Embodiment 34
Arasaponin 75g
Ka Baimu 25g
HPMC 100KM 50g
HPMC15Lcp 75g
PEG 4000 20g
Lactose 20g
Direct compression in proportion behind the mixing sieves medicine and adjuvant.Make 1000.Oral, one time three, once-a-day.
Embodiment 35
Arasaponin 75g
Ka Baimu 15g
HPMC 100KM 100g
HPMC15Lcp 25g
PEG 4000 12.5g
Lactose 10g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
The mixing that in proportion medicine and adjuvant sieved adds direct compression behind the micropowder silica gel mixing.Make 1000.Oral, one time three, once-a-day.
Embodiment 36
Arasaponin 75g
Ka Baimu 45g
HPMC 100KM 90g
HPMC 4KM 85g
PEG 4000 20g
Lactose 20g
With pressurizeing in advance with bigger punch die after medicine and the auxiliary materials and mixing, obtain sheet (5-20g) in proportion on the tablet machine of big pressure, make suitable granule through waving granulator then, tabletting is made 1000.Oral, one time three, once-a-day.
Embodiment 37
Arasaponin 85g
Ka Baimu 30g
HPMC 100KM 70g
HPMC15Lcp 75g
PEG 4000 20g
Lactose 15g
The mixture of medicine and adjuvant in advance with special big briquetting equipment such as the extruding of open-type rubber mixing machine 2-3 time, is pressed into the suitable thin slice of hardness, pulverizes again, tabletting again behind the granulate.Make 1000, oral, one time two, once-a-day.
Embodiment 38
Arasaponin 95g
Ka Baimu 25g
HPMC 100KM 60g
HPMC15Lcp 55g
PEG 4000 12.5g
Lactose 10g
Magnesium stearate 2.5g
Micropowder silica gel 1.25g
The mixing that in proportion medicine and adjuvant sieved adds direct compression behind the micropowder silica gel mixing.Make 1000.Oral, one time two, once-a-day.
Description of drawings:
Accompanying drawing 1 is adhesion test set, wherein A: tablet; B: the stainless steel substrates of having fixed the rabbit mucosa; C: peristaltic pump; D: container
Claims (30)
1, a kind of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that said preparation mainly made by following raw material: Radix Notoginseng total arasaponins 30-120 weight portion, carbomer 25-150 weight portion, Polyethylene Glycol 12.5-75 weight portion.
2, gastrointestinal tract biologic adhesion preparation as claimed in claim 1 is characterized in that adding in the said preparation filler, lubricant, fluidizer and makes tablet, granule or capsule; Wherein filler be selected from lactose, starch, glucose, microcrystalline Cellulose any or several, lubricant is selected from magnesium stearate or sodium lauryl sulphate.
3, gastrointestinal tract biologic adhesion preparation as claimed in claim 1 is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 75 weight portions
Carbomer 934 P 60 weight portions
Macrogol 4000 45 weight portions
Lactose 65 weight portions
Starch 55 weight portions.
4, a kind of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 30-140 weight portion, carbomer 25-150 weight portion,
Polyethylene Glycol 12.5-75 weight portion, lactose 50-200 weight portion,
Magnesium stearate 1.25-12.5 weight portion, micropowder silica gel 0.25-1.5 weight portion.
5, gastrointestinal tract biologic adhesion preparation as claimed in claim 4 is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 55-100 weight portion, carbomer 50-100 weight portion
Polyethylene Glycol 30-70 weight portion, lactose 60-150 weight portion
Magnesium stearate 1.25-9 weight portion, micropowder silica gel 0.25-1.5 weight portion.
6, gastrointestinal tract biologic adhesion preparation as claimed in claim 5 is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 75 weight portions
Carbomer 934 P 60 weight portions
Macrogol 4000 45 weight portions
Lactose 66.25 weight portions
Magnesium stearate 2.5 weight portions
Micropowder silica gel 1.25 weight portions.
7, a kind of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins principal agent 90 weight portions;
Carbomer 934 P adhesion material 90 weight portions
Macrogol 4000 porogen 40 weight portions
Lactose filler 50 weight portions
Magnesium 4 weight portions
Micropowder silica gel fluidizer 1 weight portion.
8, a kind of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that said preparation mainly made by following raw material: Radix Notoginseng total arasaponins 30-120 weight portion, chitosan 37.5-130 weight portion, Polyethylene Glycol 25-75 weight portion.
9, gastrointestinal tract biologic adhesion preparation as claimed in claim 8 is characterized in that adding in the said preparation filler, lubricant, fluidizer and makes tablet, granule or capsule; Wherein filler is selected from any of polyvinylpyrrolidone, lactose, pregelatinized Starch, glucose, microcrystalline Cellulose, and lubricant is selected from magnesium stearate or sodium lauryl sulphate.
10, gastrointestinal tract biologic adhesion preparation as claimed in claim 8 is characterized in that said preparation mainly made by following raw material:
Radix Notoginseng total arasaponins 30-120 weight portion, chitosan 37.5-130 weight portion, Polyethylene Glycol 25-75 weight portion, polyvinylpyrrolidone 20-75 weight portion.
11, gastrointestinal tract biologic adhesion preparation as claimed in claim 10 is characterized in that said preparation mainly made by following raw material:
Radix Notoginseng total arasaponins 75 weight portions
Chitosan 50 weight portions
Polyvinylpyrrolidone K30 30 weight portions
Macrogol 4000 37.5 weight portions.
12, a kind of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 30-140 weight portion, chitosan 25-130 weight portion
Polyvinylpyrrolidone 0-50 weight portion, Polyethylene Glycol 25-75 weight portion
Magnesium stearate 1.25-12.5 weight portion, micropowder silica gel 0.25-2.5 weight portion
Lactose 30-200 weight portion.
13, gastrointestinal tract biologic adhesion preparation as claimed in claim 12 is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 55-100 weight portion, chitosan 40-80 weight portion
Polyvinylpyrrolidone K30 20-40 weight portion, Polyethylene Glycol 35-60 weight portion,
Magnesium stearate 2-7.5 weight portion, micropowder silica gel 1-1.4 weight portion
Lactose 45-180 weight portion.
14, gastrointestinal tract biologic adhesion preparation as claimed in claim 12 is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 75 weight portions
Chitosan 50 weight portions
Polyvinylpyrrolidone K30 30 weight portions
Macrogol 4000 37.5 weight portions
Magnesium stearate 2.5 weight portions
Micropowder silica gel 1.25 weight portions
Lactose 50 weight portions.
15, gastrointestinal tract biologic adhesion preparation as claimed in claim 12 is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 65 weight portions
Chitosan 45 weight portions
Polyvinylpyrrolidone K30 35 weight portions
Macrogol 4000 55 weight portions
Magnesium stearate 5 weight portions
Micropowder silica gel 1.25 weight portions
Lactose 60 weight portions.
16, a kind of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that said preparation mainly made by following raw material: Radix Notoginseng total arasaponins 30-120 weight portion, carbomer 25-75 weight portion, hydroxypropyl emthylcellulose 25-250 weight portion, Macrogol 4000 12.5-75 weight portion.
17, gastrointestinal tract biologic adhesion preparation as claimed in claim 16 is characterized in that adding in the said preparation binding agent, filler, lubricant, fluidizer and makes tablet; Wherein hydroxypropyl emthylcellulose is hydroxypropyl emthylcellulose K100M, hydroxypropyl emthylcellulose K15M, hydroxypropyl emthylcellulose K4M, hydroxypropyl emthylcellulose 15L centipoise, and perhaps any substitutes with octadecanol or hydrogenated vegetable oil; Any substitutes Macrogol 4000 with polyethylene glycol 6000, glucose; Wherein filler is selected from any of lactose, starch, glucose, microcrystalline Cellulose, and lubricant is selected from magnesium stearate or sodium lauryl sulphate, and fluidizer is micropowder silica gel.
18, a kind of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 30-140 weight portion, carbomer 15-75 weight portion
HPMC K100M 25-150 weight portion, Macrogol 4000 12.5-75 weight portion,
Polyvinylpyrrolidone 0-75 weight portion, lactose 15-200 weight portion,
Magnesium stearate, 1.25-12.5 weight portion, micropowder silica gel 0.25-3 weight portion.
19, gastrointestinal tract biologic adhesion preparation as claimed in claim 18 is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 55-100 weight portion, carbomer 25-60 weight portion,
HPMC K100M 40-100 weight portion, Macrogol 4000 30-55 weight portion,
Polyvinylpyrrolidone 15-55 weight portion, lactose 25-160 weight portion,
Magnesium stearate 2-5.5 weight portion, micropowder silica gel 1-1.5 weight portion.
20, a kind of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that said preparation made by following raw material:
Radix Notoginseng total arasaponins 30-140 weight portion
Ka Baimu 2.5-50 weight portion
Hydroxypropyl emthylcellulose K100M 25-125 weight portion
Hydroxypropyl emthylcellulose K4M or hydroxypropyl emthylcellulose 15L centipoise 25-100 weight
Part
Macrogol 4000 12.5-25 weight portion
Lactose 15-100 weight portion.
21, gastrointestinal tract biologic adhesion preparation as claimed in claim 20 is characterized in that said preparation made by following raw material:
Arasaponin 55-100 weight portion
Ka Baimu 20-40 weight portion
Hydroxypropyl emthylcellulose K100M 40-80 weight portion
Hydroxypropyl emthylcellulose K4M or hydroxypropyl emthylcellulose 15L centipoise 40-90 weight portion
Macrogol 4000 15-25 weight portion
Lactose 20-80 weight portion.
22, a kind of preparation method of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that this method is: choose following raw material: Radix Notoginseng total arasaponins 30-120 weight portion, carbomer 25-150 weight portion, Polyethylene Glycol 12.5-75 weight portion; Adding filler, lubricant, fluidizer are made tablet, granule or capsule; Wherein filler be selected from lactose, starch, glucose, microcrystalline Cellulose any or several, lubricant is selected from magnesium stearate or sodium lauryl sulphate; With 95% ethanol system soft material, cross 20 mesh sieves and granulate, 60 ℃ of dry 1h add lubricant mixing tabletting behind the 24 order granulate.
23, a kind of preparation method of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that choosing following raw material:
Radix Notoginseng total arasaponins 30-140 weight portion, carbomer 25-150 weight portion,
Polyethylene Glycol 12.5-75 weight portion, lactose 50-200 weight portion,
Magnesium stearate 1.25-12.5 weight portion, micropowder silica gel 0.25-1.5 weight portion.
24, a kind of preparation method of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that this method is: choose following raw material: Radix Notoginseng total arasaponins 30-120 weight portion, chitosan 37.5-130 weight portion, Polyethylene Glycol 25-75 weight portion; Adding filler, lubricant, fluidizer are made tablet, capsule, granule; Wherein filler is selected from any of polyvinylpyrrolidone, lactose, pregelatinized Starch, glucose, microcrystalline Cellulose, and lubricant is selected from magnesium stearate or sodium lauryl sulphate; Adopt 95% ethanol to make soft material, cross 20 mesh sieves, 60 ℃ of dry 1h add lubricant mixing tabletting behind the 24 mesh sieve granulate.
25, the preparation method of gastrointestinal tract biologic adhesion preparation as claimed in claim 24 is characterized in that choosing raw material in this method is mainly: Radix Notoginseng total arasaponins 30-120 weight portion, chitosan 37.5-130 weight portion, Polyethylene Glycol 25-75 weight portion, polyvinylpyrrolidone 20-75 weight portion.
26, a kind of preparation method of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that this method is: choosing raw material is: Radix Notoginseng total arasaponins 30-140 weight portion, chitosan 25-130 weight portion, polyvinylpyrrolidone 0-50 weight portion, Polyethylene Glycol 25-75 weight portion, magnesium stearate 1.25-12.5 weight portion, micropowder silica gel 0.25-2.5 weight portion, lactose 30-200 weight portion; Adopt 95% ethanol to make soft material, cross 20 mesh sieves, 60 ℃ of dry 1h add lubricant mixing tabletting behind the 24 mesh sieve granulate.
27, a kind of preparation method of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that choosing in this method following raw material: Radix Notoginseng total arasaponins 30-120 weight portion, Ka Baimu 25-75 weight portion, hydroxypropyl emthylcellulose 25-250 weight portion, Macrogol 4000 12.5-75 weight portion; Said composition adding binding agent, filler, lubricant, fluidizer are made tablet; Wherein hydroxypropyl emthylcellulose is any one in hydroxypropyl emthylcellulose K100M, hydroxypropyl emthylcellulose K15M, hydroxypropyl emthylcellulose K4M, the hydroxypropyl emthylcellulose 15L centipoise; Wherein filler is selected from any of lactose, starch, glucose, microcrystalline Cellulose, and lubricant is selected from magnesium stearate or sodium lauryl sulphate; Fluidizer is micropowder silica gel.
28, a kind of preparation method of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that choosing in this method raw material and is: Radix Notoginseng total arasaponins 30-140 weight portion, Ka Baimu 15-75 weight portion, hydroxypropyl emthylcellulose K100M 25-150 weight portion, Macrogol 4000 12.5-75 weight portion, polyvinylpyrrolidone 0-75 weight portion, lactose 15-200 weight portion, magnesium stearate, 1.25-12.5 weight portion, micropowder silica gel 0.25-3 weight portion.
29, a kind of preparation method of gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins is characterized in that choosing in this method raw material and is: arasaponin 30-140 weight portion, Ka Baimu 12.5-50 weight portion, hydroxypropyl emthylcellulose K100M25-125 weight portion, hydroxypropyl emthylcellulose K4M or hydroxypropyl emthylcellulose 15L centipoise 25-100 weight portion, Macrogol 4000 12.5-25 weight portion, lactose 15-100 weight portion.
30, the preparation method of the gastrointestinal tract biologic adhesion preparation of Radix Notoginseng total arasaponins as claimed in claim 27 is characterized in that hydroxypropyl emthylcellulose is with any substitutes in octadecanol or the hydrogenated vegetable oil; Any substitutes Macrogol 4000 with polyethylene glycol 6000, glucose.
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| CNB2005100732744A CN100444845C (en) | 2005-06-03 | 2005-06-03 | Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract |
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|---|---|---|---|---|
| CN1267518A (en) * | 1999-03-18 | 2000-09-27 | 蓝桂华 | Notoginseng total saponin capsule and its preparation |
| CN1362171A (en) * | 2001-01-02 | 2002-08-07 | 杨孟君 | Nano notoginseng medicine and its preparation |
| CN1387854A (en) * | 2002-07-10 | 2003-01-01 | 云南植物药业有限公司 | Dispersed general arasaponin tablet and its prepn and application |
| CN1513462A (en) * | 2003-05-07 | 2004-07-21 | ���鼯��������ҩ�� | Intravenous inject contg. pseudo-ginseng total saponin and its prodn. method |
| CN1579410A (en) * | 2003-07-31 | 2005-02-16 | 安徽省药物研究所 | Oral total notoginsenoside blending preparation |
| CN1491659A (en) * | 2003-08-28 | 2004-04-28 | 王景成 | Notoginseng total saponin powder injection and preparing process |
| CN1491658A (en) * | 2003-09-05 | 2004-04-28 | 云南植物药业有限公司 | Notiginseng total saponin liposome and its preparation |
| CN1562056A (en) * | 2004-04-07 | 2005-01-12 | 江西天施康中药股份有限公司 | Slow and control release preparation for thromus |
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| CN1872078A (en) | 2006-12-06 |
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