CN105796518A - Diosbulbin B dispersible tablets and preparation method thereof - Google Patents
Diosbulbin B dispersible tablets and preparation method thereof Download PDFInfo
- Publication number
- CN105796518A CN105796518A CN201610217462.8A CN201610217462A CN105796518A CN 105796518 A CN105796518 A CN 105796518A CN 201610217462 A CN201610217462 A CN 201610217462A CN 105796518 A CN105796518 A CN 105796518A
- Authority
- CN
- China
- Prior art keywords
- diosbulbin
- dispersible tablet
- sodium hydroxymethyl
- hydroxymethyl stalcs
- microcrystalline cellulose
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to diosbulbin B dispersible tablets. The diosbulbin B dispersible tablets are prepared from, in percentage by weight, 2.5%-5.0% of diosbulbin B, 5%-15% of disintegrating agent crosslinked sodium carboxymethyl starch, 0.5%-3.0% of wetting agent superfine silica powder, 20%-40% of microcrystalline cellulose and the balance of cellulose lactose. Meanwhile, the invention also relates to a preparation method of the diosbulbin B dispersible tablets. A wet granulation method is adopted, the disintegrating agent is injected with an interior and exterior addition method, 1/2-3/4 of diosbulbin B, microcrystalline cellulose, cellulose lactose and crosslinked sodium carboxymethyl starch by mass are mixed for granulation, the superfine silica powder and the remaining crosslinked sodium carboxymethyl starch are added and subjected to tableting, and the dispersible tablets are prepared. The bioavailability of the diosbulbin B is improved, the medicine disintegration speed and the dissolution rate are increased, few adverse reactions are caused, and better stability is realized.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to a kind of diosbulbin B dispersible tablet and preparation method thereof.
Background technology
Rhizoma Dioscoreae Bulbiferae is the tuber of Dioscoreaceae yam Dioscorea bulbifera L., has eliminating stagnation and disappears wart, detoxifies, subsides a swelling, cooling blood for hemostasis
Effect, is used for treating kinds cancer, goiter, cough with asthma etc. clinically.Rhizoma Dioscoreae Bulbiferae also has antiviral, antibacterial action.Face
Normal and Radix Angelicae Sinensis compatibility on bed, increases the antitumor action of Rhizoma Dioscoreae Bulbiferae by reducing expressing of P-glycoprotein.
Diosbulbin B is the important component part of Diterpenoid in Rhizoma Dioscoreae Bulbiferae medical material.Diosbulbin B is at 2-16 mg/kg model
Having dose-dependent antitumor effect in enclosing, and without notable toxicity, diosbulbin B is to the propagation of stomach cancer cell SGC-7901 and turns
Shifting has obvious inhibitory action, and diosbulbin B shows the low cross resistance of SGC-7901, overcomes tumor for certain
After a kind of chemotherapeutics produces drug resistance, other chemotherapeutics to inhibition decrease to some degree produced by this tumor,
The shortcoming of the chemotherapeutics of the most identical mechanism of action.But because its poorly water-soluble, bioavailability are low, limit its exploitation and
Application, and about the preparation list marketing the most at home and abroad of diosbulbin B.Therefore, study the suitable dosage form of relevant diosbulbin B,
Improve bioavailability, will there is higher using value and wide market prospect.
Summary of the invention
For solving the problems referred to above, the present invention provides a kind of diosbulbin B dispersible tablet, improves the bioavailability of diosbulbin B, increases
Adding disintegration rate and the dissolution of medicine, untoward reaction is little, preferable stability.
Invention also provides the preparation method of diosbulbin B dispersible tablet.
The present invention is achieved by the following technical solutions:
A kind of diosbulbin B dispersible tablet, is made up of following weight percent content, diosbulbin B 2.5-5.0%, disintegrating agent crosslinking hydroxyl
Methyl starch sodium 5-15%, wetting agent micropowder silica gel 0.5-3.0%, microcrystalline Cellulose 20-40%, surplus is cellulose milk sugar.Described
Crosslinking Sodium Hydroxymethyl Stalcs uses inside and outside addition to add, and the ratio inside adding quality and outer dosage is 3:1.
Preferably, dispersible tablet adds the ethanol solution of dispersible tablet quality 4-6%, the mass fraction 70% of ethanol solution.
Preferably, diosbulbin B dispersible tablet is made up of following percentage by weight, diosbulbin B 3.13%, cross-links hydroxymethyl starch
Sodium 7.5%, micropowder silica gel 1.13%, microcrystalline Cellulose 35%, cellulose milk sugar 53.24%.
The preparation method of diosbulbin B dispersible tablet described above, uses wet granulation process, and disintegrating agent uses inside and outside addition to add
Enter, comprise the following steps:
(1) diosbulbin B, microcrystalline Cellulose, cellulose milk sugar, crosslinking Sodium Hydroxymethyl Stalcs, micropowder silica gel are weighed by weight proportion
The most finely ground, cross 100 mesh sieves, standby；
(2) by diosbulbin B, microcrystalline Cellulose, cellulose milk sugar, the 1/2-3/4 of crosslinking Sodium Hydroxymethyl Stalcs quality in step (1)
Use equal increments method mix homogeneously, with 70% ethanol soft material, cross 20 mesh sieves and pelletize, be dried to perseverance in 55 DEG C of-60 DEG C of baking ovens
Weight, crosses 20 mesh sieve granulate；
(3) add micropowder silica gel and remaining crosslinking Sodium Hydroxymethyl Stalcs, mix homogeneously, tabletting, prepare dispersible tablet, tablet weight
0.2±0.01g。
Preferably, in described step (2), crosslinking Sodium Hydroxymethyl Stalcs adds quality is crosslinking hydroxymethyl starch in step (1)
The 3/4 of sodium quality.
Beneficial effects of the present invention:
1. diosbulbin B powder addition adjuvant is made dispersible tablet by the present invention, increases disintegration rate and dissolution, the untoward reaction of medicine
Little, hot and humid and accelerate under constant temperature, there is preferable stability.
2. crosslinking Sodium Hydroxymethyl Stalcs is as disintegrating agent, uses inside and outside addition, and disintegration is short, and dissolution in vitro is high, molten
Go out speed fast；Microcrystalline Cellulose is as filler, and it does not only have good compressibility and mobility, also has disintegrating agent and suspendible
The dual function of agent；Micropowder silica gel, as lubricant, contributes to increasing granule or the mobility of powder, because it has silanol base junction
Structure, can help disintegrate and the dissolution rate of insoluble drug.
3. the hardness of dispersible tablet is 40-60N, has enough porositys, to reach quickly disintegrated purpose, to ensure tablet
Hardness is suitable, and has good outward appearance and fineness.
Detailed description of the invention
Medicine: diosbulbin B (prepared by Chinese medicine new formulation engineering center of Shandong Province, purity: 99.5%).
Adjuvant: cellulose milk sugar (lot number: L1432, Guangzhou Tian Run pharmaceutcal corporation, Ltd)；Crosslinked carboxymethyl fecula sodium
(cCMS-Na, lot number: 0011163109, Shanghai Hou Cheng Fine Chemical Co., Ltd)；Microcrystalline Cellulose (lot number: 20120306,
Upper Caulis Piperis Kadsurae letter Pharmaceuticals Ltd, pharmaceutical grade).
Embodiment 1
(1) diosbulbin B of 2.5g, the microcrystalline Cellulose of 20g, the cellulose milk sugar of 70.5g, the friendship of 5.0g are weighed by weight proportion
Connection Sodium Hydroxymethyl Stalcs, the micropowder silica gel of 2g are distinguished the most finely ground, cross 100 mesh sieves, standby；
(2) by diosbulbin B 2.5g, microcrystalline Cellulose 20g, the crosslinking Sodium Hydroxymethyl Stalcs of cellulose milk sugar 70.5g and 2.5g
Use equal increments method mix homogeneously, add 4g 70% ethanol soft material, cross 20 mesh sieves granulation, be dried in 55 DEG C of baking ovens to
Constant weight, crosses 20 mesh sieve granulate；
(3) add micropowder silica gel and 2.5g cross-links Sodium Hydroxymethyl Stalcs, mix homogeneously, tabletting, prepare dispersible tablet, every tablet weight
0.20±0.01g。
Embodiment 2
(1) weigh by weight proportion 2.5% diosbulbin B, the microcrystalline Cellulose of 20%, the cellulose milk sugar of 70.5%, the friendship of 5.0%
Connection Sodium Hydroxymethyl Stalcs, 2% micropowder silica gel difference are the most finely ground, cross 100 mesh sieves, standby；
(2) by diosbulbin B, microcrystalline Cellulose, cellulose milk sugar, the crosslinking Sodium Hydroxymethyl Stalcs of 3.75%, equal increments method mixes
Uniformly, add 70% ethanol soft material of medicine gross mass 6% in step (1), cross 20 mesh sieves granulations, be dried in 60 DEG C of baking ovens to
Constant weight, crosses 20 mesh sieve granulate；
(3) add micropowder silica gel and the crosslinking Sodium Hydroxymethyl Stalcs of residue 1.25%, mix homogeneously, tabletting, prepare dispersible tablet,
Every tablet weight 0.20 ± 0.01g.
Embodiment 3
A kind of diosbulbin B dispersible tablet, raw material consists of: the diosbulbin B of 2.5%, the microcrystalline Cellulose of 20%, the cellulose of 65.5%
Lactose, crosslinking Sodium Hydroxymethyl Stalcs, the micropowder silica gel of 2% of 10%.In crosslinking Sodium Hydroxymethyl Stalcs, dosage is 6.0%, outer dosage
4.0%。
Preparation method is with embodiment 2.
Embodiment 4
A kind of diosbulbin B dispersible tablet, raw material consists of: the diosbulbin B of 2.5%, the microcrystalline Cellulose of 20%, the cellulose of 60.5%
Lactose, 15% crosslinking Sodium Hydroxymethyl Stalcs, the micropowder silica gel of 2%.In crosslinking Sodium Hydroxymethyl Stalcs, dosage accounts for 3/4.
Preparation method is with embodiment 2.
Embodiment 5
A kind of diosbulbin B dispersible tablet, raw material consists of: the diosbulbin B of 3.75%, the microcrystalline Cellulose of 20.0%, the fiber of 64.5%
Element lactose, 10% crosslinking Sodium Hydroxymethyl Stalcs, the micropowder silica gel of 1.75%.In crosslinking Sodium Hydroxymethyl Stalcs, dosage accounts for 3/4.
Preparation method is with embodiment 2.
Embodiment 6
A kind of diosbulbin B dispersible tablet, raw material consists of: the diosbulbin B of 3.75%, the microcrystalline Cellulose of 40.0%, the fiber of 44.5%
Element lactose, 10% crosslinking Sodium Hydroxymethyl Stalcs, the micropowder silica gel of 1.75%.In crosslinking Sodium Hydroxymethyl Stalcs, dosage accounts for 3/4.
Preparation method is with embodiment 2.
Embodiment 7
A kind of diosbulbin B dispersible tablet, raw material consists of: the diosbulbin B of 3.75%, the microcrystalline Cellulose of 30.0%, the fibre of 55.75%
Dimension element lactose, 10% crosslinking Sodium Hydroxymethyl Stalcs, the micropowder silica gel of 0.5%.In crosslinking Sodium Hydroxymethyl Stalcs, dosage accounts for 3/4.
Preparation method is with embodiment 2.
Embodiment 8
A kind of diosbulbin B dispersible tablet, raw material consists of: the diosbulbin B of 3.75%, the microcrystalline Cellulose of 30.0%, the fibre of 53.25%
Dimension element lactose, 10% crosslinking Sodium Hydroxymethyl Stalcs, the micropowder silica gel of 3.0%.In crosslinking Sodium Hydroxymethyl Stalcs, dosage accounts for 3/4.
Preparation method is with embodiment 2.
Embodiment 9
A kind of diosbulbin B dispersible tablet, raw material consists of: the diosbulbin B of 3.13%, the microcrystalline Cellulose of 35.0%, the fibre of 53.24%
Dimension element lactose, the crosslinking Sodium Hydroxymethyl Stalcs of 7.5%, 1.13% micropowder silica gel.In crosslinking Sodium Hydroxymethyl Stalcs, dosage accounts for 3/4.
Preparation method is with embodiment 2.
Comparative example 1
Taking diosbulbin B 200g, beat powder, cross 100 mesh sieves, spraying into appropriate mass fraction is 70% ethanol, adds 17.5% micro-
Crystalline cellulose, wherein in add 7.5% microcrystalline Cellulose and 20% starch, cross 20 mesh sieves and pelletize and be dried, additional 10% crystallite is fine
Dimension element and the magnesium stearate of 1%, mix tabletting, tablet weight 0.20 ± 0.01g.
Comparative example 2
Prescription ratio: diosbulbin B: 3.13%, micropowder silica gel: 1.13%, microcrystalline Cellulose is 35% and cellulose milk sugar 60.74%.
Diosbulbin B, microcrystalline Cellulose, cellulose milk sugar are distinguished the most finely ground, crosses 100 mesh sieves, standby.In prescription ratio weigh diosbulbin B,
Microcrystalline Cellulose, cellulose milk sugar mix homogeneously, with 70% ethanol soft material, cross 20 mesh sieves and pelletize, in 55 DEG C ~ 60 DEG C baking ovens
It is dried to constant weight, crosses 20 mesh sieves, granulate, add micropowder silica gel, mix homogeneously, tabletting.
Performance test methods:
1.1. the assay method of dissolution in vitro: survey with release according to version " Chinese Pharmacopoeia " (four) 0931 dissolution in 2015
The 3rd method small-radius curve track determined in method is measured, and arranging temperature is 37 DEG C, and rotating speed is 75 r/min.Dispersible tablet puts into stripping rotor
In, adding 2% sodium lauryl sulphate of 250mL degassing, sample 2mL in the stipulated time, 0.45 μm filter membrane filters, and injects efficiently
Chromatograph of liquid.Supplementing equivalent fresh medium in stripping rotor, operation completes in 30 s simultaneously.
1.2. the detection method of hardness: use Monsanto durometer method, tabletting is stood between two pressing plates, diametrically side
To pressurization slowly, pressure when just crushing is the hardness of this sheet.
1.3. the detection method of sticking: whether sticking phenomenon occurs in tableting processes.
1.4. detection method disintegration: the tablet of preparation is respectively taken 6, in the water that temperature is 37 DEG C ± 1 DEG C, utilizes
Lift disintegration of tablet instrument detects.
1.5. the detection method of dispersing uniformity: take each 6 of diosbulbin B dispersible tablet respectively, according to inspection technique disintegration
(2015 editions " Chinese Pharmacopoeia " four general rules 0921), the sieve aperture internal diameter of stainless steel cloth is 710 μm, and water temperature is 20 DEG C and examines
Look into.Whether screen cloth is passed through in 3min.
1.6. friability: according to 0923 lower tablet friability inspection method pair of version " Chinese Pharmacopoeia " four general rules in 2015
The friability of 3 batches of dispersible tablets checks, every batch takes 36, is measured.Test weight loss whether < 1%, with or without sliver and
Fragment phenomenon.
Embodiment test data see table 1:
Comparative example test data see table 2:
1.7. hot test: Example 9 diosbulbin B dispersible tablet is appropriate, naked puts in suitable clean container, and 60 DEG C of temperature are transferred
Put 10 days, in sampling in 0,5,10 days, investigate the outward appearance of dispersible tablet, disintegration, dissolution in vitro, the content's index of effective ingredient
Change.
Result see table 3:
The highest wet test
Example 9 diosbulbin B dispersible tablet is appropriate, precise weighing, naked puts in suitable clean container, at 25 DEG C respectively at relatively
Humidity is 92.5%(KNO3) place 10 days, in the 5th day, sampling in the 10th day, investigate the outward appearance of dispersible tablet, disintegration, external molten
Out-degree.The weight of dispersible tablet before and after precise simultaneously, to investigate dispersible tablet moisture absorption deliquescence performance.
Experimental data see table 4:
1.9. thermostatic accelerated experiment
The diosbulbin B dispersible tablet of Example 3,7,9, uses plastic-aluminum gas blister, respectively in temperature 40 DEG C ± 5 DEG C, relatively
Humidity 75 %(NaCl saturated solution) under conditions of place 3 months, respectively at the 0th, 1,2, sampling detection in 3 months, investigate tablet
Outward appearance, disintegration, dissolution in vitro, five indexs of active constituent content, and every Index for examination and 0 month sample are compared.
Result see table 5:
Result of the test shows, diosbulbin B dispersible tablet constant temperature acceleration for stabilization test in appearance character, disintegration, effectively become
Dividing content and 45min dissolution in vitro to have no significant change, this tablet has preferable stability.
The present invention primarily looks at the impact on S180 sarcoma solid tumor of the diosbulbin B dispersible tablet.
2.1 animal subject
Mice, body weight 18～22g, purchased from Shanghai Slac Experimental Animal Co., Ltd., the animal quality certification number: SCXK
(Shanghai 2015-0005).Mouse feeder temperature (22 ± 1) DEG C, relative humidity (65 ± 10) %, lighting hours 12h every day.
2.2 test medicine
Diosbulbin B dispersible tablet prepared by Example 9 and comparative example 1-2, diosbulbin B powder.
2.3 experimental technique
Using tumor-bearing mice experiment in vivo, in euphorbia egg decoctum tumor-bearing mice abdomen, the corresponding tumor cell of extraction, contaminates with trypan blue
Color, counting, it is diluted to (1.0-1.3) × 107cells/mL in centrifuge tube with physiological saline solution, inserts on ice, subcutaneous note
Penetrating this concentration tumor cell of inoculation in the right oxter of mice, injection volume 0.1mL/ is only.By body weight random packet, respectively model group,
5-Fu group, embodiment group 1, comparative example group 1, comparative example group 2, diosbulbin B powder group.Medicine 24h after inoculation is started by body weight
Gastric infusion, model group gives the CMC-Na of 200mg/kg；5-Fu (with dd water dissolution to 2.5mg/mL) group lumbar injection
(ip), every other day inject once；Embodiment group consumption is the diosbulbin B dispersible tablet of 1/kg embodiment 9 preparation；Comparative example group
1-2 consumption is diosbulbin B dispersible tablet prepared by 1/kg comparative example 1-2；Diosbulbin B powder group consumption is 6.5mg Diosbulbin powder
With 193.5mg CMC-Na；Successive administration 12d, 24h after last administration, pluck eyeball blood sampling, for measuring blood after centrifugation serum
Clear ALT and AST vigor is used；Take tumor tissue, weigh.Tumor inhibition ratio (%)=[(C-T)/C] × 100,
Wherein C refers to model group average tumor weight, and T shows medicine group average tumor weight.Significant difference, and tumor control rate ＞ is heavily had with tumor
30% has the standard of anti-tumor activity for medicine.
2.4 experimental result
Dispersible tablet is to mice avirulence.Comparing with model group, as shown in table 1, the mice of inoculation euphorbia egg decoctum is giving Huang continuously
Solely after element B dispersible tablet 12d, tumor is heavily substantially reduced, and shows that diosbulbin B dispersible tablet is effective to S180 solid tumor；With diosbulbin B powder
Group is compared, and embodiment group tumor is heavily substantially reduced, and tumor control rate significantly improves, and shows that diosbulbin B dispersible tablet is higher than powder absorbance,
Anti-tumor activity is high.Compared with comparative example group 1-2, embodiment group tumor weight average is substantially reduced, and tumor control rate significantly improves, and shows
Diosbulbin B dispersible tablet of the present invention is higher than dispersible tablet anti-tumor activity prepared by additive method.
The present invention has investigated the inhibitory action to human tumor of diosbulbin B dispersible tablet further.
3.1 cell strain sources
Hep3B cells, gastric cancer SGC-7901, urinary bladder carcinoma T24 cell line strain are purchased from Chinese Academy of Sciences's Shanghai cytobiology
Institute.
3.2 experimental technique
Cell proliferation experiment (MTT): use 0.25% trypsin digestion cell, 1000rpm is centrifuged, with containing 5% activated carbon inactivation blood
Clearly, without phenol red DMEM height sugar culture fluid 37 DEG C, 95%CO2 cultivates 48h (to get rid of the interference of endogenous hormones), i.e. cell enters
Enter exponential phase, use 0.25% trypsin digestion cell, with 2 × 103/hole inoculating cell on 96 well culture plates, every hole
Volume 180 μ L, 24h cell attachment, each column sets 5 multiple holes, sets model photograph, 5-Fu group, embodiment group, diosbulbin B powder group respectively,
Continue after dosing to observe to cultivate 48h.
Colour generation and colorimetric: after 48h is cultivated in dosing, take out culture plate, and every hole adds MTT solution (5mg/mL) 20 μ L,
37 DEG C, 5%CO2Continue to cultivate 4h to terminate cultivating.Careful suction abandons culture supernatant in hole, and every hole adds 150 μ LDMSO vibrations
10min, makes crystal fully dissolve, select 490nm automatic microplate reader (BIO-TEK) upper measure each hole absorption value (OD,
It is directly proportional to living cells quantity), calculate inhibitory rate of cell growth.
3.3 experimental result
Inhibitory rate of cell growth=(control wells OD value-experimental port OD value)/control wells OD value × 100%.
Clinical trial:
Gastric cancer cases treats 60 examples, age 40-70 year, Tumor diameter≤3cm altogether.After above-mentioned Chemotherapy in Patients, it is divided into 3 groups,
Often organizing 20 examples, take diosbulbin B dispersible tablet, each two panels, every day twice, warm water takes, and treats six months.
Curative effect determinate standard
Recovery from illness: transference cure；Effective: symptom substantially disappears, tumorous size reduces；Invalid: ultrasound diagnosis muscular tumor volume is the most not
Become or increase.
Through treatment, find:
For the dispersible tablet of embodiment 9 preparation, 16 examples of fully recovering, effective 4 examples；
For the dispersible tablet of comparative example 1 preparation, 6 examples of fully recovering, effective 7 examples, invalid 7 examples；
For the dispersible tablet of comparative example 2 preparation, 4 examples of fully recovering, effective 8 examples, invalid 8 examples.
As can be seen here, the curative effect of the dispersible tablet of embodiment 9 preparation is unexpectedly higher than comparative example 1-2.
Choose the patient of hepatocarcinoma, gastric cancer, bladder cancer, after chemotherapy, take diosbulbin B dispersible tablet, each two panels, every day two
Secondary, warm water takes.
Case 1: XX, man 61 years old, it is diagnosed as gastric cancer mid-term, art finding, intraperitoneal lymph node extensively shifts, clothes
Using diosbulbin B dispersible tablet, each two panels, every day twice, warm water takes, recovery from illness in continuous 6 months, follows up a case by regular visits to 1 year, does not recurs.
Case 2 a: XX, female 75 years old, is diagnosed as hepatocarcinoma in 12 years, takes diosbulbin B dispersible tablet, each two panels, every day two
Secondary, warm water takes, recovery from illness, follows up a case by regular visits to 1 year, does not recurs.Case 3: permitted XX, female 68 years old, be diagnosed as bladder cancer, take Dioscorea bulbifera L.
Element B dispersible tablet, each two panels, every day twice, warm water takes, recovery from illness in continuous 6 months, and tumor tissues disappears, and follows up a case by regular visits to 1 year again
Send out.
Claims (7)
1. a diosbulbin B dispersible tablet, it is characterised in that be made up of following weight percent content, diosbulbin B 2.5-5.0%,
Disintegrating agent crosslinking Sodium Hydroxymethyl Stalcs 5-15%, wetting agent micropowder silica gel 0.5-3.0%, microcrystalline Cellulose 20-40%, surplus is fine
Dimension element lactose.
Diosbulbin B dispersible tablet the most according to claim 1, it is characterised in that dispersible tablet adds dispersible tablet quality 4-6%
Ethanol solution, the mass fraction of ethanol solution is 70%.
3. according to the diosbulbin B dispersible tablet one of claim 1-2 Suo Shu, it is characterised in that be made up of following percentage by weight,
Diosbulbin B 3.13%, cross-links Sodium Hydroxymethyl Stalcs 7.5%, micropowder silica gel 1.13%, microcrystalline Cellulose 35%, cellulose milk sugar
53.24%。
Diosbulbin B dispersible tablet the most according to claim 1, it is characterised in that in described crosslinking Sodium Hydroxymethyl Stalcs uses
Outer addition adds, and the ratio inside adding quality and outer dosage is 3:1.
Diosbulbin B dispersible tablet the most according to claim 1, it is characterised in that dispersible tablet hardness is 40-60N.
6. the preparation method of a diosbulbin B dispersible tablet as claimed in claim 1, it is characterised in that use wet granulation process,
Comprise the following steps:
(1) diosbulbin B, microcrystalline Cellulose, cellulose milk sugar, crosslinking Sodium Hydroxymethyl Stalcs, micropowder silica gel are weighed by weight proportion
The most finely ground, cross 100 mesh sieves, standby；
(2) by diosbulbin B, microcrystalline Cellulose, cellulose milk sugar, the 1/2-3/4 of crosslinking Sodium Hydroxymethyl Stalcs quality in step (1)
Use equal increments method mix homogeneously, with 70% ethanol soft material, cross 20 mesh sieves and pelletize, be dried to perseverance in 55 DEG C of-60 DEG C of baking ovens
Weight, crosses 20 mesh sieve granulate；
(3) add micropowder silica gel and remaining crosslinking Sodium Hydroxymethyl Stalcs, mix homogeneously, tabletting, prepare dispersible tablet, tablet weight
0.2±0.01g。
Preparation method the most according to claim 6, it is characterised in that in step (2), crosslinking Sodium Hydroxymethyl Stalcs adds matter
Amount is in step (1) the 3/4 of crosslinking Sodium Hydroxymethyl Stalcs quality.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610217462.8A CN105796518B (en) | 2016-04-08 | 2016-04-08 | A kind of diosbulbin B dispersible tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610217462.8A CN105796518B (en) | 2016-04-08 | 2016-04-08 | A kind of diosbulbin B dispersible tablet and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105796518A true CN105796518A (en) | 2016-07-27 |
| CN105796518B CN105796518B (en) | 2018-06-12 |
Family
ID=56460782
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610217462.8A Active CN105796518B (en) | 2016-04-08 | 2016-04-08 | A kind of diosbulbin B dispersible tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105796518B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113384575A (en) * | 2021-07-05 | 2021-09-14 | 贵州医科大学 | Use of diosbulbin in cell proliferation inhibition |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010006451A1 (en) * | 2008-07-15 | 2010-01-21 | Pharmascience Inc. | Dosage form containing a statin |
| CN101810591A (en) * | 2010-03-31 | 2010-08-25 | 昆明制药集团股份有限公司 | Mangiferin dispersible tablets and preparation method thereof |
| CN102070646A (en) * | 2011-01-11 | 2011-05-25 | 山东省中医药研究院 | Extraction method of Diosbulbin B |
| CN102309655A (en) * | 2010-07-08 | 2012-01-11 | 上海中医药大学 | Chinese medicinal composition with effect of preventing and treating cancers and application of Chinese medicinal composition |
| CN104352534A (en) * | 2014-10-16 | 2015-02-18 | 山东省中医药研究院 | Poria peel total-triterpene dispersible tablet and preparation method thereof |
-
2016
- 2016-04-08 CN CN201610217462.8A patent/CN105796518B/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010006451A1 (en) * | 2008-07-15 | 2010-01-21 | Pharmascience Inc. | Dosage form containing a statin |
| CN101810591A (en) * | 2010-03-31 | 2010-08-25 | 昆明制药集团股份有限公司 | Mangiferin dispersible tablets and preparation method thereof |
| CN102309655A (en) * | 2010-07-08 | 2012-01-11 | 上海中医药大学 | Chinese medicinal composition with effect of preventing and treating cancers and application of Chinese medicinal composition |
| CN102070646A (en) * | 2011-01-11 | 2011-05-25 | 山东省中医药研究院 | Extraction method of Diosbulbin B |
| CN104352534A (en) * | 2014-10-16 | 2015-02-18 | 山东省中医药研究院 | Poria peel total-triterpene dispersible tablet and preparation method thereof |
Non-Patent Citations (3)
| Title |
|---|
| 林芳，华碧春: "中药黄药子抗肿瘤作用研究现状", 《亚太传统医药》 * |
| 沈雄荣，董建勇: "不同产地黄药子中黄独乙素的含量测定", 《医药导报》 * |
| 郭艳伟，等: "正交设计优选黄药子中黄独素B 的提取工艺", 《中成药》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113384575A (en) * | 2021-07-05 | 2021-09-14 | 贵州医科大学 | Use of diosbulbin in cell proliferation inhibition |
Also Published As
| Publication number | Publication date |
|---|---|
| CN105796518B (en) | 2018-06-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103393821B (en) | Traditional Chinese medicine composition for treating chronic pelvic inflammation and preparation method thereof | |
| CN103316219A (en) | Traditional Chinese medicinal preparation for treating phthisis and preparation method thereof | |
| CN101181395A (en) | Medicine preparations for curing dermatosis and preparation method thereof | |
| CN102526427B (en) | Traditional Chinese medicinal composition for treating gastrointestinal diseases and quality inspection method | |
| CN103263433A (en) | Medical application of natural product 6-shogaol in enhancing chemosensitivity of pancreatic cancer on gemcitabine and compound drug composite of natural product 6-shogaol | |
| CN103191191B (en) | Preparation method of traditional Chinese medicine composition for treating advanced non-small cell lung cancers | |
| CN107669991A (en) | A kind of pharmaceutical composition for reducing serum uric acid level and preparation method thereof | |
| CN105796518A (en) | Diosbulbin B dispersible tablets and preparation method thereof | |
| CN102652819B (en) | Fuyankang dispersible tablet and preparation method thereof | |
| CN100482266C (en) | Medical composite prepared by sarcandra and oldenlandia | |
| CN101757309B (en) | Medicament for treating uterine bleeding and preparation process thereof | |
| CN100563680C (en) | Chinese medicine preparation and the method for making and the application thereof of prevention and treatment intestinal adhesion after abdominal cavity operation | |
| CN104825609B (en) | A kind of pharmaceutical composition for improving abdominal thermal infusion chemotherapy adverse effect and preparation method thereof | |
| CN103520550B (en) | Traditional Chinese medicine for treating external cold internal rheum type chronic bronchitis and preparation method thereof | |
| CN103251883A (en) | Antitumor pharmaceutical composition and preparation method thereof | |
| CN102813715A (en) | Compound medicine for treating post-infectious cough and preparation method and application thereof | |
| CN100546621C (en) | A kind of new purposes of known drug | |
| CN104800675A (en) | Medicament for treating active ulcerative colitis | |
| CN105232923A (en) | Foot bath medicine for treating specific endowment constitution and preparation method and application thereof | |
| CN105596312A (en) | Dimemorfan phosphate capsule composition and preparing method thereof | |
| CN102772540B (en) | A kind of medicine for the treatment of metabolism syndrome | |
| CN103520661A (en) | Traditional Chinese medicinal enteric-coated tablets for treating proctitis, colitis and irritable bowel syndrome, as well as preparation method and application thereof | |
| CN103463402B (en) | Traditional Chinese medicine composition for infantile asthma and preparation method thereof | |
| CN100482245C (en) | Medicine composition contg. isatis root and scutellariae glucoside | |
| CN1939325B (en) | Medicinal composition of houttuynin sodium and astragalin, its making method and usage |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |