CN102048705A - Palonosetron hydrochloride orally disintegrating tablet and preparation method thereof - Google Patents
Palonosetron hydrochloride orally disintegrating tablet and preparation method thereof Download PDFInfo
- Publication number
- CN102048705A CN102048705A CN2009102303239A CN200910230323A CN102048705A CN 102048705 A CN102048705 A CN 102048705A CN 2009102303239 A CN2009102303239 A CN 2009102303239A CN 200910230323 A CN200910230323 A CN 200910230323A CN 102048705 A CN102048705 A CN 102048705A
- Authority
- CN
- China
- Prior art keywords
- mannitol
- oral cavity
- mixture
- cavity disintegration
- palonosetron hcl
- 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
Abstract
The invention belongs to the field of pharmacy and medical technology, and relates to a palonosetron hydrochloride orally disintegrating tablet and a preparation method thereof. The orally disintegrating tablet comprises the following components in percentage by mass: palonosetron hydrochloride 0.16 to 1.5, mannite 70 to 95, disintegrating agent 1.5 to 15, taste correcting agent 1 to 3, lubricating agent 0.5 to 2, and other auxiliary materials 0 to 15. The manufacturing technology can adopt dry direct tablet compressing. The palonosetron hydrochloride orally disintegrating tablet has the advantages of simple manufacturing technology, low cost and quick effect on indications, is convenient to take, can be disintegrated into fine grains or powder in oral cavity quickly after oral administration, and is particularly suitable for patients who swallow hard and tumor patients with weak physical fitness. The preparation exists in a form of fine grain or powder before reaching the gastrointestinal tract, and the medicine dissolves out in an accelerating manner and is distributed in the gastrointestinal tract in a large area for more absorption points, so that the bioavailability can be improved.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be specifically related to a kind of palonosetron Hcl oral cavity disintegration tablet and preparation method thereof.
Background technology
China's Epidemiological study shows, urbanite's malignant tumor in 2003 fatality rate is 94.71/10 ten thousand, cancer becomes first deadly disease, and 10 kinds of cancers that mortality rate is the highest are respectively pulmonary carcinoma, hepatocarcinoma, gastric cancer, esophageal carcinoma, colon, rectum and anus cancer, leukemia, breast carcinoma, nasopharyngeal carcinoma, cervical cancer, bladder cancer; Urban residents' malignant tumor patient case fatality rate is higher, be 104.01/10 ten thousand, occupy first of whole dead diseases, wherein 10 kinds of cancers that mortality rate is the highest are respectively hepatocarcinoma, gastric cancer, pulmonary carcinoma, esophageal carcinoma, colon, rectum and anus cancer, leukemia, breast carcinoma, nasopharyngeal carcinoma, cervical cancer, bladder cancer.
Along with the raising of chemotherapy status in oncotherapy and the Application and Development of more and more novel chemotherapeutics, people are also more deep to the understanding of chemotherapy adverse effect.Nausea and vomiting is a modal toxicity in the chemotherapy of tumors, has had a strong impact on patient's quality of life, treatment compliance and curative effect.Therefore, the development of chemotherapy ancillary drug has been played crucial effects to the raising of chemotherapeutic efficacy and the minimizing of untoward reaction.Domestic in recent years Bendectin hospital administration market constantly increases, saw from IMS whole nation hospital administration statistics in 2006 and reached about 8.4 hundred million yuan, the first half of the year in 2007 was 4.93 hundred million yuan, estimate to reach about 1,000,000,000 yuan the whole year, wherein picking up anti-agent with the 5-HT receptor is absolutely main force, accounts for the share more than 99.6%.From IMS whole nation hospital administration data, the main at present Bendectin that uses is the i.e. 5 one hydroxy color amine antagonist Bendectins of 5 kinds of department's fine jade class medicines.Also just because of being extensive use of of 5-HT3 receptor antagonist, the prevention and the treatment of chemotherapy nausea and vomiting have obtained rapid progress.
Hydrochloric acid Pa Nuoluosiqiong (Palonosetron Hydrochloride) is a kind of 5-HT3 receptor antagonist of efficient, high selectivity, and chemistry is by name: 2-[1-azabicyclo (2.2.2) suffering-3S-yl]-2,3,3aS, 4,5,6-six hydrogen-1H-benzo [de] isoquinolin-1-keto hydrochloride.It is that the 4th of FDA approval is used for the treatment of that chemotherapeutics causes acute 5-HT3 receptor antagonist of feeling sick with vomiting is that first approval can be used for moderate and causes feel sick medicine with vomiting of the drug-induced retardance of vomitting.This medicine is succeeded in developing by Switzerland Helsinn Healthcare, obtains the drugs approved by FDA listing in July, 2003.At present the dosage form of external listing has capsule (specification: 0.5mg), injection; Domestic only have injection to go on the market, and also do not have the rapid release oral formulations of palonosetron Hcl clinically.
With other half-life the 5-HT of a few hours is only arranged
3Receptor antagonist is compared, the long half time of palonosetron Hcl, and can be optionally and 5-HT
3Receptors bind has stronger affinity, with the affinity of receptor almost be other 5-HT
3100 times of antagonist.Therefore clinical efficacy is remarkable, patient's compliance height, the very fast choice drug that just becomes the prevention nausea and vomiting after the listing.The palonosetron pharmacokinetic studies result of having gone on the market shows that its long half time is about 40h, thereby keeps 2-3 days curative effect after can 1h takes before chemotherapy.This shows to be developed to especially oral cavity disintegration tablet of oral solid formulation, not only improve compliance of patients, reduce drug cost; And can reach bioequivalence, make things convenient for medication, quick acting.
Oral cavity disintegration tablet is met the rapid disintegrate of saliva and is dispersed into fine particle, and the medicine stripping is accelerated, and big in the gastrointestinal tract area distributions, absorption point is many.Compare with conventional tablet, this dosage form need not water and also need not to chew, and after medicine places on the tongue disintegrate rapidly, borrows swallowing act to go into stomach; Also can place and penetrate down, after the disintegrate, medicine absorbs onset by mucosa rapidly.Take medicine conveniently for the tumor patient that has a delicate constitution, oral cavity disintegration tablet, need not water and also needn't chew; Avoided the shortcoming of conventional tablet, capsule dysphagia simultaneously, improved patient's compliance, improved clinical treatment effectiveness and should be acute.Patient for long-term treatment is more prone to this form of administration of receiving port cavity disintegrating tablet.
At present, being suitable for the big main technology of preparing of oral cavity disintegration tablet of producing has: lyophilization, compression moulding, direct compression process and wet granulation, dry-pressing granulation etc.Wherein the lyophilization production cost is higher, and technical difficulty is big, the equipment complexity, and need special blister package further increase its cost because the product friability is high.Compression moulding prepares oral cavity disintegration tablet and also needs special equipment, the shortcoming that cost is higher and friability is higher.Direct compression process is than wet granulation and the dry-pressing prepared oral cavity disintegration tablet of granulating, and disintegration is faster, and grains of sand sense is littler, and cost is lower.This technology multiselect as adjuvant, adds and is aided with correctives with the MCC that has filler, binding agent, disintegrating agent, lubricant and good fluidity and compressibility concurrently in right amount, can obtain mouthfeel oral cavity disintegration tablet preferably.
Patent about palonosetron Hcl all is chemical compound patent (the synthetic crystal formation of protection) and preparation patent both at home and abroad.And the dosage form that the preparation patent relates to mostly is injection, powder injection formulation, does not also relate to this novel dosage form of oral cavity disintegration tablet.
Summary of the invention
The present invention is directed to the deficiency of existing palonosetron Hcl formulation development, a kind of palonosetron Hcl oral cavity disintegration tablet and preparation method thereof is provided, adopted all good mannitol of compressibility and mouthfeel as filler, with the palonosetron Hcl oral cavity disintegration tablet of direct powder compression technology gained, taking convenience, to indication reach the peak early, curative effect is obvious, mouthfeel good; Its preparation method has adopted common press device and simple process, and processing step is simple, and cost is low, is suitable for promotion and application widely.
Technical scheme of the present invention is as follows: separately with mannitol as filler, its percetage by weight in whole prescription is 70-95%.
The inventor finds through production practices, during at the production of palonosetron Hcl oral cavity disintegration tablet, separately with mannitol as filler, share following advantage than mannitol and lactose: (1) compressibility better is separately to be that the prescription hardness of filler is bigger with mannitol under the uniform pressure; (2) hygroscopicity is lower.Add the oral cavity disintegration tablet that mannitol can make good mouthfeel, be easy to molding simultaneously,, the mass percent of mannitol can be controlled at 80%-90% in order to reach better result of use.The mannitol 200SD that the optional auto-flowability of mannitol is good (
200SD) or the mannitol of other model, other model can be selected from mannitol 100SD (
100SD), mannitol 400DC (
400DC), mannitol 500DC (
500DC) and granularity is thin, dissolubility is higher
Deng.Further discovering, at the palonosetron Hcl oral cavity disintegration tablet, the preferred mannitol 200SD that uses separately of mannitol, perhaps use the combination of mannitol 200SD and other model mannitol, can obtain good fluidity (be 40-45 ° the angle of repose that can make active component and all adjuvants mix powder), compressibility height, disintegrate oral cavity disintegration tablet rapidly.In order to reach better result of use, it is 70%-85% that mannitol 200SD accounts for whole constituent mass percentage ratios, preferred 75-80%, and the mannitol of other model accounts for whole constituent mass percentage ratios and is controlled at 0%-10%, preferred 5-10%.
Palonosetron Hcl oral cavity disintegration tablet provided by the invention is to be active component with the palonosetron Hcl, adopts mannitol, disintegrating agent, correctives, lubricant and other adjuvant as excipient, and concrete component and mass percent thereof are as follows:
The mass percent of active ingredient palonosetron Hcl is preferably at 0.25%-1% in the described palonosetron Hcl oral cavity disintegration tablet, especially preferred 0.3%-0.8%, the palonosetron Hcl oral cavity disintegration tablet sheet that this scope compacting obtains focuses between the 50-320mg, both can satisfy the requirement heavy of FDA oral cavity disintegration tablet guide, and can obtain excellent taste, the good preparation of disintegrate again sheet.
And the optional self-crosslinking polyvinylpyrrolidone of disintegrating agent, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose and composition thereof in the described palonosetron Hcl Orally disintegrating slice prescription, the preferred 6%-12% of mass percent; The purpose that adds disintegrating agent is to make oral cavity disintegration tablet meet behind the water disintegrate beading rapidly, satisfying disintegration less than 1min, and then less than the requirement of 30s.
Described correctives is selected from natural or artificial sweetening agent such as Aspartane, citric acid, essence and composition thereof, mass percent is 0.5%-3%, the purpose that adds correctives is to improve mouthfeel, allow the patient be happy to take, wherein citric acid can play flavored action, can quicken the saliva of buccal cavity secretion again, accelerate the tablet disintegrate.
And the lubricant in the prescription is selected from magnesium stearate, Pulvis Talci, stearic acid, calcium stearate, zinc stearate, Polyethylene Glycol, sodium lauryl sulphate, Stepanol MG and composition thereof, mass percent is 0.5%-3%, the purpose that adds lubricant is to increase to mix powder or particulate lubricity, avoid sticking or plug towards phenomenon, make the bright and clean oral cavity disintegration tablet of outward appearance; The selection of lubricant mass percent scope is bigger to the influence of oral cavity disintegration tablet compressibility, consumption is too high may to cause sliver and disintegrate slow, consumption is low excessively, filling in can appear in the tabletting process dashes even the phenomenon of sticking, and the inventor determines that through long-term experiment the mass percent of lubricant is preferably at 1.0%-2.0%.
The optional Autoadhesive of other adjuvant, fluidizer in the described palonosetron Hcl oral cavity disintegration tablet, wherein binding agent is selected from microcrystalline Cellulose, starch or its mixture, preferably microcrystalline cellulose, mass percent is 0%-15%, the purpose that adds microcrystalline Cellulose, starch is to play disintegrate and adherent dual function, can avoid the palonosetron Hcl oral cavity disintegration tablet sliver phenomenon to occur in the preparation of high speed tablet press equipment; The preferred colloidal state dioxy of fluidizer silica gel wherein, mass percent is 0.5%-2%, the fluidizer of adding can increase the flowability of mixing powder effectively, reduce tablet weight variation.But both have concurrently above-mentioned binding agent and fluidizer, also can have only a kind ofly, or do not have, and in order to reach best result of use and drug effect, preferably the two all has.
The preparation technology of palonosetron Hcl oral cavity disintegration tablet of the present invention is as follows: adopt direct powder compression, it may further comprise the steps:
(1) presses the mass percent of component in the palonosetron Hcl oral cavity disintegration tablet, take by weighing each component;
(2) with the palonosetron Hcl in the step (1), correctives, disintegrating agent respectively porphyrize cross 80 mesh sieves, then with its mix homogeneously, obtain mixture A;
(3) mannitol in the step (1) is crossed 40 mesh sieves, take by weighing respectively according to quantity, mix homogeneously obtains mixture B then;
(4) the mixture B in the step (3) is joined among the mixture A in the step (2) with the equivalent method of progressively increasing, fully mix, obtain mixture C;
(5) mixture C in step (4) adds lubricant, and the mixing that sieves carries out the intermediate content detection, determines the heavy back employing of sheet direct compression technology tabletting, promptly;
In prescription when being added with fluidizer and binding agent simultaneously, can fluidizer be added in step (5) with lubricant, thereby finish whole complete processing technique with binding agent with mannitol mistake 40 mesh sieves in step (3) man-hour adding.
The present invention directly uses direct powder compression, and with respect to existing wet granulation, and the dry-pressing prepared oral cavity disintegration tablet of granulating, disintegration is faster, and grains of sand sense is littler, and cost is lower, is suitable for producing in enormous quantities and guaranteeing the quality of final products.
The palonosetron Hcl oral cavity disintegration tablet that adopts said method to make, be 15s-30s its disintegration, 10min in distilled water stripping quantity greater than 90%.The palonosetron Hcl oral cavity disintegration tablet that adopts above-mentioned easy direct compression process to make, the heavy 50-320mg of sheet, hardness 3-7kg, friability are less than 0.5%, and the disintegration time that adopts static disintegration time mensuration method to measure is 15s-30s.
In sum, the invention provides that a kind of preparation technology is simple, cost is low, and taking convenience, to the rapid-action palonosetron Hcl oral cavity disintegration tablet of indication.The rapid disintegrate in the oral cavity of the oral back of palonosetron Hcl oral cavity disintegration tablet provided by the invention is dispersed into fine particle or powder, is particularly useful for the patient of dysphagia and the tumor patient that has a delicate constitution.And said preparation existed with fine particle or powder type before arriving gastrointestinal tract, and the medicine stripping is accelerated, and is big in the gastrointestinal tract area distributions; absorption point is many, has adopted common press device and simple process simultaneously, and processing step is simple; cost is low, is suitable for promotion and application widely.
The specific embodiment
Following examples only are used to further specify the present invention, but do not limit the present invention.
Test method and test instrunment are as follows among the embodiment:
A, hardness measurement instrument: YD-1 tablet hardness tester (Tianjin state inscription medical equipment company limited)
Get 10 of palonosetron Hcl oral cavity disintegration tablets (n=10), measure tablet hardness with YD-1 tablet hardness tester respectively.
B, disintegration time mensuration adopt static disintegrate method.Get 1 of palonosetron Hcl oral cavity disintegration tablet, put in the 10ml test tube (the test tube internal diameter is 13mm), in vitro fill 2ml water, water temperature is 37 ℃, and tablet should disintegrate in 1 minute, be dispersed in the water.Pour out and sieve, each water 2ml, wash test tube and screen cloth at twice, can be all by the screen cloth of aperture less than 710um.Check 6 (n=6) as stated above, should be up to specification.
C, friability are measured, and test according to Chinese Pharmacopoeia version appendix in 2005 XG tablet friability inspection technique.
Embodiment 1:
Palonosetron Hcl Orally disintegrating tablet recipe is:
Preparation: this dosage form can use conventional tablet pharmaceutical equipment to produce and use the direct compression prepared, concrete preparation method is as follows: with orange flavor, citric acid, Aspartane, palonosetron Hcl, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone respectively porphyrize cross 80 mesh sieves, and its mix homogeneously is got mixture A; Mannitol 200SD, mannitol 100SD cross 40 mesh sieves respectively, take by weighing respectively according to quantity, make its mix homogeneously get mixture B; The mode that adopts equivalent to progressively increase adds mixture B among the mixture A, obtains mixture C.The magnesium stearate that adds recipe quantity again, the mixing that sieves carries out the intermediate content detection.Determine the heavy back employing of sheet direct compression technology tabletting, promptly.
Embodiment 2:
Palonosetron Hcl Orally disintegrating tablet recipe is:
Preparation: this dosage form can use conventional tablet pharmaceutical equipment to produce and use the direct compression prepared, concrete preparation method is as follows: with orange flavor, citric acid, Aspartane, palonosetron Hcl, low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose respectively porphyrize cross 80 mesh sieves, and its mix homogeneously is got mixture A; Mannitol 200SD, microcrystalline Cellulose are crossed 40 mesh sieves respectively, take by weighing respectively according to quantity, make its mix homogeneously get mixture B; The mode that adopts equivalent to progressively increase adds mixture B among the mixture A, obtains mixture C.The Pulvis Talci that adds recipe quantity again, the mixing that sieves carries out the intermediate content detection.Determine the heavy back employing of sheet direct compression technology tabletting, promptly.
Embodiment 3:
Palonosetron Hcl Orally disintegrating tablet recipe is:
Preparation: with millefleurs, Aspartane, palonosetron Hcl, polyvinylpolypyrrolidone respectively porphyrize cross 80 mesh sieves, and its mix homogeneously is got mixture A; Mannitol 200SD crosses 40 mesh sieves, take by weighing according to quantity B; The mode that employing equivalent is progressively increased adds mixture A with the B of recipe quantity, obtains mixture C.The colloidal silica, the calcium stearate that add recipe quantity again, the mixing that sieves carries out the intermediate content detection.Determine the heavy back employing of sheet direct compression technology tabletting, promptly.
Embodiment 4:
Palonosetron Hcl Orally disintegrating tablet recipe is:
Preparation: with strawberry essence, steviosin, citric acid, palonosetron Hcl, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium respectively porphyrize cross 80 mesh sieves, and its mix homogeneously is got mixture A; Mannitol 200SD and microcrystalline Cellulose are crossed 40 mesh sieves respectively, take by weighing respectively according to quantity, make the two mix homogeneously get mixture B; The mode that adopts equivalent to progressively increase adds mixture B among the mixture A, obtains mixture C.The micropowder silica gel, the magnesium stearate that add recipe quantity again, the mixing that sieves carries out the intermediate content detection.Determine the heavy back employing of sheet direct compression technology tabletting, promptly.
Embodiment 5:
Palonosetron Hcl Orally disintegrating tablet recipe is:
Preparation: with orange flavor, Aspartane, palonosetron Hcl, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone respectively porphyrize cross 80 mesh sieves, and its mix homogeneously is got mixture A; Mannitol 200SD, mannitol
Starch is crossed 40 mesh sieves, take by weighing respectively according to quantity, and mix homogeneously gets mixture B; The mode that adopts equivalent to progressively increase adds mixture B among the mixture A, obtains mixture C.The stearic acid and the Polyethylene Glycol that add recipe quantity again, the mixing that sieves carries out the intermediate content detection.Determine the heavy back employing of sheet direct compression technology tabletting, promptly.
The test example
Supplementary material granulometry result is as shown in the table among each embodiment:
| The supplementary material title | d (0.1)μm | d (0.5)μm | d (0.9)μm |
| Palonosetron Hcl | 2.80 | 18.52 | 72.90 |
| Mannitol 200SD | 16.16 | 114.49 | 210.69 |
| Mannitol 100SD | 36.12 | 81.75 | 140.60 |
| MCC?PH101 | 23.04 | 58.12 | 123.86 |
| Polyvinylpolypyrrolidone | 10.00 | 24.46 | 54.82 |
| Orange flavor | 14.29 | 50.36 | 120.50 |
| Aspartame | 1.98 | 7.93 | 30.24 |
| Cross-linking sodium carboxymethyl cellulose | 12.20 | 30.56 | 60.25 |
| Low-substituted hydroxypropyl cellulose | 20.23 | 36.78 | 58.26 |
| Micropowder silica gel | 2.31 | 12.14 | 42.70 |
| Magnesium stearate | 2.76 | 12.00 | 43.3 |
Can determine the addition sequence of each adjuvant by the above-mentioned particle size range that records.
The disintegration of each embodiment, friability, tablet hardness, dissolution numerical value is as shown in the table:
By the above-mentioned every data that record as can be known: the oral cavity disintegration tablet that adopts this method to make, be 15s-30s its disintegration, hardness 3-7kg, friability be less than 0.5%, 30min in distilled water solution dissolution greater than 90%.
Influence factor's result of the test of each embodiment is as shown in the table:
Every investigation index by above-mentioned oral cavity disintegration tablet such as disintegration, friability, dissolution result be as can be known: with the palonosetron Hcl oral cavity disintegration tablet of mannitol as filler, disintegrate and stripping are all rapider in higher hardness range (3-7kg); Simultaneously, influence factor's test shows that this product illumination is its major influence factors.Therefore, both be suitable for transportation, stored by effective lucifuge, palonosetron Hcl oral cavity disintegration tablet after wet packing.
In sum, the palonosetron Hcl oral cavity disintegration tablet that proportioning provided by the present invention and processing technique make, fast disintegrate, and stability, mouthfeel are all good, and its drug effect is higher than existing other dosage forms on the market.
Claims (9)
1. palonosetron Hcl oral cavity disintegration tablet is characterized in that: separately with mannitol as filler, its percetage by weight in whole prescription is 70-95%.
2. palonosetron Hcl oral cavity disintegration tablet according to claim 1 is characterized in that: each component and mass percent thereof are in the described oral cavity disintegration tablet:
3. palonosetron Hcl oral cavity disintegration tablet according to claim 1 and 2 is characterized in that: the mass percent of described palonosetron Hcl is 0.25%-1%; Mannitol is selected from mannitol 200SD, or the combination of mannitol 200SD and other model mannitol, and it is 70%-85% that mannitol 200SD accounts for whole constituent mass percentage ratios, and it is 0%-10% that other model mannitol accounts for whole constituent mass percentage ratios.
4. palonosetron Hcl oral cavity disintegration tablet according to claim 3 is characterized in that: the mass percent of described palonosetron Hcl is 0.3%-0.8%; It is 75%-80% that mannitol 200SD accounts for whole constituent mass percentage ratios, and it is 5%-10% that other model mannitol accounts for whole constituent mass percentage ratios.
5. according to claim 2 or 3 described palonosetron Hcl oral cavity disintegration tablets, it is characterized in that: described other model can be selected from mannitol 100SD or mannitol 400DC or mannitol 500DC or
6. palonosetron Hcl oral cavity disintegration tablet according to claim 3, it is characterized in that: disintegrating agent is crospolyvinylpyrrolidone or low-substituted hydroxypropyl cellulose or carboxymethyl starch sodium or cross-linking sodium carboxymethyl cellulose or its mixture, and mass percent is 6%-12%; Correctives is Aspartane or essence or citric acid or its mixture; Lubricant is magnesium stearate or Pulvis Talci or stearic acid or calcium stearate or zinc stearate or Polyethylene Glycol or micropowder silica gel or sodium lauryl sulphate or Stepanol MG or its mixture.
7. palonosetron Hcl oral cavity disintegration tablet according to claim 2 is characterized in that: other adjuvant is binding agent or fluidizer; Wherein binding agent is microcrystalline Cellulose or starch or its mixture, the preferred 0%-15% of mass percent; Fluidizer is selected from micropowder silica gel or silicon dioxide or its mixture, and mass percent is 0%-2%.
8. oral cavity disintegration tablet according to claim 1 and 2 is characterized in that: described palonosetron Hcl oral cavity disintegration tablet, and the heavy 50-320mg of sheet, hardness 3-7kg, friability are less than 0.5%, and be 15s-30s disintegration.
9. prepare the method for the described oral cavity disintegration tablet of claim 1, it is characterized in that: adopt direct powder compression, it may further comprise the steps:
(1) presses the mass percent of component in the palonosetron Hcl oral cavity disintegration tablet, take by weighing each component;
(2) with the palonosetron Hcl in the step (1), correctives, disintegrating agent respectively porphyrize cross 80 mesh sieves, then with its mix homogeneously, obtain mixture A;
(3) mannitol in the step (1) is crossed 40 mesh sieves, take by weighing respectively according to quantity, mix homogeneously obtains mixture B then;
(4) the mixture B in the step (3) is joined among the mixture A in the step (2) with the equivalent method of progressively increasing, fully mix, obtain mixture C;
(5) mixture C in step (4) adds lubricant, and the mixing that sieves carries out the intermediate content detection, determines the heavy back employing of sheet direct compression technology tabletting, promptly;
In prescription when being added with fluidizer and binding agent simultaneously, can fluidizer be added in step (5) with lubricant with binding agent with mannitol mistake 40 mesh sieves in step (3) man-hour adding.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009102303239A CN102048705B (en) | 2009-11-10 | 2009-11-10 | Palonosetron hydrochloride orally disintegrating tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009102303239A CN102048705B (en) | 2009-11-10 | 2009-11-10 | Palonosetron hydrochloride orally disintegrating tablet and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102048705A true CN102048705A (en) | 2011-05-11 |
| CN102048705B CN102048705B (en) | 2012-07-18 |
Family
ID=43953729
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009102303239A Active CN102048705B (en) | 2009-11-10 | 2009-11-10 | Palonosetron hydrochloride orally disintegrating tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102048705B (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102860989A (en) * | 2011-07-08 | 2013-01-09 | 广州医学院 | Two formulations of chiral drug R/S (+/-)-1-[4-(2-methoxyphenyl) piperazinyl]-3-(1-naphthyloxyl)-2-propanol optical isomer |
| CN103446072A (en) * | 2012-06-02 | 2013-12-18 | 正大天晴药业集团股份有限公司 | Palonosetron solid medicine composition |
| CN113069423A (en) * | 2020-01-04 | 2021-07-06 | 广东东阳光药业有限公司 | Baroswarriol orally disintegrating tablet and preparation method thereof |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100544720C (en) * | 2006-01-24 | 2009-09-30 | 江苏正大天晴药业股份有限公司 | The palonosetron compositions of safety and stability |
| CA2666512C (en) * | 2006-10-24 | 2014-05-27 | Helsinn Healthcare S.A. | Soft capsules comprising palonosetron hydrochloride having improved stability and bioavailability |
| CN101095679A (en) * | 2007-07-28 | 2008-01-02 | 南昌弘益科技有限公司 | Granisetron hydrochloride orally disintegrating tablets |
| CN101199851A (en) * | 2007-12-20 | 2008-06-18 | 江苏奥赛康药业有限公司 | Preparing method of lyophilized powder injection via high solid amount mannite accessory |
| US8133506B2 (en) * | 2008-03-12 | 2012-03-13 | Aptalis Pharmatech, Inc. | Drug delivery systems comprising weakly basic drugs and organic acids |
-
2009
- 2009-11-10 CN CN2009102303239A patent/CN102048705B/en active Active
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102860989A (en) * | 2011-07-08 | 2013-01-09 | 广州医学院 | Two formulations of chiral drug R/S (+/-)-1-[4-(2-methoxyphenyl) piperazinyl]-3-(1-naphthyloxyl)-2-propanol optical isomer |
| CN103446072A (en) * | 2012-06-02 | 2013-12-18 | 正大天晴药业集团股份有限公司 | Palonosetron solid medicine composition |
| CN107137374A (en) * | 2012-06-02 | 2017-09-08 | 正大天晴药业集团股份有限公司 | The solid composite medicament of palonosetron |
| CN107137374B (en) * | 2012-06-02 | 2020-04-07 | 正大天晴药业集团股份有限公司 | Solid pharmaceutical composition of palonosetron |
| CN113069423A (en) * | 2020-01-04 | 2021-07-06 | 广东东阳光药业有限公司 | Baroswarriol orally disintegrating tablet and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN102048705B (en) | 2012-07-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TW201815384A (en) | Tablets comprising 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde | |
| CN101904824B (en) | Olanzapine orally-disintegrating tablet preparation and preparation method thereof | |
| JP5366233B2 (en) | Orally disintegrating tablets | |
| US20160287518A1 (en) | Ulipristal acetate tablets | |
| JP2018058910A (en) | Orally disintegrating tablet, and production method of the same | |
| CN108653226A (en) | The daily single administration sustained release preparation of Mosapride of pharmacology and clinical effect is provided | |
| CN102387802A (en) | Immediate release pharmaceutical compositions comprising oxycodone and naloxone | |
| JP3996626B2 (en) | Orally disintegrating tablets | |
| CN104546770A (en) | Azilsartan orally-disintegrating tablet and preparation method thereof | |
| KR101562608B1 (en) | Compound chemical medicine acting on respiratory disease, preparation process and use thereof | |
| CN101461788B (en) | Phloroglucine orally disintegrating tablet and preparation method thereof | |
| CN102048705B (en) | Palonosetron hydrochloride orally disintegrating tablet and preparation method thereof | |
| JP3884056B1 (en) | Method for producing intraoral rapidly disintegrating tablet | |
| CN105476967A (en) | Blonanserin pharmaceutical composition and preparation method thereof | |
| JP2008127320A (en) | Solid preparation quickly disintegrating in oral cavity | |
| CN103720674B (en) | Famotidine floating-adhesive micro-tablet capsule and preparation method thereof | |
| CN102614140B (en) | Iloperidone oral cavity disintegration tablet and preparation method thereof | |
| CN100348180C (en) | Oral disintegration tablet of tramadol hydrochloride and preparation method | |
| CN101804036B (en) | Domperidone orally disintegrating tablet and preparation method thereof | |
| TW201532634A (en) | Solid preparation | |
| CN1311830C (en) | Cefadroxil oral disintegrant tablet, and its prepn. method | |
| US8741344B1 (en) | Dispersible tablet | |
| KR102635438B1 (en) | Solid formulation for bowel cleansing and manufacturing method thereof | |
| CN100490816C (en) | Azithromycin oral disintegration tablet and its preparing method | |
| JP6004882B2 (en) | Mannitol excipient for use in compression molding and tablets containing the same |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20201026 Address after: 570314 -A, Nanhai Avenue, national hi tech Development Zone, Hainan, Haikou, 273 Patentee after: QILU PHARMACEUTICAL (HAINAN) Co.,Ltd. Address before: 250100 No. 243 industrial North Road, Licheng District, Shandong, Ji'nan Patentee before: Qilu Pharmaceutical Co.,Ltd. |
|
| TR01 | Transfer of patent right |