CN101601660A - A kind of chloride pyrrole Gray's soluble tablet - Google Patents
A kind of chloride pyrrole Gray's soluble tablet Download PDFInfo
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- CN101601660A CN101601660A CNA2009101081062A CN200910108106A CN101601660A CN 101601660 A CN101601660 A CN 101601660A CN A2009101081062 A CNA2009101081062 A CN A2009101081062A CN 200910108106 A CN200910108106 A CN 200910108106A CN 101601660 A CN101601660 A CN 101601660A
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- soluble tablet
- clopidogrel
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- soluble
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Abstract
The invention discloses soluble tablet of a kind of clopidogrel and preparation method thereof.This soluble tablet contains active component clopidogrel or its pharmaceutically acceptable salt and pharmaceutic adjuvant, and described pharmaceutic adjuvant comprises the solubility adjuvant.By weight percentage, the ratio of clopidogrel and solubility adjuvant is 1: 1-10.Can contain disintegrating agent and lubricant in addition.Clopidogrel soluble tablet preparation method can be direct compression process or wet granule compression tablet method.Compare with conventional tablet, it is fast that the present invention has a disintegrate, can form the advantage of solution state within the short time in water, and be easy to store and use, and especially makes things convenient for patient's medication of dysphagia, improved compliance of patients greatly.
Description
Technical field
The present invention relates to a kind of medicine that is used for cardiovascular and cerebrovascular disease, be specifically related to soluble tablet of a kind of chloride pyrrole Gray and preparation method thereof.
Background technology
Along with social senilization and growth in the living standard, the sickness rate and the case fatality rate of cardiovascular and cerebrovascular disease rise day by day.Studies show that according to nearest one, comprise that in 8 major areas, the whole world investigation of both developed and developing country shows that ischemic heart desease and cerebrovascular disease have become the main cause of death.As in the U.S., cardiovascular disease far surpasses cancer, accounts for 42% of whole death, becomes underlying cause of death.In China, cardiovascular and cerebrovascular disease also becomes one of old people's common frdquently encountered disease, cerebrovascular disease especially, and prevalence is up to 491.8/10 ten thousand people, apparently higher than western countries.
Clopidogrel chemistry (+)-(S)-alpha-(2-chlorphenyl)-6 by name, the 7-dihydro-thiophene is [3,2-c] pyridines-5 (4H) methyl acetate also, dissolves in water, methanol, ethanol or glacial acetic acid, is a kind of novel anticoagulant.ATC is categorized as: B01AC/04.The clopidogrel selectivity also suppresses adenosine diphosphate (ADP) (ADP) and its combining and the activation of the glycoprotein GP111b/111a complex of the ADP of secondary mediation of platelet receptor, but so anticoagulant, clopidogrel must could suppress hematoblastic gathering through biotransformation, but does not also isolate the active metabolite that produces this effect.Except that ADP, clopidogrel can also suppress the platelet aggregation of other agonist induction by blocking the amplification of the platelet activation that is caused by the ADP that discharges.Clopidogrel can not suppress the activity of phosphodiesterase.Clopidogrel works by irreversibly modifying platelet ADP receptor.The hematoblastic life-span that is exposed to clopidogrel is affected.And the regeneration rate of platelet normal function is relevant with hematoblastic renewal.
Clopidogrel is mainly used in restenosis and thrombotic complications etc. in treatment atheromatosis, dosage form coronary syndrome, the prevention intracoronary stent implantation after-poppet clinically.
Fuse is meant the non-coated tablet or the thin membrane coated tablet that can be dissolved in water.Fuse can be in water utmost point disintegrate and dissolve and form clarification or slightly opalescent solution state rapidly in the short time.Compare with other tablet types, fuse is with after water contacts, because the rapid dissolving of efficient water soluble adjuvant, medicine can be by effective wetting, thereby is dissolved in the water fast.In addition, owing to be with the administration of true solution state, patient takes the back medicine can be absorbed onset more fast.Fuse absorbs the rapid-action advantage except having liquid preparation, also have solid preparation and easily preserve, easily the advantage of transportation and good stability only needs tablet is soluble in water when patient uses, be more convenient for the patient of dysphagia to use, improved compliance of patients greatly.
The clopidogrel dosage form of using clinically still is mainly conventional tablet at present, do not see the relevant report that soluble tablet is arranged, and conventional tablet may exist the disintegrate stripping slow, and onset is slow, the problem that bioavailability is low.In view of the fuse dosage form has the advantages that above-mentioned plurality of advantages and clopidogrel are used for the cardiovascular and cerebrovascular disease patient more, a kind of chloride pyrrole Gray's of expectation research soluble tablet, reach and improve the clopidogrel oral administration biaavailability, more give full play to purposes such as drug effect and raising patient compliance.
Summary of the invention
The purpose of this invention is to provide and a kind of chloride pyrrole Gray's soluble tablet, solve the existing problem that preparation disintegrate stripping is slow, onset is slow, bioavailability is low.More give full play to drug effect and improve patient compliance.
In the process of preparation fuse, how to make tablet form the key issue that solution state is the needs solution in the short time with the utmost point after water contact.The present invention is pressed into tablet after using efficient water soluble adjuvant and super-disintegrant and medicine to make up in the proper ratio, solved this problem well.
The technical solution adopted for the present invention to solve the technical problems is: a kind of chloride pyrrole Gray's soluble tablet, contain active component clopidogrel or its pharmaceutically acceptable salt and pharmaceutic adjuvant, and described pharmaceutic adjuvant comprises the solubility adjuvant; It is characterized in that: described solubility adjuvant is selected from one or more mixture of soluble starch, lactose, sucrose, xylitol, sorbitol, maltose alcohol and mannitol, clopidogrel and solubility adjuvant count 1 by heavy percentage ratio: 1-10, preferred 1: 3-6.
In order to make tablet form fine particle quickly and to be dissolved in the water, described pharmaceutic adjuvant also contains disintegrating agent, it is 1-20% that disintegrating agent accounts for the soluble tablet total weight percent, is selected from one or more mixture of polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, crosslinked carboxymethyl fecula sodium and cross-linking sodium carboxymethyl cellulose.Disintegrating agent accounts for the soluble tablet total weight percent and is preferably 2-8%,
In order to satisfy the tabletting requirement, described pharmaceutic adjuvant also contains lubricant, and it is 1-20% that described lubricant accounts for the soluble tablet total weight percent; Described lubricant is selected from one or more mixture of Polyethylene Glycol (4000,6000), sodium chloride, adipic acid, leucine, enuatrol and boric acid.Lubricant accounts for the soluble tablet total weight percent and is preferably 2-8%.
The preparation method of clopidogrel fuse can be direct compression process and wet granule compression tablet method.
1. direct compression process: respectively principal agent and all adjuvants were pulverized more than 100 mesh sieves, then with direct compression behind principal agent and the abundant mix homogeneously of all adjuvants.
2. wet granule compression tablet method: respectively principal agent and all adjuvants were pulverized more than 100 mesh sieves, and, added binding agent system soft material, and granulated, drying, granulate, tabletting behind the adding lubricant mixing then with medicine and solubility adjuvant and disintegrating agent mix homogeneously.
Preparation dissolution test investigation method and conclusion:
Disintegration and dissolution velocity are to estimate the key index of soluble tablet, according to fuse inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2005) soluble tablet of preparation are checked.Concrete grammar is as follows:
Check according to the described apparatus and method of inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2005), each sheet should be in 3 minutes disintegrate and dissolving.
(after influence factors such as 4000 ± 500Lx) test, appearance character, pH value, content, related substance and sterility test are all up to specification through high temperature (60 ℃), high humidity (RH92.5%, RH75%, 25 ℃) and illumination for product of the present invention.
Product of the present invention through accelerated test (40 ℃, RH75%) 6 months investigation result, appearance character, pH value, content, related substance and sterility test are all up to specification.
Beneficial effect of the present invention: the present invention is owing to rationally select pharmaceutic adjuvant and component ratio for use, this soluble tablet is than conventional tablet, can be in water disintegrate and dissolve the formation solution state rapidly in several minutes, help the rapid release and the onset rapidly of medicine, soluble tablet conveniently stores and carries in addition, has possessed the characteristics of liquid preparation and solid preparation simultaneously.Owing to the solution state administration, especially made things convenient for the cardiovascular patient of swallowing inconvenience, improved compliance of patients greatly.And the production of this soluble tablet do not need special equipment and material, do not need to increase extra production cost.
Below with reference to embodiment, the present invention is carried out comparatively detailed explanation.
The specific embodiment
The preparation of embodiment 1 chloride pyrrole Gray's soluble tablet
Amounts of components (g)
Bisulfate clopidogrel 100
Mannitol 100
Crosslinked carboxymethyl fecula sodium 11.0
Polyethylene glycol 6000 9.0
Make 1000
Preparation method: bisulfate clopidogrel, mannitol, crosslinked carboxymethyl fecula sodium are crossed 100 mesh sieves respectively, then all components is placed fully mix homogeneously of mixer, direct compression promptly.
The every index of gained sheet all meets the pharmacopeia regulation, and by aforementioned inspection method, disintegration is qualified, and disintegrate and the time of dissolving are 146 seconds.
The preparation of embodiment 2 chloride pyrrole Grays' soluble tablet
Amounts of components (g)
Bisulfate clopidogrel 100
Lactose 1000
Cross-linking sodium carboxymethyl cellulose 25.0
Sodium chloride 15.0
Make 1000
Preparation method: bisulfate clopidogrel, lactose, low-substituted hydroxypropyl cellulose are crossed 100 mesh sieves respectively, to place fully mixing of mixer then, make the moderate soft material of hardness with 5% lactose aqueous solution, 24 mesh sieves are granulated, 40-45 ℃ of oven dry, the arrangement of 20 mesh sieves counts the sodium chloride mixing, and tabletting promptly.
The every index of gained sheet all meets pharmacopeia regulation, by aforementioned inspection method, and disintegrate and to dissolve the time limit qualified, disintegration time 113 seconds.
The preparation of embodiment 3 chloride pyrrole Grays' soluble tablet
Amounts of components (g)
Bisulfate clopidogrel 100
Mannitol 200
Low-substituted hydroxypropyl cellulose 15.0
Sodium chloride 5.0
Polyethylene glycol 6000 10.0
Make 1000
Preparation method: bisulfate clopidogrel, mannitol, low-substituted hydroxypropyl cellulose are crossed 100 sieves respectively, then all components is placed fully mix homogeneously of mixer, adjustment sheet is heavy, and direct compression promptly.
The every index of gained sheet all meets pharmacopeia regulation, by aforementioned inspection method, and disintegrate and to dissolve the time limit qualified, disintegration time 91 seconds.
Claims (6)
1, a kind of chloride pyrrole Gray's soluble tablet contains active component clopidogrel or its pharmaceutically acceptable salt and pharmaceutic adjuvant, and described pharmaceutic adjuvant comprises the solubility adjuvant; It is characterized in that: described solubility adjuvant is selected from one or more mixture of soluble starch, lactose, sucrose, xylitol, sorbitol, maltose alcohol and mannitol, and described clopidogrel and solubility adjuvant count 1 by heavy percentage ratio: 1-10.
2, chloride pyrrole Gray's as claimed in claim 1 soluble tablet is characterized in that: described clopidogrel and solubility adjuvant are by heavy percentage ratio 1: 3-6.
3, chloride pyrrole Gray's as claimed in claim 1 or 2 soluble tablet, it is characterized in that: described pharmaceutic adjuvant also contains disintegrating agent, it is 1-20% that disintegrating agent accounts for the soluble tablet total weight percent, is selected from one or more mixture of polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, crosslinked carboxymethyl fecula sodium and cross-linking sodium carboxymethyl cellulose.
4, chloride pyrrole Gray's as claimed in claim 3 soluble tablet is characterized in that: it is 2-8% that described disintegrating agent accounts for the soluble tablet total weight percent.
5, chloride pyrrole Gray's as claimed in claim 3 soluble tablet is characterized in that: described pharmaceutic adjuvant also contains lubricant, and it is 1-20% that lubricant accounts for the soluble tablet total weight percent; Described lubricant is selected from one or more mixture of Polyethylene Glycol (4000,6000), sodium chloride, adipic acid, leucine, enuatrol and boric acid.
6, chloride pyrrole Gray's as claimed in claim 5 soluble tablet is characterized in that: it is 2-8% that described lubricant accounts for the soluble tablet total weight percent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2009101081062A CN101601660A (en) | 2009-06-30 | 2009-06-30 | A kind of chloride pyrrole Gray's soluble tablet |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2009101081062A CN101601660A (en) | 2009-06-30 | 2009-06-30 | A kind of chloride pyrrole Gray's soluble tablet |
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| CNA2009101081062A Pending CN101601660A (en) | 2009-06-30 | 2009-06-30 | A kind of chloride pyrrole Gray's soluble tablet |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103181885A (en) * | 2011-12-30 | 2013-07-03 | 北京韩美药品有限公司 | Clopidogrel solid preparation and preparation method thereof |
| CN103284972A (en) * | 2013-06-28 | 2013-09-11 | 门毅 | Prescription of clopidogrel bisulfate tablet and preparation process thereof |
| CN104688694A (en) * | 2013-12-04 | 2015-06-10 | 长春海悦药业有限公司 | Pharmaceutical composition containing clopidogrel hydrogen sulfate |
-
2009
- 2009-06-30 CN CNA2009101081062A patent/CN101601660A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103181885A (en) * | 2011-12-30 | 2013-07-03 | 北京韩美药品有限公司 | Clopidogrel solid preparation and preparation method thereof |
| CN103284972A (en) * | 2013-06-28 | 2013-09-11 | 门毅 | Prescription of clopidogrel bisulfate tablet and preparation process thereof |
| CN104688694A (en) * | 2013-12-04 | 2015-06-10 | 长春海悦药业有限公司 | Pharmaceutical composition containing clopidogrel hydrogen sulfate |
| CN104688694B (en) * | 2013-12-04 | 2018-09-11 | 长春海悦药业股份有限公司 | A kind of pharmaceutical composition containing bisulfate clopidogrel |
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Application publication date: 20091216 |