CN101219120B - Telmisartan dispersible tablet and method for preparing the same - Google Patents
Telmisartan dispersible tablet and method for preparing the same Download PDFInfo
- Publication number
- CN101219120B CN101219120B CN2007101734318A CN200710173431A CN101219120B CN 101219120 B CN101219120 B CN 101219120B CN 2007101734318 A CN2007101734318 A CN 2007101734318A CN 200710173431 A CN200710173431 A CN 200710173431A CN 101219120 B CN101219120 B CN 101219120B
- Authority
- CN
- China
- Prior art keywords
- telmisartan
- granules
- preparation
- dispersible tablet
- excipient
- 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.)
- Active
Links
- RMMXLENWKUUMAY-UHFFFAOYSA-N telmisartan Chemical compound CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O RMMXLENWKUUMAY-UHFFFAOYSA-N 0.000 title claims abstract description 116
- 239000005537 C09CA07 - Telmisartan Substances 0.000 title claims abstract description 58
- 229960005187 telmisartan Drugs 0.000 title claims abstract description 58
- 239000007919 dispersible tablet Substances 0.000 title claims abstract description 19
- 238000000034 method Methods 0.000 title description 3
- 239000008187 granular material Substances 0.000 claims abstract description 40
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical group [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims abstract description 39
- 238000002360 preparation method Methods 0.000 claims abstract description 25
- 239000003814 drug Substances 0.000 claims abstract description 24
- 229940079593 drug Drugs 0.000 claims abstract description 18
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 16
- 239000000314 lubricant Substances 0.000 claims abstract description 15
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 14
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims abstract description 13
- 239000000945 filler Substances 0.000 claims abstract description 13
- 229960003194 meglumine Drugs 0.000 claims abstract description 13
- 239000006184 cosolvent Substances 0.000 claims abstract description 10
- 239000002904 solvent Substances 0.000 claims abstract description 7
- 239000000706 filtrate Substances 0.000 claims abstract description 5
- 239000003995 emulsifying agent Substances 0.000 claims abstract description 4
- 239000004094 surface-active agent Substances 0.000 claims abstract description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 28
- 239000000203 mixture Substances 0.000 claims description 18
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 16
- 239000000600 sorbitol Substances 0.000 claims description 16
- 235000019359 magnesium stearate Nutrition 0.000 claims description 14
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 11
- 239000011734 sodium Substances 0.000 claims description 11
- 229910052708 sodium Inorganic materials 0.000 claims description 11
- 239000011230 binding agent Substances 0.000 claims description 10
- 239000000047 product Substances 0.000 claims description 8
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 7
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 7
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 7
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 7
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 7
- 239000000741 silica gel Substances 0.000 claims description 7
- 229910002027 silica gel Inorganic materials 0.000 claims description 7
- 238000005303 weighing Methods 0.000 claims description 7
- 239000002671 adjuvant Substances 0.000 claims description 5
- 230000001476 alcoholic effect Effects 0.000 claims description 5
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 4
- 229920002472 Starch Polymers 0.000 claims description 4
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 4
- 239000002994 raw material Substances 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- 235000019698 starch Nutrition 0.000 claims description 4
- 206010013786 Dry skin Diseases 0.000 claims description 3
- 239000002253 acid Substances 0.000 claims description 3
- 238000001035 drying Methods 0.000 claims description 3
- 238000002156 mixing Methods 0.000 claims description 3
- 239000007779 soft material Substances 0.000 claims description 3
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000000463 material Substances 0.000 abstract description 7
- 239000003826 tablet Substances 0.000 abstract description 4
- 230000009286 beneficial effect Effects 0.000 abstract description 3
- 238000004090 dissolution Methods 0.000 abstract description 3
- 230000007774 longterm Effects 0.000 abstract description 2
- 239000007767 bonding agent Substances 0.000 abstract 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 abstract 2
- 229940083608 sodium hydroxide Drugs 0.000 description 10
- 239000000243 solution Substances 0.000 description 8
- 239000002245 particle Substances 0.000 description 4
- 102000005862 Angiotensin II Human genes 0.000 description 3
- 101800000733 Angiotensin-2 Proteins 0.000 description 3
- CZGUSIXMZVURDU-JZXHSEFVSA-N Ile(5)-angiotensin II Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C([O-])=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@@H]([NH3+])CC([O-])=O)C(C)C)C1=CC=C(O)C=C1 CZGUSIXMZVURDU-JZXHSEFVSA-N 0.000 description 3
- 229950006323 angiotensin ii Drugs 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- 206010020772 Hypertension Diseases 0.000 description 2
- 239000000853 adhesive Substances 0.000 description 2
- 230000001070 adhesive effect Effects 0.000 description 2
- -1 copolyvidone Chemical compound 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 239000011159 matrix material Substances 0.000 description 2
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 2
- 239000011265 semifinished product Substances 0.000 description 2
- 235000015424 sodium Nutrition 0.000 description 2
- 229960002920 sorbitol Drugs 0.000 description 2
- PFNFFQXMRSDOHW-UHFFFAOYSA-N spermine Chemical compound NCCCNCCCCNCCCN PFNFFQXMRSDOHW-UHFFFAOYSA-N 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 238000001694 spray drying Methods 0.000 description 2
- 238000005507 spraying Methods 0.000 description 2
- 101150059573 AGTR1 gene Proteins 0.000 description 1
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 description 1
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 description 1
- 108050000824 Angiotensin II receptor Proteins 0.000 description 1
- 102000008873 Angiotensin II receptor Human genes 0.000 description 1
- 101800004538 Bradykinin Proteins 0.000 description 1
- 102400000967 Bradykinin Human genes 0.000 description 1
- 102000004310 Ion Channels Human genes 0.000 description 1
- 102000016979 Other receptors Human genes 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- 206010047139 Vasoconstriction Diseases 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 210000004100 adrenal gland Anatomy 0.000 description 1
- 229960002478 aldosterone Drugs 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000007888 film coating Substances 0.000 description 1
- 238000009501 film coating Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 108091008039 hormone receptors Proteins 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 231100000053 low toxicity Toxicity 0.000 description 1
- 210000002464 muscle smooth vascular Anatomy 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 239000011236 particulate material Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000003248 secreting effect Effects 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 229940063675 spermine Drugs 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
- 239000003232 water-soluble binding agent Substances 0.000 description 1
Abstract
The invention discloses a telmisartan dispersible tablet and a preparation method thereof. The Telmisartan dispersible tablet comprises a telmisartan, an excipient, a cosolvent, a filling agent, a disintegrating agent; a bonding agent, a lubricant and a fluidizer, wherein, the fluidizer is sodium hydroxide and meglumine and the excipient is polyvidone; surfactant and emulsifier are excluded in the telmisartan dispersible tablet. The preparation method is that: the telmisartan and auxiliary materials are screened; the telmisartan, the cosolvent, and the excipient are added into a solvent in sequence to be dissolved; then the filtrate is spray-dried to obtain principal telmisartan granules; part of the filling agent, part of the lubricant and disintegrating agent are well mixed in sequence and then added with the bonding agent, and then palletized to obtain the auxiliary material granules; other auxiliary materials are added into the principal telmisartan granules and the auxiliary material granules and well mixed, and finally planished tablet. The invention has the advantages that: the tablet prepared from the telmisartan and the auxiliary materials is quick in disintegration, complete in dissolution, stable in quality, and suitable for long-term storage, and can improve the bioavailability of drug to human body; that the polyvidone is adopted as excipient as well as bonding agent reduces the auxiliary materials thus being beneficial to the stability of the preparation.
Description
Technical field
The invention belongs to field of medicaments, relate to a kind of medicine and preparation method thereof, especially a kind of telmisartan sheet and preparation method thereof.
Background technology
Telmisartan is a kind of non-peptide class angiotensin-ii receptor inhibitor of long-acting, efficient, low toxicity, with the affinity rate of AT1 receptor be AT
2More than 3000 times of receptor.Do not influence reaction, do not combine or produce blocking effect with other hormone receptor and ion channel to Kallidin I.It optionally blocks the AT in Angiotensin II and the many tissues (as vascular smooth muscle and adrenal gland)
1Receptors bind, thereby the blocking-up vasoconstriction of Angiotensin II and the secretory action of aldosterone, and disobey anti-synthetic path in Angiotensin II effectively bring high blood pressure down, but do not influence cardiovascular other receptor systems in regulating.Telmisartan is one of hypertension treatment medicine of latest generation, and application prospect is boundless.
Patent No. ZL03822605.7 discloses a kind of telmisartan pharmaceutical composition, telmisartan is dispersed in the dissolved matrix, and this dissolved matrix comprises alkaline reagent, as sodium hydroxide, sodium bicarbonate, spermine acid, meglumine etc., also comprises surfactant or emulsifying agent in addition.
Number of patent application 200510049339.1 discloses a kind of telmisartan dispersible tablet, points out that wherein disintegrating agent is polyvinylpolypyrrolidone, crospolyvinylpyrrolidone etc.
Summary of the invention
Technical problem to be solved by this invention is to provide a kind of telmisartan dispersible tablet and preparation method thereof, and the disintegration rate of dispersible tablet is fast, and stripping is complete.
The present invention solves the problems of the technologies described above the technical scheme that is adopted: a kind of telmisartan dispersible tablet, its component comprises: telmisartan, excipient, cosolvent, filler, disintegrating agent, binding agent, lubricant and fluidizer, wherein, described cosolvent is sodium hydroxide and meglumine, described excipient is a copolyvidone, and does not contain surfactant or emulsifying agent.
Copolyvidone is different from polyvinylpolypyrrolidone or crospolyvinylpyrrolidone, is applied to mainly as water-soluble binder and dry adhesive granulate and pressed-disc technique, or is used for film coating as filmogen, forms thing as the duct and is applied in the mask agent.The present invention uses copolyvidone as excipient, and the spraying granule density that makes increases, and adds tabletting behind filler, the lubricant, can be easy to reach that sheet is important asks.And use polyvinylpyrrolidone K30 to make excipient, and the spraying granule that makes is too loose, and the tabletting rear panel heavily is difficult to not reach the preparation requirement.
On the basis of such scheme, telmisartan dispersible tablet, each compositions in weight percentage % counts:
Telmisartan 8～22%
Sodium hydroxide and meglumine 1～12%
Copolyvidone 10～25%
Filler 45～65%
Disintegrating agent 3～8%
Binding agent 1～5%
Lubricant 1～5%
Fluidizer 0～5%.
Described filler, or diluent is in sorbitol, the microcrystalline Cellulose one or more.Described disintegrating agent is a carboxymethyl starch sodium, preferred super carboxymethyl starch sodium, it is a kind of of carboxymethylstach sodium, but super carboxymethyl starch sodium is drawing wet, expansion, is being better than common carboxymethylstach sodium aspect mobile, it has also overcome general adhesive " bag is sticking " effect to effective ingredient, promote drug dissolution, improved human body greatly bioavailability of medicament.
Described binding agent is a copolyvidone.Excipient and binding agent all adopt copolyvidone among the present invention, can reduce the kind of used adjuvant in the preparation, meet the few more good more principle of the supplementary product kind that uses under the situation that satisfies the preparation requirement.Used supplementary product kind is few more in the preparation, and the probability of principal agent generation related substance can be more little, more helps stability of formulation.
Described lubricant is a magnesium stearate, and described fluidizer is micropowder silica gel.
Preparation method at above-mentioned telmisartan dispersible tablet comprises the steps:
(1) take by weighing raw material by prescription, telmisartan and adjuvant are crossed 100 mesh sieves respectively;
A, granules of main drug preparation:
Telmisartan, cosolvent, excipient added in the solvent successively dissolve, 100 orders filter, and filtrate is spray-dried, granules of main drug;
B, granules of accessories preparation:
With partially filled dose, part lubricant, disintegrating agent mix homogeneously successively, add binding agent and make soft material, granulate, 50～60 ℃ of dryings, granulate, granules of accessories;
(2) remainder filler, remainder lubricant, fluidizer are added in granules of main drug, the granules of accessories mix homogeneously;
(3) tabletting is made finished product.
Another preparation method at above-mentioned telmisartan dispersible tablet comprises the steps:
(1) take by weighing raw material by prescription, telmisartan and adjuvant are crossed 100 mesh sieves respectively;
(2) telmisartan, cosolvent, excipient are added in the solvent successively dissolve, 100 orders filter, and filtrate is spray-dried, granules of main drug;
(3) with after filler, lubricant, the fluidizer mixing, with the granules of main drug mix homogeneously;
(4) tabletting is made finished product.
Described solvent is alcoholic acid aqueous solution.
Second kind of preparation method of telmisartan sheet is easy than first kind of preparation method of telmisartan sheet, but that first method prepares mobility of particle is better, and the slice, thin piece tablet weight variation is littler.
The invention has the beneficial effects as follows:
The present invention adds the tablet that appropriate amount of auxiliary materials is made with the telmisartan sheet, and it is shorter to have disintegration time, and the medicine stripping is complete, steady quality, be fit to long term storage, through check, indexs such as its content, character, discriminating, stripping, content uniformity all meet " Chinese pharmacopoeia and pertinent regulations; Adopt super sodium carboxymethyl cellulose as disintegrating agent, promote drug dissolution, improved human body greatly bioavailability of medicament; Adopt copolyvidone not only as excipient but also as binding agent, reduce supplementary product kind, be beneficial to preparation stabilization.
The specific embodiment
Embodiment 1
1000 telmisartan sheets (specification 40mg) contain following component:
Telmisartan 40g 17.7%
Sodium hydroxide 5g 2.2%
Meglumine 15g 6.6%
Copolyvidone 30g 13.3%
Sorbitol mixture granule 87g 38.5%
Microcrystalline Cellulose 43g 19.0%
Magnesium stearate 3g 1.35%
Micropowder silica gel 3g 1.35%
Wherein, sorbitol mixture granule prescription (accounting for total prescription percentage ratio %):
Sorbitol 67g 29.65%
Magnesium stearate 3g 1.35%
Super carboxymethylstach sodium 13g 5.75%
Copolyvidone 4g 1.75%.
The telmisartan sheet is prepared from through the following steps:
(1) takes by weighing telmisartan, copolyvidone, meglumine, sodium hydroxide, sorbitol, carboxymethylstach sodium, microcrystalline Cellulose, magnesium stearate, micropowder silica gel by prescription, cross 100 mesh sieves respectively.
A, granules of main drug preparation:
Sodium hydroxide, meglumine, telmisartan, copolyvidone are joined in the 95% an amount of alcoholic solution successively, make it to dissolve fully, behind the mixing, 100 eye mesh screens filter, filtering solution is got solid particle after the spray drying in spray dryer, be granules of main drug.
B, with behind sorbitol, magnesium stearate, the carboxymethylstach sodium mix homogeneously successively, the alcoholic solution that adds 15% copolyvidone while stirring is made uniform soft material, granulates with 30 mesh sieves, 50～60 ℃ of dryings, 30 mesh sieve granulate get the sorbitol mixture granule, are granules of accessories.
(2) will join by microcrystalline Cellulose, magnesium stearate, the micropowder silica gel that prescription takes by weighing in the above-mentioned granules of main drug and granules of accessories that obtains,, promptly get semi-finished product the particulate material mix homogeneously;
(3) after the inspection of semifinished product, tabletting, plastic-aluminum, packing get product, and make 10,000 telmisartan sheets (specification 40mg) altogether.
Embodiment 2
1000 telmisartan sheets (specification 40mg) contain following component:
Telmisartan 40g 17.4%
Sodium hydroxide 5g 2.2%
Meglumine 15g 6.5%
Copolyvidone 30g 13.0%
Sorbitol 134g 58.3%
Magnesium stearate 6g 2.6%.
The telmisartan sheet is prepared from through the following steps:
(1) takes by weighing telmisartan, copolyvidone, meglumine, sodium hydroxide, sorbitol, carboxymethylstach sodium, microcrystalline Cellulose, magnesium stearate, micropowder silica gel by prescription, cross 80 mesh sieves respectively;
(2) with sodium hydroxide, meglumine and telmisartan, be dissolved in 95% alcoholic solution, get solution I, in solution I, add the copolyvidone of recipe quantity, get solution II after the dissolving, solution II is got solid particle after the spray drying in spray dryer, be granules of main drug;
(3) with sorbitol and the solid particle mix homogeneously that obtains, add magnesium stearate, mix homogeneously;
(4) measure the drug content stator and weigh, with the shallow arc stamping of 9mm (specification 230mg).
Embodiment 3
1000 telmisartan sheets (specification 80mg) contain following component:
Telmisartan 80g 18.6%
Sodium hydroxide 10g 2.3%
Meglumine 30g 7.0%
Copolyvidone 60g 14.0%
Sorbitol mixture granule 150g 34.9%
Microcrystalline Cellulose 90g 20.9%
Magnesium stearate 5g 1.15%
Micropowder silica gel 5g 1.15%.
Wherein, sorbitol mixture granule prescription (accounting for total prescription percentage ratio %):
Sorbitol 115g 26.75%
Magnesium stearate 5g 1.2%
Super carboxymethylstach sodium 23g 5.35%
Copolyvidone 7g 1.6%
The telmisartan piece preparation method is with embodiment 1.
Claims (7)
1. telmisartan dispersible tablet, comprise: telmisartan, excipient, cosolvent, filler, disintegrating agent, binding agent, lubricant and fluidizer, it is characterized in that: described cosolvent is sodium hydroxide and meglumine, described excipient is a copolyvidone, and do not contain surfactant or emulsifying agent, each compositions in weight percentage % counts:
Telmisartan 8～22%
Sodium hydroxide and meglumine 1～12%
Copolyvidone 10～25%
Filler 45～65%
Disintegrating agent 3～8%
Binding agent 1～5%
Lubricant 1～5%
Fluidizer 0～5%,
Wherein, described filler is a kind of or its combination in sorbitol, the microcrystalline Cellulose, and described lubricant is a magnesium stearate.
2. telmisartan dispersible tablet according to claim 1 is characterized in that: described disintegrating agent is super carboxymethyl starch sodium.
3. telmisartan dispersible tablet according to claim 1 is characterized in that: described binding agent is a copolyvidone.
4. telmisartan dispersible tablet according to claim 1 is characterized in that: described fluidizer is micropowder silica gel.
5. at the preparation method of the described telmisartan dispersible tablet of claim 1, comprise the steps:
(1) take by weighing raw material by prescription, telmisartan and adjuvant sieve respectively;
A, granules of main drug preparation:
Telmisartan, cosolvent, excipient added in the solvent successively dissolve, filter, filtrate is spray-dried, granules of main drug;
B, granules of accessories preparation:
With partially filled dose of sorbitol, part magnesium stearate lubricant, disintegrating agent mix homogeneously successively, add binding agent and make soft material, granulate, 50～60 ℃ of dryings, granulate gets granules of accessories;
(2) remainder filler, remainder lubricant, fluidizer are added in granules of main drug, the granules of accessories mix homogeneously;
(3) tabletting is made finished product.
6. at the preparation method of the described telmisartan dispersible tablet of claim 1, comprise the steps:
(1) take by weighing raw material by prescription, telmisartan and adjuvant sieve respectively;
(2) telmisartan, cosolvent, excipient are added in the solvent successively dissolve, filter, filtrate is spray-dried, granules of main drug;
(3) with after filler sorbitol, magnesium stearate lubricant, the fluidizer mixing, with the granules of main drug mix homogeneously;
(4) tabletting is made finished product.
7. according to the preparation method of claim 5 or 6 described telmisartan dispersible tablets, it is characterized in that: described solvent is alcoholic acid aqueous solution.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2007101734318A CN101219120B (en) | 2007-12-27 | 2007-12-27 | Telmisartan dispersible tablet and method for preparing the same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2007101734318A CN101219120B (en) | 2007-12-27 | 2007-12-27 | Telmisartan dispersible tablet and method for preparing the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101219120A CN101219120A (en) | 2008-07-16 |
| CN101219120B true CN101219120B (en) | 2011-02-23 |
Family
ID=39629395
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007101734318A Active CN101219120B (en) | 2007-12-27 | 2007-12-27 | Telmisartan dispersible tablet and method for preparing the same |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101219120B (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101897676B (en) * | 2010-07-27 | 2011-12-14 | 北京京丰制药有限公司 | Telmisartan tablet composition |
| CN102532033A (en) * | 2012-02-29 | 2012-07-04 | 江西杏林白马药业有限公司 | Telmisartan salifying process |
| CN103520125B (en) * | 2013-09-28 | 2019-03-05 | 威海迪素制药有限公司 | A kind of telmisartan composition |
| CN104644575B (en) * | 2013-11-21 | 2017-11-28 | 成都苑东生物制药股份有限公司 | A kind of roflumilast dispersible tablet composition and preparation method thereof |
| CN107115305A (en) * | 2017-04-12 | 2017-09-01 | 宁波双伟制药有限公司 | Amoxicillin oral disnitegration tablet and preparation method thereof |
| CN107095844A (en) * | 2017-04-24 | 2017-08-29 | 江苏亚邦爱普森药业有限公司 | A kind of Pharmaceutical composition for being used to prepare slightly soluble oral medicine preparation |
| CN107982232A (en) * | 2018-01-29 | 2018-05-04 | 威特(湖南)药业有限公司 | Telmisartan Tablets and preparation method thereof |
| CN111265488B (en) * | 2020-03-18 | 2021-11-12 | 重庆康刻尔制药股份有限公司 | Telmisartan tablets and preparation method thereof |
| CN114392241B (en) * | 2022-01-10 | 2023-07-25 | 安徽贝克生物制药有限公司 | Ripide Wei Linpian and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1799543A (en) * | 2005-03-11 | 2006-07-12 | 浙江泰利森药业有限公司 | Telmisartan dispersible tablet and its preparation method |
| CN101052380A (en) * | 2004-10-12 | 2007-10-10 | 贝林格尔·英格海姆国际有限公司 | Bilayer tablet |
| CN101313905A (en) * | 2007-05-29 | 2008-12-03 | 上海信谊嘉华药业有限公司 | Composition containing telmisartan and preparing method thereof |
-
2007
- 2007-12-27 CN CN2007101734318A patent/CN101219120B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101052380A (en) * | 2004-10-12 | 2007-10-10 | 贝林格尔·英格海姆国际有限公司 | Bilayer tablet |
| CN1799543A (en) * | 2005-03-11 | 2006-07-12 | 浙江泰利森药业有限公司 | Telmisartan dispersible tablet and its preparation method |
| CN101313905A (en) * | 2007-05-29 | 2008-12-03 | 上海信谊嘉华药业有限公司 | Composition containing telmisartan and preparing method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN101219120A (en) | 2008-07-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101219120B (en) | Telmisartan dispersible tablet and method for preparing the same | |
| EP2136793B1 (en) | Tablet formulations containing 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one salts and tablets made therefrom | |
| CA2159419C (en) | Solid pharmaceutical composition comprising an excipient capable of binding water | |
| CN105832723B (en) | A kind of Ezetimibe atorvastatin and preparation method thereof | |
| JP2023026623A5 (en) | ||
| CN102258492B (en) | Neostigmine bromide slow release preparation and its preparation method | |
| CN109875972B (en) | Olmesartan medoxomil and amlodipine pharmaceutical composition | |
| EP1994926B9 (en) | Valsartan formulations | |
| CN103520169B (en) | Mirtazapine tablet and preparation method thereof | |
| JPH0774153B2 (en) | Loxoprofen / sodium-containing preparation | |
| CN102764254B (en) | A kind of levetiracetam medicinal composition and preparation method thereof | |
| CN100540008C (en) | Postpone Peroral solid dosage form for contraception or dissolved dosage form of termination of pregnancy medicine and application thereof | |
| PL205739B1 (en) | Matrix film tablets for the controlled release of natural mixtures of conjugated estrogen | |
| JP5662150B2 (en) | Tamsulosin hydrochloride sustained-release tablet and method for producing the same | |
| CN102247367A (en) | Pharmaceutical composition containing telmisartan and amlodipine and preparation method thereof | |
| WO2010057449A2 (en) | A solid pharmaceutical composition with atorvastatin and telmisartan as the active substances | |
| CN103181905B (en) | A kind of technique preparing pramipexole hydrochloride tablet | |
| CN107982230A (en) | A kind of uliprista acetate dispersible tablet and preparation method thereof | |
| JP5755382B2 (en) | Orally disintegrating tablets | |
| CN104758266B (en) | A kind of felodipine sustained-release tablets and its preparation technology | |
| CN109125270A (en) | A kind of solid pharmaceutical preparation and preparation method thereof | |
| CN101912390A (en) | Medicinal composite containing irbesartan | |
| CN108578404B (en) | Medicinal composition containing irbesartan and amlodipine and preparation method thereof | |
| JP4591742B2 (en) | Dioctylsodium sulfosuccinate-containing preparation and method for producing the same | |
| CN105687162A (en) | Tacrolimus preparation pharmaceutical composition and preparation method thereof |
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 | ||
| ASS | Succession or assignment of patent right |
Effective date: 20110829 Owner name: SHANGHAI FOSUN PHARMACEUTICAL INDUSTRIAL DEVELOPME |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20110829 Address after: 221004 No. 6, Yang Shan Road, Jinshan Development Zone, Jiangsu, Xuzhou Co-patentee after: Shanghai FOSUN Pharmaceutical Co.,Ltd. Patentee after: Jiangsu Wanbang Biological Pharmaceutical Co., Ltd. Address before: 221004 No. 6, Yang Shan Road, Jinshan Development Zone, Jiangsu, Xuzhou Patentee before: Jiangsu Wanbang Biological Pharmaceutical Co., Ltd. |
|
| C53 | Correction of patent for invention or patent application | ||
| CB03 | Change of inventor or designer information |
Inventor after: Qiao Deshui Inventor after: Sun Xiuli Inventor after: Gao Xueqin Inventor before: Sun Xiuli Inventor before: Qiao Deshui Inventor before: Gao Xueqin |
|
| COR | Change of bibliographic data |
Free format text: CORRECT: INVENTOR; FROM: SUN XIULI QIAO DESHUI GAO XUEQIN TO: QIAO DESHUI SUN XIULI GAO XUEQIN |
|
| ASS | Succession or assignment of patent right |
Free format text: FORMER OWNER: SHANGHAI FOSUN PHARMACEUTICAL INDUSTRIAL DEVELOPMENT CO., LTD. Effective date: 20130325 Owner name: HEBEI FOLON PHARMACEUTICAL CO., LTD.;SHANGHAI FOSU Free format text: FORMER OWNER: JIANGSU WANBANG BIOLOGICAL PHARMACEUTICAL CO., LTD. Effective date: 20130325 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| COR | Change of bibliographic data |
Free format text: CORRECT: ADDRESS; FROM: 221004 XUZHOU, JIANGSU PROVINCE TO: 054900 XINGTAI, HEBEI PROVINCE |
|
| TR01 | Transfer of patent right |
Effective date of registration: 20130325 Address after: 054900, 88 Ping'an Avenue, Linxi County, Hebei Province Patentee after: Hebei Folon Pharmaceutical Co., Ltd. Address before: 221004 No. 6, Yang Shan Road, Jinshan Development Zone, Jiangsu, Xuzhou Patentee before: Jiangsu Wanbang Biological Pharmaceutical Co., Ltd. Patentee before: Shanghai FOSUN Pharmaceutical Co.,Ltd. |
|
| DD01 | Delivery of document by public notice |
Addressee: Yang Ronghui Document name: Notification of Passing Examination on Formalities |
|
| TR01 | Transfer of patent right |
Effective date of registration: 20180209 Address after: 221004, Jiangsu, Xuzhou Jinshan Development Zone, comprehensive area, the south side of the Cave Hill Patentee after: Jiangsu Wan biochemical pharmaceutical Refco Group Ltd Address before: 054900, 88 Ping'an Avenue, Linxi County, Hebei Province Patentee before: Hebei Folon Pharmaceutical Co., Ltd. |
|
| TR01 | Transfer of patent right |