CN101066251A - Dispersed tablet of proton pump inhibitor - Google Patents
Dispersed tablet of proton pump inhibitor Download PDFInfo
- Publication number
- CN101066251A CN101066251A CNA2007100235774A CN200710023577A CN101066251A CN 101066251 A CN101066251 A CN 101066251A CN A2007100235774 A CNA2007100235774 A CN A2007100235774A CN 200710023577 A CN200710023577 A CN 200710023577A CN 101066251 A CN101066251 A CN 101066251A
- Authority
- CN
- China
- Prior art keywords
- proton pump
- pump inhibitor
- sodium
- dispersible tablet
- tablet according
- 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.)
- Pending
Links
- 229940126409 proton pump inhibitor Drugs 0.000 title claims abstract description 49
- 239000000612 proton pump inhibitor Substances 0.000 title claims abstract description 48
- 239000000203 mixture Substances 0.000 claims abstract description 41
- 229960000381 omeprazole Drugs 0.000 claims abstract description 31
- 229960003174 lansoprazole Drugs 0.000 claims abstract description 28
- MJIHNNLFOKEZEW-UHFFFAOYSA-N lansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1 MJIHNNLFOKEZEW-UHFFFAOYSA-N 0.000 claims abstract description 28
- SUBDBMMJDZJVOS-UHFFFAOYSA-N 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole Chemical compound N=1C2=CC(OC)=CC=C2NC=1S(=O)CC1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-UHFFFAOYSA-N 0.000 claims abstract description 25
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims abstract description 16
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical group [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims abstract description 16
- -1 S-omeprazole Chemical compound 0.000 claims abstract description 13
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims abstract description 12
- 239000001095 magnesium carbonate Substances 0.000 claims abstract description 12
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims abstract description 12
- 229910000029 sodium carbonate Inorganic materials 0.000 claims abstract description 8
- PSIREIZGKQBEEO-UHFFFAOYSA-N 2-(1h-benzimidazol-2-ylsulfinylmethyl)-n-methyl-n-(2-methylpropyl)aniline Chemical compound CC(C)CN(C)C1=CC=CC=C1CS(=O)C1=NC2=CC=CC=C2N1 PSIREIZGKQBEEO-UHFFFAOYSA-N 0.000 claims abstract description 7
- ZBFDAUIVDSSISP-UHFFFAOYSA-N 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methylsulfinyl]-1H-imidazo[4,5-b]pyridine Chemical compound N=1C2=NC(OC)=CC=C2NC=1S(=O)CC1=NC=C(C)C(OC)=C1C ZBFDAUIVDSSISP-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229950007395 leminoprazole Drugs 0.000 claims abstract description 7
- 229950008375 tenatoprazole Drugs 0.000 claims abstract description 7
- IQPSEEYGBUAQFF-UHFFFAOYSA-N Pantoprazole Chemical compound COC1=CC=NC(CS(=O)C=2NC3=CC=C(OC(F)F)C=C3N=2)=C1OC IQPSEEYGBUAQFF-UHFFFAOYSA-N 0.000 claims abstract description 3
- 229960005019 pantoprazole Drugs 0.000 claims abstract description 3
- 229960004157 rabeprazole Drugs 0.000 claims abstract description 3
- YREYEVIYCVEVJK-UHFFFAOYSA-N rabeprazole Chemical compound COCCCOC1=CC=NC(CS(=O)C=2NC3=CC=CC=C3N=2)=C1C YREYEVIYCVEVJK-UHFFFAOYSA-N 0.000 claims abstract description 3
- 150000003839 salts Chemical class 0.000 claims abstract description 3
- 239000007919 dispersible tablet Substances 0.000 claims description 53
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 44
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 28
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 27
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 claims description 27
- 239000000347 magnesium hydroxide Substances 0.000 claims description 27
- 229910001862 magnesium hydroxide Inorganic materials 0.000 claims description 27
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 claims description 26
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 26
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 26
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 22
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 22
- 235000019359 magnesium stearate Nutrition 0.000 claims description 22
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- 235000019408 sucralose Nutrition 0.000 claims description 16
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 16
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 14
- 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 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 14
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 14
- 239000000872 buffer Substances 0.000 claims description 14
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 14
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 14
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 14
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- 239000011734 sodium Substances 0.000 claims description 14
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- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 14
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 14
- 239000000600 sorbitol Substances 0.000 claims description 14
- 235000010356 sorbitol Nutrition 0.000 claims description 14
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 12
- 229930195725 Mannitol Natural products 0.000 claims description 12
- 239000000594 mannitol Substances 0.000 claims description 12
- 235000010355 mannitol Nutrition 0.000 claims description 12
- 229920000881 Modified starch Polymers 0.000 claims description 10
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 10
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 10
- 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 8
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 claims description 8
- 229940013618 stevioside Drugs 0.000 claims description 8
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 claims description 8
- 235000019202 steviosides Nutrition 0.000 claims description 8
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 7
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 claims description 7
- 229910021502 aluminium hydroxide Inorganic materials 0.000 claims description 7
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 7
- 239000008101 lactose Substances 0.000 claims description 7
- 108010011485 Aspartame Proteins 0.000 claims description 6
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 6
- 229930006000 Sucrose Natural products 0.000 claims description 6
- 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 claims description 6
- 239000000605 aspartame Substances 0.000 claims description 6
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 6
- 235000010357 aspartame Nutrition 0.000 claims description 6
- 229960003438 aspartame Drugs 0.000 claims description 6
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 6
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 6
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 6
- 239000005720 sucrose Substances 0.000 claims description 6
- 239000000796 flavoring agent Substances 0.000 claims description 5
- 235000013355 food flavoring agent Nutrition 0.000 claims description 5
- 239000000314 lubricant Substances 0.000 claims description 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 5
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 4
- 239000004375 Dextrin Substances 0.000 claims description 4
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- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 3
- 229940024606 amino acid Drugs 0.000 claims description 3
- 235000001014 amino acid Nutrition 0.000 claims description 3
- 150000001413 amino acids Chemical class 0.000 claims description 3
- AXCZMVOFGPJBDE-UHFFFAOYSA-L calcium dihydroxide Chemical compound [OH-].[OH-].[Ca+2] AXCZMVOFGPJBDE-UHFFFAOYSA-L 0.000 claims description 3
- 239000000920 calcium hydroxide Substances 0.000 claims description 3
- 229910001861 calcium hydroxide Inorganic materials 0.000 claims description 3
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 claims description 2
- 229920002261 Corn starch Polymers 0.000 claims description 2
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- 229930091371 Fructose Natural products 0.000 claims description 2
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- 230000000767 anti-ulcer Effects 0.000 description 1
- 229960003563 calcium carbonate Drugs 0.000 description 1
- 208000010643 digestive system disease Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000002532 enzyme inhibitor Substances 0.000 description 1
- 229940125532 enzyme inhibitor Drugs 0.000 description 1
- 208000006881 esophagitis Diseases 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 229960000905 indomethacin Drugs 0.000 description 1
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000009434 installation Methods 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 229960002702 piroxicam Drugs 0.000 description 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 description 1
- 238000004886 process control Methods 0.000 description 1
- 230000000391 smoking effect Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The dispersed tablet of proton pump inhibitor is used for treating gastric ulcer, duodenal ulcer, stomal ulcer and other indications. It contains at least one kind of proton pump inhibitor and at least one kind of biologically acceptable buffering agent in the weight ratio of 1 to 10-200. The proton pump inhibitor is one selected from omeprazole, S-omeprazole, pantoprazole, lansoprazole, rabeprazole, leminoprazole, tenatoprazole and their salts. The biologically acceptable buffering agent is sodium bicarbonate, sodium carbonate, magnesium carbonate, etc or their mixture.
Description
Technical field
A kind of proton pump inhibitor dispersible tablet of the present invention relates to a kind of dispersible tablet that contains at least a proton pump inhibitor and the acceptable buffer agent of at least a biology, be used for the treatment of gastric ulcer, duodenal ulcer, stoma ulcer, instead flow to esophagitis indications such as a tall and erect Emhorn syndrome.
Background technology
The digestive system disease is one of common frequently-occurring disease, and wherein Peptic Ulcers is for the most common, and its total incidence accounts for 10~12% of population, and main age of onset is 30~50 years old.The U.S. has 400,000 person-times to suffer from peptic ulcers every year, mainly because smoking, drink, nervous, medicine irritation (as ASP, indometacin, piroxicam etc.) causes that U.S. male sickness rate is 10%, the women is 5%.Japan's gastrointestinal tract sickness rate is 5~10%, and Germany is 12.3%.China is 11.43% according to minority ground finding, and Shanghai resident's prevalence is up to 30.23% (Beijing, Sichuan, Liaoning Province are 23.66%), and wherein the sick sickness rate of digestive tract ulcer is 4.54%.From global marketing market, according to the MIDS system statistics of IMS HEALTH, treatment Peptic Ulcers medicine is sure to occupy global marketing volume first place always.
Nearly more than ten years anti-ulcer medicament research has trended towards the excretory medicine of energy selectivity gastric acid inhibitory, proton pump inhibitor (the PPI)-H of the exploitation listing eighties
+/ K
+-APT enzyme inhibitor, because of its mechanism of action uniqueness, effect specificity height, action intensity is big and the time is long, is widely used in sour relevant various disorder diseases to be favored day by day.
The kind of the domestic and international exploitation of proton pump inhibitor at present mainly contains omeprazole, S-magnesium omeprazole, Pantoprazole Sodium, lansoprazole, RABEPRAZOLE SODIUM, leminoprazole and Tenatoprazole etc.
Because proton pump inhibitor is very easily degraded in sour environment; so common proton pump inhibitor oral formulations all adopts the mode of enteric coating to prevent that active component from degrading in gastric acid; enteric coating makes also that in the protection active component acid effect that presses down of proton pump inhibitor is postponed, and is unfavorable for treatment in time and removes patient's misery rapidly.
Summary of the invention
The objective of the invention is provides a kind of proton pump inhibitor dispersible tablet at above weak point, the proton pump inhibitor dispersible tablet is a kind of proton pump inhibitor oral formulations, this dispersible tablet onset is rapid, good stability, do not need enteric coating, technical process is simple, thereby resulting cost is lower, has considerable economic and social benefit.
A kind of proton pump inhibitor dispersible tablet is characterized in that containing at least a proton pump inhibitor, and the acceptable buffer agent of at least a biology, and wherein proton pump inhibitor is 1: 10~200 with the biological substance weight proportioning that can accept buffer agent.
Described proton pump inhibitor is selected from a kind of in omeprazole, S-omeprazole, pantoprazole, lansoprazole, rabeprazole, leminoprazole, Tenatoprazole and the salt thereof.
The acceptable buffer agent of described biology is selected from a kind of or mixture in sodium bicarbonate, sodium carbonate, magnesium carbonate, magnesium hydroxide, calcium carbonate, calcium hydroxide, aluminium hydroxide, sodium hydroxide, the aminoacid.
The acceptable buffer agent of described biology is a kind of or mixture in sodium bicarbonate, sodium carbonate, magnesium carbonate, magnesium hydroxide, the calcium carbonate preferably, is more preferably sodium bicarbonate and magnesium hydroxide.
Described proton pump inhibitor is 1: 25~100 with the biological substance weight proportion optimization that can accept buffer agent.
Described proton pump inhibitor dispersible tablet can also comprise excipient, excipient is selected from a kind of or mixture in lactose, sucrose, mannitol, sorbitol, corn starch, pregelatinized Starch, dextrin, maltodextrin, cyclodextrin, microcrystalline Cellulose, calcium hydrogen phosphate, the calcium phosphate, and the content of excipient is 10~30% of described dispersible tablet weight.
Described proton pump inhibitor dispersible tablet can also comprise disintegrating agent, disintegrating agent is selected from a kind of or mixture in polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, the cross-linking sodium carboxymethyl cellulose, and the content of disintegrating agent is 2~10% of described dispersible tablet weight.
Described proton pump inhibitor dispersible tablet can also comprise binding agent, and binding agent is selected from a kind of in polyvidone, hydroxypropyl emthylcellulose, hydroxypropyl cellulose, starch slurry, the sodium carboxymethyl cellulose.
Described proton pump inhibitor dispersible tablet can also comprise flavoring agent, flavoring agent is selected from a kind of or mixture in aspartame, sucralose, stevioside, glycyrrhizin, saccharin sodium, glucide, mannitol, xylitol, sorbitol, fructose, sucrose, maltose, essence, spice, the sodium glutamate, and the content of flavoring agent is 1~5% of described dispersible tablet weight.
Described proton pump inhibitor dispersible tablet can also comprise lubricant, and lubricant is selected from a kind of or mixture in magnesium stearate, Pulvis Talci, micropowder silica gel, calcium stearate, the stearic acid, and the content of lubricant is 0.5~3% of described dispersible tablet weight.
Because proton pump inhibitor is very easily degraded in sour environment; so common proton pump inhibitor oral formulations all adopts the mode of enteric coating to prevent that active component from degrading in gastric acid; enteric coating makes also that in the protection active component acid effect that presses down of proton pump inhibitor is postponed, and is unfavorable for treatment in time and removes patient's misery rapidly.The present invention is by adding sodium bicarbonate in the proton pump inhibitor dispersible tablet; sodium carbonate; magnesium carbonate; magnesium hydroxide; calcium carbonate; calcium hydroxide; aluminium hydroxide; sodium hydroxide; a kind of or mixture in the buffer agents such as aminoacid; when the proton pump inhibitor dispersible tablet arrives gastric; disperse rapidly; produce a relative higher environment of pH value in the buffer agent of capacity and the gastric acid and in the part; the protection of maximum proton pump inhibitor; and proton pump inhibitor is absorbed and used fast; the performance drug effect; thereby it is slow to have solved the onset of proton pump inhibitor oral enteric preparation; complicated process of preparation; need special installation; loaded down with trivial details and the high shortcoming of production cost of quality control; adopt the proton pump inhibitor dispersible tablet steady quality of technical solution of the present invention preparation; onset is rapid; buffer agent wherein itself is crossed acid environment to gastric and has also been produced neutralization in the protection active component, helps the patient and treats more timely and painful rapid releasing.Adjuvant kind few (not need of coating material) in the production, technical process and quality control are simple, and the production cycle shortens greatly, reduced the coating operation, just reduce the manpower and the equipment input of corresponding operation simultaneously, had lower production cost, can produce considerable economic and social benefit.
The specific embodiment
Further specify the present invention below by embodiment.Should correct understanding be: embodiments of the invention are only used for the present invention is described and provide, rather than limitation of the present invention, so, under method prerequisite of the present invention, simple modifications of the present invention is all belonged to the scope of protection of present invention.
Embodiment 1:
Omeprazole 20g
Sodium bicarbonate 400g
Polyvidone 70g
Magnesium stearate 10g
The omeprazole of above-mentioned amount is crossed 80 mesh sieve mixings by progressively increase method and sodium bicarbonate, polyvidone of equivalent, and rolling process is made sheet, crosses 18 mesh sieves and granulates, and adds magnesium stearate, and mix homogeneously is measured tabletting behind the intermediate content, promptly gets the omeprazole dispersible tablet.
Embodiment 2:
Omeprazole 20g
Sodium bicarbonate 500g
Pregelatinized Starch 236g
Polyvinylpolypyrrolidone 40g
Magnesium stearate 4g
The omeprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, pregelatinized Starch of equivalent, and rolling process is made sheet, crosses 16 mesh sieves and granulates, add polyvinylpolypyrrolidone and magnesium stearate, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the omeprazole dispersible tablet.
Embodiment 3:
Omeprazole 80g
Sodium bicarbonate 800g
Mannitol 408g
Carboxymethyl starch sodium 70g
Sucralose 21g
Strawberry essence 7g
Micropowder silica gel 14g
The omeprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, mannitol, sucralose, strawberry essence of equivalent, rolling process is made sheet, crossing 14 mesh sieves granulates, add carboxymethyl starch sodium and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the omeprazole dispersible tablet.
Embodiment 4:
Omeprazole 40g
Sodium bicarbonate 400g
Mannitol 400g
Carboxymethyl starch sodium 40g
Stevioside 5g
Strawberry essence 5g
Micropowder silica gel 10g
The omeprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, mannitol, stevioside, strawberry essence of equivalent, rolling process is made sheet, crossing 16 mesh sieves granulates, add carboxymethyl starch sodium and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the omeprazole dispersible tablet.
Embodiment 5:
Lansoprazole 20g
Magnesium hydroxide 800g
Sodium carbonate 1200g
Cross-linking sodium carboxymethyl cellulose 70g
Magnesium stearate 10g
The lansoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and magnesium hydroxide, sodium carbonate of equivalent, and rolling process is made sheet, crosses 12 mesh sieves and granulates, add cross-linking sodium carboxymethyl cellulose and magnesium stearate, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the lansoprazole dispersible tablet.
Embodiment 6:
Lansoprazole 30g
Magnesium hydroxide 1200g
Pregelatinized Starch 360g
Magnesium stearate 10g
The lansoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and magnesium hydroxide, pregelatinized Starch of equivalent, and rolling process is made sheet, crosses 14 mesh sieves and granulates, and adds magnesium stearate, and mix homogeneously is measured tabletting behind the intermediate content, promptly gets the lansoprazole dispersible tablet.
Embodiment 7:
Pantoprazole Sodium 44.3g
Magnesium hydroxide 1100g
Microcrystalline Cellulose 250g
Low-substituted hydroxypropyl cellulose 75g
5% polyvidone, 80% alcoholic solution 300ml
Aspartame 15g
Fructus Citri Limoniae essence 7.5g
Magnesium stearate 7.5g
The Pantoprazole Sodium of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and magnesium hydroxide, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose of equivalent, make soft material with 5% polyvidone, 80% alcoholic solution, crossing 16 mesh sieves granulates, 50 ℃ of air blast oven dry in 2 hours, cross 18 mesh sieve granulate, add aspartame, Fructus Citri Limoniae essence and magnesium stearate, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the pantoprazole sodium dispersible tablets.
Embodiment 8:
Pantoprazole Sodium 22.1g
Magnesium hydroxide 700g
Microcrystalline Cellulose 200g
Pregelatinized Starch 100g
2% polyvidone, 80% alcoholic solution 200ml
Aspartame 15g
Fructus Citri tangerinae essence 7.5g
Magnesium stearate 7.5g
The Pantoprazole Sodium of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and magnesium hydroxide, microcrystalline Cellulose, pregelatinized Starch of equivalent, make soft material with 5% polyvidone, 80% alcoholic solution, crossing 16 mesh sieves granulates, 50 ℃ of air blast oven dry in 2 hours, cross 18 mesh sieve granulate, add aspartame, Fructus Citri tangerinae essence and magnesium stearate, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the pantoprazole sodium dispersible tablets.
Embodiment 9:
Pantoprazole Sodium 44.3g
Magnesium hydroxide 600g
Calcium carbonate 400g
Low-substituted hydroxypropyl cellulose 100g
5% polyvidone, 80% alcoholic solution 250ml
Saccharin sodium 10g
Fructus Citri Limoniae essence 10g
Magnesium stearate 10g
The Pantoprazole Sodium of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and magnesium hydroxide, calcium carbonate, low-substituted hydroxypropyl cellulose, saccharin sodium of equivalent, make soft material with 5% polyvidone, 80% alcoholic solution, crossing 16 mesh sieves granulates, 50 ℃ of air blast oven dry in 2 hours, cross 18 mesh sieve granulate, add Fructus Citri Limoniae essence and magnesium stearate, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the pantoprazole sodium dispersible tablets.
Embodiment 10:
RABEPRAZOLE SODIUM 21.3g
Magnesium carbonate 1000g
Sodium hydroxide 20g
Microcrystalline Cellulose 225g
Lactose 100g
Low-substituted hydroxypropyl cellulose 75g
2% hydroxypropyl emthylcellulose (50cp), 75% alcoholic solution 230ml
Polyvinylpolypyrrolidone 45g
Magnesium stearate 15g
The RABEPRAZOLE SODIUM of above-mentioned amount is crossed 80 mesh sieve mixings by progressively increase method and magnesium carbonate, sodium hydroxide, microcrystalline Cellulose, lactose, low-substituted hydroxypropyl cellulose of equivalent, make soft material with 2% hydroxypropyl emthylcellulose (50cp), 75% alcoholic solution, crossing 16 mesh sieves granulates, 50 ℃ of air blast oven dry in 2 hours, cross 18 mesh sieve granulate, add polyvinylpolypyrrolidone and magnesium stearate, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the rabeprazole sodium dispersible tablets.
Embodiment 11:
RABEPRAZOLE SODIUM 21.3g
Magnesium carbonate 1000g
Sodium hydroxide 20g
Dextrin 200g
Sucrose 100g
2% hydroxypropyl emthylcellulose (50cp), 75% alcoholic solution 300ml
Carboxymethyl starch sodium 45g
Polyvinylpolypyrrolidone 45g
Magnesium stearate 15g
The RABEPRAZOLE SODIUM of above-mentioned amount is crossed 80 mesh sieve mixings by progressively increase method and magnesium carbonate, sodium hydroxide, dextrin, lactose, sucrose of equivalent, make soft material with 2% hydroxypropyl emthylcellulose (50cp), 75% alcoholic solution, crossing 16 mesh sieves granulates, 50 ℃ of air blast oven dry in 2 hours, cross 18 mesh sieve granulate, add carboxymethyl starch sodium, polyvinylpolypyrrolidone and magnesium stearate, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the rabeprazole sodium dispersible tablets.
Embodiment 12:
RABEPRAZOLE SODIUM 21.3g
Magnesium carbonate 1000g
Sodium hydroxide 20g
Microcrystalline Cellulose 225g
Lactose 100g
Low-substituted hydroxypropyl cellulose 75g
2% hydroxypropyl emthylcellulose (50cp), 75% alcoholic solution 230ml
Polyvinylpolypyrrolidone 45g
Magnesium stearate 15g
The RABEPRAZOLE SODIUM of above-mentioned amount is crossed 80 mesh sieve mixings by progressively increase method and magnesium carbonate, sodium hydroxide, microcrystalline Cellulose, lactose, low-substituted hydroxypropyl cellulose of equivalent, make soft material with 2% hydroxypropyl emthylcellulose (50cp), 75% alcoholic solution, crossing 16 mesh sieves granulates, 18 mesh sieve granulate are crossed in 50 ℃ of air blast oven dry in 2 hours, add polyvinylpolypyrrolidone and magnesium stearate, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the rabeprazole sodium dispersible tablets, and hardness is 6.5Kg.
Embodiment 13:
Lansoprazole 10g
Sodium bicarbonate 1200g
Magnesium hydroxide 800g
Low-substituted hydroxypropyl cellulose 170g
Pulvis Talci 20g
The lansoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, magnesium hydroxide, low-substituted hydroxypropyl cellulose of equivalent, and rolling process is made sheet, crosses 14 mesh sieves and granulates, add Pulvis Talci, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the lansoprazole dispersible tablet.
Embodiment 14:
Lansoprazole 20g
Sodium bicarbonate 1200g
Magnesium hydroxide 800g
Low-substituted hydroxypropyl cellulose 170g
Pulvis Talci 20g
The lansoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, magnesium hydroxide, low-substituted hydroxypropyl cellulose of equivalent, and rolling process is made sheet, crosses 14 mesh sieves and granulates, add Pulvis Talci, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the lansoprazole dispersible tablet.
Embodiment 15:
Lansoprazole 30g
Sodium bicarbonate 1200g
Magnesium hydroxide 800g
Low-substituted hydroxypropyl cellulose 170g
Pulvis Talci 20g
The lansoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, magnesium hydroxide, low-substituted hydroxypropyl cellulose of equivalent, and rolling process is made sheet, crosses 14 mesh sieves and granulates, add Pulvis Talci, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the lansoprazole dispersible tablet.
Embodiment 16:
Lansoprazole 40g
Sodium bicarbonate 1200g
Magnesium hydroxide 800g
Low-substituted hydroxypropyl cellulose 170g
Pulvis Talci 20g
The lansoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, magnesium hydroxide, low-substituted hydroxypropyl cellulose of equivalent, and rolling process is made sheet, crosses 14 mesh sieves and granulates, add Pulvis Talci, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the lansoprazole dispersible tablet.
Embodiment 17:
Omeprazole 20g
Sodium bicarbonate 800g
Mannitol 90g
Polyvinylpolypyrrolidone 30g
Carboxymethyl starch sodium 30g
Sucralose 15g
Flavoring orange essence 5g
Micropowder silica gel 10g
The omeprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, mannitol, polyvinylpolypyrrolidone of equivalent, rolling process is made sheet, crossing 16 mesh sieves granulates, add carboxymethyl starch sodium, sucralose, flavoring orange essence and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the omeprazole dispersible tablet.
Embodiment 18:
Omeprazole 20g
Sodium bicarbonate 800g
Sorbitol 90g
Polyvinylpolypyrrolidone 30g
Carboxymethyl starch sodium 30g
Sucralose 15g
Blue berry essence 5g
Micropowder silica gel 10g
The omeprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, sorbitol, polyvinylpolypyrrolidone of equivalent, rolling process is made sheet, crossing 16 mesh sieves granulates, add carboxymethyl starch sodium, sucralose, blue berry essence and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the omeprazole dispersible tablet.
Embodiment 19:
Omeprazole 20g
Sodium bicarbonate 600g
Mannitol 100g
Sorbitol 100g
Polyvinylpolypyrrolidone 25g
Carboxymethyl starch sodium 25g
Sucralose 15g
Flavoring orange essence 5g
Micropowder silica gel 10g
The omeprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and sodium bicarbonate, mannitol, sorbitol, polyvinylpolypyrrolidone of equivalent, rolling process is made sheet, crossing 16 mesh sieves granulates, add carboxymethyl starch sodium, sucralose, flavoring orange essence and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the omeprazole dispersible tablet.
Embodiment 20:
Lansoprazole 20g
Aluminium hydroxide 600g
Microcrystalline Cellulose 160g
Pregelatinized Starch 100g
Low-substituted hydroxypropyl cellulose 50g
Stevioside 15g
Strawberry essence 5g
Polyvinylpolypyrrolidone 30g
Pulvis Talci 10g
Micropowder silica gel 10g
The lansoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and aluminium hydroxide, microcrystalline Cellulose, pregelatinized Starch, low-substituted hydroxypropyl cellulose, stevioside, strawberry essence of equivalent, rolling process is made sheet, crossing 16 mesh sieves granulates, add polyvinylpolypyrrolidone, Pulvis Talci and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the lansoprazole dispersible tablet.
Embodiment 21:
Lansoprazole 20g
Aluminium hydroxide 350g
Magnesium hydroxide 350g
Microcrystalline Cellulose 160g
Low-substituted hydroxypropyl cellulose 50g
Stevioside 15g
Strawberry essence 5g
Polyvinylpolypyrrolidone 30g
Pulvis Talci 10g
Micropowder silica gel 10g
The lansoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and aluminium hydroxide, magnesium hydroxide, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, stevioside, strawberry essence of equivalent, rolling process is made sheet, crossing 16 mesh sieves granulates, add polyvinylpolypyrrolidone, Pulvis Talci and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the lansoprazole dispersible tablet.
Embodiment 22:
S-omeprazole 20g
Magnesium bicarbonate 600g
Sorbitol 200g
Polyvinylpolypyrrolidone 50g
Sucralose 15g
Blue berry essence 5g
Micropowder silica gel 10g
The S-omeprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and magnesium bicarbonate, sorbitol, polyvinylpolypyrrolidone of equivalent, rolling process is made sheet, crossing 18 mesh sieves granulates, add sucralose, blue berry essence and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets S-omeprazole dispersible tablet.
Embodiment 23:
Leminoprazole 20g
Magnesium bicarbonate 600g
Sorbitol 200g
Polyvinylpolypyrrolidone 50g
Sucralose 15g
Blue berry essence 5g
Micropowder silica gel 10g
The leminoprazole of above-mentioned amount is crossed 60 mesh sieve mixings by progressively increase method and magnesium bicarbonate, sorbitol, polyvinylpolypyrrolidone of equivalent, rolling process is made sheet, crossing 18 mesh sieves granulates, add sucralose, blue berry essence and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the leminoprazole dispersible tablet.
Embodiment 24:
Tenatoprazole 20g
L-arginine 500g
Sorbitol 300g
Polyvinylpolypyrrolidone 50g
Sucralose 15g
Blue berry essence 5g
Micropowder silica gel 10g
Progressively increase method and L-arginine, sorbitol, polyvinylpolypyrrolidone of the Tenatoprazole equivalent of above-mentioned amount crossed 60 mesh sieve mixings, rolling process is made sheet, crossing 18 mesh sieves granulates, add sucralose, blue berry essence and micropowder silica gel, mix homogeneously, tabletting behind the mensuration intermediate content promptly gets the Tenatoprazole dispersible tablet.
Claims (10)
1, a kind of proton pump inhibitor dispersible tablet is characterized in that containing at least a proton pump inhibitor, and the acceptable buffer agent of at least a biology, and wherein proton pump inhibitor is 1: 10~200 with the biological substance weight proportioning that can accept buffer agent.
2, proton pump inhibitor dispersible tablet according to claim 1 is characterized in that described proton pump inhibitor is selected from a kind of in omeprazole, S-omeprazole, pantoprazole, lansoprazole, rabeprazole, leminoprazole, Tenatoprazole and the salt thereof.
3, proton pump inhibitor dispersible tablet according to claim 1 is characterized in that the acceptable buffer agent of described biology is selected from a kind of or mixture in sodium bicarbonate, sodium carbonate, magnesium carbonate, magnesium hydroxide, calcium carbonate, calcium hydroxide, aluminium hydroxide, sodium hydroxide, the aminoacid.
4, proton pump inhibitor dispersible tablet according to claim 3, it is characterized in that the preferably a kind of or mixture in sodium bicarbonate, sodium carbonate, magnesium carbonate, magnesium hydroxide, the calcium carbonate of the acceptable buffer agent of described biology, be more preferably sodium bicarbonate and magnesium hydroxide.
5, proton pump inhibitor dispersible tablet according to claim 1, what it is characterized in that described proton pump inhibitor and the biological substance weight proportion optimization that can accept buffer agent is 1: 25~100.
6, proton pump inhibitor dispersible tablet according to claim 1, it is characterized in that also comprising that excipient, excipient are selected from a kind of or mixture in lactose, sucrose, mannitol, sorbitol, corn starch, pregelatinized Starch, dextrin, maltodextrin, cyclodextrin, microcrystalline Cellulose, calcium hydrogen phosphate, the calcium phosphate.
7, proton pump inhibitor dispersible tablet according to claim 1 is characterized in that also comprising that disintegrating agent, disintegrating agent are selected from a kind of or mixture in polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, the cross-linking sodium carboxymethyl cellulose.
8, proton pump inhibitor dispersible tablet according to claim 1 is characterized in that also comprising that binding agent, binding agent are selected from a kind of in polyvidone, hydroxypropyl emthylcellulose, hydroxypropyl cellulose, starch slurry, the sodium carboxymethyl cellulose.
9, proton pump inhibitor dispersible tablet according to claim 1, it is characterized in that also comprising that flavoring agent, flavoring agent are selected from a kind of or mixture in aspartame, sucralose, stevioside, glycyrrhizin, saccharin sodium, glucide, mannitol, xylitol, sorbitol, fructose, sucrose, maltose, essence, spice, the sodium glutamate.
10, proton pump inhibitor dispersible tablet according to claim 1 is characterized in that also comprising that lubricant, lubricant are selected from a kind of or mixture in magnesium stearate, Pulvis Talci, micropowder silica gel, calcium stearate, the stearic acid.
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CN101816641A (en) * | 2010-03-11 | 2010-09-01 | 沈阳亿灵医药科技有限公司 | Omeprazole quick-release solid preparation and preparation method thereof |
CN102114037A (en) * | 2010-01-06 | 2011-07-06 | 北京阜康仁生物制药科技有限公司 | Novel compound lansoprazole composition |
CN102114035A (en) * | 2010-01-06 | 2011-07-06 | 北京阜康仁生物制药科技有限公司 | Novel compound esomeprazole composition |
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US9351966B2 (en) | 2008-02-20 | 2016-05-31 | The Curators Of The University Of Missouri | Composition comprising a combination of omeprazole and lansoprazole, and a buffering agent, and methods of using same |
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CN102138930A (en) * | 2011-01-04 | 2011-08-03 | 海南美兰史克制药有限公司 | Solid preparation of compound sodium rabeprazole medicinal composition |
CN102198109A (en) * | 2011-05-20 | 2011-09-28 | 广东帅广医药有限公司 | Lansoprazole medicine composition tablet and preparation method thereof |
CN103006654A (en) * | 2012-07-12 | 2013-04-03 | 姚云 | Medicinal composition containing lansoprazole compound |
CN103006654B (en) * | 2012-07-12 | 2014-02-26 | 姚云 | Medicinal composition containing lansoprazole compound |
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CN109646413A (en) * | 2018-12-28 | 2019-04-19 | 正大制药(青岛)有限公司 | A kind of Aomei sodium magnesium sheet |
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