CN1886119A - 泮托拉唑多颗粒制剂 - Google Patents
泮托拉唑多颗粒制剂 Download PDFInfo
- Publication number
- CN1886119A CN1886119A CNA2004800352518A CN200480035251A CN1886119A CN 1886119 A CN1886119 A CN 1886119A CN A2004800352518 A CNA2004800352518 A CN A2004800352518A CN 200480035251 A CN200480035251 A CN 200480035251A CN 1886119 A CN1886119 A CN 1886119A
- Authority
- CN
- China
- Prior art keywords
- pantoprazole
- multiparticulate
- separation layer
- many particles
- pantoprazole multiparticulate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 229960005019 pantoprazole Drugs 0.000 title claims abstract description 71
- 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 title claims abstract description 63
- 239000000203 mixture Substances 0.000 title claims description 24
- 238000009472 formulation Methods 0.000 title claims description 11
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 44
- YNWDKZIIWCEDEE-UHFFFAOYSA-N pantoprazole sodium Chemical compound [Na+].COC1=CC=NC(CS(=O)C=2[N-]C3=CC=C(OC(F)F)C=C3N=2)=C1OC YNWDKZIIWCEDEE-UHFFFAOYSA-N 0.000 claims abstract description 40
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract description 36
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 36
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims abstract description 34
- 229960004048 pantoprazole sodium Drugs 0.000 claims abstract description 34
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 30
- 239000004094 surface-active agent Substances 0.000 claims abstract description 15
- 150000003839 salts Chemical class 0.000 claims abstract description 10
- 239000002245 particle Substances 0.000 claims description 69
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- 238000009505 enteric coating Methods 0.000 claims description 30
- 239000003814 drug Substances 0.000 claims description 28
- 239000002775 capsule Substances 0.000 claims description 27
- 238000000034 method Methods 0.000 claims description 24
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 19
- 229960000913 crospovidone Drugs 0.000 claims description 18
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 18
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 18
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 16
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 15
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 15
- 229920000053 polysorbate 80 Polymers 0.000 claims description 15
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- 239000007884 disintegrant Substances 0.000 claims description 12
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 11
- 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 11
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 11
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- -1 Pantoprazole compound Chemical class 0.000 claims description 8
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- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 8
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- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims description 6
- 239000001069 triethyl citrate Substances 0.000 claims description 6
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims description 6
- 235000013769 triethyl citrate Nutrition 0.000 claims description 6
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- GDCRSXZBSIRSFR-UHFFFAOYSA-N ethyl prop-2-enoate;2-methylprop-2-enoic acid Chemical compound CC(=C)C(O)=O.CCOC(=O)C=C GDCRSXZBSIRSFR-UHFFFAOYSA-N 0.000 description 10
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- RCEAADKTGXTDOA-UHFFFAOYSA-N OS(O)(=O)=O.CCCCCCCCCCCC[Na] Chemical compound OS(O)(=O)=O.CCCCCCCCCCCC[Na] RCEAADKTGXTDOA-UHFFFAOYSA-N 0.000 description 4
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- 235000019333 sodium laurylsulphate Nutrition 0.000 description 4
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- 229920003134 Eudragit® polymer Polymers 0.000 description 2
- 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 description 2
- 229920003091 Methocel™ Polymers 0.000 description 2
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 2
- 102100021904 Potassium-transporting ATPase alpha chain 1 Human genes 0.000 description 2
- 108010083204 Proton Pumps Proteins 0.000 description 2
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- 239000007864 aqueous solution Substances 0.000 description 2
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- 239000011521 glass Substances 0.000 description 2
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- 125000006216 methylsulfinyl group Chemical group [H]C([H])([H])S(*)=O 0.000 description 2
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- 229910052708 sodium Inorganic materials 0.000 description 2
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- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 1
- 206010000087 Abdominal pain upper Diseases 0.000 description 1
- ZKHQWZAMYRWXGA-KQYNXXCUSA-N Adenosine triphosphate Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O ZKHQWZAMYRWXGA-KQYNXXCUSA-N 0.000 description 1
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- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
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- 230000002378 acidificating effect Effects 0.000 description 1
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- GPRLSGONYQIRFK-UHFFFAOYSA-N hydron Chemical compound [H+] GPRLSGONYQIRFK-UHFFFAOYSA-N 0.000 description 1
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- XGZVUEUWXADBQD-UHFFFAOYSA-L lithium carbonate Chemical compound [Li+].[Li+].[O-]C([O-])=O XGZVUEUWXADBQD-UHFFFAOYSA-L 0.000 description 1
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Classifications
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Abstract
Description
介质 | 时间 | %药物释放 | |||
初始 | 6个月@25C/60%RH | 6个月@40C/75%RH | 指标 | ||
酸(pH 1.0) | 2hrs | 0.33 | 0.45 | 0.6 | NMT10% |
接着用碱性缓冲液(pH 6.8) | 3min | - | 0.91 | 0.85 | - |
6min | - | 3.61 | 1.83 | - | |
9min | - | 52.25 | 16.45 | - | |
12min | - | 89.65 | 75.15 | - | |
15min | 101.58 | 97.15 | 91.92 | - | |
30min | 105.29 | 100.67 | 98.96 | - | |
45min | 105.29 | 100.57 | 99.14 | NLT 75% | |
60min | 105.06 | 100.52 | 99.07 | - |
批 | %药物释放* | |||
酸2hrs | 缓冲液(min) | |||
15 | 30 | 45 | ||
初始 | 0.08 | 101.77 | 107.44 | 107.38 |
6个月@40C/75%RH | 0.73 | 95.44 | 101.12 | 101.21 |
12个月@25C/60%RH | 0.30 | 96.11 | 101.92 | 102.20 |
试验 | 时间 | 浓度(HPLC)%标示物 | 溶出度-释放的百分比(平均) | |
单位 | 0.1N HCl | 磷酸盐缓冲液中第二次溶出 | ||
初始 | 100.0% | 0.9% | 91.6% | |
周围环境室温 | 1个月 | 97.2% | 0.8% | 88.5% |
7个月 | 108.5% | 0.8% | 94.1% | |
30℃/60%RH | 1个月 | 99.3% | 0.5% | 83.4% |
2个月 | 98.3% | NA | NA | |
3个月 | 104.4% | 0.7% | 82.2% | |
40℃/75%RH | 1个月 | 95.4% | 0.7% | 86.11 |
2个月 | 97.3% | NA | NA | |
3个月 | 102.7% | 0.7% | 89.4% |
试验 | 外观和性状 | 浓度(HPLC) | 水份(KF) | 纯度 | 溶出度 | ||
说明 | #2不透明白色胶囊(囊帽和囊体),包 | 90.0-110.0%标示量(LC) | 见资料 | 最大的单一已知或未知杂质≤0.5 | 总的已知和未知杂质≤2.0 | 在0.1NHCl中2小时内的溶出度NMT | 在磷酸盐缓冲液中45分钟内的溶出 |
含白色至类白色的球形体 | (RRT) | 10%。符合USP<724> | 度NLT75%。符合USP<724> | ||||
单位 | % | % | % | % | % | % | |
初始 | 符合 | 100.3 | 5.1 | BRL | BRL | 0 | 105 |
初始(仅球形体)a | 0 | 107 | |||||
25℃/60%RH | |||||||
1个月 | 无变化 | 99.5 | 5.2 | 0.17(1.39) | 0.17 | 1 | 103 |
2个月 | 无变化 | 101.4 | 4.6 | 0.15(1.38)b | 0.23 | 0 | 101 |
3个月 | 无变化 | 101.2 | 4.5 | 0.17(1.39) | 0.17 | 0 | 100 |
6个月 | 无变化 | 101.3 | 4.5 | 0.18(1.38)b | 0.24 | 0 | 100 |
6个月(仅球形体)a | 0 | 112 |
试验 | 外观和性状 | 浓度(HPLC) | 水份(KF) | 纯度 | 溶出度 | ||
说明 | #2不透明的白色胶囊(囊帽和囊体), | 90.0-110.0%标示量(LC) | 见资料 | 最大的单一已知或未知杂质≤0.5 | 总的已知和未知杂质≤2.0 | 在0.1NHCl中2小时内的溶出度NMT | 在磷酸盐缓冲液中45分钟内的溶出 |
包含白色至类白色的球形体 | (RRT) | 10%。符合USP<724> | 度NLT75%。符合USP<724> | ||||
单位 | % | % | % | % | % | % | |
9个月 | 无变化 | 99.2 | 5.1 | 0.21(1.40)b | 0.33 | 0 | 101 |
9个月(仅球形体)a | 0 | 108 | |||||
12个月 | 无变化 | 99.1 | 5.1 | 0.08(0.14) | 0.23 | 0 | 102 |
12个月(仅球形体)a | 0 | 104 |
参数 | 20mg市售片剂批A泮托拉唑钠a | 40mg多颗粒胶囊有肠溶衣的泮托拉唑钠批A |
AUC(μg*hr/mL) | 16.3(2.46) | 17.3(2.33) |
Cmax(μg/mL) | 11.7(3.55) | 7.10(1.76) |
Tmax(hr) | 1.70(0.84) | 1.20(0.27) |
滞后时间(hr) | 1.10(0.91) | 0.25(0.18) |
t1/2(hr) | 0.62(0.17) | 0.77(0.21) |
相对生物利用度 | -- | AUC:106%b |
Cmax:61%b |
赋形剂 | 药物∶赋形剂的比例 | 回收百分率 | |||
药物+赋形剂 | 药物+赋形剂+水 | ||||
40℃/75%RH | 51℃ | 40℃/75%RH | 51℃ | ||
3个周 | 3个周 | 3个周 | 3个周 | ||
对照(仅药物) | - | 94.67 | 100.53 | 94.60 | 96.64 |
羟丙甲纤维素2208,USP,3cps | 10∶1 | 99.209 | 93.248 | 93.811 | 97.421 |
十二烷基硫酸钠(SLS) | 5∶3 | 99.947 | 98.763 | 95.466 | 95.088 |
交聚维酮,NF | 10∶1 | 100.080 | 98.908 | 97.201 | 105.716 |
聚山梨醇酯-80,NFBP/EP(植物源) | 10∶1 | 98.301 | 90.961 | 99.908 | 81.405 |
制剂 | 多颗粒 | |
核: | ||
组分 | 量/胶囊 | %w/w |
泮托拉唑钠倍半水合物 | 45.11 | 21.911 |
微晶纤维素,NF/EP(Avicel PH 101) | 27.39 | 13.304 |
聚山梨醇酯80,NF植物源 | 5.00 | 2.429 |
交聚维酮,NF(Polyplasdone XL) | 15.00 | 7.286 |
HPMC USP/EP(Methocel)K3 | 1.00 | 0.486 |
碳酸钠,NF | 6.50 | 3.157 |
纯化水,USP/BP/EP | 适量以制备湿团 | |
合计 | 100.00mg | 48.573 |
肠溶衣: | 100.20mg | 48.67 |
Eudragit L30D-55 | 208.00mg62.40(固体) | 30.309 |
滑石粉,USP,Altalc 500V | 31.20mg | 15.155 |
氢氧化钠,NF 1N溶液 | 9.30mg0.36(固体) | 0.175 |
柠檬酸三乙酯,PG/NF | 6.24mg | 3.031 |
纯化水,USP/BP/EP | 183.38mg* | *在加工时除去 |
总计 | 204.20mg | 99.186 |
最后隔离层: | 1.54mg | 0.748 |
羟丙基甲基纤维素,USP 2910,6 cps | 1.54mg | 0.748 |
纯化水,USP/BP/EP | 18.99mg* | *在加工时除去 |
总计 | 205.74mg | 99.934 |
滑石粉,USP,Altalc 500V | 0.14mg | 0.068 |
总计 | 205.88mg | 100.002 |
PK参数 | 供试品/参照品GM比 | 比例的90%CI* |
AUC | 90 | 84-96 |
AUCT | 89 | 84-95 |
Cmax | 62 | 56-70 |
PK参数 | 供试品/参照品GM比 | 比例的90%CI |
AUC | 94 | 88-100 |
AUCT | 94 | 88-100 |
Cmax | 66 | 67-74 |
Claims (30)
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US50781003P | 2003-10-01 | 2003-10-01 | |
US60/507,810 | 2003-10-01 | ||
PCT/US2004/033058 WO2005032513A2 (en) | 2003-10-01 | 2004-09-30 | Pantoprazole multiparticulate formulations |
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Cited By (3)
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Families Citing this family (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PE20050150A1 (es) | 2003-05-08 | 2005-03-22 | Altana Pharma Ag | Una forma de dosificacion que contiene (s)-pantoprazol como ingrediente activo |
CL2004000983A1 (es) | 2003-05-08 | 2005-03-04 | Altana Pharma Ag | Composicion farmaceutica oral en forma de tableta que comprende a pantoprazol magnetico dihidratado, en donde la forma de tableta esta compuesto por un nucleo, una capa intermedia y una capa exterior; y uso de la composicion farmaceutica en ulceras y |
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WO2006009602A2 (en) | 2004-06-16 | 2006-01-26 | Tap Pharmaceutical Products, Inc. | Multiple ppi dosage form |
NZ556673A (en) | 2005-02-03 | 2010-03-26 | Gen Hospital Corp | Method for treating gefitinib and/or erlotinib resistant cancer with an EGFR inhibitor |
DE102005032806A1 (de) | 2005-07-12 | 2007-01-18 | Röhm Gmbh | Verwendung eines teilneutralisierten, anionischen (Meth)acrylat-Copolymers als Überzug für die Herstellung einer Arzneiform mit einer Wirkstofffreisetzung bei erniedrigten pH-Werten |
EP1747776A1 (en) * | 2005-07-29 | 2007-01-31 | KRKA, tovarna zdravil, d.d., Novo mesto | Pharmaceutical composition comprising granular pantoprazole |
BRPI0618042A2 (pt) | 2005-11-04 | 2011-08-16 | Wyeth Corp | usos de uma rapamicina e de uma herceptina, produto, pacote farmacêutico, e, composição farmacêutica |
EP2010162A4 (en) * | 2006-04-03 | 2013-01-09 | Isa Odidi | COMPOSITION FOR DISPOSING A MEDICINAL PRODUCT |
US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
ITFI20070253A1 (it) * | 2007-11-09 | 2009-05-10 | Valpharma Internat S P A | Formulazioni farmaceutiche per la somministrazione di ipp. |
ES2692769T3 (es) | 2008-06-17 | 2018-12-05 | Wyeth Llc | Combinaciones antineoplásicas que contienen HKI-272 y vinorelbina |
SG10201702382RA (en) | 2008-08-04 | 2017-05-30 | Wyeth Llc | Antineoplastic combinations of 4-anilino-3-cyanoquinolines and capecitabine |
SG174382A1 (en) | 2009-04-06 | 2011-11-28 | Wyeth Llc | Treatment regimen utilizing neratinib for breast cancer |
US20110066141A1 (en) * | 2009-09-11 | 2011-03-17 | Cook Incorporated | Implantable medical device having an anti-gastric distress agent |
KR101787481B1 (ko) | 2010-10-21 | 2017-10-18 | 롯데정밀화학 주식회사 | 장용성 경질 캡슐용 조성물 및 상기 조성물을 사용하여 제조된 장용성 경질 캡슐 |
US9532952B2 (en) | 2011-01-28 | 2017-01-03 | Physician's Seal, LLC | Controlled-release compositions of melatonin combined with sedative and/or analgesic ingredients |
WO2012103411A2 (en) | 2011-01-28 | 2012-08-02 | Zx Pharma, Llc | Controlled-release melatonin composition and related methods |
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JP2015522653A (ja) * | 2012-07-26 | 2015-08-06 | ルピン・リミテッドLupin Limited | プロトンポンプ阻害剤の医薬組成物 |
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CN105263480B (zh) | 2013-04-23 | 2018-08-28 | Zx制药有限责任公司 | 肠溶包衣的多微粒控释薄荷油组合物和相关方法 |
AR096628A1 (es) | 2013-06-17 | 2016-01-20 | Raptor Pharmaceuticals Inc | Formulación en perlas de cisteamina de liberación retardada y métodos de preparación y uso de ella |
US10143665B2 (en) | 2015-11-17 | 2018-12-04 | Horizon Orphan Llc | Methods for storing cysteamine formulations and related methods of treatment |
US10537562B2 (en) * | 2016-10-06 | 2020-01-21 | Jubilant Generics Limited | Delayed release pharmaceutical composition of pantoprazole and process for formulation thereof |
WO2020104955A1 (en) * | 2018-11-20 | 2020-05-28 | Dr. Reddy’S Laboratories Limited | Pharmaceutical compositions of acotiamide and proton pump inhibitor |
Family Cites Families (102)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US597903A (en) * | 1898-01-25 | Lubricator | ||
US635184A (en) * | 1898-06-22 | 1899-10-17 | Harry Gregg Price | Fastener for shoes, &c. |
US3065143A (en) | 1960-04-19 | 1962-11-20 | Richardson Merrell Inc | Sustained release tablet |
SE7804231L (sv) * | 1978-04-14 | 1979-10-15 | Haessle Ab | Magsyrasekretionsmedel |
SE8301182D0 (sv) | 1983-03-04 | 1983-03-04 | Haessle Ab | Novel compounds |
IL75400A (en) | 1984-06-16 | 1988-10-31 | Byk Gulden Lomberg Chem Fab | Dialkoxypyridine methyl(sulfinyl or sulfonyl)benzimidazoles,processes for the preparation thereof and pharmaceutical compositions containing the same |
FR2566871B1 (fr) | 1984-06-27 | 1986-12-19 | Pont A Mousson | Joint d'etancheite pour vanne a obturateur rotatif et son procede de fabrication |
IL72684A (en) | 1984-08-14 | 1989-02-28 | Israel State | Pharmaceutical compositions for controlled transdermal delivery of cholinergic or anticholinergic basic drugs |
JPS6150978A (ja) | 1984-08-16 | 1986-03-13 | Takeda Chem Ind Ltd | ピリジン誘導体およびその製造法 |
IL76839A (en) * | 1984-10-31 | 1988-08-31 | Byk Gulden Lomberg Chem Fab | Picoline derivatives,processes for the preparation thereof and pharmaceutical compositions containing the same |
US5433959A (en) | 1986-02-13 | 1995-07-18 | Takeda Chemical Industries, Ltd. | Stabilized pharmaceutical composition |
SE8601624D0 (sv) | 1986-04-11 | 1986-04-11 | Haessle Ab | New pharmaceutical preparations |
GB2189699A (en) | 1986-04-30 | 1987-11-04 | Haessle Ab | Coated acid-labile medicaments |
GB2189698A (en) * | 1986-04-30 | 1987-11-04 | Haessle Ab | Coated omeprazole tablets |
FI90544C (fi) | 1986-11-13 | 1994-02-25 | Eisai Co Ltd | Menetelmä lääkeaineina käyttökelpoisten 2-pyridin-2-yyli-metyylitio- ja sulfinyyli-1H-bensimidatsolijohdannaisten valmistamiseksi |
DE69011645T2 (de) | 1989-11-29 | 1995-01-12 | Toa Eiyo Ltd | Cycloheptenopyridinderivate, Verfahren zu ihrer Herstellung und diese enthaltende Antiulkusmitteln. |
US5273758A (en) | 1991-03-18 | 1993-12-28 | Sandoz Ltd. | Directly compressible polyethylene oxide vehicle for preparing therapeutic dosage forms |
TW209174B (zh) | 1991-04-19 | 1993-07-11 | Takeda Pharm Industry Co Ltd | |
YU48263B (sh) * | 1991-06-17 | 1997-09-30 | Byk Gulden Lomberg Chemische Fabrik Gmbh. | Postupak za dobijanje farmaceutskog preparata na bazi pantoprazola |
IT1251153B (it) | 1991-08-06 | 1995-05-04 | Vectorpharma Int | Composizioni farmaceutiche solide per somministrazione orale aventi proungata residenza gastrica |
US5178867A (en) | 1991-08-19 | 1993-01-12 | Alza Corporation | Dosage form for delivering drug in short-time period |
US5225202A (en) | 1991-09-30 | 1993-07-06 | E. R. Squibb & Sons, Inc. | Enteric coated pharmaceutical compositions |
AU4513393A (en) | 1992-07-17 | 1994-02-14 | Astra Aktiebolag | Pharmaceutical composition containing antiulcer agent |
US5260069A (en) | 1992-11-27 | 1993-11-09 | Anda Sr Pharmaceuticals Inc. | Pulsatile particles drug delivery system |
EP0695123A4 (en) | 1993-04-27 | 1996-09-11 | Sepracor Inc | METHOD AND COMPOSITIONS FOR TREATING GASTRICAL FAULTS USING OPTICALLY PURE PANTOPRAZOLS |
SE9301489D0 (sv) | 1993-04-30 | 1993-04-30 | Ab Astra | Veterinary composition |
SI1078628T1 (sl) | 1994-07-08 | 2009-04-30 | Astrazeneca Ab | Večenotska tabletirana dozirna oblika |
SE9402431D0 (sv) * | 1994-07-08 | 1994-07-08 | Astra Ab | New tablet formulation |
US5639754A (en) * | 1994-07-12 | 1997-06-17 | Janssen Pharmaceutica N.V. | Urea and thiourea derivatives of azolones |
ES2094694B1 (es) | 1995-02-01 | 1997-12-16 | Esteve Quimica Sa | Nueva formulacion farmaceuticamente estable de un compuesto de bencimidazol y su proceso de obtencion. |
SE9500422D0 (sv) | 1995-02-06 | 1995-02-06 | Astra Ab | New oral pharmaceutical dosage forms |
SE9500478D0 (sv) | 1995-02-09 | 1995-02-09 | Astra Ab | New pharmaceutical formulation and process |
US6132768A (en) | 1995-07-05 | 2000-10-17 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Oral pharmaceutical composition with delayed release of active ingredient for reversible proton pump inhibitors |
US5945124A (en) | 1995-07-05 | 1999-08-31 | Byk Gulden Chemische Fabrik Gmbh | Oral pharmaceutical composition with delayed release of active ingredient for pantoprazole |
PL186605B1 (pl) * | 1995-09-21 | 2004-01-30 | Pharma Pass Llc | Tabletka lub mikrotabletka zawierająca rdzeń posiadający jako kwasolabilny składnik aktywny omeprazol oraz sposób wytwarzania tabletek lub mikrotabletek zawierających rdzeń posiadający jako kwasolabilny składnik aktywny omeprazol |
US6699885B2 (en) * | 1996-01-04 | 2004-03-02 | The Curators Of The University Of Missouri | Substituted benzimidazole dosage forms and methods of using same |
US6489346B1 (en) | 1996-01-04 | 2002-12-03 | The Curators Of The University Of Missouri | Substituted benzimidazole dosage forms and method of using same |
US6645988B2 (en) | 1996-01-04 | 2003-11-11 | Curators Of The University Of Missouri | Substituted benzimidazole dosage forms and method of using same |
SE9600070D0 (sv) * | 1996-01-08 | 1996-01-08 | Astra Ab | New oral pharmaceutical dosage forms |
SE9600072D0 (sv) * | 1996-01-08 | 1996-01-08 | Astra Ab | New oral formulation of two active ingredients II |
IT1282650B1 (it) | 1996-02-19 | 1998-03-31 | Jagotec Ag | Compressa farmaceutica,caratterizzata da elevato aumento di volume a contatto con liquidi biologici |
US6245351B1 (en) | 1996-03-07 | 2001-06-12 | Takeda Chemical Industries, Ltd. | Controlled-release composition |
WO1997047285A1 (en) | 1996-06-10 | 1997-12-18 | Depomed, Inc. | Gastric-retentive oral controlled drug delivery system with enhanced retention properties |
SE9602442D0 (sv) | 1996-06-20 | 1996-06-20 | Astra Ab | Administration of pharmaceuticals |
US6623759B2 (en) * | 1996-06-28 | 2003-09-23 | Astrazeneca Ab | Stable drug form for oral administration with benzimidazole derivatives as active ingredient and process for the preparation thereof |
US20010053387A1 (en) | 1997-05-23 | 2001-12-20 | Hamied Yusuf Khwaja | Benzimidazole pharmaceutical composition and process of prepatation |
DE19732903A1 (de) | 1997-07-30 | 1999-02-04 | Falk Pharma Gmbh | Pellet-Formulierung zur Behandlung des Intestinaltraktes |
EP1017370B1 (en) * | 1997-09-11 | 2003-10-29 | Nycomed Danmark ApS | MODIFIED RELEASE MULTIPLE-UNITS COMPOSITIONS OF NON-STEROID ANTI-INFLAMMATORY DRUG SUBSTANCES (NSAIDs) |
US6296876B1 (en) * | 1997-10-06 | 2001-10-02 | Isa Odidi | Pharmaceutical formulations for acid labile substances |
KR20010031034A (ko) | 1997-10-09 | 2001-04-16 | 페리오 프로덕츠 리미티드 | 전체 방출을 지연시키는 위장의 약물 송달 시스템 |
US6096340A (en) * | 1997-11-14 | 2000-08-01 | Andrx Pharmaceuticals, Inc. | Omeprazole formulation |
US6602522B1 (en) | 1997-11-14 | 2003-08-05 | Andrx Pharmaceuticals L.L.C. | Pharmaceutical formulation for acid-labile compounds |
DE19752843C2 (de) | 1997-11-28 | 2003-01-09 | Byk Gulden Lomberg Chem Fab | Arzneimittelzubereitung in Tabletten- oder Pelletform für Pantoprazol und Omeprazol |
DK1037607T3 (da) * | 1997-12-08 | 2004-06-21 | Altana Pharma Ag | Hidtil ukendt suppositoriumsform, der omfatter en syrelabil aktiv forbindelse |
SE9704869D0 (sv) | 1997-12-22 | 1997-12-22 | Astra Ab | New pharmaceutical formulaton II |
SE9704870D0 (sv) * | 1997-12-22 | 1997-12-22 | Astra Ab | New pharmaceutical formulation I |
DK173431B1 (da) | 1998-03-20 | 2000-10-23 | Gea Farmaceutisk Fabrik As | Farmaceutisk formulering omfattende en 2-[[(2-pyridinyl)methyl]sulfinyl]benzimidazol med anti-ulcusaktivitet samt fremgangs |
KR100627614B1 (ko) | 1998-04-20 | 2006-09-25 | 에자이 가부시키가이샤 | 안정화된 벤즈이미다졸계 화합물 함유 조성물로 이루어지는 의약제제 |
ZA9810765B (en) | 1998-05-28 | 1999-08-06 | Ranbaxy Lab Ltd | Stable oral pharmaceutical composition containing a substituted pyridylsulfinyl benzimidazole. |
BR9912937A (pt) * | 1998-08-10 | 2001-05-08 | Partnership Of Michael E Garst | Pró-drogas de inibidores de bomba de prótons |
US6093734A (en) | 1998-08-10 | 2000-07-25 | Partnership Of Michael E. Garst, George Sachs, And Jai Moo Shin | Prodrugs of proton pump inhibitors |
DK1105105T3 (da) * | 1998-08-12 | 2006-07-17 | Altana Pharma Ag | Oral administrationsform til pyridin-2-ylmethylsulfinyl-1H-benzimidazoler |
US6531152B1 (en) | 1998-09-30 | 2003-03-11 | Dexcel Pharma Technologies Ltd. | Immediate release gastrointestinal drug delivery system |
US6248363B1 (en) * | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
ES2168043B1 (es) | 1999-09-13 | 2003-04-01 | Esteve Labor Dr | Forma farmaceutica solida oral de liberacion modificada que contiene un compuesto de bencimidazol labil en medio acido. |
WO2001028559A1 (fr) | 1999-10-20 | 2001-04-26 | Eisai Co., Ltd. | Procede de stabilisation de composes benzimidazoles |
SE9903831D0 (sv) | 1999-10-22 | 1999-10-22 | Astra Ab | Formulation of substituted benzimidazoles |
ATE297194T1 (de) | 1999-12-16 | 2005-06-15 | Medinfar Produtos Farmaceutico | Neue stabile mehreinheitliche substituierte benzimidazole enthaltende pharmazeutische präparate |
DE60015607T2 (de) * | 2000-02-24 | 2005-11-10 | Kopran Research Laboratories Ltd. | Oral verabreichbare säurebeständige geschwürbehandelnde benzimidazolderivate |
US6346269B1 (en) | 2000-05-08 | 2002-02-12 | Standard Chem. & Pharm. Co., Ltd. | Method for preparing an oral formulation containing acid-sensitive drugs and oral formulation made thereby |
US6749867B2 (en) * | 2000-11-29 | 2004-06-15 | Joseph R. Robinson | Delivery system for omeprazole and its salts |
PL367686A1 (en) | 2001-07-16 | 2005-03-07 | Astrazeneca Ab | Pharmaceutical formulation comprising a proton pump inhibitor and antacids |
US6617388B2 (en) * | 2001-10-12 | 2003-09-09 | Atofina Chemicals, Inc. | Curing catalyst |
CA2463690C (en) | 2001-10-17 | 2011-08-23 | Takeda Chemical Industries, Ltd. | Granules containing acid-unstable chemical in large amount |
HUP0104960A2 (hu) * | 2001-11-15 | 2003-07-28 | Attila Murlasits | Berendezés és eljárás elektromos fogyasztók működésének szabályzására |
ES2198195B1 (es) | 2001-12-18 | 2004-10-01 | Laboratorios Del Dr. Esteve, S.A. | Forma de dosificacion farmaceutica oral comprimida, con recubrimiento enterico, que contiene un compuesto de bencimidazol labil en medio acido. |
JP2005535602A (ja) * | 2002-05-31 | 2005-11-24 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 新規コナゾール結晶形及び関連方法、医薬組成物及び方法 |
WO2004004682A2 (en) | 2002-07-02 | 2004-01-15 | Laboratorios S.A.L.V.A.T., S.A. | Stable oily suspension of microgranules |
US20040005362A1 (en) | 2002-07-03 | 2004-01-08 | Rajneesh Taneja | Liquid dosage forms of acid labile drugs |
US20040028737A1 (en) | 2002-08-12 | 2004-02-12 | Kopran Research Laboratories Limited | Enteric coated stable oral pharmaceutical composition of acid unstable drug and process for preparing the same |
ES2534713T3 (es) | 2002-10-16 | 2015-04-27 | Takeda Pharmaceutical Company Limited | Preparaciones sólidas estables |
AU2003277689A1 (en) * | 2002-11-02 | 2004-06-07 | Kyung-Lim Lee | Composition for preventing secretion of immunoglobulin e-dependent histamine releasing factor |
US20040146558A1 (en) | 2003-01-28 | 2004-07-29 | Kyowa Pharmaceutical Co., Ltd. | Oral enteric-coated preparation |
EP1594479A1 (en) | 2003-01-31 | 2005-11-16 | Ranbaxy Laboratories Limited | Stable oral benzimidazole compositions and processes for their preparation |
US20050220870A1 (en) * | 2003-02-20 | 2005-10-06 | Bonnie Hepburn | Novel formulation, omeprazole antacid complex-immediate release for rapid and sustained suppression of gastric acid |
WO2004089333A2 (en) | 2003-02-28 | 2004-10-21 | Cadila Healthcare Limited | A stable benzimidazole formulation |
EP1602362B1 (en) | 2003-03-12 | 2016-09-28 | Takeda Pharmaceutical Company Limited | Drug composition having active ingredient adhered at high concentration to spherical core |
US20060235053A1 (en) | 2003-05-06 | 2006-10-19 | Atlanta Pharma Ag | Agents for the treatment of lower abdominal disorders |
CL2004000983A1 (es) | 2003-05-08 | 2005-03-04 | Altana Pharma Ag | Composicion farmaceutica oral en forma de tableta que comprende a pantoprazol magnetico dihidratado, en donde la forma de tableta esta compuesto por un nucleo, una capa intermedia y una capa exterior; y uso de la composicion farmaceutica en ulceras y |
PE20050150A1 (es) * | 2003-05-08 | 2005-03-22 | Altana Pharma Ag | Una forma de dosificacion que contiene (s)-pantoprazol como ingrediente activo |
AU2003245033A1 (en) | 2003-05-08 | 2004-11-26 | Podili Khadgapathi | An improved and stable pharmaceutical composition containing substituted benzimidazoles and a process for its preparation |
JP2007522086A (ja) | 2003-07-11 | 2007-08-09 | アストラゼネカ・アクチエボラーグ | プロトンポンプインヒビターを含有する固形組成物 |
RU2375048C2 (ru) | 2003-07-17 | 2009-12-10 | Д-Р Редди'С Лабораторис Инк. | Фармацевтическая композиция с набухающим покрытием |
PL1651217T3 (pl) * | 2003-07-23 | 2008-07-31 | Nycomed Gmbh | Sole alkaiczne inhibitorów pompy protonowej |
WO2005011637A1 (ja) | 2003-08-04 | 2005-02-10 | Eisai Co., Ltd. | 用時分散型製剤 |
TWI372066B (en) * | 2003-10-01 | 2012-09-11 | Wyeth Corp | Pantoprazole multiparticulate formulations |
ITMI20040802A1 (it) * | 2004-04-23 | 2004-07-23 | Dinamite Dipharma S P A In For | Polimorfi di pantoprazolo sale sodico e procedimento per la loro preparazione |
SI1746980T1 (sl) | 2004-05-07 | 2012-03-30 | Nycomed Gmbh | Farmacevtska dozirna oblika ki obsega pelete kot tudi postopek za njeno pripravo |
CA2469427A1 (en) * | 2004-06-01 | 2005-12-01 | Pharmascience Inc. | Dry mixed dosage form containing benzimidazole derivatives |
US20060165797A1 (en) | 2005-01-12 | 2006-07-27 | Pozen Inc. | Dosage form for treating gastrointestinal disorders |
KR100692391B1 (ko) * | 2005-03-03 | 2007-03-09 | 재단법인서울대학교산학협력재단 | 역대칭 자기장 구조를 이용하여 봉부재에서 굽힘 진동을 발생 및 측정할 수 있는 전자기 음향 변환기 |
US7803817B2 (en) * | 2005-05-11 | 2010-09-28 | Vecta, Ltd. | Composition and methods for inhibiting gastric acid secretion |
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