RU2001104423A - TABLET WITH IMMEDIATE RELEASE - Google Patents

TABLET WITH IMMEDIATE RELEASE

Info

Publication number
RU2001104423A
RU2001104423A RU2001104423/14A RU2001104423A RU2001104423A RU 2001104423 A RU2001104423 A RU 2001104423A RU 2001104423/14 A RU2001104423/14 A RU 2001104423/14A RU 2001104423 A RU2001104423 A RU 2001104423A RU 2001104423 A RU2001104423 A RU 2001104423A
Authority
RU
Russia
Prior art keywords
oral preparation
preparation according
thrombin inhibitor
preparation
immediate release
Prior art date
Application number
RU2001104423/14A
Other languages
Russian (ru)
Other versions
RU2252751C2 (en
Inventor
Сигбрит ФОРСМАН
Кристер КАРЛССОН
Магнус Карлссон
Original Assignee
Астразенека Аб
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from SE9802973A external-priority patent/SE9802973D0/en
Application filed by Астразенека Аб filed Critical Астразенека Аб
Publication of RU2001104423A publication Critical patent/RU2001104423A/en
Application granted granted Critical
Publication of RU2252751C2 publication Critical patent/RU2252751C2/en

Links

Claims (12)

1. Пероральный препарат низкомолекулярного ингибитора тромбина на основе пептида с немедленным высвобождением в твердой форме, имеющего зависимую от рН растворимость, отличающийся тем, что этот препарат содержит наполнитель или комбинацию наполнителей, обладающих разрыхляющими свойствами, в количестве более чем 35 мас. %/мас. препарата, выбранных из группы, состоящей из целлюлозы самой по себе и крахмала самого по себе.1. An oral preparation of a low molecular weight thrombin inhibitor based on a peptide based on immediate release in solid form having a pH-dependent solubility, characterized in that the preparation contains a filler or a combination of fillers having loosening properties in an amount of more than 35 wt. % / wt. a drug selected from the group consisting of cellulose per se and starch per se. 2. Пероральный препарат по п. 1, отличающийся тем, что этот препарат возможно содержит сахар, разрыхлитель, связывающее вещество и/или смазывающее вещество. 2. An oral preparation according to claim 1, characterized in that the preparation possibly contains sugar, a disintegrant, a binder and / or a lubricant. 3. Пероральный препарат по п. 1 или 2, отличающийся тем, что ингибитор тромбина имеет размер частиц менее чем 300 мкм, предпочтительно менее чем 150 мкм, и предпочтительный средний размер частиц менее чем 80 мкм. 3. An oral preparation according to claim 1 or 2, characterized in that the thrombin inhibitor has a particle size of less than 300 microns, preferably less than 150 microns, and a preferred average particle size of less than 80 microns. 4. Пероральный препарат по любому из пп. 1-3, отличающийся тем, что он содержит комбинацию микрокристаллической целлюлозы и маннита. 4. The oral preparation according to any one of paragraphs. 1-3, characterized in that it contains a combination of microcrystalline cellulose and mannitol. 5. Пероральный препарат по п. 4, отличающийся тем, что микрокристаллическая целлюлоза составляет 50-90% (мас. /мас. ) препарата. 5. An oral preparation according to claim 4, characterized in that microcrystalline cellulose comprises 50-90% (w / w) of the preparation. 6. Пероральный препарат по п. 4, отличающийся тем, что маннит составляет 0-15% (мас. /мас. ) препарата. 6. An oral preparation according to claim 4, characterized in that mannitol is 0-15% (w / w) of the drug. 7. Пероральный препарат по любому из пп. 1-6, в котором ингибитором тромбина является этиловый эфир [S-(R*, S*)] -N-[1-циклогексил-2-[2-[[[[4-[(гидроксиимино)аминометил] фенил] метил] амино] карбонил] -1-азетидинил] -2-оксоэтил] глицина. 7. An oral preparation according to any one of paragraphs. 1-6, wherein the thrombin inhibitor is [S- (R *, S *)] -N- [1-cyclohexyl-2- [2 - [[[[4 - [(hydroxyimino) aminomethyl] phenyl] methyl) ethyl ester ] amino] carbonyl] -1-azetidinyl] -2-oxoethyl] glycine. 8. Пероральный препарат по любому из пп. 1-7 для применения в терапии. 8. An oral preparation according to any one of paragraphs. 1-7 for use in therapy. 9. Применение низкомолекулярного ингибитора тромбина на основе пептида, наполнителя или комбинации наполнителей, обладающих разрыхляющими свойствами, в количестве более чем 35 мас. %/мас. , по п. 1 в приготовлении препарата для профилактики и/или лечения тромбоэмболии. 9. The use of a low molecular weight thrombin inhibitor based on a peptide, excipient or combination of excipients having loosening properties, in an amount of more than 35 wt. % / wt. , p. 1 in the preparation of a drug for the prevention and / or treatment of thromboembolism. 10. Способ профилактики и/или лечения тромбоэмболии, при котором млекопитающему, нуждающемуся в таком лечении, вводят терапевтически эффективное количество препарата по п. 1. 10. A method for the prevention and / or treatment of thromboembolism, in which a mammal in need of such treatment is administered a therapeutically effective amount of a preparation according to claim 1. 11. Способ приготовления перорального препарата с немедленным высвобождением по п. 1, отличающийся тем, что указанное приготовление осуществляют путем прямого прессования или влажной грануляции. 11. A method of preparing an immediate release oral preparation according to claim 1, characterized in that said preparation is carried out by direct compression or wet granulation. 12. Применение наполнителя, выбранного из группы, состоящей из производного целлюлозы и производного крахмала, возможно сахара, разрыхлителя, связывающего вещества и/или смазывающего вещества в приготовлении перорального препарата с немедленным высвобождением, содержащего низкомолекулярный ингибитор тромбина на основе пептида, имеющий зависимую от рН растворимость. 12. The use of an excipient selected from the group consisting of a cellulose derivative and a starch derivative, possibly sugar, a disintegrant, a binder and / or a lubricant in the preparation of an immediate release oral preparation containing a low molecular weight peptide-based thrombin inhibitor having a pH-dependent solubility .
RU2001104423/15A 1998-09-03 1999-08-27 Immediate-released tablet RU2252751C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE9802973-9 1998-09-03
SE9802973A SE9802973D0 (en) 1998-09-03 1998-09-03 Immediate release tablet

Publications (2)

Publication Number Publication Date
RU2001104423A true RU2001104423A (en) 2003-01-20
RU2252751C2 RU2252751C2 (en) 2005-05-27

Family

ID=20412467

Family Applications (2)

Application Number Title Priority Date Filing Date
RU2001104423/15A RU2252751C2 (en) 1998-09-03 1999-08-27 Immediate-released tablet
RU2005100986/15A RU2005100986A (en) 1998-09-03 2005-01-19 TABLET WITH IMMEDIATE RELEASE

Family Applications After (1)

Application Number Title Priority Date Filing Date
RU2005100986/15A RU2005100986A (en) 1998-09-03 2005-01-19 TABLET WITH IMMEDIATE RELEASE

Country Status (32)

Country Link
US (3) US6521253B1 (en)
EP (2) EP1527787A1 (en)
JP (2) JP4026678B2 (en)
KR (2) KR100696350B1 (en)
CN (3) CN1544088A (en)
AR (1) AR029313A1 (en)
AT (1) ATE286385T1 (en)
AU (1) AU746129B2 (en)
BR (1) BR9913400A (en)
CA (1) CA2341397C (en)
CZ (1) CZ300830B6 (en)
DE (1) DE69923074T2 (en)
EE (1) EE200100134A (en)
ES (1) ES2234296T3 (en)
HU (1) HU227278B1 (en)
ID (1) ID29629A (en)
IL (2) IL141439A0 (en)
IS (1) IS5869A (en)
MY (1) MY124359A (en)
NO (1) NO20011085L (en)
NZ (2) NZ539749A (en)
PL (1) PL195603B1 (en)
PT (1) PT1109537E (en)
RU (2) RU2252751C2 (en)
SA (1) SA99200683B1 (en)
SE (1) SE9802973D0 (en)
SK (1) SK285507B6 (en)
TR (2) TR200100666T2 (en)
TW (1) TW561056B (en)
UA (1) UA75567C2 (en)
WO (1) WO2000013671A1 (en)
ZA (1) ZA200101762B (en)

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