HRP20120441T1 - Stabilna farmaceutska smjesa za optimiziranu dopremu inhibitora prianjanja hiv-a - Google Patents
Stabilna farmaceutska smjesa za optimiziranu dopremu inhibitora prianjanja hiv-a Download PDFInfo
- Publication number
- HRP20120441T1 HRP20120441T1 HRP20120441AT HRP20120441T HRP20120441T1 HR P20120441 T1 HRP20120441 T1 HR P20120441T1 HR P20120441A T HRP20120441A T HR P20120441AT HR P20120441 T HRP20120441 T HR P20120441T HR P20120441 T1 HRP20120441 T1 HR P20120441T1
- Authority
- HR
- Croatia
- Prior art keywords
- mixture
- amount
- weight
- hpmc
- mixture according
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title claims 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 claims abstract 22
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract 9
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract 9
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract 9
- 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 9
- 150000001875 compounds Chemical class 0.000 claims abstract 7
- 239000002532 enzyme inhibitor Substances 0.000 claims abstract 3
- 208000030507 AIDS Diseases 0.000 claims 4
- 230000000840 anti-viral effect Effects 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 229940126154 HIV entry inhibitor Drugs 0.000 claims 2
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- 229960005475 antiinfective agent Drugs 0.000 claims 2
- 239000004599 antimicrobial Substances 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000002835 hiv fusion inhibitor Substances 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- 229940121354 immunomodulator Drugs 0.000 claims 2
- 230000002584 immunomodulator Effects 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 102000002260 Alkaline Phosphatase Human genes 0.000 claims 1
- 108020004774 Alkaline Phosphatase Proteins 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 239000007983 Tris buffer Substances 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- -1 phosphate ester Chemical class 0.000 claims 1
- 230000002035 prolonged effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000000377 silicon dioxide Substances 0.000 claims 1
- 235000012239 silicon dioxide Nutrition 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- SWMDAPWAQQTBOG-UHFFFAOYSA-N fostemsavir Chemical compound C1=2N(COP(O)(O)=O)C=C(C(=O)C(=O)N3CCN(CC3)C(=O)C=3C=CC=CC=3)C=2C(OC)=CN=C1N1C=NC(C)=N1 SWMDAPWAQQTBOG-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/062—Organo-phosphoranes without P-C bonds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
Abstract
Farmaceutska smjesa u obliku tablete, sadrži pro-lijek kao fosfatni ester inhibitora prianjanja HIV-a, 1-benzoil-4-[2-[4-metoksi-7-(3-metil-1H-1,2,4-triazol-1-il)-1-[(fosfonoksi)metil]-1H-pirolo[2,3-c]piridin-3-il]-1,2-dioksoetil]-piperazin, i hidroksipropil metil celulozu (HPMC) čija je hidratna viskoznost najmanje oko 100 cP, omogućuje željenu produljenu apsorpciju izvornog spoja kada se da ljudima, omogućuje stabilnost pro-lijeka na alkalnu fosfatazu dok se još nalazi u dozirnom obliku u uvjetima nakon primjene i pri čemu ta smjesa ne sadrži nikakve inhibitore enzima i HPMC je prisutna u količini od 10-50% težinski. Patent sadrži još 14 patentnih zahtjeva.
Claims (15)
1. Farmaceutska smjesa u obliku tablete, sadrži pro-lijek kao fosfatni ester inhibitora prianjanja HIV-a, 1-benzoil-4-[2-[4-metoksi-7-(3-metil-1H-1,2,4-triazol-1-il)-1-[(fosfonoksi)metil]-1H-pirolo[2,3-c]piridin-3-il]-1,2-dioksoetil]-piperazin, i hidroksipropil metil celulozu (HPMC) čija je hidratna viskoznost najmanje oko 100 cP, omogućuje željenu produljenu apsorpciju izvornog spoja kada se da ljudima, omogućuje stabilnost pro-lijeka na alkalnu fosfatazu dok se još nalazi u dozirnom obliku u uvjetima nakon primjene i pri čemu ta smjesa ne sadrži nikakve inhibitore enzima i HPMC je prisutna u količini od 10-50% težinski.
2. Smjesa prema zahtjevu 1, gdje je spoj prisutan u smjesi u količini od 20 - 90% težinski.
3. Smjesa prema zahtjevu 2, gdje je spoj prisutan u smjesi u količini od 50-85% težinski.
4. Smjesa prema zahtjevu 3, gdje je spoj prisutan u smjesi u količini od 60-75% težinski.
5. Smjesa prema zahtjevu 1, gdje je HPMC prisutna u količini od 15-40% težinski.
6. Smjesa prema zahtjevu 5, gdje je HPMC prisutna u količini od 20-30% težinski.
7. Smjesa prema zahtjevu 1, gdje HPMC ima viskoznost od najmanje oko 2000 cP, najmanje oko 3000 cP ili najmanje oko 4000 cP.
8. Smjesa prema zahtjevu 1, koja dalje sadrži jednu ili više dodatnih pomoćnih tvari izabranih iz skupine koja obuhvaća mikrokristaliničnu celulozu, silicijev dioksid i magnezijev stearat.
9. Smjesa prema zahtjevu 8, gdje dodatnih pomoćnih tvari ima u količini od 15% težinski.
10. Smjesa prema zahtjevu 1, gdje viskoznost HMPC ne prelazi oko 120,000 cP.
11. Smjesa prema zahtjevu 1, gdje je spoj u obliku tris soli.
12. Smjesa prema zahtjevu 1, korisna u liječenju HIV infekcije, a dodatno sadrži antivirusnu učinkovitu količinu sredstva za liječenje AIDS-a izabranog iz skupine koja obuhvaća:
(a) AIDS antivirusno sredstvo;
(b) anti-infektivno sredstvo;
(c) imunomodulator; i
(d) drugi inhibitor ulaska HIV-a.
13. Postupak pripreme farmaceutske smjese u obliku tablete koji obuhvaća miješanje spoja 1-benzoil-4-[2-[4-metoksi-7-(3-metil-1H-1,2,4-triazol-1-il)-1-[(fosfonoksi)metil]-1H-pirolo[2,3-c]piridin-3-il]-1,2-dioksoetil]-piperazin zajedno s HPMC čija je viskoznost najmanje oko 2000 cP bez ikakvih inhibitora enzima i komprimiranje te smjese u tabletu.
14. Smjesa prema bilo kojem od zahtjeva 1 do 12 za uporabu u liječenju sisavca zaraženog HIV virusom.
15. Smjesa za uporabu prema zahtjevu 14, obuhvaća primjenu sisavcu antivirusne učinkovite količine smjese, u kombinaciji s antivirusnom učinkovitom količinom sredstva za liječenje AIDS-a izabranih iz skupine koja obuhvaća AIDS antivirusno sredstvo; anti-infektivno sredstvo; imunomodulator; i drugi inhibitor ulaska HIV-a.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9413108P | 2008-09-04 | 2008-09-04 | |
| PCT/US2009/055820 WO2010028108A2 (en) | 2008-09-04 | 2009-09-03 | Stable pharmaceutical composition for optimized delivery of an hiv attachment inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120441T1 true HRP20120441T1 (hr) | 2012-06-30 |
Family
ID=41726353
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120441AT HRP20120441T1 (hr) | 2008-09-04 | 2012-05-23 | Stabilna farmaceutska smjesa za optimiziranu dopremu inhibitora prianjanja hiv-a |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20100056540A1 (hr) |
| EP (1) | EP2323633B1 (hr) |
| JP (1) | JP5638527B2 (hr) |
| CN (1) | CN102143739B (hr) |
| AT (1) | ATE550016T1 (hr) |
| CA (1) | CA2735008C (hr) |
| CY (1) | CY1112816T1 (hr) |
| DK (1) | DK2323633T3 (hr) |
| ES (1) | ES2383149T3 (hr) |
| HR (1) | HRP20120441T1 (hr) |
| NL (1) | NL301118I2 (hr) |
| PL (1) | PL2323633T3 (hr) |
| PT (1) | PT2323633E (hr) |
| SI (1) | SI2323633T1 (hr) |
| SM (1) | SMT201200029B (hr) |
| WO (1) | WO2010028108A2 (hr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9248139B2 (en) | 2011-12-21 | 2016-02-02 | Bristol-Myers Squibb Company | Co-processing method and formulations for HIV attachment inhibitor prodrug compound and excipients |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5023265A (en) * | 1990-06-01 | 1991-06-11 | Schering Corporation | Substituted 1-H-pyrrolopyridine-3-carboxamides |
| US5124327A (en) * | 1991-09-06 | 1992-06-23 | Merck & Co., Inc. | HIV reverse transcriptase |
| JP2686215B2 (ja) * | 1993-04-28 | 1997-12-08 | 信越化学工業株式会社 | 徐放性錠剤 |
| US5424329A (en) * | 1993-08-18 | 1995-06-13 | Warner-Lambert Company | Indole-2-carboxamides as inhibitors of cell adhesion |
| CA2173818A1 (fr) * | 1996-04-10 | 1997-10-11 | Francois Chouinard | Comprime pharmaceutique a liberation controlee contenant un support a base d'amylose reticule et d'hydroxypropylmethylcellulose |
| US6476034B2 (en) * | 2000-02-22 | 2002-11-05 | Bristol-Myers Squibb Company | Antiviral azaindole derivatives |
| US20020061892A1 (en) * | 2000-02-22 | 2002-05-23 | Tao Wang | Antiviral azaindole derivatives |
| AR030557A1 (es) * | 2000-04-14 | 2003-08-27 | Jagotec Ag | Una tableta en multicapa de liberacion controlada y metodo de tratamiento |
| US20040110785A1 (en) * | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US6825201B2 (en) * | 2001-04-25 | 2004-11-30 | Bristol-Myers Squibb Company | Indole, azaindole and related heterocyclic amidopiperazine derivatives |
| US20040063744A1 (en) * | 2002-05-28 | 2004-04-01 | Tao Wang | Indole, azaindole and related heterocyclic 4-alkenyl piperidine amides |
| US7745625B2 (en) * | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| GT200500375A (es) * | 2004-12-20 | 2006-11-28 | Derivados de piperidina y su uso como agentes antiinflamatorios | |
| US7601715B2 (en) * | 2005-06-22 | 2009-10-13 | Bristol-Myers Squibb Company | Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein |
| US7851476B2 (en) * | 2005-12-14 | 2010-12-14 | Bristol-Myers Squibb Company | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine |
| US7807671B2 (en) * | 2006-04-25 | 2010-10-05 | Bristol-Myers Squibb Company | Diketo-piperazine and piperidine derivatives as antiviral agents |
-
2009
- 2009-09-03 AT AT09792207T patent/ATE550016T1/de active
- 2009-09-03 CA CA2735008A patent/CA2735008C/en not_active Expired - Fee Related
- 2009-09-03 CN CN200980135118.2A patent/CN102143739B/zh not_active Expired - Fee Related
- 2009-09-03 EP EP09792207A patent/EP2323633B1/en active Active
- 2009-09-03 ES ES09792207T patent/ES2383149T3/es active Active
- 2009-09-03 WO PCT/US2009/055820 patent/WO2010028108A2/en active Application Filing
- 2009-09-03 DK DK09792207.4T patent/DK2323633T3/da active
- 2009-09-03 US US12/553,310 patent/US20100056540A1/en not_active Abandoned
- 2009-09-03 PL PL09792207T patent/PL2323633T3/pl unknown
- 2009-09-03 PT PT09792207T patent/PT2323633E/pt unknown
- 2009-09-03 JP JP2011526181A patent/JP5638527B2/ja active Active
- 2009-09-03 SI SI200930268T patent/SI2323633T1/sl unknown
-
2012
- 2012-05-23 HR HRP20120441AT patent/HRP20120441T1/hr unknown
- 2012-06-01 CY CY20121100500T patent/CY1112816T1/el unknown
- 2012-06-19 SM SM201200029T patent/SMT201200029B/xx unknown
-
2014
- 2014-12-11 US US14/567,554 patent/US20150158891A1/en not_active Abandoned
-
2021
- 2021-07-26 NL NL301118C patent/NL301118I2/nl unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DK2323633T3 (da) | 2012-07-09 |
| WO2010028108A2 (en) | 2010-03-11 |
| CN102143739B (zh) | 2014-12-17 |
| JP5638527B2 (ja) | 2014-12-10 |
| US20150158891A1 (en) | 2015-06-11 |
| WO2010028108A3 (en) | 2010-09-02 |
| NL301118I2 (nl) | 2022-02-22 |
| CY1112816T1 (el) | 2016-02-10 |
| EP2323633A2 (en) | 2011-05-25 |
| CA2735008C (en) | 2016-11-29 |
| CA2735008A1 (en) | 2010-03-11 |
| PT2323633E (pt) | 2012-05-29 |
| CN102143739A (zh) | 2011-08-03 |
| EP2323633B1 (en) | 2012-03-21 |
| PL2323633T3 (pl) | 2012-08-31 |
| ES2383149T3 (es) | 2012-06-18 |
| ATE550016T1 (de) | 2012-04-15 |
| SI2323633T1 (sl) | 2012-07-31 |
| US20100056540A1 (en) | 2010-03-04 |
| NL301118I1 (hr) | 2021-07-23 |
| JP2012502042A (ja) | 2012-01-26 |
| SMT201200029B (it) | 2012-09-07 |
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