HRP20240030T1 - Nazalni sastav tapentadola - Google Patents
Nazalni sastav tapentadola Download PDFInfo
- Publication number
- HRP20240030T1 HRP20240030T1 HRP20240030TT HRP20240030T HRP20240030T1 HR P20240030 T1 HRP20240030 T1 HR P20240030T1 HR P20240030T T HRP20240030T T HR P20240030TT HR P20240030 T HRP20240030 T HR P20240030T HR P20240030 T1 HRP20240030 T1 HR P20240030T1
- Authority
- HR
- Croatia
- Prior art keywords
- tapentadol
- unit dose
- humans
- composition
- value
- Prior art date
Links
- KWTWDQCKEHXFFR-SMDDNHRTSA-N tapentadol Chemical compound CN(C)C[C@H](C)[C@@H](CC)C1=CC=CC(O)=C1 KWTWDQCKEHXFFR-SMDDNHRTSA-N 0.000 title claims 27
- 229960005126 tapentadol Drugs 0.000 title claims 27
- 239000000203 mixture Substances 0.000 title claims 22
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012458 free base Substances 0.000 claims 6
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 235000019264 food flavour enhancer Nutrition 0.000 claims 2
- 235000003599 food sweetener Nutrition 0.000 claims 2
- 230000003232 mucoadhesive effect Effects 0.000 claims 2
- 239000003755 preservative agent Substances 0.000 claims 2
- 230000002335 preservative effect Effects 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 239000003765 sweetening agent Substances 0.000 claims 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 1
- 235000014749 Mentha crispa Nutrition 0.000 claims 1
- 244000024873 Mentha crispa Species 0.000 claims 1
- 239000004384 Neotame Substances 0.000 claims 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 1
- 239000004376 Sucralose Substances 0.000 claims 1
- 239000008365 aqueous carrier Substances 0.000 claims 1
- 229960000686 benzalkonium chloride Drugs 0.000 claims 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group 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 1
- HLIAVLHNDJUHFG-HOTGVXAUSA-N neotame Chemical compound CC(C)(C)CCN[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 HLIAVLHNDJUHFG-HOTGVXAUSA-N 0.000 claims 1
- 235000019412 neotame Nutrition 0.000 claims 1
- 108010070257 neotame Proteins 0.000 claims 1
- 229960000502 poloxamer Drugs 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical group 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 1
- 235000019408 sucralose Nutrition 0.000 claims 1
Classifications
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/186—Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- 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
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Engineering & Computer Science (AREA)
- Otolaryngology (AREA)
- Emergency Medicine (AREA)
- Inorganic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Claims (14)
1. Intranazalni sastav za upotrebu kod ljudi koji sadrži tapentadol ili njegovu farmaceutski prihvatljivu sol i barem jedan nazalni nosač; pri čemu jedinična doza navedenog sastava sadrži tapentadol ili farmaceutski prihvatljivu sol u količini koja je ekvivalentna oko 19,3 mg slobodne baze tapentadola pri čemu je volumen jedinične doze od oko 25 µL do oko 150 µL.
2. Sastav prema patentnom zahtjevu 1, pri čemu je nakon intranazalne primjene kod ljudi srednja Cmax-vrijednost tapentadola postignuta navedenom jediničnom dozom jednaka ili veća od srednje Cmax-vrijednosti tapentadola postignute oralnom primjenom kod ljudi jedne doze sastava s trenutnim otpuštanjem koji sadrži tapentadol ili njegovu farmaceutski prihvatljivu sol u količini koja je ekvivalentna 50 mg slobodne baze tapentadola.
3. Sastav prema patentnom zahtjevu 2, pri čemu je nakon intranazalne primjene kod ljudi, srednja Cmax-vrijednost tapentadola postignuta navedenom jediničnom dozom u rasponu od oko 40 ng/mL do oko 65 ng/mL.
4. Sastav prema patentnom zahtjevu 1, pri čemu je nakon intranazalne primjene kod ljudi, srednja AUCo-6-vrijednost tapentadola postignuta navedenom jediničnom dozom u rasponu od oko 115 hr*ng/mL do oko 182 hr*ng/mL.
5. Sastav prema patentnom zahtjevu 1, pri čemu je nakon intranazalne primjene jedinične doze u svaku nosnicu kod ljudi, srednja Cmax-vrijednost tapentadola postignuta navedenom jediničnom dozom jednaka ili veća od srednja Cmax-vrijednosti tapentadola postignute oralnom primjenom kod ljudi jedne doze sastava s trenutnim otpuštanjem koji sadrži tapentadol ili njegovu farmaceutski prihvatljivu sol u količini koja je ekvivalentna oko 100 mg slobodne baze tapentadola.
6. Sastav prema patentnom zahtjevu 5, pri čemu je nakon intranazalne primjene jedinične doze u svaku nosnicu kod ljudi, srednja Cmax-vrijednost tapentadola postignuta navedenom jediničnom dozom u rasponu od oko 98 ng/mL do oko 155 ng/mL.
7. Sastav prema patentnom zahtjevu 5, pri čemu je nakon intranazalne primjene jedinične doze u svaku nosnicu kod ljudi, srednja AUCo-6-vrijednost tapentadola postignuta navedenom jediničnom dozom u rasponu od oko 230 hr*ng/mL do oko 365 hr*ng/mL.
8. Sastav prema bilo kojem od prethodnih patentnih zahtjeva, pri čemu je nakon intranazalne primjene kod ljudi, srednja Tmax- vrijednost postignuta navedenom jediničnom dozom oko 1 sat ili manje.
9. Sastav prema patentnom zahtjevu 8, pri čemu je nakon intranazalne primjene kod ljudi, srednja Tmax-vrijednosti postignuta navedenom jediničnom dozom oko 0,2 h do oko 0,8 h.
10. Intranazalni sastav koji sadrži tapentadol ili njegovu farmaceutski prihvatljivu sol i barem jedan nazalni nosač; pri čemu jedinična doza navedenog sastava sadrži tapentadol ili njegovu farmaceutski prihvatljivu sol u količini koja je ekvivalentna oko 19,3 mg slobodne baze tapentadola pri čemu je volumen jedinične doze od oko 25 µL do oko 150 µL, za upotrebu u liječenju boli kod ljudi, pri čemu se sastav primjenjuje intranazalno.
11. Sastav za upotrebu prema patentnom zahtjevu 10, pri čemu je nakon intranazalne primjene kod ljudi, srednja Cmax-vrijednost tapentadola postignuta navedenom jediničnom dozom jednaka ili veća od srednje Cmax-vrijednosti tapentadola postignute oralnom primjenom kod ljudi jedne doze sastava s trenutnim otpuštanjem koji sadrži tapentadol ili njegovu farmaceutski prihvatljivu sol u količini koja je ekvivalentna 50 mg slobodne baze tapentadola.
12. Sastav za upotrebu prema patentnom zahtjevu 10, pri čemu je nakon intranazalne primjene jedinične doze u svaku nosnicu kod ljudi, srednja Cmax-vrijednost tapentadola postignuta navedenom jediničnom dozom jednaka ili veća od srednje Cmax-vrijednosti tapentadola postignute oralnom primjenom kod ljudi jedne doze sastava s trenutnim otpuštanjem koji sadrži tapentadol ili njegovu farmaceutski prihvatljivu sol u količini koja je ekvivalentna 100 mg slobodne baze tapentadola.
13. Sastav za upotrebu prema bilo kojem od prethodnih patentnih zahtjeva, pri čemu je nazalni nosač odabran između oko 0,05 do oko 5% w/v mukoadhezivnog sredstva; od oko 0,2 do oko 10,0 % w/v solubilizatora; od oko 0,1 % do oko 1% zaslađivača; od oko 0,01 do oko 1 % w/v konzervansa, od oko 0,01 % w/v do oko 0,5 % w/v sredstva za poboljšanje okusa i dovoljne količine vodenog nosača.
14. Sastav za upotrebu prema patentnom zahtjevu 13, pri čemu je mukoadhezivno sredstvo odabrano između hidroksipropilmetil celuloze i karboksimetil celuloze ili njezine farmaceutski prihvatljive soli, solubilizator sadrži poloxamer, zaslađivač je odabran između sukraloze i neotama, konzervans sadrži benzalkonijev klorid, a sredstvo za poboljšanje okusa sadrži aromu zelene metvice.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201721001203 | 2017-01-11 | ||
| EP18704591.9A EP3568126B1 (en) | 2017-01-11 | 2018-01-10 | Tapentadol nasal composition |
| PCT/IB2018/050148 WO2018130948A1 (en) | 2017-01-11 | 2018-01-10 | Tapentadol nasal composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20240030T1 true HRP20240030T1 (hr) | 2024-03-29 |
Family
ID=61192975
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20240030TT HRP20240030T1 (hr) | 2017-01-11 | 2018-01-10 | Nazalni sastav tapentadola |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP3568126B1 (hr) |
| CN (1) | CN110191708A (hr) |
| BR (1) | BR112019014408A2 (hr) |
| DK (1) | DK3568126T3 (hr) |
| ES (1) | ES2968153T3 (hr) |
| FI (1) | FI3568126T3 (hr) |
| HR (1) | HRP20240030T1 (hr) |
| LT (1) | LT3568126T (hr) |
| PH (1) | PH12019501607A1 (hr) |
| PL (1) | PL3568126T3 (hr) |
| PT (1) | PT3568126T (hr) |
| RS (1) | RS65027B1 (hr) |
| SI (1) | SI3568126T1 (hr) |
| WO (1) | WO2018130948A1 (hr) |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9202464D0 (en) | 1992-02-05 | 1992-03-18 | Danbiosyst Uk | Composition for nasal administration |
| DE4426245A1 (de) | 1994-07-23 | 1996-02-22 | Gruenenthal Gmbh | 1-Phenyl-3-dimethylamino-propanverbindungen mit pharmakologischer Wirkung |
| US20040115133A1 (en) | 2000-05-10 | 2004-06-17 | Wermeling Daniel P. | Intranasal opioid compositions |
| EP1535615A4 (en) | 2002-07-11 | 2010-03-31 | Taiho Pharmaceutical Co Ltd | COMPOSITION FOR THE NASAL ABSORPTION |
| GB0300531D0 (en) * | 2003-01-10 | 2003-02-12 | West Pharm Serv Drug Res Ltd | Pharmaceutical compositions |
| US20100227921A1 (en) * | 2009-03-03 | 2010-09-09 | Shire Llc | Amino acid and peptide carbamate prodrugs of tapentadol and uses thereof |
| WO2013011477A1 (en) * | 2011-07-20 | 2013-01-24 | Torrent Pharmaceuticals Ltd | Pharmaceutical invention of tapentadol |
| CN103735500B (zh) * | 2014-01-28 | 2016-01-20 | 江苏华泽医药科技有限公司 | 盐酸他喷他多注射液及其制备方法 |
| CN110755372A (zh) * | 2014-03-14 | 2020-02-07 | 欧皮安特制药有限公司 | 适于经鼻递送药物产品、用于鼻内给予的药用组合物及其用途 |
-
2018
- 2018-01-10 FI FIEP18704591.9T patent/FI3568126T3/fi active
- 2018-01-10 DK DK18704591.9T patent/DK3568126T3/da active
- 2018-01-10 LT LTEPPCT/IB2018/050148T patent/LT3568126T/lt unknown
- 2018-01-10 EP EP18704591.9A patent/EP3568126B1/en active Active
- 2018-01-10 HR HRP20240030TT patent/HRP20240030T1/hr unknown
- 2018-01-10 SI SI201831051T patent/SI3568126T1/sl unknown
- 2018-01-10 ES ES18704591T patent/ES2968153T3/es active Active
- 2018-01-10 PT PT187045919T patent/PT3568126T/pt unknown
- 2018-01-10 RS RS20231279A patent/RS65027B1/sr unknown
- 2018-01-10 CN CN201880006573.1A patent/CN110191708A/zh active Pending
- 2018-01-10 WO PCT/IB2018/050148 patent/WO2018130948A1/en active Application Filing
- 2018-01-10 PL PL18704591.9T patent/PL3568126T3/pl unknown
- 2018-01-10 BR BR112019014408A patent/BR112019014408A2/pt active Search and Examination
-
2019
- 2019-07-09 PH PH12019501607A patent/PH12019501607A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| LT3568126T (lt) | 2023-12-11 |
| SI3568126T1 (sl) | 2024-03-29 |
| EP3568126A1 (en) | 2019-11-20 |
| EP3568126B1 (en) | 2023-11-01 |
| WO2018130948A1 (en) | 2018-07-19 |
| ES2968153T3 (es) | 2024-05-08 |
| FI3568126T3 (fi) | 2024-01-24 |
| PH12019501607A1 (en) | 2020-03-09 |
| BR112019014408A2 (pt) | 2020-04-28 |
| DK3568126T3 (da) | 2024-01-15 |
| RS65027B1 (sr) | 2024-01-31 |
| PL3568126T3 (pl) | 2024-03-25 |
| CN110191708A (zh) | 2019-08-30 |
| PT3568126T (pt) | 2023-12-19 |
| WO2018130948A9 (en) | 2019-08-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US8859531B2 (en) | Pharmaceutical composition including mometasone furoate and azelastine hydrochloride for nasal administration | |
| US8709508B2 (en) | Xylitol-based anti-mucosal compositions and related methods and compositions | |
| KR101365458B1 (ko) | 구강 투여용 아포모르핀의 약제학적 제형 | |
| JP2009503097A5 (hr) | ||
| ES2556336T3 (es) | Agente terapéutico para la rinitis | |
| WO2007123193A1 (ja) | スプレー用ゲルタイプ皮膚・粘膜付着型製剤およびそれを用いた投与システム | |
| AR055363A1 (es) | Formulaciones farmaceuticas que comprenden un beta 2- agonista de accion prolongada para administracion por nebulizacion | |
| AU2017312811B2 (en) | Liquid naloxone spray | |
| JP2015500285A5 (hr) | ||
| AU2023202420A1 (en) | Compositions, devices, and methods for the treatment of alcohol use disorder | |
| US10617637B2 (en) | Epinephrine spray formulations | |
| US11571384B2 (en) | Epinephrine spray formulations | |
| JP2020516688A (ja) | エピネフリンスプレー製剤 | |
| EP3277283B1 (en) | Sildenafil sublingual spray formulations | |
| HRP20240030T1 (hr) | Nazalni sastav tapentadola | |
| JP2013035792A (ja) | 口腔用組成物 | |
| US10052281B2 (en) | Local administration-type pharmaceutical for improving dysphagia | |
| US10111833B2 (en) | Sildenafil sublingual spray formulations | |
| WO2010119300A3 (en) | Oral suspension of dexamethasone acetate -taste masking composition of dexamethasone | |
| JP2020506930A5 (hr) | ||
| HRP20231706T1 (hr) | Intranazalni pripravak koji sadrži betahistin | |
| JPWO2021127070A5 (hr) | ||
| US8853265B2 (en) | Oral composition to reduce cold symptoms and duration of same | |
| JP2016525147A5 (hr) | ||
| HRP20221525T1 (hr) | Intranazalne formulacije epinefrina i postupci za liječenje bolesti |