TR201509009A1 - A thin film strip of asenapine - Google Patents
A thin film strip of asenapine Download PDFInfo
- Publication number
- TR201509009A1 TR201509009A1 TR2015/09009A TR201509009A TR201509009A1 TR 201509009 A1 TR201509009 A1 TR 201509009A1 TR 2015/09009 A TR2015/09009 A TR 2015/09009A TR 201509009 A TR201509009 A TR 201509009A TR 201509009 A1 TR201509009 A1 TR 201509009A1
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- Prior art keywords
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- poly
- thin film
- film strip
- asenapine
- Prior art date
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- 239000010409 thin film Substances 0.000 title claims abstract 25
- 229960005245 asenapine Drugs 0.000 title claims 19
- VSWBSWWIRNCQIJ-GJZGRUSLSA-N (R,R)-asenapine Chemical compound O1C2=CC=CC=C2[C@@H]2CN(C)C[C@H]2C2=CC(Cl)=CC=C21 VSWBSWWIRNCQIJ-GJZGRUSLSA-N 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 10
- 150000002148 esters Chemical class 0.000 claims abstract 5
- 229920003169 water-soluble polymer Polymers 0.000 claims abstract 5
- 210000002200 mouth mucosa Anatomy 0.000 claims abstract 3
- -1 polyoxyethylene Polymers 0.000 claims 23
- VSWBSWWIRNCQIJ-HUUCEWRRSA-N (S,S)-asenapine Chemical compound O1C2=CC=CC=C2[C@H]2CN(C)C[C@@H]2C2=CC(Cl)=CC=C21 VSWBSWWIRNCQIJ-HUUCEWRRSA-N 0.000 claims 18
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 12
- 230000000063 preceeding effect Effects 0.000 claims 8
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 5
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 5
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 5
- 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 5
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 4
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 4
- 229920002472 Starch Polymers 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 4
- 239000008107 starch Substances 0.000 claims 4
- 235000019698 starch Nutrition 0.000 claims 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 3
- 239000004373 Pullulan Substances 0.000 claims 3
- 229920001218 Pullulan Polymers 0.000 claims 3
- DOIRQSBPFJWKBE-UHFFFAOYSA-N dibutyl phthalate Chemical compound CCCCOC(=O)C1=CC=CC=C1C(=O)OCCCC DOIRQSBPFJWKBE-UHFFFAOYSA-N 0.000 claims 3
- 239000000796 flavoring agent Substances 0.000 claims 3
- 235000019634 flavors Nutrition 0.000 claims 3
- 229920000159 gelatin Polymers 0.000 claims 3
- 235000019322 gelatine Nutrition 0.000 claims 3
- 229920000609 methyl cellulose Polymers 0.000 claims 3
- 235000010981 methylcellulose Nutrition 0.000 claims 3
- 239000001923 methylcellulose Substances 0.000 claims 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 3
- 235000019423 pullulan Nutrition 0.000 claims 3
- 159000000000 sodium salts Chemical class 0.000 claims 3
- 229940032147 starch Drugs 0.000 claims 3
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 2
- GMDCDXMAFMEDAG-CHHFXETESA-N (S,S)-asenapine maleate Chemical compound OC(=O)\C=C/C(O)=O.O1C2=CC=CC=C2[C@H]2CN(C)C[C@@H]2C2=CC(Cl)=CC=C21 GMDCDXMAFMEDAG-CHHFXETESA-N 0.000 claims 2
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 claims 2
- 108010011485 Aspartame Proteins 0.000 claims 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 2
- 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 2
- 108010010803 Gelatin Proteins 0.000 claims 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 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 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 229920002873 Polyethylenimine Polymers 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- 235000010358 acesulfame potassium Nutrition 0.000 claims 2
- 239000000619 acesulfame-K Substances 0.000 claims 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 2
- 229960001615 asenapine maleate Drugs 0.000 claims 2
- 239000000605 aspartame Substances 0.000 claims 2
- 235000010357 aspartame Nutrition 0.000 claims 2
- 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 2
- 229960003438 aspartame Drugs 0.000 claims 2
- 235000010418 carrageenan Nutrition 0.000 claims 2
- 229920001525 carrageenan Polymers 0.000 claims 2
- 239000000679 carrageenan Substances 0.000 claims 2
- 229940113118 carrageenan Drugs 0.000 claims 2
- 239000008273 gelatin Substances 0.000 claims 2
- 235000011852 gelatine desserts Nutrition 0.000 claims 2
- 229920000591 gum Polymers 0.000 claims 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 2
- 239000001630 malic acid Substances 0.000 claims 2
- 235000011090 malic acid Nutrition 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- 229920003213 poly(N-isopropyl acrylamide) Polymers 0.000 claims 2
- 229920002401 polyacrylamide Polymers 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 229910052708 sodium Inorganic materials 0.000 claims 2
- 239000011734 sodium Substances 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 claims 2
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims 1
- WTDKNKIQGBNMKG-UHFFFAOYSA-M 1-methylpyridin-1-ium;bromide Chemical compound [Br-].C[N+]1=CC=CC=C1 WTDKNKIQGBNMKG-UHFFFAOYSA-M 0.000 claims 1
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 1
- AGBXYHCHUYARJY-UHFFFAOYSA-N 2-phenylethenesulfonic acid Chemical compound OS(=O)(=O)C=CC1=CC=CC=C1 AGBXYHCHUYARJY-UHFFFAOYSA-N 0.000 claims 1
- RSWGJHLUYNHPMX-UHFFFAOYSA-N Abietic-Saeure Natural products C12CCC(C(C)C)=CC2=CCC2C1(C)CCCC2(C)C(O)=O RSWGJHLUYNHPMX-UHFFFAOYSA-N 0.000 claims 1
- 244000215068 Acacia senegal Species 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims 1
- 229920001661 Chitosan Polymers 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- 239000001879 Curdlan Substances 0.000 claims 1
- 229920002558 Curdlan Polymers 0.000 claims 1
- 229920002307 Dextran Polymers 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 229920000896 Ethulose Polymers 0.000 claims 1
- 239000001856 Ethyl cellulose Substances 0.000 claims 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 1
- 239000001859 Ethyl hydroxyethyl cellulose Substances 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 229920003134 Eudragit® polymer Polymers 0.000 claims 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 1
- 239000001828 Gelatine Substances 0.000 claims 1
- 229920002148 Gellan gum Polymers 0.000 claims 1
- 229920002907 Guar gum Polymers 0.000 claims 1
- 229920000084 Gum arabic Polymers 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- WOBHKFSMXKNTIM-UHFFFAOYSA-N Hydroxyethyl methacrylate Chemical compound CC(=C)C(=O)OCCO WOBHKFSMXKNTIM-UHFFFAOYSA-N 0.000 claims 1
- 229920002774 Maltodextrin Polymers 0.000 claims 1
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims 1
- 229920003091 Methocel™ Polymers 0.000 claims 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims 1
- 229920000881 Modified starch Polymers 0.000 claims 1
- 244000046052 Phaseolus vulgaris Species 0.000 claims 1
- 235000010627 Phaseolus vulgaris Nutrition 0.000 claims 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 1
- 229920002504 Poly(2-vinylpyridine-N-oxide) Polymers 0.000 claims 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 1
- KHPCPRHQVVSZAH-HUOMCSJISA-N Rosin Natural products O(C/C=C/c1ccccc1)[C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 KHPCPRHQVVSZAH-HUOMCSJISA-N 0.000 claims 1
- 229920002125 Sokalan® Polymers 0.000 claims 1
- 235000010489 acacia gum Nutrition 0.000 claims 1
- 239000000205 acacia gum Substances 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 239000002269 analeptic agent Substances 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims 1
- 229920001577 copolymer Polymers 0.000 claims 1
- 235000019316 curdlan Nutrition 0.000 claims 1
- 229940078035 curdlan Drugs 0.000 claims 1
- VAYGXNSJCAHWJZ-UHFFFAOYSA-N dimethyl sulfate Chemical compound COS(=O)(=O)OC VAYGXNSJCAHWJZ-UHFFFAOYSA-N 0.000 claims 1
- 235000019325 ethyl cellulose Nutrition 0.000 claims 1
- 229920001249 ethyl cellulose Polymers 0.000 claims 1
- 235000019326 ethyl hydroxyethyl cellulose Nutrition 0.000 claims 1
- 210000000416 exudates and transudate Anatomy 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 235000003599 food sweetener Nutrition 0.000 claims 1
- 235000010492 gellan gum Nutrition 0.000 claims 1
- 239000000216 gellan gum Substances 0.000 claims 1
- 235000010417 guar gum Nutrition 0.000 claims 1
- 239000000665 guar gum Substances 0.000 claims 1
- 229960002154 guar gum Drugs 0.000 claims 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 239000011976 maleic acid Substances 0.000 claims 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 1
- 235000019426 modified starch Nutrition 0.000 claims 1
- 210000004877 mucosa Anatomy 0.000 claims 1
- 235000010987 pectin Nutrition 0.000 claims 1
- 239000001814 pectin Substances 0.000 claims 1
- 229920001277 pectin Polymers 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000004014 plasticizer Substances 0.000 claims 1
- 229920001992 poloxamer 407 Polymers 0.000 claims 1
- 229940044476 poloxamer 407 Drugs 0.000 claims 1
- 229920002883 poly(2-hydroxypropyl methacrylate) Polymers 0.000 claims 1
- 229920000885 poly(2-vinylpyridine) Polymers 0.000 claims 1
- 229920000075 poly(4-vinylpyridine) Polymers 0.000 claims 1
- 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 claims 1
- 229920001456 poly(acrylic acid sodium salt) Polymers 0.000 claims 1
- 239000004584 polyacrylic acid Substances 0.000 claims 1
- 229920000768 polyamine Polymers 0.000 claims 1
- 229920000867 polyelectrolyte Polymers 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 229940043266 rosin Drugs 0.000 claims 1
- 210000003296 saliva Anatomy 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 229940047670 sodium acrylate Drugs 0.000 claims 1
- 235000010413 sodium alginate Nutrition 0.000 claims 1
- 239000000661 sodium alginate Substances 0.000 claims 1
- 229940005550 sodium alginate Drugs 0.000 claims 1
- 229940080313 sodium starch Drugs 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
- 150000003460 sulfonic acids Chemical class 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- 239000003765 sweetening agent Substances 0.000 claims 1
- 150000003892 tartrate salts Chemical class 0.000 claims 1
- KHPCPRHQVVSZAH-UHFFFAOYSA-N trans-cinnamyl beta-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OCC=CC1=CC=CC=C1 KHPCPRHQVVSZAH-UHFFFAOYSA-N 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
- 229920001285 xanthan gum Polymers 0.000 claims 1
- 235000010493 xanthan gum Nutrition 0.000 claims 1
- 239000000230 xanthan gum Substances 0.000 claims 1
- 229940082509 xanthan gum Drugs 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
-
- 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
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7007—Drug-containing films, membranes or sheets
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Medicinal Preparation (AREA)
Abstract
Mevcut buluş, asenapinin ya da farmasötik olarak kabul edilebilir tuzunun veya esterinin, özellikle oral mukozadan oral uygulama için en az bir suda çözünür polimer içeren esterinin ince film stripi ile ilgilidir.The present invention relates to a thin film strip of acenapine or a pharmaceutically acceptable salt or ester thereof, in particular at least one water-soluble polymer-containing ester for oral administration from the oral mucosa.
Claims (17)
- . A thin film strip of asenapine or pharmaceutically acceptable salt or ester for oral administration across the oral mucosa comprising at least one water soluble polymer.
- The thin film strip tablet according to claim 1, wherein the oral mucosa is selected from the buccal, sublingual and gingival mucosa.
- The thin film strip according to claim 1 or 2, wherein the oral administration is preferably sublingual administration.
- The thin film strip according to claim 1, wherein asenapine or pharmaceutically acceptable salt or ester is selected from the group comprising asenapine fumarate, asenapine hemipamoate, asenapine maleate, asenapine palmitate, asenapine pamoate, asenapine succinate, sulfonic acid salts of asenapine, tartaric acid salts of asenapine
- The thin film strip according to claim 1 or 4, wherein said asenapine or pharmaceutically acceptable salt or ester is preferably asenapine hemipamoate and asenapine maleate.
- The thin film strip according to claim 1 to 5, wherein said asenapine amount is 40% w/w of the total weight of the composition.
- The thin film strip according to claim 1, wherein the water soluble polymer is selected from the group comprising hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose E3, E5 and E15 and K-S, hydroxyethylcellulose and derivatives, ethylcellulose and ethyl hydroxyethylcellulose, carboxymethylcellulose (CMC), carboxymethylcellulose cekol 30, methyl cellulose (MC), methyl cellulose A-3, A6 and A-15; polyvinyl alcohol (PVA), polyethylene glycol (PEG), polyethylene oxide (PEO), poly(ethylene oxide-b-propylene oxide), polyoxyethylene (POE), poly vinyl pyrrolidone (PVP), polyethylenimine (PEI), poly(N- vinylpyrrolidonelvinyl acetate), polyvinylpyrollidone PVP K-90, polyacrylic acid and copolymers, poly(vinylamine) hydrochloride, poly(acrylic acid sodium salt), poly(methacrylic acid), poly(methylacrylic acid sodium salt), poly(ethylene/acrylic acid), poly(2-hydroxyethyl methacrylate/methacrylic acid), poly(2-hydroxypropyl methacrylate), polyacrylamides (PAM), poly(acrylamide/acrylic acid), polymethacrylamide, poly(N-isopropylacrylamide) (PNIPAM), poly(etyrenesulfonic acid) sodium salt, poly(2-0xazoline), poly(2-ethyIoxazoline), poly(3-chlor0 hydroxypropyImethacryloxyethyldimethylammonium chloride), poly(2-vinyI methylpyridinium bromide), poly(2-vinylpyridine), polyamines, poly(2-vinylpyridine N- oxide), poly(N-vinylpyrrolidone/Z-dimethylaminoethyl methacrylate) dimethyl sulfate quaternary, poly(4-vinylpyridine N-oxide), poly(4-vinylpyridine), poly(styrenesulfonic acid/maleic acid) sodium salt, poly(N-vinyl acetamide), poly(N-vinyl acetamide-co- sodium acrylate), poly(vinylsulfonic acid) sodium salt, polyelectrolytes; eudragit carrageenan, chitosan, cucurbit[n]uril hydrate, curdlan, dextran, gelatin, gellan gum, guar gum and derivatives, gum carrageenan, gum arabic and other tree and shrub exudates, kollicoat, Iocust bean gum, maltodextrins, methocel, pectin, pullulan, rosin, sodium alginate, starch and starch derivatives, xanthan gum or mixture thereof.
- The thin film strip according to claim 1 or 7, wherein the water soluble polymer is preferably hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), gelatin,
- The thin film strip according to claim 1 to 8, wherein said water soluble polymer between 0.10 - 20% w/w of the total weight of the composition.
- The thin film strip according to any of the preceeding claims, further comprising at least one excipient which is selected from the group comprising plasticizers, surfactants, sweetening agents, saliva stimulating agents, fillers, acidic polymers, flavors or mixtures thereof.
- The thin film strip according any of the preceeding claims, wherein the thin film strip comprising; a. 50% to 400% by weight of asenapine or pharmaceutically acceptable salt or c. 0.1 % to 300% by weight of diethylene glycol d. 01% to 100% by weight of poloxamer 407 e. 01% to 100% by weight of acesulfame-K f. 01% to 100% by weight of citric acid 0.1 % to 00% by weight of flavor
- 12. The thin film strip according any of the preceeding claims, wherein the thin film strip comprising; a. 5.0% to 400% by weight of asenapine or pharmaceutically acceptable salt or 01% to 200% by weight of gelatine 01% to 300% by weight of di-butyl phthalate 0.1 % to 300% by weight of mannitol 01% to 100% by weight of citric acid 50% to 500% by weight of starch g. 01% to 60% by weight of flavor
- 13. The thin film strip according any of the preceeding claims, wherein the thin film strip comprising; 50% to 400% by weight of asenapine or pharmaceutically acceptable salt or 01% to 01% to 300% by weight of glycerol 01% to 100% by weight of aspartame 01% to 100% by weight of citric acid
- 14. The thin film strip according any of the preceeding claims, wherein the thin film strip comprising; 50% to 400% by weight of asenapine or pharmaceutically acceptable salt or 01% to 01% to 300% by weight of diethylene glycol 01% to 100% by weight of acesulfame-K 01% to 100% by weight of citric acid 5.0% to 500% by weight of starch
- 15. The thin film strip according any of the preceeding claims, wherein the thin film strip comprising; 5.0% to 400% by weight of asenapine or pharmaceutically acceptable salt or 0.1 % to 600% by weight of pullulan 01% to 600% by weight of cellulose acetate phthalate 01% to 300% by weight of di-butyl phthalate 01% to 50% by weight of sodium Iauryl sulfate 01% to 100% by weight of aspartame 01% to 100% by weight of malic acid
- 16. The thin film strip according any of the preceeding claims, wherein the thin film strip comprising; 5.0% to 400% by weight of asenapine or pharmaceutically acceptable salt or 01% to 600% by weight of pullulan 01% to 300% by weight of di-butyl phthalate 01% to 50% by weight of sodium Iauryl sulfate 01% to 100% by weight of mannitol 01% to 100% by weight of malic acid 50% to 500% by weight of starch
- 17. The thin film strip according to any of the preceeding claims, for use in the treatment of mental disorders, especially for schizophrenia and bipolar disorder.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR201414987 | 2014-12-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TR201509009A1 true TR201509009A1 (en) | 2017-02-21 |
Family
ID=54347800
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TR2015/09009A TR201509009A1 (en) | 2014-12-11 | 2015-07-21 | A thin film strip of asenapine |
Country Status (1)
| Country | Link |
|---|---|
| TR (1) | TR201509009A1 (en) |
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| WO1995023600A1 (en) * | 1994-03-02 | 1995-09-08 | Akzo Nobel N.V. | Sublingual or buccal pharmaceutical composition |
| CN102657635A (en) * | 2012-05-04 | 2012-09-12 | 上海现代药物制剂工程研究中心有限公司 | Spongy asenapine sublingual film agent with micropores and preparation method thereof |
| EP2572703A1 (en) * | 2011-09-21 | 2013-03-27 | Hexal AG | Compressed oral dosage form for asenapine maleate |
| CN103083284A (en) * | 2013-02-06 | 2013-05-08 | 上海现代药物制剂工程研究中心有限公司 | Film preparation and its preparation method |
| CN103099799A (en) * | 2013-02-06 | 2013-05-15 | 上海现代药物制剂工程研究中心有限公司 | Composite film-like preparation and preparation method thereof |
| CN104000800A (en) * | 2014-04-28 | 2014-08-27 | 万特制药(海南)有限公司 | Asenapine maleate oral instant membrane and making method thereof |
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2015
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| WO1995023600A1 (en) * | 1994-03-02 | 1995-09-08 | Akzo Nobel N.V. | Sublingual or buccal pharmaceutical composition |
| EP2572703A1 (en) * | 2011-09-21 | 2013-03-27 | Hexal AG | Compressed oral dosage form for asenapine maleate |
| CN102657635A (en) * | 2012-05-04 | 2012-09-12 | 上海现代药物制剂工程研究中心有限公司 | Spongy asenapine sublingual film agent with micropores and preparation method thereof |
| CN103083284A (en) * | 2013-02-06 | 2013-05-08 | 上海现代药物制剂工程研究中心有限公司 | Film preparation and its preparation method |
| CN103099799A (en) * | 2013-02-06 | 2013-05-15 | 上海现代药物制剂工程研究中心有限公司 | Composite film-like preparation and preparation method thereof |
| CN104000800A (en) * | 2014-04-28 | 2014-08-27 | 万特制药(海南)有限公司 | Asenapine maleate oral instant membrane and making method thereof |
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