TR201708233A2 - Si̇ldenafi̇l ve anti̇septi̇k i̇çeren farmasöti̇k sprey formülasyonu - Google Patents
Si̇ldenafi̇l ve anti̇septi̇k i̇çeren farmasöti̇k sprey formülasyonu Download PDFInfo
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- TR201708233A2 TR201708233A2 TR2017/08233A TR201708233A TR201708233A2 TR 201708233 A2 TR201708233 A2 TR 201708233A2 TR 2017/08233 A TR2017/08233 A TR 2017/08233A TR 201708233 A TR201708233 A TR 201708233A TR 201708233 A2 TR201708233 A2 TR 201708233A2
- Authority
- TR
- Turkey
- Prior art keywords
- spray formulation
- oral spray
- formulation according
- sildenafil
- chloride
- Prior art date
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- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 title claims abstract description 112
- 239000000203 mixture Substances 0.000 title claims abstract description 88
- 238000009472 formulation Methods 0.000 title claims abstract description 78
- 229960003310 sildenafil Drugs 0.000 title claims abstract description 55
- 230000002421 anti-septic effect Effects 0.000 title claims abstract description 18
- 239000007921 spray Substances 0.000 title claims description 13
- 229940041678 oral spray Drugs 0.000 claims abstract description 64
- 239000000668 oral spray Substances 0.000 claims abstract description 64
- 239000004599 antimicrobial Substances 0.000 claims abstract description 29
- 238000011109 contamination Methods 0.000 claims abstract description 8
- 230000000813 microbial effect Effects 0.000 claims abstract description 8
- 150000003839 salts Chemical class 0.000 claims description 27
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 20
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 15
- -1 boroglycerine Chemical compound 0.000 claims description 15
- 239000003795 chemical substances by application Substances 0.000 claims description 14
- DEIYFTQMQPDXOT-UHFFFAOYSA-N sildenafil citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 DEIYFTQMQPDXOT-UHFFFAOYSA-N 0.000 claims description 13
- 239000002904 solvent Substances 0.000 claims description 12
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims description 11
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims description 11
- 229960002639 sildenafil citrate Drugs 0.000 claims description 10
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims description 8
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 8
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 8
- 229960002798 cetrimide Drugs 0.000 claims description 8
- 235000019441 ethanol Nutrition 0.000 claims description 8
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Chlorhexidine Chemical class C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 claims description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 7
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- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 claims description 6
- CNBGNNVCVSKAQZ-UHFFFAOYSA-N benzydamine Chemical group C12=CC=CC=C2C(OCCCN(C)C)=NN1CC1=CC=CC=C1 CNBGNNVCVSKAQZ-UHFFFAOYSA-N 0.000 claims description 6
- 229960003333 chlorhexidine gluconate Drugs 0.000 claims description 6
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 5
- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 claims description 5
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- 230000000873 masking effect Effects 0.000 claims description 3
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims description 3
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- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 claims description 2
- WEEGYLXZBRQIMU-UHFFFAOYSA-N 1,8-cineole Natural products C1CC2CCC1(C)OC2(C)C WEEGYLXZBRQIMU-UHFFFAOYSA-N 0.000 claims description 2
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- NCKMMSIFQUPKCK-UHFFFAOYSA-N 2-benzyl-4-chlorophenol Chemical compound OC1=CC=C(Cl)C=C1CC1=CC=CC=C1 NCKMMSIFQUPKCK-UHFFFAOYSA-N 0.000 claims description 2
- QTWJRLJHJPIABL-UHFFFAOYSA-N 2-methylphenol;3-methylphenol;4-methylphenol Chemical compound CC1=CC=C(O)C=C1.CC1=CC=CC(O)=C1.CC1=CC=CC=C1O QTWJRLJHJPIABL-UHFFFAOYSA-N 0.000 claims description 2
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- ZISFCTXLAXIEMV-UHFFFAOYSA-N benzamidenafil Chemical compound C1=C(OC)C(OC)=CC=C1CNC(=O)C1=CC([N+]([O-])=O)=CC=C1NC(C)CO ZISFCTXLAXIEMV-UHFFFAOYSA-N 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 229910021538 borax Inorganic materials 0.000 description 1
- 230000003222 cGMP degradation Effects 0.000 description 1
- LLSDKQJKOVVTOJ-UHFFFAOYSA-L calcium chloride dihydrate Chemical compound O.O.[Cl-].[Cl-].[Ca+2] LLSDKQJKOVVTOJ-UHFFFAOYSA-L 0.000 description 1
- 229940052299 calcium chloride dihydrate Drugs 0.000 description 1
- 239000004227 calcium gluconate Substances 0.000 description 1
- 229960004494 calcium gluconate Drugs 0.000 description 1
- 235000013927 calcium gluconate Nutrition 0.000 description 1
- OLOZVPHKXALCRI-UHFFFAOYSA-L calcium malate Chemical compound [Ca+2].[O-]C(=O)C(O)CC([O-])=O OLOZVPHKXALCRI-UHFFFAOYSA-L 0.000 description 1
- 239000001362 calcium malate Substances 0.000 description 1
- 229940016114 calcium malate Drugs 0.000 description 1
- 235000011038 calcium malates Nutrition 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- NEEHYRZPVYRGPP-UHFFFAOYSA-L calcium;2,3,4,5,6-pentahydroxyhexanoate Chemical compound [Ca+2].OCC(O)C(O)C(O)C(O)C([O-])=O.OCC(O)C(O)C(O)C(O)C([O-])=O NEEHYRZPVYRGPP-UHFFFAOYSA-L 0.000 description 1
- CHRHZFQUDFAQEQ-UHFFFAOYSA-L calcium;2-hydroxyacetate Chemical compound [Ca+2].OCC([O-])=O.OCC([O-])=O CHRHZFQUDFAQEQ-UHFFFAOYSA-L 0.000 description 1
- KHAVLLBUVKBTBG-UHFFFAOYSA-N caproleic acid Natural products OC(=O)CCCCCCCC=C KHAVLLBUVKBTBG-UHFFFAOYSA-N 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
- 235000013877 carbamide Nutrition 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- QDYLMAYUEZBUFO-UHFFFAOYSA-N cetalkonium chloride Chemical compound CCCCCCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 QDYLMAYUEZBUFO-UHFFFAOYSA-N 0.000 description 1
- 229960004830 cetylpyridinium Drugs 0.000 description 1
- NEUSVAOJNUQRTM-UHFFFAOYSA-N cetylpyridinium Chemical compound CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 NEUSVAOJNUQRTM-UHFFFAOYSA-N 0.000 description 1
- 235000019693 cherries Nutrition 0.000 description 1
- 229940068911 chloride hexahydrate Drugs 0.000 description 1
- KYKAJFCTULSVSH-UHFFFAOYSA-N chloro(fluoro)methane Chemical compound F[C]Cl KYKAJFCTULSVSH-UHFFFAOYSA-N 0.000 description 1
- 229940106705 chlorophyll Drugs 0.000 description 1
- 235000019219 chocolate Nutrition 0.000 description 1
- 239000007979 citrate buffer Substances 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 229940013361 cresol Drugs 0.000 description 1
- 229940097362 cyclodextrins Drugs 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 229950003418 dasantafil Drugs 0.000 description 1
- 208000002925 dental caries Diseases 0.000 description 1
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 1
- 235000019404 dichlorodifluoromethane Nutrition 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 description 1
- 229940075557 diethylene glycol monoethyl ether Drugs 0.000 description 1
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 description 1
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229960000878 docusate sodium Drugs 0.000 description 1
- XJWSAJYUBXQQDR-UHFFFAOYSA-M dodecyltrimethylammonium bromide Chemical compound [Br-].CCCCCCCCCCCC[N+](C)(C)C XJWSAJYUBXQQDR-UHFFFAOYSA-M 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000009986 erectile function Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 229940032296 ferric chloride Drugs 0.000 description 1
- 239000007941 film coated tablet Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 239000007789 gas Substances 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 208000007565 gingivitis Diseases 0.000 description 1
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 description 1
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 description 1
- 229940093915 gynecological organic acid Drugs 0.000 description 1
- UKACHOXRXFQJFN-UHFFFAOYSA-N heptafluoropropane Chemical compound FC(F)C(F)(F)C(F)(F)F UKACHOXRXFQJFN-UHFFFAOYSA-N 0.000 description 1
- VOAPTKOANCCNFV-UHFFFAOYSA-N hexahydrate;hydrochloride Chemical compound O.O.O.O.O.O.Cl VOAPTKOANCCNFV-UHFFFAOYSA-N 0.000 description 1
- 235000003642 hunger Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 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 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- RBTARNINKXHZNM-UHFFFAOYSA-K iron trichloride Chemical compound Cl[Fe](Cl)Cl RBTARNINKXHZNM-UHFFFAOYSA-K 0.000 description 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 229950007965 meralein sodium Drugs 0.000 description 1
- FFEARJCKVFRZRR-UHFFFAOYSA-N methionine Chemical compound CSCCC(N)C(O)=O FFEARJCKVFRZRR-UHFFFAOYSA-N 0.000 description 1
- 229930182817 methionine Natural products 0.000 description 1
- 235000006109 methionine Nutrition 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 229950002245 mirodenafil Drugs 0.000 description 1
- MIJFNYMSCFYZNY-UHFFFAOYSA-N mirodenafil Chemical compound C1=C(C=2NC=3C(CCC)=CN(CC)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)N1CCN(CCO)CC1 MIJFNYMSCFYZNY-UHFFFAOYSA-N 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 229960002446 octanoic acid Drugs 0.000 description 1
- 229940066429 octoxynol Drugs 0.000 description 1
- 229920002113 octoxynol Polymers 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 235000021313 oleic acid Nutrition 0.000 description 1
- 229940041672 oral gel Drugs 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 239000003961 penetration enhancing agent Substances 0.000 description 1
- 210000003899 penis Anatomy 0.000 description 1
- 150000004686 pentahydrates Chemical class 0.000 description 1
- 230000003239 periodontal effect Effects 0.000 description 1
- 201000001245 periodontitis Diseases 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000002798 polar solvent Substances 0.000 description 1
- 239000004584 polyacrylic acid Substances 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 229960000286 proflavine Drugs 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- MCJGNVYPOGVAJF-UHFFFAOYSA-N quinolin-8-ol Chemical compound C1=CN=C2C(O)=CC=CC2=C1 MCJGNVYPOGVAJF-UHFFFAOYSA-N 0.000 description 1
- 150000007660 quinolones Chemical class 0.000 description 1
- 230000004648 relaxation of smooth muscle Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 229940039245 revatio Drugs 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 210000000329 smooth muscle myocyte Anatomy 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- FHHPUSMSKHSNKW-SMOYURAASA-M sodium deoxycholate Chemical compound [Na+].C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 FHHPUSMSKHSNKW-SMOYURAASA-M 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 239000001540 sodium lactate Substances 0.000 description 1
- 235000011088 sodium lactate Nutrition 0.000 description 1
- 229940005581 sodium lactate Drugs 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 229940001584 sodium metabisulfite Drugs 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- JAJWGJBVLPIOOH-IZYKLYLVSA-M sodium taurocholate Chemical compound [Na+].C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCCS([O-])(=O)=O)C)[C@@]2(C)[C@@H](O)C1 JAJWGJBVLPIOOH-IZYKLYLVSA-M 0.000 description 1
- 235000010339 sodium tetraborate Nutrition 0.000 description 1
- HYPOXTZKXREAOY-UHFFFAOYSA-M sodium;[3-hydroxy-2,7-diiodo-6-oxo-9-(2-sulfonatophenyl)xanthen-4-yl]mercury;hydrate Chemical compound O.[Na+].C=12C=C(I)C(=O)C=C2OC2=C([Hg])C(O)=C(I)C=C2C=1C1=CC=CC=C1S([O-])(=O)=O HYPOXTZKXREAOY-UHFFFAOYSA-M 0.000 description 1
- FIWQZURFGYXCEO-UHFFFAOYSA-M sodium;decanoate Chemical compound [Na+].CCCCCCCCCC([O-])=O FIWQZURFGYXCEO-UHFFFAOYSA-M 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 229960000835 tadalafil Drugs 0.000 description 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 description 1
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 1
- 239000000606 toothpaste Substances 0.000 description 1
- 239000003859 topical antiinfective agent Substances 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- 150000004684 trihydrates Chemical class 0.000 description 1
- BSVBQGMMJUBVOD-UHFFFAOYSA-N trisodium borate Chemical compound [Na+].[Na+].[Na+].[O-]B([O-])[O-] BSVBQGMMJUBVOD-UHFFFAOYSA-N 0.000 description 1
- 229960000438 udenafil Drugs 0.000 description 1
- IYFNEFQTYQPVOC-UHFFFAOYSA-N udenafil Chemical compound C1=C(C=2NC=3C(CCC)=NN(C)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)NCCC1CCCN1C IYFNEFQTYQPVOC-UHFFFAOYSA-N 0.000 description 1
- 229960002703 undecylenic acid Drugs 0.000 description 1
- 235000012141 vanillin Nutrition 0.000 description 1
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
- 229960002381 vardenafil Drugs 0.000 description 1
- 229940094720 viagra Drugs 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Mevcut buluş erektil disfonksiyonun tedavisi için etkili miktarda sildenafil içeren oral sprey formülasyonuna yönelik olup, kombine olarak mikrobik kontaminasyonu önleyen ve/veya oral 5hijyen sağlayan en az bir antiseptik ve/veya antimikrobial madde içerir.
Description
TARIFNAME
SILDENAFIL VE ANTISEPTIK IÇEREN FARMASÖTIK SPREY FORMÜLASYONU
Teknik Alan
Mevcut bulus sildenafil ve antiseptik veya antimikrobial ajan içeren farmasötik sprey
formülasyonu ile ilgilidir.
Teknigin Durumu
Sildenafil sitrat erektil disfonksiyon (ED) tedavisinde kullanima girmis ilk oral ilaçtir. Tip 5
fosfodiesteraz enziminin selektif bir inhibitörüdür. Seksüel stimülasyona cevap olarak nitric
oksit (NO) salgilanir. NO korpus kavernozumlarda düz kas hücrelerinde guanilat siklaz
enzimini aktive eder, bu da siklik guanozin monofosfat (cGMP) düzeylerinin yükselmesine
neden olur ve korpus kavernozumda düz kas gevsemesi suretiyle kan girisine izin verir.
Tip 5 fosfodiesteraz cGMP'nin yikimini saglar. Sildenafil ile Tip 5 fosfodiesteraz enziminin
inhibisyonu cGMP'nin yikimini Önlemek suretiyle ortamdaki cGMP'nin etkisinin devam
etmesini saglar. Sildenafilin Iibido ve düz kas üzerine direkt etkisi yoktur. Bu nedenle
sildenafil ereksiyon olusturmaz, seksüel uyari sonucu olusan ereksiyonun korunmasini
saglar ve uyari eksikliginde etkisizdir. Nitrik oksidin artmis etkisi penise kan akimini arttirarak
bozulmus erektil fonksiyonu düzeltir.
Sildenafil sitrat, maksimum serum seviyesine ortalama 1 saatte (0.5-2 saat) erisir. Etkisi 30-
60 dakikada baslar, 1-5 saat sürer. Serum yarilanma ömrü 4 saattir ve %98'i 24 saatte
vücuttan atilir. Yüksek yag içerikli gidalar Sildenafilin gastrointestinal sistemde emilimini
azaltarak, maksimum serum konsantrasyonunun %29 daha az olmasina neden olur.
Sildenafil sitrat kimyasal adi “1 -[[3-(6,7-dihydro-1-methyI-7-oxo-3-propyI-1 H-
pyrazol0[4,3d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate” olup,
yapisal formülü asagida gösterilmistir:
CH20H2CH3
Sildenafil sitrat, erektil disfonksiyonun tedavisi için film kapli tablet (Viagra®) ve oral dagilan
tablet olarak piyasada bulunmaktadir. Mutlak oral biyoyararlanimi % 40'dir.
Sindirim sisteminden absorbe edilen kati dozaj formlari ile karsilastirildiginda, yüksek damar
agi bulunan oral kavite daha hizli ve etkili ilaç absorbsiyonunu saglar.Ilaç absorbsiyonu
açisindan oral kavite minimal engele sahip olup, etkin maddenin serum konsantrasyonunun
hizli yükselmesini saglar.
Ayrica pulmoner arteriyel hipertansiyonun (PAH) tedavisi için (Revatio®) markasi ile
piyasada bulunan 20 mg Sildenafil sitrat içeren tabletleri bulunmaktadir.
Sildenafil sitrat içeren tablet 25, 50 ve 100mg sildenafil esdegeri sildenafil sitrat içerir. Ayrica
agizda dagilan tablet formu bulunmaktadir.
Sildenafil sitrat molekül olarak ilk defa U patentinde açiklanmistir. Daha
sonra erektil disfonksiyon tedavisinde etkili oldugu bulunmus ve bu etkisi ile ilgili U86469012
(Pfizer) patenti alinmistir.
Teknigin bilinen durumunda sildenafil içeren tablet, transdermal ve topikal formülasyonlarina
iliskin çesitli patentler bulunmaktadir.
EP0960621 A2 (Pfizer) ve U oral dagilan tablet formülasyonu ile
EP0967214 A1 (Pfizer) intranazal formülasyonu açiklar.
U kontrollu salim tableti ile ilgilidir.
TR oral jel formülasyonunu
açiklar.
Bunlarin disinda oral sprey formülasyonlari ile ilgili çesitli patentler bulunmaktadir.
U sublingual sprey formülasyonu ile ilgilidir.
W PDE-5 inhibitörlerinin sublingual sprey formülasyonu ile
ilgilidir. Formülasyon tad düzeltici olarak glycyrrhizinic asit, miks solvent olarak alkol ve
alkalin iyonize su içerir.
U pH'si 15-30 arasinda olan solvan olarak propilen glikol ve
etil alkol ile hazirlanmis %7-12 arasinda sildenafil içeren oral sprey formülasyonu ile ilgilidir.
Her sprey 10, 20 veya 30mg sildenafil içerir.
RU oral sprey formülasyonu ile ilgilidir. Formülasyon pH'si 3.0-
6.0 arasinda olup, %3-30 sildenafil sitrat, ve stabilizan olarak calcium Iactate pentahydrate,
calcium Iactate trihydrate, calcium gluconate, calcium malate, calcium glycolate, calcium
chloride hexahydrate and calcium chloride dihydrate içinden seçilen bir kalsiyum tuzu içerir.
Bulusun Açiklamasi
Mevcut bulus sildenafil ile erektil disfonksiyonun tedavisine yönelik olup, ayrica mikrobik
kontaminasyonu önleyici ve/veya oral hijyeni saglayici etki gösteren etkin madde içerir.
Mevcut bulus erektil disfonksiyonun tedavisi için etkili miktarda sildenafil içeren oral sprey
formülasyonuna yönelik olup, kombine olarak mikrobik kontaminasyonu bnleyen ve/veya oral
hijyen saglayan en az bir antiseptik ve/veya antiinfektif (antimikrobial) madde içerir.
Sildenafil oral sprey formülasyonu oral kaviteden sildenafil absorbe etmek ve bu sirada oral
hijyeni saglamak amaciyla formüle edilmistir. Agiz içinin hijyeninin saglanmasi suretiyle
partnerlerin birbirinden mikrobial bulasma riski minimuma inecek ve güvenlik artacaktir.
Terminolojik olarak antiseptikler; insan ve diger hayvanlarda lokal olarak kullanilan zararli
mikroorganizmalari yok etmek veya aktivitesini inhibe etmek amaciyla kullanilan maddelerdir.
Antiinfektif (antimikrobik, antimikrobial) ajanlar ise enfeksiyon hastaliklarinin önlenmesinde
ve tedavisinde kullanilan maddelerdir. Dezenfektanlar ise canli olmayan nesnelerde zararli
mikroorganizmalari yok etmek veya aktivitesini inhibe etmek amaciyla kullanilan maddelerdir.
Oral sprey formulasyonu sildenafil veya farmasötik olarak kabul edilebilir tuzunu içerir. Tercih
edilen sildenafil tuzu sildenafil sitrat tuzudur. Oral sprey formülasyonunda sildenafil veya
farmasötik olarak kabul edilebilir tuzu %5 ila %15 (m/v) arasinda olabilir. Bir püskürtme 5mg
ila 30mg veya 10mg ila 30mg arasinda sildenafil içerecek sekilde formüle edilebilir. Bir
püskürtme 10mg, 20mg, 25mg veya 30mg sildenafil içerebilir.
Oral sprey formülasyonunda sildenafil mukozal, sublingual, bukkal ve hatta gastrointestinal
yolla tasinabilir. Sildenafil veya tuzu mikronize edilmis olabilir.
Oral sprey formulasyonu sildenafil veya farmasötik olarak kabul edilebilir tuzuna ilave olarak
bir veya daha fazla antiseptik madde içerir. Antiseptik veya antimikrobial madde olarak
diguanid bilesikleri, katerner amonyum bilesikleri, antibakteriyel boyalar, halojenli fenol
türevleri, kinolon türevleri kullanilabilir.
Oral sprey formulasyonunda antiseptik veya antimikrobial maddeler diguanid bilesigi olarak
klorhekzidin tuzlari; katerner amonyum bilesigi olarak Cetylpyridinium chloride, Cetrimide,
Benzalkonium chloride, Methylbenzethonium chloride, Benzethonium chloride, Cetalkonium
chloride, Dofanium chloride, Domiphen bromide; antibakteriyel boya olarak Proflavine
hemisulphate, Triphenylmethane, Brilliant green, Crystal violet, Gentian violet; peroksitler
olarak hidrojen peroksit çözeltisi ve benzoil peroksit, halojenli fenol türevi olarak
Chlorocresol, Chloroxylenol, Chlorophene, Triclosan; kinolon türevi olarak Hydroxyquinoline
sulphate, Potassium hydroxyquinoline sulphate, Chlorquinaldol, Dequalinium chloride, Di-
iodohydroxyquinoline olabilir.
Bu maddelerin disinda benzoik asit, borik asit, borogliserin, kafur, susuz gliserinde karbamid
peroksit, kIorofiI, krezol, ökaliptol, ferri klorür, iyot, mentol, meralein sodyum, metil salisilat,
nitromersol, oksikinolin sülfat, fenol, sodyum fenolat, potasyum klorat, povidon iyodür,
sodyum kaprilat, timol, timol iyodür, myrrh tentürü, tolu balsami, 2,4-dichlorobenzyl
alcohol/amylmetacresol kullanilabilir.
Tercih edilen maddeler klorhekzidin tuzlari, setrimid ve setilpiridinyum klorürdür.
Klorhekzidin dezenfektan ve topikal anti-infektif bir ajandir. Klorhekzidin genel cilt temizleyici
ve el hijyeni saglanmasinda kullanilir. Özellikle dental operasyonlarda ve periodontit,dis
çürükleri tedavisinde tercih edilen bir ajandir. Anti-plak, anti-jinjivit ve antibakteryel aktiviteye
sahip güçlü bir antiseptiktir. Gram-pozitif, gram-negatif bakteriler, aerob ve anaerob
mikroorganizmalar, mantar ve mayalar üzerinde etkilidir.Agiz yikama çözeltisi olarak çesitli
solusyonlarin bilesiminde bulunur. Klorhekzidinin farmasötik olarak kabul edilebilen
hidroklorür, glukonat ve asetat tuzlari bulunur. Agiz yikama çözeltilerinde %0.12
konsantrasyonda klorhekzidin glukonat içeren oral yikama çözeltileri vardir. Periodontal
bakim için %005 konsantrasyonda çözeltisi önerilir.
Patent konusu sildenafil içeren oral sprey formülasyonunda oral yolla mikrobial
kontaminasyonu önlemek amaciyla seçilen ajanlardan biri klorhekzidin glukonattir. Suda çok
çözünmesi klorhekzidin glukonat için bir avantajdir.
Setilpiridinyum klorür bakterileri öldüren antiseptik bir ajan olup, agiz yikama çözeltilerinde,
dis macunlarinda, agiz ve burun spreyierinde ve pastillerde kullanilir. Agiz hijyenini korur.
Gram-pozitif, gram-negatif bakteriler, virüsler ve mantarlar üzerinde etkilidir. Jinjivit kontrolu
için %0.045 ila %O.1 arasinda konsantrasyonlarda formülasyonlari etkin ve güvenlidir.
Patent konusu sildenafil içeren oral sprey formülasyonunda oral yolla mikrobial
kontaminasyonu önlemek amaciyla seçilen ajanlardan biri setilpiridinyum klorür bilesigidir.
Ayni amaçla cetylpyridinium/benzyl alcohol karisimi kullanilabilir.
Patent konusu sildenafil içeren oral sprey formülasyonunda oral yolla mikrobial
kontaminasyonu önlemek amaciyla seçilen antiseptik ajanlardan biri setrimid bilesigidir.
Setrimid tetradecyltrimetylammonium bromide ile daha küçük miktarlarda
dodecyltrimetylammonium bromide ve hexadecyltrimetylammonium bromide içeren bir
karisimdir. %01 ila %1 arasinda konsantrasyonlarda kullanilabilir.
Sildenafil içeren oral sprey formülasyonu nonsteroid antienflamatuar ajan içerebilir. Bu
amaçla benzidamin, diklofenak gibi lokal etkili NSAID ajanlar kullanilabilir. Benzidamin agiz
ve girtlak enflamasyon durumunda kullanilir. Tantum Verde isimli ilaçta bulunur. Agiz yikama
çözeltilerinde %0.15 m/v konsantrasyonda kullanilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu bir
veya daha fazla farmasötik olarak kabul edilebilir eksipiyan ve tasiyici ajanlar içerebilir.
Eksipiyan olarak solvent ve yardimci solventler, çzündürücü ajanlar, penetrsyon arttiricilar,
stabilizanlar, tampon ajanlari ve pH düzenleyiciler, tonisite ayarlayicilari, annti-mikrobik
ajanlar, viskozite modifikasyon ajanlari kullanilabilir. Kullanilabilecek eksipiyanlar yukarida
belirtilen gruplarla sinirli degildir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu
çözücü olarak saf su, etanol veya karisimini içerebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu en az
bir yardimci çözücü içerir.Yardimci çözücü olarak propilen glikol, etil alkol, gliserin, molekül
agirligi , soya yagi, PEG-60 hidrojene hint yagi, N-metil-
2-pirolidon seçilebilir.
Oral sprey formulasyonu polar solvent karisimi olarak propilen glikol ve etanol karisimi
içerebilir. Karisimda propilen glikolietanol orani hacimce 10:1 ila 1:10 v/v olabilir. Propilen
propilen glikol ve %30-40 etanol içerebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonunun
pH'si en az 1.5'tir. Tercihen pH 8.5'i geçmemelidir. Çözelti pH'si ± 0.5, tercihen ± 0.2
Sildenafil veya farmas'otik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu pH
için en az bir tampon içerebilir. Tampon olarak sitrat, asetat ve fosfat tamponu seçilebilir.
Oral sprey formülasyonunun pH'sini düzenlemek için asit veya alkali maddeler kullanilabilir.
Asit olarak hidroklorik asit, sitrik asit, Iaktik asit, glikolik asit, asetik asit, malik asit, propiyonik
asit gibi inorganik veya organik asitler kullanilabilir. Alkali ajan olarak sodyum hidroksit,
sodyum karbonat, sodyum bikarbonat, potasyum karbonat, potasyum hidroksit, sodyum
borat, sodyum sitrat, sodyum Iaktat, sodyum glikolat seçilebilir. Asitlendirici ajan %5 ila %15,
tercihen %10 konsantrasyonda, alkalilendirici ajan %15 ila %4 tercihen %2 konsantrasyonda
hazirlanabilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu
penetrasyon arttirici içerebilir. Bu amaçla mentol, Iimonen, karvon, metil kitosan,
polisorbatlar, sodyum Iauril sulfat, gliseril oleat, kaproik asit, enantik asit, kaprilic asit,
pelargonik asit, kaprik asit, undesilenik asit, laurik asit, miristik asit, palmitik asit, oleik asit,
stearik asit, Iinolenik asit, arasidonik asit, benzethonium chloride, benzethonium bromide,
benzalkonium Chloride (BKC), setilpiridinyum klorür, edetat disodyum dihidrat, sodyum
desoksikolat, sodium deoksiglikolat, sodyum glikolat, sodyum kaprat, sodyum taurokolat, L-
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu
antioksidan olarak askorbik asit, vitamin E, EDTA veya uygun amino asit içerebilir. Stabilizan
olarak sodyum metabisulfit, sodyum bisulfit, disodyum EDTA, askorbik asit kullanilabilir.
Sildenafil veya farmas'otik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu tad
maskeleyici ve tad düzenleyici ajan olarak bir veya daha fazla yapay meyve aromalari
(portakal, limon, visne, kavun vb. veya bunlarin karisimlari), anason, tarçin, vanilya vb.
içerebilir. Bu amaçla sentetik veya dogal nane yagi veya mentol, limon yagi, çukulata
aromalari gibi aromalar seçilebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu bir
veya daha fazla tatlandirici içerebilir. Uygun tatlandirici olarak aspartam, mannitol, ksilitol,
sodyum sakarin, sukraloz, sakkaroz, glukoz, glisirhizik asit seçilebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu bir
veya daha fazla koruyucu içerebilir. Bu amaçla benzoik asit,sodyum benzoat, metil paraben,
propil paraben, m-krezol, fenol, setilpiridinyum klorür, benzyl alcohol, benzalkonium Chloride,
phenylethyl alcohol seçilebilir. Bu maddeler formülasyonda antiseptik etkin madde olarak
bulunabilirler.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu
çözünürlük arttirici ajan olarak diethylene glycol monoethyl ether (Transcutol),
siklodekstrinler, glicerol monostearat, Iesitin, poloksomer, polietilene alkil eterler,
polioksietilen kastor oil türevleri, polioksietilen sorbitan yag asiti esterleri, polyoksietilen
stearatlar, stearik asit, sitrik asit, askorbik asit, DL-metionin, kafein, nikotinamid, vanilin,
benzil alkol, etanol kullanilabilir. Formülasyon çözünürlük arttirici olarak kafein içerebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu yüzey
aktif madde olarak polisorbatlar, sorbiton esterleri, polivinil alkol, benzalkonium Chloride,
benzethonium Chloride, cetrimide, docusate sodium, sodyum Iauril sulphat ve octoxynol
içerebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu
viskozite düzenleyici içerebilir. Bu amaçla HPMC (hydroxypropyl methylcellulose), poliakrilik
asit veya carbopol, sodium carboxymethyl cellulose, HPC (hydroxypropyl cellulose), HEC
(hydroxyethyl cellulose), polivinilpirolidon (PVP K-15, K-30, K-60, K-90) gibi suda çözünen
polimerler kullanilabilir.
Sildenafil veya farmas'otik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu
hidrofilik polimer içerebilir. Hidrofilik polimer olarak ksantan zamki, sodyum
karboksimetilselüloz, hidroksipropilmetilseloz gibi selüloz türevleri seçilebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu itici
gaz olarak kloroflorokarbon (CFC), hidrokloroflorokarbon (HCFC) ve hidrofloro karbon (HFC)
içerebilir. CFC olarak trikloromonoflorometan (No.11), diklorodiflorometan (N0.12),
diklorotetraflorometan (No. ve HFC olarak
heptafloropropan (No:227) seçilebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu
çözelti veya süspansiyon olabilir. Formülasyon farmasbtik olarak kabul edilebilir boyar madde
içerebilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonu
dogrudan agiz içine dilin altina veya üstüne püskürtülür.
Sildenafil oral sprey formülasyonu oral kaviteden Sildenafil absorbe etmek ve bu sirada agiz
içinin hijyenini saglamak amaciyla formüle edilmistir. Oral sprey formülasyonunda Sildenafil
mukozal, sublingual, bukkal ve hatta gastrointestinal yolla tasinabilir.
Oral sprey formülasyonu uygulanacagi zaman bir ila bes püskürtme olacak uygulanabilir. Bir
püskürtme 100 ila 300 pl (about 0.1 - sivi formülasyon uygulanabilir. Püskürtme
hacmi yaklasik 200 ila 250 ul olabilir.
Sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formulasyonunun
etkinligi ile ilgili olarak gerektiginde klinik çalismalar yapilabilecektir. Böyle bir çalisma tek
doz, açik, çapraz çalisma olarak 24 denek üzerinde olabilir. Çalismada deneklere açlik
durumunda uygulanmis oral sprey formülasyonu ile ulasilan kan düzeyleri uygun
intervallerde ölçülerek Cmax, Tmax, AUC gibi klinik parametreler degerlendirilebilir.
Sildenafil PDE5 inhibitörlerinin prototipi sayilir. Sildenafil disinda benzer etki gösteren
avanafil, Iodenafil, mirodenafil, tadalafil, vardenafil, udenafil, benzamidenafil, dasantafil isimli
moleküller bulunmaktadir. Mevcut bulus erektil disfonksiyonun tedavisi için etkili miktarda
diger PDE5 inhibitörlerinin herhangi biri ile birlikte en az bir antiseptik ve/veya antimikrobial
madde içeren oral sprey formülasyonlarini da kapsar.
Claims (24)
1. Tedavi edici miktarda sildenafil veya farmasötik olarak kabul edilebilir tuzunu içeren oral sprey formülasyonu olup, mikrobik kontaminasyonu Önleyici ve/veya oral hijyeni saglayici etki gösteren en az bir antiseptik ve/veya antimikrobik madde içerir.
2. Istem 1'e göre oral sprey formülasyonu olup, % 5 ila % 30 arasinda sildenafil veya farmasötik olarak kabul edilebilir tuzunu içerir.
3. Istem 1 veya 2'ye göre oral sprey formülasyonu olup, farmasötik olarak kabul edilebilir sildenafil tuzu sildenafil sitrattir.
4. Istem 1 ila 3'ün herhangi birine göre oral sprey formülasyonu olup, bir püskürtme 5mg ila 30mg sildenafil içerir.
5. Önceki isteme göre oral sprey formülasyonu olup, bir püskürtme yaklasik 10mg veya 20mg veya 30mg sildenafil içerir.
6. Onceki istemlerin herhangi birine göre oral sprey formülasyonu olup, antiseptik veya antimikrobik madde klorhekzidin tuzlari; Cetylpyridinium chloride, Cetrimide, Benzalkonium chloride, Methylbenzethonium chloride, Benzethonium chloride, Cetalkonium chloride, Dofanium chloride, Domiphen bromide; Proflavine hemisulphate, Triphenylmethane, Brilliant green, Crystal violet, Gentian violet; peroksitler olarak hidrojen peroksit çözeltisi ve benzoil peroksit, Chlorocresol, Chloroxylenol, Chlorophene, Triclosan; Hydroxyquinoline sulphate, Potassium hydroxyquinoline sulphate, Chlorquinaldol, Dequalinium chloride, Di- iodohydroxyquinoline, benzoik asit, borik asit, borogliserin, kafur, susuz gliserinde karbamid peroksit, klorofil, krezol, ökaliptol, ferri klorür, iyot, mentol, meralein sodyum, metil salisilat, nitromersol, oksikinolin sülfat, fenol, sodyum fenolat, potasyum klorat, povidon iyod'ür, sodyum kaprilat, timol, timol iyodür, myrrh tentürü, tolu balsami, 2,4-dichlorobenzyl alcohol/amylmetacresol olabilir.
7. Istem 6”ya göre oral sprey formülasyonu olup, antiseptik veya antimikrobik madde klorhekzidin veya farmasötik olarak kabul edilebilir tuzudur.
8. Onceki isteme göre oral sprey formülasyonu olup klorhekzidin veya farmasötik olarak kabul edilebilir tuzu %0.05 ila %0.15 m/v miktarindadir.
9. Istem 7 veya 8'e göre oral sprey formülasyonu olup, antiseptik veya antimikrobik madde klorhekzidin hidroklorür, klorhekzidin glukonat veya klorhekzidin asetattir.
10. istem 9'a göre oral sprey formülasyonu olup, antiseptik veya antimikrobik madde klorhekzidin glukonattir.
11. Istem 6'ya göre oral sprey formülasyonu olup, antiseptik veya antimikrobik madde setilpiridinyum klorür veya setilpiridinyum kIorür/benzil alkol karisimidir.
12. Onceki isteme göre oral sprey formülasyonu olup,setilpiridinyum klorür %0.045 ila %01 m/v miktarindadir.
13. Istem 6'ya göre oral sprey formülasyonu olup, antiseptik veya antimikrobik madde setrimittir.
14. Onceki isteme göre oral sprey formülasyonu olup,setrimid %01 ila %1 m/v miktarindadir.
15. Onceki istemlerin herhangi birine göre oral sprey formülasyonu olup, solvent ve yardimci solventler, çOzündürücü ajanlar, penetrasyon arttiricilar, stabilizanlar, tampon ajanlari ve pH düzenleyiciler, tonisite ayarlayicilari, anti-mikrobik ajanlar, viskozite modifikasyon ajanlari içinden seçilmis bir veya daha fazla eksipiyan ve/veya tasiyici içerebilir.
16. Onceki isteme göre oral sprey formüllasyonu olup, çözücü ve/veya yardimci çözücü saf su, etanol, propilen glikol, gliserin, molekül agirligi , soya yagi, PES-60 hidrojene hint yagi, N-metiI-2-pirolidon veya karisimlari içinden seçilir.
17. Onceki istemlerin herhangi birine g'ore oral sprey formülasyonu olup, tad maskeleyici ve tad düzenleyici ajan içerir.
18. Onceki isteme göre oral sprey formülasyonu olup, tad maskeleyici ve tad düzenleyici ajan sentetik veya dogal nane yagi veya mentol, limon yagi, çukulata aromalari, yapay meyve aromalari, anason, tarçin, vanilya içinden seçilir.
19. Onceki istemlerin herhangi birine göre oral sprey formülasyonu olup, en az bir tatlandirici ajan içerir.
20. Onceki isteme göre oral sprey formülasyonu olup, tatlandirici ajan aspartam, mannitol, ksilitol, sodyum sakarin, sukraloz, sakkaroz, glukoz, glisirhizik asit içinden seçilir.
21. Onceki istemlerin herhangi birine göre oral sprey formülasyonu olup, en az bir koruyucu madde içerir.
22. Onceki isteme göre oral sprey formülasyonu olup, koruyucu madde benzoik asit,sodyum benzoat, metil paraben, propil paraben, m-krezol, fenol, setilpiridinyum klorür, benzyl alcohol, benzalkonium chloride, phenylethyl alcohol içinden seçilir.
23. Onceki istemlerin herhangi birine göre oral sprey formülasyonu olup, nonsteroid antienflamatuar ajan içerir.
24. Onceki isteme göre oral sprey formülasyonu olup, nonsteroid antienflamatuar ajan benzidamin veya diklofenak veya bunlarin farmasötik olarak kabul edilebilir tuzudur.
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| TR2017/08233A TR201708233A2 (tr) | 2017-06-05 | 2017-06-05 | Si̇ldenafi̇l ve anti̇septi̇k i̇çeren farmasöti̇k sprey formülasyonu |
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| TR2017/08233A TR201708233A2 (tr) | 2017-06-05 | 2017-06-05 | Si̇ldenafi̇l ve anti̇septi̇k i̇çeren farmasöti̇k sprey formülasyonu |
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