RU2002100645A - Противогрибковая композиция для перорального введения, содержащая интраконазол, и способ получения такой композиции - Google Patents
Противогрибковая композиция для перорального введения, содержащая интраконазол, и способ получения такой композицииInfo
- Publication number
- RU2002100645A RU2002100645A RU2002100645/14A RU2002100645A RU2002100645A RU 2002100645 A RU2002100645 A RU 2002100645A RU 2002100645/14 A RU2002100645/14 A RU 2002100645/14A RU 2002100645 A RU2002100645 A RU 2002100645A RU 2002100645 A RU2002100645 A RU 2002100645A
- Authority
- RU
- Russia
- Prior art keywords
- mixture
- intraconazole
- antifungal composition
- composition according
- cellulose
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims 14
- 230000000843 anti-fungal Effects 0.000 title claims 6
- VHVPQPYKVGDNFY-ZPGVKDDISA-N Itraconazole Chemical compound O=C1N(C(C)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@@H]3O[C@](CN4N=CN=C4)(OC3)C=3C(=CC(Cl)=CC=3)Cl)=CC=2)C=C1 VHVPQPYKVGDNFY-ZPGVKDDISA-N 0.000 title claims 4
- 238000004519 manufacturing process Methods 0.000 title 1
- -1 aluminum-magnesium Chemical compound 0.000 claims 7
- NBIIXXVUZAFLBC-UHFFFAOYSA-N phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 6
- 235000014113 dietary fatty acids Nutrition 0.000 claims 4
- 239000000194 fatty acid Substances 0.000 claims 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000004094 surface-active agent Substances 0.000 claims 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 2
- 150000004665 fatty acids Chemical class 0.000 claims 2
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 2
- 239000000377 silicon dioxide Substances 0.000 claims 2
- 239000007787 solid Substances 0.000 claims 2
- OXLXSOPFNVKUMU-UHFFFAOYSA-N 1,4-dioctoxy-1,4-dioxobutane-2-sulfonic acid Chemical compound CCCCCCCCOC(=O)CC(S(O)(=O)=O)C(=O)OCCCCCCCC OXLXSOPFNVKUMU-UHFFFAOYSA-N 0.000 claims 1
- VUKAUDKDFVSVFT-UHFFFAOYSA-N 2-[6-[4,5-bis(2-hydroxypropoxy)-2-(2-hydroxypropoxymethyl)-6-methoxyoxan-3-yl]oxy-4,5-dimethoxy-2-(methoxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)-5-methoxyoxane-3,4-diol Chemical compound COC1C(OC)C(OC2C(C(O)C(OC)C(CO)O2)O)C(COC)OC1OC1C(COCC(C)O)OC(OC)C(OCC(C)O)C1OCC(C)O VUKAUDKDFVSVFT-UHFFFAOYSA-N 0.000 claims 1
- CWSZBVAUYPTXTG-UHFFFAOYSA-N 5-[6-[[3,4-dihydroxy-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxymethyl]-3,4-dihydroxy-5-[4-hydroxy-3-(2-hydroxyethoxy)-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxyoxan-2-yl]oxy-6-(hydroxymethyl)-2-methyloxane-3,4-diol Chemical compound O1C(CO)C(OC)C(O)C(O)C1OCC1C(OC2C(C(O)C(OC)C(CO)O2)OCCO)C(O)C(O)C(OC2C(OC(C)C(O)C2O)CO)O1 CWSZBVAUYPTXTG-UHFFFAOYSA-N 0.000 claims 1
- WNROFYMDJYEPJX-UHFFFAOYSA-K Aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 claims 1
- PZZYQPZGQPZBDN-UHFFFAOYSA-N Aluminium silicate Chemical compound O=[Al]O[Si](=O)O[Al]=O PZZYQPZGQPZBDN-UHFFFAOYSA-N 0.000 claims 1
- 229920001353 Dextrin Polymers 0.000 claims 1
- 239000004375 Dextrin Substances 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
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- XAPRFLSJBSXESP-UHFFFAOYSA-N Oxycinchophen Chemical compound N=1C2=CC=CC=C2C(C(=O)O)=C(O)C=1C1=CC=CC=C1 XAPRFLSJBSXESP-UHFFFAOYSA-N 0.000 claims 1
- 229940067631 Phospholipids Drugs 0.000 claims 1
- 239000004698 Polyethylene (PE) Substances 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 229920001451 Polypropylene glycol Polymers 0.000 claims 1
- 229920001214 Polysorbate 60 Polymers 0.000 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- JNYAEWCLZODPBN-CTQIIAAMSA-N Sorbitan Chemical class OCC(O)C1OCC(O)[C@@H]1O JNYAEWCLZODPBN-CTQIIAAMSA-N 0.000 claims 1
- 229920002472 Starch Polymers 0.000 claims 1
- HWKQNAWCHQMZHK-UHFFFAOYSA-N Trolnitrate Chemical compound [O-][N+](=O)OCCN(CCO[N+]([O-])=O)CCO[N+]([O-])=O HWKQNAWCHQMZHK-UHFFFAOYSA-N 0.000 claims 1
- 229910052782 aluminium Inorganic materials 0.000 claims 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminum Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims 1
- 239000000440 bentonite Substances 0.000 claims 1
- 229910000278 bentonite Inorganic materials 0.000 claims 1
- 229920001400 block copolymer Polymers 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 235000019425 dextrin Nutrition 0.000 claims 1
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 235000019325 ethyl cellulose Nutrition 0.000 claims 1
- 229920001249 ethyl cellulose Polymers 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 239000000155 melt Substances 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 150000003904 phospholipids Chemical class 0.000 claims 1
- 229920001281 polyalkylene Polymers 0.000 claims 1
- 229920000573 polyethylene Polymers 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 229920005862 polyol Polymers 0.000 claims 1
- 150000003077 polyols Chemical class 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 1
- 239000008107 starch Substances 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 238000005809 transesterification reaction Methods 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
Claims (5)
1. Противогрибковая композиция для перорального введения, включающая полученную расплавом смесь интраконазола и фосфорной кислоты, фармацевтически приемлемый носитель и поверхностно-активное вещество.
2. Противогрибковая композиция по п.1, в которой массовое соотношение интраконазола и фосфорной кислоты в полученной расплавом смеси составляет от 1:0,1 до 1:10.
3. Противогрибковая композиция по п.1, в которой фармацевтически приемлемый носитель выбран из группы, включающей: лактозу, декстрин, крахмал, микрокристаллическую целлюлозу, гидроксипропилметилцеллюлозу, гидроксипропилцеллюлозу, гидроксиэтилцеллюлозу, этилцеллюлозу, метилцеллюлозу, полиэтиленгликоль, двуокись кремния, гидроталькит, силикат алюминия-магния, гидроксид алюминия, силикат алюминия, метасиликат алюминия-магния, бентонит и их смесь.
4. Противогрибковая композиция по п.1, в которой поверхностно-активное вещество выбрано из группы, включающей: полиэтилен гликолированные натуральные или гидрированные растительные масла, сложные эфиры полиоксиэтилена-сорбитана-жирной кислоты, сложные эфиры полиоксиэтилена и жирной кислоты, блок-сополимеры полиоксиэтилена-полиоксипропилена, диоктилсульфосукцинат натрия, лаурилсульфат натрия, фосфолипиды, сложные эфиры пропиленгликоля и моно- или дижирной кислоты, продукты переэтерификации триглицеридов натуральных растительных масел и полиалкиленовых многоатомных спиртов, моноглицериды, диглицериды, моно/диглицериды и сложные эфиры сорбитана и жирной кислоты.
5. Способ получения противогрибковой композиции по п.1, включающий:
(a) смешивание интраконазола и фосфорной кислоты,
(b) нагревание смеси до температуры в пределах от 100 до 170°С с получением гомогенной расплавленной смеси,
(c) добавление к полученной смеси фармацевтически приемлемого носителя и поверхностно-активного вещества,
(d) охлаждение расплавленной смеси с получением твердого вещества, и
(e) измельчение твердого вещества в порошок.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1999/22472 | 1999-06-16 | ||
| KR1019990022472A KR100331529B1 (ko) | 1999-06-16 | 1999-06-16 | 난용성 항진균제의 경구투여용 조성물 및 그의 제조 방법 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2002100645A true RU2002100645A (ru) | 2003-09-20 |
| RU2216323C2 RU2216323C2 (ru) | 2003-11-20 |
Family
ID=36441999
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2002100645/14A RU2216323C2 (ru) | 1999-06-16 | 2000-06-16 | Противогрибковая композиция для перорального введения, включающая итраконазол, и способ ее получения |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US6039981A (ru) |
| EP (1) | EP1185273B1 (ru) |
| JP (1) | JP3717849B2 (ru) |
| KR (1) | KR100331529B1 (ru) |
| CN (1) | CN1170539C (ru) |
| AT (1) | ATE324893T1 (ru) |
| AU (1) | AU754300B2 (ru) |
| CA (1) | CA2376706C (ru) |
| CZ (1) | CZ292146B6 (ru) |
| DE (1) | DE60027717T2 (ru) |
| ES (1) | ES2262517T3 (ru) |
| HU (1) | HUP0201533A3 (ru) |
| MX (1) | MXPA01012739A (ru) |
| RS (1) | RS50008B (ru) |
| RU (1) | RU2216323C2 (ru) |
| SI (1) | SI20677A (ru) |
| TR (1) | TR200103681T2 (ru) |
| WO (1) | WO2000076520A1 (ru) |
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| EP0904060B1 (en) * | 1996-05-20 | 2003-12-10 | Janssen Pharmaceutica N.V. | Antifungal compositions with improved bioavailability |
| KR100321617B1 (ko) * | 1997-06-16 | 2002-07-27 | 동아제약 주식회사 | 항진균제와 유기산류의 공융혼합물 및 이를 함유하는 약학적 제제 |
| KR100367483B1 (ko) * | 1997-12-19 | 2003-03-26 | 동아제약 주식회사 | 당류를이용하여용해도및용해속도를증가시킨이트라코나졸경구용조성물및그제조방법 |
| US6383471B1 (en) * | 1999-04-06 | 2002-05-07 | Lipocine, Inc. | Compositions and methods for improved delivery of ionizable hydrophobic therapeutic agents |
| KR100331529B1 (ko) * | 1999-06-16 | 2002-04-06 | 민경윤 | 난용성 항진균제의 경구투여용 조성물 및 그의 제조 방법 |
-
1999
- 1999-06-16 KR KR1019990022472A patent/KR100331529B1/ko not_active IP Right Cessation
- 1999-10-04 US US09/411,510 patent/US6039981A/en not_active Expired - Fee Related
-
2000
- 2000-06-16 EP EP00935726A patent/EP1185273B1/en not_active Expired - Lifetime
- 2000-06-16 RU RU2002100645/14A patent/RU2216323C2/ru not_active IP Right Cessation
- 2000-06-16 JP JP2001502853A patent/JP3717849B2/ja not_active Expired - Fee Related
- 2000-06-16 CA CA002376706A patent/CA2376706C/en not_active Expired - Fee Related
- 2000-06-16 CZ CZ20014508A patent/CZ292146B6/cs not_active IP Right Cessation
- 2000-06-16 RS YUP-886/01A patent/RS50008B/sr unknown
- 2000-06-16 MX MXPA01012739A patent/MXPA01012739A/es active IP Right Grant
- 2000-06-16 DE DE60027717T patent/DE60027717T2/de not_active Expired - Lifetime
- 2000-06-16 AT AT00935726T patent/ATE324893T1/de not_active IP Right Cessation
- 2000-06-16 TR TR2001/03681T patent/TR200103681T2/xx unknown
- 2000-06-16 SI SI200020024A patent/SI20677A/sl not_active IP Right Cessation
- 2000-06-16 ES ES00935726T patent/ES2262517T3/es not_active Expired - Lifetime
- 2000-06-16 WO PCT/KR2000/000637 patent/WO2000076520A1/en active IP Right Grant
- 2000-06-16 CN CNB008089485A patent/CN1170539C/zh not_active Expired - Fee Related
- 2000-06-16 HU HU0201533A patent/HUP0201533A3/hu unknown
- 2000-06-16 AU AU51144/00A patent/AU754300B2/en not_active Ceased
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