PL204883B3 - Pharmaceutical agent for local use in parodontium disease treatment - Google Patents
Pharmaceutical agent for local use in parodontium disease treatmentInfo
- Publication number
- PL204883B3 PL204883B3 PL379951A PL37995106A PL204883B3 PL 204883 B3 PL204883 B3 PL 204883B3 PL 379951 A PL379951 A PL 379951A PL 37995106 A PL37995106 A PL 37995106A PL 204883 B3 PL204883 B3 PL 204883B3
- Authority
- PL
- Poland
- Prior art keywords
- protease inhibitor
- cystatin
- aprotinin
- parodontium
- inhibitor
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title description 2
- 239000008177 pharmaceutical agent Substances 0.000 title description 2
- 210000004261 periodontium Anatomy 0.000 title 1
- 108010039627 Aprotinin Proteins 0.000 claims description 18
- 102000015833 Cystatin Human genes 0.000 claims description 12
- 229960004405 aprotinin Drugs 0.000 claims description 12
- 108050004038 cystatin Proteins 0.000 claims description 12
- 229940122055 Serine protease inhibitor Drugs 0.000 claims description 9
- 101710102218 Serine protease inhibitor Proteins 0.000 claims description 9
- 239000003001 serine protease inhibitor Substances 0.000 claims description 9
- 239000003112 inhibitor Substances 0.000 claims description 8
- 102000016943 Muramidase Human genes 0.000 claims description 6
- 108010014251 Muramidase Proteins 0.000 claims description 6
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 claims description 6
- ZPNFWUPYTFPOJU-LPYSRVMUSA-N iniprol Chemical compound C([C@H]1C(=O)NCC(=O)NCC(=O)N[C@H]2CSSC[C@H]3C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(N[C@H](C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N[C@@H](CC=4C=CC=CC=4)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC=4C=CC=CC=4)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC2=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H]2N(CCC2)C(=O)[C@@H](N)CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N2[C@@H](CCC2)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)N3)C(=O)NCC(=O)NCC(=O)N[C@@H](C)C(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H](C(=O)N1)C(C)C)[C@@H](C)O)[C@@H](C)CC)=O)[C@@H](C)CC)C1=CC=C(O)C=C1 ZPNFWUPYTFPOJU-LPYSRVMUSA-N 0.000 claims description 6
- 229960000274 lysozyme Drugs 0.000 claims description 6
- 239000004325 lysozyme Substances 0.000 claims description 6
- 235000010335 lysozyme Nutrition 0.000 claims description 6
- 230000000699 topical effect Effects 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 239000000969 carrier Substances 0.000 claims description 2
- 201000001245 periodontitis Diseases 0.000 claims description 2
- 101000749287 Clitocybe nebularis Clitocypin Proteins 0.000 claims 1
- 101000767029 Clitocybe nebularis Clitocypin-1 Proteins 0.000 claims 1
- 229940094664 Cysteine protease inhibitor Drugs 0.000 claims 1
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 27
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 27
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 9
- 239000007864 aqueous solution Substances 0.000 description 9
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 9
- 239000008194 pharmaceutical composition Substances 0.000 description 9
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 9
- 229960003415 propylparaben Drugs 0.000 description 9
- 239000008213 purified water Substances 0.000 description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 description 6
- 239000013543 active substance Substances 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 6
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 6
- 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 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 6
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 6
- 208000028169 periodontal disease Diseases 0.000 description 6
- 239000006071 cream Substances 0.000 description 5
- 239000007788 liquid Substances 0.000 description 4
- 102000005927 Cysteine Proteases Human genes 0.000 description 3
- 108010005843 Cysteine Proteases Proteins 0.000 description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- 239000000796 flavoring agent Substances 0.000 description 3
- 235000019634 flavors Nutrition 0.000 description 3
- 229940057995 liquid paraffin Drugs 0.000 description 3
- 239000001525 mentha piperita l. herb oil Substances 0.000 description 3
- 235000019477 peppermint oil Nutrition 0.000 description 3
- 241000894006 Bacteria Species 0.000 description 2
- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 208000007565 gingivitis Diseases 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 239000003415 peat Substances 0.000 description 2
- 235000018102 proteins Nutrition 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 102000007327 Protamines Human genes 0.000 description 1
- 108010007568 Protamines Proteins 0.000 description 1
- 102000012479 Serine Proteases Human genes 0.000 description 1
- 108010022999 Serine Proteases Proteins 0.000 description 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 1
- 208000026062 Tissue disease Diseases 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 230000000675 anti-caries Effects 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 230000000840 anti-viral effect Effects 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 210000001124 body fluid Anatomy 0.000 description 1
- 239000010839 body fluid Substances 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- 230000007123 defense Effects 0.000 description 1
- 210000004262 dental pulp cavity Anatomy 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000002439 hemostatic effect Effects 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 239000002324 mouth wash Substances 0.000 description 1
- 229940051866 mouthwash Drugs 0.000 description 1
- 239000008375 oral care agent Substances 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 229950008679 protamine sulfate Drugs 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 229940024999 proteolytic enzymes for treatment of wounds and ulcers Drugs 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- 230000003313 weakening effect Effects 0.000 description 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cosmetics (AREA)
Description
Opis wynalazkuDescription of the invention
Przedmiotem wynalazku jest środek farmaceutyczny do stosowania miejscowego w leczeniu chorób przyzębia mający postać płynu do płukania jamy ustnej, żelu lub kremu. Rozwiązanie według wynalazku stanowi uzupełnienie rozwiązania przedstawionego w zgłoszeniu patentowym P 340775.The present invention relates to a topical pharmaceutical for the treatment of periodontal disease in the form of a mouthwash, gel or cream. The solution according to the invention complements the solution presented in the patent application P 340775.
Choroby przyzębia (stany zapalne dziąseł, paradentoza, choroby tkanek okołoszczytowych) stanowią jeden z ważniejszych problemów stomatologii. Zdrowe zęby są bowiem barierą chroniącą organizm przed wnikaniem zakażenia do kanału korzeniowego. Osłabienie sił obronnych otwiera drogę zakażeniu, które może wywołać stany chorobowe nie tylko w najbliższym sąsiedztwie, ale również w odległych narządach.Periodontal diseases (gingivitis, paradentosis, apical tissue diseases) are one of the most important problems in dentistry. Healthy teeth are a barrier that protects the body against the penetration of infection into the root canal. The weakening of the defense forces opens the way for infection, which can cause disease not only in the immediate vicinity, but also in distant organs.
Znany ze zgłoszenia wynalazku o patent główny P 340775 środek farmaceutyczny do stosowania miejscowego w leczeniu chorób przyzębia zawiera jako substancję czynną inhibitor proteaz serynowych i/lub inhibitor proteaz cysteinowych w ilości nie mniej niż 100 jednostek każdego z inhibitorów w 1 g preparatu oraz ewentualne nośniki lub substancje pomocnicze, przy czym korzystnie jest, gdy środek zawiera aprotyninę lub cystatynę lub aprotyninę i cystatynę. Korzystnymi formami preparatu według zgłoszenia patentowego P 340775 są krem, żel, płyn.The pharmaceutical agent for topical application in the treatment of periodontal diseases, known from the patent application for the main patent P 340775, contains as an active ingredient an inhibitor of serine proteases and / or an inhibitor of cysteine proteases in an amount of not less than 100 units of each inhibitor in 1 g of the preparation and possible carriers or substances auxiliaries, with the agent preferably comprising aprotinin or cystatin or aprotinin and cystatin. Preferred forms of the preparation according to the patent application P 340775 are cream, gel, liquid.
Znane są profilaktyczno-lecznicze środki do pielęgnacji jamy ustnej zawierające różne środki biologicznie czynne Środki biologicznie czynne mają działanie przeciwbakteryjne, przeciwzapalne, przeciwpróchnicowe oraz pielęgnacyjne. Do znanych środków biologicznie czynnych należy 5-chloro-2-(2,4-dichlorofenoksyl)-fenol, znany pod nazwą Triclosan, hamujący wzrost wielu gatunków bakterii powodujących zapalenie dziąseł, przyzębia. Innym znanym środkiem biologicznie czynnym jest siarczan protaminy, posiadający właściwości przeciwbakteryjne i ochronne. Znanym również środkiem biologicznie czynnym jest środek zawierający ekstrakt borowiny otrzymywany z surowego torfu.Prophylactic and therapeutic oral care agents containing various biologically active agents are known. Biologically active agents have antibacterial, anti-inflammatory, anti-caries and caring properties. The known biologically active agents include 5-chloro-2- (2,4-dichlorophenoxy) -phenol, known as Triclosan, which inhibits the growth of many species of bacteria that cause gingivitis and periodontitis. Another known biologically active agent is protamine sulfate, which has antibacterial and protective properties. Also known biologically active agent is an agent containing peat extract obtained from raw peat.
Wadą znanych środków do pielęgnacji jamy ustnej jest ich działanie tylko na poziomie bakterii.The disadvantage of the known oral care products is that they only act on the bacterial level.
Nieoczekiwanie okazało się, że znacznie skuteczniej można zapobiegać chorobom przyzębia poprzez zastosowanie lizozymu - środka biologicznie czynnego w połączeniu z inhibitorem proteaz serynowych i/lub z inhibitorem proteaz cysteinowych.Surprisingly, it turned out that periodontal diseases can be prevented much more effectively by the use of lysozyme - a biologically active agent in combination with a serine protease inhibitor and / or with an inhibitor of cysteine proteases.
Środek farmaceutyczny do stosowania miejscowego w leczeniu chorób przyzębia według zgłoszenia patentowego P 340775, zawierający inhibitor proteaz serynowych i/lub inhibitor proteaz cysteinowych, przy czym korzystnie jest gdy zawiera aprotyninę lub cystatynę lub aprotynin i cystatynę w ilości nie mniej niż 100 jednostek każdego z inhibitorów wig preparatu oraz ewentualne noś niki lub substancje pomocnicze, według wynalazku charakteryzuje się tym, że zawiera lizozym w ilości nie mniej niż 2000 jm. w 1 g preparatu.Pharmaceutical for topical use in the treatment of periodontal diseases according to patent application P 340775, containing a serine protease inhibitor and / or an inhibitor of cysteine proteases, preferably containing aprotinin or cystatin or aprotinins and cystatin in an amount of not less than 100 units of each of the wig inhibitors The formulation and optional excipients or excipients according to the invention are characterized in that it contains lysozyme in an amount of not less than 2000 IU. in 1 g of the preparation.
Zaletą środka według wynalazku jest to, że podczas stosowania unieczynniane są bakterie (dzięki lizozymowi) oraz unieczynniane są enzymy proteolityczne (dzięki aprotininie i cysteinie), które przyczyniają się do rozwoju chorób przyzębia, a stosowanie lizozymu i inhibitora w jednym preparacie daje efekt synergistyczny i wzmacnia działanie.The advantage of the agent according to the invention is that when used, bacteria are inactivated (thanks to lysozyme) and proteolytic enzymes (thanks to aprotinin and cysteine), which contribute to the development of periodontal diseases, are inactivated, and the use of lysozyme and an inhibitor in one preparation gives a synergistic effect and strengthens action.
Lizozym - enzym N-acetylomuramylohydrolaza jest naturalnie występującym w płynach ustrojowych, białkiem zawierającym 129 aminokwasów o ciężarze cząsteczkowym 14500 Da i punkcie izoelektrycznym 10,5. Posiada oprócz aktywności przeciwbakteryjnej, także aktywność hemostatyczną, przeciwzapalną, przeciwhistaminową oraz działanie przeciwwirusowe.Lysozyme - the enzyme N-acetyluramylhydrolase is a naturally occurring protein in body fluids, a protein containing 129 amino acids with a molecular weight of 14,500 Da and an isoelectric point of 10.5. In addition to antibacterial activity, it also has hemostatic, anti-inflammatory, antihistamine and antiviral activity.
Wynalazek przedstawiono w poniższych przykładach wykonania.The invention is illustrated in the following examples.
P r z y k ł a d 1P r z k ł a d 1
Inhibitor proteaz serynowych - aprotynina (traskolan)Serine protease inhibitor - aprotinin (traskolan)
LizozymLysozym
Roztwór wodny wodorotlenku sodowego 10%10% sodium hydroxide aqueous solution
Glikol propylenowyPropylene glycol
Disodowy wersenianDisodium edetate
Hydroksybenzoesan metyluMethyl hydroxybenzoate
Hydroksybenzoesan propyluPropyl hydroxybenzoate
Azulan (środek korygujący smak i zapach)Azulan (flavor and aroma correcting agent)
Woda oczyszczonaPurified Water
Otrzymany środek farmaceutyczny ma postać płynu.The pharmaceutical composition obtained is in the form of a liquid.
50,0 j.Ph.Eur (tj. 100000 j.m.) 2000000,0 j.m.50.0 IU of Ph. Eur (i.e. 100,000 IU) 2,000,000.0 IU
0,01 g0.01 g
20,0 g 0,02 g 0,1 g 0,03 g 1,0 g do 100,0 g20.0 g 0.02 g 0.1 g 0.03 g 1.0 g to 100.0 g
PL 204 883 B3PL 204 883 B3
PL 204 883 B3PL 204 883 B3
Zastrzeżenie patentowePatent claim
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL379951A PL204883B3 (en) | 2006-06-19 | 2006-06-19 | Pharmaceutical agent for local use in parodontium disease treatment |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL379951A PL204883B3 (en) | 2006-06-19 | 2006-06-19 | Pharmaceutical agent for local use in parodontium disease treatment |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PL204883B3 true PL204883B3 (en) | 2010-02-26 |
Family
ID=43012381
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL379951A PL204883B3 (en) | 2006-06-19 | 2006-06-19 | Pharmaceutical agent for local use in parodontium disease treatment |
Country Status (1)
| Country | Link |
|---|---|
| PL (1) | PL204883B3 (en) |
-
2006
- 2006-06-19 PL PL379951A patent/PL204883B3/en unknown
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