HUE031013T2 - Gyógyászati kompozíció krákogás és torokfájás kezelésére - Google Patents

Gyógyászati kompozíció krákogás és torokfájás kezelésére Download PDF

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HUE031013T2
HUE031013T2 HUE13745409A HUE13745409A HUE031013T2 HU E031013 T2 HUE031013 T2 HU E031013T2 HU E13745409 A HUE13745409 A HU E13745409A HU E13745409 A HUE13745409 A HU E13745409A HU E031013 T2 HUE031013 T2 HU E031013T2
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Anna-Maria Vestweber
Sousa Jose Galan
Markus Unkauf
Michael Ploch
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Maria Clementine Martin Klosterfrau Vertriebsges Mbh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728Hyaluronic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/731Carrageenans
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/02Algae
    • A61K36/04Rhodophycota or rhodophyta (red algae), e.g. Porphyra
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/09Lichens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/48Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/68Plantaginaceae (Plantain Family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/73Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/898Orchidaceae (Orchid family)
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/04Drugs for disorders of the respiratory system for throat disorders

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Description

PHÄRMÄ?»iSAt £Ö«SIT!ÜN FSSIRß T8ËAλf f3F©pÂKiNËlS ÂND SplTHROAt mmmim ÄpöiÄlffiplieäiar a s^Äiärtylsi särniÄstfon: förheameness br asdte Strödt.
The pressât invention rotates to the field of medicina, particularly the treatment of hoarseness and inflammatory diseases of the mouth and throat (such as sere throat). in paffater. the present Invention taiaies to s compesíföni preferahiy a pharmaceutical composition, that is suitable for the topical treatment of hoarseness end inilammatery diseases of the mouth and throat (such as sorefhfoeb· Moreover, the present1 invention relates to uses according to thsinvehiion ei ihs composition according itoitfse invehiioO; §y hoarseness or dpphonia is usaeliy meant a deterioration of theyoea! part of the phonafion (arsçtiiation), vtéiemift, in this context there is generally a malfunction of the larynx and the vocal tract. According to the findings, in the case of homeness. the voice sounds hoarser, hard, rough, or aspirated and Is no longer ‘flexible*. i.e, the timbre, pitch and volume may oniy be varied to a retyped |äI: éöneemei in paffe« jar, ihe symptem: ef diy mouth (xerostomia) elten occurs in me case of hcrseness
The underlying causes eThoareeness aréimsny, jód may be both iunctionaf as weil as organic. The functional causes include, In particular, a general overuse oi the voice, for example, through singing or voice-harming speech habits. Among the most common1 organic causes: are. in particular, inflammatory diseases of the mouth and throat, such as occur, for example:,® the case of colds or fMike infections. in addlöh*; |Pi|iÄ issue growth may M, ameng organic causes cf hoaraehess. In rare cases, it is also possible that congenital nmlfcrmgtjœ fh the area of thé larynx may tend to hoarseness,
Hoarseness caused both by functional and by organic causes, particularly inflammatory diseases of ttte moufh end pharynx, is cften associated by teeipbentwith unpleasant NMI #so- PeuryltpçiÉ^ difücuit food intake^ Sfoteover, the; -$g$$g|$É # liptiSp, which is eheractedstjs of hoarseness, is felt as being very unpieasant
The treatment of hoarseness, in the case of both fonctions! as well as organic causes, In päiisüläf infiammafoty diseases of the oral and pharyngeal cavity, is usually carried out- doperiding on the severity oi the disease - by topical therapy. phorafh sedsiactory therapeutic success often: dees not result, as desertbed fesiew. The merapeuöe measdme are namely pneriiy öFftii^aremedteg* such as hot milk with honey,or gargle solutions based on sailor säge. Such treatments. Ifowsyev, efipfo de not provide satisfactory relief otsymptomsi Some of the welhknown home remedies; such as, in particular, hoi milk with honey, may even he hanoiul becsüse they cause increased mucus production in : the throatäpddhus impede tee healing process, and regeneration.
Moreover, commercial loeenpeareíöfien used put, although providing temporary relief, foairefteots usually subside very guickly. in particular, ail treatment concepts msed for hoarseness in the: prior ad ÉT net provide suffiolent'relief 0 pain and infiammation symptoms, especially if the hoarseness has underlying orgaoic:oauses, such as inflammatory diseases of; foe mouth and;threat. The same aise appites for the érhette Idffamrrtetefy diseases of the mouth and threat. Again, the therapeutic agents of the prior art are often not efficient inflammation in the oral cavity, i.e. inflammatory diseases of the moufh and pharynx and the throat area, often occurs as a side effect of colds and flu, but else as-·μ independent disesse. Such inflammatory processes of fre mouth and throat are often assoototed i^pâSenfeîv#: unpieasant pairs symptoms. NoriMfög examples ofsiich infiantoídfory isessps ef the throatarea: sîîî sera: throat. especially angles, inflammation of the larynx liiaryngitis}, inflsm matted of ôïè mrôàt {phs|yá|ÍÍ(Sj: aoíi infemmattem o? She tonsils (tonsillitis). Such diseases of the throat eras are oiler! seeompanieêhyi ρ## swallowing add asore throat. in addition. .íntoroÉtelö such es for oxarnpie: stomatitis, gingivitis, erai; mucosa lesions effet If® like, are often âeœmphied ihy pam. For further doteiiswifo; respect ts ths áforomehfiohad diseases, refer* for exs^ai-.fef Ée ifc$c!b 4$χίΙ?όη Mi@8iSi 3rd edition. 4S93, UfbaflsvS: % Hi mfa the i%chyrembsi. fledioal
Dielionary, 26?th edition. 1993. NiKeí V'erlagsgeseiisehstt mbH: Hamburg. th* Äse of the mouth and tiro# is thus to be understood very broadty and includes ait inflammatory diseases, which may occur in toe «rai cavity, pharynx and neck ares.
The treatmentof friffammstery diseaps #fo is generally effected * depending on toe severity el the disease - by using topiesl and. antibiosesare administered m more severe eases, supportive Étdi%hl^:^^i«#f^isrl^':«}epefti on topiöab syropfemslio treatment using andsepiies end (such es. tor example, astoinfiatotostories «gents, -fesal etc.};#iichi; for exsmpie, may te administered in toefop of torost wasiies. spray%ir.;|iöton^í;:^ili:ii«8$ur^:^» usuteiy not sutocientiy efficient arid sustainable M 20 2084 CIS 64o P relates fo fWÂ^tld':àôsspifo:Se;àxât#i partteuiady ictóenges, for the topical treatment of:fo^mi^^^^iÉ^:ieí;pö®rteáá:^roati.'dM*n toe compositicfo pnfoihs the active ingredient octenidtne as an antiseptic
Further, WO 2007/110874 Â2 disrtosss a mefoed :ir fto- :h^ÊmÊ Φ $$$.- threat or tores? inhammation, wherein a pharmaceutical composition is applied iri tile pharynx, The composition has an oily exefpieht and a pharmaceuMíytoölve ingredient and is preferably administered in toe form o? a spray
The present invention, therefore, has the object of providing a composition, especially a pharmaceutical composition., which, at least, largely avoids the above-described disadvantages of tire prior art or at least mitigates them.
SpeGi|sai|y, ::toe present invention seehs to pfovidc a ccmpssitisn whiah is suitable for efttefont topical treatment of hoarseness or sore throat or inflammatory diseases of the mouto and throat in addition, the pmteant invention seeks: teiprevids ;a;cotoposiiioh: which ottoreian excellent anfiongdasiig reitef of pain and inflammation pyinpfoms in toe treatment of boamsness andl infamrnatofÿ dfoeeses oi. toe meutir and throat white aiso: counteracting tire symptoms oi dry mouth.
To aohieyatoahhove-deseribeii object, toe grosÄfeyetlten proposes a composition according tociainv Tíliítoerodvahtageous eibhodimente are the subject of tedbOpehderù claims f&lailng toftis, it goes without saying that tire particular forms, embodiments or the like, which are described diiiy 1rs connection with ono jspecl of the invention, arc also sejuafiy valid with respect to toe ether aspects of tosfoveniiön, without this being expressly referred to. it should aiso be noted for any of toe relative, percentage, especially weight, quantities listed betow, that they are to be so selected by;® person skilled in the art m toe nontext of too present invention, that the sum of the respective substances, setive fngtebtedte, additives or fexcipiohfsioriÉe iiifo, always mseit in 100%. This ggasiywlfout saÿih|ifo a person: shitted in the: art. in in the art may vary toe fiumoors, area or volume information fisted: befow according te top:
Individual application or case, without leaving toe scope of toe present invention.
Fufíéttiiors, ail the paraméter infermatienerthelike iisfedteetewnnsybe öasfealsy dètomined or oefcuiated using standardized öt expfeiy indicated rnsteodS oídtetemioaien m common detenntestioe methods deterteinsd or ss^íteined by a person skied te the art.
The présem ilwerteon te thus ·· according io a first aspect. of tee invention - a composition, in particular « pharmaceutical composite«, preferably io: tee tens tee spite or liquid. In qarteuiar a solid dosap which is suitable ter toplqa! treatmehiof hoarseness, sore terosi or infiatetesh^Äases of teedPÎÂjpteî^^^vi^.sii^n'fepi^îœÂn - in eonrbinatea and in esdi case in effective, psrteuiady phermsceuifealiy effective amounts * comprises la) st least an anfivirsk and/of anteiräiiy effective. psiysacehättee selected from eafrageehans and/or teeir physiötegieaiiy acceptable Saite, galanten suifates andfer their physiologically acceptante sails ans polyuronides and/or their physiologically acceptohte satte f component: |8f):; (b) poiyhexanlde as a surface disinisctsni. (“comportent te)1'); as wett as ,{o) hyaiuronie add or saitSihsfeo? {’’componentr0)¾
Ihe pppitcant has now: sprprisinpty found teat a composition, preferably a phanhaiteutical composition comprising a comfeiftstion of active ingredients m tee Äs o? at feast one virustato or antiviral polysaccharide with polybexanide as a surface disinfectant,. aS-weii as hyaluronic acid, provides exseifeot relief from hoarseness or a sore throal as welt ss thé sssoóiatöd pain and inflammatory symptoms, while simultaneously providing effective relief pitery mouth, in this context, it has. in particular been Shewn that the .Stolon of tee;individual active ingredients. when used in 1#«$iyfdaai active ingredients in a significant way, should be seen as an indication of e synergistic effect,
The terms 'phannaceuficât compositiorite ’pharmacsutfeai preparation· or tee like, # used in tee present feyenfioe, are te be understood very compi'éheástveiy and rsfer not oniy te phateRâcteuticai preparations: or pharmaceuticals, hut atso te sp^oatied medtcal: devices, homeopathic remedies, dietary suppisnwnls. or the tike. in the context of tef term “polysaceftebdas’' pcemponent $$)*} refers to macromdiecutar carbohydrates, whose mofeoules citeslst of a natePer pf a^ least > 10 msfetefeS· fteivsacsharides include numeifeus oiopipfers or polymers of hiogonic origin, which may have extremely vanabfe chemisai or phafmspiogicat properties, Polysaccharides are mainly used as reserve substances and arc usually present as homopoiymers or Praptpans tirât undsriie one type of monosaschartp to addition, there are polysaccharides which (mm hind te term a gel wife forge amounts of water, and are therefore referred to ds so-cafiad tedcifage. TP potysaocteandes associated Ptetey^^.am:i^i8Íiyte:Éé;tep of heferopoiymers or fteferegSpehes based on differeht typo of monomer units. Known mucins ihoiede pectins, mannans, gslaeians. xytsrss, hyaiuronie acid arrd oiycosaminogiycans, as well as polymers based on sulfonated gaiactans such as carrageenans, and uronic acids. Tire use or such gelling polymers hes proven parteuferly advarhspous do tea compslten aesmtolnf to foe invehtiön, since they exhibit a partipterf strong aiteify ter tee Or# mucosa and pharynx, and, so to speak, f<m Í; protective ire whieh protects tee raucous membrane, on tee one hand, against tee porfefretfen of pathogens sup: m cold viruses, and, on the other hand, against a toss of liquid or dry mouth. Furthermore, there are also noiysacchsrxies. especially mucitage, with antiviral properties. "the use of such polysaccharides is provided ter Im tee inventive composition For further details on the concept of‘'polysaccharides’, reference may ha mads to Rompp, Chsmie lexikon, löth édition, Georg Thfeme bfepag, Stelgerl/New Vprl, page 3§S3, fteyword: Tofysertehendes", asreelífes the lltefátefo referred to therein, whose reiovant contents are hereby fully incorporated by reference.
The surfas« used In ft® context of the gmsshi in^sntiofr {“cdmporidntíbj'l srayifo particular, understood to refer to toese distofesiog agsnto^w arg suitable tor the application to foe skin or mucosa. The active Ingredient underlying each disinfectant may, tn ptioular, oe based or; oxidizing agents such as hydrogen peroxide or iodine, as well as alcohols, phenols, nitrogen compounds. teüp^lç^^-:pΧm^' tattndiftif salts, as «Il as détergents. Usually such disinfectants possess a bactodclcial. fungicidal and trucida! effective offset so that at least ensured, linear mucopolysaccharides, termed from repetitive saccharides, ere used as Ihe preferably acidic glycosaminogiycans Tfeomponen! |c}·} according to. thö invention, la genera!, toe saccharide units consists ofsuronie arldisocfl as, in particular, glucuronic add. but also iduronic acid or uronic acid, which have a 1,3-glycosidic bond to an amino sugar such as N-acetvigiucosamioo. The saccharide units used to form the;chain as such are. in torn, Ito-glyootodically linked with one another, in particular, #§#§$ ftiltto glyeosaminogJycans are ibriher esferified with sulfuric acid or acetic acid Thp giyeosandnegtpafts id: guesttoh are oiten present lh association with biological macro mdtocdles and stay, tor example, be· covalentiy-bound in large numbers to proteins, in this way, they may form the skeleton of many fiber-forming substances in too body, such as fibrillin. Á relevant advantage according is toe invention or a relevant property ol giycosamtooglycans according to the toysntiooTs, to: patortolar, toeir ablllhy to he able to tobsorb Isrp quantities of water, so that when applied topically to the skin or mucous membranes, drying nutfs prevented. ih the context ofthepresent irweafion giyeosaminogiyoan hyaluronic acid or the salts thereof Is/are used. Hyaiuronic acid is an important compdhont of eenneotore tissue in toe human or animal body sad, moreover, plays a role in ceil proliferation attbeeli fte celi-proliferssve effect has. iri paricutar, been found tőibe advantageous with respect to a rapid fobind pxtremeiy targe amounts of water, enabling up to δ litem of water to be bound With lg ef hyalufoote acl. The binding of targe amounts of «ter may prevent: drying of the skin or mucous membranes m an efficient manner, so foat arfoéísrafed regeneration of tissue is made possibis. while, moreover, the skin or mucosa remain elastic.
Chemically, in the case of hyaluronic acid, tois relates to a maoromoiecuiar chain of disaccharides based on O-glucuronlc acid and to'äeefybtbglueösamihav which are linked via a betatoj-glunoside bond- The disaccbarides atoagph keked together m a bettoiftigiyebsidto bondi to a polymeric chain, ln genetzt, a f«Surenie acid polymer consists οΐ·2δδ to p,800 disacrtoahde units. The applicant hsa surphslngiy found: in the context of the present i toveniion, ftst through the : synergi§tto: combination of at least one virustatically or antiyirally eifeetlve pelÿsacohafide, oo the one band, as well as at least one suriMe disinfeotant, on the öfter hand, and. in addition, at least one gl^samincglycahi hoarsepess as such and. moreover, the hoarseness offen caused by underlying inflammatory diseases of the moufh and threat {e g, sore throat?, in particular toe associated: pain and inflammation symptoms and the symptom of dry mouth, may be alleviated in a particularly short timeframe.
The present invention: has numerous other advantages snd special features which distinguish it compared with too prior art and are described in detail below:
The polpsccharides; used are distipguishad by goed adsorption or adhesion to toe oral mucosa, Ifowmg too formation of a protective film on the mucosa. Sutot a film ppbhtaift®.:pemft®ö^df;p^^rs suc*i;.g^ítssrus^Tariiö dry mouth and dryness of mucous: membranes in toe msuth and throat due to its strong waterfomdieg: prepérkes· lurfoemtofe, toe polysaccharides used are characterised by fofor excellent tolerability, since usually there are. at least, no substantial side effects, irt addlömfoe use: of antiviral pofyssccharidcs rnay considerably sftongtben the protective effect by fobbing a film. in the context oí the present invention, le nse of st feasi óft8::Surise:isfnÉetaetlsa$ S® sí¥ié^:!fhát:ha§:!i^y^::.^:fe!S::6^gseie;Mííy· advanfageotfe; Wtëmn yi pfofestfen against the usual bacteria end; viruses mtîSî offcerî assësfelôrf Ä and eoids, end; thus ífequentiy associated with heemaeess or sore Irbats is eiisof'ëd ifli epmbiHätipn fll iS 'dsrndb^ffeci pt dig polysaccharides used.
Overaii, therefem·, thé pbfysaeshandes used according fe fie invendon tsntpientsfit in a synergistic manner 1@ at iaasi one setlece disiftoni, snp the afacfe or the two components in the combined use exceeds the effect of each individual active ingredient Ptpa$ed:ipns,lh narticoiar. fifes v^i^edlitSdfhEÄi^ against pathogens or psihöpnic agents prate#© film of a barrier against ide pathogens, while. moreover, the surface sacb ptbogans The al^^tft>nef.#èdsw§;î^tbër pbandâf bÿâe adfihonsi use oi at last. one preferably acidic gfycosaminogiycan. rn particoiar hyaluronic acid, as wet as acidic giycosaminogiycans, faffeiiariy hyaluronic acid, with strong vysáer-btr^f»^dÍf§Md>{hti«. In particular, ina fötmaiion di a proteidhie ltm ana the prevention or rsfet of dry mouth is intensified.
Msreeyer, the eoin^bsition according to fits invention compared with the methods known from the prior arldiËinguishes ifeif by alleviating hoarseness or sors throat or inflammatory diseases in the mouth and throat by a rapid onset and yet extremely long* lasting effect, Eyed a few hoe© after application of me composition!, a good welng# theanemorysne: persists: and, moreover, there is a pleasant relief
Purtfrarore; '®»reo«posi%8: ie isfeÄ causés an overall extremely fast rsgenotaiion and restorahon oflhe disturbed phonation, i.e, the vocal implements, in partieuiar, le teeth ér hosrse voice is Quickly heated, űrt addition^ serf Iroat or other Infiarnmatory diseases of the mouth and throat my he treated In an efficient manner with the irtventive composition. Moreover, the composition # $t- jffififfi ÄntöMtss- ffséîf feyr exdélfehif tdiérâh?l*Îÿ, h&amp;esuse if íg at least sobsintidíly free trom: any side effects; Pué;;fe le iopditoferahiiity, the inv&amp;ntiye dcrnposifion 1 thus also sfetpbie; fey reiadveiy prolonged use or for use in the case of eftiidren as well.
Finaily, in the context efithe advsnfeges and featurdl^fp^^desial^yig^repce is made siffs point to me efficacy studies carried and aro described in detail below, fo the invention; may he eoniiguted tn many different ways;JFreferred embodiments are described below for better understanding. in order 1 obtain 1 good affechmenffef the ppiyeaeolidride to the oral mucosa tend pharymg it has proved; advantageous to use polysaccharides with defined weight; average moleeuiar woighfe; Acoprdihf to a preferred: embodiment of la present loysoflem ! may thus be provided let; component (a) has a weight average molecuiar weight in the range of 5.ÖÖ0 to 10,000.000 Da, PSftieaiady: in fee of 15,000 to 7,500.000 Da. preiarabfy ;|n the range of 20,000 io S,000.000 Oa, more preferably in fhe range or 30,000 to 0,800,000 Da, 1 particular as determined by gal pernfeatiom chromatography (GPC), preferabiy according: to: DIN δδδ?2. ivfereovér, 1 eheure pafSoulady goed tcietibilityi lt haspr'oved particularly advantageous if the component (a) is a btopoiymer or a poiymer of biogenic origin.
As eceady mentiened aboya, polysaccharides may be;;present as;bomepdiysacchandes pr heteropolysaccharides or :homs^|ycans::Qr;hetefegfycans as wait According to the invention, it may:thus be provided that component (a) is «ejected from lornepolysacsbandesv^dfer hsterepoiysacchahdes. Uscaity, SmteiopöÍpáechandéSfefe pofysrfehaddes with geifidg; properties, whiqh has proven to be advantageous in the context of 3 good adsorption 0? sdbesion to the oral mucosa in the context of tbs present invention, f reference is therefore given to me usa oiheteipoiysac^|i^:.is. preseritlnveifiiQh. A panicoferly good; säsoiption by the prai: mucosa and thus an excellent pretsolieoeffhe:mncoss from drying out, on the one band:, as well: ss invading germs, pm the other band, may be obtained wflifiîte |S| is : selected from mucins, in particular gatacfe« sulfates audio? their derivatives and/or their physiologiosliyidlefabfe Saits and/or polyuronides and/or their derivatives and/or sails,
According to a preferred embodiment according to the invention, it may Co provided in this connection that the component (a), in páfddtíiar Él ^ysac^äildajyfü· püs^bd preferably as muoiSsge, preferably in Ihesiorm of a drtig, is particular in; tbs form of comminufeddr putverfasdicriesfrididd digae, plant parts, or plant constituent.
According to a further preferred embodiment according to the invention, it may be provided that the comparrent (a), in particular tbepbiysaobharide, Is preferably provided as a «meus substance, preierabiyin thé form of mo sxiiaot, irr partieuief in thetorra of a dry extract, in particular wherein the sxfracf is obtained front an aqueous, alcoholic pr aquegp^álcoholic extract, preferably an aqueous extract in Ibiseonfext, the effectiveness of the composition according fo the invenfiorifs increased even fonder lithe: extract, preferably thö dry extract, iras a dnjg/extract ratio (DER), in particular calculated as a wei^ht-réiâîôç; ratio of siartlngi ämdunts of iha drug To th^ : birset to : be obtätnöd, irt ma range of 0.1:1 to 50:1, partieuiariy in the area glSiS: 1 fotp: 1, pfeferahiy lntba fangaeigti to 10:lyrnore preferably in the range of δ: 1: to 10:1,
The so-oslied dfifl/dxtfaot ratio (DEE) characterises the iweight^ased) rotation oltha starting drug used to the extract obtained. The drug/exfracf raito fDER} thus indicates whsi amount by weight di the drug used (e.g, red algae} Is obtained from what amount by weight of the extract. A drug/extreci ratio of. for example, 10:1 means that one par? by weight of the extract was recovered from tan parts by weight of the drug, The drug/extraet ratio thus indicates how many pads by weight of a phsrmaceuiscei drug are requir ed to produce extract of ths equivalent weight.
The use of extracts with a defined drug/extract ratio is paiicuiify /relevant in that the qualify of fee extract has a decisive infeiea on ths overall quality of the phsrmaceuöca! composiSqp. The aim is also to standardise the aximel in terms gf drug conpanlfStien, so that the final quality and: quantity of me phermaoeutma! preparation may be provided vdm rnspeot fb fe active substances And Ingredients with consistently good values,
The next point concerning the component (a) or the polysaccharide or the muoiiage in fhe eptexi of thé inventron. is tiret It 1$ preferable ;f this Is obtainable from Icelandic moss {Ucften vkmtlicus).. marshmaltov^ (A/fbeeo or/mma/is L), plantain ;Pmiago ianewiaia L), mallow {Malva syivasins L and M. negkeia WALLM). fenugreek {Tngomm hmira-gmamm L), saiep, quince red a|as< especially íred áígae:species of the gmw&amp;útmtfű®, eiMam and/or gigariiaa, as weil as combinations thereof tceiaodmoss is the English nameidf fciefien â itched ~ not in fact a moss contrary to tire English name - that is exported from northern countries, such as Iceland, Norway and Sweden, testend moss In the strict sense # ÉP form Is dried thailus of Iceland moss fii its preparecons: The drug contains, fefa? affSi mucilage and hitter substances as welt as bitter lasting: lichen acids. From the powdered lichen, about 60 wl-% dissolve orr boiling with very dilute sadium: bicarbonate solution, while upon cooling ihésépon forms a jejjy;: The extrsc? comprises a polysaccharide mixture çf tionenm and isolichsnln, a series ef bitter lasting lidien acids {fumamrotocelrshc. protocetraho and cotranc acids) as well ss protoiiqhqotefirho; acid which is converted in the worixb P5 Tb f I cf rib tc a^i^, a rad tr sntc aetef asQbtlbio^c-sfbtlb^t lobe dye. Iceland moss has soothing properties as a mucilaginous drug, if acts as an antimicrobial. The bitter substance content justifies its use in less si appetite. teeiandmoss is used for example in calant* and diarrhea, as a biter fertig exlernajiyfdr poorly heatng: wounds,, eosmteic preparations, ladt of appetite. as well as irteafon of mucous mem^pjt::'ie#<»iiÎ5J!^i::^ost An .oral and throat disinfectant Cased on; Icelandic moss has a sooteing ailed in teasase of a drycough, The cold: maceration and other blfto-r* tasiing fomnsfotioos. of the drug era used to treat su beeid: iy or antacidity. Dosage forms are administered orally according lo the application in site form of the comminuted drug for infusions and other galenical pmparaiiorss or in tits form of the comminuted drug preferably for cold maceration and other bitter-tasting preparations. For further detaiis concerning Icelandic moss, reference may bo made* for example, to the following references: Rompp Chemie-Lexikon.. §fh edition, volume 3* Geo?g: Thieme Vertag. Sfuögarf/Ncw York, 19SÖ, pages 2055/2056, keyword: Icelandic mess"; isprROM IID1 Springer Äag, Heidelberg, keywords: "Cetraria*, ‘'Cetraria eflcetofum OP1F, ’‘Cetraria isiandica (!,.} ACHARIUS* and "Lichen islandicus {Iceland messf; Monograph "Lichen islandicus (Icelandic moss)“, Federal Gazette No. 43 of 2 krigiSd 1S8$, H. Vyagneg •'Pharmaceutiçsl ppiegy-drugs end' their ingradfonfs'Viltisfoy: fischer Verlag, Stmigart/New York, 1S3S, pags^SI,: key word: '’Csireríac Liçfisn {* folchen isiandiddSr Icelandic moss}".
Marshmallow (Althaea officinale L). used in the form of the marshmallow root, ieavssand blossoms,jrows on spy and moist soils of npnfrai, eastern: and sgytfoeasiern Europe:. Heryesfod in Ihe autumn, treSd irdmi tbo woody main root, root fibers and oorticai layers and dried at 35 *0, the roof branches and later«) roots are available commercially. peeisd or unpeied, "Πιο browning of the peeiel d|i|: means s: reduction in qualify; a subsequent ‘teeauteyteg“ with: sulphite solution: is feadmissihie, furthermore, tie three fo lvertobed, feifod grey hairy dried leaves collected before or during flowering and about 10 cm iong and $ cm wide, as weil as the fteshreolored: dried petals coüscted in July/August, are also used: Marshmailow is a perenniaf shrub, about 1 m high, that is reproduced generativeiy cr vegetatively. Harvested in iste autumn, the root contains up to 15¾ muciiage. tri spring and summer, the gum echten) of the leaf and Sower drug is 6 to 9%. Thomuchageis located in the root in certain mucilage cells of the bate and wood parenchyma, ft consists oi gaiacturotec mar-nans, giuesns and of tee roots are prPucP by maceration a? rosm teregöfetUffe sothittfe abundant strengte is net disrupted |y swelling; Marshmsfiow drugs are used for tea preparations or for produsfng ^dtes Afihmm, the mam field m appiication is fnfemmstery irrifetlbn of the pharynx, iktemaiiy. the marshmallow is used ss softening srwelqpeg, baths and poultices.
Plantain {Pimiago lanceolate L) is found throughout Europe and in Norte and Centrai Asia. The drug is cterived from wiki niants and temps mainly from Southeast Europe, The dried, olive green to brownish grean cofored. lance-shaped leaf Pfades vrtfrnabouf terse to seven ptemiiei nerves can be used. The herbai drugs consist of the: dried teases, ·sterns and whole Sowers. Apart from the mucilage, tee piähtäin c&amp;ntains as ferteer ingredients tannins, the tedoids gfykoside Aucuhin (I S tc .2.4%). which la responsible for tee darkening dhhotteoreughiy dried drug and is used idf identity verification. fofíteWéW'öa sufforäphane.
The plantain. espaciaííy fee piantaln leaf herb. Is used In particular in tee forte of teas and syrups for treating inflammation of tee mouth arid throat.
Mdllsyy {Màlvs sylvaatiis L artdM negfodfo Äfo). usad te particular in foe form of malow flowers and leaves. Is native fo Europe, Ma Minor, the hteditertatteäh rsgfofx and the Indian subcontinent, Fgr usé, tea pink-purple colored flowers collected in the flowering season, or tee folded leaves teat are strongly shrunk through drying, are usually commercially available in me form of a package, The mallow is a iws-fearfo perennial herb: The mucilage confute of fiowers and: leaves fsl tc 5%, The hydrolysis öf mucilage glucose supplies mobihose, rhsmnose and galactose. Máiiow flowers are used for gargles and baths and as an expectorant together with the leaves Id tes blends, fo ϋΦ te bf fenugreek seed is native throughout the bfediiemansan region, esweil as ln Eastern Europa, feefia an# China. The main drug Import cames from india and Maróim The hrown-irnddish, quadrilateral andfiamonh^hapetl iieiTened, very hard seeds, about 5ü long and about 3 min wide, and characterized by a furremare used/Apart from fatty d|, the druf contains 20 to 30¾ mucilage, tigoneiline, nfcpaasnirfe* and: Saponins, The production of fe muciiage ;is obtained fntm the pwdered seeds. The powder is applied pferoalty ip envelopes fordoits, ulearsend seÄn glands, and internally as an expctorant and; mhoranf.
Seien and satep tuber, used particularly in the form of salep tubsfs is derived front various types of orchids, especially ÔHÜfe· nnmula 1., Orchis mfä^ '0$lsmM8iis 1., Anacmpîis pyrmidak L MOH, arid Pktmthm hiioüa L RICH The wrinkled, hard, brownish tubers, abetft;4 pm long and 3 cm : fhicE. £&amp; freed; f root fte covering: layer eher harvesting by sealdingiwife boiling wafer and ailed using artificial hest Saiep mucilage, :mfenly consisting of up ito 15Q% of glucomannan or giuCSn, is msinty used in p&amp;cilairic practipeas an ahiícfiarfheai; Çfeince (Cydom oh’mga Mfefc.) is native to south-eastern Arabia- The irtsin drug imports come from Spain, Portugal and Persia. The dried ripe, red-brown to; hfown-tylpioî colored, slightly tlaffehed seadsipf feeiduince pseudo MfetOosed; The seeds are; provided OhiiO outside part with e dried mucilage crust and often glued;together. They have a: weak bier elmond taste·: Them ie about 22% rnuciiage in ibéíeplöauníS that is water-soluble (or the most part. Tire sugar components ms arabinose, xylose and orbnfeaeirt,; Which is parfilly mbthylated. The drug is only applied unerusbedt The quince mucilage is used externally tor ilp and, nipple rhagades. bums and bedsores, In ointment or cream form-
The designation gfgae refers iri the broader '#n^#êblta#plpv-i^Â#ô§â&amp;r«s lying in :Wm and operated through photosynthesis, buf fe attributed tS the actual plants; Algae ere chamefehwed by apt^tecÉ^ífüabdim,;#tlcft provides for ie epthesis of numerous polysaccharides among ofeer feinp, The bbiysacghaddes synfeesysrt by aigae are In particular p^upiiage end feldtening agents Wbfeiv ate fepd mainiy fe the; toed; far, in particular, Ted algae irhodephytat are/distinguished by their abity for synthesfeof polymers, such as agar based on agarose, suifenated bg^íopécöo and carrageanan feased on sulfenefedlölácfesa and 3Änhydrogelabtose< Beth agar and eenäpenan form a gelatinous mess or a so-called muons on contact*# wafebery fee hasisof their ability to hind water in large amounts,
According to a : particularly; preferred embodiment Of fee Invention. fetm|iÄ$ä¥|®s$'feaiÄ component ta}, especially fee polysacchande. preferably the mucus. Is selected iron; fee carrogeenÉhs ahdfer loir derivatives and/or their physiologically iOlefabfe;sails, in particular from the alpha, iota, gamma, kappa and/or lambda-carrageenan and/or derivatives thereof and/or their physiologically acceptable salts, preferably lota-carrageenan and/or denvatives; tffereot and/or their physiologically compatible salts,.
Similarly, it may be provided feat the component (a), especially the polysaccharide, preferably the mucus substance. » a hetero polymer based on feta alpha, gamma, kappa feCd/ör lambda-carrageenan andfer derivatives thereof and/or their physiofegislly acceptable salts, in particular on the basis oi iota and kappa carrageenan and/or derivatives tnereof andrer their physiologically acceptable salts. to ;|h^;©Q«í^xíie:;term^esrtageghx or ^afeageenanhle used es a generfe term for d group offong-chafe polysaccharides. which occur or are synthesized in particular in ceils of various species of rod algos. Carrageenan is a linear arrionip hydrocollbid, wherein varlouslypesofcarfageener) may befeistfegulshab as aiunction of/ftie chemibaiisfructufe,
Due fe lbe pasast i&amp;ia dilferenttypes. Thedefegcáffeív fs madepnmsriiyby fee pmporfieri oipfscfese anö'^S-aii^^äictÄ-l^ ^fiton^r of sulfate groups, görÄpr#«Äi:of ^n^0PiSö:'fp5 red algae, they are first washed and boiled in an Äiiasi ÄÖön. Iba solution is then filterem fe separate fee caNtens and algáé conefeuenís lom feepoíymer. 1o elate fee eæâgësââh lrôm: fee solution, the earrapecan is finally gréêlpitated éifeor fey alcohoi or piled using potassium chloride and then pressed. The carrageenan obtained may then be dried, milted and processed ..á#ebái#.ön· paröcuiar comme«·# interest are. in particular, Kappa, iota and iampé çanageenans, ty:pes of carrageenans may alternat vely be used, wherein kappa, rota and lambda űarsagaenan are used, in particular. as precursors. in thé eontextsf me present tevafiom I was surprisingly shown, on fee one band, feat excellent antiviral effects may fee tebisyeff by fee use of carrageenan as a poiystetearfee wixmappliedtefte mucosa in fee neoK and fesssf area;; while, on fee other hand, because oils hydfocölíöiddike prppsffes, Carrageenan forms an excellerdpteSectiye film on the ffioufe end throat in order So prevent dry mouth;or te dry dot the mucous membranes efficiently· and prevent fee: penetration of pathogens.
In connection with:the at least one polysaccharide or component (a), it has also proved to fee advantageous to use the substance in deíineéarnödnfs, It has proved lo be particularly adyanfegeops in terms of effectivpnass wfeeniÉeiéomposfeon comprises fee compépéottaym eirèiafivaiémount in the range o?'0:1:^::4i.^ij:|p;.partefi^;fe the range oi 0.5 to 30 wt-%, preferably in fee rartgaof 1 to 25 wt -%. more preferably In the range of 2 to 20 wf.-%, particularly preferably in the range of 3 to 18 wt.-%, based on fee composition.
In this respect, it fees proved fe be ifevantageuus iiftfegreomposifidn eoniins fee öömponehi (a) in m absolute amount irs the range oi 0.001 to Ii|, ipailipulafiy in fee rángó of 0:005 fe 4 g. preferably ίο fee range of 0i01 to 3 g, more preferafeiy in fee range of Ö;ö5 to 2 g. in particular in relation :fe en appliçalon unit, and/or in particular to an appiication size,
As previously desbrihed; fee use of a surface disinfectant Is advantageous In particular against fee background of a reduction In fee numfeer of bacteria, in addition to fee barder effect of fee protective film based on polysaccharides, in mis context it is provided that; fee: component (bj is poiyhexsnide.
Poiyhexenide 11 a common sieffc. rfftemNl? spoakfeg, ft is psiyhexamefeyions (PHfeB). An advantage of polyhexartee is, in paditeismis breed spsferym of activity, vfeiemte also directed ogÄfgipfet^Äthp^ai.. a(x|u|rÄI?^s:§ö'to: staphylococcus is already effective in as it idirootiy binds to fee bacterial cell wail and damages % thus leading fe death. Accordingly,, fee use of extremely tow cohcentraflons is possible, which thus minimixes the oecurrencaiof side effects, Ä^v#>:p?^)pide.^8frtd^'fcy''few sysiefetc absorption, whichaiso minimises the risk of occurrence : of side effects,
As regards the amounts pf ths isuffaeo disinfecting agent employed, those may vaiy wifein wide ranges. According to fee invention, it has proved to bp; teteippdus when fee amount of surface disinfectant contpadfeifha composition is in fee range of Ö.DÖ1 to 5 wt.*%. in particular in fee range of 0.01 to 2.5 wt>%, prsferabSy in fee range of 1:01 to more pmfersbiy in fee range of 0.01 to 1 w?,-%, pehfeulariy prefsmbly in feersnge pf 0:,05 to B «&amp;>%> based upie composifloh,
Furthermore, as already menfteuedjnlte context of fealnventiofelt bus proved to be; parMmfy advantageous to enhance :;fee effect: of fee at feast one; poiysacphar|ps by tbs additional use; ói ^ a preferably acidic glycosarclnogiycan, in fee context of fee Invention,: rife: provided feat fee glycosaminoglycamis preferably hyaluronic Md or its physielegicáiiv acceptable salts,: preferably tbs sodium self of hyaluronic acid.
As: regards fee amountof thg eemponenf or i^^ ss=^îc gíycössnfsl«ögiy^ri; íh pa^ciilsr hyaluronic aeld er its salts, used, this is ëpeiiy sänäble, It bas proved Id fee advantageous if the composisyipialrts the componun? fo) is an amount ranging tom 0.01 to 10 wt.-%, inpariieular irytherange of Ο.Οδ to 6 wL-%, preferably 1rs ths range of Ö.1 to 1 wf.-1i based on the composition.
Id order to alleviate the pain symptoms associated withidafsaness or ioifemmaiory diseases of the mouth end throat (sued as som throaty it has also proved te bo advantageous it fee composition comprises at least one local anesthetic as a further component fd).
In this context It is advantageous If the local anesthetic or the component (d) is selected tom the group of poiidocanol, bopocairfe, iiddeino andfcf anferoxdk Fferticuiarly good results are gbiinedi however, when feedomporfent (d) is:plidccanel, Tbs pejipcano! used in the present Invention, as de§ö#% .is .a mlxhirs of ethers of various rnscrogols with fatty alcohols, mainly iauryl aiconoc Poiidocanol is aiso synonymously referred to sc hydroxypolyethoxydodecane, rpasrogel laufyi ether or iaursmacmgoi 400. Peiidocanol can mix well wife Wats? due to fee lipophilic dodeeyi chain and hydrophilic ether chain, MorMyer, poliddeanol has surface-active properties, in fee prior art poiidocanol is particularly used in fee area oi meskine lor the elimination ofhemofrhoids or spider veins In fee affected tissue; moreover, In fee prior erf. polidocanoi may be used in skin ointments to relievo pain and itching of fee outer sfe (sclera or dermis). For the firs; time, and surprisingly In fee context of the: presenf invenhon,::fee application af idiidpcariol could be carried out on fecsensitive mucous membrane, in psrdeulap in cooperation wife w mueiiaginous drug, no Irdfalion of the mucous membranes was observed (in a: completely isomrising mannof, For more detailed infermstion en fee drug ^pdlidocenei", reference may be made to fee Rbmpp Chemie Lexikon, löfe edition, Georg Thieme Verlag, Stuttgart/New YorK, Voiume 5, page 3403, Keyword; "poiidocanol’', as weii as in literature referred to therafe, which is hereby futy fecerporated by reference In this content;
The amount of fee local dnasfefefc used: pray also vary within wide ranges, According to the invention it; has proved to be partioufedy eifedtlve when fee eempositien contains the component, (d) in a relative amount in fee range of 0 01 to 5 wt.-fe, in paieuiSf in thfefengeoi 0,0111.¾ wL#,;prefersb|y: in fee : tango #S$1 fe ||yW1%, more;praferahly ;n fee:fengedi:0,i:to i; wi.-%, based on the phaneaceuiica! composition. in ibis connection, it may be provided that fee composition contains fee component (d) in an absoiuie amount in the range of 0.01 to SCO: mg, life particular in the: range d;9Mte 350 mg, preferably ih: fee ranpef 8,Y;fe 150 mg, moropreferafely Irr fee range;# ;8,!fd 60 mg, pefilcuferiy preferably in fee range of 1 to SOmgybased m an appiioaiirfe unit. idamover, it haspMed fe fee essondal in fee context of fee invention· to mseibe individual components m the respective specie weight ratios to one another':
As regardfefee pofesarmhanbe, on: fee one hand, and fee surface dsinfectaht, on fee other hand, according to fee invention if is advaniegedds if the cefeposion eonfefes fee component (s) and the component.(b) in a weight ratio of ([a]: p;>j) tn fee tángálom 1;: :111,008::1:, in paftofer in fee range from It ffe §00:1, preferably in the ranpfrom 1S: 1 to 108:1, more preferably in fee range from 20:1 to ?0:1.
Moreover, ft has ipwéd fe fee: advantageous if fee composition according to:fee invensen oonfenseedb least one ppiysacehande or oompohént (a), on the one head, and thé st feast one preferably acidic glycsssminoglycan, inpafecufer hyalomnio acid and the sorts thereof, of fee component (cl , on fife diner hand; fed weight raSo of (|ai: [00: in fee range from 2:1 lefeOÖfe, ih paäcuiar in the range from Jrlfo100:1, pmferahiyinfee range from 1M to 5ör 1;, more preferably In the: rarrge lrdfn 8: $ to 30:1.
Riteiÿ, May be thvenfiyeiÿ: provided that the cömpositlCh contains teetefleast one sarfâcàidisirsfeçtahl <?rJb çompbnent|h) and the jtifeast óné preferably Äte'ii^^smiiiogly^ irtpftisular hyaSafsaid sqd^r the setts thereof Qrfimwmpenent (¾} In a weight ratio of ([bj: |p| infheysngsipf 1:1 to 1:1 0, in particular in the range of 1:2 to 1: :4, ioreover, fi may be provided according to tbs Wy entrópiát the composition A substance andfor ingredient in gartieuíár selected .muca&amp;a? ^#8ν® «pets, antisaptiOs. vitentins* ttaee éîérnents, minerais, nficronutderíts and ittixtyres^eireef, it may aies concept fiat thecomposition teterer contains at least one additive, in particuter selected tram the group insisting eiprocessing aids, cotoranfe, ibuffora. Iragtemjesr pertumss, erdender*, bindere, wetting agents and/or preservatives, pH/adjbsíers, pH buffering agents, thickeners, Ifevors^fidäsps^ten^^'s^tef^g. agents, acidifiers, sisbifers: pd/or δnäseρte^ahf^|i|¢s'i8n^ï^: !n addition, it has surpnsingly been found in the context of tbe present invention that it Is advantageous with respect to the relief of hoarseness; ®re tetoai or otter infiammsipry diseases often mputh and throat, if me cdinpesltloh: sddltibftèiiy contains a foantingisgenf, A teeming agent allows a me?« eiiarsl wetting dhthe skin er mucous membrane. ® thafifbe förmatibn of the protective film is even further strengthened when based ort;poipaeoharides or acrdic giycosaminogiycans Particutsuly good résulta are achieved in mis respect v^É the nee oi Sts tfihydnc aiœhçsglycerai, or adeeptaijis derivatives or esters. in the present invention, it may thus be provided that tbs composifion eompdsgs a foaming agant as a further active substance artd/or ingredient, in particular glycerol and/or its physietogioatiy acceptable derivatives or esters. As regards the amount ol such a fcamrng agent it may likewise vary wtihm Wide radges. Typically, tee composition according .fe:fhe: teverioé$É|hâ'tÉrë$e! ohitetertysiotcgteaity acceptable in an smountid (he range of 0.01 to § wtete, in particular in the range of O^DS to 4 wlÆ, preferably in the range of 0,1 te? Si wtS, more preferably ihiherange öf 0 2 to lhsii-%, based on me pïrarmaceuflcai composition.
With regsrrst to admiolsfhsioolot^ of tdosage formöí the; present invention, ifhisiis exfremety diwrsevand may:beiSpeo|oa!ty tailored or adapted to a spécifié purpose,
Aoeerdiog te afifStiprefarrgd einbsdimenf: according: toile invention,: |f may he ptsviuedteat the imposition isprsssni as s solid dosage term ahd/or wherëiP me composition is present as a tastet, dragee, piti, bard cararpet or the lie, In particular as d lopnge, in parfcuiar vteereld tee lesenge nes s fetal weight: te tee range of O S to 5 g, in: pertiafiar in the range cf 0.0 to 4 g, preferably In the range of 1 to 3 g. irt order fe atksw a good retesse of the active substances of ingredients, it is pÄÄÄ te« e$nt^>sÎfôft-ô>n}â^s:^e:i^vé' atÄr matrix and/or mass. in partfeuiar in stpj^îtelâied on sugars andrer sugar substitutes, in patecuter where the sugars are selected tom the group of sucrose, giueese, in particuter dextrose, and fuetose and?or, in particufan wherein the suger substitutes are selected bom sugar siedhpfs, preferably from the group os mannitol xyiitol, sorbitol. fssnmif. mattitól syrup, tactitet, íeabíose, fitecfödilgosaccitaridea, giucans, petyglueese, particularly: preterabiy tsornalt
As regardstne guantities of sugar or sugar substitutes: usedythese: are variable. In tee present invention, ft is preferebie tote teb used amount Is in the range ol 30 to S9.9 wt.-%, in particutar in the range of 40 to S3 wi-%. preferably In the range ο! Si) to # *1 %. based on She composition.
As tor Μ solid dosíáíje ipmi ín its physical smitedjmant, il lg usually pröMlciiSd th^í fig solid dossga item releases o therapeutically effectip amount of fee active Ingredients and/or substances on sucking when the solid dosage form is administered in the mould sad throat of a patient and id sucked.
According to a further petsntod it may be provided tost Ida composite to |msent as a viscous arsd/dr paste-like aMi#i iorm and/or vvdemin ide composition: is present as an ointmerfe cream, paste, gel or ide iiko. in this context, it is usually provided tost the compsiikm isapeous, aicdhoic or aqueous-aietottolie or organic based.
Moreover, ii may be provided according to ifto isvanlion thai toe composition oontams water, in particular in a relative amount of toast iô wi.-%, in particular at least 20 wt preferably at toast 30 ψΙΜ, basedm toe composition.
Moreover, vsscous or paste-like forms may he provided, wherein the composition comprises at least one excipient, in this context Ids pstecuiariy preferred iffeetexcipleni is selectee iron; toe grape; pf solvents, soluhliiiers, emuisidersi arid the lie, end/dr wherein toe earner selected from toe group ol ethanol, isopropanol, ethyl carbonate, ethyl acetate. bensyi alcohol, benzyl benzoate, propylene glycoi. 1,3-butyl giycol, as weii as combinations thereof. .;ii^fâfMfb:brâil#rb?isd;6^pÂô isprevided -0¾¾ this prefeafeiy aiso inoiadesat least
Is an blaadtor felandfer in parteler wherein toe carder is selected from woof grease, eolonseed oil, #t», giyeeref fatty acid esters, plptoyfens giycois,add somhinations toereof.
To achieve a good application, on toe one hand, ami a good adhesion of the composition to toe skin or mucous membranes, in parMtiar In toe mouth and toe throat, it to advantsgecus to adjust toe compsidn of toe mvenhon to s defined viscosity in viscous or pasty form. In {Ns case, be too runny nor be excessively thick or lough, in particular with respect to toe applicability it has proved to he particularly preferred: accordihg to the invention, in particular at a temperature ol 25“C, tital toe composition has a Brookfield viscosity in the range of 500 to 1Ö0.0ÖÖ mPas, partiojiariy in: the rangs to Äitol$$DQ rtoi^as, iprdirabiy to tbsrangs of 1,000 to 10,0001 dittos, partieuiafiy preferably to the range of 1,500 to 8,000 mPas. very particularly preferably in toe range 2,000 to 6,000 mPa.
Moreover. it may * especially in too case to aqueous or aqueous-alcoholic based compositions - be provided that toe composition comprises at least one gelling egeni. toreirahiy, toe gelitog agent may be selected from ilte/group oftoenfonitos, sliicic acids, poipofyite acids,: oafhomars, polyvinyi pyridiidohes, cdMssesnu eeliuipse dsrivaiivss, xapfeensstod mixtures toareof, preferably cel iutose ahd sellutose deriveflves. írt padicuiar, tod plfig agent is selected ircte the grbup of böhitöhitbís., :$ΐϊίΡ!<ϊ acids, polyaeryiie acids, oarhöteers, pelyyinyi pybolidortesi cellulose and cellulose denvatiyes, xanfeans and mtxlpsfesreot, preferably cellulose mû cellulose denvatores.
As regards the amount oftos piling agent ased, this Is variable; Preferably; the compositibn eccordíno: to: :tod invention contains the galling agent in a relative smounl in; fee range ofö.01 to 20 in particular in toe range 0.1 to 10 wb-%, preferably ;n the rangeM to 5 wt more preferably in toe range of i ts 3 wtbased on the composition.
According to artetoer preferred alternalive embedimest cf the: ptosedt: inverioto It may be: provided: that the uumpösltibd according io toe tovstdibhiis in: toe form of a ilquid dosagfett may: ha,:in:partic«iaf, a fluid. moufepash, moufe rinse, juice, gargle or toe like.
With regards jo toe : pröviston of ithe composllien epcoring :to toe : Ihyatilibh as a iiigpiibcsags fermait Is typically iprevided that the composition is aqueous or aqueous-alcohol-c based. in this connection, It ig in pariicuiar preferred if tie imteöiÉ?n contains water, in particular #j$fpr* the composition contains: « ín pgrtïoulsr in a relative ätleast 20 wt.*%, prefembiy st least 39 wí.'%, based ön ths composition, and/or in páilioöisr ip g fsiative amount in the range of 10 to 38 wt*%, in particular in the range 20 to 95 wt-%, preferably in the range of 30 to 90 wt.-%, based on the coasposltlon. in: order that the inventite compesllibh has a -axöpÄ'.p^w^Äiri-i^g its application, It is preferred that the composition comprises at isast one add and/or base, in parficuiar for forming a buffer system, asd/or #i^^':i^:«>mfJ08i8on.:i^ifeiins at least a buifer system, and/or wherein the eomppsíSös preferably coorpdses si least a base, in pestipufar wherein the: base is selected ttom the group of amides. çarboxyietes, alitai i aod/pr aliiaiine: earth metal hydroxides as well as/mdiures: ahd eonSbinatlons: thereof, in particular alkali and aikaiineeatib mete! hydroxides:, preferably sodium hydroxide, /Within ileeirihooisnent it: may aiso beiprevidedilmi the itqirid composition is in She form of: a spray, aerosol or the like, ipthiS: context, it is usually pmÄd that1 fee composition Is in the form of spay or pumping devices that are: weii known to psrPte skilled in tne an. so mat no further types are required in this respect. lie presshihveoííon Is-»vá»íí^»^^iií=:át;:ip^!!^ - thus a composition, in particular a ptermaceoiieai composition,
In particular as desoribed: , .^i®f§r^bl^:::isR::ithS'i;ifef^ of a solid1 or liquid, preferably a solid dosage which, in particular, is suitable for the topical and ferost, wherelhtbe comp osition - in combination and mepcotlvely ihieffeoilye, partieuiadypgtmaceufaiiy effective ameubfe - comprises: (0) at least an antiviral, snd/or antiviraiiy effective, piysecehande: seieoted: 9pm osmagseoate and/or their physiologically acceptable salts, gaiactsn sulfates and/or their physiologically scceplabie suits and polyuronides and/or their physiologicaliy adseptable salts, in a miatiye ahtöuSí in the range of 0.1 io 40 wt.->%, In particular in pie ringe sí9.5 to 3Ö preferabty' in the fände of 1 id 25 wteW, more preferabiy in tie m^iëf2p;2Ô-^.--%,.pi&amp;tartypreferebiy in the on the composition} (b) polyhexanide as a surface disinfectant in a reiatlve amount in the range of 9.001 to δ wtin particular in the range of 0,092 te 2>twt<-%. prefefSbiy in: the range of Û.Ô05 to 2 MM. more preferably In ihn rnnga of ;9.01 to pariSculariy preferably In the range of Q.Ô5 to Ö.S based on the composition; and (of tipiprmtlc acid or sits thereof in a relative amount in Iterance oi 0 01 lb 19 wt-%. in particular in the range of 0.Ö5 to § ΜΙ, preferabiy in the range of 0.1 to 2 wfe%, based on the composition; (dlopikmaiiy at least one iocai anesthetic in an amount In the range of 0.01 to δ wt.-%, In particular in fee range of 0.0$ to 2.5 wm %. preferably in the range of 0.01 to 1.5 wl-%. parficulaby preferabiy in the range of 0.1 ίο 1 vvt.-%, based on the composition.
As regards the application of the composition according to the invention, it is particularly suitable for use in medical, pharmaceutical and food technology, in particular, the composition according to the Invention is suitable for use in human medicine or veíennary medicine.
The composition according to the present invention is particularly suitable for use in the prophylactic or therapeutic· treatment of hoarseness and irdiammatory diseases of the mouar pd ttfoat, esp^ieily sers thrpai, In pmiiouiar te the topisaf teátnentmf hoarseness or sore threat. thereover, the pherrhscebtieai composition: äs Ideírnod aboveis suitable for the preparation of a medicamtet cf Éefapeutie agent :te prophylactic of tbsrapeutie treatment #.^i^^eÂilipià^::âi$ÉIÉgs of tie mouth and throat, espeeiaily sore tenet, in parficuiar tor the topical treatment ol hoarseness or sore throat.
For foftherídetoils ofti lhé use of;foe: invention and lo evőid unnecessary repetition, ÄtoÄ tody be made: íQ öw abdye fernes el foe compositionaccording to the invention, which apply eefrespondtegiy to its use according to the invention.
Norther embodiments,: modifications:: and variations ns well as advantages according to ijm present invention are readily ibiSdermbte skilled in the a| upon : reading too description toitoouhidavtog ihe scope of toe present invention. the present invention Is iiiustrated by too toSlbyi!n§ exempisfy embodiments, any »ay. A) Preparation of inventive compositions in the form of lozenges on hard saraméi base and of comparative compositions topat Jy to the %m of ioxsnges on hard caramel bass
Various: oompostoons, aocoráhgfotoe Inveneoo andivot aoeorOinf to toe invention, are producodil toefemr of togenpa on hard oarsmeibase, wherein a sugar spbiitufo for storage or embedding the sctiye ingredients: and sobstonces, reigeoiiveiy xytitol and manóitok, was used in equal parts by weight. Similarly, however fructose and/or glucose syrup or other sweeteners or sugar substitotos tody iSlternetivoiy also fce osed as a matrix material, The preparation shtosefps; or hard ceramet is eftoctsd In a: customary manner by SipenreO: skilled: in foe ait
The ptaing materials (acte ingredients,: flavorings, additives or were weighed aGoordin| to is partefor formulation andlindlyidoëiytoiséd foto, foe:msinx materia! (xylite! and mönÄiJ. The addition operation took place under beating, Tbetoomogensous mixture of ail the rawmaterials was transferred into s metering o? dosing uniti,There, the lozenges were prepared iff: toeir respective Side and weighed during die j»o^?.t^lf-savtà^ÿMgh.tsof £5·§ per application unit or per toureoge. to this »ay. both hard eareme! aceording to the Invention and hard carato# not according to the invention were produced for comparison.
The hard caramels A, I and C according to the invention contained respectively 10 wt.~% carrageenan as polysaccharide and ô.25 m-% :piyirexartoto as surface dlsinfectont. as acte iogrediants. The hard commets B and C also contained U.2 »?.*% sodium hyaiuronate as an acidic gfycosaminogiycan. Hard caramel C also contained 0.5 vvt.-% poiidocanoi as a focal anesthetic as a tourto active component. The waght: fietosntagos are each based on toe dry weightM too composition. The complété formulations of the hard caramels A. 8 and C according to toe invention are shown in Tabla 1 below.
Table Trformulations of the hsrdcsramsfs A; 8 and Caccording to the invention
1¾ pondneentive comparative ieblels D sniö g dHfer&amp;ö îfom the comparative tabiots acçordiog to -thé invention in terms: of lm aoive lngrsigntSi Insofar as they did fcgrsdtotgéíPÍ^SdP «erging- te termyeniion, but rather represented monomreparations of the active ingrédients used: according to fits invention: The comprisonigOief P: onjy contained the aotiye ingradiant polysaccharide canigaenan in an amount of 10¾¾ based on the dry vyètgM; of tbs compositioo. The .d#tp^^íR' tabt§;l#^5c^^|n#á the sctive ingredient Piybsxanide In an amount; of g^SwtAl, bass# on lie dry weight si the composition. The missing ingredlehis with respect to lie ware lepiapd by equivalent weight related amounts of mslix meisriai. δ) Efficacy and application studies with the iosenges A, 8 and C according to the invention and the comparative
The lozenges A to E described above under A) ware used as iorenges according to She invention and the comparative losanges, in addificn.: gargles based on sage .isiï<ir:comrniôïiéisf:i:^ygh· drops were used for comparison purposes ;in the: context of the efhcagyahd applioation studies.
Td study the sfitefvsness: of loaasps: according fis th» invention A to S^lhedohiparison fesenges D and Hand ihartharapeutic measures of the pripr art (iie-pfglesiehd Cough: drops), a group of t SScui^cts. eged 18 te ?§ yearn old, of which 8? ware msla: : and 38 warefemale, was used; The subjects suffered hem hoarseness and iniismmgiory diseases of the temaf and pharyosdee fo Hu-like infections end the associated pais and mfiammaiion symptoms. 15 sehjeefs each cecaived1 one of the: ioeenges A fo £ three times daily over s period old days. The subject group F received gargling solution based on saltwater idndvSage aisb thfea itimes: daily over a. period ef 3 days, Moreover, the subject group © received a commercial cough drop three times daily; Äs pft of lie treatment each composition or therapeutic measure was rated in terms of the decrease in impairment of phonation, reitevlng pain symptoms, fha sustainability of the treatment, in partiauisr with respect to the; pain: symptems, relief of inflammatory symptoms andÉs moud) feeing according to the seheof grading system p* very good ;fo Sa? unsäösiacfefy): The results thereof are shown; its Taste 2 below,
Table 2: Assessmentof the myentip co^ comparative compositions or therapeutie measurss of die prior art
ixcsltenî .-«suits were acfecveb Over a very: good rang« with respect io all the examinee enteria fer ail three inventive lounges. Th« best with fee ihvanM ic&amp;enge C. In pafedular. fee ms«; ei fee less; anesthetic poSidocandi lésés fe an even teher eflviätion of the pin symptoms,: äs wetiäs wife respsÄfeö sufegioabiSily of gain főttéi. Wife iii:feväftSve losenge 8. which also gontafeed fee gtyecsaminogiyrp hyaluronic add, fee® were even belter resits, in prlicuiar with respect io: fee decrease in Impairment of phorsation, fean fee inventive ioeenge A. The additions! use of hyaluronic acid presumably Seeds · without intending to be limited fe this case to this theory - to an overall further improved wetting et the mucosa, so feat dehydration Is pavéntei even better. As the above variants show however - despite fee sight differences in fee opsrattve efficiency - ail fhefnventiy« ieasngM hada similar effect in the treeimerit of hoarseness and infiam mafery diseases of fee mpufe: and throat, especially sore fernst
Wife fee eofepasálve compositions D and £. however, no satisfactory results were obtained, in particular, the pain and: shfiammatidn symptoms could only be relieved very inadequately wife fee confearfelve; bompositiorisi® and It The fedne* preparations of fee active Ingredients used are thus nol suitable when used as fee sole application for fee effective treatment of hoarseness and inflammatory diseases Of the mouth and throat Rather. fee significant differences wife respect lo the operative efficiency of fee respective fed!viduatafeive ingredients Compared wife fee effeot when administered fef i mutual erfeänesmenf of action, should be seen as evidence of the existence of a synergistic effect,
Overaii, the worst resuits were obtained with fee two treatment methods of fee prior art. Neither fee: gargles F nor the cenyenfionsi cough crops Bi ceuid alleviate fee poblems associated wife hoarseness andMammatfey diseases of: fee mouth and throat, discomfort or symptoms inan sieient manner. in particular, such therapies do not even result In an alleviation of fee pain symptoms of inflammatory symptoms, Ip addition, ns aodaiarated; decreese in fee impairment of phonation couid be obtained with these two compositions.
Overall, fee investigations show feat fee use of compositions according to the invention fer hoarseness and inflammatory diseases of fee Uirôât and pharyns relieves: aif:generally:assdoiated symptoms; lb particular the relief of pain end inflammation symptoms. In addition, fee: application of the cofeposiihs accorCing to the invention leads to an accelerated decline in fee impairfeefe öf fed pfldnaiion, in adiiion, fee mbufifeei of the composition: accetding fe the; invention: Is improved: compared : to the treatment methods oHhe pdor arfi; WifePdf: intending to be limited here fo; a theory; this may be ascuifed: to: the wetling effect ol the poiysacChadds: used, oh the crie hand;.; and and possibly to the hysfufehie acid, on fee oihsr hand.

Claims (6)

  1. krákqgás ê$ torokfájás kezelésére SZABADALMI IGÉNYPONTOK
    1,,Kíifp2löíőv^§^(»|®B előnyösén; szilárd ;§fpg vsg$:i%aÄ fofftiätäfeao, ISiőíÉSé» sziláid dózis formájában, főleg; rekedtség {hoarseness); vágy torokfájás (sors: jiroat): helyi: kezelésére, a száj és: $psk gyulladásos befegségeioék fmM kezelésére, ahol a kompozíció - kombinációban és minder: esetben hatékony, elsősorban gyógyászatllag hatékony mennyiségekben ~ a következőkéi. tsrfaimazzs: a) legalább egy vímseiienes és/yagy yifYseteessn hatékony poiiszacffefid; ïbfêjy· ír YáfeaziaikiÉ /ksrrapnánok és/vagy fiziológiailag elfogadható sóik, gatakián szgífátok és/vagy ii2töiőgtaííág: elfogadható sóik, és poiiörbnióek és/vagy fízigíégiátlsg: eifögsdhato sóik ya) sik^s#! b) pííhexsnidok, mint té® téti fertötlenfik: (süríaoe pmfç&amp;mî} (.{Öl;aiMresz“]: valamint ej biaktronsav vagy sói („{c} alkotórész']. 2. fe l. Igénypont szerinti kompoziéi, ahol; áx (a) alkotórésznek az. áltagos moiakulafömege az OOP és ίΟθδΟΟΡ Da közötti tartományban van, különösen a loöőöés ?3QÖ00őÍa közötti tortomarpan van, eíőnyösen a 2Ö00Ö és 50ÖSÖP Da közötti tartományban van, és még előnyösebben 3 30000 és 3000000 Qa közötti tartományban van. elsősorban géipormeáoiós kromefegrMavai (#£) meghatározva,: ainyóééá a DiN SS672 szabvány szerint; és/vagy ahol az fa) ikotörész blopoiimer és/vagy biológiai ereösin polimer;: ès/vagy :áboi az (a) #|ÉÍ|^::teöpo!Ííp<dií|iddok:: kivagy hétoröpofeabhabdok közi, előnyösön hétaropoiiszacbariciók;közül választható ki.
  2. 3. Az 1. vagy 2 igénypont szerinti kompozíció, ahol az (a) ..alkotórész,. elsöspÄt * fpüfets anyagként (muc^:;^tánee|^ft^gá!t^;:»yóse« gyógpzer tormájában, kiönösén zúzott. porított vagy extrahált algáik, növényfészek vagy eötin^iiátetétéiÉÉ'ö^^ában; és/vagy ahol az (a) aloiréez, elsősorban: a pőiíszashgrta einyöseo nyáikés anyagként van szolgáitáivé, eisösoien exíraktum tormájában, itaitei, ahol az extraktum főleg vizes, aikohofos vagy vizes-alkoholos exíraku.mboi, különösen vizes exiraktomból van kinyerve; különösen #0! az exlraktumrtok, eisösöién 3 száraz ezksktomnak oipn győgyszer/exirskium hányadósápÉRIvap, abo! az úgy van kiszámítva, mini a gyógyszer kíinduiasi artyagabék főmeg-arány bányaöosa a kinyerendő extrakiomboz, a 0,1:1 öíi^&amp;áortitiÉm;::.8 0,ö:f és:,$§;1 közötti tefüietben:, előnyösen a 2:1 és;20;1 közötti tartományban, előnyösebben az 5:1 és 10:1/közötti tartományban van.
  3. 4. AZ: I# ipnypbntok bármélyike; szerínl kompozlol, |bcí az |a) mikötórész; gisosorban á poliszacbaril, előnyősén a: nyéikas anyag, a kőveíkazökböi nyerhető ki; izlandi zazmófüohen isiandicus). orvosi ziliz (Akihaea offleináiisL}, lándzsáé úfiiú (Piarrtagö laböeöleta b/):t mályvéipeiva:;eyivesirís L |s;to. negieß^ALLil)y:gör%s#gi::pgopeila foeitom-gmeplim 1,), kosborgyökér; bife^sipy^ni^oi^tpÄy,. továbbá algák, vörös algák elsősorban vörös aiga: fejtik; a CítobÉp,: Eophema;:és/vagy Gigartioa nemzetségből yeiémlbt; mindezekkombinációi: és/vagy ahol; az (à) alkotórész a kbyetkéZök közi választható ki; alfa, lóra, gamma,:lappá Ss/yagy iamödá karragenársok és/vagy é!fo|adbaiö sóik, elsősorban iőtoskarragénán és/Vágy származékai és/vagy liziollgiailag Összeférhető möi; és/vagy ahoi m |á) alkotórész, elsősorban a eoiiazecbgrid, előnyösen; a nyálkás anyag, hetsröpölimer, amply/feta, alfa;,; gammito kappa és/vagy iíambda kärragenaitpn Is/Vágy származékaikor; ::es/vagy Ozioiógiailag elfogadható sóikon.stopéi, elsősorban: az lóia és kappa karragePábon és/yagy származékaikon és/vagy ííziotogiaiiag eifogadbito sóikon átépül; és/vagy ahol az (a) alkotórész, elsősorban a poliszacharíd. előnyösen a nyáikés anyag, extrakctovaf; nyerhető ki algákból,; elsősorban vörös algákból, fölső aübondrys. Eucbema és/vagy liosríina nemzetség vörös alga fajtáiból. S, Az 1-4. igénypontok bármelyike szsrirrtl kompozíció: aho! a kompozíció olyan reiativ mennyiségben tartalmaz (a) alkotórészt. amely a 0.1 és 40 tömeg % között? lartcmánybam elsősorban a 0,5 és 30 tömeg % közötti tartományban, előnyösen az 1 és 25 tömeg % közötti tartományban. előnyösebben a 2 és 20 tömeg % közötti tartományáén. és különösen előnyösen a lés 18 tömeg % kölsttiigftöRienybae van. aike^ptöglclóf® âtatpoztvâ; és/vagy ahol a Ismpözíeíö olyan abszolút mennyiségben tartalmaz (a) alkotórészt, amely a 0,001 ás 5 g közötti tartományban, elsősorban s 0.005 és 4 g közötti tartoms??yfcan« előnyösen a 0.01 és 3 g közötti tartományban, előnyösebben s 0,05 és 2 g közötti tartományba??, és keioösen ötönyősén a 3 es 18 tömeg % közötti tartományban vám elsöserban e§y és/vagy elsősorban egy alkalmazási méretre vonatkoztatva; és/vagy ahol a kompozíció olyan mennyiségben tartalmaz (b) aikotörészt, antely a 0,001 és 5 tömeg % közötti tartományban, elsősorban a 0,01 és 2,5 tömeg % közötti tartományban, előnyösen a Q;8S éé ;| tömeg ök közötti tartományban, előnyösebben a és 1 tonlsg :% közötti tartományban, Aá köSÖRőseh előnyösen a 0,05 és 0,5 tömeg % közötti tartományban van, á kompozidéra alapozva,
  4. 8, Az 1-S. igénypontok bármelyike szerinti kompozíció, ahol á (c) alkotórész hielurptisav nátrium sója; és/vagy ahol á kompozíció tartalmaz (c) alkotórészt olyan tnennylsé^ben, amely s 0,01 és 10 tömeg % közötti tartományban, különösen e 0,05 és 5 tömeg % közötti tartományban, előnyösen a 0.1 és 1 tömeg % közötti tartományban van a kompozícióra alapozva: éSÁzgiigisí' átlót à kôîiï^Âielô tärtälmss Ciö); yáiíkötiöfi^éi tsl^íi relativ mennyiségben, smély a Q.öl és 5 tömeg % közéi tartományban, elsősorban a 0,05 és 2,5 tömeg % közötti tartományban, előnyösen a 0,01 és 1,5 tömeg % közötti taftománybaniés eíőnyöeébbeniaö.l és 1 tömeg % közlttílérioményban yapra gybgy^szgiiikompozloiora aiapozya; és/vágy ahol a kompeztdonek vae legalább egy helyi teésleleg^i {áj áikotőrész; és/vagy elsősorban ahol a (d) alkotórész a kővetkezők közül választható ki:ambroxol, különösen ahol a (ci) alkotórész poiidokanol; és/vagy különösen aboi s kompozíció tartalmaz (d) alkotórészt olyan relativ mennyiségben, amely a 0,01 és 5 tömeg % közötti tartoménpii, elsősorban a8,05 és 2,5 tömeg #!#Äv|äii3{BäöyÄ,ÄfäiÄ.3'QP:ifei:4,f tömeg % közötti tartományban ás előnyösebben a 0,1 ês 1 tömeg % közötkilsrtómányban van a győgyásza&amp; kompozicióra alapozva A Az 1-8, ígénpbntOk Öartnéiyike szenntl kompozíciójából a immpazídé tartalmaz Jdj aíköiliszt olyan abszolút mennyiségben, amely a 0,01 és 500 mg közötti tartományban, elsősorban a 0,08 és 250 mg tartományba?;, eiönyösen a 0,1 ás ISO mg közötti tartományban, eiőnyősehbéil a 0,§,§&amp;,Bc|äg és különösért előnyősén az 1 és 28 mg közötti tartományban van és/vagy abel a -½ 8 {fej alkotórészt olyan ({alifbli tÖmegsÄpaP tartsimsZza, amely az 1:1 és 1000:1 közötti ta?lomáí;yhan van, aisősörban az 5:1 és 500:1 közötti tartomâ|$â&amp;i:yif| liisyèséfi a 15:1 és 100:1 közötti tartományban van, és előnyösebben a 20.1 és ?0;1 közötti tartományban va??, és/vagy ahol a kompozíció az (a) alkotórészt ás a (c) alkotórészt oiyan ([a]:íc]) tömegarányban tartalmazza, amely a 2;1 Is SöÖil közötti tartományban van, elsösörbán a 3:1 és 100:1 közötti tartomápybán van, előnyösen az 5i és §&amp;í közői tartománpan van, és el&amp;rtyösebben a 9;4 és 38:1 közötti tartományban van; p/vagy ahol a kompözisiö á |b| aik#részt és a (e) alkotórészi oiyan (;bj:jc)} tőmagatánybán tartalmazza, amely az 4:1 és 1:10 közötti tartományban van, elsősorban az 1;2 é§1 A közötti lartontányban van. Az 1-7, igénypontok bármelyiké sprint; kompeziel, ahoi a kompozíció tartalmaz légiébe ágy tovább; aktív anyagot :ás/vagy alkotórészt, amelpkékélsőserb® a kóvetkés^ köaOí lëhei kivéííasíztaní: nyáikaszi védő szerek (mucosal protective agent), antiszeptikumok, vltarmnok, npmetsmek, ásyényi ányagok. míktdtápanyagök (mioiehotrient), és mindezek keverékei; és/vagy ahol a kampöZiciőprtaiffiaz tpvébbá legalább egy adalékanyagot (additive), amelyet elsősorban a kővetkezők közéi lehet kiválasztani: ígíoelgozásí segédanyagok {processing aids), színanyagok, pofiérek, litányagok (íragrsnGe), illatszerek (pertumé), kitöltő: anyagők |ektánfiér), kötőanyagok Ibiédér), médvesitöszerek és/vagy latiösitöszerek (preservative), pH beáiíitök, 0 puffereló aaereik, tsí/fiiöányagök Itrsiekeftör), íz- és líatanyagok (áevout), aregiák, édesítők (évreetener) és édesltőszerék (sweetening agent), savesítok (acidifier), siablzáfo äifrte^itiisöfiiok, és mindezek keverékei; küidösen ahol: aÂkanyagként a kompozíció rendelkezik glioednpf éé/vágy: »8k fizbíógiaiísl Äpdhatö azárroázékáivak végy észtemiveL elsősorban elyan mennyiségben, amejya 0,91 és: I tömeg % :köÄi tortomlhyban, etsősörban a 0,OS:öé Atömeg % közötti tartományban., előnyesért a0,1 és» .a 0(2 ss 1 tömeg % kőgííítí tsríományban van a gyógyászai kompozícióra alapozva; S. Az1-8. Igénpontök bárrnélyíp szerinti kompozíciói ahoi a.ÂpozielôÄ«ivan jóién, és/vagy shot a kemjx»iö: láblöttá, drazsé pia, kömény karamell vagy: basoniök ferrriájaban van ίοΐοη, kölönossn négyszögletes cukorka (iózenge) förmipban, ahol a négyszögletes cukorka teljes tömege elsősorban a 9,6 és S/g közötti tartományban, ikölaöóefius teftománybaa,. előnyösen az 1 és 3 9 közötti tartoményban van; aboi a kempozieié az aktív 'árt^ökáti^^gjll^i^^k^ső^fbaR szilárd mátoxbamés/vagy másszában: tartalmazza, különössn olyan mátrixban és/vagy kompozícióban* amely »fokon és eukorpóSókon f$pr sübstitoíe) álapui, ahol ® cukrok aMvgpzok közűi választhatók É; Szacharóz, glükóz elsősorban O-glükóz (dextrose) és fruktóz, és/vagy ahol s cnkorpótíók elsősorban a cukoraikoholokkózúli váiászthaíök ki, különösön a következők kÖZüi: manóit, vilit, szerbit, «ornait, maliit szirup, laktit, ieukróz, truktooiigoszaohahbök, pokánók,: ipoligiuköz, különösen előnyösen izomait; és/vagy különösen ahol a kompozíció olyan relatív mena^l^iiiiÄitÄÄfbkat és cukorpûtlôkat, amely a 30 és 99,9 iörna| I ÂÔi tartományban, különösen a 4Q és 89 tömeg % közötti taffömloyban, előnyösen m §0 és §3 tömeg; % közéi: tartományban van, á: kömpoziöiőra alapozva; és/vagy különösen ahol a szilárd adagolási: forma, eisoeorban egy négyszőgletos cokorka, ügy ven kialakítva, hogy a szuárd adagolási forma, elsősorban a négyszögletes cukorka, kibocsássa aktív alkotórészek és/vagv anyagok gyógyaszatiiag hatékony rnermyiségétlsdopogatéskok amikor s szilárd adagolási forma egy beteg szájába és torkába van bevezetve és szopogatják azt, 1Q, Az í-8> Igénypontok bárrpetyíke szerinti kompozíció, ahol a kompozíció viszkózus és/vagy^pasztsszerü be^zatém formában van jelen, és/vagy balzsamként («méhi| krémként, pásként, gélként vagy hasonló formákban van jelen; Különösen ahol a kompoxícó vizes, alkoholos, vizes-alkohotos vagy más szerves anyagos alapú; és/vagy különösön ahol a Kómpozíeló tartálmaz vizet, eisösorba« IsgÄb 1$;§mei 201ömag 1, alőnyösen leplbb 30 tÓ;me| % relativ mennyiségben a kömpoiÄf^Äp^^'iliilÄ/Äyösen legal» olyan relativ mennyiségben tádaimaz vizet, amely a 10 és 90 tömeg % közötti íadománybán, előnyösen a 20 és SS: tömeg % közöts tafibmáfiybao,: éihyosebben a 30 és 80 tömeg % közötti tartományban van a kempozíciora alapozva; Ós/vagy különösen ahol a lompszíciö; tartalmaz legalább egy gyógyszer-kotöanyagot (excipient), ahoi a gyégyszerdröianyag különösön a következik közül választható: ki: oldószerek, szolobiiizáto szerek, emulgeátö szerek : ás basoníók, és/vagy afm! a horöö^ (cerner) a kővetkezők: közül; váiászihgtó ki; eiansí, izopropáncl, étikkárbohát, s3b»t||.:|p^lalkobo?,.: píppimpitöi, 1,3-buitigi.iKoi, valamint mindezek kombinációi.
  5. 11 .Alii igénypont szerinti kompozíció, ahol a kompozicó tartalmaz íegalébb egy gycgyszer-kötöanyagot. ahoi a gyógyszer-kötőanyag otáj és/vagy: zsír; és/vagy különösen ahol a kompozléié· á JÖVélézök közöl választhat ki; gyapjézstr, gyapotmagölál; vazéíím glicerin zsirsavészísmi, poiietiiéng|koíok,: óé minié» kombinációi; küipőseo arról |S°C Pmétliltilfei:' tctepzieíó olyan Bróoktield-yiszkozííéssáí:: bír, amely :äZ: 108: és 100009 mPas közötti tortományban, különösen ;<t: l§0 és: SDöSO mftas közötti itartómánybab»·, Äyö»' M:. $$&amp;' èé 1Q0ÖS n#as- közötti tartományban, előnyösebben az 1500 és 8000 mPas közöiti tartományban, és különösen előnyösen a 2000 és 6000 mPss közötti fanománybaty vahi: és/vagy különösen ahoi a kompozíoi tartalmaz legalább égy gélképző szert (gelling agent),:: ahol a: gélképzö szer e: kövétkezök közül választható ki; behföRitök, kovásáv;; pólíókríísavak, ikarbomerek, polivinitpirrbfidonOk, cellulóz: ás cöliulöz származékok, xantánok és ceilüíöz származókek: és/vagy köiönösénáhöl áJömpózyó a gélképző szert elönylsen: olyan relativ : mennyiségben tartalmazza, amely 8:0,01 és.OÖ: tömeg % Kö^itsffemMybáf!, különösen á 0,üés 1 OÂtëg'l előnyösen a 0*5 ès: őtőmag:! közötti: tartományban és előnyösebben az 1 és 3 tömeg % között! í.artományban van a kompozícióra alapozva. 12. M1-6. Í0nypr»feft háifesiyikó -sséíiö teppefe» aboi a kompozíció vert-pién, és/Vâgy ahol a kompozicii {bipblkkénl, szájmösö készlinenyként, szájöbtító készííményk|rit, udlfifslként (julea), gargarizáló oldatként vagy/hasonló fetmákhan yen jeten; különösen ahol s kompszíeié vizes/ alkoholos vagy vizes-atehölos alapö; és/vagy különösen ahol a kompezieiO tartaimez vizet, essőserbán jepibb tö tömeg %, kpönössn iégaibb 20 fŐniég %, előnyösen legalább 30 tömeg % reíalív nmhnyíségben a fesmpoziéiéfai alapozva. és/vagy különösen előnyösen legalább olyan relativ mennyiségben tartalmaz vi^b sméiÿé 16 és: 68 tömeg % Hozói tartományban, előnyösön a 29 és SPiJmeg % közötti tartományban, előnyösebben a 30 és 9ö lőmeg % közötti fertemányban van a ikompozicióra: alapozva; és/vágy különösen aboi a kompozíció tartalmaz legalább agy savat vagy bázist. így alakítva: ki oionyosersi egy puéor rendszeri, és/vagy ábei a kompozíció tartalmaz legalább egy puffer «)Ät legalább egy bázist ahol a bázis elsősorbán a következők közűi váiasztbai ki amibofe kafboxilátökv áikiifem Mvagy alkafilöldfem bidroxidok, vagy mindezek keverékei és kombinációig elsősorban aikáiitéib és/yagy alkáliföldfé^ Jiidroxíéíísfe, küfőríósén náfeem-hidroxid: és/vagy ahol a kompozíció különösen permekként (spray), aeroszolként vagy hasonlé fermákban van jelen.
  6. 13. Kompozfcíö. elsősorban gpgyásMk kon^zfelo elsősorban az 1-12. igénypontok bármelyike szerint, előnyösén szilárd anyag vagy felpdék formájában, kionősen szilárd adagolási formában, főleg a rekedtségnek és/vagy a száj és a török gyulladásos betegségeinek helyi kezelésére, ahol a kompozíció ~ kombinációban és minden esetben hatékony, elsősorban gyógyászatiig hatékony mennyiségben - a következőket tartalmazza: a) iegaibb egy vírusellenes és/vagy ytbiÄÄö; batékoRÿipls^artl, ü? a kôvëfkezôk kőzöi yiaszfeátő ki karrageriânok és/vagy fiziológiailag : eifegadhato sóik, galaktsn szulfátok és/vagy fiziológiailag aítogadbalö séik, és liöilyronjólők ésjvragÿ fréfölóglaíisg effögádhafó sóik olyan Pativ mennyiségekben, amely a 0,1-40 töméi % közötti tartományban, különösen a ö.ő és 36 tömeg % közdítí tartományban, előnyösen az 1 és 26 tömeg % közötti tartományban, előnyösebben a: 2 és 2ö 'ii.#Ä''tbfl6möß5liK!ii: ée KOiönöseh előnyösen a 3 és tfefemeg % közötti fsrtömányban van á: kompozícióra alapozva; bj polihexánfo, mint felületi fertőtlenítő olyan relatív mennyiségbér!, amely·-a 0,001 és §: tömeg % Közöl láffömánybafe Különösért:: a §02 és 2,5 tömeg % közötti tartományban, éíőnyöásn a 0,005 és 2 tömeg % közöl· tartományban:,: elönyösébbén a 0.01 és 1 :íömeg % közötti tartományban, és különösen előnyösen a 0,S§ és Q,f tömeg % közötti tartományban van a kompozícióra alapozva; öj hiáiuronsav vagy sőiroiysn relativ mennyiségben, amely aö,01 és tó tömeg % közötti tartományban, Különösen a 0,05 és Bt.tömeg %IkőzÖti :tartöbferiyban, efönyösan a41 és 2 tömeg; % közöl tartományban van a kompozidőre alapozva. 1:4, Az 1-Í$: igényponlok báfs^fe?: $?e#f iöj&amp;pözMt tiMflá?ásrt a gyogyszefeszet, gyógyászát: és éielmíszer-feéilológia teruiéféilj és/vagy alkalmazásra :áz emben gyógyászat és az áilatgyógyásM területén; ésfeagy áikatmazásra a: rekedtségnek (höársehéssi éÂgy a száj ée:foibk|yuíiáöásö§ bstepégeibok megelőző Ős terápiás kezeiésété:, különösen alkalmazásra :s rekedtség :j{8l®hbö2§^fi»P1IÍtP^^§sWN kezelésére.
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