DK152482B - Osmotisk drevet organ til reguleret indgift af et aktivt middel til et vandigt, surt vaeskemiljoe - Google Patents

Osmotisk drevet organ til reguleret indgift af et aktivt middel til et vandigt, surt vaeskemiljoe Download PDF

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DK152482B
DK152482B DK184681A DK184681A DK152482B DK 152482 B DK152482 B DK 152482B DK 184681 A DK184681 A DK 184681A DK 184681 A DK184681 A DK 184681A DK 152482 B DK152482 B DK 152482B
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Pieter Bonsen
Patrick Seck-Lai Wong
Felix Theeuwes
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Alza Corp
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    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

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Den foreliggende opfindelse angår et osmotisk drevet organ til reguleret indgift af et aktivt middel til et vandigt, surt miljø, hvilket organ består af en med en gennemstrømningsåbning forsynet semipermeabel polymervæg, der omgiver og danner 5 et rum og er permeabel for passage af vand og i det væsentlige impermeabel for passage af et i rummet indeholdt aktivt middel .
Osmotisk drevne organer fremstillet i form af tabletter til at 1Q administrere en medicin til mave- og tarmkanalen kendes fra US-patentskrift nr. 3.845.770 og 3.916.899. Et typisk heri beskrevet drevet organ omfatter en semipermeabel væg, der omgiver et rum, der indeholder et aktivt middel. Væggen er permeabel for en ydre væske og i det væsentlige uigennemtrængelig 15 for det aktive middels passage. Der er en gennemstrømningsåbning gennem væggen til at afgive det aktive middel fra systemet. Systemet frigiver det aktive middel ved hjælp af væske, der kontinuert suges gennem væggen ind i rummet ved en hastighed, der bestemmes af væggens permeabilitet og den osmotiske 20 trykgradient gennem væggen til frembringelse af en opløsning indeholdende et opløseligt aktivt middel, der dispenseres fra systemet i løbet af tiden.· I US-patentskri ft nr. 4.036.228 beskrives et osmotisk drevet organ til at administrere aktive midler, der er vanskelige at 2 5 administrere, især aktive midler, der er praktisk taget uopløselige i vandige væsker. Det drevne organ benyttes ved at fylde organet med et par indbefattende en sur komponent og en basisk komponent, hvilke er i stand til at moussere. Ved brug, når organet er i et væskemiljø, suges væske ind i det drevne 30 organ, hvorved parret fugtes og bringes til at reagere og frembringe en mousserende opløsning i det drevne organ. Den mousserende opløsning frembringer en neutral tilstand i det drevne organ og dispenserer det aktive middel fra det drevne organ.
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Dette skrift angår ikke afgivelse af medicinsk aktive midler, der har begrænset opløselighed i surt miljø,og virkningen beror på tilstedeværelse af både den sure og den basiske komponent.
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Mange betændelsesmodvirkende aktive midler er tungt opløselige i vandholdige og sure miljøer, såsom i mavevæsken, og ved afgivelsen fra et osmotisk drevet organ udfældes disse aktive midler ved berøring med mavevæsken og akkumuleres ved mundin-5 gen af gennemstrømningsåbningen og på den ydre overflade af det drevne organs væg. Det udfældede aktive middel forhindrer opløsningen af midlet i at strømme gennem det osmotisk drevne organs gennemstrømningsåbning.
jø Det osmotisk drevne organ ifølge den foreliggende opfindelse er ejendommeligt ved, at et i rummet indeholdt aktivt middel udviser en begrænset opløselighed i vand og det sure vandige miljø, og at rummet yderligere indeholder en vandopløselig ugiftig basisk,carbondioxidfrembringende forbindelse., der udviser en osmotisk trykgradient på tværs af væggen mod den om-15 givende væske, samt at rummet i det væsentlige er fri for sure bestanddele, der er i stand til at frembringe carbondioxid med den basiske forbindelse. Den carbondioxiddannende forbindelse, der ved frigøring fra det drevne organ kommer i kontakt med 2ø syren i maveregionen, reagerer med denne,og danner carbondioxid. Denne fysiske aktivitet og gassen dispenserer det aktive middel i fin dispergeret form fra organet samtidig med, at det drevne organs gennemstrømningsåbning holdes åben.
Eksempelvise udførelsesformer for opfindelsens genstand be-25 skrives nedenfor på grundlag af tegningen. I denne viser fig. 1 i ukorrekt målestok i delvis åbnet tilstand et osmotisk drevet organ fremstillet med en semipermeabel væg benyttet til at administrere et aktive middel, 30 fig. 2 i ukorrekt målestok i delvis åbnet tilstand et osmotisk drevet organ fremstillet med en semipermeabel mikroporøs væg benyttet til at administrere et aktivt middel, fig. 3 frigørelsesmønstret for et vanskeligt opløseligt ak-3 5 tivt middel fra et osmotisk drevet organ frigivet uden gasdannende forbindelse, og fig. 4 frigivelsesmønstret for et vanskeligt opløseligt aktivt middel fra et osmotisk drevet organ frigivet med en gasdan-
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3 nende forbindelse.
Fig. 1 viser en udførel sesform for et osmotisk drevet organ 10 benyttet til at administrere et aktivt middel. Det osmotisk drevne organ 10 ses i åbnet tilstand, og omfatter en væg 11 5 dannet af en semipermeabel polymer, der omgiver og danner et rum 12. Der er en gennemstrømningsåbning 13, der forbinder rummet 12 med det drevne organ 10's ydre omgivelser for at administrere et aktivt middel 14, der er angivet ved prikker, og en basisk forbindelse 15, der er gengivet ved streger, og som har en carbondioxiddannende gruppe, fra det drevne organ 10.
Fig. 2 illustrerer en anden udførelsesform for et osmotisk drevet organ 10 benyttet til at administrere et aktivt middel.
Det osmotiske organ 10, der ses i åbnet tilstand, omfatter en 1 5 væg 11 dannet af en semipermeabel polymer, hvorpå der er lamineret et mikroporøst lag 16, der vender mod rummet 12's indre. I en anden ikke vist udførelsesform kan det mikroporøse laminat 16 være på den semipermeable væg 12's ydre overflade. Som vist i fig. 2 har organet 10 en gennemstrømningsåbning 13 gennem det semipermeable mikroporøse laminat dannet ved 11 og 16 for at forbinde rummet 12 med det drevne organ 10’s ydre omgivelser for at administrere et aktivt middel 14 og en carbondioxid dannende forbindelse 15 fra det drevne organ 10. 1 2 3 4 5 6 7 8 9 10 11
Det osmotisk drevne organ 10's semipermeable væg er dannet af 2 et semipermeabelt materiale, der ikke på uheldig måde påvirker 3 det aktive middel, den carbondioxid dannende forbindelse,el ler 4 patienten. Den semipermeable væg er dannet af et polymert ma 5 teriale, der er permeabelt for passage af vand og er i det 6 væsentlige uigennemtrængelig for passage af aktive midler, 7 opløste produkter og tilsvarende stoffer. De selektivt permea 8 ble polymerer, der er egnede til fremstilling af drevne orga 9 ner , repræsenteres ved et stof valgt fra den gruppe, der består 10 af celluloseacylat, cellulosediacylat, cellulosetriacylat, 11 celluloseacetat, cel 1ulosediacetat, cellulosetriacetat, polyamider, polyurethaner og tilsvarende stoffer. Passende semipermeable polymerer til fremstilling af osmotisk drevne organer er beskrevet i US-patentskrift nr. 3.845.770, 3.916.899,
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4 4.008.719, 4.036.228 og 4.111.210. I den i fig. 2 viste udførelsesform kan den semipermeable væg 12 være et laminat indbefattende et semipermeabelt lag 11 arrangeret til et laminat sammen med et mikroporøst lag 16. Det semipermeable lag 11 er 5 formet ud fra en af de oven for beskrevne polymere. Det mikro-porøse lag 16 har en mængde mikroporer og indbyrdes forbundne mikroveje for at tilføre væske ind i indretningen. Det mikro-porøse lag kan indbefatte de oven for omtalte polymere omfattende en poredanner, der opløses, eller udvaskes fra laget, 10 når det drevne organ er i drift i brugsmiljøet. Poredannerne er ugiftige og de kan ikke reagere med de materialer, der danner væggen. Når de fjernes fra laget, fyldes de deri dannede veje med væske, og disse veje bliver et organ for væskeindstrømning i organet. Typiske poredannere repræsenteres 15 ved natriumchlorid, kaliumchlorid, sorbitol, mannitol, polye- thylenglycol, hydroxypropylmethylcellulose, hydroxypropylbu-tylcellulose, og tilsvarende stoffer. Osmotisk drevne organer med en lamineret væg indbefattende et semipermeabelt lag og et mikroporøst lag er beskrevet i US-patentskrift nr. 4.160.452.
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Udtrykket aktivt middel som brugt her omfatter stort set forbindelser, stofsammensætninger eller blandinger deraf, der kun vanskeligt kan opløses i væsken og som kræver dannelsen af gasturbulens for at forhindre udfældning og tilstopning af gennemstrømningsåbningen og som således kan administreres fra det drevne organ til at frembringe et gunstigt og nyttigt resultat. Betegnelsen aktivt middel omfatter især ethvert stof, der frembringer en lokal eller systemisk virkning i dyr, fugle, fisk og reptiler. Betegnelsen dyr indbefatter primater, gg mennesker, hus-, sports- og landbrugsdyr, såsom geder, kvæg, heste, hunde, katte og tilsvarende dyr. Betegnelsen dyr indbefatter også laboratoriedyr, såsom mus, rotter og marsvin. De aktive midler, der kan administreres ved fremgangsmåden ifølge opfindelsen omfatter uorganiske og organiske aktive midler, 35 såsom aktive midler, der virker på det centrale nervesystem, hypnotika, sedativer, psykisk aktiverende stoffer, beroligelsesmidler, depressionsmodvirkende stoffer, krampemodvirkende stoffer, muskelafslapningsstofer, stoffer til at modvirke par-
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6 kinsonsymptomer, bedøvelsesmidler, betændelsesbekæmpende midler, lokalt bedøvende stoffer, malariabekæmpende stoffer, hormoner, sympathomimetika, dioretika, anti paras i tika, neoplasti-ka, hypoglycenika, øjenmedikamenter, hjertemedikamenter, næ-5 ringsmidler og tilsvarende stoffer.
I en mere foretrukken form omfatter betegnelsen aktive midler, der er praktisk taget uopløselige, eller har en begrænset opløselighed i neutralt og surt miljø. Dvs. at disse aktive midler udfældes i sådanne miljøer. Udtrykket neutralt indbefatter vand og tilsvarende biologiske miljøer, og udtrykket sur indbefatter maven og den der frembragte saltsyre, vagina, og den deri frembragte mælkesyre, og tilsvarende. Betegnelsen sur legemesvæske som benyttet her angiver mavevæske, vaginal væske og tilsvarende sure miljøer i et dyrelegeme.
En speciel gruppe af aktive midler egnet til administration til de oven for angivne miljøer ved fremgangsmåden ifølge opfindelsen er de sure betændelsesmodvirkende aktive midler. De betændelsesmoedvirkende aktive midler kan omfatte arylcarbo- 20 xylsyremedikamenter og enolsyremedikamenter. Eksempler på arylcarboxylsyremidler omfattende alclofenac- eller 4-allyl- oxy-3-chlorphenyleddikesyre, aspirin eller acetylsalicylsyre, fenoprofen eller dl-2-(3-phenoxypheny1)propionsyre, flufena- minsyre eller 2-(3-trif1uormethylani1 i no)benzoesyre, ibuprofen 25 eller 2(4-isobutylphenyl)prop ionsyre, indomethacin eller 5-me-thoxy-2-methyl-l-(4'-chlorbenzoyl)-3-i ndo 1 eddikesyre, keto- profen eller 2-(3-benzoyl phenyl)propionsyre, metiazinsyre eller 10-methyl-2-phenothiazinyleddikesyre, naproxen eller d-2-(6'-methoxy-2'-naphthyl)propionsyre, nifluminsyre eller 30 3-trif1uormethyl-2-phenyl ami non i kot i nsyre, tolmetin eller l-methyl-5-p-toluoylpyrrol-2-eddikesyre, og sulindac- eller cis-5-fluor-2-methyl-l-[p-(methylsulfinyl)-benzyliden]i nden- 3-eddikesyre. Eksempler på enolsyremidler omfatter azapropa- zon eller 3-dimethy1 am ino-7-methy1-1,2-(n-propyImalony1)-1,2-35 dihydro-l,2,4-benzotriazin, phenylbutazon eller 3,5-dioxo-4-n-butyl-l,2-diphenylpyrazolidin, prenazon eller 4-preny1-1,2-diphenyl-3,5-pyrazoli dindion, sudoxicam eller 4-hydroxy-2-
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6 methyl-N-(2-thiazoly1)-2H-1,2-benzothi azi n-3-carboxami d-1,1-dioxid og lignende. Andre betændelsesmodvirkende aktive midler omfatter diclofenac eller 2-[2,6-dich1orpheny1)-am i no]-benzeneddikesyre og peroxicam eller 2H-1,2-benzothiazin-3-5 carboxamid.
Eksempler på andre aktive midler som er praktisk taget uopløselige eller meget tungt opløselige i vand, og som kan indgives ved hjælp af fremgangsmåden ifølge opfindelsen omfatter diphenidon, meclizinhydroch1 or id, proch1orperazinma1eat, ani-sidon, diphenadion, erythritoltetranitrat, dizoxin, reserpin, acetazolamid, methazolamid, bendroflumethiazid, chlorpropamid, tolazamid, allupurinol, aluminiumaspirin, salicylsyre, natriumsal i cyl at , salicylamid, acetami nophen, acetophenetidin, co-læchicin, mefenamicsyre, oxophenbutazon, zomepirac, methotre-xat, acetylsulfisoxazol, hydrocorti son, desoxycorticosterona-cetat, cortisonacetat, triaminolon, 17-estradion, 17-hydroxy-progesteron, 19-norpreogesteron, prednisolon, progesteron, no-rethindronacetat, norethynodrel og lignende.
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Den i et drevet organ tilstedeværende mængde af aktivt middel vil variere afhængig af aktiviteten og den mængde af aktivt middel, der skal indgives værtsdyret. Almindeligvis vil det drevne organ rumme fra 0,5 mg til 3 g eller mere, idet enkelte drevne organer f.eks. indeholder 25 mg, 50 mg, 125 mg, 250 mg, 25 1,5 g og lignende. Det aktive middel kan foreligge i forskellig form i det drevne organ, såsom være dispergeret, granuleret, foreligge i pulverform, som en presset masse, som en hinde og på andre tilsvarende måder. Det aktive middel kan også være blandet med et bindemiddel, et diluenda, et disper-30 geringsmiddel, et stabiliseringsmiddel, farve og tilsvarende stoffer. De gavnlige aktive midler, deres opløselighed og deres doseringsmængde kendes indenfor teknikken fra "Pharmaceutical Sciences", af Remington, 15. udgave 1975, udgivet af
Mack Publishing Co., Easton, Penna.; "The Drug, the Nurse, the 3 5
Patient, Including Current Drug Handbook" 1974-1976 ved Falconer m.fl. udgivet af Saunder Company, Philadelphia, Penna.; fra "Physician Desk Reference", 33. udgave, 1979, udgivet af
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Medical Economics Co., Oradell, N.J.; fra Ann. of Allergy, bind 41, side 75 til 77, 1979; fra "Arzenim. Forsch.", bind 25, side 1629 til 1635, 1975; og fra "J. Inter. Med Res.", bind 7, side 335 til 338, 1979".
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Den gasdannende forbindelse egnet til den foreliggende opfindelses formål er en vandopløselig, ugiftig, basisk, carbondio-xidfrembringende forbindelse og som a) udviser en osmotisk trykgradient på tværs af den semipermeable væg mod den omgi-10 vende væske og suger væske ind i det drevne organ, b) virker som et puffermiddel og opløses i væsken, der trænger ind i det drevne organ under dannelse af en opløsning, der indeholder et aktivt middel, c) hæver udenfor det drevne organ pH-værdien for det område, der umiddelbart omgiver gennemstrømningsåb-15 ningen, nok til at formindske det aktive middels udfældningshastighed, og d) udenfor det drevne organ ved grænsefladen for gennemstrømningsåbningens omgivelser, reagerer med omgivelsernes syre til at frembringe carbondioxidmoussering, som styrer det aktive middel væk fra det drevne organ i en disper-2Q geret form. De basiske forbindelser indbefatter ugiftige me-talcarbonat og bicarbonatsalte, såsom alkalimetalcarbonater og bicarbonater, de alkaliske jordarters carbonater og bicarbo-nater og blandinger af disse. De foretrukne forbindelser er de, der er vandopløselige og som frembringer en hurtig mousse-25 rende virkning ved berøring med miljøets syre. Man kan benytte en blanding af forbindelser med forskellige opløsningsgrader i vand, hvoraf mindst én forbindelse er meget 1 et opløselig i vand. Eksempelvise forbindelser indbefatter lithiumcarbonat, natriumcarbonat, ka1 iumcarbonat, 1ithiumbicarbonat, natriumbi-30 carbonat, kaliumbicarbonat, magniumcarbonat, calciumcarbonat, magniumbicarbonat, calciumcarbonat, magniumbicarbonat og tilsvarende stoffer. Forbindelser, der også danner en nyttig gas, er ammon iumcarbonat, ammoniumbicarbonat, ammon i umsesqui carbonat, natriumsesquicarbonat og tilsvarende stoffer. Disse for-3g bindeiser har opløst i vand en pH-værdi større end 7, almindeligvis mellem 8 og 12. Valgfrit er det hyppigt ønskeligt at vælge det aktive middel og forbindelsen uden en fælles ioneffekt, således at deres pågældende opløseligheder i en væske,
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8 der strømmer ind i det drevne organ, er maksimale. Mængden af basisk forbindelse eller blanding af sådanne i hulrummet, andrager almindeligvis ca. 0,5 mg til 3 g eller mere, og er fortrinsvis 25 mg til 750 mg. Forbindelserne og deres opløselig-5 hed i vand fremgår af "The Handbook of Chemistry and Physics", 48. udgave, 1968 udgivet af the Chemical Rubber Co., Cleveland, Ohio.
Det aktive middel og den basiske forbindelse kan også benyttes blandet med et bindemiddel og et smøremiddel. Det aktive middel og forbindelsen blandes i et vandopløseligt bindemiddel, og eller i et vanduopløseligt bindemiddel, der frigør det aktive middel og forbindelsen ved berøring med vand.
Typiske vandopløselige bindemidler omfatter poly(ethylengly-15 col), gelatine, agar, carboxycellulose, ethylmethylcellulose, poly(vinylalkohol), poly(vinylpyrrolidon) , vandopløselig stivelsesderivater og tilsvarende stoffer. Typiske smøremidler indbefatter stearinsyre, magniumstearat, zinkstearat og tilsvarende stoffer. Den benyttede mængde af bindemiddel eller 20 smøremiddel er almindeligvis ca. 0,1 mg til 150 mg, eller mere.
De osmotisk drevne organer ifølge opfindelsen fremstilles ved standardfremstillingsmetoder. I én udførelsesform blandes det 25 aktive middel f.eks. med den basiske forbindelse og andre ingredienser ved hjælp af en kuglemølle, ved kalandrer ing, omrøring og presning til en kerne med forudvalgt form. Det drevne organs vægdannende materiale kan påføres ved at dyppe, forme eller sprøjte den pressede blanding. En fremgangsmåde 30 til påføring af væggen er luftlægnings- eller luftsuspensionsteknikken, ved hvilken en strøm af atmosfærisk luft og en opløsning af belægningsmidlet ledes forbi det drevne organs i forvejen pressede kerne, der tumler rundt i luftsuspensionen for på alle sider at belægge kernen med en væg. Luftsuspen-35 sionsteknikken kan benyttes til at fremstille en væg dannet af et enkelt lag eller dannet af et andet lag. Luftsuspensionsteknikken er beskrevet i J. Am. Pharm. Assoc.", bind 48, side 451 til 459, 1959 og i bind 49, side 82 til 84, 1960. En osmo-
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9 tisk gennemstrømningsåbning eller et hul gennem væggen fremstilles ved mekanisk boring, laserboring, stansning eller skæring ved et lokkestempel. Fremgangsmåder til formning af gennemstrømningsåbningen under brug af en laser fremgår af US-5 patentskrift nr. 3.916.899 og 4.088.864. Andre standardfremsti 11ingsfremgangsmåder er beskrevet i "Modern Plastic Encyclopedia", bind 46, side 62 til 70, 1969, i "Remingtons
Pharmaceutical Sciences", 14. udgave, side 1649 til 1698, 1970, udgivet af Mack Publishing Co., Easton, Penna., og i 10 "The Therapy and Practise of Industrial Pharmacy", ved Lachman f.fl., side 197 til 225, i 1970, udgivet af Lea & Febiger Co., Philadelphia, Penna.
De efterfølgende eksempler illustrerer den foreligende opfin- , _ delse.
1 o
Eksempel 1
Et oralt osmotisk drevet organ til at indgive et ikke-steoridt betændelsesmodvirkende aktivt middel natri umindomethacin blev 20 fremstillet som følger. En sammensætning af det aktive middel blev tilberedt til at rummes i det aktive organs hulrum ved grundigt at blande 105,2 mg natriumindomethacintrihydrat, 142 mg kaliumbicarbonat, 5,0 mg polyvinylpyrrolidon, og 7,1 mg stearinsyre og derpå presse den homogene blanding, der inde-25 holder aktivt middel og en carbondioxid producerende gruppe og andre ingredienser til en kerne eller pille til udfyldning af organets indre rum. Herefter blev den komprimerede formulering af det aktive middel anbragt i en 1 uftlægn ings- eller -suspensionsmaskine, dvs. en maskine der blander atmosfærisk luft og 30 en opløsning, der danner en væg, og hvor kernen med bl.a. det aktive middel svæver i luften og belægges med opløsningen, så der dannes et mikroporøst lag bestående af 45 vægt% celluloseacetat med et acetyl indhold på 39,8%, 27,5 vægt% hydroxypro-pylmethylcel1ulose og 27,5 vægt% polyethylenglycol 4000. Laget 35 blev påført fra en opløsning i et methylenchlor id - 95% etha-nolopløsningsmidel (80:20 vægt:vægt). Det mikroporøse lag var ca. 0,13 ml tykt.
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10
Derpå påførtes et ydre semipermeabelt lag på det mikroporøse lag i luftlægnings- eller -suspensionsmaskinen. Den sammensætning, der dannede det semipermeable lag, indbefattede 50 vægt% cel!uloseacetat med et acetyl indhold på 39,8% og 50 5 vægt% celluloseacetat med et acetyl indhold på 32%. Det semipermeable lag blev påført ud fra en opløsningsblanding indeholdende methylenchlorid og 95% ethanol, 80:20 vægt-.vægt. Systemerne blev tørret og en gennemstrømningsåbning på 0,254 mm blev laserboret gennem den laminerede væg. Systemet frigør in-10 domethacin med en hastighed på 8 mg pr. time. Ved drift frigiver det drevne organ en opløsning, der mousserer eller bruser ved berøring med den sure mavevæske ved gennemstrømningsåbningens udløbsende under frembringelse af carbondioxidbobler, der dispergerer det aktive middel i en fnugagtig ti 1 -15 stand.
Eksempel 2
Et oralt osmotisk organ for den regulerede kontinuerte indgift af indomethacin blev fremstillet ved at følge den generelt 20 ovenfor beskrevne fremgangsmåde. I det foreliggende drevne organ indeholdt rummet en formulering af det aktive middel 56,4% kaliumcarbonat, 37,6% natri umindomethacintri hydrat, 3% providon® og 3% stearinsyre. Den kerne, der skal udfylde organets rum, havde efter komprimering en diameter på 7,93 mm, et 25 overfladeareal på 1,6 cm2 og en massefylde på 1,65 g/ml. Det drevne organ havde en lamineret væg med et indre mikroporøst lag bestående i det væsentlige af 45 vægt% cel!uloseacetat med et acetyl indhold på 39,8%, 45 vægt% sorbitol, og 10 vægt% po- lyethylenglycol 400. Laget blev påført ud fra en opløsning in-30 deholdende methylenchlorid i methanol/vand, 62:35:3 pr. vægt.
Et semipermeabelt lag blev lamineret på det mikroporøse lag, hvilket semipermeable lag bestod af 50 vægt% celluloseacetat med et acetyl indhold på 39,8% og 50 vægt% af celluloseacetat med et acetyl indhold på 32%. Laget var påført ud fra en opløs-35 ning bestående af methylenchlorid og methanol 80:20 pr. vægt.
Det mikroporøse lag var 0,127 mm tykt og det semipermeable lag var 0,061 mm tykt. Det drevne organ havde en gennemstrømnings-
DK 152482 B
11 åbning på 0,23 mm og indgav indomethacin med en hastighed på 8 mg/time. Det drevne organ indgiver det aktive middel i det væsentlige fri for hurtig udfældning ved grænsefladen for gennemstrømningsåbningens omgivelser, og på det drevne organs væg 8 i nærheden af gennemstrømningsåbningen.
Eksempel 3
Fremgangsmåden ifølge eksempel 2 blev gentaget under de beskrevne betingelser med undtagelse af, at det mikroporøse lag 10 var 0,0225 mm tykt, det semipermeable lag 0,069 mm tykt og afgivelseshastigheden var 8 mg/time.
Eksempel 4 15 Det osmotisk drevne organ fra eksemplerne 1 og 2 blev fremstillet i dette eksempel, hvori (a) det mikroporøse lag var 0,127 mm tykt., det semipermeable lag var 0,086 mm tykt, og organet havde en afgivelseshastighed på 6 mg/time, og (b) et organ, hvori det mikroporøse lag var 0,127 mm tykt, det semi-2o permeable lag var 0,043 mm tykt og systemet havde en afgivelseshastighed på 12 mg/time.
Eksempel 5
En serie af orale osmotiske drevne organer til at afgive et 25 arylcarboxylsyre, betændelsesmodvirkende aktivt middel i mavetarmkanalen fremstilles ifølge opfindelsen, hvori det drevne organ rummer fra 40-250 mg natriumindomethacin og fortrinvis fra 85 til 125 mg af natri umindomethacintri hydrat ævivalent med 70 til 100 mg indomethacin, fra 50 til 300 mg af kaliumbi-30 carbonat og fortrinvis fra 130 til 190 mg natriumcarbonat, 2 til 20 mg, fortrinsvis 5 til 10 mg bindemiddel og 2 til 20 mg, fortrinsvis 5 til 10 mg smøremiddel. Det drevne organ har et indre mikroporøst lag med en vægt fra 18 til 25 mg med en tykkelse på 0,10 til 0,16 mm, og et ydre semipermeabelt lag, der 35 vejer 6 til 20 mg med en tykkelse på 0,035 til 0,100 mm. Det drevne organ har en gennemstrømningsåbning på 0,18 mm til 0,38 mm, og frigiver medikamentet ved en hastighed på 5 til 15 mg/t i me.

Claims (6)

1. Osmotisk drevet organ til reguleret indgift af et aktivt middel til et vandigt surt miljø, hvilket organ består af en p Π med en gennemstrømningsåbning forsynet semipermeabel polymervæg, der omgiver og danner et rum og er permeabel for passage af vand og i det væsentlige impermeabel for passage af et i rummet indeholdt aktivt middel, kendetegnet ved, at det aktive middel udviser en begrænset opløselighed i vand og 25 det sure vandige miljø, og at rummet yderligere indeholder en vandopløselig ugiftig basisk carbondioxidfrembringende forbindelse, der udviser en osmotisk trykgradient på tværs af væggen mod den omgivende væske, samt at rummet i det væsentlige er fri for sure bestanddele, der er i stand til at frembringe 3 0 carbondioxid med den basiske forbindelse.
2. Osmotisk drevet organ til reguleret indgift af et aktivt middel ifølge krav 1, kendetegnet ved, at den basiske forbindelse med en carbondioxiddannende gruppe er et 35 farmaceutisk accepterbart carbonat eller bicarbonat af et alkalimetal eller et jordalkalimetal.
3. Osmotisk drevet organ til reguleret indgift af et aktivt middel ifølge krav 1, kendetegnet ved, at den semi- DK 152482 B permeable polymervæg er belagt med et mikroporøst lag.
4. Osmotisk drevet organ til reguleret indgift af et aktivt middel ifølge krav 1, kendetegnet ved, at den car- _ bonxiddannende forbindelse i rummet er 1 i thiumcarbonat, natri-umcarbonat, ammon iumcarbonat, kaliumcarbonat, 1 ithiumbicarbo- nat, natriumbicarbonat, ammoniumbicarbonat, eller kaliumbicar-bonat.
5. Osmotisk drevet organ til indgift af et aktivt middel 10 ifølge krav 1, kendetegnet ved, at det polymere materiale, der danner den semipermeable væg, er celluloseacylat, cel 1u1 osed iacy1 at eller ce11u1osetriacy1 at.
6. Osmotisk drevet organ til reguleret indgift af et aktivt 15 middel ifølge krav 1, kendetegnet ved, at der på den semipermeable væg er påført et mikroporøst lag dannet af en cellulosepolymer indeholdende en poredanner. 20 25 30 35
DK184681A 1980-04-25 1981-04-24 Osmotisk drevet organ til reguleret indgift af et aktivt middel til et vandigt, surt vaeskemiljoe DK152482C (da)

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EP0040899A3 (en) 1982-08-11
DK184681A (da) 1981-10-26
ATE9267T1 (de) 1984-09-15
ES8307092A1 (es) 1983-06-16
ES267593U (es) 1983-05-16
PT72796B (fr) 1982-03-30
DK152482C (da) 1988-08-01
EP0040899A2 (en) 1981-12-02
US4265874A (en) 1981-05-05
IE51216B1 (en) 1986-11-12
EP0040899B1 (en) 1984-09-12
JPH044293B2 (da) 1992-01-27
ES510822A0 (es) 1983-06-16
JPS56167617A (en) 1981-12-23
GR73519B (da) 1984-03-09
NZ196561A (en) 1983-05-10
ES267593Y (es) 1983-11-16
DE3165901D1 (en) 1984-10-18
PT72796A (fr) 1981-05-01

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