ITMI941410A1 - Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida - Google Patents

Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida Download PDF

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ITMI941410A1
ITMI941410A1 IT001410A ITMI941410A ITMI941410A1 IT MI941410 A1 ITMI941410 A1 IT MI941410A1 IT 001410 A IT001410 A IT 001410A IT MI941410 A ITMI941410 A IT MI941410A IT MI941410 A1 ITMI941410 A1 IT MI941410A1
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composition according
moguisteine
administration
composition
mixture
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Ettore Bilato
Gabriele Lazzarini
Giancarlo Santus
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Recordati Chem Pharm
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Priority to US08/452,435 priority patent/US5674533A/en
Priority to EP95918125A priority patent/EP0769948A1/en
Priority to BR9510302A priority patent/BR9510302A/pt
Priority to CA002194374A priority patent/CA2194374A1/en
Priority to AU24176/95A priority patent/AU2417695A/en
Priority to PCT/IB1995/000412 priority patent/WO1996001628A1/en
Priority to CZ199750A priority patent/CZ287967B6/cs
Priority to KR1019970700062A priority patent/KR970704437A/ko
Priority to MX9700223A priority patent/MX9700223A/es
Priority to JP8504206A priority patent/JPH10502629A/ja
Priority to HU9700017A priority patent/HUT76832A/hu
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents

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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Description

DESCRIZIONE dell’Invenzione avente per titolo:
"COMPOSIZIONE FARMACEUTICA A RILASCIO CONTROLLATO DI MOGUISTEINA IN SOSPENSIONE LIQUIDA"
L’Invenzione riguarda composizioni farmaceutiche a rilascio controllato in forme di dosaggio liquide per la somministrazione di mogulsteina.
La moguisteina, (R,S)-2-[(2-metossifenossi)metil-3-etossicarbonil-1-acetil]-1,3-tiazolidina, e’ un potente agente antltosse perifericodescritto nel bevetto europeo EP 169,581.
Farmacologicamente la tosse può’ essere soppressa agendo sulla componente neuronica del riflesso o agendo sulla quantità’ o viscosità’ del fluidi del tratto respiratorio. Di conseguenza gli antltosse sono stati distinti in due classi terapeutiche: quelli che agiscono deprimendo i centri della tosse e gli espettoranti. Gli oppiacei ed i loro derivati agiscono attraverso la depressione centrale dei centri della tosse e la codeina, in particolare, e’ stato l'antltosse piu’ ampiamente usato. Peraltro, dato che il loro uso provoca fenomeni di assuefazione, e’ particolarmente sentita la necessita’ di farmaci antltosse non narcotici.
Come antitosse lamoguisteina e* equipotente rispetto a codeina, destrometorfano, zlplprolo e 3-4 volte piu’ potente della
(D,L)-dropropizina, inoltre non da’ assuefazione in quanto non e’ un derivato oppiaceo. Rispetto a codeina e destrometorfano la moguisteina e’ meglio tollerata ad alte dosi in quanto Induce una sedazione ed una riduzione del tono muscolare minore. La moguisteina e’ un racemo composto da una miscela 1:1 dell’enantiomero R(+) ed S(-) e, come antltosse, non e’ stata riscontrata differenza di attività’ biologica fra i due enantlomerl.
Studi sul meccanismod’azione della moguisteina hanno dimostrato che la moguisteina non agisce attraverso i recettori oppiacei, ma che il suo sito d’azione e’ a livello periferico interagendo con i
cosldettl "RapidTy adapting 1rr1tant receptor" (RARs).
Lamoguisteina ha le caratteristiche di un profarmaco in quanto, dopo soiraninistrazione orale o 1.v., nel fluidi biologici non e’ stata rilevata come tale in quantità’ misurabile, mentre e’ statotrovato e misurato 11 corrispondente acido (R,S)-2-[(2-metossifenossi)metil]--3-carbossiacetil]-1,3-tiazolidina, suo metabolita attivo. E’ stato anche determinato che tale metabolita attivoe’ assorbito 5 voltemeno della moguisteina stessa.
Le formulazioni di moguisteina fino ad ora note includono compresse e bustine per un dosaggio di 200 mg ed una sospensione tradizionale al 2%. La dose giornaliera e’ compresa nell’Intervallo di 100-800 mg, tra questi, 1 dosaggi piu’ bassi trovano principalmente impiego in pediatria.
Uno degli svantaggi che la moguisteina presenta e’ costituito dalla sua emivlta che nell’uomo e’ Inferiore all’ora. Questo impone l’uso di somministrazioni frequenti, almeno tre/quattro volte al giorno al fine di mantenere costanti i livelli ematici terapeutici [ Castoldi , D. et al. , Pharmacol. Res. 22 (Suppl. 2), 102 (1990)] .
E' pero’ noto che un numero eccessivo di somministrazioni giornaliere influenza negativamente la compì lance del pazienti e che perdo’ sono di gran lunga preferibili formulazioni dove la somministrazione può’ essere fatta due volte al giorno o ancor meglio in dose unica giornaliera. Ad esempio e’ riportato che 11 tasso di compì lance del pazienti nell’uso del farmaci varia dall’87% per 1 farmaci da assumere una volta al giorno, fino al 39X per i farmaci da assumere 4 volte al giorno [J.A. Cramer et al. JAMA 1, 601 (1989)] .
E’ noto che 11 numero di dosi può’ essere ridotto mediante l’uso di forme farmaceutiche a lento rilascio quali compresse, pellets, o simili. Tuttavia, nel caso particolare della somministrazione di farmaci antltosse, occorre tenere conto che le forme di dosaggio elettive sono quelle a somministrazione liquida.
Il brevetto statunitense US 5,296,236 descrive composizioni farmaceutiche a rilascio controllato per formulazioni liquide, consistenti in microgranuli rivestiti da piu’ strati polimerici. In tali composizioni parte del principio attivo viene reso disponibile nel tempo per diffusione dal microgranull, mentre una parte e’ presente tra i componenti extragranulari ed e’ immediatamente disponibile all’uso.
Le composizioni descritte dal brevetto US 5,296,236 non danno pero’ una soluzione al problema di somministrazione liquida della moguisteina.
Un primo inconveniente e’ Infatti costituito dal fatto che la moguisteina ha sapore altamente sgradevole e do’, oltre a rendere inaccettabile il ricorso a formulazioni in sospensione o a soluzioni di tipo tradizionale, non permette la presenzadi parti di principio attivo immediatamente disponibili all’ingestione orale. Polche’ la palatabmta’ rappresenta un punto Importante per garantire una buona compìiancedel paziente, nel caso particolare si presenta l’esigenza di disporre di una formulazione liquida a rilascio controllato che unisca ai vantaggi di essere facilmente dosabile, deglutibile e di avere una cessione graduale che compensi l’emivita breve del principio attivo, anche il fatto di disporre di una buona palatabilita’ e di una buona stabilita’ dopo ricostituzione.
Un altro problema e’ costituitodal punto di fusione
relativamente bassodella molecola che e’ di circa 65°C [Drugs of thè future 16, 618 (1991)}.
Tra 1 materiali impiegati per rivestire 1 microgranull e controllare 11 rilascio del principio attivo e’ Infatti previsto anche materiale ceroso come cera d’api bianca, alcol cetilico, alcol stearilico, gliceril monostearato, e simili, che trovano come unici solubi11zzanti l’Impiego di solventi clorurati. Purtroppo l’uso di solventi clorurati ha grosse limitazioni che sono legate, sia a problemi di ordine tossicologico (solventi residui), sia ambientale (smaltimento del solventi dopo l’utilizzazione).
Una soluzione nota per ovviare all’impiego del solventi clorurati, consiste nell'applicare le cere allo stato fuso [Pharm. Ras.
7, 1119 (1990)]. Per poter utilizzare questometodo e’ pero’ necessario impiegare aria compressa riscaldata che mantenga la temperatura delle cere ad una temperatura superiore al punto di fusione. A temperature Inferiori Infatti, le cere tendono a solidificare ed ovviamente non sono piu’ utilizzabili comemateriale fumogeno e , d’altra parte, l’uso di temperature relativamente alte costituisce un problema per principi attivi basso-fondenti.
Grazie alla presente invenzione, e’ stato tuttavia possibile, operando con opportuni accorgimenti, applicare le cere fuse anche su un microgranulato comprendente un principio attivo con punto di fusione di 65‘C. Approfittando delle particolari caratteristiche della composizione microgranulare, e’ infatti possibile utilizzare un ugello coassiale in cui il fluido di nebulizzazione e’ costituito da aria compressa riscaldata sufficiente amantenere le cere costantemente allo stato liquido. Mediante questa tecnica le cere arrivano al substrato ad una temperatura superiore al loro punto di fusione, senza tuttavia possedere una quantità’ di calore sufficiente a decomporre 11 principio attivo contenuto nel granulato.
Al fine di avere una formulazione facilmente sospendibile, e’ necessario che le dimensioni del microgranuli dopo il rivestimento siano almeno inferiori al 500 pm. Granuli con dimensioni superiori al 500 pm non sono facilmente sospendibili in quanto tendono a sedimentare rapidamente dando luogo ad una distribuzione del principio attivo non omogenea al momento della somministrazione.
Dovendo ricorrere a particelle microgranuìari aventi dimensioni inferiori a 500 μm, l'area superficiale aumenta enormemente ed e' di conseguenza più' difficoltoso, rispetto a compresse o pellets, controllare il rilascio del principio e mantenerlo inalterato nel tempo dopo ricostituzione della soluzione. La difficolta’ e' ancora maggiore se nell’ambiente che circonda il granulo non e’ già’ presente una quantità’ di farmaco in soluzione che, diminuendo il gradiente di diffusione, tende ad inibire la diffusione del farmaco dal granulo verso l’esterno.
E’ quindi oggetto della presente invenzione una composizione farmaceutica a rilascio controllato, in sospensione liquida, in grado di garantire livelli ematici terapeuticamente attivi di moguisteina o del suol derivati biologici mediante una o, preferibilmente, due somministrazioni giornaliere. Le composizione e’ in particolare caratterizzata dalla eccellente palatabilita’ e da una buona stabilita’ nel tempo dopo ricostituzione con acqua.
Tale composizione consiste in una molteplicità’ di microgranuli di forma sostanzialmente sferica costituiti da una miscela di
moguisteina ed opportuni eccipienti ricoperti da una serie di tre strati sovrapposti di materiale fumogeno rispettivamente costituiti da cellulosa acetoftalato, cere ed infine cellulosa acetoftalato.
In tal modo, la formulazione e’ in grado di mantenere intatte le caratteristiche di cessione delle forme farmaceutiche in essa veicolate e può’ essere concepita, sia come formulazione a dosaggio liquido già’ prontae stabile nel tempo, sia come formulazione liquida che, preparata al momento dell’uso, rimane poi stabile per tutto il periodo in cui la terapia viene effettuata.
Per le sue caratteristiche peculiari la composizione si presta a diverse forme di presentazione quali ad esemplo una formulazione granulare plurldose in cui la flessibilita’ del dosaggio viene ottenuta dosando quantità diverse di granulare da rlsospendere al momento dell’uso, oppure formulazioni monodose accuratamente dosabili sotto forma di bustine, flacondnl con sottotappo per la ricostituzione al momento ed altre forme note nell’arte.
Per uso pediatrico la formulazione permette anche presentazioni sotto forma di gocce concentrate in cui viene sospeso 11 granulare contenente moguisteina.
I vantaggi della presente invenzione sono evidenti, in quanto per mezzo di essa si ottiene un sensibile miglioramento della compìlance dei pazienti sia in termini di riduzione del numero di dosi giornaliere sia in termini di buona palatabillta’. Sono Inoltre prevedibili ulteriori vantaggi dovuti alla facilita’ di somministrazione e di deglutizione specie nell’area pediatrica. E’ inoltre certa una migliore risposta terapeutica in quanto la formulazione permette di modulare il dosaggio in funzione della necessita’, semplicemente attraverso la misura del volumi di sospensione necessari.
Nel dettaglio l’Invenzione consiste quindi in una composizione farmaceutica a rilascio controllato dosabile in forma liquida
comprendente:
1) mlcrogranull per il rilascio controllato di moguistaina aventi dimensioni comprese fra 50 e 500 μm (preferibilmente tra 1 90 e 300 pm), atti a rimanere facilmente in sospensione in un liquido per tempi prolungati, costituiti da: a) unamiscela di moguisteina ed opportuni eccipienti trattata in modo da formare un nucleo mlcrogranulare di forma sostanzialmente sferica avente caratteristiche tecnologiche e morfologiche definite ed essenziali ad assicurare la riproducibilità’ e l’uniforme distribuzione del successivi rivestimenti fllmogeni; b) un rivestimento per isolare il mlcrogranulare avente caratteristiche essenzialmente idrofile; c) un secondo rivestimento sovrapposto al primo avente caratteristiche lpoflle; d) un ultimo rivestimento esterno avente caratteristiche idrofile.
2) Un sistema di veicolazione per le suddette forme a rilascio controllato costituito da sospendenti, edulcoranti ed aromatizzanti, sostanze tamponanti, preservanti, e simili.
Tali sostanze, in funzione del tipo di presentazione, possono essere presenti allo stato secco o gia’ in soluzione.
Secondo la presente invenzione e’ statoquindi trovato che, impastando ad umidomogulsteinamicronizzata ed eccipienti, preferibilmente: lattosio come substrato, polivinilpirrolidone come legante ed acqua come solvente, in presenza di polietilenglicole (PEG), e’ possibile ottenere granuli ad elevato contenuto in principio attivo aventi dimensioni inferiori a 500 pm, preferibilmente nel range 90-300 pm, una superficie uniforme, una forma quasi sferica, una densità' apparente di circa 500-600 g/l e friabilità’ molto bassa.
In particolare si e' trovato che il polietilenglicole (PEG 6000) inserito nel microgranulato in quantità’ da 0.5 a 1X ha una influenza molto positiva sulla forma sferica e sulla regolarità’ della superficie del microgranuli da filmare. Il PEG 6000 era stato Introdotto nella composizionedel nucleomlcrogranulare per la sua nota proprietà’ di essere idrosolubile ad alte concentrazioni (>10%) allo scopo del favorire la bagnatura della moguisteina che e’ invece insolubile nel liquidi acquosi. S1 e’ poi sorprendentemente trovato che, gia’ in quantità’ inferiori all’1%, il PEG aveva un effetto positivo sulla forma sferica del microgranuli.
Vengono ora precisati gli elementi che caratterizzano i
componenti della formulazione farmaceutica oggetto dell’Invenzione: Nucleomlcrogranulare
Gli eccipienti usati per la realizzazione del nucleo possono essere scelti fra quelli comunemente Impiegati in un impasto ad umido come lattosio, caldo fosfato bibasico, cellulosamlcrocristallina, amido, talco, zuccheri, polivinilpirrolidone, gelatina, copolimero tra polivinllpirrolidone e vlnllacetato e simili.
Si e’ trovata utile l’aggiunta di sostanze quali il
poiiatilengllcole ed in particolare il PEG 6000. Il liquido di Impasto con cui fare la granulazione ad umido, per esemplo in impastatori granulatori ad alta velocita’, può’ essere acqua o un solvente miscibile con acqua come ad esemplo alcol etilico, o altri alcoli usati nell‘industria farmaceuticao loromiscele con acqua.
Le condizioni operative di impasto e granulazione sono il passaggio critico per l’ottenimento di un mlcrogranulato con caratteristiche ottimali per un efficace rivestimento. La tecnica di flimatura preferita e’ quella a letto fluido secondo la tecnologia Wurster.
Sempre secondo l'invenzione, il granulato, dopo essiccamento e vagliatura, viene ricoperto con flimatura a diversa composizione usando tecniche di flimatura note.
Film di rivestimento Sostanze idonee alla prima flimatura sono sostanze idrofile quali derivati delle cellulose, del polimeri acrilici ed in particolare sostanze quali la cellulosa acetoftelatoe l’idrossipropilmetilceiluiosa ftalato in presenza di plastificanti quali dietilftalato dlbutllsebacato, oli vegetali, e simili.
Sostanze idonee al secondo rivestimento, che ha carattere lipofilo, sono sostanze grasse comemono- di- e trigliceridi di acidi grassi aventi catena da 6 a 36 atomi di carbonio, cera carnauba, cera d’api, cera candellla, alcoli e acidi grassi. Questi possono essere applicati o con ausilio di solventi clorurati o, preferibilmente, allo stato fuso senza impiegodi solventi.
Le stesse sostanze costituenti il primo rivestimento possono essere utilizzate anche per l’ultimo strato.
valsala
Il mlcrogranulato, rivestito secondo lemodalità’ sopra descritte, può’ essere quindi assodato al veicolo con miscela solida sospenditele in modo estemporaneo al momento dell’impiego come sospensione pronta.
Elementi costitutivi del veicolo sono:
sospendenti e strutturanti come esteri della cellulosa, cellulosa microcristallina, derivati dell’acido alginico, derivati del polivinilpirrolidone;
zuccheri come saccarosio, sorbitolo, xilitolo, destrosio, e slmili;
sostanze tamponanti come acido citrico e sodio citrato, glicina e addo cloridrico, fosfati di sodio e potassio;
conservanti e batteriostatici come esteri dell’acido
p-idrossibenzoico;
aromi vari e dolcificanti comunemente usati nella tecnica farmaceutica.
La forma farmaceutica da veicolare pronta all’uso comprende oltre al sopraddetti elementi anche acqua o miscele di acqua e cosoìventl come glicoli, alcoli e glicerina.
Il microgranulato, filmato e cosi’ veicolato, presenta non solo le caratteristiche di cessione controllata desiderate per ridurre il numero di somministrazioni e mantenere livelli ematici piu’ costanti, ma anche una ottima palatablilta’, in quanto il principio attivo rimane inglobato all’internodel mlcrogranulato rivestito fino al momento dell’assunzione e in tal modo supera facilmente l’apparato gustativo.
Vengono qui di seguito forniti metodi, tabelle ed esempi che hanno il solo fine di meglio illustrare l’invenzione in oggetto dimostrandone 1 vantaggi e l’applicabilita’, senza tuttavia costituire una limitazione della stessa.
ESEMPIO 1
Preparazione dal mlcrogranulato basedi moguIsteina
Una miscela costituita da moguisteina 79%, polivinilpirrolidone (PVP K30) 10% e lattosio 450 mesh 10%, viene mescolato in impastatore granulatore Diosna P25 per 10’. Mantenendo la miscela sotto mescolazione, s1 aggiunge soluzione acquosa di PEG al 5% p/p alla velocita’ di 25 ml/min. utilizzando un ugello da 0.8 mm alla pressione di 2 bar. Durante la fase di bagnatura la velocita’ del mescolatore e’ di 175 r.p.m. e la velocita’ del frantumatore e’ di 3000 r.p.m.. Il tempo necessario per l’aggiunta della soluzione e’ di 20’. Dopo la bagnatura la fase di Impasto e sferonlzzazlone e’ effettuatamantenendo costanti le velocita’ di mescolatore e frantumatore per 15’. Il microgranulato, cosi’ ottenuto, viene sottoposto ad essiccamento in forno statico a ventilazione forzata e successivamente setacciato attraverso vaglioda 225 maglie/cm<2 >fino ad ottenere un mlcrogranulato avente distribuzione granulometrlca compresa fra 90 e 300 μm di forma sferoidale con densità’ impaccata di 0.593 g/ml e densità’ reale di 1.36 g/ml.
ESEMPIO 2
Una miscela costituita da: moguisteina 79.4%, lattosio 10%, PVP K3010%e PEG 60000.6%, viene mescolata ed Impastata secondo l’esemplo precedente.
ESEMPIO 3
Una miscela costituita da: moguisteina 79.4%, lattosio 450 mesh 10%, PVP K3010%e PEG 60000.6%, viene bagnata con 500 ml di acqua con velocita’ di aggiunta di 25 ml/min per 15’. La velocita’ del mescolatore e’ di 175 g1r1/min e quella del frantumatore di 3000 giri/min. Il microgranulato ottenutodopo essiccamento ha umidita’ residua di 4%, densità’ aerata di 0.548 g/ml, densità’ impaccata di 0.669 g/ml, indice di Carr 18.08% e densità’ reale di 1.38 g/ml. Per le definizioni riferite ai parametri sopradtatal si veda: "Pharmaceutical preformulation”; pagg. 209-214, 1988; ElUs Horwood Ed. - Chlchester, England; e" Avances in Pharmaceutical Sciences"; Voi.2, pagg. 181-220, 1967; Acad. Press Ed. - New York. Il mlcrogranulato ottenuto e’ caratterizzato da una particolare"levigatezza" della superficie delle singole particelle legata alla presenza di PEG 6000.
ESEMPIO 4
Primo strato di ricopertura fumogena (Cellulosa acetoftalato)
2 Kg del microgranulato preparato secondo l’esempio 3 vengono lasciati agitare per 1’ in una apparecchiatura a letto fluido Glatt GPCG3, nella quale viene insufflata alla portata di 40 nr/ora aria riscaldata alla temperatura di 40-45’C. Sul granulato vengono spruzzati, alla pressione di 2 bar con portata 10-13 g/min., 400 mi di soluzione avente la seguente composizione percentuale:
ESEMPIO 5
Secondostratodi ricopertura fumogena (Cere) Al primo strato ricoperto secondo quanto riportato nell’esempio 4 nelle stesse operazioni operative, s1 applicano 1152 g di una soluzione avente la seguente composizione percentuale:
ESEMPIO 6
Al primo strato ricoperto secondo quanto riportato nell’esempio 4 si applica allo stato fuso una miscela di cere aventi la seguente composizione:
Le cere vengono fuse ad una temperatura di circa 110°C e vengono spruzzate allo stato fuso ad una temperatura di circa 80 °C su 2 kg di microgranulato con l’utilizzo di aria compressa preriscaldata ad una temperatura di 125*C e alla pressione di 3 bar utilizzando un ugello chemiscela la cera fusa all’aria calda compressa. La fase di spruzzo viene effettuata con un inserto Wurster da 7" in apparecchiatura Glatt. Vengono spruzzate quantità’ pari a 3.8* in peso di cere ad una velocita’ di circa 1,5 g/min.
Terzo stratodi ricopertura fumogena
Per la ricopertura finale sono utilizzati gli stessi componenti e le metodiche descritti nell’Esempio 4 per 11 deposito del 1° strato.
ESEMPIO 8
A) Sospensione in flaconi multldose
Il microgranulato ritardo (12.5*) preparato secondo esempi 3, 4, 5 e 7 viene aggiunto ad una miscela di cellulosa microcristallna 6.2%, sodio carbossimetllcellulosa 0.8%, sodio citrato 0.5%, acido citrico 0.8%, metile p-idrossibenzoato 0.2%, proplle p-idrossibenzoato 0.05%, gomma adragante 2%, Span 200,05%, dimetilpolisilessano 0.2%, glycamll 0.01%, aroma arando pompeimo 0.25% e zucchero a velo quanto basta a 100%. Aggiungendo a 33 g di miscela per sospensione, 80 g di acqua, s1 ottengono 100 mi di sospensione contenente 30 mg/ml di moguisteina. B) Sospensione in bustinemonodose
3,3 g dellamiscela per sospensione preparata come descritto nel punto A vengono ripartite in bustine di carta/allumlnlo/poiitene. Ogni bustina contiene 300 mg di moguisteina e va risospesa in mezzo bicchiere di acqua.
C) Sospensione In flaconi monodose
1,25 g di mlcrogranulato ritardo preparato secondo gli esempi 3, 4, 5 e 7 vengono messi nel sottotappodi un flacondnomonodose (Bormioli) e sono tenuti separati dal liquido contenuto nel fisconcino monodose. La composizione del liquido monodose e’ sorbitolo 70X 3500 mg, aroma ananas limone 15 mg, addo citrico 15 mg, sodio benzoato 10 mg, acqua depurata q.b. a 8 mi. Prima dell’uso 11 contenuto del sottotappo viene posto in contatto con il liquido del flaconcino premendo sul sottotappo. Ogni flaconcino contiene 300 mg di moguistelna come sospensione monodose.
ESEMPIO 9
Controllodellacessione in vitro
Il controllo della cessione e’ statoeffettuato utilizzando l’apparato II (paddle) della Farmacopea degli Stati Uniti Ed. XXII operando a 37*C, 75 g1r1/minuto, in 900 mi di mediumdi dissoluzione che per la prima orae’ HC1 0.1 N e dalla seconda alla dodicesima ora e’ tampone fosfato a pH 7.4. La determinazione del principio attivo rilasciato e’ stata effettuata spettrofotometricamente a 275 μm.
Vengono qui riportate le percentuali di principio attivo rilasciato nel tempo (ore) da un microgranulato preparato secondo quanto descritto negli esempi 3, 4, 5 e 7:
21* ( 1 h), 46% (2 h), 78* (4 h), 93* (8 h) e 98* (12 h).
ESEMPIO 10
Stabilita' della composizione nel tempo
La stabilita’ della sospensione a rilascio controllato preparato secondo l’esemplo 8 e’ stata studiata valutando da 3 e 6 mesi il profilo di rilascio percentuale della moguisteina secondo la metodica descritta al punto 9. I risultati sono riportati nella Tabella 1:
TABELLA 1
Il profilo di rilascio dopo ricostituzione con acqua e’ risultato praticamente Invariato anche su campioni ricostituiti dopo 6 mesi di conservazione a 35 °C.
Il profilo di dissoluzione della sospensione e’ stato valutato anche dopo 15 gg dalla sua ricostituzione con acqua. I risultati ottenuti sono riportati in Tabella 2.
TABELLA 2
Dalla tabella si vede come, dopo ricostituzione con acqua, il profilo di dissoluzione dellamoguisteina risulti Invariato anche dopo 15 gg assicurando cosi’ una buona stabilita’ alla dissoluzione per il periodo di terapia.
ESEMPIO 11
Sospendibilita' ed altre caratteristiche tecnologiche della sospensione A 33 g di sospensione preparata secondo quanto descritto nell’esempio 8, e’ stata aggiunta acqua fino a 100ml. Sono stati misurati: la sedimentazione F (espressa come rapporto fra altezza del sedimento ed altezza della sospensione agitata e lasciata a riposo per 3 gg), 11 pH, la viscosità’ (misurata con apparecchiatura Brookfleld DVII) e la densità’. I risultati sono riportati di seguito:
F = 0.6, pH = 4.3, Viscosità’ (cps) = 226; Densità’ (g/ml) = 1.1
ESEMPIO 12
B1odispon1bnita*
Per valutare la biodisponibilita’, e’ stato effettuato uno studio cinetico in dose singola su 6 volontari sani che hanno ricevuto una dose singola di 10 mi di formulazione liquida a rilascio controllato pari a 300 mg di moguisteina preparata secondo l’esempio 8. Campioni di sangue sono stati prelevati al diversi tempi ed e' stata determinata la concentrazione plasmatlca di moguisteina (valutata come addo) con metodo HPLC. Nella Tabella 3 sono riportati 1 principali parametri farmacocinetici risultanti dalla sperimentazione a confronto con dati ottenuti dalla somministrazione di una dose di sospensione al 2% tradizionale pari a 200 mg di moguisteina.
TABELLA 3
In Figura 1 sono riportati 1 livelli ematici normalizzati per dose, ottenuti dopo somministrazione delle due sospensioni sopradtate.
Il grafico, che ha in ordinate 1 valori di concentrazione su dose (L<-1>) ed in ascisse il tempo, evidenzia chiaramente come la somministrazione di moguisteina mediante la composizione oggetto dell’invenzione permette di evitare l’effetto di picco Iniziale e di ridurre il numero delle somministrazioni giornaliere, garantendo al contempo una buona copertura terapeutica.

Claims (12)

  1. RIVENDICAZIONI 1. Composizione farmaceutica mlcrogranulare a rilascio controllato per somministrazione di moguisteina in sospensione liquida, comprendente: a) una pluralità’ di nuclei mlcrogranularl contenenti moguisteina ed opportuni eccipienti, detti microgranuli aventi dimensioni variabili da 50 a 500 μm ed una superficie levigata adatta alla ricopertura con materiale polimerico o ceroso; b) almeno tre rivestimenti successivi costituiti da una alternanza di strati idrofili e strati applicati su detti nuclei, atti a garantire 11 rilascio della moguisteina in tempi predeterminati ed 11 mantenimento nel tempo del medesimo profilo di rilascio; c) un veicolo per la somministrazione del suddetti nuclei mlcrogranularl rivestiti.
  2. 2. Composizione secondo la rivendicazione 1, caratterizzata dal fatto che gli eccipienti contenuti nel nucleo mlcrogranulare sono scelti nel gruppo costituito da: polivin1ìp1rrolidone, lattosio, caldo fosfato bibasico, cellulosamlcrocristallina, amido, talco, zuccheri, copolimero polivinilpirrolidone/vinilacetato e gelatina, in presenzadi una quantità’ di polietilenglicole.
  3. 3. Composizione, secondo la rivendicazione 2, caratterizzata dal fatto che la quantità’ di polietilenglicole presente nellamiscela di granulazione e’ lo 0.5-1 % in peso rispetto al peso totale dei componenti.
  4. 4. Composizione secondo le precedenti rivendicazioni, caratterizzata dal fatto che i materiali polimerici che costituiscono gli strati Idrofili di rivestimento, sono selezionati nel gruppo costituito da: cellulosa acetoftalato e idrossipropilmetilcellulosa ftalato, eventualmente in presenza di dietilftalato, dlbutilsebacato o olii vegetali come plastificanti.
  5. 5. Composizione secondo la rivendicazione 4, caratterizzata dal fatto che la quantità’ di plastificante varia dal 10 al 30* in peso rispetto al peso totale del componenti la miscela di flimatura dello strato idrofilo.
  6. 6. Composizione secondo le precedenti rivendicazioni, caratterizzata dal fatto che i materiali cerosi che costituiscono gli strati lipofili di rivestimento, sono selezionati nel gruppo costituito da: mono- di- e tr1glicer1di di acidi grassi aventi catena da 6 a 36 atomi di carbonio, cera carnauba, cerad’api, cera candelilla, alcoli e addi grassi.
  7. 7. Composizione secondo la rivendicazione 6, caratterizzata dal fatto che lo strato cerosoe’ applicato allo stato fuso utilizzando come fluido di nebulizzazione aria compressa riscaldata.
  8. 8. Composizione secondo le precedenti rivendicazioni, caratterizzata dal fatto che il veicolo utilizzato per la somministrazione contiene sospendenti, strutturanti, dolcificanti, tamponanti, conservanti ed aromi.
  9. 9. Composizione secondo la rivendicazione 8, caratterizzata dal fatto che la miscela di componenti pronta all’uso e’ sospesa in acquao in miscele di acqua e coso!venti miscibili con acqua selezionati nel gruppo costituito da: glicoli, alcoli e glicerina.
  10. 10. Composizione secondo le precedenti rivendicazioni, caratterizzata dal fatto che può’ essere veicolata in forme farmaceutiche pronte all’uso o ricostituibili al momento dell’utilizzomediante presentanzioni che comprendono bustine e flaconcini monodose.
  11. 11. Composizione secondo le precedenti rivendicazioni, caratterizzata dal fatto di permettere il mantenimento di livelli plasmatici terapeuticamente efficaci di moguisteina o del suoi derivati metabolici.
  12. 12. Uso della composizione secondo le precedenti rivendicazioni per il trattamento sintomatico della tosse.
ITMI941410A 1994-07-07 1994-07-07 Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida IT1270594B (it)

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ITMI941410A IT1270594B (it) 1994-07-07 1994-07-07 Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
US08/452,435 US5674533A (en) 1994-07-07 1995-05-26 Pharmaceutical composition for the controlled release of moguisteine in a liquid suspension
PCT/IB1995/000412 WO1996001628A1 (en) 1994-07-07 1995-05-29 Pharmaceutical composition for the controlled release of moguisteine in a liquid suspension
BR9510302A BR9510302A (pt) 1994-07-07 1995-05-29 Forma de dosagem farmacêutical de liberação controlada método para tratamento sintomático da tosse método para preparar uma forma de dosagem farmacêutica de liberação controlada composição para uso no tratamento sintomático da tosse e aplicação de uma forma dosagem de moguisteina de liberação controlada
CA002194374A CA2194374A1 (en) 1994-07-07 1995-05-29 Pharmaceutical composition for the controlled release of moguisteine in a liquid suspension
AU24176/95A AU2417695A (en) 1994-07-07 1995-05-29 Pharmaceutical composition for the controlled release of moguisteine in a liquid suspension
EP95918125A EP0769948A1 (en) 1994-07-07 1995-05-29 Pharmaceutical composition for the controlled release of moguisteine in a liquid suspension
CZ199750A CZ287967B6 (cs) 1994-07-07 1995-05-29 Farmaceutická dávková forma s řízeným uvolňováním a způsob její přípravy a prostředek pro ošetřování kašle
KR1019970700062A KR970704437A (ko) 1994-07-07 1995-05-29 방출이 조절되는, 현탁액 상의 모귀스타인 의약 조성물(pharmaceutical composition for the controlled release of moguisteine in a liquid suspension
MX9700223A MX9700223A (es) 1994-07-07 1995-05-29 Composicion farmaceutica para la liberacion controlada de moguisteina en una suspension liquida.
JP8504206A JPH10502629A (ja) 1994-07-07 1995-05-29 懸濁液中のモグイステインの制御放出のための薬剤組成物
HU9700017A HUT76832A (en) 1994-07-07 1995-05-29 Pharmaceutical composition for the controlled release of moguisteine in a liquide suspension

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US5674533A (en) 1997-10-07
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WO1996001628A1 (en) 1996-01-25
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