BRPI1103093A2 - oral pharmaceutical composition and use of the oral pharmaceutical composition - Google Patents
oral pharmaceutical composition and use of the oral pharmaceutical composition Download PDFInfo
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- BRPI1103093A2 BRPI1103093A2 BRPI1103093-3A BRPI1103093A BRPI1103093A2 BR PI1103093 A2 BRPI1103093 A2 BR PI1103093A2 BR PI1103093 A BRPI1103093 A BR PI1103093A BR PI1103093 A2 BRPI1103093 A2 BR PI1103093A2
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
- A61K9/2846—Poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Abstract
COMPOSIÇçO FARMACÊUTICA ORAL E USO DA COMPOSIÇçO FARMACÊUTICA ORAL. A presente invenção diz respeito a uma composição farmacêutica oral contendo ao menos um agente de supressão de ácido gástrico, particularmente um inibidor da bomba de prótons (RPI), e um agente prócinético (PA), voltada ao uso em transtornos relacionados ao excesso de ácido gástrico, por exemplo, a doença de refluxo gastroesofágico.ORAL PHARMACEUTICAL COMPOSITION AND USE OF ORAL PHARMACEUTICAL COMPOSITION. The present invention relates to an oral pharmaceutical composition containing at least one gastric acid suppressing agent, particularly a proton pump inhibitor (RPI), and a prokinetic agent (PA), intended for use in excess acid related disorders. gastric disease, for example, gastroesophageal reflux disease.
Description
COMPOSIÇÃO FARMACÊUTICA ORAL E ÜSO DA COMPOSIÇÃOORAL PHARMACEUTICAL COMPOSITION AND USE OF COMPOSITION
FARMACÊUTICA ORAL CAMPO DA INVENÇÃOORAL PHARMACEUTICAL FIELD OF THE INVENTION
A presente invenção diz respeito a uma composicão "farmacêutica- oral contendo..ao_menos um agente de supressão de ácido gástrico, particularmente um inibidor da bomba de prótons (PPI) , e um agente prócinético (PA) , voltada ao uso em transtornos relacionados ao excesso de ácido gástrico, por exemplo, a doença de refluxo gastroesofágico.The present invention relates to an oral pharmaceutical composition containing only a gastric acid suppressing agent, particularly a proton pump inhibitor (PPI), and a prokinetic agent (PA), intended for use in disorders related to Excess gastric acid, for example, gastroesophageal reflux disease.
ANTECEDENTES DA INVENÇÃOBACKGROUND OF THE INVENTION
Os distúrbios relacionados ao ácido gástrico, entre _ os= quais, a doença de refluxo gastroesofágico, esofagite de refluxo, úlcera péptica, úlcera gástrica", "têm patogenia relacionada à motilidade gástrica e emissão excessiva de ácido gástricoTais distúrbios - são .tipicamente tratados com inibidores de ácido gástrico, como ranitidina e omeprazol, que são agentes de supressão de ácido.Gastric acid-related disorders, including gastroesophageal reflux disease, reflux esophagitis, peptic ulcer, gastric ulcer, have pathogenesis related to gastric motility and excessive gastric acid emission. These disorders are typically treated with gastric acid inhibitors such as ranitidine and omeprazole which are acid suppressing agents.
Há publicações que propõem acelerar a cicatrização de úlcera gástrica por estimulação da motilidade gástrica. Agentes pró-cinéticos, entre os quais bromoprida, cisaprida, alizaprida, cleboprida, domperidona, e metoclopramida têm conhecida ação no aumento da motilidade gastrintestinais, evitando refluxo duodenogástrico, com uso conhecido para tratar a doença de refluxo gastroesofágico.There are publications that propose to accelerate the healing of gastric ulcer by stimulation of gastric motility. Prokinetic agents, including bromopride, cisapride, alizapride, clebopride, domperidone, and metoclopramide have been known to increase gastrointestinal motility, preventing duodenogastric reflux, which is known to treat gastroesophageal reflux disease.
Inibidores da bomba de ' prótons, entre eles omeprazol, lansoprazol e pantoprazol, tem rapidamente substituído os antagonistas de receptores H2 no tratamento de refluxo esofágico, pois apresentam grande eficácia, com melhor resolução de sintomas.Proton pump inhibitors, including omeprazole, lansoprazole and pantoprazole, have rapidly replaced H2 receptor antagonists in the treatment of esophageal reflux, as they are highly effective, with better resolution of symptoms.
Uma terapia combinada de um agente pró-cinético e um agente de diminuição de ácido gástrico já demonstrou mais efetividade do que a monoterapia com inibidores da bomba de prótons. A administração de cisaprida e ranitidina mostrou diminuir a exposição do esôfago a acidez (Inauen W. et al., Gut. 1993; 34:1025-1031) . Tal terapia mostrou também melhora na rapidez da cura (de Boer WA et al., Aliment Pharmacol. Ther. 1994; 8:147-157).Combination therapy of a prokinetic agent and a gastric acid lowering agent has already been shown to be more effective than proton pump inhibitor monotherapy. Administration of cisapride and ranitidine has been shown to decrease esophageal exposure to acidity (Inauen W. et al., Gut. 1993; 34: 1025-1031). Such therapy has also been shown to improve the speed of cure (de Boer WA et al., Aliment Pharmacol. Ther. 1994; 8: 147-157).
No estado da . técnica, podemos destacar: US 4.786.505 (omeprazol com revestimento entérico); WO 9501803 (agente pró-cinético); EP 247.983, WO 9427988, US 5.330.982, US 6.046.183 e US 6.521.255. ' ~ = " - " -In the state of. technique, we can highlight: US 4,786,505 (enteric coated omeprazole); WO 9501803 (prokinetic agent); EP 247,983, WO 9427988, US 5,330,982, US 6,046,183 and US 6,521,255. '~ = "-" -
0 PI 9607344-6 descreve uma forma de dosagem unitária" fixada," ~ tablete- -ou - cápsula, _ em. .revestimento entérico na forma de pellets.PI 9607344-6 describes a "fixed," tablet-or-capsule unit dosage form, in. enteric coating in the form of pellets.
O PI 0401556-8 refere-se a uma combinação de PPI e agente pró-cinético, particularmente lanzoprazol + bromoprida.PI 0401556-8 relates to a combination of PPI and prokinetic agent, particularly lanzoprazole + bromopride.
0 PI 0506704-9 menciona uma composição de liberação retardada, agente pró-cinético de liberação bimodal.PI 0506704-9 mentions a delayed release composition, bimodal prokinetic release agent.
0 pedido internacional, WO 2004071374, revela uma composição de dose única onde o PPI é de liberação retardada e o agente pró-cinético de liberação imediata e/ou sustentada.International application WO 2004071374 discloses a single dose composition wherein the PPI is delayed release and the prokinetic immediate and / or sustained release agent.
0 pedido internacional, WO 2005117870, destaca uma composição de PPI, agente de tamponamento e agente pró- cinético·International application, WO 2005117870, highlights a composition of PPI, buffering agent and prokinetic agent.
Entretanto, ainda existe a busca por uma medicação para distúrbios relacionados ao ácido gástrico, agindo também sobre náuseas e vômito que podem ocorrer em paralelo, _e que permitam^ alta adesão do paciente ao tratamento.However, there is still a search for a medication for gastric acid-related disorders, also acting on nausea and vomiting that may occur in parallel, and that allow high adherence of the patient to treatment.
DESCRIÇÃO DA INVENÇÃODESCRIPTION OF THE INVENTION
Em vista das deficiências do estado da técnica, a presente invenção refere-se a uma composição farmacêutica contendo um ou mais agentes de supressão de ácido gástrico, particularmente um inibidor da bomba de pró tons, um ou mais agentes pró-cinéticos, e excipientes farmaceuticamente aceitáveis. Tal composição é útil no tratamento de distúrbios relacionados ao ácido gástrico, como"azia,"doença" de refluxo gastroesofágico, esofagite de refluxo, úlcera péptica, úlcera gástrica, e similares. · _ _ _ _In view of the prior art deficiencies, the present invention relates to a pharmaceutical composition containing one or more gastric acid suppressing agents, particularly a proton pump inhibitor, one or more prokinetic agents, and pharmaceutically excipients. acceptable. Such a composition is useful in treating gastric acid related disorders such as "heartburn, gastroesophageal reflux disease", reflux esophagitis, peptic ulcer, gastric ulcer, and the like.
Conforme utilizado aqui, "composição" refere-se tanto à mistura de todos os componentes entre si, numa forma de dosagem unitária, quanto a duas ou mais formulações individuais e autônomas de componentes, inseridas dentro de lima forma de dosagem unitária, por exemplo, uma cápsula de gelatina, cápsula de hidroxipropilmetil celulose (HPMC) e similares. Estão cobertas pela invenção concretizações em que:As used herein, "composition" refers to either mixing all components together in a unit dosage form or to two or more individual, stand alone component formulations within a single unit dosage form, e.g. a gelatin capsule, hydroxypropyl methyl cellulose (HPMC) capsule and the like. Embodiments are covered by the invention in which:
- uma cápsula contém um PPI e excipientes, outra cápsula contém um PA e excipientes, e tais duas cápsulas por sua vez estão contidas em uma única cápsula;- one capsule contains a PPI and excipients, another capsule contains a PA and excipients, and such two capsules in turn are contained in a single capsule;
- uma cápsula contém um PPI e excipientes, e um comprimido contém um PA e excipientes, e dita cápsula e dito comprimido estão ambos contidos em uma única cápsula. De forma alternativa, a cápsula pode conter um PA è oa capsule contains a PPI and excipients, and a tablet contains a PA and excipients, and said capsule and said tablet are both contained in a single capsule. Alternatively, the capsule may contain a PA è the
comprimido pode conter um PPI;tablet may contain a PPI;
- um comprimido contém um PPI e excipientes, e outro comprimido contém um PA e excipientes, e tais _dois_ comprimidos estão contidos em uma única cápsula;.One tablet contains a PPI and excipients, and another tablet contains a PA and excipients, and such two tablets are contained in a single capsule.
iam comprimido com duas camadas, uma camada contendo um PPI e outra camada contendo um PA.iam compressed with two layers, one layer containing a PPI and another layer containing a PA.
De forma preferencial, sem excluir qualquer outra, a invenção refere-se a uma composição oral, caracterizada ' pelo fato de compreender em uma única forma ^ de dosagem unitária, particularmente em uma cápsula, ' comprimidos ■ - -distintos de *(a) um ou mais 'inibidores"- dã bomba de prótons escolhidos entre omeprazol, esomeprazol, pantoprazol, lansoprazol e rabeprazol, com _os_ respectivos, excipientes _e (b) um ou mais agentes pró-cinéticos escolhidos entre bromoprida, cisaprida, alizaprida, cleboprida, domperidona, e metoclopramida, com os respectivos excipientes.Preferably, without excluding any other, the invention relates to an oral composition, characterized in that it comprises in a single unit dosage form, particularly in a capsule, disintegrated tablets of (a). one or more 'inhibitors' - give proton pump selected from omeprazole, esomeprazole, pantoprazole, lansoprazole and rabeprazole, with their respective excipients and (b) one or more prokinetic agents selected from bromopride, cisapride, alizapride, clebopride, domperidone , and metoclopramide, with their excipients.
Tal configuração particular propicia: 2 0 - a preparação autônoma de comprimidos que levamSuch a particular configuration provides: 20 - the autonomous preparation of tablets that carry
em conta as características particulares tanto dos inibidores da bomba de prótons quanto dos agentes pró- cinético. Por exemplo, sabe-se que inibidores da bomba de prótons são instáveis em meio ácido, sendo, portanto sujeitos a degradação, podendo ser protegidos poraccount the particular characteristics of both proton pump inhibitors and prokinetic agents. For example, proton pump inhibitors are known to be unstable in an acidic environment and therefore subject to degradation and may be protected by
revestimento específico;specific coating;
- a separação entre tais princípios ativos, em- the separation between such active principles in
virtude da característica individual de sítio de liberação no organismo,due to the individual release site characteristic in the body,
a utilização independente, se desejada, dos comprimidos isoladamente um do outro;the independent use, if desired, of the tablets alone from one another;
a facilitação da adesão ao tratamento, por tratar-se de uma única unidade de administração contendo osfacilitating adherence to treatment as it is a single administration unit containing
dois princípios ativos.two active principles.
Dentro dessa configuração preferencial da composição da invenção, com características versáteis quanto à forma de dosagem unitária, cada comprimido pode apresentar características específicas, iguais ou distintas entre si, como:Within this preferred embodiment of the composition of the invention, having versatile unit dosage characteristics, each tablet may have specific, same or distinct characteristics as:
- revestimento entérico; .. _ . - -velocidade " dé" 'liberação (imediata, lenta,- enteric coating; .. _. - "speed" 'release (immediate, slow,
adiada, controlada, e similares); - mistura individual^ de.= cada ^.ati.vo -com- outros-delayed, controlled, and the like); - individual mixture of = each - active - with - others -
princípios ativos ou ingredientes de atividades específicas.active ingredients or ingredients of specific activities.
Inibidores da bomba de prótons presentes nas formas de dosagem da invenção podem ser utilizados na forma neutra ou na forma de sal alcalino, por exemplo, como sais 20" de magnésio, cálcio, sódio, potássio ou lítio. Onde aplicável, os inibidores da bomba de prótons, podem ser utilizados na forma racêmica, ria forma de enantiômero puro, ou sais alcalinos de enantiômeros.Proton pump inhibitors present in the dosage forms of the invention may be used in neutral or alkaline salt form, for example as magnesium, calcium, sodium, potassium or lithium salts. Where applicable, pump inhibitors of protons may be used in racemic form, pure enantiomer form, or alkaline salts of enantiomers.
Dentro de uma realização particular da invenção, o inibidor da bomba de prótons preferido é escolhido entre o pantoprazol, seus sais, ésteres, hidratos, derivados, pró- drogas ou metabólitos, sob qualquer forma polimórfica. Mais particularmente, utiliza-se pantoprazol sódico sesquiidratado.Within a particular embodiment of the invention, the preferred proton pump inhibitor is chosen from pantoprazole, its salts, esters, hydrates, derivatives, prodrugs or metabolites in any polymorphic form. More particularly, pantoprazole sodium sesquihydrate is used.
Dentro de uma realização particular da invenção, o agente pró-cinético preferido é escolhido entre a domperidona, seus sais, ésteres, hidratos, derivados, pró-Within a particular embodiment of the invention, the preferred prokinetic agent is chosen from domperidone, its salts, esters, hydrates, derivatives,
drogas ou metabólitos, sob qualquer forma polimórfica. _______drugs or metabolites in any polymorphic form. _______
A composição da invenção em sua acepção ampla, e particularmente na realização de dois comprimidos distintos contidos em uma cápsula de gelatina, cápsulas de hidroxipropilmetil celulose (HPMC) e similares, contém excipientes farmaceuticamente aceitáveis, como diluentes, aglutinantes, desintegrantes, corantes, antiaderentes, lubrificantes, plastificantes, sequestrantes, agentes de revestimento; " an t i óx idan t es, ~ opacificantes, aromatizantes, edulcorantes, e similares, utilizados sós ou em combinações entre si . Uma ^ referência_ conhecida, do .homem, da técnica-sobre excipientes farmaceuticamente aceitáveis é no livro "Remington? s Pharmaceutical Sciences", 18a edição, (1990), Mack Publishing Co., USA.The composition of the invention in its broad sense, and particularly in the realization of two distinct tablets contained in a gelatin capsule, hydroxypropyl methylcellulose (HPMC) capsules and the like, contains pharmaceutically acceptable excipients such as diluents, binders, disintegrants, colorants, nonstick, lubricants, plasticizers, sequestrants, coating agents; "Antioxidants, opacifiers, flavors, sweeteners, and the like, used alone or in combination with each other. A well-known reference in the art of pharmaceutically acceptable excipients is in the book" Remington? Pharmaceutical Sciences, 18th edition, (1990), Mack Publishing Co., USA.
Exemplos de diluentes adequados à invenção, sem excluir quaisquer outros, são escolhidos entre celulose microcristalina, lactose monoidratada ou anidra, fosfato dibásico de cálcio, sacarideos como manitol, sorbitol, sacarose e glicose,Examples of diluents suitable for the invention, without excluding others, are chosen from microcrystalline cellulose, lactose monohydrate or anhydrous, dibasic calcium phosphate, saccharides such as mannitol, sorbitol, sucrose and glucose,
Exemplos de agentes alcalinizantes adequados à invenção, sem excluir quaisquer outros, são escolhidos entre óxido de magnésio, hidróxido de sódio, bicarbonato de sódio, carbonato de sódio e suas misturas.Examples of alkalinizing agents suitable for the invention, without excluding any others, are selected from magnesium oxide, sodium hydroxide, sodium bicarbonate, sodium carbonate and mixtures thereof.
Exemplos de agentes aglutinantes adequados à invenção, sem excluir quaisquer outros, são escolhidos entre povidona, crospovidona e hidroxipropilcelulose.Examples of suitable binding agents to the invention, without excluding any others, are chosen from povidone, crospovidone and hydroxypropylcellulose.
Exemplos de desintegrantes adequados à invenção, sem excluir quaisquer outros, são selecionados entre polivinilpirrolidona, reticulados ou não, amido (de^ milho, de batata, e similares) , amidos modificados, croscarmelose, croscarmelose sódica, amido . glicolato de sódio, hidroxipropi lmetil celulose, hidroxipropilcelulose de baixa substituição, e misturas destes.Examples of disintegrants suitable for the invention, without excluding any others, are selected from cross-linked polyvinylpyrrolidone or not, starch (corn, potato, and the like), modified starches, croscarmellose, croscarmellose sodium, starch. sodium glycolate, hydroxypropyl methylcellulose, low substitution hydroxypropylcellulose, and mixtures thereof.
Exemplos de lubrificantes adequados à invenção, sem excluir quaisquer outros, são dióxido de silício coloidal, talco, ácido esteárico, estearato de magnésio, -estearato de- cálcio, estearato de zinco, fumarato de sódio estearila, e misturas destes.Examples of lubricants suitable for the invention, without excluding any others, are colloidal silicon dioxide, talc, stearic acid, magnesium stearate, calcium stearate, zinc stearate, sodium stearyl fumarate, and mixtures thereof.
Exemplos adequados_;à _invenção ,de materiais - dej revestimentos e seus complementar es, para comprimidos, sem excluir quaisquer outros, são, hidroxipropilmetil celulose, Eudragit (fabricado por Evonik), Opadry (fabricado por Colorcon) , trietilcitrato, propileno glicol e similares.Suitable examples of the inventive tableting materials and supplements therefor, without excluding others, are hydroxypropyl methylcellulose, Eudragit (manufactured by Evonik), Opadry (manufactured by Colorcon), triethylcitrate, propylene glycol and the like.
Dentro de realizações preferenciais, asWithin preferred embodiments, the
quantidades dos ativos nas composições da invenção, na sua forma livre, são de:The amounts of the actives in the compositions of the invention in their free form are:
- pantoprazol: 20 ou 4 0mg.pantoprazole: 20 or 40mg.
- domperidona: 1Omg.- domperidone: 10mg.
Dentro de outro aspecto, a invenção refere-se ao uso da composição descrita anteriormente na manufatura de um medicamento utilizado no tratamento dos distúrbios causados por ácido gástrico, particularmente azia, doença de refluxo gastroesofágico, esofagite de refluxo, úlcera péptica, úlcera gástrica.Within another aspect, the invention relates to the use of the composition described above in the manufacture of a medicament for the treatment of disorders caused by gastric acid, particularly heartburn, gastroesophageal reflux disease, reflux esophagitis, peptic ulcer, gastric ulcer.
EXEMPLOEXAMPLE
Os exemplos dados a seguir devem ser entendidos como concretizações particulares da invenção, ^sem por_esse motivo imporem restrição de qualquer forma ou natureza, além do conteúdo das reivindicações apresentadas mais adiante.The following examples are to be understood as particular embodiments of the invention, without, therefore, imposing restrictions of any form or nature beyond the content of the claims set forth below.
TABELA 1TABLE 1
PANTOPRAZOL 20MG COMPRIMIDO REVESTIDOPANTOPRAZOL 20MG COATED TABLET
Ingrediente Quantidade Pantoprazol sódio sesquiidratado 21,14Omg Manitol 29,032mg "Povidona K90 " 1,995mg Carbonato sódio 11,243mg Povidona -ret iculada „ _ ,_ " - _ _12,.500mg — -=^ Água deionizada NA Estearato cálcio 1,60 Omg Hidroxipropilmetil celulose 91% + Polietileno Glicol 9% 6,3 62mg Hidroxipropilcelulose 0, 07 8mg Povidona K30 0,10Omg Dióxido de -titânio 0,088mg Propilenoglicol 1,114mg Oxido ferro amarelo 0,009mg Álcool etilico absoluto NA Eudragit L 30 D 55 27,384mg Polissorbato 80 0,292mg Trietilcitrato 0,7 82mg Simeticona USP 0, Ollmq Talco 3,844mg Hidróxido de sódio . qs pH Água deionizada NAIngredient Amount Pantoprazole sodium sesquihydrate 21,14Omg Mannitol 29,032mg "Povidone K90" 1,995mg Sodium carbonate 11,243mg Povidone-reticulated „_, _" - _ _12, .500mg - - = ^ Deionized water NA Calcium stearate 1.60 Omg Hydroxypropylmethyl cellulose 91% + Polyethylene Glycol 9% 6.3 62mg Hydroxypropylcellulose 0.07 8mg Povidone K30 0.10Omg Titanium dioxide 0.088mg Propylene glycol 1,114mg Yellow iron oxide 0.009mg Absolute ethyl alcohol NA Eudragit L 30 D 55 27,384mg Polysorbate 80 0,292 mg Triethylcitrate 0.7 82mg Simethicone USP 0, Ollmq Talc 3,844mg Sodium hydroxide qs pH Deionized water NA
TABELA 2 ___TABLE 2 ___
PANTOPRAZOL 4OMG COMPRIMIDO REVESTIDO4OMG PANTOPRAZOL COATED COATED
Ingrediente Quan ti dade Pantoprazol sódio sesquiidratado 42,28Omg Manitol 58,O 65mg Povidona K90 3,99mg Carbonato sódio 22, 4 85mg Povidona reticulada 25,OOOmg •Água deionizada NA Estearato cálcio 3, 2 Omg Hidroxipropilmetil - celulose _ 9.1%. ._ +_ Polietileno Glicol 9 _ _ 10,-17-lmg - - Hidroxipropilcelulose 0, 124mg Povidona K30 0, 16 Omg Dióxido de titânio 0,14 Omg Propilenoglicol 1,78 Omg Oxido ferro amarelo 0,015mg Álcool etilico absoluto NA Eudragit L 30 D 55 51,874 Polissorbato 80 0,557mg Trietilcitrato 1,49Img Simeticona USP 0,148mg Talco 7,354mg Hidróxido de sódio qs pH Água deionizadaIngredient Amount Pantoprazole sodium sesquihydrate 42.28Omg Mannitol 58.0 65mg Povidone K90 3.99mg Sodium carbonate 22.4 85mg Reticulated Povidone 25.04mg • Deionized water NA Calcium stearate 3.2 Omg Hydroxypropyl methylcellulose _ 9.1%. ._ + _ Polyethylene Glycol 9 _ _ 10, -17-lmg - - Hydroxypropylcellulose 0.124mg Povidone K30 0.16 Omg Titanium Dioxide 0.14 Omg Propylene Glycol 1.78 Omg Oxide Yellow Iron 0.015mg Absolute Ethyl Alcohol NA Eudragit L 30 D 55 51,874 Polysorbate 80 0,557mg Triethylcitrate 1,49Img Simethicone USP 0,148mg Talc 7,354mg Sodium hydroxide pH Deionized water
TABELA. 3 DOMPERIDONA IOMG COMPRIMIDOTABLE. 3 IOMG DOMPERIDONE COMPRESSED
Ingrediente Quantidade Domperidona base 10,2 Omg______ Amido totalmente pré-gelatinizado 7,OOmg Lauril sulfato de sódio 0, 5 Omg Dióxido de silício coloidal 200 1,5 Omg Lactose compressão direta 60,OOmg Estearato de magnésio vegetal 1,OOmg Óleo vegetal hidrogenado 0,7Omg Glicolato de amido sódico 5,0 Omg Celulose microcristalina 102 14,IOOmgIngredient Quantity Domperidone base 10.2 Omg______ Fully pregelatinized starch 7.0Omg Sodium Lauryl Sulfate 0.5 Omg Colloidal Silicon Dioxide 200 1.5 Omg Direct Compression Lactose 60.0 OOmg Vegetable Magnesium Stearate 1, OOmg Hydrogenated Vegetable Oil 0 Sodium Starch Glycolate 5.0 Omg Microcrystalline Cellulose 102 14, 100mg
Apesar do homem da técnica, com o auxilio dos .ensinamentos- aqui- apresentados,- serem "capaz" dè "concretizar de formas não expressamente divulgadas aqui, mas com as mesmas funções em busca do mesmo resultado, tais realizações equivalentes também estão protegidas nas reivindicações a seguir.Although the man of the art, with the help of the teachings presented herein, is "capable" of realizing in ways not expressly disclosed herein, but with the same functions in pursuit of the same result, such equivalent realizations are also protected in following claims.
Claims (11)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BRPI1103093-3A BRPI1103093A2 (en) | 2011-06-03 | 2011-06-03 | oral pharmaceutical composition and use of the oral pharmaceutical composition |
| PCT/BR2012/000168 WO2012162777A1 (en) | 2011-06-03 | 2012-05-29 | Oral pharmaceutical composition comprising a proton pump inhibitor and a prokinetic agent that can be used in excess stomach acid disorders |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BRPI1103093-3A BRPI1103093A2 (en) | 2011-06-03 | 2011-06-03 | oral pharmaceutical composition and use of the oral pharmaceutical composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI1103093A2 true BRPI1103093A2 (en) | 2013-07-02 |
Family
ID=47258191
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI1103093-3A BRPI1103093A2 (en) | 2011-06-03 | 2011-06-03 | oral pharmaceutical composition and use of the oral pharmaceutical composition |
Country Status (2)
| Country | Link |
|---|---|
| BR (1) | BRPI1103093A2 (en) |
| WO (1) | WO2012162777A1 (en) |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9600072D0 (en) * | 1996-01-08 | 1996-01-08 | Astra Ab | New oral formulation of two active ingredients II |
| AU2001227744A1 (en) * | 2000-01-13 | 2001-07-24 | Osmotica Corp. | Osmotic device containing ranitidine and a prokinetic agent |
| WO2004071374A2 (en) * | 2003-02-11 | 2004-08-26 | Torrent Pharmaceuticals Limited | Once a day orally administered pharmaceutical compositions |
| AU2005204014B2 (en) * | 2004-01-06 | 2008-02-28 | Panacea Biotec Ltd. | Pharmaceutical compositions comprising a proton pump inhibitor and a prokinetic agent |
| BRPI0401553A (en) * | 2004-03-02 | 2004-11-23 | Marchesan Implement & Maquin | Drive an electronically controlled electric motor fertilizer feeder |
| MXPA06011820A (en) * | 2004-04-16 | 2006-12-15 | Santarus Inc | Combination of proton pump inhibitor, buffering agent, and prokinetic agent. |
| CN101305995A (en) * | 2007-05-17 | 2008-11-19 | 北京利乐生制药科技有限公司 | Sustained release preparation containing domperidone pantoprazole sodium and its preparation method |
| CN102125689A (en) * | 2010-01-12 | 2011-07-20 | 上海中邦斯瑞生物药业技术有限公司 | Compound preparation of proton pump inhibitor and domperidone |
-
2011
- 2011-06-03 BR BRPI1103093-3A patent/BRPI1103093A2/en not_active Application Discontinuation
-
2012
- 2012-05-29 WO PCT/BR2012/000168 patent/WO2012162777A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| WO2012162777A9 (en) | 2013-07-25 |
| WO2012162777A1 (en) | 2012-12-06 |
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