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1.
Artigo em Inglês | IMSEAR | ID: sea-163293

RESUMO

Aims: Sustained release floating drug delivery systems or gastro retentive drug delivery systems enables prolonged and continuous input of drug to the upper part of gastrointestinal tract and improves the bioavailability of medication. A new strategy is proposed for the development of floating drug delivery systems of Fluoroquinolone antibiotic, Ofloxacin, a potent moiety for treating UTI’s. Methodology: Various rate retarding polymers like HPMC K4M, HPMC 5 cps and swelling agent as Sodium carboxymethyl cellulose in different proportions were tried and optimized to achieve the drug release for 8 hr. All the formulations were evaluated for floating properties, swelling characteristics and in vitro drug release studies. The in vitro drug release was found to be matrix diffusion controlled. Optimized formulation was subjected to intermediate stability studies at various combinations of temperature and humidity according to ICH guidelines. Results: Lower hardness and higher thickness decreased the floating lag time and increased floating duration. Based on drug release studies, formulation F5 was optimized as the best formulation because it released about 89.27 ±2.6% of the drug at the end of 8 hr while other formulations released not more than 80 ±2.2%. This may be due to high NaCMC content which might have caused excessive channeling, thereby giving a burst release. Optimized formulation F5 was found to follow zero order kinetics with r2 value of 0.993. Conclusion: In conclusion we have been proved that HPMC K4M has retarded the drug release, while HPMC 5cps has facilitated high buoyancy time for the tablets. NaCMC has influenced as channeling agent. Formulation F5 was optimized for its long buoyancy time, prolonged duration of drug release, zero order and diffusion controlled drug release kinetics which can assure 100% bioavailability.


Assuntos
Química Farmacêutica , Carboximetilcelulose Sódica/farmacocinética , Preparações de Ação Retardada/química , Sistemas de Liberação de Medicamentos , Derivados da Hipromelose/farmacocinética , Ofloxacino/análise , Ofloxacino/química , Ofloxacino/metabolismo , Polímeros/farmacocinética , Solubilidade , Comprimidos , Água
2.
Rev. ciênc. farm ; 13: 23-36, 1991. tab, ilus
Artigo em Português | LILACS | ID: lil-167871

RESUMO

Investigou-se comparativamente o comportamento reológico de dispersöes de carboximetilcelulose sódica A.V. e Hidroxietilcelulose (cellosize-QP 15MH) a 0,5, 1,0, e 2,0 por cento, considerando o efeito produzido pelo aquecimento em processos de esterilizaçäo que aplicam calor úmido (vapor sob pressäo e vapor fluente). Procurou-se quantificar o comportamento reológico, antes e após processos de esterilizaçäo, objetivando qualificar os referidos produtos no que tange à sua aplicaçäo na forma de veículos estruturados esterilizados. Os resultados evidenciaram que: a) as dispersöes consideradas apresentaram uma similar perda de consistência independentemente do método de esterilizaçäo aplicado; b) apesar de diminuiçäo de consistência, as características reológicas, concernentes à pseudoplasticidade e tixotropia, foram relativamente bem mantidas; c) as dispersöes apresentaram diferentes graus de reversibilidade de consistência com nítidas vantagens para as dispersöes de hidroxietilcelulose


Assuntos
Carboximetilcelulose Sódica/farmacocinética , Hidróxidos/farmacocinética , Reologia , Esterilização
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