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1.
Article in English | IMSEAR | ID: sea-163293

ABSTRACT

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.


Subject(s)
Chemistry, Pharmaceutical , Carboxymethylcellulose Sodium/pharmacokinetics , Delayed-Action Preparations/chemistry , Drug Delivery Systems , Hypromellose Derivatives/pharmacokinetics , Ofloxacin/analysis , Ofloxacin/chemistry , Ofloxacin/metabolism , Polymers/pharmacokinetics , Solubility , Tablets , Water
2.
Article in English | IMSEAR | ID: sea-152848

ABSTRACT

Gastric retentive floating drug delivery system (GFDDS) is enabled the prolonged continuous input of the drug to the upper parts of the gastrointestinal (GI) tract and improves the bioavailability of medications with narrow absorption window. The design of the delivery system is based on the controlled release formulation with floating and swelling features in order to prolong the gastric retention time of the drug delivery systems. In the present study norfloxacin as candidate, guar gum, sodium CMC, HPMC15 KM is studied along with other excipients like PVP K30 (binder), sodium bicarbonate microcrystalline cellulose were used in different concentrations to get the desired controlled release profile over a period of 12 hrs. All the formulations were evaluated for buoyancy lag time, duration of buoyancy, dimensional stability, drug content and in vitro drug release profile. Based on the in vitro studies carried out for the optimized formulation by dissolution the performance of the developed formulation promises to be efficient in controlling the drug release rate with the guar gum , a natural polymer.

3.
Article in English | IMSEAR | ID: sea-167846

ABSTRACT

Gastric retentive floating drug delivery system (GFDDS) is enabled the prolonged continuous input of the drug to the upper parts of the gastrointestinal (GI) tract and improves the bioavailability of medications with narrow absorption window. The design of the delivery system is based on the controlled release formulation with floating and swelling features in order to prolong the gastric retention time of the drug delivery systems. In the present study norfloxacin as candidate, guar gum, sodium CMC, HPMC15 KM is studied along with other excipients like PVP K30 (binder), sodium bicarbonate microcrystalline cellulose were used in different concentrations to get the desired controlled release profile over a period of 12 hrs. All the formulations were evaluated for buoyancy lag time, duration of buoyancy, dimensional stability, drug content and in vitro drug release profile. Based on the in vitro studies carried out for the optimized formulation by dissolution the performance of the developed formulation promises to be efficient in controlling the drug release rate with the guar gum , a natural polymer.

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