Development of gastroretentive metronidazole floating raft system for targeting Helicobacter pylori

Youssef, Nancy Abdel Hamid Abou; Kassem, Abeer Ahmed; El-Massik, Magda A.; Boraie, Nabila

doi:10.1016/j.ijpharm.2015.04.004

Cited by 56 publications

(43 citation statements)

References 26 publications

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“…Studies reported that sodium bicarbonate is preferred as the gas-generating agent and that CaCO 3 showed internal ionotropic gelation during storage 2. Thus, in our study, sodium citrate was added to prevent premature gelation which may occur during storage, as sodium citrate complexes the free Ca 2+ ions and only releases them in the acidic environment of the stomach.…”

Section: Resultsmentioning

confidence: 91%

“…In most of the cases, the conventional oral delivery systems show limited bioavailability because of fast gastric emptying time among many other reasons involved 1,2. However, the recent technological development has resulted in too many novel pharmaceutical products, mainly the controlled release drug delivery systems to help overcome this problem.…”

Section: Introductionmentioning

confidence: 99%

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Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl

El-Nabarawi

Teaima

El-Monem

et al. 2017

DDDT

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To prolong the residence time of dosage forms within the gastrointestinal tract until all drug is released at the desired rate is one of the real challenges for oral controlled-release drug delivery systems. This study was designed to develop a controlled-release floating matrix tablet and floating raft system of Mebeverine HCl (MbH) and evaluate different excipients for their floating behavior and in vitro controlled-release profiles. Oral pharmacokinetics of the optimum matrix tablet, raft system formula, and marketed Duspatalin® 200 mg retard as reference were studied in beagle dogs. The optimized tablet formula (FT-10) and raft system formula (FRS-11) were found to float within 34±5 sec and 15±7 sec, respectively, and both remain buoyant over a period of 12 h in simulated gastric fluid. FT-10 (Compritol/HPMC K100M 1:1) showed the slowest drug release among all prepared tablet formulations, releasing about 80.2% of MbH over 8 h. In contrast, FRS-11 (Sodium alginate 3%/HPMC K100M 1%/Precirol 2%) had the greatest retardation, providing sustained release of 82.1% within 8 h. Compared with the marketed MbH product, the Cmax of FT-10 was almost the same, while FRS-11 maximum concentration was higher. The tmax was 3.33, 2.167, and 3.0 h for marketed MbH product, FT-10, and FRS-11, respectively. In addition, the oral bioavailability experiment showed that the relative bioavailability of the MbH was 104.76 and 116.01% after oral administration of FT-10 and FRS-11, respectively, compared to marketed product. These results demonstrated that both controlled-released floating matrix tablet and raft system would be promising gastroretentive delivery systems for prolonging drug action.

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Section: Resultsmentioning

confidence: 91%

Section: Introductionmentioning

confidence: 99%

Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl

El-Nabarawi

Teaima

El-Monem

et al. 2017

DDDT

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“…Calcium carbonate was selected as a gas-forming agent, as it releases carbon dioxide in the presence of gastric fluid resulting in the formation of gel with floating characteristics (24). On the basis of various literature reports, the quantity of calcium carbonate used in the formulation was fixed at 300 mg (24,25), which is considerably lower than the permissible limit of 550 mg suggested by FDA (26) and much lower than the amount (i.e., 1250 mg) known to cause flatulence and/or systemic acidosis (27). A total of 13 different formulations were prepared employing sodium alginate (X 1 ) and gellan (X 2 ) as the CMAs at three different levels, i.e., low (−1), intermediate (0), and high (+1) levels, including quintuplicate studies at the center point (0,0) formulations.…”

Section: Formulation Optimization Of Stimuli-responsive Gr Systemsmentioning

confidence: 99%

QbD-Enabled Development of Novel Stimuli-Responsive Gastroretentive Systems of Acyclovir for Improved Patient Compliance and Biopharmaceutical Performance

et al. 2015

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Abstract. The current studies entail systematic quality by design (QbD)-based development of stimuliresponsive gastroretentive drug delivery systems (GRDDS) of acyclovir using polysaccharide blends for attaining controlled drug release profile and improved patient compliance. The patient-centric quality target product profile was defined and critical quality attributes (CQAs) earmarked. Risk assessment studies, carried out through Ishikawa fish bone diagram and failure mode, effect, and criticality analysis, helped in identifying the plausible risks or failure modes affecting the quality attributes of the drug product. A face-centered cubic design was employed for systematic development and optimization of the concentration of sodium alginate (X 1 ) and gellan (X 2 ) as the critical material attributes (CMAs) in the stimuli-responsive formulations, which were evaluated for CQAs viz. viscosity, gel strength, onset of floatation, and drug release characteristics. Mathematical modeling was carried out for generation of design space, and optimum formulation was embarked upon, exhibiting formulation characteristics marked by excellent floatation and bioadhesion characteristics along with promising drug release control up to 24 h. Drug-excipient compatibility studies through FTIR and DSC revealed absence of any interaction(s) among the formulation excipients. In vivo pharmacokinetic studies in Wistar rats corroborated extension in the drug absorption profile from the optimized stimuli-responsive GR formulations vis-à-vis the marketed suspension (ZOVIRAX®). Establishment of in vitro/in vivo correlation (IVIVC) revealed a high degree of correlation between the in vitro and in vivo data. In a nutshell, the present investigations report the successful development of stimuli-responsive GRDDS of acyclovir, which can be applicable as a platform approach for other drugs too.

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“…MT is an active adjunct in treatment of Helicobacter pylori (Prasanthi et al, 2011;Emara et al, 2014). It is classified as Class I by Biopharmaceutical Classification System, has pH independent activity, and it is mainly absorbed in the stomach (Krishnaiah et al, 2003;Abou Youssef et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

“…Floating microparticles for the treatment of H. pylori allow the buoyancy of dosage form in the gastric fluid providing adequate prolongation of drug release near to the ecological niche of the bacterium (Abou Youssef et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

Floating ability and drug release evaluation of gastroretentive microparticles system containing metronidazole obtained by spray drying

Nohemann

Almeida

Ferrari

2017

Braz. J. Pharm. Sci.

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Gastroretentive floating microparticles were developed and evaluated for the controlled metronidazole delivery for treatment of gastric disease. Floating microparticles, varying in proportions of chitosan and hydroxypropyl methylcellulose or ethylcellulose, were obtained by spray drying. Floating microparticles were characterized by physicochemical and in vitro studies, according to their floating ability and drug delivery. Microparticles presented mean diameter from 1.05 to 2.20 µm. The infrared spectroscopy confirmed the drug encapsulation and showed no chemical linkage between microparticles components. X-ray diffraction showed changes in the drug`s solid state, from crystalline to amorphous, indicating partial drug encapsulation, due to the presence of some crystalline peaks of metronidazole in microparticles. All microparticles floated immediately in contact of simulated gastric fluid and both floating and drug release profiles were dependent of microparticles composition. Microparticles samples constituted by chitosan and hydroxypropyl methylcellulose revealed the best relationship between floating duration and drug release, remaining floating during the occurrence of the drug release, ideal condition for the floating gastroretentive systems.Uniterms: Floating microparticle. Chitosan. Ethylcellulose. Hydroxypropyl methylcellulose. Controlled drug delivery.

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Development of gastroretentive metronidazole floating raft system for targeting Helicobacter pylori

Cited by 56 publications

References 26 publications

Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl

Formulation, release characteristics, and bioavailability study of gastroretentive floating matrix tablet and floating raft system of Mebeverine HCl

QbD-Enabled Development of Novel Stimuli-Responsive Gastroretentive Systems of Acyclovir for Improved Patient Compliance and Biopharmaceutical Performance

Floating ability and drug release evaluation of gastroretentive microparticles system containing metronidazole obtained by spray drying

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