Effect of stearic acid on the properties of metronidazole/methocel K4M floating matrices

Lara-Hernández, Belem; Hernández-León, Alejandra; Villafuerte-Robles, Leopoldo

doi:10.1590/s1984-82502009000300016

Cited by 8 publications

(5 citation statements)

References 20 publications

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“…It is also considered that the gas bubbles dissipating from the inside to the outside of the matrix debilitate the matrix structure. 44 The reduction in HPMC K15M-based FT size was greater than that in HPMC K100M FTs.…”

Section: Resultsmentioning

confidence: 89%

“…It was observed that polymers in the matrix undergo simultaneous swelling, dissolution, and diffusion into the bulk medium, resulting in erosion and reduction of the matrix strength. It is also considered that the gas bubbles dissipating from the inside to the outside of the matrix debilitate the matrix structure 44. The reduction in HPMC K15M-based FT size was greater than that in HPMC K100M FTs.…”

Section: Resultsmentioning

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: 89%

Section: Resultsmentioning

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

View full text Add to dashboard Cite

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“…The carbon di-oxide bubbles produced by sodium bicarbonate expand the matrices facilitating the drug dissolution and their presence might also obstruct the diffusion path through the hydrated gel layer (Lara-Hernández et al, 2009). This explains the difference in release and swelling behaviors between the effervescent and non effervescent mini-tablet formulations.…”

Section: Resultsmentioning

confidence: 99%

“…The polymer in the matrix undergoes simultaneous swelling, dissolution and diffusion into the bulk medium, resulting in erosion and reduction of the matrix strength. It is also considered that the gas bubbles dissipating from the inside to the outside of the matrix debilitate the matrix structure (Lara-Hernández et al, 2009).…”

Section: Resultsmentioning

confidence: 99%

Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori

El‐Zahaby

Kassem

El-Kamel

2014

Saudi Pharmaceutical Journal

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Gastroretentive levofloxacin (LVF) floating mini-tablets for the eradication of Helicobacter pylori (H. pylori) were prepared using the matrix forming polymer hydroxypropyl methylcellulose (HPMC K100M), alone or with Carbopol 940P in different ratios by wet granulation technique. Buoyancy of mini-tablets was achieved by an addition of an effervescent mixture consisting of sodium bicarbonate and anhydrous citric acid to some formulations. The prepared mini-tablets were evaluated for weight variation, thickness, friability, hardness, drug content, in vitro buoyancy, water uptake and in vitro release. The optimized formula was subjected to further studies: FT-IR, DSC analysis and in vivo examination in healthy volunteers. The prepared mini-tablets exhibited satisfactory physicochemical characteristics. Incorporation of gas-generating agent improved the floating parameters. HPMC K100M mini-tablet formulation (F1) offered the best controlled drug release (>8 h) along with floating lag time <1 s and total floating time >24 h. The obtained DSC thermograms and FT-IR charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. The in vivo test confirmed the success of the optimized formula F1 in being retained in the stomach of the volunteers for more than 4 h. LVF floating mini-tablets based on HPMC K100M is a promising formulation for eradication of H. pylori.

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“…They also found that HPMC formulated films were strongly dependent on SA content. Lara-Hernández et al (2009) found that the hydration volume, the tablet hardness and the ejection pressure decrease as the stearic acid content increases in the HPMC drug formulations. They also found that drug dissolution increases with increasing proportions of SA and decreasing proportions of the HPMC in the tablets.…”

Section: Materials Description: Hpmc MCC and Samentioning

confidence: 99%

Stearic acid crystals stabilization in aqueous polymeric dispersions

Jarray

Gerbaud

Hémati

2016

Chemical Engineering Research and Design

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In wet granulation processes, coatings or binders generally consist of mixtures of various raw materials that confer or enhance specific properties to the final product. Typically, a coating solution is composed of water, film forming polymer (such as hydroxypropylmethylcellulose, HPMC) and filler (such as stearic acid, SA). One of the important issues in wet granulation processes is the stability of the aqueous coating (or binder) dispersion. An unstable dispersion results in the agglomeration of the colloidal particles, thereby affecting the film coating properties and eventually the coating process. In this study, we use dissipative particle dynamics (DPD) to elucidate the structure of aqueous colloidal formulations. DPD is a coarse-grained molecular dynamics simulation method where the materials are described as a set of soft beads interacting according to the Flory-Huggins (1942) model. The DPD simulation results are compared to experimental results obtained by Cryogenic-SEM and particle size distribution analysis. It is shown from the DPD simulation results that the HPMC polymer is able to form a layer that covers SA particles and thus produces stable colloids. Microcrystalline cellulose (MCC) also covers SA agglomerate but it is not able to diffuse inside its inner core. The agglomerate structure is characterized via the density distribution and the polymer chain end-to-end distance. Experimental results show similar trends; particle size distribution analysis shows that in the presence of HPMC, the majority of SA particles are below 1 m in diameter, also MCC is able to prevent the formation of big SA agglomerates and may be a better stabilizing agent than HPMC. SEM images reveal that HPMC surrounds SA agglomerates with a hatching textured film and anchors on their surface.

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Effect of stearic acid on the properties of metronidazole/methocel K4M floating matrices

Cited by 8 publications

References 20 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

Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori

Stearic acid crystals stabilization in aqueous polymeric dispersions

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