A potent preparation method combining neutralization with microfluidization for rebamipide nanosuspensions and its<i>in vivo</i>evaluation

Shi, Yijie; Zou, Meijuan; An, Yue; Ji, Zhaoshuai; Gao, Ping; Cheng, Gang

doi:10.3109/03639045.2012.689765

Cited by 16 publications

(7 citation statements)

References 29 publications

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“…For preparation of stock solution 10 mg REB REB powder was dissolved in 200 ml methanol for a final concentration of 50 µg/ml Using methanol, REB stock solution was serial diluted to 10, 5, 2.5, 1, 0.5, 2.5, and 0.1µg/ml. from the dilutions, a calibration curve with different concentration ranges was constructed 15 .…”

Section: Construction Of Hplc Calibration Curvementioning

confidence: 99%

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Formulation and Characterization of Cubosomes Containing REB for Improvement of Oral Absorption of the Drug in Human Volunteers

Hashem

Nasr

Youssif

2018

Journal of Advanced Pharmacy Research

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Objective: To prepare rebamipide (REB) -loaded cubosomal nanoparticles to improve the oral bioavailability of the drug in human volunteers. Methodology: The poorly water soluble drug REB was incorporated into cubosomal nanoparticles by solvent dilution method. The prepared REB-loaded cubosomes were in vitro characterized for particle size, polydispersity index (PDI), zeta potential, drug crystallinity and in vitro drug release. In vivo absorption of REB-loaded cubosomes was compared with drug powder and commercially available tablets Mucosta ® (Egypt Otsuka Pharmaceutical Company) in healthy human volunteers. Results: In vitro, REB-loaded cubosomes entrapped about 82.44 % drug and revealed nanometer-size ranged from 303.1 ± 4.9 to 444.9 ± 6 nm. In vitro REB release from cubosomes exhibited a phase of rapid and high release of the drug during the first hour followed by a slower and complete drug release over a period of 3 hrs. The results of bioavailability study in healthy human volunteers showed that cubosomes significantly improved the rate and extent of REB absorption. The mean relative bioavailability of the REB loaded cubosomes compared to the drug powder and commercially available tablets (Mucosta ® ) was 267.67 % and 166.29 % respectively. Conclusion: The prepared cubosomes significantly improved the In-vivo absorption of REB in comparison with drug powder and commercially available tablets (Mucosta ® ).

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Section: Construction Of Hplc Calibration Curvementioning

confidence: 99%

“…Solutions were vortex mixed for 1 min, then centrifuged for 20 min at 5000. After centrifugation, supernatant was transferred to clean glass tubes and evaporated to dryness then reconstituted in 200 μL mobile phase and placed in clean injection vials for HPLC analysis 15 .…”

Section: Entrapment Efficiency %mentioning

confidence: 99%

Formulation and Characterization of Cubosomes Containing REB for Improvement of Oral Absorption of the Drug in Human Volunteers

Hashem

Nasr

Youssif

2018

Journal of Advanced Pharmacy Research

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“…However, a persistent and insuperable problem was that common particles were quickly evacuated from the GIT, despite reports suggesting that nano-and micro-sized colloidal particles innately bioadhered to the gastrointestinal mucosa 33,34 . For insoluble drugs with high membrane permeability, such as CoQ10, a short residence time at a high concentration does not result in ideal bioavailability.…”

Section: Introductionmentioning

confidence: 98%

The 12-3-12 cationic gemini surfactant as a novel gastrointestinal bioadhesive material for improving the oral bioavailability of coenzyme Q10 naked nanocrystals

Song

Han

Feng

et al. 2016

Drug Development and Industrial Pharmacy

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To improve the oral bioavailability of nanocrystalline drug preparations, the cationic 12-3-12 quaternary ammonium surfactant gemini was introduced into nanocrystals as a novel gastrointestinal bioadhesive material. Coenzyme Q10 (CoQ10), a typical Biopharmaceutics Classification System (BCS) class II drug, was used as a model drug. The 12-3-12 gemini surfactant was added to the preparation at a low concentration and imbued the particles with abundant positive charges. In vitro and in vivo gastrointestinal adhesion tests confirmed that the gemini-modified nanocrystals were prone to adhere to the upper gastrointestinal tract (GIT), thereby prolonging retention time in the GIT and enhancing absorption. In the distribution study in rats, the use of nanocrystals modified with gemini led to greater drug distribution to the heart and the liver than that achieved with the naked nanocrystals. A pharmacokinetic study in beagle dogs showed that the gemini-modified CoQ10 nanocrystals improved the oral bioavailability of CoQ10 in a dose-dependent manner, and the smaller size produced a much better effect with the same gemini modification. These results demonstrate that the cationic surfactant gemini is a promising oral bioadhesive material with applications in nanoscale drug delivery systems.

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“…Referred to solubility test of the literature [3], RBM was nearly indissolvable not only in polar but also in non-polar solvents. Shi YJ [4] prepared rebamipide nanosuspensions and improved its oral bioavailability. Nanosuspensions, also called nanocrystals, was regarded as an alternative and promising approach to settle these problems.…”

Section: Introductionmentioning

confidence: 99%

Enhanced bioavailability of rebamipide nanocrystal tablets: Formulation and in vitro/in vivo evaluation

Guo

Wang

2015

Asian Journal of Pharmaceutical Sciences

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a b s t r a c tThe purpose of this study was to formulate rebamipide nanocrystal tablets (REB-NTs) by wet-milling technique to enhance its dissolution rate and oral bioavailability. The formulation and preparation technology were screened by single factor tests with particle size and distribution as indicators. Rebamipide nanocrystals (REB-NSs) was then achieved by freeze-dry from the prepared nanosuspensions which were characterized by differential scanning calorimetry (DSC) and x-ray powder diffraction (XRD), while the vitro dissolution and the plasma drug concentration of the nanocrystal tablets were investigated. The results indicated that the prepared nanosuspensions got an average particle size of 286 nm, PI of 0.173 and the average Zeta potential of À18.2 mv. The average particle size of obtained REB-NSs' redispersibility was 278 nm, and the crystalline of REB-NSs was the same as the rebamipide bulk drug as shown by DSC and XRD. The drug dissolution rate of self-made nanocrystal tablets in different dissolutions was slightly faster than that from the reference tablets, REB-MTs (Mucosta ® ), while the C max and AUC 0e24 of REB-NTs were 1 and 1.57 times higher than that of REB-MTs, which means the nanotechnology could significantly improve the oral bioavailability of rebamipide.

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A potent preparation method combining neutralization with microfluidization for rebamipide nanosuspensions and itsin vivoevaluation

Abstract: The REB-NSs prepared by the combining method exhibited a higher plasma drug concentration and superior GI distribution, thereby demonstrating positive results for preparing nanosuspensions of local effective BCS IV drugs with pH dependence such as REB by this method.

Cited by 16 publications

References 29 publications

Formulation and Characterization of Cubosomes Containing REB for Improvement of Oral Absorption of the Drug in Human Volunteers

Formulation and Characterization of Cubosomes Containing REB for Improvement of Oral Absorption of the Drug in Human Volunteers

The 12-3-12 cationic gemini surfactant as a novel gastrointestinal bioadhesive material for improving the oral bioavailability of coenzyme Q10 naked nanocrystals

Enhanced bioavailability of rebamipide nanocrystal tablets: Formulation and in vitro/in vivo evaluation

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