Application of ascorbic acid 2-glucoside as a solubilizing agent for clarithromycin: Solubilization and nanoparticle formation

Inoue, Yutaka; Yoshimura, Sachie; Tozuka, Yuichi; Moribe, Kunikazu; Kumamoto, Takuya; Ishikawa, Tsutomu; Yamamoto, Keiji

doi:10.1016/j.ijpharm.2006.09.014

Cited by 30 publications

(8 citation statements)

References 14 publications

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“…It is also the drug of choice for the treatment of peptic ulcer caused by H. pylori since the resistance is much lower when Clarithromycin is used compared to other antibiotics (Ramteke et al, 2006;Zakeri-Milani et al, 2009). Clarithromycin belongs to the class II of BCS having low solubility resulting in dissolution rate-limited absorption and low bioavailability when taken orally (Inoue et al, 2007;Shahbaziniaz et al 2013). It is extensively metabolized by CYP3A to 14-hydroxyClarithromycin and N-desmethylClarithromycin, exhibiting nonlinear pharmacokinetics, demonstrated by reduced clearance with increased doses.…”

Section: Introductionmentioning

confidence: 99%

Development of a biocompatible creatinine-based niosomal delivery system for enhanced oral bioavailability of clarithromycin

et al. 2016

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Section: Introductionmentioning

confidence: 99%

Development of a biocompatible creatinine-based niosomal delivery system for enhanced oral bioavailability of clarithromycin

et al. 2016

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“…It also exhibits P-gp inhibitory action and has been widely known to increase the solubility and bioavailability of water-insoluble drugs by many folds [15,16]. AA2G is a facile hydrophilic excipient that has been approved as a food additive and is expected to be used as a principal ingredient for solubilization in fat-soluble vitamin formulations and in other cosmetic products [17].…”

Section: Introductionmentioning

confidence: 99%

Improved Aqueous Solubility and Antihypercholesterolemic Activity of Ezetimibe on Formulating with Hydroxypropyl-β-Cyclodextrin and Hydrophilic Auxiliary Substances

Srivalli

Mishra

2015

AAPS PharmSciTech

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Abstract. The purpose of this study was to improve the aqueous solubility, dissolution, and pharmacodynamic properties of a BCS class II drug, ezetimibe (Eze) by preparing ternary cyclodextrin complex systems. We investigated the potential synergistic effect of two novel hydrophilic auxiliary substances, D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) and L-ascorbic acid-2-glucoside (AA2G) on hydroxypropyl-β-cyclodextrin (HPBCD) solubilization of poorly water-soluble hypocholesterolemic drug, Eze. In solution state, the binary and ternary systems were analyzed by phase solubility studies and Job's plot. The solid complexes prepared by freeze-drying were characterized by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), nuclear magnetic resonance (NMR), and scanning electron microscopy (SEM). The log P values, aqueous solubility, dissolution, and antihypercholesterolemic activity of all systems were studied. The analytical techniques confirmed the formation of inclusion complexes in the binary and ternary systems. HPBCD complexation significantly (p<0.05) reduced the log P and improved the solubility, dissolution, and hypocholesterolemic properties of Eze, and the addition of ternary component produced further significant improvement (p<0.05) even compared to binary system. The remarkable reduction in log P and enhancement in solubility, dissolution, and antihypercholesterolemic activity due to the addition of TPGS or AA2G may be attributed to enhanced wetting, dispersibility, and complete amorphization. The use of TPGS or AA2G as ternary hydrophilic auxiliary substances improved the HPBCD solubilization and antihypercholesterolemic activity of Eze.

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“…Clarithromycin is also the drug of choice to treat peptic ulcer as H. pylori resistance rate is much lower for clarithromycin as compared to other antibiotics like amoxicillin and tetracycline (Jain et al, 2006; Zakeri-Milani et al, 2005). However, like many other macrolide antibiotics, clarithromycin exhibits poor absorption and low bioavailability when administered orally (Inoue et al, 2007). It is extensively metabolized by CYP3A (which is highly expressed in the gastrointestinal tract) to 14-hydroxyclarithromycin and N-desmethylclarithromycin and exhibits nonlinear pharmacokinetics, demonstrated by reduced clearance with increasing doses.…”

Section: Introductionmentioning

confidence: 99%

A study on enhanced intestinal permeability of clarithromycin nanoparticles

Zakeri–Milani

Islambulchilar

Majidpour

et al. 2014

Braz. J. Pharm. Sci.

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The main objective of the present study was to determine the permeability of clarithromycin (CLA)-PLGA nanoparticles using single-pass intestinal perfusion technique in rats. Clarithromycin nanoparticles were prepared by nano-precipitation according to the modified quasi emulsion solvent diffusion technique and evaluated for their physicochemical characteristics. Permeability coefficients (P eff ) in anaesthetized rats were determined at 3 different concentrations. Drug solution or suspensions in PBS was perfused through a cannulated jejunal segment and samples were taken from outlet tubing at different time points up to 90 min. Microbiological assay of CLA and phenol red in the samples were analyzed using an agar well diffusion procedure and HPLC method respectively. The average particle size of prepared nanoparticles was 305 ± 134 nm. The mean P eff of CLA solution in concentrations of 150, 250 and 400 µg/mL was found to be 1.20 (±0.32) ×10 -3 , 9.62 (±0.46) ×10 -4 , and 1.36 (±0.95) ×10 -3 cm/sec, respectively. The corresponding values for the same concentration of nanoparticles were found to be 2.74 (±0.73) ×10 -3 , 2.45 (±0.88) ×10 -3 , and 3.68 (±0.46) ×10 -3 cm/s, respectively. The two-tailed Student's t-test showed that the intestinal permeability of CLA nanoparticle suspensions in prepared concentrations were significantly increased in comparison with its solution.Uniterms: Clarithromycin/nanoparticles/ permeability. Single-Pass Intestinal Perfusion. Intestinal permeability.O objetivo principal do presente estudo foi determinar a permeabilidade de nanopartículas de claritromicina (CLA)-PLGA, utilizando a técnica de perfusão intestinal de passo único em ratos. As nanopartículas de claritromicina foram preparadas por nanoprecipitação, de acordo com a técnica modificada de difusão de solvente quase-emulsão, e suas características físico-químicas avaliadas. Os coeficientes de permeabilidade (P eff ) em ratos anestesiados foram determinados em três concentrações diferentes. A solução, ou suspensões, do fármaco em PBS foi perfundida através do segmento de jejuno canulado e as amostras foram tomadas do tubo externo em diferentes tempos até 90 minutos. Os ensaios microbiológico de CLA e de vermelho de fenol das amostras foram realizados, utilizando-se o procedimento de difusão em poço de ágar e de CLAE, respectivamente. O tamanho médio das partículas das nanopartículas preparadas foi de 305 ± 134 nm. O P eff médio da solução de CLA em concentrações de 150, 250 and 400 µg/mL foi de 1.20(±0.32)×10 -3 , 9.62(±0. INTRODUCTIONOral administration remains the most convenient and useful route for delivering most pharmaceutical agents. However, the major problem of many orally administered drugs is to overcome several barriers before reaching their target site (Cook, Shenoy, 2003;Rao et al., 2008). Several approaches have been applied in order to improve the oral bioavailability of poorly permeable and soluble compounds intended for oral administration. Using nanoparticulate drug delivery system is considered as one of...

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Application of ascorbic acid 2-glucoside as a solubilizing agent for clarithromycin: Solubilization and nanoparticle formation

Cited by 30 publications

References 14 publications

Development of a biocompatible creatinine-based niosomal delivery system for enhanced oral bioavailability of clarithromycin

Development of a biocompatible creatinine-based niosomal delivery system for enhanced oral bioavailability of clarithromycin

Improved Aqueous Solubility and Antihypercholesterolemic Activity of Ezetimibe on Formulating with Hydroxypropyl-β-Cyclodextrin and Hydrophilic Auxiliary Substances

A study on enhanced intestinal permeability of clarithromycin nanoparticles

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