A simple and effective method to improve bioavailability of glimepiride by utilizing hydrotropy technique

Li, Haiying; Ma, Lilan; Li, Xiaxia; Cui, Xin; Yang, Wenzhi; Shen, Shigang; Chen, Mingmao

doi:10.1016/j.ejps.2015.06.016

Cited by 25 publications

(16 citation statements)

References 53 publications

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“…Compared with the literature 26 reported about the GM release profiles in pH 7.4 PBS, there was no initial burst release. Greater release of GM from ME formulations may be attributed to the small spherical size, which increases the surface area for dissolution.…”

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confidence: 75%

“…However, recent studies have shown that enhanced apparent solubility, which is because of micellarization or complexation, does not induce an enhanced permeation rate of a poorly soluble drug in vitro. 26,[40][41][42][43][44] The solubility-permeability interplay cannot be ignored when using solubility-enabling formulations. 45,46 As mentioned earlier, we can draw a conclusion that increasing drug solubility utilizing pharmaceutical techniques does not necessarily lead to improved bioavailability.…”

Section: Pharmacokinetic Studymentioning

confidence: 99%

“…26 Because meglumine exhibited extensive H-bonding with all possible H-bond acceptors in the GM molecule, this extensive H-bonding between the two species appears to regulate the mobility of GM molecules in amorphous systems. Unlike other solubilization techniques, it has been shown that using the amorphous form allows to increase both molecularly solubility and drug flux through the membrane.…”

Section: Pharmacokinetic Studymentioning

confidence: 99%

“…Meanwhile, a noticeable enhancement in GM dissolution was observed in the GM-MU complex -the solubility of GM was found to increase up to 24,000 times. 26 It is interesting that the hydrotropy technique improves GM solubility much better than the ME technique, whereas the AUC of GMME is superior to that of GM-MU complex solution. The enhanced bioavailability of GMME was probably attributed to the following effects: first, the solubility of GM in GMME was significantly improved.…”

Section: Pharmacokinetic Studymentioning

confidence: 99%

“…26 Briefly, the mixture of GM and meglumine (1:3, w/w) was dissolved in 5 mL distilled water at 80°C in a water bath until the mixture was completely dissolved. The solution was lyophilized by using a freeze dryer (FD-1A-50, Beijing Boyikang Laboratory Instruments Co., Ltd, Beijing, People's Republic of China) until the GM-MU complex powder was obtained.…”

mentioning

confidence: 99%

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Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique

Li¹,

Pan²,

Cui³

et al. 2016

IJN

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The objective of this work was to prepare an oil/water glimepiride (GM) microemulsion (ME) for oral administration to improve its solubility and enhance its bioavailability. Based on a solubility study, pseudoternary phase diagrams, and Box–Behnken design, the oil/water GMME formulation was optimized and prepared. GMME was characterized by dynamic laser light scattering, zeta potential, transmission electron microscopy, and viscosity. The in vitro drug release, storage stability, pharmacodynamics, and pharmacokinetics of GMME were investigated. The optimized GMME was composed of Capryol 90 (oil), Cremophor RH40 (surfactant), and Transcutol (cosurfactant), and increased GM solubility up to 544.6±4.91 µg/mL. The GMME was spherical in shape. The particle size and its polydispersity index were 38.9±17.46 nm and 0.266±0.057, respectively. Meanwhile, the GMME was physicochemically stable at 4°C for at least 3 months. The short-term efficacy in diabetic mice provided the proof that blood glucose had a consistent and significant reduction at a dose of 375 µg/kg whether via IP injection or IG administration of GMME. Compared with the glimepiride suspensions or glimepiride-meglumine complex solution, the pharmacokinetics of GMME in Wistar rats via IG administration exhibited higher plasma drug concentration, larger area under the curve, and more enhanced oral bioavailability. There was a good correlation of GMME between the in vitro release values and the in vivo oral absorption. ME could be an effective oral drug delivery system to improve bioavailability of GM.

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confidence: 75%