Repaglinide-Cyclodextrin complexes: Preparation, Characterization and in vivo evaluation of antihyperglycemic activity

Desai, Neha; Bramhane, D. M.; Nagarsenker, Mangal S.

doi:10.1007/s10847-010-9895-0

Cited by 9 publications

(4 citation statements)

References 16 publications

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“…The main techniques available for the CD inclusion complexes preparation in the solid state can be grouped as follows: Methods in solution , where drug and CD are dissolved in water or organic solvent/water mixtures, with pH and temperature adjusted to achieve maximum interaction between the components. In the case of B s -type complexes, mainly occurring with natural CDs, the product is isolated by crystallization [14], whereas in the case of A-type complexes, the solvent is removed by an adequate drying technique, such as coevaporation under reduced pressure (COE) [22,23], spray-drying (SPD) [24,25], or freeze-drying (FD) [26,27]. The drawbacks of such methods are in high consumption of time, energy and organic solvents (such as ethanol and methanol) whose complete removal from the final solid product could be quite costly and challenging, due to the ability of such solvents for the inclusion complex formation [28], that could lead to toxic effects.…”

Section: Introductionmentioning

confidence: 99%

Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Jug

Mura

2018

Pharmaceutics

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Among the different techniques proposed for preparing cyclodextrin inclusion complex in the solid state, mechanochemical activation by grinding appears as a fast, highly efficient, convenient, versatile, sustainable, and eco-friendly solvent-free method. This review is intended to give a systematic overview of the currently available data in this field, highlighting both the advantages as well as the shortcomings of such an approach. The possible mechanisms involved in the inclusion complex formation in the solid state, by grinding, have been illustrated. For each type of applied milling device, the respective process variables have been examined and discussed, together with the characteristics of the obtained products, also in relation with the physicochemical characteristics of both the drug and cyclodextrin subjected to grinding. The critical process parameters were evidenced in order to provide a useful guide for a rational selection of the most suitable conditions for an efficient inclusion complex preparation by grinding, with the final purpose of promoting a wider use of this effective solvent-free cyclodextrin inclusion complex preparation method in the solid state.

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Section: Introductionmentioning

confidence: 99%

Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Jug

Mura

2018

Pharmaceutics

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“…The antidiabetic activity was evaluated in Alloxan induced diabetic male Wistar rats (250–300 g). [ 35 36 37 ] Powder PE and PE-CDs prepared by kneading method (BCDK2, HPBCDK2, and SBEBCDK2) were studied or glucose-lowering efficacy. The institutional animal ethics committee clearance was obtained prior to conducting these studies.…”

Section: Methodsmentioning

confidence: 99%

Characterization of pioglitazone cyclodextrin complexes: Molecular modeling to in vivo evaluation

et al. 2016

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Aims:The objective of present study was to study the influence of different β-cyclodextrin derivatives and different methods of complexation on aqueous solubility and consequent translation in in vivo performance of Pioglitazone (PE).Material and Methods:Three cyclodextrins: β-cyclodextrin (BCD), hydroxypropyl-β-cyclodextrin (HPBCD) and Sulfobutylether-7-β-cyclodextrin (SBEBCD) were employed in preparation of 1:1 Pioglitazone complexes by three methods viz. co-grinding, kneading and co-evaporation. Complexation was confirmed by phase solubility, proton NMR, Fourier Transform Infrared spectroscopy, Differential Scanning Calorimetry (DSC) and X-Ray diffraction (XRD). Mode of complexation was investigated by molecular dynamic studies. Pharmacodynamic study of blood glucose lowering activity of PE complexes was performed in Alloxan induced diabetic rat model.Results:Aqueous solubility of PE was significantly improved in presence of cyclodextrin. Apparent solubility constants were observed to be 254.33 M–1 for BCD-PE, 737.48 M–1 for HPBCD-PE and 5959.06 M–1 for SBEBCD-PE. The in silico predictions of mode of inclusion were in close agreement with the experimental proton NMR observation. DSC and XRD demonstrated complete amorphization of crystalline PE upon inclusion. All complexes exhibited >95% dissolution within 10 min compared to drug powder that showed <40% at the same time. Marked lowering of blood glucose was recorded for all complexes.Conclusion:Complexation of PE with different BCD significantly influenced its aqueous solubility, improved in vitro dissolution and consequently translated into enhanced pharmacodynamic activity in rats

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“…The oral glucose tolerance test (OGTT) was performed as per reported method [31].The rats were divided into three groups (n=6) and kept in fasted condition at overnight for 16 h. Group I served as control, Group II with pure RPGD (66.66µg/kg) and Group III with prepared R-acetostarch immediate-release tablet 5 min. The glucose load 3 g/kg was in all groups of an animal through oral route and blood glucose levels were reached peak at 60 min [32]. The blood samples were withdrawn from the retro-orbital sinus under ether inhalation after 0, 60, 90 and 120 min.…”

Section: In-vivo Study (Antihyperglycemic Activity)mentioning

confidence: 99%

In-vitro and in-vivo Consideration of Repaglinide Immediate-release Tablet: Assessment of Porous Aceto-starch as a Promising Carrier for Dissolution Rate Enhancement

Chatap¹,

Patil²

2016

fst

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Acetostarch was prepared using aqua-gel to an aceto-gel method and used as carrier to improved solubility and dissolution rate of Repaglinide (RPGD) to enhance oral bioavailability. The RPGD was selected as a model drug due to its low aqueous solubility and dissolution rate in GI fluid. In present research work, acetostarch was prepared by solvent exchange method and characterized by using FT-IR, DSC, XRPD, BET and FESEM studies followed by in-vitro drug release rate. In order to study drug interaction, compatibility, surface area, structural and morphological characteristics. Repaglinide loaded acetostarch (R-acetostarch) showed significant improvement in drug dissolution rate. Consequently, R-acetostarch immediate-release tablets were prepared by direct compression method. Pre and post-compression parameters for blend and tablets were studied and found within pharmacopoeial acceptable limits. R-acetostarch and immediate-release tablets demonstrated improved dissolution rate, when compared with pure crystalline RPGD, physical mixture and marketed tablets. The in-vivo assessment of R-acetostarch and immediate-release tablets were study by using oral glucose tolerance test and its indicated efficient control of blood glucose levels than pure RPGD and showed good in-vitro and in-vivo correlation. The results of stability studies revealed that there were no significant differences in physico-chemical parameters and dissolution rate between the initial and stored R-acetostarch immediate-release tablets. In a nutshell, it can be concluded that encapsulating poorly soluble drugs in porous acetostarch would be an innovative strategy for dissolution rate enhancement of BCS II drugs, when administered orally.

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Repaglinide-Cyclodextrin complexes: Preparation, Characterization and in vivo evaluation of antihyperglycemic activity

Cited by 9 publications

References 16 publications

Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Grinding as Solvent-Free Green Chemistry Approach for Cyclodextrin Inclusion Complex Preparation in the Solid State

Characterization of pioglitazone cyclodextrin complexes: Molecular modeling to in vivo evaluation

In-vitro and in-vivo Consideration of Repaglinide Immediate-release Tablet: Assessment of Porous Aceto-starch as a Promising Carrier for Dissolution Rate Enhancement

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