Physicochemical and molecular modeling studies of cefixime–l-arginine–cyclodextrin ternary inclusion compounds

Jadhav, Priyanka; Petkar, Bhushan; Pore, Yogesh; Kulkarni, Anita S.; Burade, Kishorkumar

doi:10.1016/j.carbpol.2013.07.070

Cited by 60 publications

(46 citation statements)

References 29 publications

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“…The ternary systems may further improve the physicochemical and transport properties of drugs in comparison to binary complexes [8]. Literature reports several studies on the effect of water-soluble substances like polymers [9][10][11], surfactants [12], metal salts [13], and amino acids [14] on CD solubilization of drugs. In the present study, we evaluated the effect of two hydrophilic auxiliary substances, namely, D-α-tocopheryl polyethylene glycol 1000 succinate (Vitamin E TPGS or simply TPGS) and L-ascorbic acid-2-glucoside (AA2G), as third components to the CD complexes, for the first time.…”

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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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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“…When the drug is complexed in CD cavity, its melting points usually shift to different temperatures or disappears. [16][17][18] DSC pattern of FBX and all systems are shown in Figure 5. DSC thermogram of FBX showed sharp melting point endotherm at 195.36ºC ( Figure 5A), while thermogram of HPβCD did not exhibit any melting endotherm ( Figure 5B) indicating its amorphous nature.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Physicochemical Characterization of Febuxostat Microcomplexes with Parent and Modified Cyclodextrins

Aher¹,

Pore²

2018

Dhaka Univ. J. Pharm. Sci

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Febuxostat, a BCS class II antigout drug was complexed with β-cyclodextrin (βCD), hydroxypropyl-β-cyclodextrin (HPβCD) and / or methyl-β-cyclodextrin (MβCD), to improve its physicochemical properties. Earlier phase solubility and thermodynamic investigations in acetate buffer (pH 4.5) illustrated AL (linear) type of solubility curve and enthalpy driven complexation process, respectively. The association constant and complexation efficiency of modified cyclodextrins (CDs) were significantly higher than that of parent cyclodextrin (CD). The microcomplexes prepared by spray drying process were examined for their spectral, diffractometric, thermal, particle size, saturation solubility, Log P and dissolution properties. The physicochemical properties of pure drug were improved upon complexation with CDs. However, modified CDs produced amorphous micro-complexes contributing for their better performance as compared to parent CD.

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“…Despite the wide research on the applications of arginine in food [21,22] and pharmaceuticals industries [23], the compaction properties of this amino acid were never investigated. Prior to evaluating the compaction behaviour of ARG, the micromeritic characteristics; particle size, are shown in Fig.…”

Section: Powder Characterisationmentioning

confidence: 99%

A methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets

ElShaer

Kaialy

Akhtar

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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Physicochemical and molecular modeling studies of cefixime–l-arginine–cyclodextrin ternary inclusion compounds

Cited by 60 publications

References 29 publications

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

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

Physicochemical Characterization of Febuxostat Microcomplexes with Parent and Modified Cyclodextrins

A methodological evaluation and predictive in silico investigation into the multi-functionality of arginine in directly compressed tablets

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