Potential Use of 2-Hydroxypropyl-.BETA.-cyclodextrin for Preparation of Orally Disintegrating Tablets Containing dl-.ALPHA.-Tocopheryl Acetate, an Oily Drug

Motoyama, Keiichi; Nagatomo, Kiyoshi; Elazim, Soliman Osama Abd; Hirayama, Fumitoshi; Uekama, Kaneto; Arima, Hisatomi

doi:10.1248/cpb.57.1206

Cited by 13 publications

(5 citation statements)

References 23 publications

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“…Figure 4 shows that the addition of HPβCD to water results in a small decrease in the surface tension. This small decrease in surface tension is in agreement with earlier observations by various investigators [ 24 , 26 , 30 , 31 ].…”

Section: Resultssupporting

confidence: 93%

“…A linear increase of viscosity is observed at HPβCD concentration below 11% ( w / v ), after which a positive deviation from linearity is observed. This upward curvature at higher HPβCD concentrations is not a novel observation, and similar results have also been described before [ 13 , 24 , 25 , 26 , 27 ].…”

Section: Resultssupporting

confidence: 89%

“…A decrease of 14 mN/m was observed at 0.5% ( w / v ) HPβCD concentration (corresponding to CMC), after which constant values are obtained even at HPβCD concentration as high as 35% ( w / v ). Yoshida et al suggested that this decrease in surface tension is due to the surface activity of HPβCD [ 24 , 30 ]. Other substituted βCDs also possess surface activity greater than that of the natural βCD [ 13 , 26 , 31 ].…”

Section: Resultsmentioning

confidence: 99%

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2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques

2018

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It is extremely important for pharmaceutical formulators to have analytical methodology that provides efficient detection and quantification of HPβCD aggregates. Five different methods were then evaluated for their potential to detect these aggregates and to determine critical aggregation concentration (cac): osmometry, viscometry, tensiometry, dynamic light scattering (DLS), and permeability studies. Overall, tensiometry was an inadequate method with which to study HPβCD aggregation, since the addition of HPβCD to water resulted in only minor changes in surface tension. Osmolality and viscosity studies have shown that for HPβCD, solute–solvent interactions are the main contributors for the observed deviation from ideality. These deviations might be related to the presence of aggregates. The DLS method proved to be an effective method with which to detect HPβCD aggregates and estimate their hydrodynamic diameter, although it presented some limitations concerning their quantification. In terms of the assessed methods, permeation studies were shown to be the best to study HPβCD aggregation phenomena, since they were the only method where the detection of aggregates and the determination of apparent cac values was possible. Also, it was the least invasive for the HPβCD samples and the method that provided more conclusive data. Results suggested that HPβCD, as expected, has less tendency to form aggregates than βCD.

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Section: Resultssupporting

confidence: 93%

Section: Resultssupporting

confidence: 89%

Section: Resultsmentioning

confidence: 99%

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2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques

2018

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“…Here, solutions of inclusion complexes between Vitamin E and HPβCD (Vitamin E/HPβCD-IC) having two different molar ratio (1:2 and 1:1 of Vitamin E/HPβCD) were prepared, and then these highly concentrated solutions (160% (w/v) HPβCD) were electrospun to produce nanofibrous webs (Figure ). As reported in the literature, Vitamin E molecules intend to form inclusion complexes with HPβCD by 1:2 molar ratio . The 1:2 molar ratio (Vitamin E/HPβCD) can be optimal because the long chain structure of Vitamin E molecule might induce steric effect during the complexation and so at least two HPβCD molecules needed for the full molecular coverage of Vitamin E in HPβCD cavities (Figure ).…”

Section: Resultsmentioning

confidence: 90%

“…As reported in the literature, Vitamin E molecules intend to form inclusion complexes with HPβCD by 1:2 molar ratio. 34 The 1:2 molar ratio (Vitamin E/HPβCD) can be optimal because the long chain structure of Vitamin E molecule might induce steric effect during the complexation and so at least two HPβCD molecules needed for the full molecular coverage of Vitamin E in HPβCD cavities (Figure 1). Even so, along with 1:2 molar ratio of Vitamin E/HPβCD, we have also prepared Vitamin E/HPβCD-IC with 1:1 molar ratio for the electrospinning to have higher loading (∼26% (w/w, respect to total fiber matrix) of Vitamin E in the nanofiber matrix.…”

Section: ■ Materials and Methodsmentioning

confidence: 99%

Antioxidant Vitamin E/Cyclodextrin Inclusion Complex Electrospun Nanofibers: Enhanced Water Solubility, Prolonged Shelf Life, and Photostability of Vitamin E

Çelebioğlu

Uyar

2017

J. Agric. Food Chem.

103

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Here, we demonstrated the electrospinning of polymer-free nanofibrous webs from inclusion complex (IC) between hydroxypropyl-β-cyclodextrin (HPβCD) and Vitamin E (Vitamin E/HPβCD-IC NF). The inclusion complexation between HPβCD and Vitamin E was prepared by using two different molar ratios (Vitamin E/HPβCD; 1:2 and 1:1), which correspond to theoretical value of ∼13% (w/w) and 26% (w/w) loading of Vitamin E in the nanofiber (NF) matrix. After electrospinning and storage, a very high loading of Vitamin E (up to ∼11% w/w, with respect to fiber matrix) was preserved in Vitamin E/HPβCD-IC NF. Because of the cyclodextrin inclusion complexation, only a minimal weight loss (only ∼2% w/w) was observed. While pure Vitamin E is insoluble in water, Vitamin E/HPβCD-IC NF web has displayed fast-dissolving behavior. Because of the greatly enhanced water-solubility of Vitamin E, Vitamin E/HPβCD-IC NF web has shown effective antioxidant activity. Additionally, Vitamin E/HPβCD-IC NF web has provided enhanced photostability for the sensitive Vitamin E by the inclusion complexation in which Vitamin E/HPβCD-IC NF still kept its antioxidant activity even after exposure to UV-light. Moreover, a 3 year-old Vitamin E/HPβCD-IC NF sample has shown very similar antioxidant efficiency when compared with freshly prepared Vitamin E/HPβCD-IC NF indicating that long-term stability was achieved for Vitamin E in the CD-IC fiber matrix. In brief, our results suggested that polymer-free electrospun Vitamin E/HPβCD-IC nanofibrous webs could have potential applications in food, pharmaceuticals, and healthcare thanks to its efficient antioxidant activity along with enhanced water-solubility, prolonged shelf life, and high photostability of Vitamin E.

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Combined use of cyclodextrins and hydroxypropylmethylcellulose stearoxy ether (Sangelose®) for the preparation of orally disintegrating tablets of type-2 antidiabetes agent glimepiride

Aldawsari

Banjar

Okubo

et al. 2014

J Incl Phenom Macrocycl Chem

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Potential Use of 2-Hydroxypropyl-.BETA.-cyclodextrin for Preparation of Orally Disintegrating Tablets Containing dl-.ALPHA.-Tocopheryl Acetate, an Oily Drug

Cited by 13 publications

References 23 publications

2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques

2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques

Antioxidant Vitamin E/Cyclodextrin Inclusion Complex Electrospun Nanofibers: Enhanced Water Solubility, Prolonged Shelf Life, and Photostability of Vitamin E

Combined use of cyclodextrins and hydroxypropylmethylcellulose stearoxy ether (Sangelose®) for the preparation of orally disintegrating tablets of type-2 antidiabetes agent glimepiride

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