Investigation of inclusion complex of trazodone hydrochloride with hydroxypropyl-β-cyclodextrin

Misiuk, Wieslawa; Zalewska, Magdalena

doi:10.1016/j.carbpol.2009.01.033

Cited by 80 publications

(32 citation statements)

References 17 publications

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“…4. a FTIR spectra, b X-ray diffractograms, and c DSC thermograms ternary systems were similar to the graphs of HPBCD because with the increase in complexation efficiency and addition of TPGS/AA2G, an excess of free HPBCD may have been present in each of the inclusion complex samples [30].…”

Section: Discussionmentioning

confidence: 75%

“…Beyond the results from solid-state analysis, it is the remarkable enhancement in solubility and release properties that could be seen as proof for the ternary complex formation and for possible interactions between HPBCD/Eze and TPGS/AA2G. The octanol-water partition coefficient, P, is the measure of the differential solubility of drug in octanol and water, and log P is Hansch factor and indicates the lipophilicity [21,30]. The log P results were in the order Eze>E-CD>E-CD-TPGS>E-CD-AA2G (p<0.05 for each comparison).…”

Section: Discussionmentioning

confidence: 99%

“…Δ log P (the relative hydrophilicity enhancement) was also determined to express the improved hydrophilicity brought about by HPBCD complexation and addition of auxiliary substances to the binary complex. The Δ log P can be defined as Δ log P=log P guest (pure drug)−log P complex (binary/ternary) [30]. The aqueous saturation solubility results of pure drug and binary and ternary systems are shown in Table III.…”

Section: Characterizationmentioning

confidence: 99%

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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: Discussionmentioning

confidence: 75%

Section: Discussionmentioning

confidence: 99%

Section: Characterizationmentioning

confidence: 99%

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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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“…Actually, the salmon industry is concerned about the need for optimize the therapeutic regimes, and one way to achieve predictable drug concentrations in plasma and tissues (taking into account the low and pH dependent solubility of EB) after an oral dose of a drug is improving its aqueous solubility with the use of cyclodextrins [9][10][11][12] . Of all the cyclodextrins used, hydroxypropyl-β-cyclodextrin (HP-β-CD) has been the most studied, because of its toxicological profile and better aqueous solubility [13][14][15] . Since there is no evidence of previous research, the aim of this work is to study the possibility of form an inclusion complex of EB and HP-β-CD, characterizing the final product in its physicochemical and dissolution properties.…”

Section: -Introduction Emamectin Benzoate (4′'r)-4″-deoxy-4″-(methmentioning

confidence: 99%

Preparation and Characterization of the Emamectin Benzoate/Hydroxypropyl-B-Cyclodextrin Inclusion Complex

Torres¹,

Villa²,

González³

et al. 2011

J. Chil. Chem. Soc.

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The objective of this study was to prepare an inclusion complex of the insecticide emamectin benzoate (EB) with hydroxypropyl-β-cyclodextrin (HP-β-CD) by co-evaporation and spray drying methods. The complexation of both compounds was evaluated on the aqueous and solid state using phase solubility diagrams, differential scanning calorimetry (DSC), X-Ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). The aqueous solubility of the inclusion complexes at pH 8 had a 2-fold increase respect to the drug alone and dissolution profiles showed a rise in the dissolution rate. These results suggest that the use of HP-β-CD could be an interesting alternative to enhance the bioavailability of EB in salmons.Key Words: Emamectin benzoate, cyclodextrin, inclusion complex, salmon.e-mail: cvonples@udec.cl 1.-INTRODUCTIONEmamectin benzoate, (4′'R)-4″-deoxy-4″-(methylamino)avermectin b1 benzoate, is one of the most widely used compounds in the salmon industry. Chemically, is a semisynthetic derivative of avermectins (Figure 1), which shows insecticide properties against the sea lice (Lepeophteirus salmonis), an ectoparasite that infests farmed salmons [1][2][3] . Unfortunately, it has been demonstrated that the efficacy of anti-infective treatments in salmons and trouts is low because is very difficult to control the dosage in medicated foods, which results in high intra-inter variability in plasma concentrations of the agents used [4][5][6] Of the approaches considered for improvement of the accuracy in the administration of EB, Glover et al. demonstrated that the intraperitoneal injection of the drug in farmed salmons resulted in higher and more predictable concentrations, but there are constraints that have relation with the manipulation of individual specimens 7 . From a point of view of the drug, one of the factors that influence the bioavailability of active compounds in living systems are their physicochemical properties like the solubility, which is often the limiting step in the absorption process. EB is a compound that has an erratic bioavailability and poor water solubility, which depends on the pH of the aqueous medium. At pH higher than 7, the solubility is drastically reduced and this is a relevant issue, because the intestinal pH of some fish can reach values of 7 -9 8 . Actually, the salmon industry is concerned about the need for optimize the therapeutic regimes, and one way to achieve predictable drug concentrations in plasma and tissues (taking into account the low and pH dependent solubility of EB) after an oral dose of a drug is improving its aqueous solubility with the use of cyclodextrins [9][10][11][12] . Of all the cyclodextrins used, hydroxypropyl-β-cyclodextrin (HP-β-CD) has been the most studied, because of its toxicological profile and better aqueous solubility [13][14][15] . Since there is no evidence of previous research, the aim of this work is to study the possibility of form an inclusion complex of EB and HP-β-CD, characterizing the...

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“…They have been well known to increase the solubility, stability, and bioavailability of hydrophobic drugs by the formation of inclusion complexes (7,8). Hydroxypropyl-β-cyclodextrin (HP-β-CD) is a hydroxypropylated derivative of β-cyclodextrin that has attracted growing interest because of its improved inclusion complexing ability, greater water solubility, and lesser toxicity (9,10). Literature lacks any data about the CLZ-CD systems and no related dosage forms are available on the market.…”

Section: Introductionmentioning

confidence: 99%

Formulation and In Vivo Evaluation of Orally Disintegrating Tablets of Clozapine/Hydroxypropyl-β-cyclodextrin Inclusion Complexes

et al. 2013

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Abstract. The aim of this study was to improve the solubility and oral bioavailability of clozapine (CLZ), a poorly water-soluble drug subjected to substantial first-pass metabolism, employing cyclodextrin complexation technique. The inclusion complexes were prepared by an evaporation method. Phase solubility studies, differential scanning calorimetry, X-ray powder diffraction, and Fourier transform infrared spectroscopy were used to evaluate the complexation of CLZ with hydroxypropyl-β-cyclodextrin (HP-β-CD) and the formation of true inclusion complexes. Characterization and dissolution studies were carried out to evaluate the orally disintegrating tablets (ODTs) containing CLZ/HP-β-CD complexes prepared by direct compression. Finally, the bioavailability studies of the prepared ODTs were performed by oral administration to rabbits. The ODTs showed a higher in vitro dissolution rate and bioavailability compared with the commercial tablets. It is evident from the results herein that the developed ODTs provide a promising drug delivery system in drug development, owing to their excellent performance of a rapid onset of action, improved bioavailability, and good patient compliance.

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Investigation of inclusion complex of trazodone hydrochloride with hydroxypropyl-β-cyclodextrin

Cited by 80 publications

References 17 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

Preparation and Characterization of the Emamectin Benzoate/Hydroxypropyl-B-Cyclodextrin Inclusion Complex

Formulation and In Vivo Evaluation of Orally Disintegrating Tablets of Clozapine/Hydroxypropyl-β-cyclodextrin Inclusion Complexes

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