Inclusion compounds of psychotropic agents and cyclodextrins

Андронаті, С. А.; Shapiro, Yu. E.; Yakubovskaya, L. N.; Gorbatyuk, V. Ya.; Andronati, K. S.; Krasnoschekaya, S. P.; Bogaisky, A. V.

doi:10.1007/bf01053430

Cited by 11 publications

(6 citation statements)

References 6 publications

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“…[43][44][45] Formation of non-inclusion complexes and CD aggregates contribute to the overall drug solubilization in aqueous CD solutions. [46][47][48][49][50][51][52][53] AN-type profiles have been explained by changes in the complexation media and self-association of CD molecules or their complexes at higher CD concentrations. B-type phase-solubility diagrams ( Figure 2) indicate formation of complexes with limited aqueous solubility and they are commonly observed in complexationmedia containing the natural aCD, bCD and gCD.…”

Section: Phase-solubility Diagramsmentioning

confidence: 99%

“…The natural CDs and their derivatives, as well as their complexes, are known to form aggregates [43–45] . Formation of non‐inclusion complexes and CD aggregates contribute to the overall drug solubilization in aqueous CD solutions [46–53] . A N ‐type profiles have been explained by changes in the complexation media and self‐association of CD molecules or their complexes at higher CD concentrations.…”

Section: Introductionmentioning

confidence: 99%

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Pharmaceutical applications of cyclodextrins: basic science and product development

Loftsson

Brewster

2010

Journal of Pharmacy and Pharmacology

810

496

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Objectives Drug pipelines are becoming increasingly difficult to formulate. This is punctuated by both retrospective and prospective analyses that show that while 40% of currently marketed drugs are poorly soluble based on the definition of the biopharmaceutical classification system (BCS), about 90% of drugs in development can be characterized as poorly soluble. Although a number of techniques have been suggested for increasing oral bioavailability and for enabling parenteral formulations, cyclodextrins have emerged as a productive approach. This short review is intended to provide both some basic science information as well as data on the ability to develop drugs in cyclodextrin-containing formulations. Key findings There are currently a number of marketed products that make use of these functional solubilizing excipients and new product introduction continues to demonstrate their high added value. The ability to predict whether cyclodextrins will be of benefit in creating a dosage form for a particular drug candidate requires a good working knowledge of the properties of cyclodextrins, their mechanism of solubilization and factors that contribute to, or detract from, the biopharmaceutical characteristics of the formed complexes. Summary We provide basic science information as well as data on the development of drugs in cyclodextrin-containing formulations. Cyclodextrins have emerged as an important tool in the formulator's armamentarium to improve apparent solubility and dissolution rate for poorly water-soluble drug candidates. The continued interest and productivity of these materials bode well for future application and their currency as excipients in research, development and drug product marketing.

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Section: Phase-solubility Diagramsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pharmaceutical applications of cyclodextrins: basic science and product development

Loftsson

Brewster

2010

Journal of Pharmacy and Pharmacology

810

496

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“…It is however becoming increasingly apparent that such assumptions may not be universally applicable or all encompassing. Specifically, there is a growing body of evidence that supports the important contribution of noninclusion aspects for drug solubilization by cyclodextrins including surfactant‐like effects and molecular aggregation, that is, formation of particulate systems 3–10. It is known that spontaneous opalescence occurs in aqueous γ‐cyclodextrin (γCD) solutions during storage11 and investigations of aqueous 1% (w/v) γCD solutions have shown that about 0.02% (w/w) of γCD in the solutions is in the form of aggregates 12.…”

Section: Introductionmentioning

confidence: 99%

Cyclodextrins as solubilizers: Formation of complex aggregates

Jansook

Kurkov

Loftsson

2010

Journal of Pharmaceutical Sciences

112

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“…Other investigators have shown that acridine/dimethyl‐β‐cyclodextrin 2:1 complex is formed when a 1:1 acridine/dimethyl‐β‐cyclodextrin inclusion complex forms a non‐inclusion complex with a second acridine molecule 13. Furthermore, some 1:2 and 2:2 drug/cyclodextrin complexes have been shown to consist of a mixture of inclusion and non‐inclusion complexes 14. Having said this, in current complexation models, formation of non‐inclusion cyclodextrin complexes is generally ignored.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Process‐Induced Dimensional Changes in the Membrane Structure of Biological Cells Using Impedance Measurement

Angersbach¹,

Heinz²,

Knorr³

2002

Biotechnology Progress

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The impact of high intensity electric field pulses, high hydrostatic pressure, and freezing-thawing on local structural changes of the membrane was determined for potato, sugar beet tissue, and yeast suspensions. On the basis of the electrophysical model of cell systems in biological tissues and suspensions, a method was derived for determining the extent of local damage of cell membranes. The method was characterized by an accurate and rapid on-line determination of frequency-dependent electrical conductivity properties from which information on microscopic events on cellular level may be deduced. Evaluation was based on the measurement of the relative change in the sample's impedance at characteristically low (f(l)) and high (f(h)) frequencies within the beta-dispersion range. For plant and animal cells the characteristic frequencies were f(l) approximately 5 kHz and f(h) > 5 MHz and for yeast cells in the range f(l) approximately 50 kHz and f(h) > 25 MHz. The observed phenomena were complex. The identification of the underlying mechanisms required consideration of the time-dependent nature of the processing effects and stress reactions of the biological systems, which ranged from seconds to several hours. A very low but significantly detectable membrane damage (0.004% of the total area) was found after high hydrostatic pressure treatment of potato tissue at 200 MPa. The membrane rupture in plant tissue cells was higher after freezing and subsequent thawing (0.9% of total area for potato cells and 0.05-0.07% for sugar beet cells determined immediately after thawing), which increased substantially during the next 2 h.

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Inclusion compounds of psychotropic agents and cyclodextrins

Cited by 11 publications

References 6 publications

Pharmaceutical applications of cyclodextrins: basic science and product development

Pharmaceutical applications of cyclodextrins: basic science and product development

Cyclodextrins as solubilizers: Formation of complex aggregates

Evaluation of Process‐Induced Dimensional Changes in the Membrane Structure of Biological Cells Using Impedance Measurement

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