scispace - formally typeset
Search or ask a question
Journal ArticleDOI

Methods of Investigating and Preparing Inclusion Compounds

20 Mar 1990-ChemInform (Wiley)-Vol. 21, Iss: 12
About: This article is published in ChemInform.The article was published on 1990-03-20. It has received 62 citations till now.
Citations
More filters
Journal ArticleDOI
TL;DR: Cyclodextrins are a family of cyclic oligosaccharides composed of α-(1,4) linked glucopyranose subunits.

2,917 citations


Cites background from "Methods of Investigating and Prepar..."

  • ...While it is possible to use both guest or host changes to generate equi- librium constants, guest properties are usually most easily assessed....

    [...]

  • ...Additive properties that can be titrated in this way to provide information on theK-values include[32] aqueous solubility [33–35], chemical reactivity[36,37], molar absorptivity and other optical properties (e.g. optical rotation dispersion), phase solubility measurements[38], nuclear magnetic…...

    [...]

Journal ArticleDOI

1,198 citations

Journal ArticleDOI
TL;DR: 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.
Abstract: 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.

724 citations


Cites background from "Methods of Investigating and Prepar..."

  • ...drug– CD) interaction, and NMR, which can be used to determine the value of the stability constants (such as K1:1) and gives at the same time the solution geometry of the complexes.([20,40]) CDs and their complexes tend to self-associate in aqueous solutions to formaggregates and the aggregate formation is concentration dependent, increasing with increasing CD concentration....

    [...]

  • ...Properties that can be titrated in this way include aqueous solubility, chemical reactivity (stability), molar absorptivity, NMR chemical shifts, pKa values and HPLC retention times.([6,20,40]) It is also possible to titrate changes in the physicochemical properties of the host molecule (i....

    [...]

Journal ArticleDOI
TL;DR: In the pharmaceutical industry cyclodextrins have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs, and to increase their bioavailability and stability.
Abstract: Cyclodextrins are a family of cyclic oligosaccharides with a hydrophilic outer surface and a lipophilic central cavity. Cyclodextrin molecules are relatively large with a number of hydrogen donors and acceptors and, thus, in general they do not permeate lipophilic membranes. In the pharmaceutical industry cyclodextrins have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs, and to increase their bioavailability and stability. Studies in both humans and animals have shown that cyclodextrins can be used to improve drug delivery from almost any type of drug formulation. However, the addition of cyclodextrins to existing formulations without further optimisation will seldom result in acceptable outcome. Currently there are approximately 30 different pharmaceutical products worldwide containing drug/cyclodextrin complexes on the market.

719 citations


Cites methods from "Methods of Investigating and Prepar..."

  • ...Various methods can be applied to prepare D/CD complexes, including the solution method, the co-precipitation method, neutralisation method, the slurry method, the kneading method and the grinding method [23,32]....

    [...]

  • ...In theory, any methodology that can be used to observe these changes in additive physicochemical properties may be utilised to determine the stoichiometry of the complexes formed and the numerical values of their stability constants [23-25]....

    [...]

Journal ArticleDOI
TL;DR: It appears that cyclodextrins can only enhance topical drug delivery in the presence of water.

442 citations