Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1997-09-15
2000-12-26
Lee, Howard C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
4241841, 514938, A61K 31715, A61K 3900
Patent
active
061659959
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a novel family of cyclodextrin-derivatives and, in particular, to a novel family of cyclodextrin-derivatives having both "higher" alkyl groups and sulfate groups, which are useful for, inter alia, biopharmaceutical applications and to methods for the preparation thereof.
Cyclodextrins (CDs) are a well-known family of crystalline, nonhygroscopic molecules comprised of a chain of either six, seven or eight glucopyranose units that are joined to one another at the terminal ends thereof. Due to steric reasons, cyclodextrins form a cyclic structure of torus-shaped macrorings which have an internal axial cavity. The outer surface of these molecules is hydrophilic. The internal cavity of these molecules is of apolar nature.
Used for a variety of purposes, a particularly important use for cyclodextrins has been as a carrier for drug molecules and antigens, which may be entrapped in the internal cavity thereof.
Drawbacks with cylcodextrins include the fact that they have various physical, chemical and physiochemical properties (such as solubility) which, while being appropriate for its intended use, are not appropriate for use with other molecules and/or other uses.
To provide CDs having desired physical, chemical and physiochemical properties, various chemical and/or enzymatic modifications have been made to the CD molecule to provide CD derivatives thereof.
In such CD derivatives, at least one of the free hydroxyl groups of the CD molecule (there being three such free hydroxyl groups on each of the glucopyranose units of the CD molecule) has been modified. Such modification is made by substitution of either the hydrogen atom of the hydroxyl group or of the entire hydroxyl group itself, with one of a large variety of substituting groups. In this fashion, depending upon the number and the type of substitution(s) performed, CD derivatives may be obtained which possess certain specific physiochemical properties desired for its intended use.
Relative to the use of CD derivatives as a carrier for drug molecules and antigens, it is noted that the complexation of a drug molecule or an antigen with a CD derivative can provide significant advantages in regards to improving the bioavailability and stability of the drug molecule. In such cases, improvements in the association between the CD derivative and the drug molecule can provide concomitant improvements in the bioavailability and/or stabilization of the drug molecule.
Unfortunately, the fabrication of such CD derivatives can often prove difficult and/or involve the use of procedures which are difficult, costly and even dangerous, especially on an industrial scale.
A further problem with CD derivatives is that, like conventional CDs, they possess specific physical, chemical and physiochemical properties (such as its shape, which can effect the fitting of the guest molecule in the internal axial cavity) which, while making them suitable for specific intended purposes, limit their wider for other purposes.
Accordingly, it is obvious that there remains a need for cyclodextrin derivatives which possess physiochemical properties that permit their wider use for various purposes. It can further be seen that there remains a need for an easy, safe and inexpensive method for the preparation of such CD derivatives on an industrial scale.
It is a primary object of the present invention to provide CD derivatives which are capable of forming complexes with a wide variety of guest molecules, especially drug molecules and antigens, and which possess physiochemical properties suitable for a wide variety of purposes.
It is another primary object of the present invention to provide CD derivatives which are capable of forming complexes with particular guest molecules, and especially with particular drug molecules and antigens, and which possesses certain physiochemical properties which are suitable for the specific purpose for which it is intended.
In another aspect of the present invention, it is a primary object herein to provide simple, easy and inexpens
REFERENCES:
patent: 4247535 (1981-01-01), Lewis et al.
patent: 5134127 (1992-07-01), Stella et al.
patent: 5180716 (1993-01-01), Yaksh et al.
patent: 5385891 (1995-01-01), Moriya et al.
patent: 5658894 (1997-08-01), Weisz
American Cyanamid Company
Lee Howard C.
LandOfFree
Cyclodextrin-derivatives and methods for the preparation thereof does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Cyclodextrin-derivatives and methods for the preparation thereof, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cyclodextrin-derivatives and methods for the preparation thereof will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-994972