Carvedilol (CAR) - hydroxypropyl - cyclodextrin inclusion complex

Carvedilol is alpha, beta blockers, and inhibit receptor vasodilation and effect for the treatment of mild and moderate hypertension or renal dysfunction in patients with hypertension, diabetes. But the water soluble, low oral bioavailability. CAR can be made of HP- beta -CD inclusion compounds, using polyethylene oxide bioadhesive polymer material (PEO) made of buccal tablets as auxiliary materials, produced by the porous structure of permeability and hydrophilicity and dissolution rate of cyclodextrin change matrix, and then adjust the drug effective liquidity in hydrated polymer materials, improve the rate of drug release, increase the bioavailability of the drug.

HP- beta -CD CAR prepared by freeze drying method of clathrate (molar ratio 1:2), PEO CAR and CAR/HP- -CD beta prepared by direct compression method. The results indicated that adhesion test, HP- beta -CD does not change the bioadhesive tablets. The change in in vitro dissolution test, two kinds of tablet dissolution curve a linear, tablet 10 hours without HP- -CD 40% beta release, containing HP- beta -CD package tablet compounds almost completely release. In the two kinds of tablets through the test of oral mucosa in pigs, tablets containing HP- mucosa beta -CD transmission rate is more than 3 times without HP- beta -CD the further study shows that with the increase of the amount of -CD HP- beta, CAR mucosa permeability declined.

Alpha Cyclodextrin sulfate & Hydrocortisone phosphate

Alpha-Cyclodextrin (synonyms: cyclohexaamylose, cyclomaltohexaose, alpha-Schar-dinger dextrin) is a non-reducing cyclic saccharide comprised of six glucose units linked by alpha-1, 4 bonds.

It is produced by the action of cyclodextrin glucosyltransferase (CGTase, EC 2.4.1.19) on hydrolysed starch syrups at neutral pH (6.0–7.0) and moderate temperature (35–40°C).

The annular (or doughnut-shaped) structure of alpha-cyclodextrin provides a hydrophobic cavity that allows formation of inclusion complexes with a variety of non-polar organic molecules of appropriate size.

The hydrophilic nature of the outer surface of the cyclic structure makes alpha-cyclodextrin water-soluble.

Other name: Cyclohexapentylose

CAS Registry Number: 10016-20-3

MF: C36H60O30

MW: 972.84

EINECS NO.: 233-007-4

Appearance: white crystalline or powder

Assay:99%min

[Structure]

[ Properties Computed from Structure] 

Gamma-cyclodextrin is a ring-shaped molecule made up of eight glucose units linked by alpha-1,4-bonds. The solubility degree of gamma-cyclodextrin in water is 23.2 g/100ml @ 25°C, which is higher than alpha-cyclodextrin and beta-cyclodextrin, and it is used to allow formation of inclusion complexes with bigger molecules.

CAS No.:  17465-86-0

Molecular Formula: C48H80O40

Molecular Weight: 1297.12

 

Application:

Gamma-cyclodextrin can be used as a carrier for flavours, sweeteners, and colours. In chemistry it is a valuable chemical reagent. When gamma-cyclodextrin exists,  fluorescence intensity of fluorescence pigment will become much bigger, so it is used as the analysis of protein and amino acid. Gamma-cyclodextrin is also used to separate long-chain organic compound, racemic modification and so on. Besides, the adsorbent made by gamma-cyclodextrin is used chromatographic analysis. It also can be used as complexing agent and cultivation agent in study of enzymatic activity.

Save

Natural Gamma Cyclodextrin

γ-cyclodextrin, Gamma Cyclodextrin Pharmaceutical Grade

Zhiyuan Biotchnology , http://www.zycydextrin.com