High-quality Sulfobutyl Ether-beta-cyclodextrin Sodium Salt

Sulfobutyl Ether-beta-cyclodextrin Sodium Salt is an excipient compound incorporating a chemically modified cyclodextrin with a structure that optimises the solubility and stability of active pharmaceuticals and their properties. It is a highly water-soluble anionic cyclodextrin derivative. It can easily form non-covalent inclusion complexes with drug molecules and therefore reduce drug toxicity and haemolysis as well as control drug release rate. Its complexing properties also make it suitable for masking unpleasant odours and tastes of pharmaceutical products. It is used as an excipient in injection, oral, nasal and eye medication. 

FURTHER INFORMATION:

β-cyclodextrins have been used in pharmaceutical formulations for many years. Their structure of six to eight glucose units linked by 1,4-glucosidic bonds provides an internal hydrophobic cavity, able to “capture” a range of target molecules. Unlike some 

β-cyclodextrins which have produced toxic effects during long-term use, β-cyclodextrin sulfobutyl ether offers a comparatively safe and effective agent for increasing the solubility and bioavailability of therapeutics, in particular for biopharmaceutical classification system class II drugs (low solubility and high permeability).

The attachment of a sulfobutyl group to the parent β-cyclodextrin creates a molecule with a lower toxicity profile (e.g. higher haemocompatibility) and an increased capacity for forming complexes with drug molecules. When the hydroxyl groups of glucopyranose units are substituted with anionic groups, such as the sulfate and sulfobutyl-ether, the cyclodextrin showed negligible haemolytic activity due to its lower ability to disrupt and solubilise membrane lipids. In vivo studies have shown that β-cyclodextrin sulfobutyl ether is pharmacologically inactive and well tolerated at high doses. One study has demonstrated that β-cyclodextrin sulfobutyl ether administered intravenously is filtered renally and eliminated intact in urine as inulin, a finding that suggests the product has little or no nephrotoxicity. The substance has also shown antiangiogenic properties when co-administered with angiostatic steroids.

Use of the molecule in novel drug delivery systems is a growing area of interest. For example, the product has been included in the formulation of microspheres, liposomes, PEGylated liposomes, nanoparticles and nanofibres.

The molecule is able to form stable inclusion complexes with a range of guest molecules, from small molecules to large compounds, peptides and proteins, via relatively simple processes. This provides the opportunity for its use in optimised inclusion complexes as an efficient strategy for increasing the efficacy and reducing toxicity of many active pharmaceutical ingredients. For example, Sulfobutyl Ether-beta-cyclodextrin Sodium Salt  was found to significantly decrease the eye irritation of an ophthalmically applied pilocarpine prodrug solution by lowering the amount of free drug concentration in the recorneal area below typical thresholds for irritation。