Hydroxypropyl betadex is prepared by the treatment of an alkaline
solution of b-cyclodextrin with propylene oxide. The substitution
pattern can be influenced by varying the pH. Formation of O-6 and
O-2 substituted products is favored by high and low alkali
concentration, respectively. The mixture of products produced
may be refined by preparative chromatography.
The pharmaceutical toxicology of hydroxypropyl betadex has been
reviewed, and in general, the material was found to be of low
toxicity. It has been suggested that hydroxypropyl betadex may
have a synergistic toxic effect with, for example, carcinogens, by
increasing their solubility and thus bioavailability.
Included in oral and parenteral medicinal products. Included in an
injectable preparation licensed in the UK for intramuscular or
enteric coating, sustained release formulations, buccal and transdermal drug delivery
White to slightly yellow powder
2-Hydroxypropyl-β-cyclodextrin can be used as selective estrogen receptor modulator for the prevention of osteoporosis
Hydroxypropyl betadex occurs as a white or almost white,
amorphous or crystalline powder.
Store in well-closed containers.
Hydroxypropyl betadex has been widely investigated in pharmaceutics
and has principally been used as a solubilizer for
hydrophobic molecules in oral liquids,oral solids, parenterals,
pressurized metered dose inhalers, dry powder inhalers,
and topical formulations. It has also been shown to act as a
stabilizer during processing and storage of formulations.
Hydroxypropyl betadex inclusion complexes have been reported
to show mechanical properties distinct from the pure materials.
The reported advantage of hydroxypropyl betadex over unsubstituted
b-cyclodextrin is its greater water solubility.
2-Hydroxypropyl-β-cyclodextrin (HBC) is a widely used modified cyclodextrin, the lipophilic cavity formed by 7 glucose units. Drug solubility in water is greatly enhanced by complexing with 2-Hydroxypropyl-β-cyclodextrin.