128446-35-5/2-Hydroxypropyl-β-cyclodextrin

Chemical Properties

White to slightly yellow powder

Uses

2-Hydroxypropyl-β-cyclodextrin (HPβCD) is a modified cyclodextrin that serves as an excipient in pharmaceutical and biomedical applications. HPβCD is widely used in the pharmaceutical industry to enhance the solubility of poorly water-soluble drugs. HPβCD is commonly employed as a substitute for other types of cyclodextrins, including alpha-cyclodextrin, beta-cyclodextrin, and gamma-cyclodextrin, due to its improved properties.

Production Methods

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.

General Description

2-Hydroxypropyl-β-cyclodextrin (HPβCD) is a versatile excipient with applications in drug solubilization, drug delivery, stability improvement, and potential treatments for certain medical conditions. It plays a crucial role in improving the bioavailability and effectiveness of various drugs. HPβCD is approved by the Food and Drug Administration (FDA) and other regulatory authorities for use as an excipient in pharmaceutical formulations.

Pharmaceutical Applications

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.

Safety

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.

storage

Store in well-closed containers.

Regulatory Status

Included in oral and parenteral medicinal products. Included in an injectable preparation licensed in the UK for intramuscular or intravenous administration.