Betadex Sulfobutyl Ether Sodium

Category

Biocompatibility enhancers; Chelating Agentss; Dissolution enhancers; Penetrants; Solubilizers; Stabilizers; Diluents; Viscosifiers; Water activity reducers

Molecular Formula

C42H70-nO35(C4H8SO3Na)n

Molecular Weight

1134+158n

Grade

Pharmceutical Excipients

UNII

2PP9364507

Chemical Name

β-Cyclodextrin sulfobutylether, sodium salt

CAS Number

182410-00-0

Synonyms

Sulfobutyl Ether Beta Cyclodextrin Sodium

Administration route

Intramuscular injection; Intravenous injection; subcutaneous

Stability and Storage Conditions

This product is stable in the solid state, should avoid high humidity, stored in an airtight container, in a cool dry place. It will reversibly absorb moisture at up to 60% RH without affecting the appearance of the material. Breaking the balance at RH above 60% will cause deliquescent. Once in this state, the material needs to be dried, but a glassy product will be obtained. This water-absorbing behavior is typical of amorphous hygroscopic materials. This product is stable in aqueous solutions greater than about pH 1.

Commonly used amount and the maximum amount

This product can be used as an penetrant and/or solubilizer for controlled release administration and has antibacterial and anticorrosive properties when the concentration is sufficient. The dosage of this product depends on its role in the formulation, the route of administration, and the ability of the cyclodextrin to combine with the drug being delivered. In general, the minimum amount required for solubilization is a cyclodextrin/drug molar ratio of about 1 to 5 (the exact ratio is determined by the test based on the complexation data). The maximum dosage in the formulation may be subject to physical and chemical limitations such as viscosity (for example, the concentration for injection can be as high as 50% w/v), tension, or the total weight and size of the solid dosage form (for example, less than 1g per tablet). It may also be subject to pharmacokinetic/pharmacodynamic (PK/PD) constraints. Dilution of preparations containing cyclodextrins can lead to an increase in the amount of the uncompounded drug, so it is not diluted when administered, such as ophthalmic preparations that are sensitive to cyclodextrin concentrations. In these preparations that are sensitive to the concentration of cyclodextrin, a concentration greater than the minimum required for drug solubility can reduce the appearance of non-complex drugs, thereby producing PK/PD intended effects such as slower onset, lower Cmax, and bioavailability.

Source and Preparation

The product was prepared by alkylation reaction with 1, 4-butane sulfone as raw material and cyclodextrin as raw material under alkaline conditions. The degree of substitution is controlled by the stoichiometric ratio of β-cyclodextrin to sulfonolactone used in the process.

Safety

This product is derived from β-cyclodextrin, which has renal toxicity when administered parenterally. However, studies have shown that this product is well tolerated at high doses when administered by intravenous push, orally, and by inhalation. In approved voriconazole formulations, intravenous infusion can reach a dose of 9g per day. The safety of this product after intravenous administration is under continuous study. This product has undergone a series of in vitro and in vivo genotoxicity and pharmacological evaluations. No genotoxic or mutagenic changes were observed. This product is biocompatible and has no pharmacological activity. It is quickly eliminated when given intravenously.

Incompatibilities

This product reduces the antiseptic activity of benzalkonium chloride.