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We join the fight against COVID-19 by offering SBE-β-CD: the critical excipient that improves the efficacy of remdesivir

May 21, 2020
Solubility

The critical role of sulfobutyl ether β-cyclodextrin sodium (SBE-β-CD) in the efficacy of remdesivir

Currently the medical community turns its attention to SBE-β-CD-enabled remdesivir, a broad-spectrum antiviral medication that promises a faster recover from COVID-19.

Remdesivir finished product contains the excipients sulfobutyl ether β-cyclodextrin sodium (SBE-β-CD), hydrochloric acid and/or sodium hydroxide.

Sulfobutyl ether β-cyclodextrin sodium (SBE-β-CD) is a cyclodextrin excipient used as a solubility and stability enhancer in numerous drug formulations. Remdesivir is practically insoluble in water and studies have shown that the use of SBE-β-CD in its formulation will significantly improve its solubility. The enhanced absorption rate and bioavailability of the drug will lead to the successful exert of its effect that will effectively fight the virus.

Advantages of cyclodextrins 

Cyclodextrins (CDs) are oligosaccharides used as complexing agents to increase the water solubility of lipophilic compounds and bioavailability of medicinal products.

Due to their cyclic structure, cyclodextrins can form inclusion complexes when they interact with hydrophobic drug substances; as a result, they demonstrate higher aqueous solubility than that of comparable acyclic saccharides.

The mechanism for the increased solubility of cyclodextrins is rooted in their ability to form non-covalent dynamic inclusion complexes in solution. High solubility can lead to high dissolution rates and greater oral bioavailability and stability of biopharmaceuticals with high or low permeability and low solubility, BCS Class II and IV drug substances.

Cyclodextrins can also lower the free concentration of the drug and therefore significantly affect the pharmacokinetics and pharmacodynamics of the active substance.

In addition, cyclodextrins can reduce or prevent gastrointestinal and ocular irritation, reduce or eliminate unpleasant smells or tastes, prevent pre-systemic drug-drug or drug-additive interactions within a formulation or help to convert oils and liquid drugs into microcrystalline or amorphous powders.

What we offer

With the unexpected COVID-19 situation, the pharmaceutical industry is working globally to combat the pandemic. With the current medical attention on remdesivir the world demand in SBE-β-CD, the excipient that can enable its therapeutic effect, has increased significantly.

We join the fight by maximizing our manufacturing efforts in producing SBE-β-CD, an excipient, designed to further safety, improve the solubility, stability, and bioavailability of the drug.

Examples of API formulations containing SBE-β-CD, currently on the market: Remdesivir, Carfilzomib, Voriconazole, Ziprasidone maleate, Posaconazole, Itraconazole and Maropitant (veterinary drug).

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