Gilead’s Captisol-enabled Remdesivir Approved for Use in Renally Impaired Patients
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Captisol is not only in approved products worldwide, it is also used as a solubilization tool for early non-clinical formulations. Using Captisol early in the development process can decrease development time and enable the preparation of aqueous formulations for many water insoluble API’s by many routes of administration including but not limited to nasal, inhalation, oral, parenteral, intravitreal, and ophthalmic. Aqueous formulations with Captisol may be simpler and less toxic than the use of organic solvents, surfactants, and extreme pH conditions to achieve desired dosages. Contact the Captisol Team for guidance on the extensive safety studies previously performed with Captisol.

Captisol has been shown to increase water solubility by a factor of 10 to 150,000 depending on the compound structure. The extent of solubilization observed is related to the concentration of CAPTISOL®, the strength of the complex and the pH effects on the extent of drug ionization.

Stability of drugs in aqueous solution may be markedly improved on complexation with CAPTISOL®. Enclosure of the labile area of the drug in the cyclodextrin cavity or interaction with the SBE substituent can serve to reduce the rate of decomposition by ‘hiding’ the reactive center. Some protein and peptide formulations can be stabilized by minimizing aggregation, preventing adsorption to containers, and aiding in refolding. Studies show that the presence of CAPTISOL® decreases the aggregation of insulin and doubles subcutaneous bioavailability to 96%.

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The following table lists some examples of approved products and the formulation challenges that were overcome with the addition of Captisol to the drug product:

Product Table