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Captisol – Cyclodextrin

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The leading sulfobutylether beta-cyclodextrin (SBECD)

Captisol is a derivatized beta cyclodextrin used in 16 FDA-approved products to date, including VEKLURY® (remdesivir) and KYPROLIS® (carfilzomib) to help solubilize & stabilize difficult to deliver molecules. Made by CyDex Pharmaceuticals (a Ligand Company), Captisol is the leading pharmaceutical-grade sulfobutylether beta-cyclodextrin (SBECD), with an excellent record of safety and consistency.

Captisol has been used in therapeutics across many routes of administration, including parenteral, oral, subcutaneous, ophthalmic, nasal, inhalation, and dermal. It is prepared by an all-aqueous process and distributed world-wide.

Captisol® Solubilizes

What is Captisol?

By significantly improving the solubility, stability, and therefore bioavailability of insoluble active pharmaceutical ingredients (APIs), Captisol is an ideal excipient for difficult to formulate compounds. Partners have successfully used Captisol to overcome formulation issues to enable commercially successful products for the past twenty years, with additional approvals on the near horizon.


Captisol® Solubilizes

Neutral, cationic and anionic APIs have been effectively associated with Captisol®. Aqueous solubilities have increased by a factor of 10 to 25,000, depending on the compound. In contrast to other solubilization technologies, product or traditional formulation system, the feasibility and solubility effectiveness of Captisol® can be rapidly assessed with a few simple lab experiments.

Captisol® Facilitates Delivery

Typically, the inherent pharmacokinetics and pharmacodynamics of the drug are unaffected by Captisol®, however onset may be manipulated and dose sparing maybe observed compared to classical formulations such as co-solvent based, emulsions or suspensions. Upon administration, Captisol® is readily and essentially completely renally eliminated. Captisol® formulations are biocompatible and can be administered parenterally, orally, ophthalmically, nasally, topically and via inhalation.

News on Captisol

Captisol® is Safe

Captisol is eliminated by glomerular filtration in the kidneys. Two decades of patient experience and recent data have shown that Captisol is safe, even in patients with severe renal impairment. Clinical studies were performed in renally compromised patients on BAXDELA (a Captisol-enabled product). Conclusions from these studies stated that “Increased SBECD exposures did not result in any noticeable increase in drug-related TEAEs in this study.” And “… decreasing renal function causes reduced SBECD (Captisol) clearance and increased exposures, but SBECD continues to exhibit a good safety and tolerability profile in IV formulations.”

In another Captisol-enabled drug product, Gilead performed clinical safety studies for VEKLURY in patients with moderately and severely reduced kidney function. The results of the study were favorable and in August 2023 the package insert for Veklury was changed to state that “No dosage adjustment of VEKLURY is recommended for patients with any degree of renal impairment, including those on dialysis...”

Read Gilead Article

Captisol® Stabilizes

Interaction with Captisol® provides a beneficial and protected environment for the API in its lipophilic cavity, while Captisol’s hydrophilic surface provides excellent water solubility- boosting both solubility and stability. Interaction of the API with Captisol® can reduce decomposition by protecting labile regions from the potential reactants in the aqueous environment.


Captisol® Facilitates Faster Development

Using Captisol® early in the development process can increase the number of candidates that can be evaluated, decrease development time and increase lead candidate survivability. Captisol® enables an aqueous formulation for many water insoluble APIs as oral, nasal, topical, ophthalmic or liquid-presented medications.

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The Captisol® Advantage

  • Improved Stability
  • Allows formulation of water-insoluble APIs in all dosage forms, including oral, injectables, ophthalmic, nasal, topical and inhalation products

Attributes

  • Tastelessness in oral formulas (taste masking in oral, nasal and Inhalation preperations)
  • Reduction of Irritation at site of injection in injectable formulas (parenteral)

Rapid Onset

  • Potential to enable faster acting versions of many currently approved oral products

Manufacturing

  • cGMP manufacturing via a validated process
  • Multi-metric ton Commercial scale
  • Well-defined impurtiy profile and long-term stability

Enables high Levels of API to reach dosing Targets

  • Improved Stability
  • Interaction with Captisol shelter the API from oxidative and hydrolytic degradation
  • Protects against effects from Elements such as heat and light

Improved Bioavailability and Delivery Efficiency

  • Better bioavailability than Methods of solubulization using nanoparticles and solvent systems
  • Permits lower dosing of APIs (i.e. potential for dose sparing)

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Contact

Captisol, brought to you by Ligand Pharmaceuticals

2033 Becker Drive, Suite 310

Lawrence, KS 66047

Jessica Beach

Assoc. Director Customer Support

P: 858-550-5632

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Captisol

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