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Dosage forms of cyclosporine
1Department of Pharmacy Practice, College of Pharmacy, University of Florida, Gainesville.
Pharmacotherapy
|January 1, 1991
Summary
Cyclosporine, a vital immunosuppressant, is formulated with ethoxylated plant fats and ethanol due to its poor water solubility. These excipients enhance the bioavailability of both intravenous and oral cyclosporine dosage forms.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Biochemistry
Background:
- Cyclosporine is a critical immunosuppressive agent used in organ transplantation and autoimmune diseases.
- Its therapeutic efficacy is significantly limited by poor aqueous solubility.
- Conventional formulations face challenges in achieving adequate bioavailability.
Purpose of the Study:
- To describe the formulation strategies for commercially available cyclosporine dosage forms.
- To highlight the role of excipients in overcoming solubility challenges.
- To explain the rationale behind the inclusion of specific solubilizing agents.
Main Methods:
- Analysis of excipient composition in marketed cyclosporine solutions and soft gelatin capsules.
- Review of physicochemical properties influencing drug absorption.
- Examination of formulation techniques for poorly soluble drugs.
Main Results:
- Commercially available cyclosporine formulations utilize ethoxylated plant fats and ethanol as key excipients.
- These excipients are crucial for enhancing the solubility and subsequent absorption of cyclosporine.
- Both intravenous and oral dosage forms incorporate these agents to ensure therapeutic drug levels.
Conclusions:
- The formulation of cyclosporine relies heavily on specific excipients to manage its poor water solubility.
- Ethoxylated plant fats and ethanol are essential components for achieving adequate bioavailability in clinical use.
- Understanding these formulation aspects is key for optimizing cyclosporine therapy.