Approximately 60% of potential active pharmaceutical ingredients (APIs) under development, and more than 40% of those in reformulation, are poorly water soluble. Excipients offer the most versatile approach to solving these solubility challenges and have long played a key role in allowing poorly soluble APIs to be formulated into products with improved bioavailability and therapeutic effects. However, as the number of poorly soluble APIs grows, existing excipients are still not able to solve all of the complex formulation challenges.
Apisolex™, the injectable-grade excipient is a safe, GMP-validated, polyamino acid-based polymer that enhances the solubility of BCS Class II and IV APIs by 50,000-fold.
Apisolex technology has been designed to work with straight forward formulation techniques, helping you to streamline your manufacturing and saving precious time during drug development. Solubilized excipient and API can be mixed in an aqueous based solution followed by sterile filtration and lyophilization to produce a stable formulation that is readily resuspended in common diluents for administration. This technique forms micellar structures which encapsulate the API during lyophilization. In saline, the lyophilized drug product reconstitutes in less than 30 seconds.
| Test | Results | |
|---|---|---|
| Systemic toxicity | Tolerability (rats and mice) | Well tolerated at doses as high as 1,500 mg/kg |
| 32-day IV injection 28-day recovery (rats) | No treatment-related side effects detected | |
| Pharmacokinetics | [14C] labelled Apisolex IV dose in male and female rats | - Can be distributed to distant organs without accumulation - Tissue: plasma AUC0-t ratios <1.0 |
Made under GMP conditions, Apisolex excipient is constituted of amino acid building blocks. It’s biocompatible, biodegradable and tested for safety in parenteral projects.
The solubilization properties of Apisolex polymer were evaluated in comparison with other excipients using a series of ten (10) poorly water soluble active pharmaceutical ingredients – some common and some from Boehringer Ingelheim’s opnMe program. We set the success criteria to show that even at a low bar many traditional excipients do not hit the mark. See how Apisolex polymer fared in comparison to your favorite go-to excipient.
Discover how our excipient can help meet the solubilization needs for your most challenging parenteral projects.
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