Stability of APIs in Super Refined Oils - Maximise the Performance of Your Active Pharmaceutical Ingredients

Discover the Benefits of Super Refined Excipients

Excipient choice can make all the difference in successful formulation development. The selection of pharmaceutical excipients in a drug formulation can have a significant impact on development timescales, Active Pharmaceutical Ingredient (API) integrity and product stability. These in turn negatively impact upon the time to market, storage conditions, shelf life, efficacy and product safety.

Croda’s range of Super Refined™ excipients has been specially developed to optimise API stability and improve the performance of pharmaceutical formulations. Super Refined materials demonstrate clear benefits, adding real value to the drug development process.

Benefits of Super Refined Excipients

Enhanced API and formulation stability
Fewer formulation degradation products
Minimised analytical complexity
Simplified formulations
Reduced resource, time and development costs
Improved chance of formulation success
Multi-compendial – NF, PhEur, JPE

The following case studies with ritonavir and haloperidol decanoate demonstrate the importance of excipient selection in formulation development.

Case Study: Ritonavir Stability in Oleic Acid

Ritonavir (Figure 1) is a water-insoluble drug for the treatment of HIV/AIDS. It is used either alone or in combination with lopinavir in a range of tablet, liquid and capsule formats. The soft gel capsule product is formulated with oleic acid. Ritonavir has been shown to be unstable in a range of standard compendial excipients.

This case study investigates the stability of ritonavir in Super Refined and standard compendial grade oleic acid to determine the effect of excipient purity on API degradation.

API recovery

The results for ritonavir recovery at 40ºC in oleic acid are
shown in Figure 2. In standard compendial grade oleic acid the API recovery rate after 12 weeks was 24%. In contrast, the recovery rate in Super Refined Oleic Acid was more than double that at 55%. This demonstrates that the stability of ritonavir in Super Refined Oleic Acid is substantially higher than in the corresponding standard compendial grade excipient.

Stability of APIs in Super Refined Oils_Figure 2

API degradation

Ritonavir appears in the chromatogram as a single peak at a retention time of 4.8 minutes (Figure 3). In standard compendial grade oleic acid, numerous additional peaks are observed, indicating extensive API degradation. In Super Refined Oleic Acid, fewer, smaller peaks are seen, confirming the increased stability of ritonavir in comparison with that in the standard compendial grade excipient.

Stability of APIs in Super Refined Oils_Figure 3

Key Findings

The stability of ritonavir is enhanced in Super Refined Oleic Acid in comparison with that in standard compendial grade oleic acid
Formulation in Super Refined Oleic Acid results in fewer degradation products than are seen in a standard compendial grade product

Excipient choice can make all the difference in formulation development.

Case Study: Haloperidol Decanoate Stability in Sesame Oil

Haloperidol decanoate (Figure 4) is an antipsychotic drug used in the treatment of schizophrenia. It is administered by
intramuscular injection as an extended release formulation in sesame oil.

See the full brochure “Maximise the Performance of Your Active Pharmaceutical Ingredients” by Croda´s Stability of APIs in Super Refined Oils here

(click the picture to download the brochure)

Source: Croda brochure “Maximise the Performance of Your Active Pharmaceutical Ingredients”

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