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Lipid Based Formulations in Hard Gelatin and HPMC Capsules: a Physical Compatibility Study
Niklas J Koehl1, Sanket Shah1, Ingrid Djouka Tenekam1
1Drug Product Development, Janssen Research and Development, Johnson & Johnson, Turnhoutseweg 30, 2340, Beerse, Belgium.
Pharmaceutical Research
|August 11, 2021
Summary
Gelatin capsules showed better compatibility with lipid-based formulations than hydroxypropyl methylcellulose (HPMC) capsules. Formulation components significantly influenced capsule compatibility, with water addition improving it for both types.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Lipid-based formulations (LBFs) are crucial for enhancing the solubility and bioavailability of poorly soluble drugs.
- The choice of capsule material is critical for the stability and performance of LBFs.
- Understanding capsule-excipient interactions is essential for successful drug product development.
Purpose of the Study:
- To evaluate the compatibility of hard gelatin and hydroxypropyl methylcellulose (HPMC) capsules with various isotropic lipid-based formulations.
- To identify formulation components that influence capsule compatibility.
- To assess the potential for predicting capsule compatibility based on excipient properties.
Main Methods:
- Investigated 350 systems using five oils, five surfactants, and three cosolvents.
- Assessed capsule compatibility in gelatin and HPMC capsules at 25°C and varying relative humidity (40%, 60%).
- Monitored physical capsule integrity and weight changes post-storage.
Main Results:
- Lipid-based vehicles showed best miscibility with monoglycerides and surfactants (hydrophilic-lipophilic balance <12).
- Gelatin capsules demonstrated superior compatibility compared to HPMC capsules across tested formulations.
- Incorporating water into formulations enhanced capsule compatibility for both gelatin and HPMC types.
- Capsule mass change in binary systems could be partially predicted by excipient proportions.
Conclusions:
- Capsule compatibility is primarily determined by the formulation's excipient composition.
- Gelatin capsules offer broader compatibility with tested lipid-based formulations than HPMC capsules.
- Predictive models based on individual excipient contributions provide a preliminary estimate but require experimental validation.
Keywords:
HPMC capsulesSNEDDScapsule compatibilityhard gelatin capsuleslipid based formulationlipid excipientsliquid filled capsulesoft gel capsulesMore Related Videos
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