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Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Sitagliptin Phosphate Monohydrate
Naseem A Charoo1, Daud B Abdallah2, Ahmed Abdalla Bakheit2
1Succor Pharma Solutions, Dubai Science Park, Dubai, United Arab Emirates.
Journal of Pharmaceutical Sciences
|October 1, 2021
Summary
Sitagliptin, a type 2 diabetes medication, can use Biopharmaceutics Classification System (BCS) methods for bioequivalence assessment. This allows for biowaivers for solid oral forms, avoiding human pharmacokinetic studies.
Area of Science:
- Pharmaceutical Sciences
- Drug Regulatory Affairs
Background:
- Sitagliptin is a key antihyperglycemic agent for Type 2 Diabetes.
- Current bioequivalence assessment for solid oral dosage forms often requires pharmacokinetic studies in human volunteers.
Purpose of the Study:
- To evaluate the suitability of Biopharmaceutics Classification System (BCS)-based biowaivers for sitagliptin phosphate monohydrate solid immediate-release (IR) oral dosage forms.
- To determine if BCS classification can replace in vivo pharmacokinetic studies for assessing bioequivalence.
Main Methods:
- Comprehensive review of sitagliptin's solubility, permeability, dissolution, and pharmacokinetic properties.
- Assessment of therapeutic index, drug-excipient interactions, and existing bioequivalence data.
- Application of BCS criteria to classify sitagliptin's drug substance.
Main Results:
- Sitagliptin meets the criteria for BCS Class 1, indicating high solubility and high permeability.
- The drug possesses a broad therapeutic index with minimal risks from dose variations.
- Existing data supports the classification of sitagliptin as BCS Class 1.
Conclusions:
- A BCS-based biowaiver is feasible for sitagliptin phosphate monohydrate solid IR oral products.
- Implementation requires adherence to specific excipient, data collection, and dissolution testing guidelines.
- This approach offers an alternative to in vivo bioequivalence studies, streamlining drug product approval.
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