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Reversed-phase high-performance liquid chromatography for evaluating the distribution of pharmaceutical substances in
B Dimitrova1, I Doytchinova, M Zlatkova
1Department of Chemistry, Faculty of Pharmacy, Medical University-Sofia, Bulgaria. bdimitrova@mbox.pharmfac.acad.bg
Journal of Pharmaceutical and Biomedical Analysis
|November 30, 2000
Summary
Reversed-phase high-performance liquid chromatography (RP-HPLC) can effectively predict drug distribution in Witepsol H15 suppository bases. This method offers a faster, more reliable alternative to traditional shake-flask experiments for drug formulation development.
Area of Science:
- Pharmaceutical Sciences
- Analytical Chemistry
- Drug Delivery Systems
Background:
- Accurate in vitro assessment of drug distribution in suppository bases is crucial for effective rectal drug delivery.
- Traditional methods like the shake-flask method can be time-consuming and labor-intensive.
- Witepsol H15 is a commonly used suppository base, and understanding drug partitioning is key for formulation.
Purpose of the Study:
- To evaluate the efficacy of reversed-phase high-performance liquid chromatography (RP-HPLC) for determining drug distribution coefficients.
- To compare RP-HPLC method with the classical shake-flask method for drug partitioning between Witepsol H15 and a simulated rectal fluid (phosphate buffer, pH 7.2).
- To establish correlations between RP-HPLC parameters and traditional lipophilicity measures.
Main Methods:
- Drug distribution coefficients (log K) were determined using the shake-flask method for nine model compounds.
- Capacity factors (log k') were measured using RP-HPLC on a C18 column with varying methanol-buffer mobile phases.
- Apparent (log k(w)app) and real (log k'(w)) capacity factors were calculated, alongside CLOGP and CLOGD7.2 for lipophilicity assessment.
Main Results:
- Strong correlations were found between RP-HPLC parameters (log k'(w), log k(w)app) and lipophilicity descriptors (CLOGP, CLOGD7.2).
- A significant correlation between log k(w)app and the shake-flask derived log K was observed, indicating predictive capability.
- The RP-HPLC method demonstrated high stability and reproducibility for assessing drug distribution behavior.
Conclusions:
- RP-HPLC is a potent and reliable analytical technique for the in vitro evaluation of drug distribution in Witepsol H15 suppository bases.
- The log k(w)app parameter derived from RP-HPLC can effectively predict drug partitioning in the Witepsol H15-rectal liquid system.
- RP-HPLC offers a rapid, stable, and reproducible alternative to the conventional shake-flask method, streamlining drug formulation studies.
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