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Physical characterization of two oxyphenbutazone pseudopolymorphs
M Stoltz1, A P Lötter, J G Van der Watt
1College of Pharmacy, University of Pretoria, Brooklyn, Pretoria, South Africa.
Journal of Pharmaceutical Sciences
|December 1, 1988
Summary
New pseudopolymorphic forms of oxyphenbutazone, a benzene solvate and a cyclohexane solvate, exhibit superior dissolution rates compared to previously reported forms. These findings offer potential improvements for drug formulation and bioavailability.
Area of Science:
- Pharmaceutical Sciences
- Solid-State Chemistry
Background:
- Oxyphenbutazone exists in various polymorphic and solvate forms.
- Understanding these solid forms is crucial for drug development and bioavailability.
Purpose of the Study:
- To prepare and characterize new pseudopolymorphic forms of oxyphenbutazone.
- To evaluate the dissolution rates of these novel forms.
Main Methods:
- Recrystallization from benzene and cyclohexane.
- Characterization using DSC, TGA, IR, XRPD, and thermomicroscopy.
- Assessment of powder and intrinsic dissolution rates.
Main Results:
- Successful preparation of a benzene solvate (Solvate B) and a cyclohexane solvate (Solvate C).
- Characterization confirmed the distinct pseudopolymorphic nature of Solvates B and C.
- Both pseudopolymorphs demonstrated significantly higher dissolution rates than anhydrate, hemihydrate, and monohydrate forms.
Conclusions:
- The benzene and cyclohexane solvates of oxyphenbutazone represent novel pseudopolymorphic forms.
- These pseudopolymorphs offer enhanced dissolution properties, potentially improving oxyphenbutazone's therapeutic efficacy.