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Drug binding and solubility in milk
P E Macheras1, M A Koupparis, S G Antimisiaris
1Department of Pharmacy, University of Athens, Greece.
Pharmaceutical Research
|May 1, 1990
Summary
Drug binding and solubility in bovine milk were studied for seven common medications. Milk fat content and temperature significantly influenced drug binding, enhancing overall drug solubility for improved delivery.
Area of Science:
- Pharmacokinetics and Drug Delivery
- Dairy Science and Food Chemistry
Background:
- Understanding drug behavior in milk is crucial for pediatric and maternal pharmacotherapy.
- Bovine milk composition, particularly fat content, can influence drug disposition.
Purpose of the Study:
- To quantify the binding and solubility of seven model drugs in bovine milk.
- To investigate the impact of temperature and milk fat content on drug-milk interactions.
- To correlate drug physicochemical properties with observed binding and solubility.
Main Methods:
- Determined drug binding and solubility for nitrofurantoin, piroxicam, indomethacin, prednisolone, diazepam, dicumarol, and griseofulvin.
- Utilized bovine milk samples with varying fat content (0.75% and 3.50%) at temperatures of 15, 25, and 37°C.
- Correlated binding and solubility data with drug physicochemical properties (logP, pKa, aqueous solubility).
Main Results:
- Drug binding to milk components was concentration-independent but significantly affected by milk fat content and temperature.
- Most drugs exhibited increased binding with decreased temperatures.
- All tested drugs showed significantly enhanced solubility in milk compared to aqueous buffers.
Conclusions:
- Milk fat content and temperature are critical factors influencing drug binding in bovine milk.
- Enhanced drug solubility in milk is not solely explained by binding to milk components.
- Findings have implications for formulating and delivering drugs intended for administration with milk.