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Rate-controlled absorption enhancement of rectally administered cefazolin in rats by a glyceride mixture (MGK)
E J van Hoogdalem1, A M Stijnen, A G de Boer
1Center for Bio-Pharmaceutical Sciences, Sylvius Laboratories, State University of Leiden, The Netherlands.
Abstract:
The enhancing effect of the medium chain glyceride preparation MGK on the rectal absorption of the cephalosporin antibiotic cefazolin sodium was evaluated in relation to the rate of delivery. Cefazolin sodium proved to be absorbed to a small extent (15 to 27%) after rectal administration without MGK. Bolus administration with MGK enhanced rate and extent of cefazolin sodium absorption, resulting in a bioavailability of 57 +/- 26%. Linear infusion of 3 mg cefazolin sodium with MGK in 32 min produced complete absorption of the antibiotic (102 +/- 7%), but absorption occurred slower in comparison with bolus delivery. The rate of administration proved to be an important variable of the absorption enhancing effect of MGK.
Insights
The medium chain glyceride preparation MGK significantly enhances rectal absorption of cefazolin sodium. Bolus delivery with MGK improved bioavailability, while linear infusion achieved complete absorption, highlighting the importance of administration rate.
Area of Science:
- Pharmacology
- Drug Delivery Systems
Background:
- Rectal administration offers an alternative route for drug delivery.
- Enhancing the absorption of antibiotics like cefazolin sodium is crucial for effective treatment.
Purpose of the Study:
- To evaluate the effect of medium chain glyceride preparation MGK on rectal absorption of cefazolin sodium.
- To determine the influence of administration rate on MGK's absorption-enhancing effect.
Main Methods:
- Rectal administration of cefazolin sodium with and without MGK.
- Comparison of bolus delivery versus linear infusion of cefazolin sodium with MGK.
- Assessment of cefazolin sodium bioavailability and absorption extent.
Main Results:
- Rectal absorption of cefazolin sodium without MGK was limited (15-27%).
- Bolus administration with MGK increased bioavailability to 57 +/- 26%.
- Linear infusion of cefazolin sodium with MGK resulted in complete absorption (102 +/- 7%) but at a slower rate.
Conclusions:
- MGK significantly enhances the rectal absorption of cefazolin sodium.
- The rate of administration is a critical factor influencing MGK's absorption-enhancing efficacy.
- Optimizing administration rate can lead to complete rectal absorption of cefazolin sodium.