Effect of Five Alive fruit juice on the dissolution and absorption profiles of ciprofloxacin.
OBJECTIVE
To determine the effect of interaction of five Alive fruit juice on the dissolution and absorption profiles of ciprofloxacin tablets using urinary excretion.


METHODS
In-vitro dissolution of ciprofloxacin 500 mg tablets was studied using US Pharmacopoeia dissolution apparatus II. This was conducted using 0.1N HCl and equal volumes of the fruit juice and 0.1N HCL. Samples were collected at predetermined time intervals for two hours. For the in-vivo study, eleven (5 males and 6 females) healthy volunteers participated in an open, single dose, cross-over randomized trial. After an overnight fasting, each volunteer either ingested a 500 mg ciprofloxacin tablet with 250 ml table water or with the fruit juice. Total urine voided was collected for 72 hrs after each dose of ciprofloxacin. Dissolution and urine samples were assayed using a controlled and validated UV spectrophotometric analysis.


RESULTS
A lag time of 5 minutes was observed in dissolution profile of ciprofloxacin in the juice. The percent dissolved of ciprofloxacin in 0.1NHCl and fruit juice were found to be dissimilar (f2 =18.2) using similarity factor. There was statistical difference between the K(el) (elimination constant), K(e) (excretion rate) and X(u) (cumulative amount excreted unchanged) of subjects on water (0.1759 +/- 0.0144; 12.81 +/- 1.36; 375.5 +/- 41.2) and that of fruit juice (0.1250 +/- 0.0161; 7.6 +/- 1.07; 241.6 +/- 34.0). However, there was no difference between the t(1/2) of the subjects (4.2 +/- 0.3; 5.5 +/- 0.8). There was a decrease in relative availability of the drug by 35.75%.


CONCLUSIONS
We conclude that the absorption of ciprofloxacin can be reduced by concomitant ingestion of the juice containing calcium carbonate and grape. Therefore to avoid drug therapeutic failures and subsequent bacterial resistance as a result of subtherapeutic level of the drug in the systemic circulation, ingestion of the juice with ciprofloxacin should be discouraged.
Akinleye
M O
MO
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, College of Medicine, University of Lagos, Idi-Araba, Lagos, Nigeria.
Coker
H A B
HA
Chukwuani
C M
CM
Adeoye
A W
AW
D000328:Adult; D000890:Anti-Infective Agents / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics*; D001628:Beverages / Q000009:adverse effects*; D001682:Biological Availability; D002119:Calcium Carbonate / Q000009:adverse effects; D002626:Chemistry, Pharmaceutical; D002939:Ciprofloxacin / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics*; D002957:Citrus; D018592:Cross-Over Studies; D016903:Drug Monitoring; D005260:Female; D018565:Food-Drug Interactions; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D016014:Linear Models; D008297:Male; D008657:Metabolic Clearance Rate; D009549:Nigeria; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013607:Tablets; D013997:Time Factors; D027843:Vitis
D000890:Anti-Infective Agents; D013607:Tablets; D002939:Ciprofloxacin; D002119:Calcium Carbonate