Introduction: Although Nigerian herbal practitioners have shown some improvements in the standardization of doses and dosages, many herbal supplements have poor toxicological assessment to ensure human safety. A toxicological assessment of B-Success herbal supplement commonly used in Nigeria was carried out on liver, heart and kidney of adult albino rats. Method: Twenty albino rats divided into four groups of five rats each were used. Twenty male rats were divided into four dose groups of five rats each namely 0.00, 315,630, 945mg/kg/day (representing 0, 25, 50 and 75% of the LD50 of B-Success herbal supplement) orally for 90 days. Animals had access to deionized water and were fed ad libitum with rat chow for 90 days. The feed and fluid consumption of the animals were measured on daily basis while the body weight was measured weekly. Animals were anaesthetized after 90 days, bled and bilirubin, creatinine, high density lipoprotein cholesterol (HDL),low density lipoprotein (LDL), alanin transaminase (ALT), and aspartate transaminase (AST) were measured.Result: The alanin transaminase (ALT), aspartate transaminase (AST) and urea of 630, 945 mg/kg/day dose groups were significantly increased compared to control. While only the creatinine value of 945mg/kg/day dose group was significantly increased compared to control p 0.05) the bilirubin levels compared to control. The total cholesterol, high density lipoprotein (HDL) cholesterol of all the B-Success treated groups were significantly increased p<0.05 compared to control. The low density lipoprotein (LDL) cholesterol values of 630, 945mg/kg/day groups were significantly decreased p<0.05 compared to control.Conclusion: Taken together B-Success may be toxic to liver and kidney and protective to heart in albino rats at the doses studied.
To investigate the effect of the ciprofloxacin on the urinary excretion of the rifampicin in humans, ciprofloxacin and rifampicin were coadministered. Five healthy volunteers between the ages of 20 and 35 years received, on 2 separate occasions (phases 1 and 2) and at weekly intervals, 600 mg rifampicin and 600 mg plus 500 mg ciprofloxacin, respectively, with 350 mL of water. Urinary levels of rifampicin were measured from 1–72 hours later. In phase 1, 15.6% urinary rifampicin was recovered compared with 15.5% urinary rifampicin recovered in the second phase. An increased excretion rate and higher plateau were obtained in ciprofloxacin plus rifampicin treatment. The study indicates that rifampicin may be coadministered with ciprofloxacin to check the development of drug resistance to single-drug therapy by susceptible organisms.
The effect of pefloxacin on the pharmacokinetics parameters of rifampicin in humans was investigated using plasma and saliva concentrations. Five healthy volunteers (4 male and 1 female), ages 20-35 years, each received 600 mg rifampicin alone, and after a 1-week drug washout period, 600 mg rifampicin plus 500 mg pefloxacin was administered with 350 mL of water. Plasma and saliva concentrations of rifampicin were measured at 7 different time intervals and different pharmacokinetics parameters calculated. Pefloxacin coadministered with rifampicin reduced plasma and saliva elimination half-life, peak plasma concentration, area under the concentration time curve, volume of distribution, minimum absorption time, absorption rate constant, and absorption half-life showed a significant increase (P < 0.05). Time to reach peak plasma concentration was not affected with or without pefloxacin. Pefloxacin increases bioavailability of rifampicin and hence extends its detection in the body as demonstrated by rifampicin being estimated at 24 hours when coadministered with pefloxacin, whereas at 24 hours, it was completely absent when administered alone.
The effect of pefloxacin on the urinary excretion of rifampicin was investigated in 5 healthy volunteers between the ages of 20 and 35 years. The investigation was carried out in 2 different phases, with a 1-week drug washout separating the phases. Each subject received 600 mg rifampicin with 350 mL of water. After 1 week, the subjects were given 600 mg rifampicin plus 500 mg pefloxacin with 350 mL of water. Urinary levels of rifampicin were measured spectrophotometrically for the 2 phases from 0 to 72 hours. Coadministration of rifampicin with pefloxacin led to 20.1% urinary recovery of rifampicin. The increased rifampicin excretion rate following pefloxacin coadministration is supported by the competitive liver clearance between rifampicin and pefloxacin, which favors pefloxacin and causes rifampicin secretion, thus increasing its elimination through the kidney. Pefloxacin increases the absorption and urinary excretion of rifampicin by decreasing the gastrointestinal motility through chelation mechanisms.
Salivary and urinary excretion and plasma-saliva concentration ratios of isoniazid (INH) in the absence and presence of ciprofloxacin (CP) were investigated in healthy female volunteers. Results obtained indicated an absorption form of interaction between INH and CP. This led to delay in gastric emptying and onset of absorption of INH in the upper part of the gastrointestinal tract, resulting in a corresponding delay in the onset of salivary and urinary excretion of the drugs. There was a 1-hour reduction in the time to attain peak saliva concentration of INH (tmax), an insignificant difference in peak saliva concentration (Cmax), and a significant (P = 0.05) increase in AUC(0-24h) of INH in the presence of CP. Cumulative amount of INH excreted in the urine increased approximately 38% in the presence of CP. The calculated plasma-saliva concentration ratios of INH were reduced in the presence of CP and were slightly lower than the experimental values. This indicates increased amount of the drug secreted into saliva in the presence of CP and possible buccal partitioning of the drug. Overall, results of the current study indicate that CP delayed the onset but not the extent of INH absorption. Therefore, concurrent administration of the two drugs was considered relatively safe, and the absorption interaction that may have occurred may not be of reasonable clinical consequence.
The effect of magnesium sulphate and sodium sulphate on the in vitro adsorption of rifampicin to activated charcoal (AC) was investigated. Solutions of rifampicin alone and rifampicin with 7.5 mg/ml cathartic solution were vortex mixed for 30 s with different quantities of AC, incubated for 30 min at 37o and analyzed for free rifampicin spectrophotometrically at 320 nm. Addition of sodium and magnesium sulphates significantly increased (P<0.05) the adsorption of rifampicin to activated charcoal. In all, the adsorption obeyed quantity-dependent kinetics.
The effect of saline cathartics magnesium sulphate, sodium sulphate, and sodium citrate on adsorptive capacity of activated charcoal (AC) was investigated in vitro. Solutions of artesunate alone and artesunate with 7.5 mg/ml cathartics solution were vortex mixed for 30 sec with different quantities of AC, incubated in water bath shaker for 30 min at 37°C and analysed for free artesunate spectrophotometrically at 328 nm. Addition of the cathartics caused a significant increase (p < 0.05) in the adsorption of artesunate to activated charcoal. The descending order of increased adsorption by the cathartics is magnesium sulphate, sodium citrate and sodium sulphate.