Oral pharmacokinetics of the acidic drugs, diclofenac and sulfamonomethoxine in male Shiba goats
نویسندگان
چکیده
In the present study, we examined the oral pharmacokinetics of the acidic drugs, diclofenac (DF) and sulfamonomethoxine (SMM), which have different physicochemical properties, in Shiba goats. DF and SMM were intravenously and orally administered to 5 male goats using a crossover design. The T(max) of DF and SMM were reached 1.5 and 5.6 hr after they have been orally administered, respectively, and this was followed by their slow elimination. The elimination of both drugs was markedly faster after being intravenously rather than orally administered, which indicated flip-flop phenomena after the oral administration. The mean absorption times (MATs) of DF and SMM were 6 and 15 hr, respectively. This slow absorption may have been due to slow gastric emptying in goats. The large difference observed in MATs between DF and SMM may have been because DF, which is more lipophilic than SMM, was partly absorbed from the forestomach. Therefore, these results suggest that the absorption of highly lipophilic drugs from the forestomach may be markedly high in Shiba goats. In case of drugs whose elimination is quite fast, their efficacies may appear from the early stage after oral administration even in ruminants, because elimination rate is the determinant factor of T(max) in flip-flop phenomena. Such drugs may be used orally even in ruminants.
منابع مشابه
Oral absorption profiles of sulfonamides in Shiba goats: a comparison among sulfadimidine, sulfadiazine and sulfanilamide
The oral pharmacokinetics of three sulfonamides, sulfadimidine (pKa 7.5), sulfadiazine (pKa 6.5) and sulfanilamide (pKa 10.5), with different rates of unionization in rumen juice, were compared in Shiba goats to clarify the relationship between drug absorption profiles after their oral administration as well as their degree of unionization in the rumen. Sulfonamides were administered either int...
متن کاملOral pharmacokinetics of acetaminophen to evaluate gastric emptying profiles of Shiba goats
The pharmacokinetics of acetaminophen was investigated following oral dosing to Shiba goats in order to evaluate the properties of gastric emptying. Acetaminophen was intravenously and orally administered at 30 mg/kg body weight to goats using a crossover design with a 3-week washout period. The stability of acetaminophen in rumen juice was also assessed. Acetaminophen concentrations were measu...
متن کاملThe Pharmacokinetics of Rafoxanide following Single Dose Intravenous and Oral Administration in Goats
The study was conducted to determine the plasma concentrations and pharmacokinetic parameters of rafoxanide after a single intravenous (10 mg/kg) and oral (22.5 mg/kg) administrations in black Bengal female goats. Maximum (87.63 11.71 mg/mL) and minimum (1.8 0.24 mg/mL) plasma concentrations of rafoxanide were recorded at 0.08 and 12 h respectively after i.v. administration. The elimination h...
متن کاملEffects of CYP2C9*3 and CYP2C9*13 on Diclofenac Metabolism and Inhibition-based Drug-Drug Interactions.
Cytochrome P450 2C9 (CYP2C9) is a polymorphic enzyme responsible for the metabolism of many important drugs, including diclofenac. CYP2C9*3 and CYP2C9*13 are the principal variant alleles found in the Chinese population. CYP2C9*3 has been reported to reduce the metabolism of diclofenac and alter the extent of drug-drug interactions (DDIs). The effects of CYP2C9*13 on diclofenac metabolism are n...
متن کاملPharmacokinetics of Ecofriendly Meloxicam in Healthy Goats
Diclofenac Sodium, a Non-steroidal anti-Inflammatory drug (NSAID) was banned for veterinary use in Pakistan, India and Nepal in 2005-06 due to its relay toxicity associated with catastrophic decline in the populations of vulture in South Asia. The main aim of the present research was to study pharmacokinetics of meloxicam in goats under local conditions. Meloxicam is another NSAID, reported as ...
متن کامل