Topic:Bioavailability
Bioavailability in horses refers to the proportion of a nutrient or drug that enters the systemic circulation when introduced into the body and is thus available for use or storage. It is a key factor in determining the efficacy of nutritional supplements and medications administered to horses. Factors influencing bioavailability include the method of administration, the horse's digestive physiology, and the chemical properties of the substance. Understanding bioavailability is essential for optimizing dosing regimens and ensuring effective treatment outcomes. This page gathers peer-reviewed research studies and scholarly articles that explore the mechanisms, influencing factors, and implications of bioavailability in equine nutrition and pharmacology.
Dexamethasone and prednisolone in the horse: pharmacokinetics and action on the adrenal gland. Pharmacokinetics of dexamethasone and prednisolone were studied in 6 horses given dexamethasone alcohol (IV or IM) or dexamethasone 21-isonicotinate as a solution IV or IM (50 micrograms/kg of body weight), prednisolone 21-sodium succinate IV or IM (0.6 mg/kg of body weight), or prednisolone acetate IM (0.6 mg/kg of body weight). Plasma concentrations were determined using a high-performance liquid chromatographic method. After dexamethasone alcohol (IV) or dexamethasone 21-isonicotinate (IV), the half-life of elimination was similar (53 minutes) for both formulations. After dexamethasone (alc...
Pharmacokinetics of ascorbic acid in horses. The pharmacokinetics of ascorbic acid were studied in 29 horses after intravenous (iv), subcutaneous, intramuscular (im) and oral administration. Following iv injection of 5 and 10 g ascorbic acid, respectively, a biphasic decline of ascorbic acid serum levels was found, indicating that the vitamin distributes in the body according to a two-compartment open model. The apparent volume of distribution (average value for Vd(ss) = 0.6 litre/kg) was approximately equivalent to the volume of total body water. The terminal half-life of the biexponential serum level-time curve (t1/2 beta) varied betwe...
Phenylbutazone kinetics and metabolite concentrations in the horse after five days of administration. Phenylbutazone (PBZ) was administered (8.8 mg/kg of body weight) every 24 hours for 5 consecutive days, orally for the first 4 days and IV on day 5. The half-life (t 1/2) after this daily administration was 6.2 hours and the volume of distribution was 0.152 +/- 0.014 L/kg; the bioavailability after oral administration was 91.8 +/- 2.5%. The plasma concentration of PBZ at experimental hour (EH) 24 (24 hours after the 1st oral dose) was 1.7 +/- 0.39 micrograms/ml and increased to 4.2 +/- 0.29 micrograms/ml at EH 48 (24 hours after the 2nd oral dose). Values at EH 72, 96, and 120 (24 hours after ...
A pharmacokinetic study of digoxin in the horse. Digoxin was administered orally and intravenously to seven healthy adult mares and geldings in two separate trials. At a dose of 44 microgram digoxin/kg body weight, the oral study was characterized by an absorption phase with a mean (+/- 1 standard deviation) peak serum digoxin concentration of 2.21 ng/ml (+/- 0.45) at a mean of 2.29 h (+/- 1.52) after administration. A second rise in serum digoxin concentration started about 6-8 h after administration and extended to about 20 h after administration. The mean bioavailability (F) was 23.38% (+/- 5.96). At a dose of 22 microgram digoxin/kg body...
Studies on a new paste preparation of phenylbutazone. The absorption characteristics of a new paste preparation of phenylbutazone were studied in ponies and thoroughbreds. The results suggested that at a similar dose rate of 5 mg/kg greater bioavailability results from the paste than from a powder preparation. Delivery of an accurate dosage of the paste was not possible using the multidose applicator. Repeated administration of the paste preparation (5 mg/kg twice daily) indicated that it is more toxic to both ponies and thoroughbreds than a powder preparation. In addition to the toxic manifestations previously reported, a neutropenia developed d...
Pharmacokinetics of phenytoin (diphenylhydantoin) in horses. The pharmacokinetics of the anti-convulsant phenytoin were investigated in clinically healthy horses after oral (p.o.) and intravenous (i.v.) administration. A single dose of phenytoin (8.8 mg/kg body weight) was given i.v. as a bolus to nine horses and one horse received 13.2 mg/kg. A two-compartment open model was used to describe the disposition of phenytoin. Four of the horses that received an i.v. dose (three at 8.8 mg/kg and one at 13.2 mg/kg) were then given the same dose 3 days later by the oral route. Phenytoin achieved a peak concentration in serum within 1-4 h after p.o. administrat...
Bioavailability of phenylbutazone preparations in the horse. Plasma phenylbutazone concentrations were determined for up to 12 h in 6 horses following intravenous and oral phenylbutazone administration. To evaluate the bioavailability of different oral preparations, phenylbutazone was administered in a paste as well as the traditional powder form. The effect of the state of stomach contents on the absorption of phenylbutazone was investigated by administering the paste before and after feeding; the powder was given in a small bran mash and a full feed of lucerne chaff, wheaten chaff and bran. Despite great variability among individual horses both the pa...
The pharmacokinetics of some aminoglycoside antibiotics in the horse. The disposition kinetics and bioavailability of streptomycin, kanamycin and neomycin were determined following their administration as parenteral preparations to horses. Single doses (10 mg/kg) of each aminoglycoside were given by the intravenous (i.v.) and intramuscular (i.m.) routes and, at a later time, seven intramuscular doses were injected at 12-h intervals. The pharmacokinetic behaviour of the three aminoglycosides was similar, in that a rapid distribution phase was followed by a relatively short half-life. The half-life (mean +/- SD, n = 6) of kanamycin (1.80 +/- 0.17 h) was significan...
The pharmacokinetics of xylazine hydrochloride: an interspecific study. The pharmacokinetic disposition of xylazine hydrochloride is described after both intravenous and intramuscular injection of a single dose, in four domestic species: horse, cattle, sheep and dog, by an original high performance liquid chromatographic technique. Remarkably small interspecific differences are reported. After intravenous administration, systemic half-life (t1/2 beta) ranged between 22 min (sheep) and 50 min (horse) while the distribution phase is transient with half-life (t1/2 alpha) ranging from 1.2 min (cattle) to 5.9 min (horse). The peak level of drug concentration in the pla...
The pharmacokinetics of meclofenamic acid in the horse. The pharmacokinetics of meclofenamic acid were studied in Thoroughbred horses and in ponies. After intravenous (i.v.) administration of either 2 mg/kg or 4 mg/kg sodium meclofenamate the elimination half-life was of the order of 0.9 h while the volume of distribution was found to be 0.128 litre/kg. Elimination was in accordance with a one-compartment model. Following oral administration of either meclofenamic acid (4 mg/kg) or sodium meclofenamate (4 mg/kg) a much longer terminal half-life than that calculated for Kel from i.v. data was found. This anomaly indicated that the 'flip-flop' phenom...
Digoxin pharmacokinetics, bioavailability, efficacy, and dosage regimens in the horse. The pharmacokinetics of IV administered digoxin and the bioavailability of intragastrically administered powdered digoxin tables suspended in water were investigated in 6 clinically normal adult horses by 125I radioimmunoassay. The effect of 3 to 5 sequential IV doses of 5 micrograms of digoxin/kg of body weight at 2-hour intervals on a left ventricular index of contractility (Vmax) was assessed in 5 clinically normal horses. Standard pharmacokinetic equations and mean pharmacokinetic variables were used to derive parenteral and oral (loading and maintenance) doses for digoxin in horses. The c...
Bioavailability of bromhexine in the horse. Bromhexine was administered orally (2 mg./kg.) and intravenously (i. v.) (1 mg./kg.) in 3 horses. Plasma levels were measured and the pharmacokinetic behaviour and bioavailability were estimated. The half-life of elimination after i. v. administration ranged from 3.1 to 4.4 hours. The mean values of the apparent volume of distribution and the volume of distribution of the central compartment amounted to 16.2 and 3.3 1./kg., respectively. A very high plasma clearance, ranging from 49.8 to 59 ml./kg./min., was found.
One hour after oral administration, a mean peak plasma level of about 14 ng....