生物分析与生物医学杂志

The pharmacokinetic study of diminazene aceturate (DMZ) was carried out in two separate groups of 4 e ach clinically healthy female Murrah buffalo calves aft er single dose i.v. (8 mg/kg) and i.m. (16 mg/kg) administrat ion. The mean free peak serum concentration of DMZ (CS max ) after i.v. (26.28±0.67μ g/ml) and i.m. (8.41±2.43 μ g/ml) a dmin- istrations were obtained at t max of 5 and 30 min respectively. The DMZ serum concentrations time data were best fi tted to the two compartment open model. The calculated s erum half life (t ½ β ) values of DMZ were 15.099±2.504 and 14.225±2.682 h after i.v. and i.m. administration r espec- tively. The mean values of total body clearance rat e of DMZ (ClB) after i.m. (3.785±1.119 ml/kg/min) was signif icantly higher (P<0.05) as compared with the i.v. (0.537±0. 063 ml/kg/min). DMZ was highly bound (77.14 to 94.40%) to buffalo calf plasma protein and its penetration int o erythro- cytes increased with increasing concentrations in b lood (7.60 to 33.00μ g/ml). Based on pharmacokinetic profiles, the satisfactory dosage regimens of diminazene aceturat e in buffalo calves were derived (2 mg/kg, i.v. and 12mg /kg, i.m). In case of emergent disease conditions to ens ure high DMZ serum concentrations, i.v. route may be preferr ed over i.m. route.

The docetaxel of sterile freeze-dried powder inject ions was new developed injections due to overcome some drawb acks of Taxotere. We has been evaluated the pharmacokine tic properties and bioequivalence of the docetaxel of s terile freeze-dried powder injections and Taxotere by high ly selective and accurate LC-MS/MS method in healthy r ats. The pharmacokinetic parameters and bioequivalence o f two injections were obtained by the profession software (DAS, version 2.0). The 90% CIs for the In-transformed ra tios of C max : AUC 0-t and AUC 0~8 were 101.3%-104.1%, 99.8%- 100.8% and 99.4-100.6%, respectively (all, p < 0.001). In this study, we attained the pharmacokinetic paramet ers of the two injections’, meanwhile docetaxel of sterile freeze- dried powder injections appeared to be bioequivalen t to Taxotere in healthy rats. The result was beneficial ly to further study the pharmacokinetics and bioequivalen ce of the human in the future research.

A regulation with respect to bioequivalence and invitro dissolution of solid oral dosage forms in USA and Japan is summarized and compared. Significant differences in vari- ous parameters like dissolution, biowaiver, inclusion- ex- clusion criteria of subjects in the clinical trials, statistical results were found between two systems. The regulatory experienced gained up to now is studied and compared.

Anthum graveolens (dill) seeds are a common and very effective household remedy for a wide range of digestive problems. The present study was performed to investigate the effect of dill extracts on altered biochemical parameters in deltamethrin-exposed rats. Deltamethrin was adminis- tered orally at doses 7.5 and 15 mg /kg of body weight on the basis of LD 50 for 30 days. The sub-acute toxicity of pyrethroid insecticide deltamethrin varies markedly with the dose employed. Oral administration of plant extracts to rats for 30 days afforded a good protection against deltamethrin elevation in serum marker enzymes. They decreased the lev- els of aspartate aminotransferase (AST), alanine ami- notransferase (ALT) and alkaline phosphatase (ALP) which was increased by DLM administration. Deltamethrin sig- nificantly increased the level of plasma total protein (TP), cholesterol and triglyceride. The concentration of urea and creatinine were also increased and all these parameters were decreased by the effect of plant extract. Results were also indicated that, the enzyme activities of acetyl cholinesterase (AchE), catalase (Cat) and glutathione-S-transferase (GST) were increased as compared to the DLM group. Dose de- pendant of histopathological changes which observed in both liver and kidney are also described.

A simple a nd sensitive high per for ma nce liquid chromatography (HPLC) method was developed for qua ntification of clobeta sol (CLB) in r a t pla sma . Aripiprazole was used as an internal standard (IS). The present method uses protein precipitation with acetonitrile, followed by the liquid-liquid extraction with methyl tertiary butyl ether for extraction of the CLB from the matrix. Separation was carried out using Variance C 18 (250.0 × 4.6 mm, 5 μ m particle size) column and the effluent was monitored by an ultra violet (UV) detector at 240 nm. The mobile phase used was acetonitrile: phosphate buffer (pH 7.0; 25.0mM containing 0.2 %v/v triethylamine) (65: 35 % v/v) at a flow rate of 1.0 ml/min. The present method was va lida ted a s per the United States Food and Dr ug Administration (USFDA) guideline. This method was linear over the range of 25.0-1000.0 ng/ml with regression coefficient greater than 0.99. The mean recovery of CLB and IS were 70.8±1.9 and 83.32 ± 1.55 % respectively. The method was found to be precise, accurate and specific. The developed HPLC method was applied for the estimation of CLB in plasma after topical application of various zinc salts in rats to study the penetration of CLB through rat skin.