6 research outputs found
Enhancing Effect of Îē-Lactoglobulin on the Rate of Cyclosporin Absorption
tic  The aim of this study was to determine the effects of Îē-lactoglobulin (Îē-LG) on the intestinal absorption of cyclosporin A (CsA) in vivo and in vitro. After intraduodenal co-administration of CsA (5 mg/kg) with 150 mg/kg Îē-LG, Tmax was significantly lower than that of control rats which were given the same dose of CsA without Îē-LG. Cmax and AUC were significantly increased as compared with the control while T1/2 were not significant. Moreover, a deconvolution method revealed that the rate of CsA absorption was enhanced by Îē-LG (150 mg/kg) by about 12 times. These results indicate that Îē-LG significantly enhanced the rate of CsA absorption and the extent of CsA bioavailability in the gut. Îē-LG did not change the solubility of CsA in vitro, but Îē-LG increased the apical-to-basolateral permeability clearance of CsA (PScell), with pronounced increase in the permeability of unbound CsA (PSu,cell), across the Caco-2 monolayers in a concentration-dependent manner in vitro.  It was thus considered that Îē-LG-mediated transport of CsA might be a possible mechanism to enhance the intestinal absorption of CsA in vivo
Effect of Thiotriazinone Impurity on Insoluble Microparticle Generation Associated with Ceftriaxone-calcium Salt Precipitation in Original (RocephinÂŪ) and Japanese Generic Ceftriaxone ProductsÂ
This study examined the effect of thiotriazinone impurity on the generation of insoluble microparticles (IMPs) associated with ceftriaxone-calcium salt precipitation in original (RocephinÂŪ) and Japanese generic ceftriaxone (A; Sawai, B; Nichi-Iko) products when mixed with Ca2ïž 4.3mEq/l. We found that the generation rate of IMPs associated with ceftriaxone-calcium salt precipitation among the three ceftriaxone products tested was in the order of generic (A)ïžoriginalïžgeneric (B), as assessed by light obscuration particle counting. Typically, after 60 min, one of the generic ceftriaxone (B)-calcium mixtures was highly opaque with numerous aggregates of milky-white precipitates, the original ceftriaxone-calcium mixture exhibited noticeable IMPs, and the second generic ceftriaxone (A)-calcium mixture was transparent. The levels of thiotriazinone contaminants, known to be a major impurity in ceftriaxone products, were determined by HPLC and found to be in the order of generic Aïžoriginalïžgeneric B. Moreover, the addition of a small amount of thiotriazinone into the generic ceftriaxone (B)-calcium mixture significantly decreased the amount of IMPs, suggesting that the impurity retards ceftriaxone-calcium crystal growth. We thus concluded that the thiotriazinone impurity acts as a suppressive factor of ceftriaxone-calcium salt precipitation, and that the high level of thiotriazinone impurity in the ceftriaxone (B) product could underlie its lowest rate of IMP generation when mixed with calcium. We thus recommend caution regarding the clinical risk of ceftriaxone-calcium compatibility due to impurity contamination in ceftriaxone products
DEMONSTRATION OF DOCOSAHEXAENOIC ACID AS A BIOAVAILABILITY ENHANCER FOR CYP3A SUBSTRATES: IN VITRO AND IN VIVO EVIDENCE USING CYCLOSPORIN IN RATS
Pharmacological effects of Chatuphalatika in hyperuricemia of gout
Context: Chatuphalatika (CTPT), is a Thai herbal formulation mixture of Phyllanthus emblica Linn. (Euphorbiaceae), Terminalia belerica Linn. (Combretaceae), T. chebula and the fruit of T. arjuna (Roxb.) Wight & Arn. CTPT is considered to exert anti-inflammatory and antihyperuricemic effects, but there have been no reports to demonstrate these pharmacological effects in a quantitative manner. Objectives: To investigate the antioxidative, anti-inflammatory and antihyperuricemic effects of CTPT. Materials and methods: Antioxidant activities of CTPT extracts were measured in vitro by DPPH, ABTS and FRAP assays, and anti-inflammatory effect by measuring inflammatory mediator production induced by lipopolysaccharide (LPS) in RAW264.7 macrophages. The mechanism of the hypouricemic effect was investigated using oxonate-induced hyperuricemic ddY mice treated with oral administrations of CTPT at 250, 500 and 1000âmg/kg. Results: Antioxidant activities of CTPT measured by ABTS and FRAP assays were 1.35âg TEAC/g extract and 10.3âmmol/100âg extract, respectively. IC50 for the inhibition of DPPH radical was 13.8âÂĩg/mL. CTPT (10âÂĩg/mL) significantly downregulated the mRNA expression of TNF-Îą and iNOS in RAW 264.7 cells. LineweaverâBurk analysis of the enzyme kinetics showed that CTPT inhibited xanthine oxidase (XOD) activity in a noncompetitive manner with the Ki of 576.9âÂĩg/mL. Oral administration of CTPT (1000âmg/kg) significantly suppressed uric acid production by inhibiting hepatic XOD activity, and decreased plasma uric acid levels in hyperuricemic mice by approximately 40% (pâ<â0.05). Conclusions: This study demonstrated for the first time the antioxidative, anti-inflammatory and antihyperuricemic effects of CTPT in vivo and in vitro, suggesting a possibility of using CTPT for the treatment of hyperuricemia in gout
The Evaluation and Development of Computer-Assisted Instruction Program in Pharmacology of Asthma-āļāļēāļĢāļāļĢāļ°āđāļīāļĄāļīāļāđāļĨāļ°āļāļąāļāļāļēāđāļāļĢāđāļāļĢāļĄāļāļāļĄāļāļīāļ§āđāļāļāļĢāđāļāđāļ§āļĒāļŠāļāļāđāļāļĢāļēāļĒāļ§āļīāļāļēāđāļ āļŠāđāļāļ§āļīāļāļĒāļēāđāļĢāļ·āđāļāļāđāļĢāļāļŦāļ·āļ
AbstractObjective: To develop and evaluate the computer-assisted instructionprogram (CAI) in asthma pharmacology.Methods: Quasi-experimentaldesign was used to collect data related to the impact of CAI and hand-outself-study on studentsâ achievement in learning asthma pharmacology. The20 Doctor of Pharmacy (PharmD) students at Faculty of Pharmacy,Mahasarakham University were randomly allocated to 2 groups by drawinglots. Intervention group (n = 10) was provided a self-study CAI and controlgroup (n=10) was given a self-study handouts. The experiment wasconducted from November to December 2010. Between groups and withingrouppre-post comparisons on knowledge about asthma (30 questions)were carried out. Opinions on the learning process from both groups werealso obtained.Results: Post-test knowledge score in either group wassignificantly higher than its pre-test score (P = 0.005 in both groups).However, post-test scores between the two groups were not statisticallydifferent. In terms of participantsâ opinion, it was found that opinion scoreson knowledge gained, self-study skills acquired and student satisfaction inthe intervention group were significantly greater than control group (P =0.044, = 0.018 and = 0.014, respectively). Students in study groupsuggested improve CAI in the following aspects: color setting, font size,and narration speed.Conclusion: Using CAI stimulates learning processand improves understanding in the learning subject. It could be analternative means of self-learning.Key words: computer-assisted instruction program, asthma, pharmacologyāļāļāļāļąāļāļĒāđāļāļ§āļąāļāļāļļāļāļĢāļ°āļŠāļāļāđ: āđāļāļ·āđāļāļĻāļķāļāļĐāļēāļāļĨāļāļēāļĢāđāļāđāļŠāļ·āđāļāļāļēāļĢāđāļĢāļĩāļĒāļāļĢāļđāđāļāđāļ§āļĒāļāļāđāļāļāđāļāļĒāđāļāđāđāļāļĢāđāļāļĢāļĄāļāļāļĄāļāļīāļ§āđāļāļāļĢāđāļāđāļ§āļĒāļŠāļāļ (computer-assisted instruction; CAI) āļāļēāļāđāļ āļŠāļąāļāļ§āļīāļāļĒāļēāđāļāļāļāđāļĢāļĩāļĒāļāđāļĢāļ·āđāļāļāđāļĢāļāļŦāļ·āļāļ§āļīāļāļĩāļāļēāļĢāļĻāļķāļāļĐāļē: āļāļēāļĢāļĻāļķāļāļĐāļēāđāļāļ quasi-experimental design āđāļāđ CAI āđāļāļĢāļĩāļĒāļāđāļāļĩāļĒāļāļāļąāļāļāļēāļĢāđāļāđāđāļāļāļŠāļēāļĢāļāļĢāļ°āļāļāļāļāļēāļĢāļŠāļāļāđāļāļāļīāļŠāļīāļāđāļ āļŠāļąāļāļĻāļēāļŠāļāļĢāđāļāļąāļāđ āļāļĩāļāļĩāđ 3 āļāļāļ°āđāļ āļŠāļąāļāļĻāļēāļŠāļāļĢāđ āļĄāļŦāļēāļ§āļīāļāļĒāļēāļĨāļąāļĒāļĄāļŦāļēāļŠāļēāļĢāļāļēāļĄ āļĻāļķāļāļĐāļēāļāļąāđāļāđāļāđāđāļāļ·āļāļāļāļĪāļĻāļāļīāļāļēāļĒāļāļāļķāļāļāļąāļāļ§āļēāļāļĄ āļ.āļĻ. 2553 āđāļāđāļāļāļīāļŠāļīāļāđāļāđāļ 2 āļāļĨāļļāđāļĄ (āļāļĨāļļāđāļĄāļāļ§āļāļāļļāļĄāđāļĨāļ°āļāļĨāļļāđāļĄāļāļāļĨāļāļ) āļāļĨāļļāđāļĄāļĨāļ° 10 āļāļ āđāļāļĒāļ§āļīāļāļĩāļŠāļļāđāļĄāļāļĒāđāļēāļāļāđāļēāļĒ āđāļāļāļĨāļļāđāļĄāļāļ§āļāļāļļāļĄāļāļīāļŠāļīāļāđāļĢāļĩāļĒāļāļĢāļđāđāļāđāļ§āļĒāļāļāđāļāļāđāļāļĒāđāļāđāđāļāļāļŠāļēāļĢāļāļĢāļ°āļāļāļāļāļēāļĢāļŠāļāļāļāļĩāđāļĄāļĩāđāļāļ·āđāļāļŦāļēāđāļŦāļĄāļ·āļāļāđāļ CAI āļāļĩāđāļāļđāđāļ§āļīāļāļąāļĒāļāļąāļāļāļēāļāļķāđāļ āđāļĨāļ°āļāļĨāļļāđāļĄāļāļāļĨāļāļāđāļĢāļĩāļĒāļāļĢāļđāđāļāđāļ§āļĒāļāļāđāļāļāđāļāļĒāđāļāđ CAI āđāļĨāļ°āđāļāļĩāļĒāļāļāļĨāļāļēāļĢāđāļĢāļĩāļĒāļāļāļēāļāļāļģāļāļ§āļāļāđāļāļāļģāļāļēāļĄāļāļ§āļēāļĄāļĢāļđāđāļāļĩāđāļāļāļāļāļđāļāļāđāļāļ (āļāļąāļāđ āļŦāļĄāļ 30 āļāđāļ) āđāļāļĢāļĩāļĒāļāđāļāļĩāļĒāļāļāļ°āđāļāļāļāđāļāļāđāļĨāļ°āļŦāļĨāļąāļāđāļĢāļĩāļĒāļāļāđāļ§āļĒāļāļāđāļāļāđāļāđāļāđāļĨāļ°āļāļĨāļļāđāļĄāđāļĨāļ°āļĢāļ°āļŦāļ§āđāļēāļāļāļĨāļļāđāļĄ āđāļĨāļ°āļāļ§āļēāļĄāđāļŦāđāļāđāļĨāļ°āļāđāļāđāļŠāļāļāđāļāļ°āļāđāļāļŠāļ·āđāļāļāļĩāđāļāļđāđāđāļĢāļĩāļĒāļāđāļāđāđāļĢāļĩāļĒāļāļĢāļđāđāļāđāļ§āļĒāļāļāđāļāļāļāļēāļāļāļąāļāđ āļŠāļāļāļāļĨāļļāđāļĄ āļāļĨāļāļēāļĢāļĻāļķāļāļĐāļē: āļŦāļĨāļąāļāļāļēāļĢāđāļĢāļĩāļĒāļāļĢāļđāđāļāđāļ§āļĒāļāļāđāļāļāļāđāļēāļāļŠāļ·āđāļāļāļąāđāļ 2 āļāļāļīāļ āļāļāļ§āđāļēāļāļąāļāđ āļāļĨāļļāđāļĄāļāļ§āļāļāļļāļĄāđāļĨāļ°āļāļĨāļļāđāļĄāļāļāļĨāļāļāļĄāļĩāļāļ°āđāļāļāļŦāļĨāļąāļāđāļĢāļĩāļĒāļāļāđāļēāļāļŠāļ·āđāļāļāļąāđāļ 2 āļāļāļīāļāļŠāļđāļāļāļ§āđāļēāļāđāļāļāđāļĢāļĩāļĒāļāļāļĒāđāļēāļāļĄāļĩāļāļąāļĒāļŠāļģāļāļąāļāļāļēāļāļŠāļāļīāļāļī (P = 0.005 āļāļąāļāđ āļŠāļāļāļāļĨāļļāđāļĄ) āđāļāđāļāļ°āđāļāļāļŦāļĨāļąāļāđāļĢāļĩāļĒāļāļāļāļāļāļąāđāļ 2 āļāļĨāļļāđāļĄāđāļĄāđāđāļāļāļāđāļēāļāļāļąāļ āļāļĒāđāļēāļāđāļĢāļāđāļāļēāļĄ āļāļĨāļļāđāļĄāļāļāļĨāļāļāđāļŦāđāļāļ°āđāļāļāļāļ§āļēāļĄāđāļŦāđāļāļāđāļāļāļēāļĢāđāļāđāļŠāļ·āđāļāļŠāļđāļāļāļ§āđāļēāļāļĨāļļāđāļĄāļāļ§āļāļāļļāļĄāļāļĒāđāļēāļāļĄāļĩāļāļąāļĒāļŠāļģāļāļąāļāđāļāļāđāļēāļ 1) āļāļ§āļēāļĄāļĢāļđāđāļāļĩāđāđāļāđāļĢāļąāļāļāļēāļāļŠāļ·āđāļ 2) āļŠāļ·āđāļāļāđāļ§āļĒāđāļŦāđāļĄāļĩāļāļąāļāļĐāļ°āđāļāđāļāļąāļāļŦāļēāļĄāļēāļāļāļķāđāļ āđāļĨāļ° 3) āļāļ§āļēāļĄāļāļķāļāļāļāđāļāļāļēāļāļāļēāļĢāđāļāđāļŠāļ·āđāļ (P = 0.044, P = 0.018, P = 0.014 āļāļēāļĄāļĨāļģāļāļąāļ) āļāļĨāļļāđāļĄāļāļāļĨāļāļāđāļŠāļāļāđāļāļ°āđāļŦāđāļāļĢāļąāļāļāļĢāļļāļāđāļāļĢāđāļāļĢāļĄāļāļāļĄāļāļīāļ§āđāļāļāļĢāđāļāđāļ§āļĒāļŠāļāļāđāļāđāļĢāļ·āđāļāļāļŠāļĩ āļāļāļēāļāļāļąāļ§āļāļąāļāļĐāļĢāļāļĩāđāļĄāļāļāđāļŦāđāļāđāļĄāđāļāļąāļāđāļāļāđāļĨāļ°āļāļ§āļēāļĄāđāļĢāđāļ§āļāļāļāđāļŠāļĩāļĒāļāļāļĢāļĢāļĒāļēāļĒāđāļāļ·āđāļāļŦāļē āļŠāļĢāļļāļ: āđāļāļĢāđāļāļĢāļĄāļāļāļĄāļāļīāļ§āđāļāļāļĢāđāļāđāļ§āļĒāļŠāļāļāļŠāļēāļĄāļēāļĢāļāļāļĢāļ°āļāļļāđāļāļāļēāļĢāđāļĢāļĩāļĒāļāļĢāļđāđāđāļĨāļ°āđāļāļīāđāļĄāļāļ§āļēāļĄāļĢāļđāđāļāļ§āļēāļĄāđāļāđāļēāđāļ āļāļķāļāđāļāđāļāļāļĩāļāļāļēāļāđāļĨāļ·āļāļāļŦāļāļķāđāļāļāļĩāđāļāļđāđāđāļĢāļĩāļĒāļāļŠāļēāļĄāļēāļĢāļāđāļāđāđāļĢāļĩāļĒāļāļĢāļđāđāđāļĨāļ°āļāļāļāļ§āļāđāļāđāļāđāļ§āļĒāļāļāđāļāļāļāļģāļŠāļģāļāļąāļ : āđāļāļĢāđāļāļĢāļĄāļāļāļĄāļāļīāļ§āđāļāļāļĢāđāļāđāļ§āļĒāļŠāļāļ, āđāļĢāļāļŦāļ·āļ, āđāļ āļŠāļąāļāļ§āļīāļāļĒ