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Bioavailability of indomethacin-saccharin cocrystals.
Jung, Min-Sook,Kim, Jeong-Soo,Kim, Min-Soo,Alhalaweh, Amjad,Cho, Wonkyung,Hwang, Sung-Joo,Velaga, Sitaram P Pharmaceutical Society of Great Britain 2010 Journal of pharmacy and pharmacology Vol.62 No.11
<P>Objectives??Pharmaceutical cocrystals are new solid forms with physicochemical properties that appear promising for drug product development. However, the in-vivo bioavailability of cocrystals has rarely been addressed. The cocrystal of indomethacin (IND), a Biopharmaceutical Classification System class II drug, with saccharin (SAC) has been shown to have higher solubility than IND at all pH. In this study, we aimed to evaluate the in-vitro dissolution and in-vivo bioavailability of IND-SAC cocrystals in comparison with IND in a physical mixture and the marketed product Indomee®. Methods??Scale-up of the cocrystals was undertaken using cooling batch crystallisation without seeding. The chemical and physical purity of the up-scaled material was verified using high-performance liquid chromatography, differential scanning calorimetry and powder X-ray diffraction. The IND-SAC cocrystals and IND plus SAC were mixed with lactose and the formulations were placed into gelatin capsules. In-vitro dissolution studies were then performed using the rotating basket dissolution method. The intrinsic dissolution rate of IND and IND-SAC cocrystals was also determined. Finally, a bioavailability study for the formulations was conducted in beagle dogs. The plasma samples were analysed using high-performance liquid chromatography and the pharmacokinetic data were analysed using standard methodologies. Key findings??The bulk cocrystals (i.e. scaled-up material) were chemically and physically pure. The in-vitro dissolution rate of the cocrystals was higher than that of IND and similar to that of Indomee® at pH 7.4 and pH 1.2. The in-vivo bioavailability of the IND-SAC cocrystals in dogs was significantly higher (ANOVA, P??lt;??.05) than that of IND but not significantly different from Indomee® (ANOVA, P??gt;??.05). Conclusions??The study indicates that the improved aqueous solubility of the cocrystals leads to improved bioavailability of IND. Thus, the cocrystals are a viable alternative solid form that can improve the dissolution rate and bioavailability of poorly soluble drugs.</P>
Coptidis Rhizoma attenuates repeated nicotine-induced behavioural sensitization in the rat.
Lee, Bombi,Yang, Chae Ha,Hahm, Dae-Hyun,Lee, Hye-Jung,Choe, Eun Sang,Pyun, Kwang-Ho,Shim, Insop Pharmaceutical Society of Great Britain 2007 Journal of pharmacy and pharmacology Vol.59 No.12
<P>Repeated injections of nicotine can produce an increase in locomotor activity and the expression of immediate-early gene, c-fos, in the central dopaminergic areas. Many studies have shown that Coptidis Rhizoma (CR) and its main alkaloid compound, berberine (BER), have a suppressive effect on the central nervous system. We examined the influence of CR or BER on repeated nicotine-induced locomotor activity in rats and the change of c-Fos expression in the brain by using immunohistochemistry. Male Sprague-Dawley rats were given CR and BER before repeated injections of nicotine hydrochloride (0.4 mg kg(-1), s.c.) twice daily for 7 days. After 3 days withdrawal, rats received a challenge injection of nicotine. Pretreatment with CR (100 mg kg(-1), i.p.) and BER (100 mg kg(-1), i.p.) significantly inhibited the nicotine-induced locomotor activity and expression of c-Fos in the striatum and the nucleus accumbens. These results suggest that CR and BER may produce inhibitory effects of nicotine on behavioural sensitization by possibly reducing postsynaptic neuronal activation in the central dopaminergic systems.</P>
Jung, Chang Hwa,Kim, Jeong-Hyun,Kim, Ji Hye,Chung, Joo Hee,Choi, Han-Seok,Seo, Jong Bok,Shin, Yong-Cheol,Kim, Sung-Hoon,Ko, Seong-Gyu Pharmaceutical Society of Great Britain 2011 Journal of pharmacy and pharmacology Vol.63 No.5
<P>Objectives??Rhus verniciflua Stokes (RVS), which has valuable medicinal properties, has for many years been prescribed for inflammation in east Asian medicine. Recent studies suggest that RVS has potent antioxidative, antitumor and anti-inflammatory properties. Methods??In this study, the anti-inflammatory effects of RVS in vitro and in vivo were investigated. The ethanol extract from RVS was partitioned with different solvents in order of increasing polarity. Key findings??Among the various extracts, the n-butanol extract displayed the most potent activity against nitric oxide and reactive oxygen species. The n-butanol extract also significantly regulates expression of nitric oxide synthase, which inhibits nitric oxide production at the transcriptional level in activated macrophages. Immunoblot analysis also showed that n-butanol extract suppresses the phosphorylation of extracellular signal-regulated kinase and Akt, suggesting that nitric oxide synthase suppression might be mediated via the extracellular signal-regulated kinase and Akt signaling pathways. This study also investigated whether n-butanol exerts an anti-inflammatory effect in an animal model. n-butanol extract significantly reduces carrageenan-induced mouse paw edema at 5?. Conclusions??These results suggest that RVS could be a promising candidate agent for inflammation prevention and combination therapy with anti-inflammatory drugs.</P>
Jeong, Seung Il,Kwon, Oh Deog,Kwon, Seung Chun,Jung, Kyu Yong Pharmaceutical Society of Great Britain 2011 Journal of pharmacy and pharmacology Vol.63 No.2
<P>Objectives??We have previously reported that methylisogermabullone (MIGB) stimulates small bowel motility through activation of acetylcholinergic receptors. This study investigated the cellular signalling pathways implicated in the regulation of ileal contractility by MIGB. Methods??The ileal longitudinal muscles prepared from rats were treated with MIGB isolated from radish roots, and muscle contractility and protein expression were measured by force transducer and Western blot, respectively. Key findings??MIGB at 30? induced a sustained phasic contraction of ileal longitudinal muscles. Acetylcholine (ACh, 0.5?) and MIGB stimulated translocation of protein kinase C (PKC) to cell membrane of ileal longitudinal muscles, and these stimulatory effects were remarkably attenuated by atropine (0.5?). ACh and MIGB induced phosphorylation of ERK 1/2 and p38 MAPKs in ileal longitudinal muscles, and they also phosphorylated the caldesmon and 20-kDa regulatory light chain of myosin (MLC(20) ). Additionally, PD-98058 (10?), a selective ERK 1/2 MAPK inhibitor, and SB-203580 (10?), a selective p38 MAPK inhibitor, significantly reduced the MIGB-induced contraction of ileal longitudinal muscles. Conclusions??The muscarinic receptor activated by MIGB translocates the PKC to cell membrane which phosphorylates the ERK 1/2 and p38 MAPKs, resulting in subsequent phosphorylation of caldesmon and MLC(20) . These cellular events likely converge on the contraction of ileal longitudinal muscles in rats.</P>
Hong, Soon-Pyo,Yang, Joon-Seung,Han, Jung-Yeon,Ha, Sung-Il,Chung, Joong-Wha,Koh, Young-Youp,Chang, Kyong-Sig,Choi, Dong-Hyun Pharmaceutical Society of Great Britain 2011 Journal of pharmacy and pharmacology Vol.63 No.1
<P>The purpose of this study was to examine the effects of lovastatin on cytochrome P450 (CYP) 3A4 and P-glycoprotein (P-gp) in vitro and then to determine the effects of lovastatin on the pharmacokinetics of diltiazem and its main metabolite, desacetyldiltiazem, in rats.</P>
Lee, Do Ik,Huh, Yoon Joo,Hwang, Kwang Woo,Choi, YoungWook,Choi, Jae-Seok,Han, Sam-Yong,Gyoung, Young-Soo,Joo, Seong Soo Pharmaceutical Society of Great Britain 2011 Journal of pharmacy and pharmacology Vol.63 No.10
<P>In the present study, we aimed to examine the anti-atopic properties of bile from the cat fish, Silurus asotus, to determine its possible use as a pharmaceutical product.</P>
Fang, Minghao,Lee, Seung-Youp,Park, Seung-Moon,Choi, Ki-Choon,Lee, Young Jae,Cho, Hyoung-Kwon,Cho, Seong-Wan,Whang, Wan Kyunn,Lee, Jeong-Chae Pharmaceutical Society of Great Britain 2011 Journal of pharmacy and pharmacology Vol.63 No.1
<P>The seed of Phaseolus calcaratus Roxburgh (PHCR) has traditionally been used as a herbal medicine, considered to have anti-inflammatory potential. Here we examined the ability of PHCR seed extract to inhibit inflammatory responses of macrophages to bacterial toxin and the mechanism involved.</P>