Aim To study the effect of complexation with hydroxylpropyl-β-cyclodextrin(HP-β-CD) on the solubility, dissolution rate and chemical stability of prostaglandin E_1 (PGE_1) ,thereby providing a basis for preparing a ...Aim To study the effect of complexation with hydroxylpropyl-β-cyclodextrin(HP-β-CD) on the solubility, dissolution rate and chemical stability of prostaglandin E_1 (PGE_1) ,thereby providing a basis for preparing a stable solid or aqueous preparation of PGE_1 formulatedwith HP-β-CD. Methods The effect of HP-β-CD on the solubility of PGE_1 was studied by phasesolubility method. The formation of inclusion complexes of PGE_1 with HP-β-CD in the aqueoussolution was confirmed by UV spectra, circular dichroism spectroscopy, and that in the solid stateby IR spectra and X-ray diffractome-try. An solid inclusion complex of PGE_1 with HP-β-CD wasprepared by lyophilization. The dissolution rate and stability of the inclusion complex weredetermined and compared with those of PGE_1 alone. Meanwhile, the stability of PGE_1 aqueoussolutions in the presence of HP-β-CD was studied under different pH conditions. Results Thesolubility of PGE_1 increased linearly with increasing HP-β-CD concentration in various pH bufferedsolutions, showing typical A_L-type phase solubility diagrams. The stability and dissolution rateof the solid inclusion complex of PGE_1 were significantly increased, compared with those of purePGE_1 . The stability of PGE_1 in HP-β-CD solutions was also obviously improved under acidic andbasic conditions, but the stabilizing effect was absent under neutral conditions. Conclusions Thesolubility,dissolution rate and chemical stability of PGE_1 are markedly improved by complexationwith HP-β-CD: It is quite possible to prepare a stable PGE_1 inclusion complex-containing soliddosage forms, but almost impossible to obtain a stable aqueous preparation of PGE_1 formulated withHP-β-CD.展开更多
Objective: To study the anti-inflammatory activity and tissue distribution patterns of intravenousemulsion of dexamethasone acetate in mice. Methods: The anti-inflammatory solution for injection andLimethasone(Jepanes...Objective: To study the anti-inflammatory activity and tissue distribution patterns of intravenousemulsion of dexamethasone acetate in mice. Methods: The anti-inflammatory solution for injection andLimethasone(Jepanese product) given intravenously were evaluated by using the preformed carrageenan granulomapouch method in rats. Results: The anti-inflammatory activity of dexamethasone acetate emulsion at low dose of 0.05mg.kg1 was as potent as dexamethasone sodium phosphate solution at high dose of 0.3 mg.kg1. The distributionpatterns in mice tissues of [^3H]dexamethasone acetate emulsion and [^3H]dexamethasone sodium phosphate solution inmice were markedly different. Dexamethasone acetate emulsion showed a much higher concentration in the liver,spleen, lung, and inflamed tissues, whereas dexamethasone sodium phosphate had a high concenti,mon in themuscles of vastus lateralis. These results may indicate that dexamethasone incoporated in lipid emulsion was taken upby the reticuloendothelial system and inflammatory cells much more than dexamethasone sodium phosphate solution.Conclusion: When dexamethasone acetate was incorporated in emulsion, the distribution patterns in tissues werechanged and they had a stronger anti-inflammatory activity.展开更多
The protective effects of iptakalim hydrochloride (Ipt) 0.5-4.0mg·kg^-1 ip on global cerebral ischemia/reperfusion-evoked insult in gerbil were studied using bilateral carotid artery ligation to prepare the globa...The protective effects of iptakalim hydrochloride (Ipt) 0.5-4.0mg·kg^-1 ip on global cerebral ischemia/reperfusion-evoked insult in gerbil were studied using bilateral carotid artery ligation to prepare the global cerebral ischemia model.The NMDA receptor blocker,ketamine was administered as a positive control drug and saling was administered as a negative model control.The results shown that Ipt decreased the increasing locomotor activity evoked by ischemia and had reliable functional protection of ischemia-induced hippocampus injury.Ipt could also improve global cerebral ischemia-induced working memory impairments.Ipt decreased the number of necrotic and apoptotic neurons and increased the remaining number of healthy neurons in hippocampus CAl zone.Ipt promoted the recovery of hippocampus function.Ipt reversed ischemia-evoked increases of grutamate,aspartate,glycine and glutamine in hippocampus,striatum and cortex of gerbils completely and reversed the increase of GABA and taurine partly.It is concluded that Ipt has experimental therapeutic effects on global cerebral ischemia.展开更多
Aim: To obtain the C-terminal DNA and construct the expression plasmid in yeast two-hybrid. Methods: About 177bp DNA fragment was amplified from the complete sequence of ( receptor by PCR. After being sequenced, the C...Aim: To obtain the C-terminal DNA and construct the expression plasmid in yeast two-hybrid. Methods: About 177bp DNA fragment was amplified from the complete sequence of ( receptor by PCR. After being sequenced, the C-terminal fragment was ligased into EcoR I-BamH I site of pGBKT7 vector to form recombinants. The recombinant展开更多
AIM: Many studies suggest that the mesolimbic dopamine system is a major neural substrate for the rewarding effect produced by morphine. Morphine cause an increase in dopamine release in the nucleus accumbens through ...AIM: Many studies suggest that the mesolimbic dopamine system is a major neural substrate for the rewarding effect produced by morphine. Morphine cause an increase in dopamine release in the nucleus accumbens through indirect mechanisms that is related to its psychological dependence. However, many other neurotransmitters and their receptor systems,展开更多
AIM: To establish a primary culture technique of acutely isolated dorsal root ganglion (DRG) neurons, and provide a simple & useful in vitro model for study of analgesia. Methods: Acutely isolated dorsal root gang...AIM: To establish a primary culture technique of acutely isolated dorsal root ganglion (DRG) neurons, and provide a simple & useful in vitro model for study of analgesia. Methods: Acutely isolated dorsal root ganglion (DRG) neurons were planted and cultured; the configuration and growth characters of DRG neurons were observed through inverted microscope.展开更多
文摘Aim To study the effect of complexation with hydroxylpropyl-β-cyclodextrin(HP-β-CD) on the solubility, dissolution rate and chemical stability of prostaglandin E_1 (PGE_1) ,thereby providing a basis for preparing a stable solid or aqueous preparation of PGE_1 formulatedwith HP-β-CD. Methods The effect of HP-β-CD on the solubility of PGE_1 was studied by phasesolubility method. The formation of inclusion complexes of PGE_1 with HP-β-CD in the aqueoussolution was confirmed by UV spectra, circular dichroism spectroscopy, and that in the solid stateby IR spectra and X-ray diffractome-try. An solid inclusion complex of PGE_1 with HP-β-CD wasprepared by lyophilization. The dissolution rate and stability of the inclusion complex weredetermined and compared with those of PGE_1 alone. Meanwhile, the stability of PGE_1 aqueoussolutions in the presence of HP-β-CD was studied under different pH conditions. Results Thesolubility of PGE_1 increased linearly with increasing HP-β-CD concentration in various pH bufferedsolutions, showing typical A_L-type phase solubility diagrams. The stability and dissolution rateof the solid inclusion complex of PGE_1 were significantly increased, compared with those of purePGE_1 . The stability of PGE_1 in HP-β-CD solutions was also obviously improved under acidic andbasic conditions, but the stabilizing effect was absent under neutral conditions. Conclusions Thesolubility,dissolution rate and chemical stability of PGE_1 are markedly improved by complexationwith HP-β-CD: It is quite possible to prepare a stable PGE_1 inclusion complex-containing soliddosage forms, but almost impossible to obtain a stable aqueous preparation of PGE_1 formulated withHP-β-CD.
文摘Objective: To study the anti-inflammatory activity and tissue distribution patterns of intravenousemulsion of dexamethasone acetate in mice. Methods: The anti-inflammatory solution for injection andLimethasone(Jepanese product) given intravenously were evaluated by using the preformed carrageenan granulomapouch method in rats. Results: The anti-inflammatory activity of dexamethasone acetate emulsion at low dose of 0.05mg.kg1 was as potent as dexamethasone sodium phosphate solution at high dose of 0.3 mg.kg1. The distributionpatterns in mice tissues of [^3H]dexamethasone acetate emulsion and [^3H]dexamethasone sodium phosphate solution inmice were markedly different. Dexamethasone acetate emulsion showed a much higher concentration in the liver,spleen, lung, and inflamed tissues, whereas dexamethasone sodium phosphate had a high concenti,mon in themuscles of vastus lateralis. These results may indicate that dexamethasone incoporated in lipid emulsion was taken upby the reticuloendothelial system and inflammatory cells much more than dexamethasone sodium phosphate solution.Conclusion: When dexamethasone acetate was incorporated in emulsion, the distribution patterns in tissues werechanged and they had a stronger anti-inflammatory activity.
文摘The protective effects of iptakalim hydrochloride (Ipt) 0.5-4.0mg·kg^-1 ip on global cerebral ischemia/reperfusion-evoked insult in gerbil were studied using bilateral carotid artery ligation to prepare the global cerebral ischemia model.The NMDA receptor blocker,ketamine was administered as a positive control drug and saling was administered as a negative model control.The results shown that Ipt decreased the increasing locomotor activity evoked by ischemia and had reliable functional protection of ischemia-induced hippocampus injury.Ipt could also improve global cerebral ischemia-induced working memory impairments.Ipt decreased the number of necrotic and apoptotic neurons and increased the remaining number of healthy neurons in hippocampus CAl zone.Ipt promoted the recovery of hippocampus function.Ipt reversed ischemia-evoked increases of grutamate,aspartate,glycine and glutamine in hippocampus,striatum and cortex of gerbils completely and reversed the increase of GABA and taurine partly.It is concluded that Ipt has experimental therapeutic effects on global cerebral ischemia.
文摘Aim: To obtain the C-terminal DNA and construct the expression plasmid in yeast two-hybrid. Methods: About 177bp DNA fragment was amplified from the complete sequence of ( receptor by PCR. After being sequenced, the C-terminal fragment was ligased into EcoR I-BamH I site of pGBKT7 vector to form recombinants. The recombinant
文摘AIM: Many studies suggest that the mesolimbic dopamine system is a major neural substrate for the rewarding effect produced by morphine. Morphine cause an increase in dopamine release in the nucleus accumbens through indirect mechanisms that is related to its psychological dependence. However, many other neurotransmitters and their receptor systems,
文摘AIM: To establish a primary culture technique of acutely isolated dorsal root ganglion (DRG) neurons, and provide a simple & useful in vitro model for study of analgesia. Methods: Acutely isolated dorsal root ganglion (DRG) neurons were planted and cultured; the configuration and growth characters of DRG neurons were observed through inverted microscope.
