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Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier

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World Journal of Gastroenterology 2008年第31期14卷 4928-4937页

作者： Bei-Bei Huang Guo-Feng Li Jing-Hui Luo Lian Duan Kishimoto Nobuaki Yamamoto Akira Department of pharmacy Nanfang Hospital Southern Medical University Guangzhou 510515 Guangdong Province China Department of Biopharmaceutics Kyoto Pharmaceutical University Misasagi Yamashinaku Kyoto 6078414 Japan

AIM: To investigate the permeability characteristics of rebamipide across intestinal mucosa, and examine the effects of some absorption enhancers on the permeability across the colonic tissue. Another purpose is to demonstrate the colon-specific delivery of rebamipide with or without absorption enhancers using chitosan capsule as a carrier. METHODS: The permeability of rebamipide was evaluated using an in vitro diffusion chamber system, and the effects of some absorption enhancers on the permeability via colon were further investigated. The release of rebamipide from chitosan or gelatin capsule was studied by Japan Pharmacopoeia rotating basket method. The colonic and plasma concentrations were analyzed by high performance liquid chromatography (HPLC) to evaluate colon-targeting action after oral administration of various dosage forms, and rebamipide with absorption enhancers in chitosan dosage forms. RESULTS: The permeability of rebamipide across the jejunal or ileal membranes was higher than the colonic membranes. Both sodium laurate (C12) and labrasol signifi cantly increased permeability across the colon membranes. On the other hand, the release of rebamipide from chitosan capsule was less than 10%totally within 6 h. The area under concentration-time profile of drug in the colon mucosa using chitosan capsules (AUCLI, 1 6011.2 ng·h/g) was 2.5 times and 4.4 times greater than using gelatin capsules and CMC suspension, respectively. Meanwhile, the area under concentration-time profile of drug in the plasma (AUCPL) was 1016.0 ng·h/mL for chitosan capsule, 1887.9 ng·h/mL for CMC suspension p and 2163.5 ng·h/mL for gelatin capsule. Overall, both AUCLI and AUCPL were increased when C12 was co-administrated, but the increase of AUCLI was much greater; the drug delivery index (DDI) was more than 1 compared with simple chitosan capsule group. CONCLUSION: There was a regional difference in the permeability of Rabamipide across the jejunum, ileum and the colon, and passive

关键词： Rebamipide Diffusion chamber Permeability sodium laurate Chitosan capsule Colon-specific delivery

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A New Rat Model of Cerebral Infarction Based on the Injury of Vascular Endothelial Cell

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Chinese Journal of Integrated Traditional and Western Medicine 2005年第3期11卷 195-200页

作者：陈懿葛金文邓冰湘 Department of Physiology Hunan University of Traditional Chinese Medicine Department of Science and Technology Hunan University of Traditional Chinese Medicine

Objective： A new rat model of cerebral infarction was developed to elucidate the contribution of vascular endothelial cell during focal cerebral infarction formation. Methods： Forty-eight Sprague-Dawley （SD） rats were randomly divided into the model group, sham operation group, and control group for indexes observation of triphenyltetrazolium chloride （TTC） dyeing, neurological deficit, plasma tissue-type plasminogen activator （tPA） activity, plasminogen activator inhibitor （PAl） activity, thromboxane B2（TXB2） content, and 6-keto-prostaglandin （6-keto-PGF1α） content. Results：（1） The highest neurological score appeared at 6 h after operation, descending significantly at sequential time. （2） Using TTC dyeing and optical microscope technique, pathological changes in brains were observed. （3） Compared with control group and sham operation groups, there was a decrease in tPA activity of model rats at the initial 12 h after injection of sodium laurate （P〈0.05）, PAl activity decreased markedly in the model group at 24 h after injection of sodium laurate. （4） In plasma TXB2 concentration reached the highest level compared at 6 h after injection of sodium laurate, but there were not obvious differences in plasma 6-keto-PGF1α concentration among all groups （P〉 0.05）. Conclusion. Focal cerebral infarction in rats could be induced by some sodium laurate, showing ischemic cerebrum necrosis, function disorder of vascular endothelium-platelet, fibrinolysis abnormality. This model could play an important role in researching the contribution of vascular endothelial cell during cerebral infarction development, preventing and curing by traditional Chinese medicine.

关键词： sodium laurate cerebral infarction vascular endothelial cell

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A New Rat Model of Cerebral Infarction Based on the Injury of Vascular Endothelial Cell

A New Rat Model of Cerebral Infarction Based on the Injury o...

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湖南省生理科学学会2004年度学术年会

作者：陈懿葛金文邓冰湘 Department of Physiology Hunan University of Traditional Chinese Medicine Changsha410007China Lab of Vascular Biology Hunan University of Traditional Chinese MedicineChangsha410007China Department of Physiology Hunan University of Traditional Chinese MedicineChangsha410007China

＜正＞Objective A new rat model of cerebral infarction was developed to elucidate the contribution of vascular endothelial cell during focal cerebral cerebral infarction formation. Methods Forty-eight Sprague-Dawley（SD） rats were randomly divided into the model group with 21 rats in which sodium laurate was injected into the left internal carotid artery, sham operation group with 21 rats in which sodium laurate was substituted with 0.9% sodium chloride solution, and control group with 6 rats without any treatment. 7 rats were respectively executed for indexes observation in model group and sham operation group at 6, 12, 24 h after operation, as well as 6 rats in control group. These indexes included triphenyltetrazolium chloride （TTC） dyeing, neurological deficit, plasma tissue-type plasminogen activator（tPA） activity, plasminogen activator inhibitor（PAI） activity, thromboxaneB2 （TXB2） content, and 6-keto-PGF1 α content.

关键词： sodium laurate cerebral infarct vascular endothelial cell

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