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OBJECTIVE:To prepare Clopidogrel bisulfate tablets,and to optimize its formulation and technology. METHODS:The single factor test and compatibility test were used to optimize the fillers,disintegrating agents,adhesive,lubricants and prepa-ration technology;using sticking situation and disintegration time as indexes,the orthogonal test was used to optimize the amount of disintegrating agents [low substituted hydroxypropyl cellulose(L-HPC)],lubricants(hydrogenated vegetable oil and PEG6000), and the optimal technology was validated. The dissolution of prepared tablet and imported tablet(Plavix)in water,pH 2.0 hydro-chlorate buffer,pH 4.5 phosphate buffer(PBS)and pH 6.8 PBS were investigated,and influential factor test was conducted. RE-SULTS:Clopidogrel bisulfate tablets were prepared with dry granulating. The optimal formulation (1 000 tablets) was as follows as clopidogrel bisulfate 97.8 g,mannitol 84 g,amylum pregelatinisatum 36 g,L-HPC 8 g,hydrogenated vegetable oil 8 g, PEG6000 6 g;no tablet compressing sticking situation was found in prepared tablets and it owned medium disintegration time;ac-cumulative dissolution curves of prepared tablets in 4 kinds of medium were similar to those of Plavix;there were no significant dif-ference in results of influential factor test between prepared tablet and Plavix. CONCLUSIONS:Clopidogrel bisulfate tablets are prepared successfully,and the formulation is reasonable,practical,stable and controllable in quality.
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<p><b>OBJECTIVE</b>To study the pharmacokinetics and bioavailability of ginkgolides sustained-release tablet and conventional tablet in Beagle dogs.</p><p><b>METHOD</b>The concentrations of ginkgolides in plasma were determined by LC-MS. The main pharmacokinetic parameters of ginkgolides sustained-release tablet and conventional tablet in vivo were obtained using Pharmacokinetic software DAS 2.0.</p><p><b>RESULT</b>The C(max) of grinkgolide A in ginkgolide sustained-release tablet and conventional tablet were 443.51, 1 039.30 microg x L(-1), respecitvely. t(max) were 2.92, 1.08 h, respectively. AUC(0-12h) were 1 808.21, 2 041.37 h x microg(-1) x L(-1), respectively. MRT were 5.18, 3.18 h, respectively. The relative bioavailability of ginkgolides A was 88.58%. The C(max) of ginkgolide B in ginkgolide sustained-release tablet and conventional tablet were 407.13, 547.38 microg x L(-1), respectively. t(max) were 2.92, 1.08 h, respectively. AUC(01-12 h) were 1 987.31, 1 748.04 h x microg(-1) x L(-1), respectively. MRT were 6.05, 4.98 h, respectively. The relative bioavailability of ginkgolides B was 113.69%.</p><p><b>CONCLUSION</b>The ginkgolides sustained-release tablets have good sustained release characteristics and are bioequivalent to the reference formulation.</p>
Subject(s)
Animals , Dogs , Male , Area Under Curve , Biological Availability , Chromatography, High Pressure Liquid , Methods , Delayed-Action Preparations , Pharmacokinetics , Ginkgolides , Pharmacokinetics , Lactones , Mass Spectrometry , Methods , Quality Control , Tablets , Pharmacokinetics , Therapeutic EquivalencyABSTRACT
Objective:To investigate the reasonable approach and surgical indication for acute necrotizing pancreatitis(ANP)by analyzing the factors that affecting the mortality of ANP.Methods:One hundred and twelve patients with ANP were retrospectively divided into two groups-the dead and the survivors.Some parameters were analyzed statistically to reveal what's the reason for death.Results:The average age,sex ratio and onset of illness were similar between two groups.And the ratio of early shock,early adult respiratory distress syndrome (ARDS),high temperature,leukocytosis and high blood glucose between two groups were also similar between two groups(P＞0.05,respectively).The important factors that affecting the mortality were:①severity of pancreatic necrosis,②improper surgical approach,③incorrect surgical indication.Conclusion:The patiets with mild or moderate ANP should mainly receive conservative treatment for 48～72 hours.The early shock and ARDS should be redressed before surgical intervention.If the operation is unavoidable,the swelling pancreas should be dissected fully,which will provide sufficient drainage after operation,and duodenostomy should be performed during operation.
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Objective To investigate the clinical and histopathologic features of patients with primary gastrointestinal malignant lymphoma ( PGIML). Methods The clinical and histopathologic data of 22 patients with PGIML were reviewed and analyzed retrospectively. All cases were confirmed with histological specimen obtained from endoscopic biopsies or surgery. Results Abdominal pain was the most common presenting symptom, seen in 15 of 22 patients (68.2% ). The incidence of PGIML was highest in stomach, seen in 12 of 22 patients (54. 5% ). Modularity of the mucosal surface was the most common endoscopic finding, seen in 15 of 21 patients (71. 4% ). The positive rate of endoscopic biopsy for the diagnosis of PGIML was 52. 6% (10/19 biopsy cases). All cases were non-Hodgkins lymphomas ( NHL). Twenty cases were muco-sa associated lymphoid tissue (MALT) lymphoma, and 13 of 20 cases were extra-nodal marginal zone B-cell lymphoma of MALT. Conclusions Abdominal pain is the most common symptom and the stomach was the most common location in PGIML. Extra nodal marginal zone B-cell lymphoma of MALT is the main histopathologic feature. The prognosis of PGIML is related to the surgical procedure and the post operative chemotherapy.
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Objective To investigate the expression of neurokinin 3 receptor (NK 3R) in normal pancreas and pancreatic cancer, and to study the localization of this receptor in pancreatic cancer Methods The expression of NK 3R mRNA was investigated using reverse transcription polymerase chain reaction (RT PCR) in normal pancreas and pancreatic cancer tissues The protein level of NK 3R was investigated by Western blot Immunohistochemistry was used to localize expression site of NK 3R Results NK 3R mRNA was overexpressed in pancreatic cancer tissue when compared with normal pancreas NK 3R protein was 1 1?0 5 in normal pancreas and 14 6?3 6 in pancreatic cancer, P
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AIM: To investigate the expression of neurok inin-2 receptor (NK-2R) in normal pancreas and chronic pancreatitis (CP) tissues. The relation of expres sion of NK-2R with pain in CP was also evaluated. METHODS: CP tis sues were ob tained from 18 men and 7 women undergoing pancreatic head resection as a result of CP. Normal human pancreatic tissues were obtained from 20 patients (11 males/ 9 females). Real-time quantitative reverse transcription polymerase chain reacti on was used to determine the mRNA expression of NK-2R, Western blot analysis was used to determine its protein expression level, and immunohistochemistry was us ed to localize expression site of NK-2R protein. NK-2R mRNA level and pain were also analysed whether correlation exists. RESULTS: NK-2R mRNA and p rotein level were enhanced expressed in CP tissue samples compared with normal pancreas. Ove rexpression of NK-2R was related to the intensity ( r=0 59, P
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Objective To investigate the role of substance P (SP) and its neurokinin-1 receptor (NK-1R) in the pathophysiologic process of Crohn′s disease. Methods In 23 surgical patients of Crohn′s disease and 24 healthy controls, reverse transcription polymerase chain reaction (RT-PCR) was used to determine the mRNA expression of NK-1R, Western blot analysis was used to determine NK-1R protein expression levels, and immunohistochemistry was used to localize expression of NK-1R. Results Compared with normal gut NK-1R mRNA and NK-1R protein in Crohn′s disease were overexpressed. In Crohn′s disease moderate to strong intestinal NK-1R immunoreactivity was found in the lamina propria mononuclear cells, lymphoid follicles, and the surface and crypt epithelium, lymphoid follicles, submucosal vessels, smooth muscle and myoenteric plexus neurones. Conclusions In cases of Crohn′s disease, overexpression of NK-1R may disturb neuropeptides loop balance, and may be involved in the pathophysiological change in this disease.