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OBJECTIVE:To optimize the formulation optimization of Nicorandil sustained-release matrix tablet,and evaluate its drug release properties in vitro. METHODS:Based on single factor test,powder direct compression method was used,using nicorandil cumulative release rate (Q) in 1,4,8,12 h as evaluation indexes,central composite design-response surface method was adopted to optimize the amount of hydroxypropyl methylcellulose(HPMC)and ethyl cellulose(EC);Q values within 12 h in different pH (1.0,5.0,6.8,7.4) media were compared. RESULTS:The optimized formulation (every tablet) was nicorandil 10 mg,HPMC 150 mg,EC 90 mg,microcrystalline cellulose 80 mg,lactose 60 mg,magnesium stearate 2%. Q1 h,Q4 h,Q8 h and Q12 h of the obtained formulation were 23.6%,51.3%,83.7% and 96.9%,respectively;deviation from the predicted values were 2.1%,1.6%,1.0%,0.2%. Q values were similar in pH 1.0-7.4 at different time points. CONCLUSIONS:The obtained Nicor-andil sustained-release matrix tablet by optimal formulation shows sustained-release effect,and the change of pH 1.0-7.4 has no in-terference in the release characteristics of main drug.
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Objective To evaluate the effect of 8% emulsified isoflurane preconditioning on renal ischemia-reperfusion (I/R) injury in rats.Methods Thirty-two male Sprague-Dawley rats,aged 10-13 weeks,weighing 220-300 g,were randomly divided into 4 groups (n =8 each):sham operation group (group S); I/R group;emulsified isoflurane preconditioning group (group E) ; intralipid preconditioning group (group I).Renal ischemia was induced by occlusion of the left renal pedicle for 45 min with atraumatic microclips followed by 3 h reperfusion.8 % emulsified isoflurane and 30 % intralipid 4 ml· kg-1· h-1 were infused intravenously for 30 min followed by 15 min washout before renal UR in groups E and I,respectively.Arterial blood samples were taken at 3 h of reperfusion to determine the concentrations of serum creatinine (Cr),cystatin C (Cys C),TNF-α,IL-6 and IL-10.The animals were then sacrificed and left kidneys were removed and stained with hematoxylin-eosin for microscopic examination and assessment of necrosis of renal proximal convoluted tubules (0 =normal,4 =necrosis of whole segment of proximal convoluted tubules).Results Compared with group S,the serum Cr,Cys C,TNF-α,IL-6 and IL-10 concentrations and severity of necrosis of renal proximal convoluted tubules were significantly increased in groups I/R,E and I (P ＜ 0.05).The serum Cr,Cys C,TNF-α and IL-6 concentrations and severity of necrosis of renal proximal convoluted tubules were significantly lower,while the serum IL-10 concentration was higher in group E than in groups I/R and I (P ＜0.05).There was no significant difference in the indexes mentioned above between groups L and I/R (P ＞ 0.05).The damage to renal tissues was less serious in group E than in groups I/R and L.Conclusion Preconditioning with 8 % emulsified isoflurane can attenuate renal I/R injury by inhibiting inflammatory responses in rats.
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OBJECTIVE: To compare the pharmacokinetics and relative bioavailability between ganciclovir-chitosan eye drops and ganciclovir eye drops in rabbit eyes. METHODS: Japan big-eared rabbits were randomly assigned to the receive 50 ?L ganciclovir-chitosan eye drops (experiment group) or ganciclovir eye drops (control group) in both eyes. The rabbit tears,corneas and aqueous humor were collected at different time for the determination of drug concentration by RP-HPLC. The pharmacokinetics parameters were calculated as well. RESULTS: In the experimenal group,the half-life(t1/2) in tears,corneas and aqueous humor were 15.41,45.21,59.43 minutes,respectively versus 16.22,32.55,and 48.53 minutes in the control group. The Cmax were 2.03 ?g?mL-1 and 1.22 ?g?mL-1,respectively. In the experimental group,the AUC0→240 in tears,corneas and aqueous humor were 1.66,1.89,and 2.77 times those in control group. CONCLUSION: The bioavailability of ganciclovir-chitosan eye drops was significantly higher than that of ganciclovir eye drops.
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0.05)and the main pharmacokinetic parameters were close to each other.CONCLUSION:No stereoselective differences lies in the pharmacokinetics processe of amlodipine enatiomers in the body of rabbits.
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OBJECTIVE:To get to know medical staff's recognition of ADR monitoring in our city.METHODS:The concept,reporting consciousness,range and reasons for ADR reporting,reporting processes,professional organization of ADR and law consciousness of ADR etc.were investigated in400medical staff members through questionnaires on“Medical Staff's Recognition Degree to the Monitoring of ADR”.RESULTS:The medical staff in our city were basically clear about the range and the reasons for ADR reporting,but they lacked adequate recognition to the concept and the consciousness of ADR report?ing,they were not clear about the reporting processes and the organization of ADR and they lack the law consciousness of ADR reporting.CONCLUSION:It is necessary to carry out training on professional knowledge,laws and regulations of ADR among the medical staff so as to enhance their recognition to ADR monitoring and to make ADR monitoring as a self-conscious behavior.
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OBJECTIVE:To prepare ganciclovir hydrochloride chitosan eye drops and establish its quality control method.METHODS:The eye drops was prepared using chitosan as thickening agent and synergist with ganciclovir as principal agent.The content of ganciiclovir was determined by HPLC.The stability of the preparation was investigated as well.RESULTS:The prepared eye drops was colorless transparent glutinous limpid liquid with its identification items all up to the related standards stipulated in Chinese Pharmacopoeia(2005 edition).The linear range of ganciclovir was 5～80 mg?L-1(r=0.999 9) with average recovery of 99.02%(RSD=0.71%).The preparation was stable under light with all its indexes showed no obvious change in the accelerated test at 6 month.CONCLUSION:The preparation technology is simple and feasible and the quality of preparation is stable and controllable with a validity duration tentatively set at 2 years.
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OBJECTIVE:To construct the database of“The Time and Age Limit in the Use of Common Orally Adminis-tered Drugs”in order to guide the rational drug use in patients.METHODS:The frequently used instructions of common orally administered drugs in the hospital where the authors worked were collected,and then were classified and listed according to the elements in“The Time and Age Limit in the Use of Common Orally Administered Drugs”,and further summarized according to the basic knowledge in drug administration.RESULTS:Ante cibum drugs accounted for22.2%,post cibum drugs11.7%,either ante cibum or post cibumor or unmarked drugs59.4%,bedtime drugs6.7%,wholly swallowed drugs12.2%,chewed drugs1.7%,children restricted drugs32.2%,and the drugs taken once daily with the set time accounted for13.9%.CONCL_ USION:The construction of“The Time and Age Limit in the Use of Common Orally Administered Drugs”database can guide patients to use medicine rationally.
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OBJECTIVE:A RP-HPLC method to determine the contents of furacilin and ephedrine hydrochloride in compound furacilin nasal drops was established METHODS:Chromatographic detection was performed with a mixture of methanol-water-triethylamine-acetic acid(12∶88∶0 2∶1) as mobile phase and Kromasil C18(4 6mm?250mm,5?m) as separate column Chloramphenicol was selected as internal standard and the detection wavelength was 254nm RESULTS:The ingredients of compound furacilin nasal drops and internal standard were well separated within 18min Good linearities and recoveries for furacilin and ephedrine hydrochloride were obtained in their assay ranges CONCLUSION:The RP-HPLC method was found to be simple,accurate and suitable for the quality control of compound furacilin nasal drops