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??OBJECTIVE To evaluate the effects of hormone replacement therapy(HRT) on the quality of life in climacteric women.METHODS The 202 patients were collected and divided into three groups according to whether or not they were treated with HRT: group 1 (not HRT), group 2 (HRT for the first time), group 3 (HRT for more than one year). All patients received follow-up visiting once per three months for one year. They were evaluated by the professionals through Kupperman index(KI), menopause-specific quality of life questionnaire(MENQOL), self-rating anxiety scale(SAS), self-rating depression scale(SDS). All patients were guided to improve the way of life.RESULTS After a year, KI, MENQOL and SAS in the three groups were improved significantly (P=0.003, 0.007, 0.014). KI and MENQOL were improved earlier than SAS. SDS was improved but not significantly(P=0.109). KI, MENQOL, SAS and SDS of patients in group 1 were improved significantly, but improved more weakly than those in group 2 and group 3. There is negative correlation between HRT and the values of every scale, and there is positive correlation between culture degree and SAS, SDS score values. CONCLUSION HRT canim prove the quality of life in climacteric women. The improvement in physical symptoms is earlier than that in mental symptoms. Anxiety and depression are more likely to occur in menopausal patients with high degree of education. Traditional Chinese medicine, exercise therapy and physical rehabilitation can be used as an auxiliary treatment for patients who are unable or unwilling to accept the HRT.     

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??OBJECTIVE To establish an RP-HPLC analytical method for simultaneous determination of crysoeriol and centaureidin in the aeries parts of Echinops integrifolius. METHODS The separation was achieved on a Kromasil C₁₈ column ( 4. 6 mm??250 mm,5 ??m)at 30 ?? using acetonitrile-water-acetic acid solution (35??65??2) as mobile phase at a flow rate of 1.0 mL??min^-1 and 350 nm as the detection wavelength. RESULTS The linear ranges of crysoeriol and centaureidin were 0.4-2.4 mg??L^-1(r=0.999 8), 0.6-2. 6 mg??L^-1 (r=0.999 9), respectively. The average recoveries (n=6) were 91.6% and 92.7%, and RSDs were 1.37% and 1.08% respectively. CONCLUSION The methodology validation shows that this method is accurate,simple and reliable,which is applicable for the simultaneous determination of two flavonols crysoeriol and centaureidin in the aeries parts of Echinops integrifolius.     

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??OBJECTIVE To analyze the regularity, clinical reactions and outcomes of the adverse reaction of sorafenib to provide reference for safe medication in clinical practice. METHODS The case reports of sorafenib ADR which were published at international medical academic periodicals during 2006-2016 were collected and analyzed statistically in respect of gender, age, disease informations, clinical manifestation and RESULTS of treatment. RESULTS A total of 93 adverse reactions were identified and included in the analysis, 22 cases were unexpected ADR. The ADR happened in male was more than in female, and the age of 61-80 was the most common population (45.16%). The ADR was mostly happened in 1 month (71.11%) after therapy. Lesions of skin and its appendants were the most commonly reported ADRs (51.52%), followed by the lesions of digestive system (22.73%) ,which reported the most of the death cases (n=19 , 6 death). The ADR correlation rate was high in these case reports. CONCLUSION Multiple organ systems are involved in the ADRs of sorafenib, amd careful clinical observation and symptomatic treatment in time are necessary.     

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??OBJECTIVE To examine the in vitro release profile and in vivo retention of estradiol vaginal thermosensitive gel (E2-VTG).METHODS E2-VTISG was prepared by cold dissolving method.The dynamic membrane dialysis method and HPLC-fluorometric method were used to determine the in vitro release characteristic of the estradiol vaginal thermosensitive gel.CRi Maestro was applied to evaluate the retention of E2-VTG in ICR mice with IR820 as the fluorescent marker. RESULTS Estradiol could be released slowly from the thermosensitive gel and the release profile was fitted with Higuchi equation. It was speculated that estradiol was mainly released through diffusion.NIR imaging and fluorescence quantitative analysis showed that thermosensitive gel could reside in vagina for at least 8 h. CONCLUSION Estradiol thermosensitive gel can prolong the drug residence time in vagina and sustain the drug release rate.     

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??OBJECTIVE To prepare the total alkaloids of Strychni Semen(TASS)-total glucosides of Paeony(TGP) gel and study its in vitro transdermal absorption of two alkaloids(strychnine and brucine) after the combination of TASS and TGP. METHODS The excised abdominal skin of mice was used as the permeation model. Utilizing the modified Franz diffusion cell, the suitable receiving solution was elected to test the content of two alkaloids by HPLC, and thus the percutaneous rates and permeability coefficients were obtained. RESULTS 20% Ethanol-normal saline was taken as receiving solution. With combination use of TASS and TGP, the penetration quantities of strychnine and brucine in different (1:1,1:3,1:6) gels were felled by 22.7%,48.4%,69.1% and 5.93%,23.8%,80.7% after 24 h. And with the increase of compatibility proportion, infiltration rate and skin retention rate also gradually reduced. CONCLUSION The compatibility of TASS and TGP drug delivery can reduce the toxic ingredients through capacity, there is a “attenuated” effect, the best ratio is 1:6.     

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??Quercetin could affect both the in vivo and in vitro transport of a variety of commonly used drugs by modulating the uptake transporter organic anion transporter polypeptides (OATPs), organic anion transporters (OATs), efflux transporter P-glycoprotein (P-gp), multidrug resistance-related protein (MRP) and breast cancer resistance protein (BCRP), respectively. Quercetin can regulate various drug transporters, thereby affecting other drugs in vivo process.     

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??OBJECTIVE To establish dose-related lung inflammatory injury in rats model with intratracheal atomization of lipopolysaccharide (lipopolysaccharides, LPS). METHODS Four groups of 4 rats were subjected to solvent or a single dose of LPS by intratracheal route using a IA-1B-2 inches-microsprayer. The male rats received 200 ??L solvent (control), LPS solutions (15, 5, 0.5 mg??kg^-1). All rats were sacrificed 24 h after dose administration, biochemical analysis and cell counts on bronchoalveolar lavage fluid (BALF) were performed on each rat. Lung, trachea and kidney were examined histologically. Serum chemistry profiles of creatinine, ALB, Na, K, Cl^- were detected. RESULTS Cell counts in BALF showed LPS groups had different degrees of inflammatory reaction. The alkaline phosphatase and total protein concentration were higher in LPS high dose group compared with other groups. In addition, the concentration of TNF-?? increased consistently with LPS dose and has statistical significance compared with the control group. Histopathology findings demonstrated that LPS produced an accumulation of foamy macrophages in the lungs and high degree of inflammation. CONCLUSION The results recommends intratracheally atomizing doses of LPS in rats model produced ranks of lung inflammatory injury.     

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??To improve the in vitro dissolution and in vivo absorption as well as the bioavailability after oral administration by increasing the solubility with the formation of solid dispersion remains a great challenge for the oral dosage form design of poorly water-soluble drugs. Compared with the other pharmaceutical techniques in improving the solubility for poorly water-soluble drugs, priorities are usually given to solid dispersion for its manufacturing convenience. Following the characteristics introduction, we were focused this review on the novel carriers and advanced techniques used for preparing solid dispersions. Amphiphilic polymers used as novel solid dispersion carriers are Solutol HS 15, Soluplus and poly [MPC-co-BMA]. Inorganic materials like magnesium aluminum metasilicat, mesoporous silica microparticle and mesoporous magnesium carbonate are introduced together with the advanced solid dispersing techniques such as supercritical fluid technology, high speed electro-spinning and microenvironmental pH modified technology.     

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??OBJECTIVE To investigate the chemical constituents of the seeds of Lepidium apetalum Willd. METHODS The compounds were isolated and purified by Diaion HP-20, Toyopearl HW-40, MCI Gel CHP-20, ODS, silica gel chromatography combined with Pre-HPLC and the structures were identified on the basis of spectral data and physiochemical properties. RESULTS Sixteen compounds were isolated and identified from the water extract as catechol(1), protocatechuic aldehyde(2), 2-phenyl acetamide(3), methyl- 5-hydroxypyridine-2-carboxlate(4), benzylcarbamic acid(5), N-benzylacetamide(6), raphanuside C(7), 1-phenyl-1,2-ethanediol(8), 2-(4-hydroxyphenyl)-ethanol(9), isorhamnetin-7-O-??-L-rhamnopyranoside(10), kaempferol(11), methyl 2,4,6-trihydroxybenzoate(12), 2-(4-hydroxyphenyl)acetonitrile(13), syringic acid(14), protocatechuic acid(15), and methyl sinapate(16). CONCLUSION Compounds 1-16 are isolated from this plant for the first time.     

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??OBJECTIVE To develop a rapid DNA detection kit for DNA extraction and PCR identification of Panax ginseng C.A. Mey. METHODS The classical DNA extraction and PCR identification METHODS for Panax ginseng C.A. Mey were modified, and the compositions and reaction conditions of the kit were determined. In addition, the specificity, stability, sensitivity, and repeatability of the kit were evaluated. The genomic DNAs of genuine and counterfeit ginseng goods were extracted by the kit and PCR was performed to identify the authenticity. The purity of the extracted DNA was detected by UV spectrophotometry. Finally, commercially available ginseng samples were verified. RESULTS The purity of the genomic DNA extracted by the kit was (1.73??0.13)(OD₂₆₀/ OD₂₈₀), and a fragment between 150 and 200 bp could be amplified only from authentic Panax ginseng C.A. Mey. The specificity of the kit was 100%. The repetitive experiments showed that the average intra-assay CV% and inter-assay CV% of the kit were 2.38% and 2.62%, respectively. The DNA in solutions diluted by 200 times could still be detected. Stability experiment proved that repeated freeze-thawing for 20 times had no significant effect on the activity of this kit and the test sample could be stored at -20 ?? for one year. The specificity test confirmed that 8 samples among the 10 commercial products were genuine, and 2 were counterfeit. CONCLUSION The nucleic acid extraction and purity of the DNA detection kit can meet the requirement for identification of Panax ginseng C.A. Mey.The kit has good specificity, high sensitivity, and good stability, so it is suitable for the rapid detection of Panax ginseng C.A. Mey.     

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??OBJECTIVE To investigate the effect of high-fat and high-calorie diets on pharmacokinetics of cefuroxime axetil in healthy Chinese subjects. METHODS A randomized, open-label, single dose and two-way crossover clinical study was conducted. Twelve healthy subjects were randomly divided into two groups, each of which includes six males, then they were given 250 mg of cefuroxime axetil respectively before and after meal. Blood samples were collected at different time points before and after drug administration. The concentration of cefuroxime in plasma was determined by HPLC-MS/MS. The pharmacokinetic parameters were calculated by DAS3.2.8 and were analyzed by DAS3.2.8 and SPSS19.0. RESULTS The main pharmacokinetic parameters of fasting and postprandial were as follows: AUC_0-t was (11 402.8??3 556.7) and (18 565.7??2 917.9) ng??h??mL^-1, AUC_0-?? was (11 492.5??3 581.8) and (18 754.7??2 885.6) ng??h??mL^-1, ??_max was (3 406.7??1 188.9) and (5 439.2??1 118.2) ng??mL^-1, t_max was (2.01??0.64) and (2.08??0.79) h, t_1/2 was (1.66??0.38) and (1.60??0.60) h, respectively. The main pharmacokinetic parameters between fasting and high-fat meal groups were analyzed by SPSS19.0 software. There was significant difference in AUC_0-t, AUC_0-?? and ??_max(P<0.01), and no significant difference in t_max and t_1/2 (P>0.05). The ??_max and AUC were increased by 59.7% and 63.2% respectively, t_max is almost unchanged. The equivalence analysis was performed with DAS.3.2.8 software, the 90% confidence intervals for the ratios of AUC_0-t, AUC_0-?? and ??_max for the postprandial/fasting were 137.6%-217.5%, 138.4%-217.3%, 135.4%-207.6%, respectively. None of them fall within the acceptable interval of 80%-125%. CONCLUSION High-fat and high-calorie diets can significantly improve the extent of absorption of cefuroxime axetil in vivo, but does not affect the absorption rate of cefuroxime axetil.     

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??OBJECTIVE To investigate the pharmacokinetics of matrine injection by different routes of administration. METHODS Twenty healthy SD rats were enrolled in this study. They were randomly divided into two groups and received intraperitoneal and intravenous administration of matrine injection at dose of 15 mg??kg^-1 respectively. Blood samples (0.3-0.4 mL) were immediately collected into heparinized tubes before injection and at 0.033, 0.083, 0.167, 0.333, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 12 h after injection. Plasma sample concentrations were determined by a validated LC-MS/MS method. The pharmacokinetic parameters including AUC_0-12, AUC_0-??, MRT_0-12, MRT_0-??, t_1/2, Vd, CL and ??_max were calculated. RESULTS The main pharmacokinetic parameters for matrine after intraperitoneal and intravenous administration at dose of 15 mg??kg^-1 were as follows:AUC_0-12 (10 166??2 426), (12 217??2 968) ng??mL^-1??h;AUC_0-?? (10 230??2 432), (12 300??3 031)- ng??mL^-1??h;MRT_0-12 (1.91??0.41), (2.14??0.54) h;MRT_0-?? (2.01??0.41), (2.26??0.64) h; t_1/2(2.26??0.89), (2.60??1.25) h;Vd(4 998??2 010), (6 175??2 540) mL;CL (1 531??315.0), (1 727??475.6) mL??h^-1??kg^-1; ??_max (5 246??1 187), (8 503??1 101) ng??mL^-1, respectively. The bioavailability of intraperitoneal administration is 83.21%. CONCLUSION No significant differences were observed in AUC, MRT, t_1/2 and CL values of matrine between different administrations except for ??_max and Vd.     

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??OBJECTIVE To evaluate the bioequivalence of cefdinir suspension and reference cefdinir capsule in Chinese healthy male subjects.METHODS A single oral dose of 100 mg cefdinir suspension or cefdinir capsule was given to 24 subjects according to a 2-way crossover design. The plasma concentrations of cefdinir were determined by UPLC-MS/MS. The pharmacokinetic parameters were calculated and bioequivalence was compared by WinNonlin 6.3 program. RESULTS The main pharmacokinetic parameters of cefdinir suspension and cefdinir capsule were as follow: ??_max were (1 034.78??358.17), (969.71??297.38) ng??mL^-1;t_max were (2.98??0.60), (3.44??0.70) h; AUC_0-12 were (4 911.24??1 675.30), (4 522.35??1 600.13) ng??h??mL^-1; AUC_0-?? were (5 026.24??1 735.32),(4 680.69??1 699.93) ng??h??mL^-1;t_1/2 were (1.71??0.23), (1.79??0.39) h. The 90% confidential interval of ??_max, AUC_0-12, AUC_0-?? of tested formulation were 95.6%-115.3%, 99.9%-117.2%, 99.0%-116.0%. CONCLUSION The two formulations are bioequivalent.     

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??OBJECTIVE To study the pharmacokinetics of pirfenidone in Chinese healthy volunteer after a single dose and multiple-dose administration. METHODS Twelve Chinese healthy volunteers were randomly divided into low, medium and high dose groups(200, 400, 600 mg). The multiple-dose group was administrated with pirfenidione 400 mg three times daily for 5 d. Intensive blood sampling was performed from 12 volunteers within 12 h after the single dosing and the last dose of the multiple dosing. HPLC-MS/MS was used to determine the plasma concentrations of pirfenidone. The pharmacokinetic parameters were calculated by DAS software. RESULTS The main pharmacokinetic parameters of pirfenidone after single-dose administration of 200,400,600 mg qd as follows: ??_max were(5.00??1.42),(9.43??2.74)and(14.14??3.36)mg??L^-1;t_max were(0.57??0.33),(0.60 ??0.30)and(0.60??0.38)h;t_1/2 were(2.16??0.77),(2.15??0.75)and(2.01??0.76)h; AUC_0-?? were(13.87??7.79),(29.26??12.02)and(45.85??20.25)mg??h??L^-1;AUC_0-12 were?(13.27??7.08),(27.92??10.56)and(43.98??18.14)mg??h??L^-1,respectively. The main pharmacokinetic parameters after 400 mg tid for 5 d were as follows: ??_max was(9.46??2.77)mg??L^-1,??_min was(1.14??1.11)mg??L^-1,t_max was(0.52??0.34)h,t_1/2 was(1.93??0.63)h,AUC_0-?? was(26.74??13.49)mg??h??L^-1,AUC_0-12 was (25.79 ??12.34)mg??h??L^-1,AUC_sswas(23.53??10.59)mg??h??L^-1.CONCLUSION The pharmacokinetic parameters of pirfenidone show that ??_max and AUC were linear in the dose range from 200-600 mg and the pharmacokinetic parameters were similar as reference.
     

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??OBJECTIVE To evaluate the bioequivalence of tested and reference torasemide tablets in healthy male volunteers. METHODS A single oral dose of the two formulations was given to 24 healthy male volunteers according to a randomized crossover design. Plasma drug concentrations were determined by HPLC-MS. RESULTS The pharmacokinetic parameters of torasemide of the two preparations were as follows: ??_max (1 408.29??337.27) and (1 487.86??360.24) ng??mL^-1, t_max (0.90??0.42) and (1.03??0.50) h, t_1/2(4.43??0.57) and (4.43??0.60) h, MRT (3.90??0.60) and (4.01??0.72) h, AUC_{0-24 h}(3 886.86??865.99) and (3 906.06??761.72) ng??h??mL^-1, AUC_0-?? (3 936.57??903.93) and (3 956.96??789.98) ng??h??mL^-1, respectively. The relative bioavailability of tested torasemide tablets were (99.8??11.7)% and (99.7??12.0)% when calculated by AUC_{0-24 h} and AUC_0-??, respectively. CONCLUSION The two formulations of torasemide are bioequivalent in healthy Chinese volunteers.     

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??OBJECTIVE To assess the impact of chrysin and naringenin on the pharmacokinetics (PK) of saquinavir (SQV), a substrate of P-glycoprotein (P-gp), in rats. METHODS Fifteen rats were randomized into 3 groups of equal size, and administered orally 30 mg??kg^-1 SQV with or without 40 mg??kg^-1 chrysin or naringenin. The PK of SQV was assessed using non-compartmental analysis and the plasma concentrations of three groups were determined by LC-MS/MS. RESULTS The PK parameters values of SQV, SQV+ naringenin, SQV+ chrysin are as follows:AUC_0-t,882.91,861.32,934.84 ng??h??mL^-1; AUC_0-??,903.97,865.90,947.92 ng??h??mL^-1; ??_max,177.72,89.8,130.72 ng??mL^-1; t_max,1,2,0.5 h;t_1/2,11.73,12.61,13.33 h; MRT_0-??,27.09,31.63,26.60 h; CL/F,21.65,21.45,20.62 mL??kg^-1??h^-1. CONCLUSION Double peak phenomenon is observed in the plasma SQV profiles. Our study demonstrates that chrysin and naringenin can not significantly affect the SQV oral bioavailability and SQV PK profiles in rats.     

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??OBJECTIVE To prepare compound aspirin and esomeprazole magnesium enteric-coated pellet capsules and evaluate the drug release in vitro/in vivo. METHODS The aspirin pellet cores were prepared by using extrusion-spheronization method, and the esomeprazole magnesium-containing drug pellets were prepared with fluidized bed. By using fluidized bed coating method, the two kinds of drug-containing pellets were respectively coated with enteric layer to obtain enteric-coated pellets. After determining the loading capacity by measuring drug content, the two kinds of drug-containing pellets were filled into No.1 capsules. In vitro release was evaluated by measuring release percentage. The in vivo release behavior was evaluated by determination of pharmacokinetic parameters in rats. RESULTS The cumulative release percentage of the two drugs was less than 5% in 2 h in 0.1 mol??L^-1 hydrochloric acid solution. The cumulative release percentage of aspirin was more than 70% in 45 min in pH 6.8 PBS and it was more than 80% in 30 min for esomeprazole magnesium. Aspirin was metabolized to salicylic acid in plasma and its main pharmacokinetic parameters were as follows:t_1/2=9.47 h, MRT_0-??=14.43 h, t_max=3.00 h, ??_max=51.34 mg??L^-1, AUC _0-24=703.39 mg??h??L^-1, AUC _0-??=860.52 mg??h??L^-1. The pharmacokinetic parameters for esomeprazole magnesium were as follows:t_1/2=3.72 h, MRT_0-??=7.44 h, t_max=1.50 h, ??_max=2.71 mg??L^-1, AUC_0-24=11.89 mg??h??L^-1, AUC_0-??=13.79 mg??h??L^-1. CONCLUSION The formulation of compound enteric-coated pellet capsules is reasonable, and the preparation technology has good reproducibility. The drug release is located in the intestinal tract, thus esomeprazole magnesium can antagonize the gastrointestinal side effects of aspirin and aspirin can produce better antithrombotic effect .     

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??OBJECTIVE To evaluate the pharmacokinetics characteristics and safety of antipsytrotic ziprasidone mesylate with single dose intramuscularly injected in healthy volunteers. METHODS A total of 12 healthy Chinese volunteers(male 6 cases and female 6 cases) were received intramuscularly single dose of ziprasidone mesylate, the dosage was 10 mg.Blood samples were collected at different time after intramuscularly injection.The concentrations of ziprasidone in serum were determined by LC-MS/MS, and the pharmacokinetic parameters were calculated. RESULTS The concentration-time curves of ziprasidone fitted to two-compartment model.The pharmacokinetic parameters were stated as follows, ??_max was (97.85?? 29.24) ng??mL^-1;t_max was (0.56??0.30)h;MRT was (5.35??0.96) h; t_1/2 was (4.29??0.88)h; AUC_0??t was (405.6??98.68) ng??h??mL^-1,AUC_0???? was (413.3?? 100.69)ng??h??mL^-1; CL was (25.50??6.10)L??h^-1; Vd was (157.48??47.60)L; Kel was (0.168??0.035)h. There were no significant differences of the parameters between the male and female subjects. The common adverse events were somnolence, nausea and weakness with the severity of mild to moderate. CONCLUSION The pharmacokinetic parameters in 12 healthy volunteers after intramuscular injection of 10 mg ziprasidone mesylate are in line with that reported in the literature. This medicine has effect of sedation, so that it could be used to control the excited agitation.     

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??OBJECTIVE To determine the concentrations of low molecular weight heparin (LMWH) in dermal and plasma of rats after administration of LMWH gel to evaluate its pharmacokinetic characteristics. METHODS The rats were treated with abdominal hair removal, followed by administrating LMWH gel. The concentrations of LMWH in the dermal of rats at different time points were measured by microdialysis technique combined with colorimetric method, and the concentrations of LMWH in the blood of rats at different time points were measured by cutting-tail method and Coatest Heparin Kit. RESULTS The LMWH t_max in dermis was 270 min, c_max was (4.40??0.54) IU??mL^-1, t_1/2 was (137.04??87.98) min, AUC_0-t was (911.76??330.69) IU??mL??min^-1, MRT_0-t was (322.67??40.94) min; the LMWH t_max in plasma was 540 min, c_max was (2.23??0.40) IU??mL^-1, t_1/2 was (294.99??183.74) min, AUC_0-t was (110.59??212.41) IU??mL??min, MRT_0-t was (422.48??52.96) min after LMWH gel was percutaneous administrated. CONCLUSION In vivo microdialysis technique combined with colorimetric method can be used for the evaluation of pharmacokinetic characteristics of LMWH gel. The method has the advantages of simple operation with high sensitivity and specificity. LMWH gel have the characteristics of slow transdermal penetration speed and stabilized concentration.
     

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??OBJECTIVE To investigate the pharmacokinetics of mycophenolate mofetil in patients with myasthenia gravis, and evaluate the correlation between plasma concentration and AUC. METHODS Eight myasthenia gravis patients older than 18 years old with normal liver and renal function were included in this study. Blood samples were collected at 0, 1, 2, 3, 4, 6, 8, 10 h after the patients were continuously given oral mycophenolate mofetil 2 g??d ^-1for one week. Plasma concentrations of mycophenolate mofetil were determined by HPLC method and data analysis was done by WinNonlin program. RESULTS The main pharmacokinetic parameters of mycophenolate mofetil were as follows??_max was (11.39??3.23) ??g??mL^-1,t_max was (1.5??0.8) h,AUC_{0-12 h} was (38.71??11.23) ??g??h??mL^-1. The ??₂ had the best correlation with AUC (r²=0.80) followed by ??₀ and ??₄ (r²=0.75). CONCLUSION The pharmacokinetics of mycophenolate mofetil has great inter-individual differences, but without significant difference with those in healthy volunteers and transplant patients. The ??₀ can be used for routine therapeutic drug monitoring because of convenience and feasibility.