Effect of iron dextran dispersible tablets on heart failure patients with iron deficiency / 中国临床药理学与治疗学

AIM: To evaluate the clinical effect of Iron Dextran Dispersible Tablets on patients with chronic heart failure who reduced ejection fraction after 24 weeks. METHODS: From January 2020 to June 2022, forty-five patients with heart failure complicated with iron deficiency and reduced ejection fraction were selected as the research objects. According to the random number table, they were randomly divided into control group and observation group.The control group was given routine anti-heart failure treatment such as Sacubitril Calsartan sodium tablets, while the observation group was given iron dextran dispersible tablets 50 mg three times a day on the basis of the anti-heart failure treatment of the control group for 8 weeks. The 6-minute walking distance, Hemoglobin, Serum Ferritin, N-terminal B-type natriuretic peptide precursor, Left Ventricular Ejection Fraction, Left Ventricular end Diastolic Diameter and 12-item Kansas City Cardiomyopathy Questionnaire (KCCQ-12) overall summary score and clinical summary score were compared between the two groups. RESULTS: There was no significant difference in baseline data between the two groups (P > 0.05). After treatment, the 6-minute walking distance in the observation group was longer than that in the control group, while the serum ferritin level in the observation group was higher than that in the control group. The N-terminal pro-B-type natriuretic peptide level in the two groups was lower than that before treatment, and the left ventricular end diastolic diameter was shorter than that before treatment, and the left ventricular ejection fraction, clinical comprehensive score and symptom score were higher than that before treatment. The difference was statistically significant (P 0.05). CONCLUSION: Iron Dextran Dispersible Tablets can improve the exercise endurance and quality of life of patients with chronic heart failure who reduced ejection fraction after 24 weeks.

Expert consensus on clinical application of GBE50 Dispersible Tablets for ischemic cardiovascular and cerebrovascular diseases / 中国中药杂志

Ginkgo biloba Extract( GBE50) Dispersible Tablets is a new standardized prescription,which is widely used in the treatment of ischemic cardiovascular and cerebrovascular diseases. However,there are still many problems in its clinical application.Rational and safe use of GBE50 Dispersible Tablets is pivotal to the medication safety and clinical prognosis of patients. This consensus has been jointly formulated by clinical experts of traditional Chinese medicine and western medicine in cardiovascular and cerebrovascular diseases and followed the Manual for the Clinical Experts Consensus of Chinese Patent Medicine published by the China Association of Chinese Medicine. The present study identified clinical problems based on clinical investigation,searched the research papers according to PICO clinical problems,carried out evidence evaluation,classification,and recommendation by GRADE system,and reached the expert consensus with nominal group technique. The consensus combines evidence with expert experience. Sufficient evidence of clinical problems corresponds to " recommendations",while insufficient evidence to " suggestions". Safety issues of GBE50 Dispersible Tablets,such as indications,usage and dosage,and medication for special populations,are defined to improve clinical efficacy,promote rational medication,and reduce drug risks. This consensus needs to be revised based on emerging clinical issues and evidencebased updates in practical applications in the future.

Full-factor design of experiment application in the development of printing ink for binder jetting 3D printed preparation / 药学学报

The development of printing ink is a challenge for binder jetting 3D printed preparations, which directly determines the quality of the printed product. This study adopted a 23 full-factor Design of Experiment (DoE) with three central points to optimize the printing ink composition of levetiracetam 3D printed dispersible tablet based on the concept of Quality by Design. Firstly, using polyvinyl pyrrolidone K30, glycerin and polysorbate 20 as independent variables based on 40% (v/v) isopropanol aqueous solution, and weight variation, hardness, friability and dispersion uniformity of the printed tablets were used as dependent variables. Then obtained the design space of the printing ink prescription by DoE model analysis, and the response optimizer was used to obtain the optimal printing ink prescription: isopropanol aqueous solution containing 0.1% (w/w) polyvinyl pyrrolidone K30 and 4.0% (w/w) glycerin. The jetting mechanism and wettability of the printing ink were analyzed, and different strengths of personalized 3D printed tablets were prepared and characterized, which verified the rationality of the printing ink formulation. This study provided a reference for the development of printing ink for binder jetting 3D printed preparations.

Economic Evaluation of Two Preparations of Mycophenolate Mofetil for Immunosuppressive Therapy after Renal Transplantation / 中国药房

OBJECTIVE：To evaluate the cost-effectiveness between Mycophenolate mofetil （MMF）dispersible tablets versus MMF capsules for the immunosuppressive therapy after renal transplantation ，and to provide reference for selecting more economical MMF preparations. METHODS ：Based on a systematic review about MMF dispersible tablets and MMF capsules for immunosuppressive therapy after renal transplantation （involving 6 clinical studies ），with simulation period of 6 months，Treeage 2010 software was used to establish decision tree model ，which included four states of graft normal ，acute rejection ，graft loss and death. Using QALYs as effect measurement index ，the cost-effectiveness analysis of two MMF preparations was carried out in combination with the cost data of West China Hospital of Sichuan University. Signal factor sensitivity analysis and probability sensitivity analysis were performed . RESULTS ：The incremental cost-effectiveness ratio of MMF capsules group to MMF dispersible tablets group was 623 111.614 0 yuan/QALY，which was higher than Chinese willing-to-pay value （212 676 yuan/QALY）；the results of sensitivity analysis supported the above results. CONCLUSIONS ：MMF dispersible tablets are better than MMF capsules in cost-effectiveness of immunosuppressive therapy after renal transplantation.

Effect of needling technique on diabetic gastroparesis and transmembrane protein 16A / 中国针灸

OBJECTIVE@#To observe the therapeutic effect of needling technique (acupuncture for regulating spleen and stomach) on diabetic gastroparesis (DGP), and to explore its possible mechanism.@*METHODS@#A total of 128 patients with DGP were randomized into an observation group (64 cases, 4 cases dropped off) and a control group (64 cases, 4 cases dropped off). On the basis of intervention on controlling blood glucose by western medication, needling technique was adopted at Zhongwan (CV 12), Zusanli (ST 36), Yinlingquan (SP 9), Xuehai (SP 10), Sanyinjiao (SP 6), Diji (SP 8), etc. in the observation group, once a day. Mosapride citrate dispersible tablet 5 mg was given orally 3 times a day in the control group. The treatment was given 6 times a week in the both groups, and totally 4-week treatment was required. Before and after treatment, the DGP symptom score, serum content of transmembrane protein 16A (ANO1) were observed, and the clinical therapeutic effect and the safety were evaluated in the both groups.@*RESULTS@#After treatment, the each subitem score (belching, abdominal distension, inappetence, nausea and vomiting, epigastric pain, abnormal defecation) and the total score of DGP symptom were decreased in both groups (<0.05), the subitem scores of belching, abdominal distension, inappetence, nausea and vomiting and the total score in the observation group were lower than those in the control group (<0.05). After treatment, the serum contents of transmembrane protein 16A were reduced in both groups (<0.05), and that in the observation group was lower than the control group (<0.05). The total effective rate was 86.7% (52/60) in the observation group, which was superior to 70.0% (42/60) in the control group (<0.05). Subcutaneous hematoma occurred in 5 cases in the observation group, which was improved after cold compress without other particular intervention.@*CONCLUSION@#The therapeutic effect of needling technique on improving symptoms in patients with diabetic gastroparesis is superior to mosapride citrate dispersible tablet, its mechanism may be related to alleviating the damage of interstitial cells of Cajal (ICC).

Micro and nanocrystalline cellulose based oral dispersible film; preparation and evaluation of in vitro/in vivo rapid release studies for donepezil

Oral fast-dispersible film was prepared by utlizing donepezil hydrochloride (drug) and various cellulose derivatives such as hydroxypropyl methyl cellulose (hypermellose) (HPMC), microcrystalline cellulose (MCC) and nanocrystalline cellulose (NCC) to treat Alzheimer's disease. NCC was synthesized by ultra-sonication method using MCC and this was converted to thinfilm formulation (NCC-F) using solvent casting technique. The interaction between the polymer and the drug was investigated by spectral analysis such as UV, FTIR, and 1H- NMR. FTIR confirmed that the compatibility of drug and polymer in ODF formulation. NCC-F has shown an average surface roughness of 77.04 nm from AFM and the average particle size of 300 nm from SEM analysis. Nano sized particle of NCC-F leads faster in vitro dissolution rate (94.53%) when compared with MCC-F and F3 formulation. Animal model (in vivo) studies of NCC-F formulation has reached peak plasma concentration (Cmax) up to 19.018 ng/mL in the span of (tmax) 4 h with greater relative bioavailability of 143.1%. These results suggested that high surface roughness with nanosized NCC-F formulation attained extended drug availability up to (t1/2) 70 h.

Study on puerarin dispersible tablet based on solubilization effect of glycyrrhizic acid / 中国中药杂志

Based on the fact that glycyrrhizic acid can form micelles in aqueous solution and play a role in solubilization, the optimal compatibility ratio between puerarin and glycyrrhizic acid was screened to prepare puerarin-glycyrrhizic acid dispersible tablets and investigate the dissolution of puerarin. The particle size, Zate potential and puerarin dissolution were compared among the micellar solutions with mass ratio of 7∶1, 6∶1, 5∶1, 4∶1, 3∶1 and 2∶1(puerarin to glycyrrhizic acid), and it was found that when the mass ratio of puerarin and glycyrrhizic acid was 5∶1, the micelle showed smallest particle size, uniform distribution, and largest puerarin dissolution, so mass ratio of 5∶1 was determined as the optimal condition. The formulation of puerarin-glycyrrhizic acid dispersible tablets was optimized by single factor and orthogonal test: puerarin 100.0 mg, glycyrrhizin 20.0 mg, polyvinylpolypyrrolidone 24.0 mg as disintegrating agent, microcrystalline cellulose 135.0 mg as stuffing bulking agent, hydroxypropyl methyl cellulose 18.0 mg as adhesive agent, magnesium stearate 2.7 mg as lubricant, and tablet weight of 300.0 mg. High-performance liquid chromatography(HPLC) method was used to determine the content of puerarin in dispersible tablets. Puerarin showed a good linear relationship(r=0.999 8) in the range of 15.5-248 g·L~(-1), with high precision(RSD<2.0%) and good repeatability(RSD<2.0%), and the recovery rate was 101.1%, RSD 0.89%. There was no significant difference in the quantity of puerarin in different batches of puerarin-glycyrrhizic acid dispersible tablets. When the artificial gastric juice was used as the dissolution medium, the dissolution of puerarin in puerarin-glycyrrhizic acid dispersible tablets could reach over 85% within 15 min. When phosphate buffer(pH 6.8) was used as the dissolution medium, the dissolution of puerarin in the puerarin-glycyrrhizic acid dispersible tablets had a faster dissolution rate in vitro, 99.8% in 30 min. Therefore, puerarin-glycyrrhizic acid dispersible tablets could improve the dissolution of puerarin in vitro due to the solubilization effect of glycyrrhizic acid.

Effects of combination therapy of calcium dobesilate dispersible and monosialotetrahex-osylganlioside sodium on serum inflammatory cytokines IL-6 and MCP-1 in elderly patients with painful diabetic peripheral neuropathy / 中国基层医药

Objective To observe the efficacy of combination therapy of calcium dobesilate dispersible and monosialotetrahexosylganlioside sodium on interleukin-6 (IL-6) and monocyte chemotactic protein-1 (MCP-1) in elderly patients with painful diabetic peripheral neuropathy.Methods From January 2012 to May 2017,in the Second People's Hospital of Lianyungang 70 patients of painful diabetic peripheral neuropathy,aged ≥60 years,were analyzed in this study.They were randomly divided into observation group (35 cases) and control group (35 cases).The observation group was treated with 40mg monosialotetrahexosylganlioside sodium dissolved in 250mL physiological saline,intravenous infusion per day,and oral calcium dobesilate dispersible 0.5g twice a day for two weeks.The control group was treated with methylcobalamin injection 0.5mg per day for two weeks.The clinical treatment effects and levels of IL-6 and MCP-1 were observed and compared between the two groups.Results After two weeks of treatment,the MDNS and MNSI scores of the observation group [(13.09 ± 5.38)points,(2.53 ± 1.19)points] were significantly lower than those of the control group [(18.31 ± 6.13) points,(4.19 ± 1.05) points,t =2.036,2.365,all P ＜ 0.05] and those before treatment [(21.26 ± 4.28) points,(5.40 ± 0.89) points,t =3.251,3.698,all P ＜ 0.05].The VAS-PI scores in the observation group [(6.24 ± 1.25) points,(4.13 ± 1.69) points] were significantly lower than those in the control group[(7.26 ± 1.28) points,(6.34 ± 2.65) points] at the first and second week (t =3.265,5.395,all P ＜ 0.05).The serum levels of inflammatory cytokines IL-6 and MCP-1 in the observation group [(15.16 ±0.88) ng/L,(157.19 ± 11.22) ng,/L] were significantly lower than those in the control group[(17.87 ± 1.19) ng/L,(198.21 ± 12.07)ng/L,t =2.152,1.365,all P ＜0.05]and those before treatment[(20.26 ± 1.05) ng/L,(260.44 ± 13.63) ng,/L,t =1.235,0.965,all P ＜ 0.05].Conclusion Combination of calcium dobesilate and mono-sialotetrahexosyl ganglioside may alleviate the sensory and pain sensations in patients with painful diabetic peripheral neuropathy,possibly by reducing the level of inflammatory cytokines IL-6 and MCP-1.

Comparison of effect of desloratadine citrate disodium tablets and loratadine dispersible tablets in treatment of patients with allergic rhinitis / 中国基层医药

Objective To compare the efficacy and adverse reactions of desloratadine citrate disodium tablets and loratadine dispersible tablets in treatment of patients with allergic rhinitis,and their influence on leukotriene B4(LTB4),interleukin-4 (IL-4),interleukin-10 (IL-10) and interferon gamma (INF-γ).Methods From June 2015 to June 2016,a total of 110 patients with allergic rhinitis in the Second People's Hospital of Cangnan County were selected and randomly divided into control group and observation group according to the digital table,with 55 cases in each group.The control group was given loratadine dispersible tablets,while the observation group was given desloratadine citrate disodium tablets.Both two groups were treated for 14 days.The clinical efficacy,adverse reactions and changes of LTB4,IL-4,IL-10,INF-γ levels before and after treatment were compared between the two groups.Results The total effective rate of the observation group was 94.5 ％,which was significantly higher than 80.0％ of the control group(x2 =6.310,P ＜ 0.05).The incidence rate of adverse reactions in the observation group was 16.4％,which was similar to 20.0％ in the control group.Before treatment,there were no statistically significant differences in LTB4,IL-4,IL-10,INF-γ levels between the two groups (all P ＞ 0.05).After 2 weeks of treatment,the levels of LTB4,IL-4,IL-10 and INF-γ in the observation group were (67.74 ±10.15) ng/L,(52.37 ± 5.12) μg/L,(81.26 ± 11.78) μg/L,(94.47 ± 7.87) μg/L,respectively,which in the control group were (80.32 ± 9.97) ng/L,(62.95 ± 5.45) μg/L,(96.32 ± 11.57) μg/L,(86.74 ± 7.63) μg/L,respectively,there were statistically significant differences between the two groups (t =7.124,5.262,4.654,3.718,all P ＜ 0.05).Conclusion Both desloratadine citrate disodium tablets and loratadine dispersible tablets can effectively treat patients with allergic rhinitis,improve the symptoms and physical signs,reduce the levels of LTB4,IL-4 and IL-10,increase the level of INF-γ,and the adverse reactions are less and slight,but the efficacy of desloratadine citrate disodium tablets is better than loratadine dispersible tablets.

Preparation Process and Formula of Kang'aiping Dispersible Tablets / 中国药学杂志

OBJECTIVE: To study preparation process and formula of Kang'aiping dispersible tablets. METHODS: Orthogonal designs were used to optimize water extraction process of traditional Chinese herbs from Kang'aiping pills, spray drying process of extracts and formulas of Kang'aiping dispersible tablets. RESULTS: The optimal water-extraction process is established by adding eight times water of raw materials, boiling for 60 min and extracting for two times. The optimal spray drying process parameters are that the density of the liquid extracts is 1.20 g•mL-1, inlet air temperature is 180 ℃ and outlet air temperature is 80 ℃. And the optimal formula consists of 37% microcrystalline cellulose, 5:1 of the ratio of croscarmellose sodium and PVPP, and 0.15% magnesium stearate. CONCLUSION: Formula and process optimized by using orthogonal experimental design is suitable for preparation of Kang'aiping dispersible tablets.

Pharmacokinetics study of mycophenolic acid in early renal transplant patients / 中国药学杂志

OBJECTIVE: To investigate the pharmacokinetic characteristics of enteric-coated sodium mycophenolate(EC-MPS) or mycophenolate mofetil (MMF) dispersible tablets after multiple oral doses in early renal transplant patients, providing references for the rational use of the study drugs in clinical practice. METHODS: Thirty-eight first-time renal transplant patients were selected and randomly divided into EC-MPS group (n=18) or MMF dispersible tablets group (n=19). The patients received EC-MPS (540 mg, q12h) or MMF dispersible tablets (750 mg, q12h), combined with tacrolimus and methylprednisolone to prevent acute rejection, respectively. Blood samples were collected at pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 h after oral administration on the postoperative day 5. Enzyme multiplied immunoassay technique (EMIT) was employed to determine the plasma concentration of MPA. The main pharmacokinetic parameters of the two durgs were assessed. RESULTS: Pharmacokinetic parameters on the postoperative day 5 of EC-MPS and MMF dispersible tablet were as follows: AUC0-12 h were(43.62±16.20) and(42.02±14.40)mg•h•L-1(P>0.05);ρmax were (17.85±11.32) and (13.96±5.11) mg•L-1(P>0.05);tmax were (2.72±1.74) and(1.32±0.42)h(P0.05); ρ12were(1.84±2.09) and (1.81±1.76) mg•L-1(P>0.05); CL were (14.12±5.30) and (19.66±5.99) L•h-1(P<0.05). Most of the patients revealed a second small peak in the 4-12 h after taking MPA in the two study groups. CONCLUSION: There are large individual differences of pharmacokinetic between EC-MPS and MMF dispersible tablets in early renal transplant patients. It is necessary to carry out therapeutic drug monitoring of MPA to guide the adjustment of drug dosage.

Effects of radix notoginseng saponin dispersible tablets combined with rivaroxaban in treatment of tibial fracture after operation and its effects on joint function and the leves of inflammatory factors / 中国生化药物杂志

Objective To study curative efficacy of radix notoginseng saponin dispersible tablets combined with rivaroxaban in treatment of tibial fracture after operation and its effects on joint function and the leves of inflammatory factors .Methods 90 patients of tibial fracture who received therapy from March 2014 to March 2016 in our hospital were selected.According to random number table,all elective surgery,those patients were divided into the observation group (n=45) and the control group (n=45),the control group was treated with radix notoginseng saponin dispersible tablets,while the observation group was treated combined with rivaroxaban.After two weeks of treatment, the hemorheology, inflammatory factors, joint function were compared between two groups.Results The patient swelling time and bed time in the observation group were shorter than the control group (P<0.05);after treatment,the levels of red cell volume, whole blood viscosity,fibrinogen in the observation group were lower than the control group (P<0.05);the levels of tumor necrosis factor TNF-α, IL-1,IL-6 in the observation group were lower than the control group (P<0.05);after treatment three months and six months,the Baird-Jackson scores in the observation group were higher than the control group (P <0.05).Conclusion Radix notoginseng saponin dispersible tablets combined with rivaroxaban is well for tibial fracture after operation,which can improve hemorheology,reduce the level of inflammatory factors,promote joint functional recovery.

Dissolution of Yinxingye Dispersible Tablets by Quantitative Analysis of Multi-components with Single-marker / 中国药师

Objective:To establish a quantitative analysis method for determining the dissolution of Yinxingye dispersible tablets by quantitative analysis of multi-components with single-marker ( QAMS) . Methods:A small glass method was adopted. Hydrochloric acid (0. 1 mol·L-1 ) was used as the dissolution medium, and the stirring speed was at 50 r·min-1 . HPLC-ELSD with gradient elu-tion combined with QAMS was used to simultaneously determine the dissolution of 3 total flavonoids ( artemisinin, quercetin and isorh-amnetin) and 4 total lactones (ginkgo esters and lactones a, b and c) in Yinxingye dispersible tablets. Results:Within a certain line-ar range, the relative correction factors (RCFs) of quercetin and isorhamnetin with the reference of artemisinin was 1. 873 and 0. 324, respectively, and the RCFs of lactones a, b and c with the reference of ginkgo esters was 2. 280, 1. 659 and 1. 429, respectively, and the repeatability was good under the different experimental conditions. There were no significant differences between the calculated val-ues by QAMS and those by the external standard method in 5 batches of Yinxingye dispersible tablets, and the results showed that the RCFs was authentic. The dissolution uniformity of Yinxingye dispersible tablets was good in 0. 1 mol·L-1 hydrochloric acid. Conclu-sion:The method is simple, accurate and reproducible in the dissolution determination of Yinxingye dispersible tablets.

Effect of Elemene Emulsion Injection Combined with Ganciclovir on Invasive Ability and TIMP-1 mRNA Expression in C6 Brain Tumor Stem Cells / 中国药房

OBJECTIVE:To study the effect of Elemene emulsion combined with ganciclovir on invasive ability and TIMP-1 mRNA expression in C6 brain tumor stem cells. METHODS:Cells with 3 generations were isolated and cultured from rats'C6 ma-lignant glioma cell lines,and immunocytochemistry was adopted to detect the protein expressions of stem cell markers CD133,Nes-tin. 20 rats were randomly divided into blank control group(normal saline),ganciclovir group(intragastrically administrated,216 mg/kg),Elemene emulsion injection group (intravenously injected in tail,36 mg/kg) and combination group (intragastrically ad-ministrated 216 mg/kg of ganciclovir+intravenously injected 36 mg/kg of Elemene emulsion injection in tail),5 in each group, once every day,for 10 d. After 2 h of last administration,the blood of rats in each group was collected,serum was isolated and co-cultured 24 h with C6 BTSCs in in vitro culture medium. Boyden invasion test was used to detect the invasive ability of C6 BTSCs,and real-time quantitative polymerase chain reaction(RT-PCR)method was used to determine the TIMP-1 mRNA expres-sion of C6 BTSCs. RESULTS:Cells with 3 generations had obvious protein expressions in CD133 and Nestin,indicating they were BTSCs. Compared with blank control group,the cell invasion rates of C6 BTSCs in ganciclovir group,Elemene emulsion in-jection group and combination group were obviously decreased,TIMP-1 mRNA expression was obviously enhanced,with statisti-cal significances(P<0.05). Compared with ganciclovir group and Elemene emulsion injection group,the cell invasion rate of C6 BTSCs in combination group was obviously decreased,TIMP-1 mRNA expression was obviously enhanced,with statistical signifi-cances(P<0.05). CONCLUSIONS:Elemene emulsion injection combined with ganciclovir can obviously inhibit the cell invasion of C6 BTSCs,the mechanism may be associated with promoting the TIMP-1 generation,and combination use shows better effect than single use.

Analysis on the effect of entecavir dispersible tablets on the treatment of patients with decompensated hepatitis B cirrhosis / 中国生化药物杂志

Objective To study and analyze of entecavir dispersible tablets on the treatment of patients with decompensated hepatitis B cirrhosis. Methods From February 2014 to September 2016, 100 patients with decompensated hepatitis B cirrhosis were randomly divided into the control group and the experimental group, 50 patients in each group. The control group were received routine treatment, while the experimental group were received entecavir dispersible tablets treatment on the basis of conventional treatment. The therapeutic effects in the two groups were compared and analyzed. Results The effective rate in the experimental group was 92.0%, and 70.0% in the control group. The effective rate in the experimental group was significantly higher than that in the control group, the difference has statistically significant (P<0.05). The Child-pugh score in the experimental group was (6.12±1.43) points, and the score in the control group was (7.23±1.95) points. The score in the control group was significantly higher than that in the experimental group, with statistical difference (P<0.05). The negative rate of HBeAg in the experimental group was 22.0%, while 86% in the control group the difference has statistically significant (P<0.05). Conclusion The clinical effect is better which entecavir dispersible tablets is used in the treatment of the patients with decompensated hepatitis B cirrhosis, which can improve the treatment efficiency to a great extent, recover the liver function, has the further promotion and application significance.

Simultaneous Determination of 7 Components in Zhizi Jinhua Dispersible Tablets by HPLC / 中国药房

OBJECTIVE:To develop a method for simultaneous determination of geniposide,baicalin,aloe-emodin,rhein, emodin,chrysophanol and physcion in Zhizi jinhua dispersible tablets. METHODS:HPLC method was adopted. The determination was performed on Dimonsil C18 column with mobile phase consisted of methanol-0.05%phosphoric acid(gradient elution)at the flow rate of 0.8 mL/min. The detection wavelength was set at 254 nm,and the column temperature was 25℃. The sample size was 20 μL. RESULTS:The linear ranges of geniposide,baicalin,aloe-emodin,rhein,emodin,chrysophanol and physcion were 0.0323-0.323 μg (r=0.9998),0.1374-1.374μg(r=0.9999),0.00372-0.0372μg(r=0.9997),0.0069-0.069μg(r=0.9995),0.00332-0.0332μg (r=0.9997),0.00864-0.0864 μg(r=0.9997) and 0.00122-0.0122 μg(r=0.9995),respectively. The limits of quantitation were 0.0321,0.1374,0.00372,0.0067,0.00330,0.00864,0.00122 μg,respectively. The limits of detection were 0.0095, 0.0041,0.0012,0.0020,0.0010,0.0026,0.0003 μg,respectively. RSDs of precision,stability and reproducibility tests were all lower than 3%. The average recoveries were 96.54%-99.52%(RSD=1.17%,n=6),97.23%-101.23%(RSD=1.36%,n=6), 97.22%-101.25%(RSD=1.83%,n=6),97.32%-100.23%(RSD=1.09%,n=6),97.99%-102.71%(RSD=1.73%,n=6), 96.99%-100.23%(RSD=1.21%,n=6),96.99%-103.01%(RSD=2.31%,n=6),respectively. CONCLUSIONS:The methods is simple and reproducible. It can be used for the content determination of 7 components in Zhizi jinhua dispersible tablets.

Study on the Extraction Technology of Medicinal Materials in Yanyanling Dispersible Tablets / 中国药师

Objective: To optimize the extraction technology of Chinese medicinal materials in Yanyanling dispersible tablets.Methods: Orthogonal design was used to study the effects of three factors, including the ratio of liquid to materials, extraction time and extraction times on the extraction rate of Chinese medicinal materials and the comprehensive score of gallic acid content and total solid yield was used as the index.Results: The optimum extraction conditions were as follows: the ratio of materials to liquid was 1∶10 (g·ml-1), the extraction time was one hour, and the extraction times was three.Conclusion: Under the optimum conditions, the extraction rate of gallic acid in Chinese medicinal materials in Yanyanling dispersible tablets is 0.058%, and the total solid yield is 21.4%.The optimal process is stable and feasible, which can provide reference for the production of Yanyanling dispersible tablets.

Pharmacokinetics Study of Mycophenolate Mofetil Dispersible Tablets in Early Renal Transplant Patients / 中国药学杂志

OBJECTIVE: To develop an UPLC method for the determination of mycophenolic acid(MPA) for studying the pharmacokinetics of mycophenolate mofetil(MMF) dispersible tablets after multiple oral doses in early kidney transplant recipients for the rational use in the clinical practice. METHODS: A total of 15 Chinese postoperative renal transplant recipients were given a multiple-dose of MMF (750 mg, q12 h) for 6 d. Their blood specimens (2 mL) were collected at 0 and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 h after drug oral administration on day 7. The concentrations of MPA in plasma were determined using UPLC-UV. The main pharmacokinetic parameters were assessed. RESULTS: Determination of MPA had good linearity in the concentration range of 0.1-40 μg·mL-1, lower limit of quantization was 0.10 μg·mL-1.The main pharmacokinetic parameters on day 7 of MMF dispersible tablets were as follows: AUC0-12 h was (24.63±9.51) μg·h·mL-1, ρmax was (6.51±3.27) μg·mL-1, tmax was (1.83±1.30) h, ρ0 was (1.26±0.99) μg·mL-1, CL was (34.66±12.45) L·h-1. Most of the patients revealed a second small peak in the 4-12 h. CONCLUSION: This established method is simple, rapid and suitable for determination of MPA in human plasma.Interindividual variability in AUC0-12 h, ρmax and ρ0 values was considerable in the early renal transplant patients. The MPA exposures under the fixed dose of MMF are low. It is necessary to monitor the MPA-AUC0-12 h to guide the adjustment of drug dosage.