Clinical Efficacy of Fuzheng Huaji Longbi Decoction in Treating Benign Prostatic Hyperplasia with Syndrome of Healthy Qi Deficiency and Blood Stasis / 中国实验方剂学杂志

ObjectiveTo explore the clinical efficacy and safety of Fuzheng Huaji Longbi decoction in treating benign prostatic hyperplasia （BPH） in the patients with the syndrome of healthy Qi deficiency and blood stasis. MethodA total of 94 BPH patients were randomized into control and observation groups， with 47 patients in each group. The control group was treated with doxazosin mesylate sustained-release tablets， and the observation group with Fuzheng Huaji Longbi decoction on the basis of the therapy in the control group. After eight weeks， the international prostate symptom score （IPSS）， quality of life （QOL） score， residual urine volume （RUV）， maximum urinary flow rate （Qmax）， TCM syndrome score， TCM symptom score， electrocardiogram， and liver and kidney function were determined to evaluate the clinical efficacy and safety of the two groups. ResultAfter 8 weeks of treatment， the total response rate in the control group was 63.64% （28/44）， which was lower than that （84.44%， 38/45） in the observation group （χ2=5.026， P<0.05）. The clinical efficacy in the observation group was higher than that in the control group （Z=-2.17， P=0.030）. The treatment in both groups decreased the IPSS， QOL score， RUV， and TCM syndrome scores and increased the Qmax （P<0.05）. Moreover， the observation group had lower IPSS， QOL score， RUV， and TCM syndrome score （P<0.05） and higher Qmax than the control group after treatment （P<0.05）. The treatment in the observation group decreased all the TCM symptom scores （P<0.05）， while that in the control group only decreased the frequency of urination at night and the scores of dysuria， weak urine stream， and post-urinary drainage （P<0.05）. After treatment， the observation group had lower frequency of urination at night and lower scores of mental fatigue， cold limbs， lower abdominal discomfort， and loose stool than the control group （P<0.05）. No adverse events associated with the administration of Fuzheng Huaji Longbi decoction were observed during the treatment period. ConclusionFuzheng Huaji Longbi decoction is effective in treating BPH in the patients with the syndrome of healthy qi deficiency and blood stasis. It can relieve the clinical symptoms and improve the quality of life， being a safe and reliable choice for clinical application.

Bioequivalence of metformin hydrochloride sustained-release tablets under fed condition in healthy subjects / 中国药科大学学报

@#To evaluate bioequivalence and safety of two kinds of metformin hydrochloride sustained-release tablets (test preparation vs reference preparation) under the condition of fed and single administration.A single center, randomized, open, single-dose, two-period, two-sequence, and double-crossover design was used.32 healthy subjects took 0.5 g of test preparation or reference preparation under fed and single-dose administration.4 mL of venous blood was collected from before administration (0 h) to 1, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 9, 10, 12, 15, 24, 36 and 48 h after administration.The concentration of metformin in plasma samples was detected, and then the pharmacokinetic parameters were calculated by WinNonlin 7.0 software.When the 90% confidence intervals of cmax, AUC0-t and AUC0-∞ geometric mean ratio of test preparation and reference preparation were within 80.00%-125.00% equivalent intervals respectively, the bioequivalence of the two preparations was proved.One subject fell off due to adverse events.The main pharmacokinetic parameters of test preparation and reference preparation as follows: cmax were (0.68 ± 0.14) and (0.65 ± 0.11) mg/L, AUC0-t were (7.33 ± 1.65) and (7.00 ± 1.89) h·mg/L, AUC0-∞ were (7.39 ± 1.67) and (7.06 ± 1.91) h·mg/L, respectively.The 90% confidence intervals of the geometric mean ratio of the two main pharmacokinetic parameters were 101.45%-109.14%, 100.08%-112.32% and 100.24%-112.28%, respectively, which fell within the bioequivalence interval of 80.00%-125.00%.There were no serious adverse events and unexpected adverse events during the trial.The results show that test preparation and reference preparation are bioequivalent under fed and single-dose administration, safe and well tolerated in healthy subjects.

Efficacy of maintenance electroconvulsive therapy combined with quetiapine treatment for manic episode of bipolar disorder / 中国基层医药

Objective:To investigate the efficacy of maintenance electroconvulsive therapy (MECT) combined with quetiapine treatment for manic episodes of bipolar disorder.Methods:A total of 103 patients with manic episodes of bipolar disorder received treatment in Kangci Hospital of Jiaxing from January 2019 to August 2020 and were included in this study. They were randomly divided into observation ( n = 46) and control groups ( n = 57). The observation group was given MECT combined with quetiapine treatment and the control group was treated with magnesium valproate sustained-release tablets combined with quetiapine. All patients received 4 weeks of treatment. Clinical efficacy, total hospital cost, drug cost during hospitalization, drug proportion, adverse reactions, and scores of the Bech-Rafaelsdn Mania Rating Scale and the Wisconsin Card Sorting Test pre- and post-treatment were compared between the two groups. Results:After 4 weeks of treatment, total response rate was significantly higher in the observation group than in the control group [76.09% (35/46) vs. 56.14% (32/57), χ2 = 4.45, P < 0.05]. In the observation group, total hospital cost, drug cost during hospitalization, and drug proportion were (16074.52 ± 1019.81) yuan, (1374.52 ± 619.81) yuan, and 8.70% respectively, which were not significantly different from those in the control group [(15618.14 ± 1550.34) yuan, (1261.14 ± 750.34) yuan, 10.53%, t = 1.71, 0.82, χ2 = 0.09, all P > 0.05]. After 4 weeks of treatment, Bech-Rafaelsdn Mania Rating score was significantly lower in the observation group than in the control group [(7.36 ± 3.04) points vs. (10.23 ± 2.37) points, t = 5.38, P < 0.001]. The number of wrong responses and the number of perseverative errors in the Wisconsin Card Sorting Test in the observation group were (40.45 ± 3.61) counts and (9.56 ± 1.39) counts, respectively, which were significantly lower than those in the control group [(48.59 ± 4.51) counts, (12.08 ± 1.25) counts, t = 10.17, 9.56, both P < 0.001]. The number of perseverative errors in the Wisconsin Card Sorting Test was significantly higher in the observation group than in the control group [(33.85 ± 2.50) counts vs. (29.71 ± 2.14) counts, t = 8.90, P < 0.001]. There was no significant difference in total incidence of adverse reactions between observation and control groups (21.74% vs. 22.81%, χ2 = 0.01, P > 0.05). Conclusion:MECT combined with quetiapine treatment is highly effective on the manic episodes of bipolar disorder. The combined therapy is worthy of clinical application.

In vitro evaluation of saxagliptin and metformin hydrochloride sustained-release tablets / 中国药科大学学报

@#In order to evaluate the consistency of the release behavior between the self-made saxagliptin and metformin hydrochloride sustained-release tablets and the reference preparations in vitro, the similarity of the dissolution curves between the self-made preparations and the reference preparations in four dissolution mediums: HCl (pH 1.0), acetate buffer saline (pH 4.5), phosphate buffer saline (pH 6.8) and pure water, and the gel morphology and strength of the self-made preparations and the reference preparations in the HCl (pH 1.0) solution medium were compared.Results showed that in four dissolution mediums, the dissolution rates of saxagliptin in the self-made preparations and the reference preparations at 15 min were greater than 85%, and the ?2 similarity factors of metformin hydrochloride were 89, 83, 80, 86, all greater than 50, so the dissolution of the self-made preparations was consistent with those of the reference preparations.The volume expansion rate, water absorption rate and erosion rate were consistent with those of the reference preparations, and the gel strength of the self-made preparations was the same as that of the reference preparations.The in vitro release behaviors of the self-made preparations and the reference preparations are consistent, which provide a good guarantee for bioequivalence.

Bioequivalence of metformin hydrochloride sustained-release tablets in healthy subjects / 中国临床药理学与治疗学

AIM: To study the bioequivalence of two metformin hydrochloride sustained-release tablets in Chinese healthy subjects. METHODS: A randomized, open-label, two-period, crossover study design was adopted in the study. In fasting test 36 and in fed test 23 healthy subjects were given a single oral dose of metformin hydrochloride sustained-release tablet (0.5 g). The concentration of metformin in plasma was measured by HPLC-MS/MS. The pharmacokinetic parameters were calculated by WinNonlin 7.0 program, and statistical analysis were performed by using SAS9.4 statistics software. RESULTS: In the fasting test, the pharmacokinetic parameters of metformin of the test (T) and reference(R) preparation were as follow: C

In vitro release and in vivo pharmacokinetics in Beagle dogs of pregabalin sustained-release tablets / 国际药学研究杂志

Objective: To evaluate the in vitro release degree, release mechanism and dose dumping of test tablet and reference tablet Lyrica® CR. The in vivo pharmacokinetics of the test tablet and the reference tablet were further investigated using the Beagle dog as a model. Methods: With Pfizer's pregabalin sustained-release tablets(Lyrica® CR)as the reference listed drug, the in vitro release behavior was evaluated using an automatic dissolution apparatus, and similarity factor(f2)method was used to analyze the in vitro release similarity between the reference tablet and the test tablet. The in vitro release equation was fitted to evaluate the drug release mechanism. Study was conducted on dose dumping of preparations based on the relevant guiding principles of the United States, Europe and China. Finally, the pharmacokinetic parameters of the test tablet and the reference tablet in Beagle dogs were compared. Results: The f2 of the test tablet and the reference tablet were more than 80 in all five release media, and there was no sudden release in the release medium containing ethanol. The pharmacokinetic parameters of the reference tablet and the test tablet were as follows: The Tmax was(6.00±2.19)and(4.00±2.19)h, the Cmax was(19.35±11.43)and(17.25±7.77)μg/ml, and the AUC0-t was(340.37± 220.66)and(281.65 ± 196.25)h•μg/ml for the reference tablet and the test tablet, respectively. Conclusion: In this study, the release curve of the test tablet was similar to that of the reference tablet in the five media. The drug was released slowly without sudden release, and the release mechanism in vitro was similar. There was no significant difference in pharmacokinetic parameters between the test tablet and the reference tablet in beagle dogs, and the relative bioavailability was more than 80%.

In-vitro and In-vivo Relationship of Gabapentin from Floating and Immediate Release Tablets

Gabapentiniseffectiveagainst post-traumaticspinalinjury-inducedneuropathicpain.Itrequireshighdosageand frequency inthemanagementofneuropathicpain.Thepresentresearchworkwasanattempttoformulate andevaluategabapentingastro-retentivetabletstoprolonggastricresidenceandincreasedrug absorptionand furtherincreasebioavailability.Thefloatingtabletsofgabapentinwerepreparedintwodoses(300and600mg) byusingtwopolymers(hydroxylpropylmethylcelluloseandhydroxylpropylcellulose).Immediaterelease tabletsofgabapentincontaining thesamedoseswerepreparedandusedasreferenceformulations.The physicochemicalcharacteristicsofthepreparedtabletsweredetermined(drug content,weightvariation,friability, hardness,thicknessand diameter). Drugreleasefromthepreparedtabletswasfollowed and foundthatby increasingdrug concentrationinthetabletsreleaserateincreases.Floatingtabletsshowedprolongeddrugrelease (over96%)tomorethan15hrs.Immediatereleasetabletsshowedover97%drugreleasewithin48min.In-vivoresultsshowedthatplasmaexposuretogabapentininanimalsreceivingthedrug doesnotdose proportionalandtherefore maynotreachtherapeuticallyusefullevels.AUC0-24andCmaxincaseof300mgtabletsaremorethanthoseincaseof 600 mgtablets.Thein-vivo releaseofgabapentin doesnot correlatewiththein-vitroreleaseofthedrug.

Design and Optimization of the Formulation and Technology of Theophylline Gel Matrix Sustained-release Tablets Based on QbD Concept / 中国药房

OBJECTIVE： To design and optimize the formulation and technology of Theophylline hydrophilic gel matrix sustained-release tablets （self-made sustained-release tablets for short） based on the concept of “Quality by Design” （QbD）. METHODS： Diluent type， tablet diameter， the property of adhesive （ratio of different adhesive types）， the amount of adhesive were regarded as critical process parameters （CPPs）. Similarity factor of dissolution curves of self-made Theophylline sustained-release tablets and reference preparation and its accumulative release rate at different time points were regarded as critical quality attributes （CQAs）. L18（34） orthogonal tablet was adopted for design and trial， and secondary polynomial regression model was established. By using Modde 12.0 software， the design space and its acceptable range （PAR） were calculated through the optimal model. The optimal formulation and technology of Theophylline sustained-release tablets was determined， and validation test and Monte Carlo simulation verification were conducted. RESULTS： The optimal model with good coincidence， accuracy， validity and reproducibility was obtained， which could better fit the relationship between CQAs and CPPs. The design space and PAR value were obtained by further calculation （The optimum value of diluent was lactose； tablet diameter was 9.07-9.33 mm， and the optimal value was 9.20 mm； ratio of HPMC K4M to HPMC was 0.50-0.83， and the optimal value was 0.80； total amount of HPMC was 0.036 0-0.041 3 g per tablet， and the optimal value was 0.038 g per tablet）. The optimal formulation and technology included that ratio of theophylline， HPMC K4M and HPMC K100M were 50％， 15.48％ and 3.87％， respectively； the rest was filled with lactose and the diameter of the tablet was 9.20 mm. The results of validation confirmed that self-made Theophylline sustained-release tablets had similar in vitro release behavior compared with reference preparation. CONCLUSIONS： Based on the concept of QbD， the formulation and technology of Theophylline sustained-release tablets can meet the requirements of design， and the CPPs can be adjusted within the PAR range to meet the requirements of CQAs. This shows that the QbD concept is scientific and effective in the design and optimization of the formulation and technology of sustained and controlled release preparations.

Study on Release Rate in vitro of Risperidone Sustained-release Tablets and Its Pharmacokinetics in Rabbits / 中国药房

OBJECTIVE： To study release behavior in vitro of Risperidone sustained-release tablets and its pharmacokinetics in rabbits. METHODS： Risperidone sustained-release tablets were prepared by using mesoporous silica as matrix. Release rates in vitro within 12 h （Q12 h） of commercially available Risperidone tablets， Risperidone sustained-release tablets and its physical mixture in 0.1 mol/L HCl fluid were investigated with basket method. The release model of Risperidone sustained-release tablets were fitted. Using clozapine as an internal standard， HPLC method was used to determine blood concentration of risperidone and 9-hydroxyrisperidone in rabbits 48 h （n＝6） after intragastric administration of commercially available Risperidone tablets and Risperidone sustained-release tablets 2 mg. Pharmacokinetic parameters were calculated by using non-compartmental model of Kinetica 4.4 software. RESULTS： Compared with commercially available Risperidone tablets （Q12 h＝97％） and physical mixtures （Q12 h＝95％）， release rate of Risperidone sustained-release tablets （Q12 h＝83.7％） slowed down significantly， and the release of Risperidone sustained-release tablets in 0.1 mol/L HCl fluid was closed to first-order release （R2＝0.998 9）， with diffusion as the main factor and dissolution as the supplement. By risperidone， the pharmacokinetic parameters of commercially available Risperidone tablets and Risperidone sustained-release tablets included that t1/2 were （4.64±0.93），（6.65±0.92） h； cmax were （34.46±7.75） and （8.57±6.91） ng/mL； MRT were （11.48±1.23）， （17.46±2.10） h； AUC0-48 h were （314.39±10.33），（192.98±49.14） ng·h/mL， respectively. By 9-hydroxyrisperidone， the pharmacokinetic parameters of them included that t1/2 were（7.08±0.93），（10.45±0.78） h； cmax were （98.08±5.43），（54.55±4.88） ng/mL； MRT were （11.48±1.23）， （17.46±2.10） h； AUC0-48 h were （894.71±131.15）， （1 227.99±112.12） ng·h/mL （n＝6）， respectively. Compared with commercially available Risperidone tablets， t1/2 and MRT of Risperidone sustained-release tablets prolonged significantly， while cmax decreased significantly （P＜0.05）. CONCLUSIONS： Risperidone loaded in mesoporous silica has sustained release effect and prolong the time of drug efficacy.

Pharmacokinetic study on six active ingredients of Qikui Sustained-release Tablets in rabbit plasma / 中草药

Objective: To compare the differences in pharmacokinetic behavior of six ingredients in Qikui Sustained-release Tablets in rabbit plasma. Qikui Granules was taken as reference. Methods: Diazepam was used as internal standard. LC-MS/MS detection methods of astragaloside, hyperin, isoquercitrin, rutin, morroniside, and loganin in rabbit plasma were established, and pharmacokinetic parameters of six components were calculated. Results: Six active ingredients’ equation of linear regressions were: astragaloside Y = 1.0 × 10-4 X - 0.009 9 (r = 0.999 7), morroniside Y = 1.0 × 10-4 X + 0.038 7 (r = 0.999 4), loganin Y = 3.0 × 10-5 X + 0.008 7 (r = 0.999 3), hyperin Y = 1.0 × 10-3 X - 0.016 1 (r = 0.999 0), rutin Y = 5.0 × 10-4 X - 0.011 5 (r = 0.999 4), isoquercitrin Y = 1.7 × 10-3X - 0.307 5(r = 0.999 2). Intra-day and inter-day precision and accuracy and recovery rate were up to the mustard. After Qikui Sustained-release Tablets and Qikui Granules being given by gavege, the maximal concentration (Cmax) of morroniside, loganin, astragaloside, rutin, hyperin, and isoquerctirin in Qikui Granules were (1.333 ± 0.051), (1.238 ± 0.164), (0.83 ± 0.079), (0.127 ± 0.017),(0.444 ± 0.048), and (0.223 ± 0.048) mg/L, t1/2 were (3.848 ± 0.311), (3.822 ± 0.757), (4.982 ± 1.14), (3.73 ± 0.298), (4.732 ± 0.642), and (5.132 ± 0.901) h, respectively, AUC(0-t) were (3.069 ± 0.307), (2.891 ± 0.943), (2.079 ± 0.306), (0.313 ± 0.068), (1.087 ± 0.177), (0.496 ± 0.129) mg∙h/L, respectively, Cmax of morroniside, loganin, astragaloside, rutin, hyperin, and isoquerctirin in Qikui Sustained-release Tablets were (0.985 ± 0.13), (0.961 ± 0.175), (0.693 ± 0.101), (0.094 ± 0.012), (0.354 ± 0.045), (0.201 ± 0.037) mg/L, t1/2 were (4.691 ± 0.337), (5.62 ± 1.64), (6.408 ± 0.707), (4.103 ± 0.341), (6.048 ± 0.882), (5.803 ± 0.59) h, AUC(0-t) were (5.191 ± 1.046), (6.168 ± 1.25), (4.293 ± 0.823), (0.485 ± 0.103), (1.84 ± 0.432), (0.924 ± 0.19) mg∙h/L. Contrast with Qikui Granules, relative bioavailability of morroniside, loganin, astragaloside, rutin, hyperin, and isoquerctirin in Qikui Sustained-release Tablets were 169.1%, 213.3%, 206.5%, 156.0%, 169.3%, and 186.3%, respectively. Conclusion: Qikui Sustained-release Tablets can significantly improve the bioavailability of each active ingredient in rabbit.

Preparation of sustained-release tablets of tilianin nanosuspension lyophilized powder / 中草药

Objective: To prepare sustained-release tablets of tilianin nanosuspension lyophilized powder. The factors that might influence drug release and release mechanism were studied in present study. Methods: High pressure homogenization method was used to prepare tilianin nanosuspension. Lactose and mannitol (3:1) were employed as freeze-drying protective agent to prepare lyophilized powder. HPMC was used as framework material to prepare sustained-release tablets of tilianin nanosuspension lyophilized powder. Based on single factor test, the effects of proportion and amounts of HPMC K4M and HPMC K15, amounts of PEG 4000 and magnesium stearate on in vitro drug release of sustained-release tablets were investigated. Orthogonal test was designed to gain the optimum prescription. Results: The particle size and zeta potential of tilianin nanosuspension were (164.41 ± 9.72) nm and (-37.21 ± 2.38) mV, respectively. The particle size and zeta potential of re-dispersed freeze-drying products were (211.83 ± 11.26) nm and (-31.66 ± 2.92) mV, respectively. The optimum prescription was as follow: the proportion and amounts of HPMC K4M and HPMC K15 were 2:1 and 40 mg, amounts of PEG 4000 was 20 mg, and amounts of magnesium stearate were 0.5%. Sustained release tablets of tilianin nanosuspension were well accorded with Higuchi kinetics model. The equation was Mt/M∞ = 0.286 8 t1/2-0.073 8, r2 = 0.981 4. And the cumulative release could achieve 92.36% in 12 h. The drug release from the tablets was controlled by diffusion and degradation of the matrix. Conclusion: The preparation technology of sustained release tablets of tilianin nanosuspension lyophilized powder has good reproducibility. This sustained release tablets could control the release of tilianin

Study on matrix sustained release tablets of brucine solid lipid nanoparticles / 中草药

Objective To prepare brucine solid lipid nanoparticles (SLN) and its lyophilized powder, and then hydrogel matrix sustained-release tablets (HMST) of brucine SLN (SLN-HMST) were prepared. The factors that may influence drug release in vitro and release mechanism were also investigated in present study. Methods Based on single factor test, orthogonal test was designed to gain the optimum prescription. Zero-order, First-order and Higuchi models were used for the model fitting of drug release. Ritger-Pappas models were employed to study release mechanism of brucine SLN-HMST. Results Brucine SLN-HMST was better agreed with First-order kinetics model. The equation was ln(1-Mt/M∞) = -0.212 1 t + 0.106 4 (r = 0.992 3). The cumulative release could achieve 91.48% in 12 h. The sustained release features were obviously. The drug release from the tablets was controlled by diffusion and degradation of the matrix. Conclusion The prepared brucine SLN-HMST can deliver drug continually for 12 h with good reproducibility.

Effect of sodium valproate tablets and venlafaxine hydrochloride sustained-release tablets in the treatment of female schizophrenia with affective disorder / 中国基层医药

Objective To investigate the clinical effect of sodium valproate tablets combined with venlafaxine hydrochloride sustained-release tablets in female patients with schizophrenia complicated with affective disorders and its influence on the recurrence time.Methods From January 2013 to July 2016,98 female patients with schizophrenia complicated by affective disorder in Taiyuan Mental Hospital were selected and randomly divided into single group (n =49) and combination group (n =49) according to the digital table.The single drug group was treated with sodium valproate tablets,and the combination group was treated with venlafaxine hydrochloride sustained-release tablets on the basis of a single drug group.The clinical efficacy and recurrence time of the two groups were compared.Results The scores of withdrawal symptoms [(4.39 ± 0.94) points],positive symptoms [(11.55 ± 4.30) points],negative symptoms [(11.09 ± 1.21) points] and psychiatric symptoms [(12.01 ±2.16) points] in the combination group were all significantly lower than those at 1 month after treatment[(10.98 ±1.43) points,(16.74 ± 3.89) points,(18.43 ± 2.05) points,(19.83 ± 3.44) points] (t =12.957,18.471,all P ＜0.05).The incubation period and amplitude of the P300 potentials in the combination group were (314.55 ± 9.21) s,(4.05 ± 1.76)s,respectively,which were both higher than those of the single drug group [(341.60 ± 25.87)s,(2.58 ± 2.30)s] (t =18.251,15.738,all P ＜ 0.05).The eye movements of the combination group 12 weeks after operaion were (27.30 ± 1.41) s and (6.15 ± 0.98) s,respectively,which were higher than those of the single drug group[(25.10 ± 2.93) s and (5.10 ± 1.20) s] (t =13.992,15.836,all P ＜ 0.05).The recurrence rate of the combined group was 8.16％,which was lower than 18.37％ of the single drug group(x2 =6.893,P ＜ 0.05).The hospitalization duration [(14.83 ± 4.61)d],symptom improvement time [(34.94 ± 7.85)d] of the combined group were shorter than those of the single drug group [(27.91 ± 7.49) d,(59.81 ± 10.94) d] (t =18.946,21.461,all P ＜ 0.05).The recurrence time at 12 weeks after treatment of the combination group was (148.48 ± 33.19)d,which was longer than (109.46 ±28.88)d of the single drug group(t =16.893,P ＜0.05).Conclusion The combination of sodium valproate tablets and venlafaxine hydrochloride sustained-release tablets in.patients with schizophrenia complicated with affective disorders can improve the clinical effect,shorten the recurrence time and improve the cognitive function of patients,which is worth popularizing and applying.

Preventive effect of potassium citrate sustained-release tablets on formation of adherent stone in ureteral stent-graft after retrograde intrarenal surgery / 实用医学杂志

Objective To investigate the preventive effect of potassium citrate sustained-release tablets on the formation of adherent stone in ureteral stent-graft after retrograde intrarenal surgery. Methods Patients with upper urinary tract calculi after retrograde intrarenal surgery and without stasis confirmed by color ultrasound were randomly divided into test group and control group. Patients in test group were given potassium citrate sustained release tablets 3 times(1.08 grams each time)orally but those in the control group did not take the drug. Two groups of patients received conventional health education and diet guidance. The formation of adherent stone in ureteral stent-graft during surgical removal of ureteral stent and the adverse reactions during taking the medication 3,6 and 16 weeks after the surgery were compared. Results There were few cases of adherent stone formed 3 weeks after the operation,which can not be statistically analyzed. The incidence of adnexal calculus in the test group 6 and 16 weeks after the operation was significantly lower than that of the control group,which was statistically significant.No serious adverse reactions and complications occurred in the test group during the medication-taking. Conclusions Potassium citrate sustained-release tablet is safe and effective for preventing the formation of adher-ent stone in ureteral stent-graft after upper urinary tract calculi retrograde intrarenal surgery.

Optimization of the Formulation of Roxatidine Acetate Hydrochloride Sustained-release Tablets by Central Composite Design-response Surface Methodology / 中国药房

OBJECTIVE:To optimize the formulation of Roxatidine acetate hydrochloride(ROX)sustained-release tablets. METHODS:ROX sustained-release tablets were prepared by direct powder compression method. Central composite design-response surface methodology was used to optimize the formulation with composite index of 1,4,8 h in vitro accumulative release rate as index,using mass ratio of lactose/microcrystalline cellulose(MCC)(m/m),ethyl cellulose(EC)amount and HPMC amount as factors. Validation test was also conducted. RESULTS:The optimal formulation was as follows as ROX 75 mg,lactose 45 mg, MCC 91 mg,EC 65 mg,HPMC 124 mg,micropowder silica gel 2 mg. 1,4,8 h in vitro accumulative release rates of prepared sustained-release tablets were(30.7 ± 0.5)%,(65.8 ± 0.7)%,(89.4 ± 0.6)%,respectively. Related errors of them to predicted value were 0.6%,0.8%,1.2%,respectively. CONCLUSIONS:ROX sustained-release tablets are prepared successfully,and sustained-release effect is consisted with the expected effect.

In vivo pharmacokinetics of tectorigenin floating sustained-release tablets in rabbits and evaluation of in vitro-in vivo correlation / 中草药

Objective: To evaluate therelease characteristicsin vitro, pharmacokinetics in rabbits and in vivo-in vitro correlation of tectorigenin floating sustained-release tablets (TFSRT). Methods: The release characteristics of TFSRTin vitro was detected with HPLC in the artificial gastric fluid. Six Japanese Giant Ear Rabbits as self crossover control, which were given TFSRT and suspension liquid (200mg). The concentration of tectorigenin in plasma was determined with HPLC and the data were processed with PKsolver 2.0 software. Results:The cumulative releaserate of TFSRTin vitro was over 70% in 10 h.The pharmacokineticsin rabbits showed that TFSRT and tectorigenin suspension liquid conformed to the single compartment model and the pharmacokinetic parameters were obtained: tmax: (2.809±0.371) and (0.442±0.138)h, Cmax: (6.317±1.337) and (9.662±2.759) μg/mL, AUC0-t: (74.156±10.420) and (57.059±13.309) μg∙h/mL. The relative bioavailability of TFSRT was (134.63±27.94)%, so there was significant difference between them. Conclusion: TFSRT can release slowly, so it increase the relative bioavailability significantly. The correlation between the absorption in vivo and release in vitro is fine (r=0.9879), so the release rate in vitro can control the quality of TFSRT.

Effects of amiodarone combined with succinylmetroprolol sustained-release tablets on cardiac function in patients with atrial fibrillation and congestive heart failure / 中国生化药物杂志

Objective To investigate the clinical efficacy of amiodarone combined with succinylmetroprolol sustained-release tablets in patients with atrial fibrillation and congestive heart failure (CHF) complicated with atrial fibrillation (AF), and to observe the effect of amiodarone on heart function and ventricular rate.MethodsIn people's hospital of Anji county from June 2013 to June 2016 a total of 80 patients with atrial fibrillation and heart failure were enrolled in this study.The patients were randomly divided into control group and treatment group, 40 cases.(Ventricular rate, resting ventricular rate), cardiac function (ejection fraction-EF, stroke volume-SV, cardiac output-CO and left ventricular function) were measured before treatment and 6 months after treatment Ventricular end-diastolic early/late peak velocity ratio-VA/VE).The clinical efficacy and side effects during the treatment were statistically analyzed.ResultsThe ventricular rate and resting ventricular rate after exercise were significantly lower than those before treatment, but the ventricular rate and resting ventricular rate were significantly lower in the treatment group than those in the control group after 6 months of treatment (P<0.05).The VA/VE was significantly lower than that of the control group at 6 months after treatment, and the values of EF, SV and CO were significantly higher than those of the control group at 6 months after the treatment, SV, CO were significantly higher than the control group(P<0.05).Treatment group, the total effective rate was 92.5%, significantly higher than the control group 72.5%(χ2=7.77, P=0.02).No significant adverse reactions during treatment.ConclusionRapid ventricular rate of atrial fibrillation with congestive heart failure were treated with amiodarone combined with metoprolol succinate sustained release tablets can conducive to the ventricular rate and heart function of patients, and the effect is remarkable, safe, so it can be recommended as the drug of choice for clinical treatment of patients.

In vitro Dissolution and Virtual Bioequivalence of Domestic Nifedipine Sustained Release Tablets / 中国药师

Objective: To evaluate the quality consistency of four domestic nifedipine sustained release tablets by dissolution test and virtual bioequivalence study by GastroPlus software.Methods: The dissolution curves of the four preparations were determined with the methods described in Japanese orange book and Chinese Pharmacopeia.The f2 factor of dissolution curves was calculated to compare the similarity.The in vitro dissolution data of the original preparation were combined with GastroPlus software to obtain the simulated in vivo absorption curves which were correlated with the actual concentration-time curves.The suitable dissolution medium was selected to evaluate the quality of domestic nifedipine sustained release tablets according to the better in vivo-in vitro correlation (IVIVC).The simulated in vivo absorption parameters obtained from the dissolution data combined with GastroPlus software were used to conduct the virtual bioequivalence study of domestic nifedipine sustained release tablets compared with the original products.Results: The f2 similar factors of the four domestic nifedipine sustained release tablets compared with the original preparation were all less than 50.Compared with that from the method in Japanese orange book, the correlation between the dissolution profiles in vitro and in vivo of original nifedipine sustained release tablets obtained from the method in Chinese Pharmacopoeia was better.The deviation between the simulated Cmax and AUC0-∞ values of the four test tablets and the measured values of the original preparation was within the range of ±20%.Conclusion: The dissolution curves of the four domestic nifedipine sustained release tablets are not similar to that of the original preparation, however, the four preparations are all bioequivalent to the original preparation according to the simulated absorption parameters based on the dissolution method in Chinese Pharmacopeia and GastroPlus software.

Effect of metformin tablet on type 2 diabetes mellitus patients complicated with atherosclerosis and its influence on blood glucose level and clinical biochemical index / 中国基层医药

Objective To investigate the clinical effect of mefformin tablets in the treatment of type 2 diabetes mellitus(T2DM) with atherosclerosis.Methods A total of 84 T2DM patients with atherosclerosis were divided into control group and treatment group according to the random number table method,42 cases in each group.All patients were given diet control,health education and exercise,etc..The control group was treated with gliclazide sustained-release tablets.The treatment group was treated with mefformin and treated for 6 months.The levels of fasting blood glucose(FBG) and 2 h postprandial blood glucose(2hPBG) were measured before and 6 months after treatment.The levels of intima-media thickness (cIMT),leptin (LP),adiponectin (TC),chitinase-3-like protein-1 (YKL-40),triglyceride (TG),low density lipoprotein cholesterol (HDL-C) and high-density lipoprotein cholesterol (HDL-C) were measured.The adverse reactions were observed in the two groups.Results After treatment for 6 months,the levels of FBG and 2hPBG in the treatment group were (6.71 ±0.41) mmol/L and (8.82 ±0.61) mmol/L,respectively,which were significantly lower than those in the control group [(6.96 ± 0.48) mmol/L,(9.58 ± 0.57) mmol/L,t =2.56,5.89,P =0.01,0.00].The levels of cIMT,TC,TG and LDL-C in the treatment group were significantly lower than those in the control group at 6 months after treatment (t =5.36,6.46,9.10,2.31,P =0.00,0.00,0.00,0.02).After 6 months of treatment,the HDL-C level of the treatment group was significantly higher than that of the control group (t =2.84,P =0.00).After treatment for 6 months,HDL-C level in the two groups was significantly higher than before treatment,the other indicators in the two groups were significantly lower than before treatment (all P ＜ 0.05).There were no adverse reactions in the two groups during treatment.Conclusion Metformin in the treatment of T2DM patients with atherosclerosis has significant effect,it can improve blood glucose levels and the clinical and biochemical indicators,and it is safe.

Preparation and Determination of Release of Berberine Sustained-release Tablets Containing Chitosan in Vitro / 医药导报

Objective To prepare berberine chitosan sustained-release tablets and to study the in vitro release characteristics. Methods The chitosan sustained-release tablets were prepared by chitosan as the skeleton material,and the drug release rate of berberine hydrochloride at different time was determined by high performance liquid chromatography. Results The in vitro cumulative release of berberine chitosan sustained-release tablets was increased with time.Furthermore,it can sustain for 24 h and the accumulative release was above 95%, the dissolution time of 63. 2% of the drug was 12. 63 h. Artificial gastric juice had the best performance on the dissolution of berberine,while rotations only influenced the dissolution at the beginning of drug release. Conclusion This method is convenient, accurate and reproducible.Berberine chitosan sustained-release tablets have further development and application value.