OBJECTIVE:To investigate the characteristics of drug release and the factors affecting the in vitro dissolubility of diclofenac potassium double-layer tablets(DPD).METHODS:UV-spectrophotometry and rotating basket method in the pha-rmacopeia of China 2000 edition were used to determine the in vitro dissolubility of DPD and Higuchi equation was adopeted to simulate the in vitro drug release.The main parameters of dissolution were stastistically analysed.RESULTS:Dissolution parameters of DPD were as follows:T0.3=0.10h,Td=3.30h,T0.9=9.19h.Hardness of tablets did not affect the dissolution rate significantly;pH of dissolution media significantly influenced on the rate.Rotation speed had a significant effect on dissolution action only at the beginning of test.CONCLUSION:DPD has good properties of fast and sustained release.Proper media is the key of in vitro drug release test,however,the ultimate results should be based on in vivo trial.

OBJECTIVE:To prepare temperature sensitive hydrogel which is of strength.METHODS:The hygrogel was prepared using CS,PVA and GP as matrix with concentration of CS(A),weight ratio of CS to PVA(B) and pH value(C) as factors and with initial gelatination temperature,strength and dehydration as indexes.The formula was optimized by orthogonal experiment and verified.RESULTS:The optimal formula was as follows:A 20 mg?mL-1,B 1 :1,C 7.2.The prepared hydrogel was fluid at 4 ℃ or room temperature while gelatinized at 37 ℃ within 10 min with strength of about 1.4 kPa.Gelatination time reduced along with the increase of temperature.The pH value had hardly changed during degradation in vitro within 28 d.CONCLUSION:The CS/PVA/GP hydrogel is simple and practical in preparation technique and is temperature sensitive and of strength.

Objective:To establish a determination method for the content and entrapment efficiency of ropivacaine hydrochloride-loaded multivesicular liposomes. Methods: The separation of the multivesicular liposomes from the free drug was achieved by low-speed centrifugation. The concentration of ropivacaine hydrochloride in the supernatant and the multivesicular liposomes was determined by HPLC, and the entrapment efficiency was calculated. Results: The linear range of ropivacaine hydrochloride was 1. 0-80. 0μg· ml-1(r=0. 999 8). The average recovery was 99. 95% and RSD was 0. 72%(n=9). The content and entrapment efficiency of three batches of ropivacaine hydrochloride-loaded multivesicular liposomes was within the range of 99. 1%-100. 3% and 80. 06%-82. 14%, respectively. Conclusion:The method is simple and accurate, and can be used in the determination of content and entrapment efficien-cy of ropivacaine hydrochloride-loaded multivesicular liposomes.

Objective:To determine the equilibrium solubility and the apparent oil/water partition coefficient of nebivolol hydrochloride to provide experimental basis for the development of new preparations.Methods:The concentration of nebivolol hydrochloride was determined by an HPLC method,and a saturated solution method and a shake-flask method were respectively applied to determine the equilibrium solubility and the apparent oil/water partition coefficient of nebivolol hydrochloride in water,0.1 mol·L-1 HCl solution and phosphate buffer solution with different pH values(pH2.0,pH6.8,pH7.4 and pH8.0).Results:At (37±0.5)℃,the equilibrium solubility of nebivolol hydrochloride in water and in 0.1 mol·L-1 HCl solution was 722.53 μg·ml-1and 56.07μg·ml-1,respectively.The apparent oil/water partition coefficient (Log P) of nebivolol hydrochloride was 1.17 and 1.32,respectively.Within the pH range of 2.0-7.4,with the increase of pH value, the equilibrium solubility and the Log P decreased and increased,respectively,while pH value increased from 7.4 to 8.0,the equilibrium solubility of nebivolol hydrochloride increased and Log P decreased.Conclusion:The method is accurate and reliable.Nebivolol hydrochloride has poor water solubility,and the equilibrium solubility and the Log P are both influenced by pH values.

Objective To investigate the relationship between plasminogen activator inhibitor(PAI) activity and coronary artery disease(CAD) in elderly patients. Methods Plasma samples from 93 patients with CAD were analyzed for the PAI activity, plasminogen activator(t-PA) activity, serum levels of cholesterol and triglyceride. The values of these parameters were compared between the CAD and the control groups. Results Higher plasma PAI activity 〔(810?360) AU/L vs. (640?300) AU/L,P

Objective To observe the effect of electromyographic biofeedback therapy(EMGBFT)on dysphagia in stroke patients.Methods Fifty-three stroke patients with dysphagia were divided randomly into an EMGBFT group and a control group.The patients of EMGBFT group were given EMGBFT,electrical stimulation therapy (EST)and dysphagia training,while those in the control group were given EST and dysphagia training.All the patients were assessed with Kubota drinking test before treatment and 30 days after treatment.Results After treatment swallowing function of patients in both groups improved(P ＜0.05).The effective rate was 76.92％ in EMGBFT group and 55.56％ in control group,with statistically significant difference between the two groups(P ＜ 0.05).It showed that the EMGBFT group has significantly better outcome than the control group after treatment(P ＜ 0.05).Conclusions EMGBFT combined with regular rehabilitation therapy can improve patient's motor and swallowing function.

Objective To observe the effect of electromyographic biofeedback combined with swallowing training on dysphagia after stroke.Methods Ninety-five patients with difficulty in swallowing after stroke were randomly divided into a treatment group (48 eases) and a control group (47 cases).The patients in the treatment group were provided electromyographic biofeedback and swallowing training; the patients in the control group received swallowing training only.The therapeutic effect was assessed with Kubota's drinking water test before treatment and 30d after treatment.Results Swallowing in both groups improved after treatment.The total recovery rate in the treatment group was 87.5％,and in the control group it was 68.0％,a significant difference.Conclusion Electromyographic biofeedback can improve the effectiveness of swallowing training after stroke.

Objective:To optimize the formula of ropivacaine hydrochloride transdermal gel. Methods:The steady transdermal rate and cumulative transdermal percentage in 24 h of ropivacaine hydrochloride gel were used as the indices, an orthogonal design was applied to select the optimal formula, and Design Expert 8. 0. 5. 0 software was used to analyze the results. Results: The optimal formula con-tained 2% carbomer, 10% propylene-glycol and 5% Azone. The steady transdermal rate of the optimal formula was 0. 6951 mg·h-1 · cm-2 . The cumulative transdermal percentage in 24 h of the optimal formula was 91. 04%, which was 22. 79% higher than that of ropiva-caine hydrochloride solution with the same concentration. Design Expert 8. 0. 5. 0 software could predict the steady transdermal rate and cumulative transdermal percentage in 24 h of the optimal formula. Conclusion: The preparation design is reasonable, and the gel has promising properties, which is suitable for skin local application.

Objective:To investigate the effects of three herb extracts on cell proliferation and collagen synthesis in cultured hu-man dermal fibroblasts. Methods:The human dermal fibroblasts were isolated and cultured with tissue explant culture technique. Im-munohistochemical staining was performed to observe vimentin in fibroblasts. The proliferation of fibroblasts was determined by MTT as-say. Hydroxyproline in the cultural medium was determined by a digestion method. Results:The cells were typical fibroblasts, and the immunohistochemistry staining of vimentin in the cells was positive. The three herb extracts could promote the proliferation of the fibro-blasts at appropriate concentrations in a time-dependent manner. After the 72-hour culture in the medium, 0. 312 5-5. 000 0 mg·ml-1 Aloe vera gel extract, 0. 156 3-2. 500 0 mg·ml-1 Bletilla striata extract and 0. 075 0 mg·ml-1 salvianolate showed significant effects on the proliferation of fibroblasts (P<0. 05 or P<0. 01 vs the blank group). Compared with that in the blank group, the amount of hydroxyproline in the three herb extracts cultural medium was also increased (P<0. 05 or P<0. 01). The effect of salvianolate on the cell proliferation was closely related with time and concentration, and the high concentration group could inhibit the growth of fibroblasts as the extension of time. Conclusion:Aloe vera gel extract, bletilla striata extract and salvianolate can promote the proliferation of fi-broblasts and the production of hydroxyproline, which may contribute to the wound healing.

Objective:To optimize the formula of amlexanox nasal thermosensitive gel spray and establish the quality control meth-od. Methods:Amlexanox nasal thermosensitive gel spray was prepared by a cold dissolving method, and poloxamer 407 (P407) and poloxamer 188 (P188) were used as the carrier materials. Central composite design-response surface methodology was used to optimize the formula with the amount of P407 and P188 as the influencing factors and the gel temperature and the viscosity before gelling as the indices. The content of amlexanox was determined by HPLC. According to Chinese Pharmacopoeia (2010 edition), the other indices of the preparation such as appearance, pH, viscosity, content, total spray times of each bottle and the content of each spray were deter-mined as well. Results:The optimum ratio of P407 and P188 was 17. 0% and 0. 9%,respectively . The average recovery of amlexanox was 98. 8% and RSD was 1. 7%(n=9). The quality of 3 batches of amlexanox nasal thermosensitive gel spray met the related require-ments. Conclusion:The formula and preparation process of amlexanox nasal thermosensitive gel spray are reasonable and feasible with controllable quality, which is worthy of further research.