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 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 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 establish a method to determine the content of lidocaine hydrochloride in buccal adhesive tablets contai-ning carbomer as an excipient by HPLC. Methods:Calcium chloride was used to precipitate carbomer in buccal adhesive tablets. The HPLC analysis was performed on a Welch C18 column(250 mm × 4. 6 mm,5 μm)with the column temperature of 40℃. The mobile phase was the mixture of 0. 05% sodium acetate solution(added 50 ml acetic acid into 930 ml distilled water,adjusting pH to 3. 40 with 1 ml·min-1 sodium hydroxide solution)and acetonitrile(70:30). The flow rate was 1. 0 ml·min-1 ,the detection wavelength was at 254 nm and the injection volume was 20 μl. Results:Within the range of 0. 10-2. 00 mg·ml-1 ,there was a good linear rela-tionship between the concentration and the peak area of lidocaine hydrochloride(r=0. 999 9). The average recovery was 100. 2%( RSD=1. 4%,n=9). Conclusion:The established method is simple,accurate and reproducible,which can be applied to determine the content of lidocaine hydrochloride in buccal adhesive tablets.

Objective:To prepare PLGA nanoparticles modified with folic acid conjugated chitosan oligosaccharide containing pa-clitaxel (F-CS-PLGA-NPs) and study the inhibitory effect on SKOV-3. Methods:F-CS-PLGA-NPs were prepared by an interface dep-osition method, 30% ethanol was used as the release medium for the in vitro release profiles of nanoparticles, and MTT was adopted to evaluate the inhibitory effect of paclitaxel with different formulations and concentrations on SKOV-3. Results:The particle size and zeta potential of F-CS-PLGA-NPs was (321 ± 0. 76) nm and (22. 6 ± 0. 26) mV, respectively, the drug loading was (5. 1 ± 0. 25)%, and the encapsulation efficiency was (41. 96 ± 1. 96)%. F-CS-PLGA-NPs had a similar in vitro release profiles with the ordinary nanoparti-cles ( PLGA-NPs) . About 35% of paclitaxel was released from the nanoparticles in the initial 24 h, and then a near zero order release at a relative slow rate was shown, and the cumulative release rate in 144 h was about 75%. The results of cell experiments suggested that at the same paclitaxel concentration, the inhibition effect of F-CS-PLGA-NPs group was stronger than that of the PLGA-NPs group and the solution group. The inhibition effect of F-CS-PLGA-NPs could be reduced by free folic acid. Conclusion:PLGA nanoparticles modified with folic acid conjugated chitosan oligosaccharide can increase the targeting efficiency in SKOVS-3 tumor cells.

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.

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.