ABSTRACT
@#Most drugs taste bitter and irritating, resulting in poor compliance of patients, and the bad odor affects the therapeutic effect. The successful research and development of a drug should not only conform to the five quality characteristics of effectiveness, stability, safety, uniformity and economy, but also the compliance of patients to drugs with bad odor. The development of taste masking techniques is critical for bitter drugs.This review describes the principles, advantages and drawbacks of traditional taste masking techniques, and introduces the mechanism and application of novel taste masking techniques, such as melt granulation, hot melt extrusion, 3D printing, drug complex preparation, and bitter taste inhibitors. The in vitro evaluation methods of drug taste masking effect, such as functional magnetic resonance imaging, in vitro dissolution, and electronic tongue technology, are described. And introduce in vivo evaluation methods, such as animal and human taste, in the field of taste masking effect. A new strategy of BP neural network prediction model for drug taste evaluation is proposed, with a view to providing theoretical reference for the future research on drug taste masking.
ABSTRACT
Objective@#To investigate the effects of sinomenine on brain edema and the expression of aquaporin 4 (AQP-4) and aquaporin 5 (AQP-5) in rats with acute brain injury.@*Methods@#According to random number table method, rats were divided into sham operation group, model group, low-dose sinomenine group, high-dose sinomenine group, 20 in each group. In addition to the sham operation group, the rat brain injury model was established by Feeney free falling impact method. Rats in low and high dose of sinomenine group were given sinomenine 30, 60 mg/kg by intraperitoneal injection, and the sham operation group and model group were injected intraperitoneally with the same volume of normal saline, once per day for 7 days. Histopathological changes in each group were observed by HE staining and electron microscope. Western blot and RT-PCR were used to detect AQP-4 and AQP-5 protein and gene expression in brain tissue.@*Results@#The pathological results showed that the nerve cells in the model group were loosely arranged, disordered in hierarchy, some cells appear to have degenerated. The degeneration and necrosis of nerve cells in the low and high dose sinomenine group were less than those in the model group. Compared to the model group, the expression of AQP-4 (0.74 ± 0.13, 0.49 ± 0.11 vs. 1.30 ± 0.21), AQP-5 (0.98 ± 0.07, 0.45 ± 0.10 vs. 1.47 ± 0.18) in the low dose and high dose sinomenine group significantly decreased (P<0.05). The expression of AQP-4 (1.48 ± 0.18, 1.26 ± 0.12 vs. 2.04 ± 0.14), AQP-5 (1.31 ± 0.17, 1.20 ± 0.11 vs. 1.87 ± 0.15) mRNA in the low dose and high dose sinomenine group significantly decreased (P<0.05).@*Conclusions@#Sinomenine could alleviate cerebral injury by lowering the expression of AQP-4 and AQP-5.
ABSTRACT
Objective:To investigate the effects of sinomenine on brain edema and the expression of aquaporin 4 (AQP-4) and aquaporin 5 (AQP-5) in rats with acute brain injury.Methods:According to random number table method, rats were divided into sham operation group, model group, low-dose sinomenine group, high-dose sinomenine group, 20 in each group. In addition to the sham operation group, the rat brain injury model was established by Feeney free falling impact method. Rats in low and high dose of sinomenine group were given sinomenine 30, 60 mg/kg by intraperitoneal injection, and the sham operation group and model group were injected intraperitoneally with the same volume of normal saline, once per day for 7 days. Histopathological changes in each group were observed by HE staining and electron microscope. Western blot and RT-PCR were used to detect AQP-4 and AQP-5 protein and gene expression in brain tissue.Results:The pathological results showed that the nerve cells in the model group were loosely arranged, disordered in hierarchy, some cells appear to have degenerated. The degeneration and necrosis of nerve cells in the low and high dose sinomenine group were less than those in the model group. Compared to the model group, the expression of AQP-4 (0.74 ± 0.13, 0.49 ± 0.11 vs. 1.30 ± 0.21), AQP-5 (0.98 ± 0.07, 0.45 ± 0.10 vs. 1.47 ± 0.18) in the low dose and high dose sinomenine group significantly decreased ( P<0.05). The expression of AQP-4 (1.48 ± 0.18, 1.26 ± 0.12 vs. 2.04 ± 0.14), AQP-5 (1.31 ± 0.17, 1.20 ± 0.11 vs. 1.87 ± 0.15) mRNA in the low dose and high dose sinomenine group significantly decreased ( P<0.05). Conclusions:Sinomenine could alleviate cerebral injury by lowering the expression of AQP-4 and AQP-5.
ABSTRACT
[Objective]To explore the relationship between peripheral arterial disease(PAD)and diabetic retinopathy(DR)in type 2 diabetes patients.[Methods]A total of 99 patients diagnosed with PAD were classified into grade 1-3 by their total scores of peripheral arterial stenosis assessed by color doppler ultrasound examinations,where the degree of stenosis 30% ~ 49% scored 0, 50%~99%scored 1,lumen occlusion(i.e. degree of stenosis 100%)scored 2,and therefore the total score 0-2 was categorized into Grade 1 ,3~4 into Grade 2 ,5~12 into Grade 3. The bilateral anterior tibial artery ,posterior tibial artery and dorsalis pedis artery of these patients were analyzed. The presence of diabetic retinopathy(DR)was graded from retinal photographs using a standard protocol.[Results]Among 99 cases of type 2 diabetic patients with peripheral arterial disease ,58.6%of them were male with average age of 67.3 ± 7.9 years old. Patients of Grade 1,Grade2,Grade 3 lesion accounted for 45.4%,30.3%,24.2%,respectively. Age, gender,smoking history,SBP,DBP,BMI,FBG,TC,TG,LDL-C,HDL-C,HbA1C among 3 groups were not statistically signifi-cant. The associations of DM duration and HbA1C value were significantly larger in DR than in PAD. The proportion of DR patients increased with the severity degree of PAD(p for trend=0.004). Degree of stenosis Grade 2 and Grade 3 could be predictive for DR.[Conclusions]DR is associated with the severity degree of PAD in type 2 diabetes patients as evaluated by duplex ultrasonography.Degree of stenosis Grade 2 and 3 could be used for screening or finding DR. Strategies for optimum treatment and early prevention are needed.