Ultrasound Transmission Technique as a Potential Tool for Physical Evaluation of Monolithic Matrix Tablets

The aim of this study was to investigate the effects of tablet porosity and particle size fraction of compacted Starch acetate powders, with and without model drug caffeine, on acoustic properties of tablets. The ultrasound velocity was determined from the transmission measurements. Tablets of starch acetate (SA DS 2.7) powder with two particle size fractions of 0–53 and 0–710 μm were compressed with a compaction simulator. Porosities of tablets varied in the range from 12% to 43% for both particle size fractions. Strong associations were found between the ultrasound velocity and physical properties of the tablets such as porosity and particle size fraction. Interestingly, ultrasound velocity was practically insensitive to inclusion of the model drug caffeine with the concentrations used. Based on this study ultrasound transmission method is a potential non-destructive tool for studying structural changes of tablets and other solid dosage forms.     

Application of π acceptors to the spectrophotometric and spectrofluorimetric determination of vincamine and naftidrofuryl oxalate in their pharmaceutical preparations

Three different spectrophotometric and two spectrofluorimetric methods have been developed and validated for the determination of vincamine (VN) and naftidrofuryl oxalate (NF) in tablets. The spectrophotometric methods depend on charge transfer complex formation between each of VN and NF with 7,7,8,8‐tetracyano‐quinodimethane (TCNQ), 2,6‐dichloroquinone‐4‐chloroimide (DCQ) and 2,3‐dichloro‐5,6‐dicyano‐1,4‐benzoquinone (DDQ) at 843, 580 and 588 nm, respectively. The spectrofluorimetric methods are based on the formation of charge transfer complex between each of the two drugs and TCNQ, with measurement of the fluorophore formed at 312/375 and 284/612 nm, respectively, or with DDQ at 400/475 and 284/396 nm, respectively. In the spectrophotometric measurements, Beer's law was obeyed at concentration ranges of 1.5–16, 10–180 and 12–140 μg/ml for VN with TCNQ, DCQ, and DDQ, respectively. For NF, the corresponding concentrations were 2–28, 5–75 and 25–150 μg/ml with TCNQ, DCQ, and DDQ, respectively. In the spectrofluorimetric measurements, the ranges for VN were 0.05–0.9 and 0.3–4 μg/ml with TCNQ and DDQ, respectively, whereas for NF the ranges were 0.05–0.85 and 0.5–8 μg/ml with TCNQ and DDQ, respectively. The different experimental parameters affecting the development and stability of the formed color or fluorophore were studied and optimized and the molar ratios of the complexes were calculated. The proposed methods were validated according to ICH guidelines and were successfully applied for the determination of VN and NF in their tablet dosage forms.     

芪丹通脉片对阿霉素诱导扩张型心肌病大鼠lncRNA XIST表达的影响

摘要 目的：探究芪丹通脉片（QDTM）对阿霉素诱导扩张型心肌病（DCM）大鼠的治疗作用及其对长链非编码RNA（lncRNA）X-无活性特异性转录物（XIST）表达的影响。方法：将大鼠分为Con组（n=12）、DCM组（n=13）、L-QDTM组（n=13）、M-QDTM组（n=13）、H-QDTM组（n=13）。Con组大鼠为正常对照大鼠,其他组大鼠均为阿霉素诱导的扩张型心肌病模型大鼠。Con组和DCM组大鼠灌胃生理盐水,L-QDTM组、M-QDTM组和H-QDTM组大鼠分别灌胃500、1000和2000 mg/kg/d的芪丹通脉片浸膏干粉,每日给药1次,共4周。治疗结束后,分别检测各组大鼠的心功能参数,血清心肌损伤指标和心肌组织氧化应激指标。通过心肌组织苏木素伊红（HE）染色、Masson三色染色和TUNEL染色观察心肌形态变化、纤维化和细胞凋亡情况。通过RT-qPCR检测心肌组织中XIST、collagen I、collagen Ⅲ、TGF-β1、Bax和Bcl-2的转录水平。结果：与Con组比较,DCM组大鼠的左室射血分数（LVEF）和左室短轴缩短率（FS）降低,左室舒张末期内径（LVIDd）和左心室收缩末期内径（LVIDs）升高,乳酸脱氢酶（LDH）、肌酸激酶（CK）和心肌肌钙蛋白I（cTnI）升高;心肌出现明显损伤,纤维化面积升高;collagen I、collagen Ⅲ和TGF-β1的mRNA水平均升高,TUNEL阳性率升高;Bax mRNA水平升高,Bcl-2 mRNA水平降低,超氧化物歧化酶（SOD）和过氧化氢酶（CAT）水平降低,丙二醛（MDA）水平升高,XIST水平升高（均P<0.05）。与DCM组比较,L-QDTM组、M-QDTM组和H-QDTM组的LVEF和FS均升高,LVIDd和LVIDs均降低,LDH、CK和cTnI均降低;心肌损伤减轻,纤维化面积降低;collagen I、collagen Ⅲ和TGF-β1的mRNA水平均降低,TUNEL阳性率降低;Bax mRNA水平降低,Bcl-2 mRNA水平升高,SOD和CAT水平升高,MDA水平均降低,XIST水平降低（均P<0.05）。结论：本研究表明芪丹通脉片在治疗阿霉素诱导扩张型心肌病大鼠中效果显著,其机制可能与抑制lncRNA XIST有关。     

Handwriting Analysis Indicates Spontaneous Dyskinesias in Neuroleptic Na?ve Adolescents at High Risk for Psychosis

Growing evidence suggests that movement abnormalities are a core feature of psychosis. One marker of movement abnormality, dyskinesia, is a result of impaired neuromodulation of dopamine in fronto-striatal pathways. The traditional methods for identifying movement abnormalities include observer-based reports and force stability gauges. The drawbacks of these methods are long training times for raters, experimenter bias, large site differences in instrumental apparatus, and suboptimal reliability. Taking these drawbacks into account has guided the development of better standardized and more efficient procedures to examine movement abnormalities through handwriting analysis software and tablet. Individuals at risk for psychosis showed significantly more dysfluent pen movements (a proximal measure for dyskinesia) in a handwriting task. Handwriting kinematics offers a great advance over previous methods of assessing dyskinesia, which could clearly be beneficial for understanding the etiology of psychosis.     

Development and In Vivo Floating Behavior of Verapamil HCl Intragastric Floating Tablets

A novel gastro retentive controlled release drug delivery system of verapamil HCl was formulated in an effort to increase the gastric retention time of the dosage form and to control drug release. Hydroxypropylmethylcellulose (HPMC), carbopol, and xanthan gum were incorporated for gel-forming properties. Buoyancy was achieved by adding an effervescent mixture of sodium bicarbonate and anhydrous citric acid. In vitro drug release studies were performed, and drug release kinetics was evaluated using the linear regression method. The optimized intragastric floating tablet composed of 3:2 of HPMC K4M to xanthan gum exhibited 95.39% drug release in 24 h in vitro, while the buoyancy lag time was 36.2 s, and the intragastric floating tablet remained buoyant for >24 h. Zero-order and non-Fickian release transport was confirmed as the drug release mechanism from the optimized formulation (F7). X-ray studies showed that total buoyancy time was able to delay the gastric emptying of verapamil HCl intragastric floating tablet in mongrel dogs for more than 4 h. Optimized intragastric floating tablet showed no significant change in physical appearance, drug content, total buoyancy time, or in vitro dissolution pattern after storage at 40°C/75% relative humidity for 3 months.     

Once-daily tablet formulation and in vitro release evaluation of cefpodoxime using hydroxypropyl methylcellulose: A technical note

Summary and Conclusions  Decreasing the dose frequency of cefpodoxime proxetil increases patient compliance; patients prefer to take the drug once daily. It also improves the rate of bacterial killing and hastens the cure from the indications, and therefore increases compliance. The hydrophilic matrix of HPMC controlled the cefpodoxime proxetil release effectively for 24 hours; hence, the formulation can be considered as a once-daily sustained-release tablet of cefpodoxime proxetil. The formulation showed acceptable pharmacotechnical properties and assay requirements. In vitro dissolution studies indicated a sustained-release pattern throughout 24 hours of the study that was comparable to the theoretical release profile. Drug release kinetics indicated that drug release was best explained by Higuchi’s equation, as these plots showed the highest linearity (r ²=0.9734), but a close relationship was also noted with zero-order kinetics (r ²=0.9708). Korsmeyer’s plots indicated ann value of 0.57, which was indicative of an anomalous diffusion mechanism or diffusion coupled with erosion; hence, the drug release was controlled by more than one process. Hixson-Crowell plots indicated a change in surface area and diameter of the tablets with the progressive dissolution of the matrix as a function of time. Published: September 22, 2006     

Monitoring tablet surface roughness during the film coating process

The purpose of this study was to evaluate the change of surface roughness and the development of the film during the film coating process using laser profilometer roughness measurements, SEM imaging, and energy dispersive X-ray (EDX) analysis. Surface roughness and texture changes developing during the process of film coating tablets were studied by noncontact laser profilometry and scanning electron microscopy (SEM). An EDX analysis was used to monitor the magnesium stearate and titanium dioxide of the tablets. The tablet cores were film coated with aqueous hydroxypropyl methylcellulose, and the film coating was performed using an instrumented pilot-scale side-vented drum coater. The SEM images of the film-coated tablets showed that within the first 30 minutes, the surface of the tablet cores was completely covered with a thin film. The magnesium signal that was monitored by SEM-EDX disappeared after ∼15 to 30 minutes, indicating that the tablet surface was homogeneously covered with film coating. The surface roughness started to increase from the beginning of the coating process, and the increase in the roughness broke off after 30 minutes of spraying. The results clearly showed that the surface roughness of the tablets increased until the film coating covered the whole surface area of the tablets, corresponding to a coating time period of 15 to 30 minutes (from the beginning of the spraying phase). Thereafter, the film only became thicker. The methods used in this study were applicable in the visualization of the changes caused by the film coating on the tablet surfaces.     

双唑泰泡腾片与乳酸杆菌活菌胶囊联合治疗细菌性阴道病的临床疗效分析

本文旨在探讨双唑泰泡腾片与乳酸杆菌活菌胶囊联合治疗细菌性阴道病的临床疗效.将100例就诊于江苏省中西医结合医院妇产科的细菌性阴道病患者随机平均分为两组:治疗组给予阴道内放置双唑泰泡腾片与乳酸杆菌活菌胶囊联合治疗;对照组单用阴道内放置双唑泰泡腾片.药物剂量、治疗时间相同.结果显示,治疗组细菌性阴道病48例(失访2例),3...     

Social organization in the Mongolian gerbil

The Mongolian gerbil (Meriones unguiculatus) has a social system based on an adult male and female and their juvenile and infant offspring. The adult male and juveniles, as well as the adult female, interact with the infants. This species is active during the day and the night thus making it ideal for observational studies on social behaviour, particularly in relation to the rearing of the infants. Several factors are considered each of which may influence the maternal behaviour and the behavioural and physical development of the young. These factors may be varied in simple experiments which are suitable for school projects.