排序方式: 共有124条查询结果,搜索用时 15 毫秒
61.
Muhammad Harris Shoaib Saniah Al Sabah Siddiqi Rabia Ismail Yousuf Kamran Zaheer Muhammad Hanif Saeed Rehana Sabahat Jabeen 《AAPS PharmSciTech》2010,11(2):708-718
The objective of the present study was to develop a once-daily sustained-release (SR) matrix tablet of famotidine. Nine different
formulations (F1–F9) were prepared by direct compression method using Avicel PH101 as filler/binder in the range of 41–27%
in F1–F3, 18–22% in F4–F7, and 16–18% in F8–F9 and hydroxypropyl methylcellulose (4,000 cps) as hydrophilic matrix was used
in F1–F3 from 19% to 30%, around 40% in F4–F7, and 42–45% in F8–F9. Talc and Aerosil were added in the ratio of 0.7–1.2%.
The tablets were subjected to various physical parameters including weight variation test, hardness, thickness, diameter,
friability, and in vitro release studies. Assay was also performed according to the USP 30 NF 25 procedure. The results of the physical parameters
and assay were found to be within the acceptable range. In vitro dissolution results indicated that formulation F4–F7, having around 40% of rate control polymer, produced a SR pattern throughout
24 h. F1–F3 showed drug release at a faster rate, while F8–F9 released much slower, i.e., <80% in 24 h. Model-dependent and
model-independent methods were used for data analysis and the best results were observed for F4 in zero order (r
2 = 0.984) and F6 in Korsmeyer and Higuchi (r
2 = 0.992 and 0.988). The parameter n indicated anomalous diffusion, while β in Weibull showed a parabolic curve with higher initial slope. The f
2 similarity test was performed taking F4 as a reference formulation. Only the F5–F7 formulations were similar to the reference
formulation F4. The mean dissolution time was around 10 h for the successful formulation. 相似文献
62.
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 相似文献
63.
Stewart DA Shoaib T Durani AJ 《Plastic and reconstructive surgery》2006,117(6):2078; author reply 2078-2078; author reply 2079
64.
65.
Objective
The objective of the study was to identify the occurrence and outcome of low back ache amongst computer users and their relation to age, gender, occupation and duration of computer use.Materials and Methods
A self reported questionnaire tailored from Occupational Health and Safety Act of the Ministry of Labor, Ontario, Canada was used.Results
416 participants 55.5% males and 45% females using computers for a minimum of five years with age range 22 to 59 years belonged to different occupational groups. Consecutive hours of computer work was found to be associated with work related backache or discomfort in 27.4% (n = 114) participants (16.1% male, 11.3% female). Frequent short breaks improved backache (p value <0.001) in 93 (22.4%) participants (13.2% male, 9.2% female). No significant relation was observed with the duration of computer usage or usage per day; between the two genders or occupational groups. Backache had no significance within age groups.Conclusion
Our study identifies the occurrence of low back pain among those who are using computer for consecutive hours without breaks and the results suggest the need to create health awareness especially use of short breaks to minimize the risk and occurrence of low back pain. The result of this study can also be used to improve ergonomic design and standards. 相似文献66.
PUB-MS: a mass spectrometry-based method to monitor protein-protein proximity in vivo 总被引:1,自引:0,他引:1
Kulyyassov A Shoaib M Pichugin A Kannouche P Ramanculov E Lipinski M Ogryzko V 《Journal of proteome research》2011,10(10):4416-4427
The common techniques to study protein-protein proximity in vivo are not well adapted to the capabilities and the expertise of a standard proteomics laboratory, typically based on the use of mass spectrometry. With the aim of closing this gap, we have developed PUB-MS (for proximity utilizing biotinylation and mass spectrometry), an approach to monitor protein-protein proximity, based on biotinylation of a protein fused to a biotin-acceptor peptide (BAP) by a biotin-ligase, BirA, fused to its interaction partner. The biotinylation status of the BAP can be further detected by either Western analysis or mass spectrometry. The BAP sequence was redesigned for easy monitoring of the biotinylation status by LC-MS/MS. In several experimental models, we demonstrate that the biotinylation in vivo is specifically enhanced when the BAP- and BirA-fused proteins are in proximity to each other. The advantage of mass spectrometry is demonstrated by using BAPs with different sequences in a single experiment (allowing multiplex analysis) and by the use of stable isotopes. Finally, we show that our methodology can be also used to study a specific subfraction of a protein of interest that was in proximity with another protein at a predefined time before the analysis. 相似文献
67.
BenYounès A Tajeddine N Tailler M Malik SA Shen S Métivier D Kepp O Vitale I Maiuri MC Kroemer G 《Autophagy》2011,7(8):883-891
Autophagic flux can be measured by determining the declining abundance of autophagic substrates such as sequestosome 1 (SQSTM1, better known as p62), which is sequestered in autophagosomes upon its direct interaction with LC3. However, the total amount of p62 results from two opposed processes, namely its synthesis (which can be modulated by some cellular stressors including autophagy inducers) and its degradation. To avoid this problem, we generated a stable cell line expressing a chimeric protein composed by p62 and the HaloTag (?) protein, which serves as a receptor for fluorescent HaloTag (?) ligands. Upon labeling with HaloTag (?) ligands (which form covalent, near-to-undissociable bonds with the Halotag (?) receptor) and washing, the resulting fluorescent labeling is not influenced by de novo protein synthesis, therefore allowing for the specific monitoring of the fusion protein decline without any interference by protein synthesis. We demonstrate that a HaloTag (?) -p62 fusion protein stably expressed in suitable cell lines can be used to monitor autophagy by flow cytometry and automated fluorescence microscopy. We surmise that this system could be adapted to high-throughput applications. 相似文献
68.
Background
Mycobacterium tuberculosis infects nearly 1/3 of the world population and this reservoir forms the largest pool from which new cases arise. Among the cytokines, IFN-γ is a key determinant in protection against tuberculosis. Single nucleotide polymorphisms (SNPs) in IFN-γ gene (+874 T/A) which determine TT high (hi), AA low (lo) and TA intermediate (int) responder phenotypes have shown variable associations with tuberculosis disease outcome in different ethnic populations. The objective of the current study was to analyze IFN-γ gene combinations with other IFN-γ regulating cytokine genes (IL-10, TNF –α, IL-6) to see the effect of gene- combinations on disease severity outcome in pulmonary tuberculosis.Methods and Findings
Study groups comprised of pulmonary TB patients stratified according to lung tissue involvement into mild (Pmd = 74) or advance (Pad = 23) lung disease and compared with healthy controls (TBNA = 166). Genotype analysis was carried out using amplification refractory mutation system-PCR (ARMS-PCR). IFN-γ gene (+874 T/A) functional SNP combinations in TNFα (−308 G/A), IL-10 (−1082 A/G) and IL-6 (−174 G/C) were analyzed. Single gene analysis (Pearson χ2) showed a dominant association of IFN-γ TT hi genotype (p = 0.001) and T allele (p = 0.001) with mild disease. IFN-γ lo -IL-10 lo genotype combination was associated with advanced disease (p = 0.002). IFN-γ hi –IL-6 hi combination was associated with mild disease (p = 0.0005) while IFN-γ lo –IL-6 int was associated with protection against both forms of pulmonary disease (p = 0.002).Conclusion
Our results show that a limited number of IFN-γ gene combinations with other cytokine functional SNPs determine the outcome of disease severity in tuberculosis. 相似文献69.
70.
Khan KM Shah Z Ahmad VU Ambreen N Khan M Taha M Rahim F Noreen S Perveen S Choudhary MI Voelter W 《Bioorganic & medicinal chemistry》2012,20(4):1521-1526
6-Nitrobenzimidazole derivatives (1-30) synthesized and their phosphodiesterase inhibitory activities determined. Out of thirty tested compounds, ten showed a varying degrees of phosphodiesterase inhibition with IC(50) values between 1.5±0.043 and 294.0±16.7 μM. Compounds 30 (IC(50)=1.5±0.043 μM), 1 (IC(50)=2.4±0.049 μM), 11 (IC(50)=5.7±0.113 μM), 13 (IC(50)=6.4±0.148 μM), 14 (IC(50)=10.5±0.51 μM), 9 (IC(50)=11.49±0.08 μM), 3 (IC(50)=63.1±1.48 μM), 10 (IC(50)=120.0±4.47 μM), and 6 (IC(50)=153.2±5.6 μM) showed excellent phosphodiesterase inhibitory activity, much superior to the standard EDTA (IC(50)=274±0.007 μM), and thus are potential molecules for the development of a new class of phosphodiesterase inhibitors. A structure-activity relationship is evaluated. All compounds are characterized by spectroscopic parameters. 相似文献