Syntheses and Antibacterial Activity of N-Acylated Ciprofloxacin Derivatives Based on the Trimethyl Lock

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复方夏天无片治疗老年骨质疏松性桡骨远端骨折的疗效观察

复方夏天无片具有祛风逐湿、舒筋通络、行血止痛等功效,临床广泛应用于风湿性关节炎、腰椎间盘突出症、骨关节炎等的治疗,但未见对骨折治疗的有关报道。该文观察复方夏天无片治疗老年骨质疏松性桡骨远端骨折的疗效,通过选取2011年1月—2014年6月在我院就诊骨质疏松性桡骨远端骨折患者180例,随机数字表法将患者分为观察组和对照组,每组各90例。对照组予以手法复位,石膏外固定后,予以钙尔奇D,观察组在对照组的基础上加复方夏天无片治疗。观察2组治疗后的疗效,腕关节功能和并发症发生率。结果显示观察组的优良率为95.56%,明显高于对照组的77.78%,差异有统计学意义(χ²=4.712,P<0.05)。观察组的并发症发生率明显低于对照组(P<0.05)。结果说明复方夏天无片能够提高老年骨质疏松性桡骨远端骨折的疗效,减少并发症的发生率, 减轻患者的痛苦,对提高生命质量具有重要作用。     

甲氧氯普胺口崩片的制备及体外溶出度考察

摘 要 目的： 制备甲氧氯普胺口崩片并优化处方,并对其体外溶出度进行考察。方法: 采用全因子试验设计,以填充剂配比（X₁）、崩解剂（X₂,%）用量为影响因素,以脆碎度（Y₁,%）、崩解时限（Y₂,s）、甲氧氯普胺在15 min的溶出度（Y₃,%）为片剂考察指标优化处方;并考察其在4种溶出介质中的溶出行为。结果: 甲氧氯普胺口崩片的最优处方组成为：填充剂甘露醇与微晶纤维素比例为2.5∶1、崩解剂占片重为6.5%。甲氧氯普胺口崩片在4种溶出介质中累积溶出度均大于80%。结论:甲氧氯普胺口崩片处方设计合理,制备工艺可行,质量可控。     

Dissolution Curve Comparisons Through the F2 Parameter,a Bayesian Extension of the f2 Statistic

Dissolution (or in vitro release) studies constitute an important aspect of pharmaceutical drug development. One important use of such studies is for justifying a biowaiver for post-approval changes which requires establishing equivalence between the new and old product. We propose a statistically rigorous modeling approach for this purpose based on the estimation of what we refer to as the F₂ parameter, an extension of the commonly used f₂ statistic. A Bayesian test procedure is proposed in relation to a set of composite hypotheses that capture the similarity requirement on the absolute mean differences between test and reference dissolution profiles. Several examples are provided to illustrate the application. Results of our simulation study comparing the performance of f₂ and the proposed method show that our Bayesian approach is comparable to or in many cases superior to the f₂ statistic as a decision rule. Further useful extensions of the method, such as the use of continuous-time dissolution modeling, are considered.     

Formulation development,in vitro and in vivo evaluation of microemulsion-based gel loaded with ketoprofen

Abstract

Background: Anti-inflammatory agents are widely used to relieve inflammation caused by various factors.

Aim: This study was initiated with the intention to deliver low aqueous soluble ketoprofen to enhance its solubility by developing microemulsion system as a template and then incorporating it into gel phase.

Materials and methods: Initially ketoprofen was solubilized into microemulsion preparation made up of clove oil, Tween 20 and propylene glycol as oil phase, surfactant and co-surfactant respectively, then it was incorporated into different concentration of gelling phase using gelling agents namely Carbopol 940, Carbopol 934 and hydroxypropyl methyl cellulose K₄M (HPMC K₄M). Formulated emulgels were evaluated for their physical appearance, pH, rheological properties, globule size, extrudability, drug content, spreadability, bioadhesion strength, in vitro and ex vivo drug release, skin irritation test and anti-inflammatory activity.

Results: Microemulsion had shown globule size 396?nm, pH 6–6.7, viscosity 29.4?cps and zeta potential ?12?mV indicating good stability. Formulated emulgels showed good physical appearance, skin acceptable pH 6–6.9, non-Newtonian shear thinning system, drug content 99.28?±?0.16%, bioadhesion strength 48.4 gram force, globule size 473?nm, spreadability 22.96?gm.cm/s, good extrudability, in vitro release, ex vivo release did not showed any irritation reaction and possess a good anti-inflammatory activity.

Conclusions: Selected batch showed enhanced drug release (92.42?±?4.66%) as compared to marketed gel (65.94?±?3.30). Similarly ex vivo release of formulation showed 72.22% release through mice skin compared with marketed gel. Formulations followed Korsmeyer–Peppas diffusion kinetic model. It was observed from the results that the formulated emulgel can provide promising delivery of ketoprofen.     

Calendering as a direct shaping tool for the continuous production of fixed-dose combination products via co-extrusion

In this study calendering is used as a downstream technique to shape monolithic co-extruded fixed-dose combination products in a continuous way. Co-extrudates with a metoprolol tartrate-loaded sustained-release core and a hydrochlorothiazide-loaded immediate-release coat were produced and immediately shaped into a monolithic drug delivery system via calendering, using chilled rolls with tablet-shaped cavities. In vitro metoprolol tartrate release from the ethylcellulose core of the calendered tablets was prolonged in comparison with the sustained release of a multiparticulate dosage form, prepared manually by cutting co-extrudates into mini-matrices. Analysis of the dosage forms using X-ray micro-computed tomography only detected small differences between the pore structure of the core of the calendered tablet and the mini-matrices. Diffusion path length was shown to be the main mechanism behind the release kinetics. Terahertz pulsed imaging visualized that adhesion between the core and coat of the calendered tablet was not complete and a gradient in coat thickness (varying from 200 to 600 μm) was observed. Modulated differential scanning calorimetry and X-ray diffraction indicated that the solid-state properties of both drugs were not affected by the calendering procedure.     

辖区一级医院评审中的护理缺陷与分析

目的:通过新一轮的医疗机构评审,探讨和分析存在的护理缺陷,强调护理工作的持续质量改进。方法:对97所一级医院的评审资料进行分析。结论:通过分析评审资料感到护理工作亟待改进。医院评审是一种很好的行业自律行为,是一种促进自身发展和提高的手段。     

Self-curing acrylic formulations with applications in intervertebral disk restoration: drug release and biological behaviour

New injectable acrylic formulations have been prepared to be applied in restoration processes for intervertebral disks (IVDs). The solid phase of the formulations is composed of poly(methyl methacrylate) (PMMA), incorporating in some cases chondroitin sulphate (CS) as a regenerative bioactive molecule, whereas the liquid phase is constituted by an amphiphilic macromonomer (MT), 2-hydroxyethyl methacrylate (HEMA) and, in some formulations, acrylic acid (AA). The curing parameters and the mechanical properties of the IVD formulations make them excellent candidates for intervertebral application. In vitro and in vivo evaluation of the prepared IVD formulations is described in terms of CS release, surface analysis after immersion in SBF solutions, and biocompatibility studies based on MTT assay and Alamar blue test, as well as in vivo implantation in female Wistar rats, by injection of the IVD formulations followed by histological evaluations to assess tissue response.