盐酸左氧氟沙星乳膏的的制备

目的：研制盐酸左氧氟沙星乳膏。方法：拟订处方组成及制备工艺，建立紫外分光光度法用于含量测定。结果与结论：乳膏的制备工艺可行，质量稳定，用UV法测定盐酸左氧氟沙星的含量，方法可行，重现性好，可用于医药制剂的质量控制。     

复方左氧氟沙星滴鼻液的制备

左氧氟沙星（Levofloxacin）是新一代全合成氟喹诺酮类抗菌药，是氧氟沙星的左旋异构体，对革兰阳性菌及包括绿脓杆菌在内的革兰阴性菌，有广谱和高效的抗菌活性，其抗菌活性是氧氟沙星的2倍，是诺氟沙星的8倍。为了增加局部用药的药物浓度，减少全身用药的不良反应，制备了复方左氧氟沙星滴鼻液用于治疗急慢性鼻炎、鼻窦炎、副鼻窦炎、过敏性鼻炎等疾病。     

氧氟沙星注射液的制备

氧氟沙星（氟嗪酸,Ofloxacin,OFLX）是目前广泛应用于临床的第三代喹诺酮类药物,主要用于治疗呼吸道、泌尿道、肠道、皮肤、关节及软组织等多种系统的感染,具有抗菌谱广、作用强、与多种抗菌药物间无交叉耐药性的特点。有关其滴耳剂、滴眼剂的制备已有报道。我们根据有关资料「’」配制了氧氟沙星注射液,经临床使用,效果较为满意。现将其制备工艺介绍如下。工仪器与试剂751－GW型可见紫外分光光度计（上海分析仪器厂）;PHS－25A型酸度计（上海理达仪器厂）;注射用氧氟沙星粉（江苏省昆山制药总厂）;注射用氯化钠（南通勤奋制…     

氧氟沙星软膏的制备和含量测定

介绍了氧氟沙星软膏的处方和制备工艺,建立了紫外分光光度法测定其含量的方法,该方法稳定、准确可靠,回收率为99.74％,RSD为0.52％,软膏中的附加剂对测定无干扰。     

紫外分光光度法测定左氧氟沙星滴耳液中左氧氟沙星的含量

目的建立左氧氟沙星滴耳液中左氧氟沙星的含量测定。方法紫外分光光度法。溶剂为0.1 mol.L-1盐酸溶液,检测波长293 nm。结果左氧氟沙星在2~8 mg.L-1范围内,线性关系良好,r=0.9995。回收率为99.6%。结论该法可准确测定左氧氟沙星滴耳液中左氧氟沙星的含量,适用于制剂的质量控制。     

紫外分光光度法测定氧氟沙星片剂的含量

应用紫外分光光度法测定氧氟沙星及其片剂的含量，方法简便、快速，结果准确，平均回收率为９９．８％，变异系数为０．２３％（ｎ＝６），测定结果与部颁标准法一致。     

氧氟沙星滴鼻液的稳定性研究

目的 :探讨氧氟沙星滴鼻液的室温稳定性。方法 :采用紫外分光光度法测定氧氟沙星滴鼻液的含量及经典恒温法预测本品的室温储存期。结果 :氧氟沙星滴鼻液的室温有效期为 2 .1a。结论 :紫外分光光度法测定氧氟沙星滴鼻液的含量及经典恒温法操作简便 ,结果准确 ,可作为常规方法用于药品稳定性检测。     

紫外分光光度法测定氧氟沙星片的含量

采用紫外分光光度法测定氧氟沙星片剂的含量。以０．１ｍｏｌ／Ｌ盐酸为溶剂，测定波长为２９３ｎｍ，浓度在２～１０ｍｇ／Ｌ范围内，吸收度与浓度呈线性关系。测得平均回收率为９９．６８％（ｎ＝５），ＲＳＤ为０．２２％。该法操作简单、快速、结果准确。     

紫外分光光度法测定氧氟沙星颗粒剂的含量

本文以盐酸液（０．１ｍｏｌ／Ｌ）为溶剂，采用紫外分光光度法测定氧氟沙星颗粒剂的含量。考察了光照和温对含量测定的影响，并与ＨＰＬＣ法（部标准）作了比较试验。方法平均回收率为９８．７１％，ＲＳＤ＝０．０６％，ｎ＝９；样品含量测定的平均ＲＳＤ为０．９９％，ｎ＝６。与ＨＰＬＣ法相比，无显著性差异。     

盐酸达克罗宁氧氟沙星凝胶的制备与质量控制

目的选择羧甲基纤维素钠为主要基质,以聚山梨酯80为增溶剂,研制了达克罗宁氧氟沙星凝胶。方法采用单波长分光光度法及双波长分光光度法分别测定凝胶中氧氟沙星及达克罗宁的含量。以0.1mol.L-1HCl为溶媒分别于335nm;282nm;302.3nm处测定。结果氧氟沙星在5~25μg.mL-1,A=0.027841C 0.01103其相关系数为0.9999;盐酸达克罗宁在4~20μg.mL-1,A=0.030653C 0.00061其相关系数为0.9999。两主药在各自浓度范围内,浓度与吸光度有良好的线性关系。氧氟沙星平均回收率为100.02%,RSD=0.6897%,(n=3);达克罗宁平均回收率为100.08%,RSD=0.8544%,(n=3)。结论该方法简便、快速、准确可靠。     

Preparation and characterization of ofloxacin microspheres for the eradication of bone associated bacterial biofilm

Biodegradable polymers for localized delivery of antibiotics have emerged as an important approach to treating orthopaedic infections. In chronic forms of osteomyelitis which arethought tobeassociated with bacterial biofilm, localized delivery of a suitable antibiotic is desirable. This paper describes the formulation and in vitro evaluation of biodegradable ofloxacin microspheres for the eradication of bone associated bacterial biofilm infections. Ofloxacin microspheres were formulated using poly(glycolic acid-co-dl-lactic acid) (PGLA) by the emulsion solvent evaporation technique. The effects of process parameters such as phase volume, poly(vinyl alcohol) (PVA) concentration, and viscosity grade of the polymer during preparation on encapsulation efficiency (EEF) and in vitro release profiles were investigated. An increase in the phase volume or volume fraction from 21 to 35% at a constant internal phase volume resulted in an increase in EEF from 34 to 74%. Increasing PVA concentration from 0.25 to 2.5% w/v at a constant phase volume or volume fraction did not have an effect on the EEF. Ofloxacin release from the microsopheres was biphasic with an initial burst release followed by a slow release phase. An optimum slowing down of release was observed when the phase volume was 29%. Above and below this phase volume, release of ofloxacin was higher. The higher the viscosity grade of the polymer used for the preparation of microspheres, the higher the PVA concentration needed to prepare microspheres with slower release. The study indicates that various rates of ofloxacin release is possible by varying formulation conditions. This should provide a means for formulating sustained release microspheres of antibiotics for the treatment of biofilm infections associated with the bone.     

复方氧氟沙星滴鼻液的制备及应用

本文拟定了复方氧氟沙星滴鼻液处方制备工艺和质量控制标准，并对其进行了稳定性试验。采用紫外分光光度法测定了氧氟沙里的吸收度，盐酸麻黄碱在波长293nm处无干扰。结果表明该制剂应用安全．疗效可靠．室温放置12mo质量仍符合要求。     

Novel inclusion complex of ibuprofen tromethamine with cyclodextrins: Physico-chemical characterization

Guest–host interactions of ibuprofen tromethamine salt (Ibu.T) with native and modified cyclodextrins (CyDs) have been investigated using several techniques, namely phase solubility diagrams (PSDs), proton nuclear magnetic resonance (¹H NMR), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), X-ray powder diffractometry (XRPD), scanning-electron microscopy (SEM) and molecular mechanics (MM). From the analysis of PSD data (A_L-type) it is concluded that the anionic tromethamine salt of ibuprofen (pK_a = 4.55) forms 1:1 soluble complexes with all CyDs investigated in buffered water at pH 7.0, while the neutral form of Ibu forms an insoluble complex with β-CyD (B_S-type) in buffered water at pH 2.0. Ibu.T has a lower tendency to complex with β-CyD (K₁₁ = 58 M⁻¹ at pH 7.0) compared with the neutral Ibu (K₁₁ = 4200 M⁻¹) in water. Complex formation of Ibu.T with β-CyD (ΔG° = −20.4 kJ/mol) is enthalpy driven (ΔH° = −22.9 kJ/mol) and is accompanied by a small unfavorable entropy (ΔS° = −8.4 J/mol K) change. ¹H NMR studies and MM computations revealed that, on complexation, the hydrophobic central benzene ring of Ibu.T and part of the isobutyl group reside within the β-CyD cavity leaving the peripheral groups (carboxylate, tromethamine and methyl groups) located near the hydroxyl group networks at either rim of β-CyD. PSD, ¹H NMR, DSC, FT-IR, XRPD, SEM and MM studies confirmed the formation of Ibu.T/β-CyD inclusion complex in solution and the solid state.     

Preparation, characterization and dissolution enhancement of mefloquine hydrochloride-betaCD inclusion complex

The solid state properties and dissolution behaviour of binary systems of mefloquine hydrochloride (MH) with betaCD were investigated. MH-betaCD interaction in the solution state was studied by phase solubility analysis and demonstrates the ability of 3CD to complex with MH giving AL type profile with 120.34 M-1 stability constant. The kneading method was adopted to prepare binary sytems of MH with betaCD in 1:1 molar ratio. The solid inclusion was characterized by differential scanning calorimetry, fourier transformation infrared spectroscopy and X-ray powder diffractometry. Experimental results confirmed the existence of 1:1 inclusion complex of MH with ICD. Aqueous solubility of MH was found to be enhanced by 118% for inclusion complex. The dissolution properties of binary systems were studied in simulated gastric fluid without enzyme and compared with MH alone. The inclusion complex of MH prepared with 3CD showed a dissolution rate several times faster than that of physical mixture and pure drug.     

复方氧氟沙星双层口腔贴膜的研制及质量控制

目的：本文阐述复方氧氟沙星双层口腔贴膜的研制及质量控制。方法：以西药氧氟沙星、达克罗宁，中药玄参，红花为主药，以PVA17-88、CMC-Na按适当比例为基质制成一定厚度的膜剂，以紫外分光光度计扫描和薄层色谱法来控制质量。结果：制成的膜剂塑性，色泽良好，以紫外扫描在288nm处有明显的吸收峰，薄层层析供试品与对照品在相同的位置有斑点。结论：该制剂符合《中国人民解放军医疗单位制剂规范》膜剂项下的有效规定。     

氟苯尼考-β-环糊精包合物的制备与结构表征#br#

目的 为改善氟苯尼考的水溶性,采用β-环糊精包合技术制备氟苯尼考可溶性粉。方法 通过正交试验筛选最佳包合工艺,以包合率和包合物产率为评价指标,以差示扫描量热分析法,傅里叶红外光谱法,电镜扫描对包合物进行结构确证。结果 试验结果表明：最佳包合条件为氟苯尼考与β-环糊精投料摩尔比1:1、包合温度80℃、包合时间2h、搅拌速度 500r/min;差示扫描量热分析,傅里叶红外光谱分析和电镜扫描结果证实氟苯尼考-β-环糊精包合物的形成;氟苯尼考-β-环糊精包合物的包合率平均值为91.85%,产率平均值为91.26%,15min溶出率达到100%,为氟苯尼考的5倍。结论 采用饱和水溶液法制备氟苯尼考-β-环糊精包合物的制备工艺方法简单,可提高氟苯尼考水溶性。     

双氢青蒿素羟丙基-β-环糊精包合物的制备与表征

采用正交设计法,以双氢青蒿素(dihydroartemisinin,DHA)和羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)的摩尔比、包合温度和包合时间为考察因素,以包合物中DHA的包封产率和载药量为评价指标,优选包合工艺。用红外光谱法、差示扫描量热法和粉末X-射线衍射法表征制备的包合物,并采用分子模拟技术研究HP-β-CD包合DHA的可行性。结果显示,最佳包合条件:DHA与HP-β-CD的投料摩尔比为1∶5、包合温度为50℃、包合时间为1 h。红外光谱法、差示扫描量热法和粉末X-射线衍射分析均表明DHA与HP-β-CD形成了包合物,分子模拟结果揭示了DHA与HP-β-CD包合物具有较低的结合自由能和较高的溶剂可及表面积,HP-β-CD包合DHA可行,能显著提高DHA的水溶性。DHA-HP-β-CD包合工艺可行,为研究生产工艺提供了理论和实验依据。     

Novel,potent calmodulin antagonists derived from an all‐d hexapeptide combinatorial library that inhibit in vivo cell proliferation: activity and structural characterization

Abstract: Calmodulin is known to bind to various amphipathic helical peptide sequences, and the calmodulin–peptide binding surface has been shown to be remarkably tolerant sterically. d ‐Amino acid peptides, therefore, represent potential non‐hydrolysable intracellular antagonists of calmodulin. In the present study, synthetic combinatorial libraries have been used to develop novel d ‐amino acid hexapeptide antagonists to calmodulin‐regulated phosphodiesterase activity. Five hexapeptides were identified from a library containing over 52 million sequences. These peptides inhibited cell proliferation both in cell culture using normal rat kidney cells and by injection via the femoral vein following partial hepatectomy of rat liver cells. These hexapeptides showed no toxic effect on the cells. Despite their short length, the identified hexapeptides appear to adopt a partial helical conformation similar to other known calmodulin‐binding peptides, as shown by CD spectroscopy in the presence of calmodulin and NMR spectroscopy in DMSO. The present peptides are the shortest peptide calmodulin antagonists reported to date showing potential in vivo activity.     

伊曲康唑/羟丙基-β-环糊精包合物的制备和特性

目的:研究伊曲康唑/羟丙基-β-环糊精包合物的特性.方法:用冷冻干燥法制备包合物.通过测定粒径、ζ电位、渗透压、溶血性、相溶解度和差示扫描量热分析、傅立叶红外光谱及粉末X-射线衍射,表征包合物的特性.结果:粒径(12.1±1.8)nm,渗透压(611±3)mOsm·L-1.伊曲康唑的溶解度随羟丙基-β-环糊精浓度的提高明显增大,曲线呈AP型,表明药物与环糊精形成1:n(n＞1)的包合物.羟丙基-β-环糊精浓度＞0.6mg·mL-1(0.388 1mmol·L-1)可引起家兔红细胞溶血.结论:伊曲康唑/羟丙基-β-环糊精包合物能显著提高伊曲康唑的溶解度.