10例脑外伤病人硫酸妥布霉素的药物动力学特性

目的：比较硫酸妥布霉素ｉｖ ｇｔｔ或气管滴入的药物动力学。方法：用ＦＰＩＡ法测定１０例脑外伤病人ｉｖ ｇｔｔ或气管滴入硫酸妥布霉素后的血药浓度。结果：２种给药方法均符合一房室模型的药物动力学特征，且给药后２ｈ均能达到有效血浓度（２￣１２μｇ／ｍｌ），但血药浓度及主要药物动力学参数个体差异较大。结论：ｉｖ ｇｔｔ给药和于脑外伤短期预防给药、气管滴入能有效地预防肺部感染。     

The effect of therapeutic soft contact lenses on antibiotic delivery to the cornea

The effects of high (71%) and low (38.6%) water content lenses on antibiotic delivery to the cornea were studied in rabbits by measuring corneal tobramycin concentrations 1, 2, 4 and 6 hours after topical application at intervals of 15 minutes. In the presence of the low water content lens corneal drug levels were higher than in control corneas for every time point assayed. This difference was only significant at 4 hours (P less than 0.05). In eyes wearing the high water content contact lens corneal drug concentration was also higher at every time point tested except one hour. The difference was significant only at 4 hours (P less than 0.01). The data suggest that in the normal, noninflammed eye, the presence of a therapeutic soft contact lens will not compromise aminoglycoside delivery to the cornea.     

Formulation and Characterization of Lipid-Coated Tobramycin Particles for Dry Powder Inhalation

Purpose This study was conducted to develop and evaluate the physicochemical and aerodynamic characteristics of lipid-coated dry powder formulations presenting particularly high lung deposition. Methods Lipid-coated particles were prepared by spray-drying suspensions with different concentrations of tobramycin and lipids. The solid-state properties of the formulations, including particle size and morphology, were assessed by scanning electron microscopy and laser diffraction. Aerosol performance was studied by dispersing the powders into a Multistage Liquid Impinger and determining drug deposition by high-performance liquid chromatography. Results Particle size distributions of the formulations were unimodal, narrow with more than 90% of the particles having a diameter of less than 2.8 μm. All powder formulations exhibited mass median diameters of less than 1.3 and 3.2 μm, as determined by two different laser diffraction methods, the Malvern's Mastersizer? and Spraytec?, respectively. The fine particle fraction varied within a range of 50.5 and 68.3%. Conclusions Lipid coating of tobramycin formulations resulted in a reduced agglomeration tendency and in high fine particle fraction values, thus improving drug deposition. The very low excipients content (about 5% m/m) of these formulations offers the benefit of delivering particularly huge concentrations of antibiotic directly to the site of infection, while minimizing systemic exposure, and may provide a valuable alternative treatment of cystic fibrosis.     

Tobramycin for inhalation in cystic fibrosis: Beyond respiratory improvements

European consensus guidelines recommend nebulised antibiotics for maintenance therapy in patients with cystic fibrosis and chronic Pseudomonas aeruginosa infection. Two formulations of tobramycin for inhalation are available in Europe (Tobi^®; Novartis AG, Switzerland; Bramitob^®; Chiesi Farmaceutici S.p.A., Italy). Data from a series of randomised controlled studies in patients with mild-to-moderate cystic fibrosis and chronic P. aeruginosa infection show that both Tobi^® and Bramitob^® significantly improve lung function and reduce the density of P. aeruginosa in sputum. Bacterial resistance may develop but does not seem to be clinically important. Other benefits, such as improved patient nutritional status and reductions in the need for hospitalisation, antipseudomonal antibiotics and productivity losses have also been documented with Tobi^® and Bramitob^®. Both formulations of inhaled tobramycin are well tolerated with no evidence of renal or ototoxicity. Improved patient compliance may be achieved through reducing nebulisation time, either by using Bramitob^®, which is formulated in a smaller volume than Tobi^®, or with new generation nebulisers. In conclusion, inhaled tobramycin not only improves lung function in patients with cystic fibrosis, but also offers other benefits which have implications for healthcare costs and patient quality of life.     

氯替泼诺妥布霉素混悬滴眼液微生物限度检查方法的探讨

目的：建立氯替泼诺妥布霉素混悬滴眼液的微生物限度检查方法。方法：参照中国药典2005年版二部附录微生物限度检查方法进行试验。结果：采用直接接种法对人工污染的六种菌株进行试验,该药品对四株细菌有不同程度的抑菌作用．采用薄膜过滤法用0.1％蛋白胨水加聚山梨酯进行样品处理,300ml 0.1％蛋白胨水分三次冲洗,可消除其抑菌成分。结论：建立的氯替泼诺妥布霉素混悬滴眼液微生物限度检查方法简单,准确、可靠。     

Novel approach to the eradication of Pseudomonas aeruginosa in an infant with CF after outpatient treatment failure

Intravenous continuous infusion of betalactam (CIBL) antibiotic and high dose extended interval (HDEI) aminoglycoside therapy theoretically maximize bacterial killing in treatment of Pseudomonas aeruginosa (PsA) in pulmonary exacerbations of cystic fibrosis (CF). We present the case of a 3-month-old female infant with CF who failed outpatient eradication of PsA with subsequent eradication using intravenous CIBL antibiotic and HDEI aminoglycoside therapy. This antibiotic combination should be considered in order to optimize pharmacodynamics for PsA eradication in CF patients before development of chronic colonization.     

HPLC梯度洗脱法测定氯替泼诺妥布霉素复方混悬滴眼液中氯替泼诺含量及有关物质

摘 要 目的： 建立HPLC梯度法测定氯替泼诺妥布霉素复方混悬滴眼液中氯替泼诺含量及有关物质。方法: 采用HPLC法,色谱柱：Inertsil ph苯基柱（250 mm×4.6 mm,5 μm）;流动相A：0.25%醋酸溶液 乙腈（80∶20）;流动相B：乙腈;流速：2.0 ml·min^-1,进行线性梯度洗脱;检测波长：244 nm;柱温：30℃;进样量：20 μl。结果: 主成分与各杂质峰分离度良好。氯替泼诺浓度在0.001~1.02 mg·mL^-1（r=0.999 9）范围内与峰面积线性关系良好,平均回收率为99.9%,RSD为0.9%（n=9）。结论:该方法灵敏准确,色谱峰分离完全,可用于氯替泼诺妥布霉素混悬滴眼液的质量控制。     

逍遥散联合妥布霉素地塞米松治疗睑板腺功能障碍性干眼症的研究

目的：观察逍遥散联合妥布霉素地塞米松治疗睑板腺功能障碍(MGD)性干眼症的临床疗效。

方法：选取2015-11/2017-11就诊于南阳市卧龙区第一人民医院的睑板腺功能障碍性干眼症患者106例134眼,随机分为对照组和观察组,各53例67眼。两组均给予热敷、按摩等基础治疗,对照组给予妥布霉素地塞米松治疗,观察组在对照组基础上联合逍遥散治疗。观察两组患者的临床疗效及治疗前后干眼症症状、角膜荧光染色(FL)、视功能损害眼病患者生活质量量表(SQOL DVI)评分、泪膜破裂时间(BUT)和泪液分泌量(SⅠt)等情况。

结果：治疗后,观察组患者治疗总有效率(86.6%)显著高于对照组(67.2%),干眼症症状、角膜FL评分均显著低于对照组,BUT和SⅠt值及SQOL DVI评分均显著高于对照组,差异均有统计学意义(P<0.01)。治疗期间,观察组眼压升高发生率显著低于对照组,差异有统计学意义(P<0.05)。

结论：逍遥散联合妥布霉素地塞米松治疗睑板腺功能障碍性干眼症,能够显著提高疗效,改善预后情况。