复方黄连素注射液的差示分光光度测定

复方黄连素注射液的差示分光光度测定朱建永（淮北市药品检验所，安徽２３５０００）ＤＥＴＥＲＭＩＮＡＴＩＯＮＯＦＣＯＭＰＯＵＮＤＢＥＲＢＥＲＩＮＥＩＮＪＥＣＴＩＯＮＢＹＤＩＦＦＥＲＥＮＴＩＡＬＳＰＥＣＴＲＯＰＨＯＴＯＭＥＴＲＹ￥ＺＨＵＪｉａｎ－Ｙｏｎｇ（...     

复方黄连素注射液的HPLC测定

复方黄连素注射液的ＨＰＬＣ测定杜兴，阚学瑾（甘肃省药品检验所，兰州７３００００）ＤＥＴＥＲＭＩＮＡＴＩＯＮＯＦＣＯＭＰＯＵＮＤＢＥＲＢＲＩＮＥＩＮＪＥＣＴＩＯＮＢＹＨＰＬＣ￥ＤＵＸｉｎｇ；ＫＡＮＸｕｅ－Ｊｉｎ（ＧａｎｓｕＰｒｏｖｉｎｃｉａｌＩｎｓｔｉ...     

复方丹参注射液治疗慢性肾衰的疗效观察

本文观察了复方丹参注射液对慢性肾衰的治疗作用。选择慢性肾衰患者５４例，随机分为治疗组（２７例）和对照组（２７例）。观察治疗前后血尿素氮（ＢＵＮ）、血肌酐（Ｓｃｒ）、血红蛋白（Ｈｂ）、血钙、血磷等指标的变化。结果：复方丹参治疗后ＢＵＮ、Ｓｃｒ较治疗前明显下降（Ｐ＜０．０５和Ｐ＜０．０１），与对照组比较ＢＵＮ也有显著下降（Ｐ＜０．０５），显示复方丹参注射液对慢性肾衰有一定的治疗作用。     

重组人表皮生长因子联合无环鸟苷治疗单疱病毒性角膜炎

目的：观察重组人表皮生长因子滴眼剂联合无环鸟苷治疗单疱病毒性角膜炎的疗效。方法：采用随机双盲法将113例（124只眼）患者分为治疗组64只眼，接受重组人表皮生长因子滴眼剂联合0．1％无环鸟苷滴眼剂治疗；对照组60只眼接受0．1％无环鸟苷滴眼剂治疗，两组均在用药1～3周后观察疗效。结果：对照组有效率为71．7％，治疗组有效率为96．9％，组间差异有极显著性（P〈0．01）。结论：重组人表皮生长因子滴眼剂联合0．1％无环鸟苷滴眼剂治疗单疱病毒性角膜炎的疗效确切，且安全可靠，不良反应少。     

抗血小板药物与溶栓剂联合溶栓治疗深静脉栓塞治疗机制的研究

抗血小板药物与溶栓剂联合溶栓治疗深静脉栓塞治疗机制的研究山西医学院第一附属医院（０３０００１）李正中，贺抗，温柱德，李思晋我们联合应用尿激酶（ＵＫ）、前列腺素Ｅ１（ＰＧＥｌ）和中药，对５６例深静脉栓塞（ＤＶＴ）病人进行治疗并检测凝血及纤溶指标，以探讨治疗机制及监测指标。材料与方法一、材料：ＵＫ：２万单位／Ａｍｐｌｅ，南京大学制药厂提供。１０万单位／Ａｍｐｌｅ，太原生化制药厂。ＰＧＥ１：白求恩医科大学制药厂。６０％泛影葡胺，上海信谊药厂。二、病例选择：７１例深静脉栓塞（ＤＶＴ）病人。随机分为二组进行治疗。治疗前均经９９ｍＴｃ－ＲＢＣ，ＥＣＴ血管显像及静脉造影确诊。①ＵＫ治疗组：５４例５６肢体，男２６例，女２８例；年龄２２～７８岁（４８．５±１５．９２）。病程２天～３年。５０例左下肢栓塞，２例左上肢，２例双下肢栓塞。②对照组：１５例。男７例，女８例。年龄２９～６８岁（４１．３±２０．６）。病程６月～１０年。三、治疗方案：①治疗组：ＵＫ２０００００Ｕ／日。静脉滴注，３小时滴完，每日一次，同时滴注ＰＧＥ１２００ｎｇ／日及中药通脉汤口服，１０天为一疗程。根据病情治疗２～３疗程。两疗程间休息３～５大。②对照组：１０例静     

RP－HPLC法测定人血清中卡马西平及其环氧化物

用ＲＰ－ＨＰＬＣ法测定人血清中卡马西平（ＣＢＺ）及活性代谢产物卡马西平１０，１１－环氧化物（ＣＢＺ－Ｅ）的含量。血清样品用乙醚－二氯甲烷（３：１，Ｖ／Ｖ）混合溶剂提取，以硝基安定为内标，乙腈－水（４０：６０，Ｖ／Ｖ）为流动相，流速为１．２０ｍｌ／ｍｉｎ，ＵＶ２１５ｎｍ处测定；ＣＢＺ－Ｅ和ＣＢＺ最低检测浓度分别为５０和６０ｎｇ／ｍｌ；线性范围为０．１～５．０μｇ／ｍｌ和０．２～２０μｇ／ｍｌ；ＲＳＤ在５％以下。应用本法测定了８名癫痫病人单一服用ＣＢＺ治疗血清中ＣＢＺ和ＣＢＺ－Ｅ的浓度。     

人血清中替卡西林的改良离子对高压液相色谱法

人血清中替卡西林的改良离子对高压液相色谱法朱珠，宣大伟，ＣｈａｒｌｅｓＨＮＩＧＨＴＩＮＧＡＬＥ（美国康涅狄格州大学暨哈特福德医院药物研究室，Ｈａｒｔｆｏｒｄ，ＣＴ０６１０２，ＵＳＡ）关键词替卡西林；高压液相色谱法；青霉素类目的：建立测定人血清中替卡西...     

复方丁胺卡那霉素注射液的毒性研究

复方丁胺卡那霉素注射液的毒性研究曹秀文，陈林滨，刘炜，韩文华（河北省药品检验所，石家庄０５００１１）ＳＴＵＤＹＯＮＴＯＸＩＣＩＴＹＯＦＣＯＭＰＯＵＮＤＡＭＩＫＡＣＩＮＩＮＪＥＣＴＩＯＮ￥ＣＡＯＸｉｕ－Ｗｅｎ；ＣＨＥＮＬｉｎ－Ｂｉｎ；ＬＩＵＷｅｉ；ＨＡ...     

原因不明发热198例分析

对１９８例原因不明发热（ＦｅｖｅｒｏｆＵｎｋｎｏｗｎＯｒｉｇｉｎＦＵＯ）患者生病原学、血清学、组织学等方法检查确定其诊断。结果为感染性疾病占首位（５１．０１％），且以局限于某一器官感染为多，血管－结缔组织疾病占２５．７６％，肿瘤占９．６０％，药物热占４．５４％，出院或死亡时仍珍断不清者占９．０９％。肿瘤在ＦＵＤ中比例呈下降趋势（Ｐ＜０．０５），可能由于新的诊断仪器如Ｂ超，ＣＴ等在临床广泛使用，命名     

氧氟沙星滴眼剂临床疗效评价

目的：评价氧氟沙星滴眼剂的临床疗效及其安全性。方法：眼疾病病人验证组１２１例（男性６３例,１００只眼,女性５８例,８８只眼,年龄３０ａ±ｓ２１ａ）,用伊犁哈萨克自治州友谊医院研制的０．３％氧氟沙星滴眼剂。对照组３９例（男性１５例,２２只眼,女性２４例,３５只眼,年龄３５ａ±１０ａ）,用日本参天制药株式会社生产的０．３％氧氟沙星滴眼剂。每次均１滴（约０．２ｍＬ）,ｔｉｄ。治疗开始后ｄ４,ｄ７及ｄ１４复诊。结果：验证组细菌性眼疾病总显效率为７１．３％,对照组为３２％（Ｐ＜０．０１）。结论：伊犁哈萨克自治州友谊医院研制的氧氟沙星滴眼剂对细菌性眼疾有明显治疗作用。     

氟康唑原位胶化滴眼液眼内药代动力学研究

目的　比较氟康唑滴眼液及其原位胶化滴眼液在兔眼内药代动力学。方法　两种制剂滴眼后,用气相色谱法测定不同时间的兔眼结膜囊内泪液和房水中氟康唑浓度,药动学参数用非线性最小二乘法进行计算机拟合求得。结果　用药后180 min内,原位胶化组各时间点结膜囊内泪液药物浓度均明显高于一般滴眼液组。原位胶化组的房水药物浓度-时间曲线下面积和消除半衰期明显高于对照组,达峰时间延迟,但达峰浓度与一般滴眼液组无明显差异。结论　氟康唑原位胶化滴眼液可明显延长药物在眼部的滞留时间,提高药物的生物利用度。     

Topically applied 1% voriconazole induces dysplastic changes on the ocular surface: animal study

Purpose: To identify the risk of inducing ocular surface dysplasia following topical administration of 1% voriconazole eye drop.

Methods: Fourteen noninflamed healthy eyes of 14 white adult New Zealand rabbits were included in the study. The rabbits were randomly divided into two groups comprised of 7 rabbits each. Group 1 received topical 1% voriconazole and Group 2 received topical saline as the control group. In all animals, right eye was selected for the study. In Group 1 (Voriconazole Group), single drop of voriconazole was instilled every 10?min consecutively for 17 times a day for 60?days. In Group 2 (Control Group), single drop of saline was instilled every 10?min consecutively for 17 times a day for 60?days. At two months, animals were sacrificed and study eyes were enucleated with the eyelids. The specimens were stained with hematoxylin-eosin and histopathologic changes in cornea, bulbar and palpebral conjunctiva were evaluated under light microscope.

Results: There were no macroscopically visible lesions on the ocular surface of any rabbits. Histopathological evaluation showed mild to moderate dysplasia localized mainly in the limbus and extending to the adjacent cornea and bulbar conjunctiva in all rabbits in Voriconazole Group. Severe dysplasia or carcinoma in situ was not observed. In the Control Group, dysplasia was not observed, at all.

Conclusion: This animal study provides a possible relationship between topically administered 1% voriconazole and ocular surface dysplasia. We recommend ophthalmologists to be aware of the risk of ocular surface dysplasia in patients received voriconazole eye drop.     

A comparison of the fourth-generation fluoroquinolones gatifloxacin 0.3% and moxifloxacin 0.5% in terms of ocular tolerability

PURPOSE: To compare the ocular tolerability of the commercially available ophthalmic solutions of the fourth-generation fluoroquinolones, gatifloxacin 0.3% (Zymar, Allergan, Inc., Irvine, CA) with benzalkonium chloride (BAK) and moxifloxacin 0.5% (Vigamox) without BAK. METHODS: A baseline evaluation was conducted on 30 healthy volunteers for conjunctival hyperemia, conjunctival vascularity, pupil size, and anterior chamber (AC) cell and flare. Pupils were measured under scotopic conditions with a Colvard pupillometer. Conjunctival hyperemia and vascularity, and AC reaction were measured on a Likert-like scale of 0-3. Subjects then received drops in both eyes from masked bottles of gatifloxacin ophthalmic solution 0.3% with BAK (in one eye determined randomly) and moxifloxacin ophthalmic solution 0.5% without BAK (in the contralateral eye) in a double-masked fashion. Subjects graded pain and ocular irritation in each eye on a scale of 1-10 after 5 min with their eyes closed. The examination was then repeated. RESULTS: The average age of this study population was 34.4 years. The groups of eyes receiving moxifloxacin 0.5% demonstrated an increase in mean conjunctival hyperemia (0.21 [range: 0-1] at baseline to 1.52 [range: 0-3] at 5 min.) that was significantly greater (p = 0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.22 [range: 0-1] at baseline to 0.45 [range: 0-2] at 5 min). The group receiving moxifloxacin 0.5% showed an increase in conjunctival vascularity (0.55 [range: 0-1] at baseline to 1.61 [range: 0.5-3] at 5 min.) that was significantly greater (p = 0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.52 [range: 0-1] at baseline to 0.68 [range: 0-2] at 5 min.). Significantly less pain (1.2 vs. 3.2, p = 0.001) and irritation (0.64 vs. 3.42, p = 0.001) occurred with gatifloxacin 0.3% than with moxifloxacin 0.5%. Pupil size was significantly reduced (5.65 mm-5.05 mm) in eyes receiving moxifloxacin 0.5% (p = 0.004) and no significant change occurred in pupil size (5.60 mm-5.65 mm) in eyes that received gatifloxacin 0.3% (p = 0.878). No AC reaction was noted with either medication. CONCLUSIONS: The group of eyes receiving gatifloxacin 0.3% with BAK demonstrated greater ocular tolerability in comparison to the group receiving moxifloxacin 0.5% without BAK. Moxifloxacin-induced pupillary miosis may be due to prostaglandin release in the anterior chamber. A limitation of this study is the relatively young age of the study population.     

Ocular pharmacokinetics of verapamil in rabbits

Previously, it had been demonstrated that cataract in diabetic rats can be prevented by systemical administration of the calcium channel blocker verapamil. In addition to that, 0.125% verapamil eye drops were found to significantly reduce the intraocular pressure in ocular hypertensive human subjects. The purpose of this study was to investigate the ocular penetration and elimination of verapamil after topical administration of the drug in rabbits. Two drops of a 0.125% aqueous solution of RS-verapamil hydrochloride (corresponding to a total dose of 125 μg RS-verapamil hydrochloride) were administered into the conjunctival sac. Aqueous humor and blood samples were taken at different times after administration and analysed for drug concentration by combined gas chromatography-mass spectroscopy. Following the instillation of 0.125% verapamil eye drops in a total dose of 125 μg RS-verapamil, mean (± SEM) aqueous humor peak levels of 1607 ± 272 ng/ml were achieved after 20 min. Mean half-life for the elimination from the aqueous humor was 33 min. Topical application of verapamil produced very low serum peak concentrations (10.5 ± 1.3 ng/ml). The results of our study demonstrate that topically administered verapamil readily penetrates into the anterior chamber leading to aqueous humor drug levels in the μM range without producing serum levels that are high enough to cause cardiovascular side effects. Received: 9 September 1997 / Accepted: 18 November 1997     

Novel mucoadhesive polysaccharide isolated from Bletilla striata improves the intraocular penetration and efficacy of levofloxacin in the topical treatment of experimental bacterial keratitis

Objectives The objective of the present study was to evaluate a novel mucoadhesive polymer extracted from Bletilla striata for ocular delivery of 0.5% levofloxacin in rabbits, and to determine its improved efficacy against experimental keratitis. Methods B. striata polysaccharide (BsP) was subjected to cell cytotoxicity and ferning tests. The pharmacokinetics and bioavailability of topically applied 0.5% levofloxacin‐BsP eye drops was investigated and compared with 0.5% levofloxacin eye drops (Cravit). Experimental Staphylococcus aureus keratitis was induced and treated with levofloxacin or levofloxacin‐BsP eye drops. Key findings BsP markedly increased the proliferative capacity of a human corneal endothelial cell line. The ferning test showed that BsP exhibited optimal performance as a tear fluid. The polysaccharides significantly increased intra‐aqueous penetration and corneal accumulation in rabbits. Treatment with levofloxacin‐BsP reduced the number of organisms more significantly than eye drops containing levofloxacin alone. Conclusions BsP appears to be a promising candidate as a vehicle for topical ophthalmic drug delivery, especially for antibiotics.     

糖尿病视网膜病变患者围手术期散瞳策略

目的：探讨糖尿病视网膜病变患者围手术期最佳散瞳方法,以利于玻璃体切割手术顺利进行。方法：回顾性分析我院2007年6月-2011年6月所有糖尿病视网膜病变患者的手术资料,选取术前常规应用复方托吡卡胺滴眼液、术中瞳孔直径≥7mm的患者手术时散瞳药的应用记录,共189例,204眼。术前点复方托吡卡胺滴眼液,每5min1次,共6次。点滴眼液后,0.5h内瞳孔散大（直径≥7mm）者为A组（78眼）;超过0.5h,但瞳孔散大时间在1h以内者为B组（75眼）;瞳孔散大时间大于1h者为C组（51眼）。B、C组于术前一天随机应用硫酸阿托品眼用凝胶或盐酸环喷托酯滴眼液,术前1h频点复方托吡卡胺滴眼液。结果：术中瞳孔直径能维持≥7mm的眼数比例,B、C组应用硫酸阿托品眼用凝胶者与应用盐酸环喷托酯滴眼液者差异均无统计学意义（P〉0.5）。术中有134眼因白内障同时行超声乳化白内障摘除术,其术中瞳孔直径能维持≥7mm的眼数比例,B组应用盐酸环喷托酯滴眼液者瞳孔维持的比例较用硫酸阿托品眼用凝胶者高（P〈0.5）,C组中二者比较差异无统计学意义（P〉0.5）。结论：对于术前单用复方托吡卡胺滴眼液散瞳时间超过0.5h者,术前点硫酸阿托品眼用凝胶或盐酸环喷托酯滴眼液有利于维持术中瞳孔大小,且二者效果差异无统计学意义。     

Comparative efficacy of olopatadine 0.1% ophthalmic solution versus levocabastine 0.05% ophthalmic suspension using the conjunctival allergen challenge model

OBJECTIVE: To compare the efficacy of olopatadine and levocabastine in reducing ocular allergic itching and vascular hyperemia (redness) induced by conjunctival allergen challenge. RESEARCH DESIGN AND METHODS: The study was a randomized, double-masked, contralateral study using the conjunctival allergen challenge (CAC) model. At Visit 1, subjects with a positive allergen skin test and a history of allergic conjunctivitis were administered increasing concentrations of allergen until at least a moderate grade 2 ocular itching and conjunctival redness response was obtained in both eyes. Allergic signs were graded on standardized 0-4 scales. Subjects who reacted positively were re-challenged at Visit 2 with the pre-determined concentration of allergen. Subjects who again responded with at least a grade 2 bilateral ocular itching and conjunctival redness score at Visit 2 were eligible for drug evaluation. At Visit 3, subjects received olopatadine in one eye and levocabastine in the contralateral eye according to a computer-generated randomization scheme generated prior to commencement of the study. Ocular discomfort was then graded in both eyes. Subjects were bilaterally challenged with the predetermined concentration of allergen 27 min after topical drug administration, such that the first post-challenge assessment was made 30 min post-drug instillation. Allergic signs and symptoms were evaluated at 3 min, 10 min, and 20 min postchallenge and safety and efficacy analyses were performed. RESULTS: Sixty-eight subjects received study drug and were included in the safety and efficacy analyses. Ocular itching scores for olopatadine were significantly lower than levocabastine at 3 min and 10 min post-challenge (p < 0.001). Ocular redness scores for olopatadine were significantly lower than levocabastine at all time points post-challenge (p < 0.0001). Of all subjects, 4.41% reported ocular discomfort in the olopatadine eye and 26.5% in the levocabastine treated eye. CONCLUSION: Olopatadine treated eyes had significantly less itching and redness than levocabastine treated eyes after conjunctival allergen challenge. Olopatadine was also associated with less discomfort upon instillation than levocabastine.     

A comparison of the fourth-generation fluoroquinolones gatifloxacin 0.3% and moxifloxacin 0.5% in terms of ocular tolerability

SUMMARY

Purpose: To compare the ocular tolerability of the commercially available ophthalmic solutions of the fourth-generation fluoroquinolones, gatifloxacin 0.3% (Zymart, Allergan, Inc., Irvine, CA) with benzalkonium chloride (BAK) and moxifloxacin 0.5% (Vigamoxt) without BAK.

Methods: A baseline evaluation was conducted on 30 healthy volunteers for conjunctival hyperemia, conjunctival vascularity, pupil size, and anterior chamber (AC) cell and flare. Pupils were measured under scotopic conditions with a Colvard pupillometer. Conjunctival hyperemia and vascularity, and AC reaction were measured on a Likert-like scale of 0-3. Subjects then received drops in both eyes from masked bottles of gatifloxacin ophthalmic solution 0.3% with BAK (in one eye determined randomly) and moxifloxacin ophthalmic solution 0.5% without BAK (in the contralateral eye) in a double-masked fashion. Subjects graded pain and ocular irritation in each eye on a scale of 1-10 after 5min with their eyes closed. The examination was then repeated.

Results: The average age of this study population was 34.4years. The groups of eyes receiving moxifloxacin 0.5% demonstrated an increase in mean conjunctival hyperemia (0.21 [range: 0-1] at baseline to 1.52 [range: 0-3] at 5min.)

that was significantly greater (p?=?0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.22 [range: 0-1] at baseline to 0.45 [range: 0-2] at 5min). The group receiving moxifloxacin 0.5% showed an increase in conjunctival vascularity (0.55 [range: 0-1] at baseline to 1.61 [range: 0.5-3] at 5?min.) that was significantly greater (p?=?0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.52 [range: 0-1] at baseline to 0.68 [range: 0-2] at 5?min.). Significantly less pain (1.2 vs. 3.2, p?=?0.001) and irritation (0.64 vs. 3.42, p?=?0.001) occurred with gatifloxacin 0.3% than with moxifloxacin 0.5%. Pupil size was significantly reduced (5.65mm-5.05mm) in eyes receiving moxifloxacin 0.5% (p?=?0.004) and no significant change occurred in pupil size (5.60mm-5.65mm) in eyes that received gatifloxacin 0.3% (p?=?0.878). No AC reaction was noted with either medication.

Conclusions: The group of eyes receiving gatifloxacin 0.3% with BAK demonstrated greater ocular tolerability in comparison to the group receiving moxifloxacin 0.5% without BAK. Moxifloxacin-induced pupillary miosis may be due to prostaglandin release in the anterior chamber. A limitation of this study is the relatively young age of the study population.     

牛磺酸滴眼液的渗透压考察及其影响因素分析

目的:了解牛磺酸滴眼液的渗透压现状及处方组成对其影响情况。方法:采用SMC-30B渗透压摩尔浓度测定仪,采用冰点下降法对国内5个厂家牛磺酸滴眼液进行渗透压摩尔浓度测定。结果:多数牛磺酸滴眼液的渗透压均高出人眼可耐受的渗透压范围,处方组成的不合理是造成渗透压超标的主要因素。结论:牛磺酸滴眼液的渗透压现状亟待解决,其处方组成需要进一步研究改进。     

Comparative efficacy of olopatadine 0.1% ophthalmic solution versus levocabastine 0.05% ophthalmic suspension using the conjunctival allergen challenge model

SUMMARY

Objective: To compare the efficacy of olopatadine and levocabastine in reducing ocular allergic itching and vascular hyperemia (redness) induced by conjunctival allergen challenge.

Research design and methods: The study was a randomized, double-masked, contralateral study using the conjunctival allergen challenge (CAC) model. At Visit 1, subjects with a positive allergen skin test and a history of allergic conjunctivitis were administered increasing concentrations of allergen until at least a moderate grade 2 ocular itching and conjunctival redness response was obtained in both eyes. Allergic signs were graded on standardized 0–4 scales. Subjects who reacted positively were re-challenged at Visit 2 with the pre-determined concentration of allergen. Subjects who again responded with at least a grade 2 bilateral ocular itching and conjunctival redness score at Visit 2 were eligible for drug evaluation. At Visit 3, subjects received olopatadine in one eye and levocabastine in the contralateral eye according to a computer-generated randomization scheme generated prior to commencement of the study. Ocular discomfort was then graded in both eyes. Subjects were bilaterally challenged with the predetermined concentration of allergen 27?min after topical drug administration, such that the first post-challenge assessment was made 30?min post-drug instillation. Allergic signs and symptoms were evaluated at 3?min, 10?min, and 20?min post-challenge and safety and efficacy analyses were performed.

Results: Sixty-eight subjects received study drug and were included in the safety and efficacy analyses. Ocular itching scores for olopatadine were significantly lower than levocabastine at 3?min and 10?min post-challenge (?p < 0.001). Ocular redness scores for olopatadine were significantly lower than levocabastine at all time points post-challenge (?p < 0.0001). Of all subjects, 4.41% reported ocular discomfort in the olopatadine eye and 26.5% in the levocabastine treated eye.

Conclusion: Olopatadine treated eyes had significantly less itching and redness than levocabastine treated eyes after conjunctival allergen challenge. Olopatadine was also associated with less discomfort upon instillation than levocabastine.