鱼腥草热敏凝胶滴眼液的特性及临床疗效

目的观察鱼腥草热敏凝胶滴眼液的特性和临床疗效。方法以鱼腥草为主药、热敏材料泊洛沙姆407为辅料配制热敏凝胶滴眼液,测定其相转变温度、吸附量、凝胶累积溶蚀量,并与鱼腥草滴眼液和病毒唑滴眼液进行临床对照研究。结果其液态转变为凝胶的相转变温度为34.5℃,于37℃变成凝胶后其吸附量比液态滴眼液大大增加,凝胶累积溶蚀量与溶出介质加入量呈线性关系,40m in累积溶蚀量达98.76%;其临床疗效比同浓度的鱼腥草滴眼液和病毒唑滴眼液均好。结论鱼腥草热敏凝胶滴眼液是眼科长效制剂,滴眼次数少,临床疗效高。     

贝复舒滴眼液联合眼用凝胶治疗眼表面损伤疗效观察

目的：观察贝复舒滴眼液联合眼用凝胶治疗眼表面损伤的临床疗效。方法：将89例眼表面损伤患者随机分为对照组44例（44眼）,观察组45例（45眼）,观察组予以贝复舒滴眼液联合眼用凝胶治疗,对照组予以复方硫酸软骨素滴眼液,比较两组患者治疗2周后的临床疗效。结果：治疗2周后,观察组总有效率为100.00%,治愈率为62.22%,均高于对照组的86.36%、34.09%,差异有统计学意义。结论：贝复舒滴眼液联合眼用凝胶治疗眼表面损伤疗效确切,优于复方硫酸软骨素滴眼液。     

双黄连滴眼液联合更昔洛韦眼用凝胶治疗单疱病毒性角膜炎的临床研究

目的：观察双黄连滴眼液与更昔洛韦眼用凝胶治疗单疱病毒性角膜炎的效果。方法：回顾性分析我院2013年10～12月收治的单疱病毒性角膜炎30例患者的临床资料,随机分为对照组和实验组。实验组给予双黄连滴眼液联合更昔洛韦眼用凝胶治疗,对照组给予更昔洛韦眼用凝胶治疗,比较两组患者的治疗效果。结果：双黄连滴眼液联合更昔洛韦眼用凝胶临床疗效评价15例,总有效率为93.3%,更昔洛韦眼用凝胶临床疗效评价15例,总有效率为86.7%,两组治疗后角膜情况、视力、患者主观感受均比治疗前有明显改善,但实验组改善优于对照组。结论：双黄连滴眼液与更昔洛韦眼用凝胶两组药物联合治疗单疱病毒性角膜炎比单纯采取更昔洛韦眼用凝胶滴眼治疗,效果更好,值得推广。     

两种剂型盐酸左氧氟沙星治疗急性细菌性结膜炎64例

目的:观察盐酸左氧氟沙星眼用凝胶与滴眼液对急性细菌性结膜炎的临床疗效.方法:对64例(128眼)患者采用单盲随机分组、平行对照方法,观察其疗效和不良反应.盐酸左氧氟沙星眼用凝胶32例(64眼)为甲组,盐酸左氧氟沙星滴眼液32例(64眼)为乙组.结果:甲组显效26例52眼,好转4例8眼,显效率81.3%,总有效率93.8%;乙组显效25例50眼,好转4例8眼,显效率78.1%,总有效率90.6%.结论:盐酸左氧氟沙星两种剂型用于急性细菌性结膜炎均安全有效,但凝胶剂不易外溢,给药次数仅是滴眼剂的1/3,故凝胶剂优于滴眼剂.     

阿昔洛韦眼用凝胶在兔离体角膜中的渗透释药行为研究

目的:研究阿昔洛韦眼用凝胶在兔离体角膜中的渗透释药行为。方法:以谷胱甘肽缓冲液作为释放介质,采用高效液相色谱法测定阿昔洛韦眼用凝胶及阿昔洛韦滴眼液在兔离体角膜中的累积渗透释药量,并绘制曲线。结果:阿昔洛韦眼用凝胶的渗透释药曲线符合一级释药方程;0·25h时阿昔洛韦滴眼液的累积渗透释药量高于阿昔洛韦眼用凝胶,0·25h以后则相反。结论:在给药后很短时间内(0·25h),阿昔洛韦滴眼液的房水药物浓度要高于阿昔洛韦眼用凝胶,但凝胶在眼部滞留时间较长,且角膜有一定的药物储库作用。     

依诺沙星眼用即用型凝胶的研制

眼用即用型凝胶(situ forming eye gel)是一种新型眼用制剂,它不同于传统的眼用凝胶,根据体内的不同生理环境发生相转化,体外以溶液形式存在,滴入眼内立即发生相转化,变为凝胶。国外已有产品上市。依诺沙星滴眼液是临床常用的滴眼液,滴眼液在使用过程中,由于眼睑的眨动和泪液的     

局部麻醉药利多卡因透皮吸收的研究

评价了局部麻醉药利多卡因的透皮吸收和制成压敏胶粘贴片皮肤局部给药麻醉的可能性。在考察利多卡因游离碱(分子型)和盐酸盐(离子型)从水和硅酮中透过无毛鼠皮肤的基础上,试制了利多卡因游离碱的橡胶型压敏胶粘贴片,对药物的体外释放和皮肤透过进行了考察,并与日本的利多卡因凝胶剂(xylocainejelly)的皮肤透过进行了比较,考察了10%～60%的利多卡因压敏胶粘贴片中药物浓度与皮肤透过之间的关系。     

滴眼剂的这些注意事项 您可得记住了

正王女士就诊于眼科,医师开了一种滴眼液和一种眼用凝胶,她想了解一下这两种药如何正确使用?滴眼剂在眼科临床上用于诊断、预防、治疗眼部疾病,正确使用有助于眼部疾患的早日康复。但其中有些注意事项患者往往容易忽略,本文就来详细的说一说。一、滴眼液的正确使用方法:(1)用药前先洗手,用药时不要让眼药水瓶口直接接触眼睑和睫毛;(2)混悬型滴眼剂在使用前应摇匀,如醋酸可的松眼药水,静止时有     

2种抗胆碱药在虹膜睫状体炎中的应用比较

目的:比较硫酸阿托品眼用凝胶、盐酸环喷托酯滴眼液在虹膜睫状体炎中的应用效果。方法:回顾性分析我院2004-2010年收治的单纯虹膜睫状体炎病例,其中以1%硫酸阿托品眼用凝胶为主要睫状体麻痹剂的16例,以1%盐酸环喷托酯滴眼液为主的12例。观察所有病例瞳孔阻滞解除时间、房闪变化、角膜后沉着物变化及其并发症发生情况。结果:在单纯虹膜睫状体炎的治疗中,盐酸环喷托酯滴眼液和硫酸阿托品眼用凝胶麻痹睫状肌的效果差异无统计学意义(P>0.05)。结论:盐酸环喷托酯滴眼液和硫酸阿托品眼用凝胶在虹膜睫状体炎治疗效果中无明显差异,但盐酸环喷托酯滴眼液麻痹效果解除时间较硫酸阿托品眼用凝胶短。     

阿奇霉素滴眼液对大鼠和兔眼铜绿假单胞菌角膜炎的治疗作用

目的评价阿奇霉素滴眼液对大鼠和兔眼铜绿假单胞菌性角膜炎的治疗作用。方法采用铜绿假单胞菌分别制备大鼠和兔角膜炎模型,眼部滴入质量分数为1.0%、1.5%、2.0%、2.5%的阿奇霉素滴眼液并与模型组对比,评价其药效学(包括治愈率、清除率、组织病理学的评价)。结果阿奇霉素滴眼液各剂量组对大鼠和兔眼铜绿假单胞菌性角膜炎均具有治疗作用,且呈剂量-效应关系;高剂量(质量分数2.5%)阿奇霉素滴眼液治疗效果优于阳性药(质量分数1.0%眼用凝胶)(P<0.05),中剂量(质量分数2.0%)阿奇霉素滴眼液治疗效果与阳性药相近。结论不同浓度的阿奇霉素滴眼液在大鼠和兔眼角膜炎的治疗试验中均有效,质量分数2.0%和2.5%的阿奇霉素滴眼液疗效更佳。     

盐酸利多卡因眼用凝胶在兔眼房水中药物浓度测定及药动学研究

目的：建立兔眼房水中利多卡因的LC-MS/MS检测方法,研究盐酸利多卡因眼用凝胶在兔眼房水中的药动学特征。方法：72只雄性新西兰兔分成Ⅰ和Ⅱ两组,每组36只,Ⅰ和Ⅱ组分别给予盐酸利多卡因眼用凝胶受试制剂和参比制剂,左右眼均滴入15μL,于不同时间点取房水样品,经沉淀蛋白后,采用LC-MS/MS法测定房水中的利多卡因。以来曲唑为内标,采用Hanbon Hedera ODS-2 C18（2.1 mm×150 mm,5μm）色谱柱,流动相为甲醇-20 mmol·L-1醋酸铵水溶液（含0.1%甲酸）（55∶45,v/v）,质谱采用气动辅助电喷雾离子化和正离子多重反应监测。结果：利多卡因房水浓度在2.070~10350 ng·mL-1范围内线性关系良好（r=0.9995）。单次给予新西兰兔受试制剂和参比制剂后,房水中利多卡因的Cmax分别为（10193±4535）ng·mL-1和（11046±2734）ng·mL-1,AUC0-8分别为7582 ng·h·mL-1和8125 ng·h·mL-1,t1/2分别为2.6 h和1.9 h,Tmax均为0.3 h。结论：盐酸利多卡因眼用凝胶受试和参比制剂在房水中药动学特征一致,眼部给药后利多卡因可快速穿透角膜到达房水,并在房水中达到较高的浓度。     

Polyoxyethylated nonionic surfactants and their applications in topical ocular drug delivery

Topical dosing of ophthalmic drugs to the eye is a widely accepted route of administration because of convenience, ease of use, and non-invasiveness. However, it has been well recognized that topical ocular delivery endures a low bioavailability due to the anatomical and physiological constraints of the eye which limit drug absorption from the pre-corneal surface. Nonionic surfactants as versatile functional agents in topical ocular drug delivery systems are uniquely suited to meet the challenges through their potential ability to increase bioavailability by increasing drug solubility, prolonging pre-corneal retention, and enhancing permeability. This review attempts to place in perspective the importance of polyoxyethylated nonionic surfactants in the design and development of topical ocular drug delivery systems by assessing their compatibility with common ophthalmic inactive ingredients, their impact on product stability, and their roles in facilitating ocular drugs to reach the target sites.     

利多卡因凝胶经皮吸收的动力学和药效学

目的研究利多卡因凝胶的经皮吸收动力学以及药效学。方法用经皮微渗析的方法测定大鼠真皮内药物浓度的变化,计算相关参数;用电刺激法考察药效,并与市售EMLA(eutectic mixture of local anesthetics)霜剂进行药效比较。结果持续用药1 h,利多卡因经皮吸收动力学曲线在1.25 h达到峰值;起效时间与EMLA霜剂相近,局麻作用维持时间和局麻强度优于EMLA。结论利多卡因凝胶具有良好的局麻作用;局部用药后,利多卡因产生局部麻醉作用的真皮中最低有效浓度为12 mg·L^-1。     

Topical anesthetics

Topical anesthetics have become valuable tools in the field of dermatology, especially in pediatric patients, who have particular need for such anesthesia. The ideal topical anesthetic should provide effective, painless cutaneous analgesia with quick onset, sufficient duration and minimal adverse effects. This article reviews the basic science concepts relevant to the safe and judicious use of topical anesthetic agents in children, examines the specific characteristics and practical uses of these agents, and discusses the various unique delivery systems currently available.     

Pharmacokinetics and Tissue Distribution of Pilocarpine After Application to Eyelid Skin of Rats

Extending the delivery of drugs into the eyes while reducing systemic bioavailability is of utmost importance in the management of chronic ocular diseases. Topical application onto the lower eyelid skin, as an alternative to eye drops, is seen to be a valuable strategy in the treatment of chronic eye diseases. To elucidate the critical value of delivering drugs in solution onto the eyeball through the eyelid skin, pharmacokinetic studies of pilocarpine were conducted, and the results were verified using a direct pharmacodynamic study in rats. The mean residence time of pilocarpine after topical eyelid application to the eyelid skin, conjunctiva, eyeball, and plasma were 14.9, 8.50, 6.29, and 8.11 h, respectively. Conjunctiva and eyeball concentrations of pilocarpine at 8 h were 80-fold and 8-fold higher after topical eyelid application, respectively, than those for eye drops. Pupillary constriction was sustained over 8 h after topical eyelid application. Topical eyelid skin application exhibited a localized drug absorption and specific drug accumulation in the ocular tissues. Hence, it is rational to prepare topical formulations directed onto the eyelid skin, which is suitable for drugs required for long-term treatment.     

Trends in ophthalmic antimicrobial utilization pattern in Bahrain between 1993 and 2000: a resurgence of chloramphenicol?

OBJECTIVES: The occurrence of aplastic anemia following topical administration of ophthalmic chloramphenicol is controversial and debated internationally. We have determined the influence of such debate on the utilization of ophthalmic chloramphenicol in Bahrain, through studying the utilization patterns of ophthalmic antimicrobial preparations by the Ministry of Health, with an emphasis on chloramphenicol, between 1993 and 2000. Cost-implications of these patterns are examined. MATERIAL AND METHODS: Information on the annual purchase of ophthalmic antimicrobial drug preparations and their unit price was obtained from the Directorate of Materials Management, Ministry of Health, and analyzed. RESULTS: In 1993, the 3 most commonly purchased ophthalmic antibacterial preparations were oxytetracycline 1% eye ointment (40.1%); sulfacetamide 10% and 20% eye drops (25.3%); and chloramphenicol 0.5% eye drops and 1% eye ointment (10.8%). In 2000, oxytetracycline remained the most frequently purchased preparation (33%), followed by chloramphenicol (21.2%). Between 1993 and 1999, chloramphenicol purchases fluctuated between 10% to 16.4% with a remarkable increase to 21.2%, in 2000. Chloramphenicol accounted for 8.6% and 15.1% of cost of total ophthalmic preparations purchased in 1993 and 2000, respectively. CONCLUSION: Despite continued concerns of potential risks of ophthalmic chloramphenicol, this preparation is extensively utilized in Bahrain. We are of the opinion that for minor infections, chloramphenicol ophthalmic preparations should be replaced by safer alternatives. Further, we recommend that their use be reserved for ocular infections that are resistant to other antimicrobials, and that ophthalmologists, at the secondary care level, should supervise such treatment.     

Safety and efficacy of various concentrations of topical lidocaine gel for intravitreal injection

Introduction: Intravitreal injection (IVT) is one of the most common vitreoretinal procedures, a large majority are performed with local anesthesia. The purpose of this study was to investigate the safety to the cornea and anesthetic efficacy of five concentrations of lidocaine gel.

Methods: A prospective clinical trial was conducted testing lidocaine gel in five preparations: 2, 3.5, 5, 8 and 12%. Patients with macular degeneration, diabetic edema or retina vein occlusion were scheduled for intravitreal treatment received topical anesthesia with lidocaine gel 5 and 10 min before the procedure. Patients answered the visual analog scale for pain during the procedure. Corneal and conjunctival was evaluated using the Oxford scale.

Results: In total, 260 patients were randomized into five groups. The mean pain scores (± standard deviation) were 2.63 (± 1.68) in the 2% group, 2.08 (± 1.35) in the 3.5%; 2.00 (± 1.65) in the 5%, 1.93 (± 1.40) in the 8% and 1.83 (± 1.35) in the 12% group. Mean pain score among all groups was similar (p = 0.077). There was no significant difference between groups in regard to keratitis mean score (p = 0.897).

Conclusions: Lidocaine gel at concentrations from 2 to 12% induced similar anesthetic effect for IVTs, without adverse effects on cornea and conjunctiva.     

Controlled and continuous release ocular drug delivery systems: pros and cons

Topical ocular drug administration is the most preferred route for treating conditions affecting the surface of the eye as well as anterior segment diseases; this is mainly due to the rapid and localised drug action and patient acceptability. However, the ocular bioavailability is typically less than 5% from conventional ophthalmic dosage forms such as eye drops. This is mainly due to the unique anatomical and physiological features of the eye. One of the effective pharmaceutical approaches is to provide a controlled and continuous drug release to the surface of the eye to compensate drug loss by nasolacrimal drainage and non-productive absorption of the topically applied drug. This review provides a critical appraisal (advantages and drawbacks) of the different drug delivery strategies that provides controlled and continuous drug supply to the surface of the eye; it covers research conducted over the past three decades.