3.5%利多卡因眼用凝胶的研究进展

局部麻醉药在眼科的各类操作和手术中应用广泛,目前临床上使用的主要是表面麻醉药滴眼液。3.5%利多卡因眼用凝胶是眼科表面麻醉用新品,与表面麻醉药滴眼液相比,具有麻醉效果更好、有效麻醉作用时间更长、术中重复给药次数减少、角膜上皮毒性降低并能保护眼表等特性。本文介绍3.5%利多卡因眼用凝胶及其药代动力学、临床疗效和安全性方面的研究进展。     

更昔洛韦眼用凝胶联合干扰素治疗单纯疱疹病毒性角膜炎疗效观察

目的：探讨更昔洛韦眼用凝胶联合干扰素治疗单纯疱疹病毒性角膜炎的临床效果。方法：选取单纯疱疹病毒性角膜炎患者59例（78眼）,将其随机分为观察组和对照组,观察组29例（40眼）,采用干扰素球结膜下注射,联用更昔洛韦眼用凝胶治疗;对照组30例（38眼）,单独采用更昔洛韦眼用凝胶治疗,并对两组治疗效果进行对照分析。结果：观察组疗效明显优于对照组,差异有统计学意义（P〈0.05）。结论：应用更昔洛韦眼用凝胶联合干扰素治疗单纯疱疹病毒性角膜炎具有治愈率高、副作用少的优点,值得临床推广应用。     

阿昔洛韦滴眼液和更昔洛韦凝胶治疗单疱病毒性角膜炎的临床效果比较

目的：观察并分析阿昔洛韦滴眼液与更昔洛韦凝胶治疗单疱病毒性角膜炎的效果。方法选择80例单疱病毒性角膜炎患者,随机分为治疗组和对照组,各40例。对照组给予阿昔洛韦滴眼液治疗,治疗组采用更昔洛韦凝胶治疗,比较两组的疗效。结果治疗组总有效率为95.0%,对照组总有效率为87.5%,差异有统计学意义（P<0.05）。治疗组的治疗时间为（13.60±3.51）d,对照组的治疗时间为（18.27±4.47）d,差异有统计学意义（P<0.05）。结论更昔洛韦凝胶治疗单疱病毒性角膜炎的效果优于阿昔洛韦滴眼液。     

Treatment of venous leg ulcers with 5% amikacin gel: phase IV trial.

A phase IV trial with 5% amikacin gel was carried out on 100 adult in patients of both sexes suffering from venous infected leg ulcers. After 2 weeks' therapy the microbiological culture tests were negative for more than 80% of the patients. The mean ulcer surface area was reduced by 34% and the accompanying symptoms of erythema, inflammation and pain were improved. Only very mild unwanted local effects were reported by four out of the 100 patients. Five percent amikacin gel was judged a safe and effective topical treatment for curing infected venous leg ulcers.     

Moxifloxacin 0.5% ophthalmic solution: in bacterial conjunctivitis

The fourth-generation 8-methoxyfluoroquinolone moxifloxacin is available as an 0.5% ophthalmic solution for use in the treatment of bacterial conjunctivitis. Moxifloxacin had good activity against various Gram-positive and -negative ocular isolates in vitro, and moxifloxacin 0.5% ophthalmic solution achieved good penetration into ocular tissues in healthy volunteers and patients undergoing ocular surgery. The efficacy of moxifloxacin 0.5% ophthalmic solution in the treatment of bacterial conjunctivitis has been shown in three randomized, double-blind, multicentre trials. In a trial in patients aged ≥1 year, the clinical success rate was significantly higher with moxifloxacin 0.5% ophthalmic solution than with placebo. In a trial in patients aged ≥12 years, moxifloxacin 0.5% ophthalmic solution was noninferior to levofloxacin 0.5% ophthalmic solution in terms of the clinical success rate. In a third trial, the clinical cure rate was significantly higher with moxifloxacin 0.5% ophthalmic solution than with trimethoprim 1.0%/polymixin B 10,000?IU/mL ophthalmic solution in paediatric patients aged ≤18 years. Moxifloxacin 0.5% ophthalmic solution was well tolerated in patients with bacterial conjunctivitis. Ocular adverse events (e.g. eye pain, eye irritation) were the most commonly reported treatment-related adverse events, with the majority being of mild severity.     

左布匹卡因与罗比卡因用于手术后患者硬膜外自控镇痛的观察

目的：观察左布匹卡因与罗比卡因用于腹部手术后自控硬膜外镇痛（PCEA）的效果及不良反应。方法：60例ASAⅠ～Ⅱ级腹部手术患者，随机分为0．15％左布匹卡因加2mg／L芬太尼组（A组）30例与0．2％罗比卡因加2mg／L芬太尼组（B组）30例，以5mL／h行术后硬膜外泵注镇痛。记录术后4、8、24、48h的疼痛视觉模拟评分（VAS0～10分）、满意度评分、运动阻滞测试（改良Bromage评分）及术后活动能力4级评分；48h内按压PCA次数（PCAd）、PCA有效次数（PCAe）、D／D比值（PCAd／PCAe）及不良反应。结果：2组镇痛效果满意，2组各观察指标差别均无统计学意义（P〉0．05）。在术后第1天。A组有14例（46．7％）可以短时间行走，而B组有25例（83．3％）。第2天，A组有15例（50．0％）可以自由行走，而B组有26例（86．7％），2组差别有统计学意义（P〈0．05）。不良反应：恶心发生率A组13．3％（4／30），B组10．0％（3／30）。皮肤瘙痒发生率2组均为6．7％（2／30），差异无统计学意义（P〉0．05）。结论：0．15％左布匹卡因与0．2％罗比卡因用于患者术后硬膜外镇痛均可获得满意的效果，而0．2％罗比卡因较0．15％左布匹卡因术后活动能力恢复早。     

Evaluation of 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5-ethyluracil in a rabbit model of herpetic keratitis.

The nucleoside analog 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5- ethyluracil (FEAU) was tested in a rabbit model of acute herpetic keratitis and its effectiveness compared with that of acyclovir (ACV). FEAU or ACV was applied topically 3 times daily, beginning 3 days post-HSV-1 inoculation and continued for a period of 7 days. FEAU at a concentration of 1% (w/v) or 3% ACV resulted in significant lessening of the severity of corneal lesions, conjunctivitis, iritis, and corneal clouding at 24 to 48 h after beginning chemotherapy. No toxic reaction was observed in any rabbit eyes treated with either FEAU or ACV. The duration of virus shedding into tear film and colonization of the trigeminal ganglia, however, were not reduced by either FEAU or ACV treatment begun 3 days post-inoculation. Fifty percent effective dose (ED50) of FEAU determinations performed on isolates from tear film and on the virus inoculum in secondary rabbit kidney cultures yielded a range of 4.6-7 microM, with two in vitro resistant isolates having ED50S of greater than or equal to 1500 microM of FEAU. Fifty percent cell growth inhibition for FEAU was 3000 microM at 72 h.     

更昔洛韦眼用凝胶与阿昔洛韦滴眼液治疗126例单疱性病毒性角膜炎的临床疗效比较

目的比较单疱性病毒性角膜炎中应用更昔洛韦眼用凝胶与阿昔洛韦滴眼液的疗效,以探索最佳治疗措施。方法选择我科收治的126例单疱性病毒性角膜炎患者,分为两组,即观察组予以更昔洛韦眼用凝胶治疗,对照组阿昔洛韦滴眼液治疗,每组各63例。治疗后观察不同程度患者的治疗时间,评定疗效及安全性,随访1年观察复发情况。结果本研究中的所有患者均完成治疗,与观察组有效率95.24%比较,对照组有效率降低明显,差异具统计学意义(P0.05)。与对照组比较,观察组不同病情患者的治疗时间,浅层型、深层型以及混合型的治疗时间均缩短明显,不良反应发生率以及复发率均降低明显,差异可见统计学意义(P0.05)。结论在单疱性病毒性角膜炎患者中应用更昔洛韦可缩短不同程度患者的治疗时间,疗效较好,且安全性较高,复发率低。     

Topical brimonidine 0.2%/timolol 0.5% ophthalmic solution: in glaucoma and ocular hypertension

A fixed combination of brimonidine (a highly selective alpha(2)-adrenergic agonist) and timolol (a non-selective beta-blocker) [brimonidine 0.2%/timolol 0.5% ophthalmic solution; brimonidine/timolol] is available for the topical treatment of glaucoma and ocular hypertension (OH). Brimonidine and timolol decrease elevated intraocular pressure (IOP) by complementary mechanisms of action and have an additive effect when coadministered to healthy volunteers and patients with glaucoma or OH. When assessed over a 3- or 12-month period in large, well designed clinical studies, brimonidine/timolol instilled twice daily (one drop in each eye) was superior to monotherapy with the individual components instilled two (brimonidine) or three (timolol) times daily, and noninferior to concomitant therapy with the individual components instilled twice daily, in lowering raised IOP in patients with glaucoma or OH. In small, randomised, comparative studies of 1 or 3 months' duration, the IOP-lowering effect of brimonidine/timolol twice daily was similar or superior to that of fixed combination dorzolamide 2%/timolol 0.5% ophthalmic solution (dorzolamide/timolol) twice daily (preliminary data). Brimonidine/timolol is generally well tolerated with a predictable local and systemic adverse event profile based on that of the individual components used alone and concomitantly. No unexpected or serious adverse events associated with the fixed combination were reported in key clinical trials. Brimonidine/timolol may be advantageous over dorzolamide/timolol with respect to ocular tolerability and comfort (preliminary data).     

Evaluation of clinical efficacy and safety of tobramycin/dexamethasone ophthalmic suspension 0.3%/0.05% compared to azithromycin ophthalmic solution 1% in the treatment of moderate to severe acute blepharitis/blepharoconjunctivitis

Abstract

Objective:

To evaluate the clinical efficacy and safety of tobramycin/dexamethasone (TobraDex ST^*; ‘ST’) ophthalmic suspension 0.3%/0.05% compared to azithromycin (Azasite^?) ophthalmic solution (1%) in the treatment of moderate to severe blepharitis/blepharoconjunctivitis.     

Azithromycin 1.5% ophthalmic solution: in purulent bacterial or trachomatous conjunctivitis

The second-generation macrolide azithromycin is available as a 1.5% ophthalmic solution for use in the treatment of bacterial or trachomatous conjunctivitis. This article reviews the pharmacological properties of azithromycin 1.5% ophthalmic solution and its clinical efficacy and tolerability in patients with purulent bacterial conjunctivitis or trachomatous conjunctivitis caused by Chlamydia trachomatis. Azithromycin 1.5% ophthalmic solution had good in vitro activity against Haemophilus influenzae and C. trachomatis, and achieved good concentrations in tear samples from healthy volunteers. Azithromycin 1.5% ophthalmic solution for 3 days (1 drop twice daily) was noninferior to tobramycin 0.3% ophthalmic solution for 7 days (1 drop every 2 hours) in paediatric and adult patients with purulent bacterial conjunctivitis, with regard to clinical cure and bacteriological resolution on day 9, in a randomized, investigator-masked, multicentre study. In children with trachomatous inflammation, 3-day treatment with azithromycin 1.5% ophthalmic solution was noninferior to a single dose of azithromycin oral suspension, with regard to clinical cure rate in the worst eye at 60 days, in a randomized, double-masked, multicentre study. Azithromycin 1.5% ophthalmic solution was well tolerated in patients with bacterial or trachomatous conjunctivitis. Most events were of mild to moderate severity.     

Safety and efficacy of micronized tretinoin gel (0.05%) in treating adolescent acne

Tretinoin is widely used in the treatment of acne. Despite significant advances in formulation development, irritation and dryness can be particularly bothersome, especially during the first 3-4 weeks, impacting adherence. Dose titration and adjunct use of moisturizers have been commonly employed. Co-prescribing with benzoyl peroxide (BPO) or a BPO/antibiotic combination is also common practice. The tretinoin molecule is unstable and can be degraded by BPO, further complicating treatment regimens. Lately, formulation technology has focused on providing more efficient penetration of the tretinoin into the skin layers so that lower concentrations of tretinoin might afford better tolerability, but maintain good efficacy; incorporating moisturizing excipients to minimize irritation; and providing greater stability to the tretinoin molecule. This approach would be particularly relevant in a pediatric acne population where efficacy/tolerability balance is important and treatment regimens must take into account lifestyles, but little data exist on the use of tretinoin in this patient population. A micronized formulation of tretinoin (0.05%) gel has been developed that provides a more efficient delivery of tretinoin, because of its optimal particle size, no degradation by BPO and better cutaneous tolerability than tretinoin microsphere (0.1%) gel without compromising efficacy in a pediatric population.     

Sustained ophthalmic in situ gel of ketorolac tromethamine: rheology and in vivo studies

Most ocular diseases are treated with topical eye drops. The poor bioavailability and therapeutic response exhibited by these conventional eye drops due to rapid precorneal elimination of the drug may be overcome by the use of in situ gelling systems that are instilled as drops into the eye and undergo a sol‐to‐gel transition in the cul‐de‐sac. The present work describes the formulation and evaluation of an ophthalmic delivery system of the nonsteroidal anti‐inflammatory drug (NSAID), ketorolac tromethamine, based on the concept of pH‐triggered in situ gelation. Polyacrylic acid (Carbopol^® 934) was used as the gelling agent in combination with hydroxypropylmethylcellulose (Methocel E15LV), which acted as a viscosity enhancer. The prepared formulations were characterized for clarity, pH, drug content, rheology, and in vivo drug release. Clarity, pH, and drug content of the developed formulations were found to be satisfactory. The developed formulation showed pseudo‐plastic rheology. The formulation with benzalkonium chloride and edetate disodium improved the rate of corneal absorption but not the extent. The developed formulation is a viable alternative to conventional eye drops by virtue of its ability to enhance bioavailability through its longer precorneal residence time and ability to sustain drug release. Also importantly is the ease of instillation afforded and decreased frequency of instillation resulting in better patient acceptance. Drug Dev Res, 2009. © 2009 Wiley‐Liss, Inc.     

Brimonidine-purite 0.1% versus brimonidine-purite 0.15% twice daily in glaucoma or ocular hypertension: a 12-month randomized trial*

ABSTRACT

Objective: To compare the safety and intraocular pressure (IOP)-lowering effects of brimonidine-purite^? 0.1% with the marketed formulation of brimonidine-purite 0.15% (Alphagan P^§ 0.15%) when used twice daily (BID) by patients with glaucoma or ocular hypertension previously treated with brimonidine-purite 0.15% for at least 6 weeks.

Methods: In a 12-month, randomized, double-masked, multicenter, parallel group, non-inferiority study, patients with glaucoma or ocular hypertension who were treated with brimonidine-purite 0.15% BID were randomly assigned to continue brimonidine-purite 0.15% (n = 102) or to administer brimonidine-purite 0.1% (n = 105) BID for 12 months. IOP was measured at approximately 8 a.m. (hour 0) and 10 a.m. (hour 2).

Main outcome measures: Mean change from baseline IOP and adverse events.

Results: Demographics and baseline characteristics were similar between treatment groups. Treated-baseline mean IOPs at both timepoints were similar between groups (p ≥ 0.606). Brimonidine-purite 0.1% provided IOP-lowering that was non-inferior to brimonidine-purite 0.15% at each of the 12 follow-up timepoints, and there were no statistically significant between-group differences at any timepoint. The most commonly reported adverse event was conjunctival hyperemia (13.5% for brimonidine-purite 0.1%; 10.8% for brimonidine-purite 0.15%). No significant differences in the incidence of adverse events were noted between the two formulations.

Conclusions: Brimonidine-purite 0.1% BID is as effective as brimonidine-purite 0.15% BID in lowering IOP in patients with glaucoma or ocular hypertension who were previously treated with brimonidine-purite 0.15%, and both formulations are well tolerated. Limitations of the study include enrollment of only patients who were already on treatment with brimonidine-purite 0.15%. The 0.1% formulation of brimonidine-purite allows for decreased exposure to brimonidine while providing an IOP-lowering effect comparable to that of the 0.15% formulation. Clinical trial registered at clinicaltrials.gov; identifier: NCT00168363.