美国FDA批准Sirion Therapeutics公司的0.05%二氟泼尼酯眼用乳液上市，用于治疗术后炎症和疼痛。本品辅料：硼酸、蓖麻油、吐温80、醋酸钠、EDTA钠、氢氧化钠（调节PH值至5.2～5.8）和纯水。

眼科术后快速解决炎症和疼痛非常重要，本品可快速减轻炎症和疼痛。所有研究组患者的平均眼内压在整个研究中始终保持在正常范围内。

在2项Ⅲ期临床研究中，以安慰剂为对照品评价了本品对眼科术后24小时后一日2次和一日4次用药的安全性和疗效，研究纳入438例存在明显炎症、表现为术后当日前眼房细胞2级（>10个细胞）的患者。

2种给药方案（一日2次和一日4次）在减少术后2周前房细胞总的疗效相似（一日2次为86％，一日4次为87％）。然而，一日4次用药在1周时少数患者完全消除了炎症和疼痛。故医生推荐一日4次的给药方案。

TAMPA, Fla., October 6, 2008 /PRNewswire/ — Sirion Therapeutics, Inc., a privately held ophthalmic-focused biopharmaceutical company, announced today that Durezol™ (difluprednate ophthalmic emulsion) 0.05% is now commercially available. Durezol, which was approved by the U.S. Food and Drug Administration in June 2008, is a topical ophthalmic corticosteroid indicated for the treatment of inflammation and pain associated with ocular surgery.

"We are excited to provide eye care professionals with a new and powerful topical steroid," said Susan Benton, Senior Vice President of Sales and Marketing for Sirion Therapeutics, Inc. "Because Durezol is the first and only steroid with an approval for both inflammation and pain, it is the first innovation in the strong steroid class in over 35 years. We believe Durezol will give patients and physicians a more comprehensive option for postoperative care."

Sirion Therapeutics has built a fully-staffed commercial infrastructure comprised of a national specialty sales force that will promote Durezol, a Medical Science Liaison team that will communicate clinical information to the medical community, and a managed markets group that will secure access to Durezol through pharmacies and insurance plans.

Other marketing and product support initiatives in progress include an extensive sampling program, direct mail communications to physicians and pharmacists, the Durezol web site telemarketing, a reimbursement hotline, a patient-assistance program, and a customer support number (1-866-4SIRION).

Durezol Phase 3b Studies
Sirion also announced today the completion of two Phase 3b studies that evaluated Durezol for the management of postoperative inflammation in which treatment was initiated one day prior to surgery. The multicenter, randomized, double-masked, placebo-controlled, parallel-group trials were conducted in 245 patients undergoing unilateral ocular surgery. In the first study of 124 patients, Durezol or placebo was dosed 4 times daily (QID), while in the second study, 121 patients received Durezol or placebo twice daily (BID).

"The Phase 3b studies represent an approach to therapy that is most similar to the current standard of care, meaning most physicians treat inflammation prophylactically rather than waiting for it to occur," explained Steven Silverstein, M.D. of Silverstein Eye Centers. Dr. Silverstein was a principal investigator in the QID study and also serves as a clinical assistant professor of ophthalmology at the University of Missouri-Kansas City School of Medicine and the University of Health Sciences. "Overall, the results from these studies show that by any definition utilized, Durezol administered both BID and QID was more effective than placebo in treating postoperative ocular inflammation and relieving ocular pain/discomfort as early as Day 3/4."

A significantly greater percentage of patients receiving Durezol QID or BID achieved a clinical response (defined as less than or equal to 5 anterior chamber cells and no flare) by Day 14: 81.3% of the Durezol treated patients in the QID group had a clinical response versus 25.0% of the placebo QID group (P < 0.0001); 74.7% of the Durezol BID patients had a clinical response versus 42.5% of patients in the placebo BID group (P < 0.001). Both Durezol groups maintained superiority over the placebo groups through Day 28, demonstrating that efficacy was definitive and did not decrease or reverse over time.

Ocular pain/discomfort was measured using the Visual Analogue Scale (VAS) score of 0-100 with 0 equal to no pain and 100 equal to maximal pain. The percentage of patients who were free of ocular pain/discomfort, reflected by a VAS score of 0, was superior and statistically significant for the Durezol groups versus the placebo groups in both the QID and BID studies as early as Day 3/4 and throughout the study period.

Six percent of the Durezol QID patients and 3.7% of the Durezol BID patients experienced a criterion increase in intraocular pressure, defined as a pressure of ≥21 mmHg and a change from baseline ≥10 mmHg at the same visit, compared with 0% in both of the placebo groups.

"Durezol has shown efficacy across multiple endpoints, including pain reduction. I believe it provides a potent new treatment option with a favorable safety profile," commented Dr. Silverstein. "It is a welcome improvement to the armamentarium of ocular pharmaceuticals, particularly since ocular inflammation is common to the majority of conditions that ophthalmologists treat."

About Postoperative Inflammation
More than five million ophthalmic surgeries are performed each year in the United States. Postoperative inflammation and pain are common occurrences following these procedures and if left untreated, can interfere with a patient's visual rehabilitation or lead to further complications. Corticosteroids and non-steroidal anti-inflammatory drugs are commonly used by healthcare professionals following ophthalmic surgery.

About Durezol
Durezol (difluprednate ophthalmic emulsion) 0.05% is a topical ophthalmic corticosteroid for the treatment of inflammation and pain associated with ocular surgery. Difluprednate, the active ingredient in Durezol, is a difluorinated derivative of prednisolone and has potent anti-inflammatory activity. Prior to U.S. approval, the efficacy and safety of difluprednate in ocular inflammatory diseases had been demonstrated in an extensive preclinical and clinical program in Japan. In two U.S. Phase 3 trials evaluating Durezol in patients diagnosed with significant postoperative inflammation (more than 10 anterior chamber cells), Durezol effectively reduced inflammation and pain. Mean intraocular pressure for all study groups remained within the normal range throughout the study. Durezol is being studied in other ocular inflammatory diseases, including a U.S. Phase 3 study evaluating Durezol for the treatment of anterior uveitis.

Dosage and Administration
The recommended dosage and administration of Durezol is to instill one drop into the conjunctival sac of the affected eye(s) 4 times daily beginning 24 hours after surgery and then continue throughout the first 2 weeks of the postoperative period, followed by 2 times daily for a week with tapering based on the response.

Important Safety Information
Durezol, like other corticosteroids, is contraindicated in patients with viral diseases of the cornea and conjunctiva, and also in fungal infections or mycobacterial infections of the eye or ocular structures. Prolonged use of corticosteroids may increase the hazard of secondary ocular infections, exacerbate the severity of ocular viral infections, and increase the development of fungal infections of the cornea. It is important to monitor intraocular pressure when using ophthalmic steroids. The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation.

Adverse reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera.

Ocular adverse reactions occurring in 5-15% of subjects in clinical studies with Durezol included corneal edema, ciliary and conjunctival hyperemia, eye pain, photophobia, posterior capsule opacification, anterior chamber cells, anterior chamber flare, conjunctival edema, and blepharitis. Other ocular adverse reactions occurring in 1-5% of patients included reduced visual acuity, punctate keratitis, eye inflammation, and iritis. Ocular adverse events occurring in <1% of patients included application site discomfort or irritation, corneal pigmentation and striae, episcleritis, eye pruritis, eyelid irritation and crusting, foreign body sensation, increased lacrimation, macular edema, scleral hyperemia, and uveitis. Most of these events may have been the consequence of the surgical procedure.

About Sirion Therapeutics, Inc.
Sirion Therapeutics is a privately held biopharmaceutical company pursuing the discovery, development, and commercialization of products addressing unmet medical needs in the protection and preservation of eyesight. Sirion's diverse product portfolio includes products that address ocular diseases and conditions including uveitis, herpetic keratitis, dry eye, and geographic atrophy associated with dry AMD. For more information, please 。

 
Durezol (二氟泼尼酯(difluprednate)) 眼科乳液使用说明
批准日期：2008年6月23日；公司：Sirion Therapeutics, Inc.

一般描述：Durezol (二氟泼尼酯眼科乳液)0.05%是一种为眼科使用消毒，局部用抗炎皮质激素。化学名是6α,9difluoro-11β,17,21-trihydroxypregna-1,4-diene-3,20-dione 21-acetate 17butyrate (CAS号23674-86-4)。二氟泼尼酯结构式如下：

 
适应证：

Durezol是一种局部用皮质激素适用于伴眼手术治疗炎症和疼痛。

剂量和用法：
滴1滴至患眼的结膜囊，每天4次，从术后24小时开始和继续至术后头2周，接着每天2次共一周然后根据反应逐渐减量。

禁忌证：

Durezol，如同其它言可用皮质激素一样，在大多数角膜和结膜病毒疾病，包括上皮单纯疱疹性角膜炎(树枝状角膜炎)，牛痘,和水痘，和还有眼的结核分枝杆菌感染和眼结构的真菌疾病禁忌。

不良反应：

伴眼科皮质激素不良反应包括眼内压升高，它可伴有视神经损伤 which may be伴optic nerve damage, 视力和视野缺损，后囊下白内障形成，来自病原体包括单纯疱疹的继发性眼感染，和在角膜或巩膜变薄处的眼球穿孔。

警告和注意事项：

眼内压(IOP)增高-延长使用皮质激素可能导致有视神经损伤的青光眼，视力和视野缺陷。如此产品使用10天或更长，应监查IOP。
白内障- 皮质激素的使用可能导致后囊下白内障形成。
 
愈合延迟- 白内障手术后使用甾体激素可能延缓愈合和增加泡形成的发生率。在引起角膜或巩膜变薄疾病中，已知使用局部甾体曾发生穿孔。应由医生在检查借助裂隙灯放大下如裂隙灯生物显微镜和其中适当时，荧光素染色检查病人后开最初处方和重建医药次序超过28天。
细菌感染- 延长使用皮质激素可能抑制宿主反应和因此增加继发眼感染的危害。在急性化脓性条件，甾体可能掩盖感染或增强存在的感染。如2天后征象和症状没有改善，应重新评价患者。
病毒感染-在应用皮质激素类药物治疗有单纯疱疹史患者时需要极大谨慎。使用眼甾体可能延长病程和可能加重许多眼科病毒感染的严重性(包括单纯疱疹)。
真菌感染- 与局部长期使用皮质激素同时特别容易发生角膜的真菌感染。在曾使用甾体或正在使用甾体时，任何持久角膜溃疡时必须考虑真菌侵袭。