Rebamipide Ophthalmic Suspension Research Articles

Enhancing Corneal Drug Penetration Using Penetratin for Ophthalmic Suspensions.

Eye drops, including solutions and suspensions, are essential dosage forms to treat ophthalmic diseases, with poorly water-soluble drugs typically formulated as ophthalmic suspensions. In addition to low bioavailability, suspensions exhibit limited efficacy, safety, and usability due to the presence of drug particles. Improving bioavailability can reduce the drug concentrations and the risk of problems associated with suspended drug particles. However, practical penetration enhancers capable of improving bioavailability remain elusive. Herein, we focused on penetratin (PNT), a cell-penetrating peptide (CPP) that promotes active cellular transport related to macromolecule uptake, such as micropinocytosis. According to the in vitro corneal uptake study using a reconstructed human corneal epithelial tissue model, LabCyte CORNEA-MODEL24, PNT enhanced the uptake of Fluoresbrite® YG carboxylate polystyrene microspheres without covalent binding. In an ex vivo porcine eye model, the addition of 10 µM PNT to rebamipide ophthalmic suspension markedly improved the corneal uptake of rebamipide; however, the addition of 100 µM PNT was ineffective due to potentially increased particle size by aggregation. This article provides basic information on the application of PNT as a penetration enhancer in ophthalmic suspensions, including the in vitro and ex vivo studies mentioned above, as well as the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay and storage stability at different pH values.

The Efficacy and Safety of Rebamipide Ophthalmic Suspension (OPC-12759) in Patients with Dry Eye Disease: A Systematic Review of Randomized Controlled Trials.

The aim of this paper is to evaluate the efficacy and safety of Rebamipide (REB) ophthalmic suspension in dry eye disease (DED). A systematic review that only included full-length randomized controlled studies (RCTs) reporting the effects of REB ophthalmic suspension in three databases, PubMed, Scopus and Web of Science, was performed according to the PRISMA statement. The Cochrane risk of bias tool was used to analyze the quality of the studies selected. A total of seven studies were included in this systematic review. Although the overall risk of bias was low, most studies were sponsored by the manufacturer. REB ophthalmic suspension treatment achieved higher improvement than the control group in all reported variables. The mean differences between both groups were in favor of the REB group and were as follows: dry eye-related quality of life score (DEQS) -3.5 ± 2.9 points, tear film break-up time (TBUT) of 0.7 ± 0.6 s, Schirmer test (ST) without anesthesia of 0.3 ± 0.6 mm and total corneal fluorescein staining (tCFS) of -1.2 ± 0.7 points. Adverse events (AEs) were 5.2 ± 7.6% superior in the REB group, with an overall compliance > 95%. Therefore, REB ophthalmic suspension is a safe and effective treatment that could be recommended in patients with DED.

The Effect of Rebamipide on Refractive Accuracy of Cataract Surgery in Patients with Dry Eye.

Introduction Refractive accuracy is crucial for increasing patient satisfaction after cataract surgery. Tear film instability caused by dry eye can lead to inaccurate measurement of corneal power, which is one of the most important factors for postoperative refractive calculation. This study investigated the effect of 2% rebamipide ophthalmic suspension on the predicted refractive accuracy for cataract surgery in patients with dry eye.MethodsThis single-center, prospective, open-label study included 35 dry eyes (with tear breakup time < 5 s) who underwent cataract surgery. The patients were treated with rebamipide for 4 weeks before the preoperative examination. In addition to the usual evaluation of biometric variables essential for cataract surgery, tear breakup time (TBUT), superficial punctate keratopathy in the central part of the cornea (C-SPK), corneal higher-order aberrations (HOAs), and predicted postoperative spherical equivalent (P-SE) were evaluated at baseline and 4 weeks after dry eye treatment. The patients’ subjective spherical equivalent (S-SE) was evaluated 1 month postoperatively. The difference between S-SE and P-SE was used to assess the accuracy of the P-SE. Improvement in TBUT, C-SPK, HOA, and the accuracy of P-SE after dry eye treatment were analyzed.ResultsThe accuracy of the biometry readings for the achieved P-SE was within 0.25 D in 42.9% and 54.3%; within 0.5 D in 71.4% and 88.6%; and within 0.75 D in 88.6% and 97.1% of eyes before and after rebamipide treatment, respectively (p < 0.01). TBUT, C-SPK, and HOAs significantly improved after rebamipide treatment (p < 0.01).ConclusionRebamipide significantly improved the corneal surface condition and accuracy of the predicted postoperative refraction in dry eyes.Supplementary InformationThe online version contains supplementary material available at 10.1007/s40123-022-00457-3.

Effects of Rebamipide on Differences in Power and Axis of Corneal Astigmatism Between Two Intra-patient Keratometric Measurements in Dry Eyes.

IntroductionThis study investigated the effect of rebamipide on discrepancies in the power and axis of astigmatism between two intra-patient keratometric measurements in patients with dry eyes.MethodsFifty-eight dry eyes (with a short tear breakup time [TBUT] of less than 5 s) were analyzed. Patients with dry eye were treated with 2% rebamipide ophthalmic suspension (group R) or Mytear® artificial tear ophthalmic solution (group M) for 4 weeks. TBUT and corneal higher-order aberrations (HOAs) were evaluated at baseline and 4 weeks after treatment. Astigmatism power and axis were measured twice during both evaluations, at 5-min intervals. Baseline and post-treatment measurements were compared. Changes in TBUT and HOAs, and intra-patient discrepancies in astigmatism power and axis measurements were evaluated.ResultsHOAs showed significant positive correlations with intra-patient differences in astigmatism power and axis (P < 0.001). At the 4-week post-treatment follow-up, TBUT increased, and HOAs and astigmatism power and axis discrepancies decreased in a significant number of patients in group R (P < 0.001). In group M, only differences in astigmatism power decreased in a significant number of cases (P = 0.005). The degree of change in the intra-patient difference in astigmatism power between the two post-treatment keratometric measurements was significantly greater in group R than in group M (P < 0.001). In group R, baseline HOAs exhibited a significant positive correlation with changes in HOAs and intra-patient differences in astigmatism power (both P < 0.001). In group M, baseline HOAs were only significantly correlated with changes in intra-patient differences in astigmatism power (P = 0.030).ConclusionIn dry eyes with short TBUTs, rebamipide significantly improved the corneal surface condition and significantly reduced intra-patient discrepancies in astigmatism power and axis measurements. Rebamipide may improve the accuracy of intraocular lens (IOL) power calculations in dry eyes, particularly when toric IOLs are implanted.Supplementary InformationThe online version contains supplementary material available at 10.1007/s40123-021-00368-9.

Histochemical Analysis of Lacrimal Concretions in a Patient Using Rebamipide Ophthalmic Suspension: Case Report

Concretions of the lacrimal drainage system can cause dacryocystitis. In the present study, our patient developed dacryocystisis with lacrimal concretions of a white soft mass. Rebamipide ophthalmic suspension had been applied for treatment of dry eye. To evaluate the pathogenic mechanism of the case, histological and chemical studies were performed. Our case was woman in her seventies. She had a medical history of rheumatoid arthritis. She was referred to our hospital for dacryocystitis after showing a poor response to treatment with antibiotic agents. A head computed tomography (CT) scan showed ductal high-density deposits along the lacrimal sacs. During dacryocystotomy, the hypertrophy of the lacrimal sacs was found replete with pus and cottage cheese-like white substances. The extracts were surgically removed, and histological and chemical analysis was performed. The histological examination showed granulation tissues and acellular amorphous material with crystal-like structures. Positive staining by Alcian blue and Kossa was found in crystal-like legions. The extract obtained from the concretions showed the same fluorescence band and UV absorption spectrum in thin layer chromatography (TLC) and spectrometry, respectively, as rebamipide. Our findings suggest that the obstruction by lacrimal concretions containing rebamipide resulted in dacryocystitis in this case. In addition, it is speculated that in patients who have impaired tear secretion, refractory dacryocystitis may be evoked following the accumulation of rebamipide in the lacrimal sacs.

Novel Sustained-Release Drug Delivery System for Dry Eye Therapy by Rebamipide Nanoparticles.

The commercially available rebamipide ophthalmic suspension (CA-REB) was approved for clinical use in patients with dry eye; however, the residence time on the ocular surface for the traditional formulations is short, since the drug is removed from the ocular surface through the nasolacrimal duct. In this study, we designed a novel sustained-release drug delivery system (DDS) for dry eye therapy by rebamipide nanoparticles. The rebamipide solid nanoparticle-based ophthalmic formulation (REB-NPs) was prepared by a bead mill using additives (2-hydroxypropyl-β-cyclodextrin and methylcellulose) and a gel base (carbopol). The rebamipide particles formed are ellipsoid, with a particle size in the range of 40–200 nm. The rebamipide in the REB-NPs applied to eyelids was delivered into the lacrimal fluid through the meibomian glands, and sustained drug release was observed in comparison with CA-REB. Moreover, the REB-NPs increased the mucin levels in the lacrimal fluid and healed tear film breakup levels in an N-acetylcysteine-treated rabbit model. The information about this novel DDS route and creation of a nano-formulation can be used to design further studies aimed at therapy for dry eye.

Role of 2% rebamipide ophthalmic suspension in the management of dry eye disease

Role of 2% rebamipide ophthalmic suspension in the management of dry eye disease - IJCEO- Print ISSN No: - 2395-1443 Online ISSN No:- 2395-1451 Article DOI No:- 10.18231/j.ijceo.2019.110, Indian Journal of Clinical and Experimental Ophthalmology-Indian J Clin Exp Ophthalmol

Retrospective Observational Study on Rebamipide Ophthalmic Suspension on Quality of Life of Dry Eye Disease Patients.

Purpose The Dry Eye-Related Quality-of-Life Score (DEQS) is a Japanese dry eye-specific questionnaire that has been used to assess the symptoms of dry eye and their effects on the quality of life (QOL) in Japanese individuals. The purpose of this study was to determine the effect of rebamipide (RBM) on the QOL of Japanese patients with dry eye disease (DED). Method The medical records of 43 patients (3 men and 40 women; mean age: 64 ± 14 years; range: 32 to 83 years), who were diagnosed with DED and treated with RBM at the Ehime University Hospital between November 2012 and June 2016, were reviewed. The effects of 2% rebamipide (RBM) ophthalmic suspension on the symptoms of DED was determined by the answers to the DEQS questionnaire and clinical findings. The clinical findings before and 1, 3, 6, 12, and 24 months after initiating the RBM treatment were reviewed. The following data were collected from the DEQS: the Summary score and two subscale scores, the Bothersome ocular symptoms score, and the Impact on daily life score. In addition, the standard fluorescein staining score, the Schirmer I test score, and the tear breakup time (TBUT) score were analyzed. Result The Summary score and Impact of daily life score of the DEQS were improved significantly after 1, 3, 6, and 12 months of RBM, and the Bothersome ocular symptoms scores of the DEQS were also improved after 1, 3, and 6 months. The fluorescein staining scores were significantly decreased after 1, 3, 6, and 12 months, and the TBUT score was significantly increased after 1 month. Conclusion RBM treatment improves the QOL by alleviating the corneal and conjunctival epithelial damages. The DEQS is a useful questionnaire that can assess the severity of the DED symptoms and their impact on the QOL. This trial is registered with UMIN000024405.

Polyvinyl alcohol-iodine induced corneal epithelial injury in vivo and its protection by topical rebamipide treatment.

Periocular povidone-iodine (PI) and polyvinyl alcohol-iodine (PAI) have had a major role in the prevention of endophthalmitis. The purpose of this study was to investigate the corneal epithelial toxicity of PAI in a rabbit eye model using corneal resistance (CR) measurement, which is a good indicator of cell barrier function. Rabbit eyes were administered PAI solution at 4-, 6-, 8-, or 16-fold dilution with physiological saline solution (saline) or saline alone (control), to the conjunctival sac with/without wash-out with saline. Corneal epithelial injury assessed by fluorescein staining and the CR ratio was measured at 10 minutes (min) to 96 hours (h) after the initial administration. Histological observation was performed in the eyes following the PAI or control administrations. At 120 min after administration of PAI solution, the CR ratio was decreased and superficial punctate keratopathy (SPK) was significantly increased in each of the PAI-administered groups compared to the control. Recovery of CR and SPK after administration of 6- or 8-fold dilution of PAI was significantly delayed in eyes that were not subsequently washed with saline compared with eyes that were. Pre- or post-instillation of 2% rebamipide ophthalmic suspension significantly reduced PAI induced-SPK and -decrease of CR ratio. The CR method was able to accurately and quantitatively evaluate fine corneal epithelial injury. It is suggested that eyes should be washed with saline solution after administration of PAI solution or the instillation of rebamipide to prevent or reduce corneal epithelial injury.

Tear Film-Oriented Diagnosis and Tear Film-Oriented Therapy for Dry Eye Based on Tear Film Dynamics.

In December 2010 and January 2012, 3% diquafosol sodium ophthalmic solution and 2% rebamipide ophthalmic suspension, respectively, appeared first in Japan as prescription drugs for the treatment of dry eye (DE). Since then, not only the diagnosis and treatment but also the understanding of the pathophysiology of DE have greatly advanced, and a new concept of layer-by-layer diagnosis and treatment for DE, respectively termed "tear-film-oriented diagnosis" (TFOD) and "tear-film-oriented therapy" (TFOT) was born. This new concept is currently in the process of expanding from Japan to other Asian countries. TFOD is the method used for the differential diagnosis of DE, which includes aqueous-deficiency DE (ADDE), decreased wettability DE (DWDE), and increased evaporation DE (IEDE), through the dynamics of tear film (TF) and breakup patterns (BUPs) after the eye is opened. BUPs and/or each diagnosed DE subtype are/is able to distinguish the insufficient components of the ocular surface that are responsible for each BUP in a layer-by-layer fashion. Aqueous fluid, membrane-associated mucins (especially MUC16), and the lipid layer and/or secretory mucins must be insufficient in ADDE, DWDE, and IEDE, respectively, and this allows for a layer-by-layer treatment to be proposed for each BUP via the supplementation of the insufficient components, using the topical therapy currently available. In Japan, TF breakup is regarded as a visible core mechanism for DE, and an abnormal breakup time (i.e., ≤5 seconds) and symptoms are currently used for the diagnosis of DE. Therefore, TFOD and TFOT could be an ideal and practical pathway for clinicians to manage DE.

Patients Preference of Diquafosol or Rebamipide Eye Drops for the Treatment of Mild Dry Eye: A Pilot Study

Purpose: To investigate the preference rates of recently developed eye drops, 3% diquafosol ophthalmic solution and 2% rebamipide ophthalmic suspension, as a randomized clinical trial in patients with dry eye.Methods: Eighteen patients (mean age: 59.7 years old, females: 77.8%) with reduced tear film break-up time (TBUT ? 5 sec) were enrolled in this study. They were treated with either diquafosol or rebamipide for 1 week, and treated for an additional week after switching to the other eye drop. This treatment was repeated one more time. Then, the patients were treated with one of either eye drop for an additional 4 weeks. Patients’ preferences for eye drops were investigated using a questionnaire at the end of 4-week treatment. To confirm the effectiveness of the treatments, objective and subjective assessments including superficial punctate keratopathy (SPK) score, TBUT measurement, and Dry Eye-Related Quality-of-Life Score (DEQS) were performed at baseline, and 4 and 8 weeks.Results: SPK score was improved after treatment (P &lt; 0.05). Patients tended to prefer diquafosol (64.7%) torebamipide (35.4%), however there was no significant difference in two eye drops (P = 0.23). Bitterness was reported significantly more frequently after rebamipide administration (66.7%) than diquafosol administration (5.6%, P &lt; 0.001). The diquafosol bottle was considered “ease to use” by a larger percentage of users (94.1%) as compared to the rebamipide bottle (58.8%, P &lt; 0.05). The effectiveness of the signs and symptoms were similar for both groups at 8 weeks.Conclusions: Diquafosol and Rebamipide were both effective in treating dry eye and 65% of the patients choose Diquafosol. Bitterness after administration and ease to use of the bottles seemed to affect the patients’ preferences for these two eye drops.

Lacrimal Canaliculus Imaging Using Optical Coherence Tomography Dacryography

Lacrimal canaliculus (LC) has a key role in tear drainage, but it is difficult to evaluate the LC in detail, using the existing examinations. In this study, our novel LC imaging technique provided the high-resolution images of LC in a non-invasive manner. Three-dimensional images of LC were acquired via the palpebral conjunctiva from 20 healthy volunteers (20 eyes) and 10 patients with various lacrimal disorders (10 eyes), using optical coherence tomography (OCT) dacryography (OCTD). The LC images showed morphological differences between the vertical and horizontal segments. The function of LC could be evaluated by measuring the intralumen signal intensity over time after instillation of a contrast agent (2% rebamipide ophthalmic suspension). OCTD clearly visualised the blind extremity of the LC in four patients with punctal obstruction, which was useful for deciding the punctal incision location. In one patient with canalicular obstruction, contrast agent successfully highlighted the LC that had become narrow toward the site of obstruction. Significant differences were not found in the function and morphology of LC between the patients with NLDO and the healthy subjects. OCTD may be a useful tool for LC imaging, because it facilitates quantitative and simultaneous evaluation of LC morphology and function.

The effect of rebamipide ophthalmic suspension on ocular surface mucins in soft contact lens wearers.

To evaluate the changes in ocular surface mucins with 2%rebamipide ophthalmic suspension treatment in soft contact lens (SCL) wearers. Rebamipide suspension is a mucin secretagogue approved for the treatment of dry eye syndrome in Japan. In this study, the fluorescence intensity of wheat germ agglutinin conjugate of fluorescein (F-WGA) was used as a marker of membrane-associated mucins, and sialic acid concentration in tear fluids as a marker of secreted mucins. Thirty-two eyes of 16 SCL wearers with discomfort were treated with rebamipide suspension at a dose of one drop in each eye four times daily for two weeks. The parameters of clinical efficacy were tear break-up time, fluorescein staining scores for the cornea and conjunctiva, and Schirmer test values. Fluorescence intensities in the central cornea were measured by fluorophotometry after the application of 5% F-WGA solution. Tears collected by Schirmer test strips were analyzed by high-performance liquid chromatography, and the concentrations of sialic acid, total protein, and the four major tear proteins, namely secretory IgA, lactoferrin, lipocalin-1, and lysozyme were measured. Significant increases in F-WGA fluorescence intensities (p < 0.005) were seen in the corneal surfaces. Sialic acid concentrations increased over time; however, the differences were not statistically significant. Except for a slight increase in kerato-conjunctival staining scores (p < 0.05) and secretory IgA (p < 0.05), no other significant differences were seen among clinical parameters or tear proteins. Topical application of rebamipide suspension significantly increased F-WGA intensity, a marker of membrane-associated mucins in SCL wearers.

Preparation of an Ultrafine Rebamipide Ophthalmic Suspension with High Transparency.

A 2% commercially available, milky-white, rebamipide micro-particle suspension is used to treat dry eyes, and it causes short-term blurring of the patient's vision. In the current study, to improve the transparency of a rebamipide suspension, we attempted to obtain a clear rebamipide suspension by transforming the rebamipide particles to an ultrafine state. In the initial few efforts, various rebamipide suspensions were prepared using a neutralizing crystallization method with additives, but the suspensions retained their opaque quality. However, as a consequence of several critical improvements in the neutralizing crystallization methods such as selection of additives for crystallization, process parameters during crystallization, the dispersion method, and dialysis, we obtained an ultrafine rebamipide suspension (2%) that was highly transparent (transmittance at 640 nm: 59%). The particle size and transparency demonstrated the fewest level of changes at 25°C after 3 years, compared to initial levels. During that period, no obvious particle sedimentation was observed. The administration of this ultrafine rebamipide suspension (2%) increased the conjunctival mucin, which was comparable to the commercially available micro-particle suspension (2%). The corneal and conjunctival concentration of rebamipide following ocular administration of the ultrafine suspension was slightly higher than that of the micro-particle suspension. The ultrafine rebamipide suspension (eye-drop formulation) with a highly transparent ophthalmic clearness should improve a patient's QOL by preventing even a shortened period of blurred vision.

Effect of rebamipide ophthalmic suspension on the success of lacrimal stent intubation

To evaluate the effect of the postoperative administration of rebamipide ophthalmic suspension on the success rate of lacrimal stent intubation (LSI) for the treatment of primary acquired nasolacrimal duct obstruction (PANDO). This comparative interventional cohort study investigated 110 consecutive patients with PANDO who were treated with LSI and followed up for 12 months postoperatively at one institution. LSI was performed by one surgeon, and all patients received identical postoperative care. Among the total 110 patients, 71 underwent LSI with postoperative administration of rebamipide ophthalmic suspension, and 39 underwent LSI without administration of the suspension. Data related to patient age, gender, laterality, and postoperative administration of rebamipide ophthalmic suspension were collected and used as independent variables, and logistic regression analyses were performed to compare the anatomical success rate at 12 months postoperatively between patients with and without postoperative administration of the suspension. The anatomical success rate of LSI in patients with and without postoperative administration of rebamipide ophthalmic suspension was 90.1 and 69.2%, respectively. A comparison of these success rates showed statistical significance, in that the rate of treatment success was higher in PANDO patients who underwent LSI with postoperative administration of the suspension [odds ratio (OR), 3.37; P < 0.05]. The findings of this study show that postoperative administration of rebamipide ophthalmic suspension increases the rate of anatomical success in patients who undergo LSI for the treatment of PANDO.

Effect of Rebamipide Ophthalmic Suspension on Intraocular Light Scattering for Dry Eye After Corneal Refractive Surgery.

To assess the changes in intraocular scattering before and after instillation of rebamipide ophthalmic suspension in patients with dry eye after corneal refractive surgery. This study enrolled 60 eyes of 30 dry eye patients undergoing corneal refractive surgery. Patients were randomly assigned to start topical administration of rebamipide ophthalmic suspension (rebamipide group) or artificial tears (control group) 4 times daily for 4 weeks. Tear secretion, tear break-up time (TBUT), and the fluorescein score were measured before and after treatment. Intraocular light scattering was also measured as the objective scattering index (OSI) at 0.5-second intervals over 10 seconds. In the rebamipide group, the Schirmer I test, TBUT, and fluorescein score improved significantly, from 11.4 ± 9.0 mm, 2.2 ± 0.7 seconds, and 4.3 ± 1.3 to 14.9 ± 7.4 mm, 4.5 ± 1.7 seconds, and 1.9 ± 1.0, respectively (P = 0.006, P < 0.001, P < 0.001, Wilcoxon signed rank test). We found significant improvements in OSI at 5.0 to 10.0 seconds after blinking (5-8 seconds, P = 0.01; 9 seconds, P = 0.02; 10 seconds, P < 0.001). The mean OSI, the OSI change rate, and the OSI slope of the linear regression line improved significantly, from 2.73 ± 1.52, 74.7 ± 69.5%, and 0.10 ± 0.12 to 2.19 ± 1.19, 28.6 ± 48.7%, and 0.04 ± 0.08, respectively (P = 0.02, 0.003, and 0.03). Rebamipide ophthalmic suspension was effective for improving both ocular surface parameters and optical quality in patients with dry eye undergoing corneal refractive surgery, suggesting that it may hold promise for the treatment of such patients.

Effectiveness and relevant factors of 2% rebamipide ophthalmic suspension treatment in dry eye.

BackgroundRebamipide with mucin secretagogue activity was recently approved for the treatment of dry eye. The efficacy and safety in the treatment of rebamipide were shown in two pivotal clinical trials. It was the aim of this study to evaluate the effect of 2 % rebamipide ophthalmic suspension in patients with dry eye and analyze relevant factors for favorable effects of rebamipide in clinical practice.MethodsThis was a retrospective cohort study of 48 eyes from 24 patients with dry eye treated with 2 % rebamipide ophthalmic suspension. Dry eye-related symptom score, tear film break-up time (TBUT), fluorescein ocular surface staining score (FOS) and the Schirmer test were used to collect the data from patients at baseline, and at 2, 4, 8, and 12 week visits. To determine the relevant factors, multiple regression analyses were then performed.ResultsMean dry eye-related symptom score showed a significant improvement from the baseline (14.5 points) at 2, 4, 8 and 12 weeks (9.80, 7.04, 7.04 and 7.83 points, corrected P value <0.001, respectively). Median FOS showed a significant improvement from the baseline (3.0 points) at 2, 4, 8 and 12 weeks (2.0, 2.0, 1.0 and 1.0 points, corrected P value <0.001, respectively). TBUT and Schirmer test values were not significantly improved after the treatment. For ocular symptoms, three parameters (foreign body sensation, dry eye sensation and ocular discomfort) showed significant improvements at all visits. The multiple regression analyses showed that the fluorescein conjunctiva staining score was significantly correlated with the changes of dry eye-related symptom score at 12 weeks (P value = 0.017) and dry eye-related symptom score was significantly correlated with independent variables for the changes of FOS at 12 weeks (P value = 0.0097).ConclusionsTwo percent rebamipide ophthalmic suspension was an effective therapy for dry eye patients. Moreover the fluorescein conjunctiva staining score and dry eye-related symptom score might be good relevant factors for favorable effects of rebamipide.Electronic supplementary materialThe online version of this article (doi:10.1186/s12886-015-0040-0) contains supplementary material, which is available to authorized users.

The role of Rebamipide ophthalmic suspension in management of dry eye disease

Purpose of review: Review of the drug Rebamipide, an ophthalmic suspension, in the treatment of dry eye and other ocular surface disorders. Method: An extensive literature search was done on articles published in various ophthalmic journals to review the work on the latest drug rebamipide and its role in treating dry eye and other ocular surface disorders. Recent Findings: Rebamipide is a novel drug for the treatment of dry eye disorders. It is a mucin-secretogogue, has a cytoprotective, anti-inflammatory effect and also suppresses the detrimental oxygen free radicals and helps in faster healing of epithelium. No major side effect has been noticed apart from dysguesia. Summary: Rebamipide is the latest drug introduced in the treatment of dry eye. It seems to be a safe and effective treatment in chronic and severe forms of dry eye particularly due to mucus deficiency. Key Words: Dry eye, Goblet cell, Microvilli, Rebamipide, Tear film

Evaluation of dacryocystorhinostomy using optical coherence tomography and rebamipide ophthalmic suspension.

PurposeTo evaluate the surgical outcome of dacryocystorhinostomy (DCR) by measuring the tear meniscus, using optical coherence tomography and rebamipide ophthalmic suspension.MethodsPatients with nasolacrimal obstruction and chronic dacryocystitis who were scheduled for an endonasal DCR underwent tear meniscus examinations before and 2 months after surgery. Vertical scans of the inferior menisci were performed before and at 1, 3, 5, 7, and 10 minutes after the instillation of rebamipide ophthalmic suspension. The tear menisci areas were measured with imaging software. Ten young adults without epiphora formed the control group.ResultsAnatomical success was achieved on 22 sides of 21 patients. The patients’ postoperative tear menisci were significantly smaller than the preoperative menisci at all points during the test, and the response to volume loading in the postoperative patients was corrected to nearly that of the young, healthy adults. Nevertheless, the postoperative meniscus area tended to be larger than that of the young adults at all points.ConclusionThe reduced tear meniscus area after DCR reflected the success of the surgical procedure. However, incomplete recovery of the meniscus after the test might suggest a residual disorder of the lacrimal drainage system after DCR.

Effect of rebamipide ophthalmic suspension on signs and symptoms of keratoconjunctivitis sicca in Sjögren syndrome patients with or without punctal occlusions.

The aim of this study was to investigate the efficacy of 2% rebamipide suspension in treatment of keratoconjunctivitis sicca (KCS) in patients with Sjögren syndrome (SS) with or without punctal occlusions. Thirty patients with SS, diagnosed based on the presence of autoantibodies and/or focus score >1 on lip biopsies, with corneal fluorescein staining scores (FSS) >3, and conjunctival lissamine green-staining scores (LSS) >3, were treated 4 times daily for 4 weeks with 2% rebamipide ocular suspension. Ocular examinations were performed before treatment and 2 and 4 weeks after treatment to evaluate FSS (0-9), LSS (0-6), and tear film break-up time (BUT). Hyaluronate and/or artificial tears were not discontinued. The patients were interviewed regarding the 5 major KCS symptoms, foreign body sensation, dry eye sensation, photophobia, ocular pain, and blurred vision, with each graded from none (0) to very severe (4). Of the 30 patients, 3 failed to attend all sessions, leaving 27 (25 females, 2 males, mean age 62.5 ± 10.8 years) to be studied. FSS and LSS showed improvement at week 2, but BUT showed improvement later, at week 4. All 5 symptoms improved significantly. When the patients were divided into 3 groups according to the presence of punctal occlusions, FSS and LSS were found to improve in all groups, but BUT improved only in patients with both puncta occluded at week 4. Rebamipide ophthalmic suspension was effective in treating KCS of patients with SS, probably by increasing mucins and suppressing inflammatory cytokines. Punctal occlusions resulted in sufficient retention of tear fluid to enhance the activities of rebamipide and improve BUT.