Keratin Formed Bioadhesive Ophthalmic Gel for the Bacterial Conjunctivitis Treatment.

Keratin has the potential to function as the gel matrix in an ophthalmic formulation for the encapsulation of the macrolide antibiotic azithromycin. The quality of this formulation was thoroughly evaluated through various analyses, such as in vitro release assessment, rheological examination, intraocular retention studies in rabbits, assessment of bacteriostatic efficacy, and safety evaluations. It is worth mentioning that the gel demonstrated shear thinning properties and exhibited characteristics of an elastic solid, thereby confirming its structural stability. The gel demonstrated a notable affinity for mucosal surfaces in comparison to traditional azithromycin aqueous solutions. In vitro release testing revealed that drug release transpired via diffusion mechanisms, following a first-order kinetic release pattern. Additionally, the formulated gel exhibited remarkable antibacterial efficacy against Staphylococcus aureus and Pseudomonas aeruginosa in bacteriostatic evaluations. Lastly, safety assessments confirmed that the gel eye drops induced minimal irritation and displayed no apparent cytotoxicity, indicating their good safety and biocompatibility for ocular application. Thus, these findings indicated that the prepared azithromycin gel eye drops complied with the requisite standards for ophthalmic preparations.

Reduced Posology of an Ophthalmic Hydrogel Containing Dexamethasone/Netilmicin to Prevent and Treat Ocular Inflammation After Cataract Surgery: Efficacy and Tolerability.

INTRODUCTION: To demonstrate efficacy and safety of an ophthalmic hydrogel formulation of netilmicin/dexamethasone, containing xanthan gum twice a day (b.i.d.) versus netilmicin/dexamethasone eye drops four times a day (q.i.d) to treat inflammation and prevention of infection after cataract surgery. METHODS: Patients undergoing phacoemulsification with intraocular lens implantation (IOL) were randomised in two groups: group 1, twice daily (b.i.d.) dexamethasone 0.1%/netilmicin 0.3% (Netildex) ophthalmic gel; group 2, four times daily (q.i.d.) dexamethasone 0.1%/netilmicin 0.3% (Netildex) eye drops. Both treatments were administered for 14 days after surgery. Patients were evaluated before surgery, on the day of surgery and at 1, 7, 15 and 60 postoperative days. The primary efficacy endpoint was evaluation of cellularity and flare in the anterior chamber through slit-lamp biomicroscopy 7 days after surgery. Secondary endpoints included: presence of signs/symptoms of postoperative ocular inflammation and incidence of infection. RESULTS: One hundred seventy-three patients were randomised and 168 were evaluable. Flare and cellularity were resolved at day 7 in 92.5% of patients and almost completely by day 15. In both intent to treat (ITT) and per-protocol (PP) populations, the efficacy analysis demonstrated that the gel formulation administered twice a day was non-inferior to the eye drops administered four times a day. For ITT analysis, the lower limit of the 97.5% confidence interval (- 0.0535) was greater than the non-inferiority limit of -0.10. For the PP analysis, the lower limit of the 97.5% confidence interval (- 0.0526) was greater than the non-inferiority limit of - 0.10. The patient's global tolerability and reported symptoms were similar between treatment groups. No microbial load and no safety events were observed. CONCLUSIONS: Efficacy of the gel reduced posology (twice a day) is not inferior to four times a day eye drops. Both treatments were well tolerated and efficacious. The new reduced posology hydrogel formulation may improve patient compliance and quality of life. TRIAL REGISTRATION: Eudract: 2016-0021138-63; ClinicalTrial.gov: NCT029738880.

Cyclosporine A (0.05%) Ophthalmic Gel in the Treatment of Dry Eye Disease: A Multicenter, Randomized, Double-Masked, Phase III, COSMO Trial.

Purpose: To confirm the efficacy and safety of a novel ophthalmic cyclosporine A gel (CyclAGel, 0.05% CsA) in treating patients with moderate-to-severe dry eye disease (DED). Patients and Methods: The COSMO trial was a randomized, multicenter, double-masked, vehicle-controlled, phase III trial. Patients with moderate-to-severe DED were enrolled in 37 hospitals in China between November 2020 and April 2021. Eligible patients were randomized 1:1 to receive CyclAGel 0.05% or vehicle eye drops once nightly (QD). The primary endpoint was the proportion of subjects with at least a 1-point improvement in ICSS at day 84. Treatment-emergent adverse events (TEAEs) were recorded. Results: The full analysis set (FAS) included 315 and 312 participants in the CyclAGel and vehicle groups, respectively. The primary efficacy endpoint was achieved. The proportion of subjects with at least a 1-point improvement in ICSS from baseline to day 84 was significantly higher in the CyclAGel group than in the vehicle group (73.7% [232/315] vs 53.2% [166/312], P<0.0001). Significant improvements relative to the vehicle were also observed in the ICSS and Oxford scale scoring of corneal and conjunctival fluorescein staining at day 14, 42, and 84. The Schirmer tear test results were significantly higher in the CyclAGel group than in the vehicle group on days 14 and 84 (all P<0.05). The CyclAGel 0.05% was well tolerated, and the TEAEs were mostly mild. The most frequent treatment-related TEAE was eye pain (6.9% vs 1.6% in the CyclAGel and vehicle groups, respectively). No serious treatment-related TEAEs were reported. Conclusion: Clinically and statistically significant improvements in ICSS, tear production, and symptoms were observed in participants administered CyclAGel 0.05% QD for moderate-to-severe DED. CyclAGel 0.05% QD is a new effective, safe, and well-tolerated therapeutic option that might bring additional benefits of convenience and compliance as a once-A-day treatment for DED.

Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research.

Eyesight is one of the most well-deserved blessings, amid all the five senses in the human body. It captures the raw signals from the outside world to create detailed visual images, granting the ability to witness and gain knowledge about the world. Eyes are exposed directly to the external environment; they are susceptible to the vicissitudes of diseases. The World Health Organization has predicted that the number of individuals affected by eye diseases will rise enormously in the next decades. However, the physical barriers of the eyes and the problems associated with conventional ocular formulations are significant challenges in ophthalmic drug development. This has generated the demand for a sustained ocular drug delivery system, which serves to deliver effective drug concentration at a reduced frequency for consistent therapeutic effect and better patient treatment adherence. Recent advancement in pharmaceutical dosage design has demonstrated that a stimuli-responsive in situ gel system exhibits the favorable characteristics for providing sustained ocular drug delivery and enhanced ocular bioavailability. Stimuli-responsive in situ gels undergo a phase transition (solution-gelation) in response to the ocular environmental temperature, pH, and ions. These stimuli transform the formulation into a gel at the cul de sac to overcome the shortcomings of conventional eye drops, such as rapid nasolacrimal drainage and short contact time with the ocular surface This review highlights the recent successful research outcomes of stimuli-responsive in situ gelling systems in treating in vivo models with glaucoma and various ocular infections. Additionally, it also presents the mechanism, recent development, and safety considerations of stimuli-sensitive in situ gel as the potential sustained ocular delivery system for treating common eye disorders.

Advancement on Sustained Antiviral Ocular Drug Delivery for Herpes Simplex Virus Keratitis: Recent Update on Potential Investigation.

The eyes are the window to the world and the key to communication, but they are vulnerable to multitudes of ailments. More serious than is thought, corneal infection by herpes simplex viruses (HSVs) is a prevalent yet silent cause of blindness in both the paediatric and adult population, especially if immunodeficient. Globally, there are 1.5 million new cases and forty thousand visual impairment cases reported yearly. The Herpetic Eye Disease Study recommends topical antiviral as the front-line therapy for HSV keratitis. Ironically, topical eye solutions undergo rapid nasolacrimal clearance, which necessitates oral drugs but there is a catch of systemic toxicity. The hurdle of antiviral penetration to reach an effective concentration is further complicated by drugs' poor permeability and complex layers of ocular barriers. In this current review, novel delivery approaches for ocular herpetic infection, including nanocarriers, prodrugs, and peptides are widely investigated, with special focus on advantages, challenges, and recent updates on in situ gelling systems of ocular HSV infections. In general congruence, the novel drug delivery systems play a vital role in prolonging the ocular drug residence time to achieve controlled release of therapeutic agents at the application site, thus allowing superior ocular bioavailability yet fewer systemic side effects. Moreover, in situ gel functions synergistically with nanocarriers, prodrugs, and peptides. The findings support that novel drug delivery systems have potential in ophthalmic drug delivery of antiviral agents, and improve patient convenience when prolonged and chronic topical ocular deliveries are intended.

In silico modeling of functionalized poly(methylvinyl ether/maleic acid) for controlled drug release in the ocular milieu.

Controlling structurally defined properties of drug-bound macromolecules such as surface adhesion and interaction with endogenous proteins in the surrounding environment using prior data from computer-assisted simulation can be of great use in designing controlled release macromolecular therapeutic systems. In this paper, we describe experimental correlation of real-time properties of a polymer with pendant drug molecules, with predicted values obtained from studying in silico molecular interactions of this polymer with ocular surface proteins (mucin) for formulating an ophthalmic in situ gel. Mucoretention of the drug (norfloxacin) within the eye sac is closely associated with binding interactions occurring on the ocular surface, and covalent association of the drug with the mucoadhesive polymer, poly(methylvinyl ether/maleic acid), can largely reduce dosing frequency eliciting prolonged antibacterial action much required in treating conjunctival infections. The physicochemical properties and 3D conformation of the drug-polymer conjugate were predicted by computational studies. Molecular docking of the drug-polymer conjugate with ocular surface mucin (MUC-1) suggested that amino acid residues Arg1095, Asn1091, and Gln1070 of mucin are involved in hydrogen bonding with carboxyl residues in the polymer structure. The orientation of the drug-polymer conjugate in solution profoundly depends on the properties of the drug. The studies further reveal that molecular interactions of MUC-1 with the drug in the drug-polymer conjugate influence the binding orientation of the drug-polymer to mucin. Computationally predicted solvation energies revealed a significant difference in energy values between drug molecule alone (- 113.04 kcal/mol) and the drug-polymer (- 492.44 kcal/mol) suggesting higher aqueous solvation of the drug-polymer conjugate compared with less-soluble drug, and that interactions between polymer chains and ocular aqueous environment dictate the drug-polymer conjugate's free energy. Our results demonstrate the fabrication of a macromolecular therapeutic gel using drug-polymer with controlled release properties and mucoadhesion guided by information predicted from computational software. Notably, in silico studies reveal that even small variations in molecular composition, in this case, an antibacterial drug that contributes less than half of the entire molecular weight can considerably change the drug's presentation to the ocular environment. Graphical abstract Table of contents graphic.

New Combined Eye Gel with Alpha-2-Beta Interferon.

The results of the development of combined eye gel with interferon alpha-2-beta are presented. Experimental samples of the gel based on different gelling agents were prepared and their biotechnological and technological characteristics (the absence of the cytotoxic effect, aggregation stability, osmotic activity, bioadhesion, and rheological parameters) were evaluated. The composition with hydroxyethyl cellulose, Natrosol 250HHX, in a concentration of 1.5% as a gelling agent showed the best results and the best one-year stability.

Effect of vitamin A palmitate ophthalmic gel adjunctive therapy on tear film stability and inflammatory cytokines in patients with dry eye / 国际眼科杂志(Guoji Yanke Zazhi)

· AIM:To investigate the effect of sodium hyaluronate eye drops combined with vitamin A palmitate ophthalmic gel on levels of tear film stability and inflammatory cytokines in patients with dry eye.· METHODS:A total of 100 patients with dry eye treated in our hospital from January 2015 to February 2017 were randomly divided into control group and observation group,50 cases in each group.Patients in the control group were treated with sodium hyaluronate eye drops.Patients in the observation group were given vitamin A palmitate ophthalmic gel on the basis of the control group,and then the clinical efficacy,tear film stability and the level of inflammatory cytokines were detected in the two groups.· RESULTS:After treatment,the levels of BUT and S I t in both groups increased significantly compared with that before treatment,and FL was significantly lower than that before treatment.The levels of BUT and S I t in the observation group after treatment were 11.24±0.22s and I1.4 ± 0.17mm/5min respectively,which was high than that of control groups(P＜0.05).FL level was 1.78±0.10 points,which was significantly lower than that of the control group after treatment (P＜0.05).After treatment,the levels of IL-1β and TNF-αsignificantly decreased in both groups.The levels of IL-1β and TNF-α in the observation group were 34.38± 5.58ng/L and 134.47 ± 12.14ng/L,significantly lower than those of the control group after treatment,the difference was statistically significant (P ＜ 0.05).The total effective rate of observation group after treatment was 91.7％,significantly higher than that of the control group after treatment,the difference was statistically significant (P＜ 0.05).· CONCLUSION:Sodium hyaluronate eye drops combined with vitamin A palmitate ophthalmic gel can relieve the symptoms of patients with dry eye effectively,increase the stability of tear film,and reduce the levels of inflammatory factors in tears,which is reliable in clinical application.

Clinical study on the treatment of lacrimal duct obstruction with lomefloxacin hydrochloride eye ophthalmic gel / 国际眼科杂志(Guoji Yanke Zazhi)

AIM:To study the clinical effect of silica gel drainage tube combined with lomefloxacin hydrochloride eye ophthalmic gel in the treatment of lacrimal duct obstruction.METHODS:Totally 86 cases (138 eyes) of lacrimal duct embolism treated in our hospital from February to December 2015 were divided into 43 cases (68 eyes) as control group and 43 cases (70 eyes) of the observation group according to whether they were treated with lomefloxacin hydrochloride eye ophthalmic gel.Patients in the control group were treated with silica gel drainage, while the observation group was treated with lomefloxacin hydrochloride eye ophthalmic gel on the basis of the control group.The total effective rate, serum hypersensitivity C-reactive protein (h-CRP) level, complications and recurrence rate were observed and compared between the two groups.RESULTS:The total effective rate in the patients with obstructive nasolacrimal duct, common lacrimal duct obstruction, and lacrimal duct obstruction in observation group were 95.2%, 100.0%, 96.7%, higher than those in control group (P0.05).The serum levels of h-CRP in patients in the observation group at 3d and 7d after operation respectively were 2.40±0.84g/mL, 1.94±0.84g/mL, lower than those of control group at the same time (P<0.05).The complication rate of the observation group was 1.4%, which was lower than that of the control group (P<0.05).Follow up for 6-18mo, the recurrence rate was 11.4% in the observation group, which was significantly lower than the control group (P<0.05).CONCLUSION:The combination of silica gel drainage tube and lomefloxacin hydrochloride eye ophthalmic gel in the treatment of obstruction of lacrimal duct has good clinical efficacy, low inflammatory reaction, low complication rate and low recurrence rate.

Effect comparison of keratoconjunctivitis sicca treated by different medicines after phacoemulsification in patients with diabetes / 国际眼科杂志(Guoji Yanke Zazhi)

AIM: To analyzed the effect of keratoconjunctivitis sicca treated by different medicines after phacoemulsification in patients with diabetes.METHODS: Totally 78 diabetic patients 78 eyes with keratoconjunctivitis sicca (KCS) after phacoemulsification from March 2015 to March 2016 were selected and divided into two groups using random number table.In Group A, 39 eyes were treated with pranoprofen eye drops + artificial tears + Qiming granules.In Group B, 39 eyes were treated with pranoprofen eye drops + artificial tears.the two groups were observed for clinical symptoms, tear film break up time(BUT), corneal fluorescein staining and adverse reaction and so on before and after treatment.RESULTS: Total effective rate of Group A was 97%, significantly higher than that of Group B (64%)(P<0.05).After treatment, symptoms and signs scores of the two groups were significantly lower, BUT were significantly prolonged.At 1, 2wk and 1mo after treatment, symptoms and signs scores of Group A were significantly lower the BUT was longer than those of Group B (P<0.05).Corneal fluorescein staining of Group A at 2wk was lower than that of Group B (P<0.05).CONCLUSION: The combined therapy, pranoprofen eye drops + artificial tears + Qiming granules, is able to quickly and effectively improve the clinical symptoms and signs, with no serious adverse reactions for keratoconjunctivitis sicca after phacoemulsification in patients with diabetes.

Research in rheological properties of four types of ophthalmic preparations / 药学学报

This study is prepared to provide the basis of rheological parameters for the additional quality standard of ophthalmic gels, the rheological properties of the ophthalmic gels and the other three types of ophthalmic preparations. The medicines were compared through the study of the rheological properties for four types of ophthalmic preparations. The cone-plate rheometer was used to determine the dynamic and steady rheological parameters of four types of ophthalmic preparations. The similarities and differences of the measured results were analyzed to summarize the rheological indexes and parameters which are applied to distinguish the ophthalmic gels and the other types of ophthalmic preparations. ① The elastic modulus should be greater than the viscous modulus for the ophthalmic gels in the range of the linear viscoelastic region. ② The ophthalmic gels should be shear thinning non-Newtonian fluid with a certain yield stress and thixotropy. ③ The dynamic viscosity of the ophthalmic gels should be greater than 0.5 Pa·S at the temperature of 25℃ with the 50 s-1 shear rate. The typical rheological indexes and parameters of the ophthalmic gels were proposed in this article. The determination methods are simple and feasible. The rheological indexes and parameters have an important significance in the prescription design, production technology and quality control of the ophthalmic gels.

Preparation of Levofloxacin and Triamcinolone Acetonide Double-loaded Ophthalmic Gel / 中国药房

OBJECTIVE:To prepare Levofloxacin and triamcinolone acetonide double-loaded ophthalmic gel. METHODS:Us-ing levofloxacin hydrochloride and triamcinolone acetonide as main components,carbopol-940P as base material,HPMC K4M as tackifier,Levofloxacin and triamcinolone acetonide double-loaded ophthalmic gel was prepared. Using dissolution time as index, the contents of carbopol-940P and HPMC K4M were determined by single factor test,and dissolution time,viscosity and the con-tents of 2 main components were also determined. RESULTS:The concentrations of carbopol-940P and HPMC K4M were 0.4%and 1.2%,separately. The dissolution time was more than 24 h and viscosity was 1 142.67 Pa·s. The content of levofloxacin hydro-chloride was 97.3% of labelled amount (RSD=0.84%,n=3),and that of triamcinolone acetonide was 92.97% of labelled amount(RSD=1.32%,n=3). CONCLUSIONS:Levofloxacin and triamcinolone acetonide double-loaded ophthalmic gel has been prepared successfully.

Combined eye gel containing sodium hyaluronate and xanthan gum for the treatment of the corneal epithelial defect after pterygium surgery.

AIM: The aim of this study is to compare the effectiveness of the ophthalmic gels containing hyaluronate, xanthan gum, and netilmycine with fusidic acid in terms of recovery periods of corneal epithelium in the patients who underwent pterygium surgery. METHODS: Patients who underwent pterygium surgery were separated into two groups. Forty patients in group 1 were given eye gel containing sodium hyaluronate, xanthan gum, and netilmycine, and 40 patients in group 2 were given one drop of eye gel containing fusidic acid. The patients in both groups were examined at the 12th, 24th, and 48th hours in the postoperative period by using slit-lamp technique. The subjective complaints of the patients such as pain and stinging, and the recovery periods of the corneal epithelial defect were evaluated comparatively by fluorescein staining. RESULTS: The mean ages were 26±8 years (range: 18-35) and 24±6 years (range: 18-33) in groups 1 and 2, respectively. The closure period of the corneal epithelial defect was observed as 24±8 hours (range: 16-42) and 36±12 hours (range: 18-48) in groups 1 and 2, respectively. The number of the patients suffering from subjective complaints such as pain and stinging in the first 12 hours was six and 29 in groups 1 and 2, respectively. The difference was significant both clinically and statistically (P=0.001). CONCLUSION: Combined eye gel containing hyaluronate, xanthan gum, and netilmycine accelerates the recovery of corneal epithelial defect and reduces the complaints of the patients, when compared to the fusidic acid gel. Combined eye gel should be considered as an option for the treatment of the corneal epithelial defect related with pterygium surgery.

Comparison of Drug Concentrations in Human Aqueous Humor after the Administration of 0.3% Gatifloxacin Ophthalmic Gel, 0.3% Gatifloxacin and 0.5% Levofloxacin Ophthalmic Solutions.

PURPOSE: To investigate the penetration of 0.3% gatifloxacin ophthalmic gel, 0.3% gatifloxacin ophthalmic solution and 0.5% levofloxacin ophthalmic solution into aqueous humor after topical application. MATERIALS AND METHODS: Age-related cataract patients (150 eyes in 150 cases) receiving phacoemulsification were randomly divided into three groups: a 0.3% gatifloxacin gel group (n=50), a 0.3% gatifloxacin solution group (n=50), and a 0.5% levofloxacin solution group (n=50). Each group was administered one drop of gel or solution every 15 minutes for four doses. Aqueous samples were collected at different time points after the last drop. High pressure liquid chromatography (HPLC) was applied to determine the concentrations. The one-way ANOVA analysis was performed. RESULTS: Our data indicated that the concentration of the gatifloxacin gel group was higher than that of the gatifloxacin solution group at all time points (P <0.05); moreover, the gatifloxacin gel group exhibited higher levels than the levofloxacin solution group at 120.0 min and 180.0 min (P<0.05). Furthermore, the gatifloxacin gel produced the highest concentration at 120.0 min, and the gatifloxacin and levofloxacin solutions reached their peak values at 60.0 min. CONCLUSIONS: 0.3% gatifloxacin ophthalmic gel application produced highest aqueous humor drug concentration, maintained the longest time, had the best penetration and bioavailability.

Protective Effects of Ketorolac Tromethamine Ophthalmic Gel against Staphylococcus aureus Corneal Ulcer in Rabbits / 中国药房

OBJECTIVE:To study protective effects of Ketorolac tromethamine ophthalmic gel against Staphylococcus aureus corneal ulcer in rabbits. METHODS:S. aureus corneal ulcer in rabbits model was induced by corneal substance layer inoculation, and then divided into model group,positive control group (Clarithromycin ophthalmic gel),gel high-dose,medium-dose and low-dose groups(Ketorolac tromethamine ophthalmic gel 120,80,40 mg/ml),with 20 rabbits in each group. They were given re-levant medicine,once a day for 2 weeks. The keratopathy of rabbits was observed;the clinical efficacy and keratopathy score were compared. The change of ratina was observed under micrescope. RESULTS:Compared with model group,the keratopathy score de-creased while total effective rate increased in positive control group and gel groups after medication, and the effects of gel high-dose and low-dose groups were significantly lower than that of positive control group,with statistical significance(P<0.05). The retina of rabbits had not affected by the experiment. CONCLUSIONS:Ketorolac tromethamine ophthalmic gel has protective effect against S. aureus corneal ulcer in rabbits.

Clinical observation on eyelid herpes zoster with external use ganciclovir ophthalmic gel / 国际眼科杂志(Guoji Yanke Zazhi)

AlM: To observe the treatment efficacy of eyelid herpeszoster with external use ganciclovir ophthalmic gel.METHODS:A total of 77 patients were randomly divided into treatment group and control group. ln the treatment group, ganciclovir ophthalmic gel was topical coated on the basis of antiviral drugs, while the control group was coated with conventional acyclovir ointment and antiviral treatment. RESULTS: The cure rate was 95% in the treatment group, and the control group was 83% after 10d treatment. The difference was significant. CONCLUSlON: The efficacy of ganciclovir ophthalmic gel treated eyelid herpes zoster is obvious.

Efficacy of protein-free calf blood extract ophthalmic gel for children dry eye / 国际眼科杂志(Guoji Yanke Zazhi)

AlM:To evaluate the clinic efficacy of protein-free calf blood extract ophthalmic gel on healing children dry eye.METHODS: One hundred patients ( 50 patients each group) with children dry eye were divided into two groups randomly: control group was dropped 1g/L sodium hyaluronate eye drop four times per day and experimental group was dropped protein-free calf blood extract ophthalmic gel four times per day. Both groups received the depathogeny treatment at the same time. Symptom scores, Schirmer l test values, tear break-up time ( BUT ) , cornea fluorescein staining scores were recorded on the prior treatment and 30d post-treatment, then they were analyzed. RESULTS:There were statistically significant difference (P CONCLUSlON: There is a clearly beneficial effect of protein-free calf blood extract ophthalmic gel on healing children dry eye.

Comparative Study of the Character of Release in vitro between New MU-AN Ophthalmic Gel and the Old / 中国药师

Objective:To search the release in vitro of new MU-AN ophthalmic gel consist of ganciclovir instead of aciclovir is whether better than the Old. Methods:Using the content of ganciclovir and acyclovir as the index, taking the second oar method ( in Ch. P 2010), drug release in vitro test was investigated. Results:The character of drug release of new MU-AN ophthalmic gel was e-qual to the old, the rate of drug release was similar, The amount of drug release was the same. Both drugs met the requirements of clin-ical medication. The character corneal permeability of new MU-AN ophthalmic gel was better than the old. Gel matrix had no influ-ences on drug release, drug would be bring treatment effect after the way that it was released quickly then was dissolved in tear. Con-clusion:The drug release characteristics consistent with ophthalmic preparation requirements. The character of drug release of new MU-AN ophthalmic gel consist of ganciclovir instead of aciclovir is equal to the old, the time administer drug and interval time is gener-ally scientific, reasonable and feasible, providing the basis for the pharmacodynamics , toxicology and clinical study in the next step.

Effectiveness and safety of 0.15% ganciclovir in situ ophthalmic gel for herpes simplex keratitis - a multicenter, randomized, investigator-masked, parallel group study in Chinese patients.

OBJECTIVES: Parallel comparison with 0.15% ganciclovir (GCV) ophthalmic gel to evaluate the effectiveness and safety of 0.15% GCV in situ ophthalmic gel for the treatment of herpes simplex keratitis (HSK). METHODS: This was a multicenter, randomized, investigator-masked, parallel group study. HSK patients were randomly divided into two groups, with the corresponding treatment of 0.15% GCV ophthalmic gel or 0.15% GCV in situ ophthalmic gel. Symptoms and signs were observed before administration, and 3 (±1), 7 (±1), 14 (±2), and 21 (±3) days after the administration. The clinical effective rate was considered as the primary outcome. The safety profile was evaluated by AEs, visual acuity, and ocular tolerance. RESULTS: The clinical effective rate in the per-protocol (PP) dataset for the treatment group and the control group were 95.10% and 93.00%, respectively (P = 0.5282). The noninferiority test showed significant differences (P = 0.000305, P < 0.025), indicating that the tested drug was noninferior to the control. Patients in the PP dataset of both groups experienced decreases in the total scores of clinical indicators. Ocular AEs were few but similar between the two groups. There were no significant differences between patients' visions between the two groups before and after administration in the safety analysis set. In terms of drug tolerance, the rates of patients without transient blurred vision during all the visits in the treatment group were higher than those for the control group (P < 0.05). During the third and fourth visits, the rates of patients with eye itching were 4.08% and 1.22% in the treatment group, and 13.59% and 8.14% in the control group, respectively (P < 0.05). During the second visit, the rates of patients with eye irritation were 14.42% in the treatment group and 25.71% in the control group (P < 0.05). CONCLUSION: The 0.15% GCV in situ ophthalmic gel was effective and safe for the treatment of HSK, and was not inferior to 0.15% GCV ophthalmic gel. The 0.15% GCV in situ ophthalmic gel presented superior ocular tolerance.

Preparation and Quality Control of Pazufloxacin Mesilate Ophthalmic Gel / 中国药房

OBJECTIVE:To prepare pazufloxacin mesilate ophthalmic gel and to establish its quality control method.METHODS:The gel was prepared with pazufloxacin mesilate ophthalmic as principal agent and with PVA-124 as base material.The content of pazufloxacin mesilate was determined by HPLC and the stability of the gel was investigated as well.RESULTS:The prepared gel was yellowish liquid and its property fitted the description of Chinese Pharmacopeia(2005 edition).The linear range of pazufloxacin mesilate was 20.0～80.0 ?g?mL-1(r=0.999 9),and the average recovery was 98.67%(RSD=0.79%,n=3).No stratification was noted for the sample within 2-month storage under room temperature.CONCLUSION:The preparation technique of the pazufloxacin mesilate ophthalmic gel is simple and feasible,its quality control method is rapid and the determination result is accurate and reliable.