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Loteprednol etabonate

CAS# 82034-46-6

Loteprednol etabonate

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Chemical structure

Loteprednol etabonate

3D structure

Chemical Properties of Loteprednol etabonate

Cas No. 82034-46-6 SDF Download SDF
PubChem ID 444025 Appearance Powder
Formula C24H31ClO7 M.Wt 466.95
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 45 mg/mL (96.37 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name chloromethyl (8S,9S,10R,11S,13S,14S,17R)-17-ethoxycarbonyloxy-11-hydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene-17-carboxylate
SMILES CCOC(=O)OC1(CCC2C1(CC(C3C2CCC4=CC(=O)C=CC34C)O)C)C(=O)OCCl
Standard InChIKey DMKSVUSAATWOCU-HROMYWEYSA-N
Standard InChI InChI=1S/C24H31ClO7/c1-4-30-21(29)32-24(20(28)31-13-25)10-8-17-16-6-5-14-11-15(26)7-9-22(14,2)19(16)18(27)12-23(17,24)3/h7,9,11,16-19,27H,4-6,8,10,12-13H2,1-3H3/t16-,17-,18-,19+,22-,23-,24-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Loteprednol etabonate Dilution Calculator

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Loteprednol etabonate Molarity Calculator

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Preparing Stock Solutions of Loteprednol etabonate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1416 mL 10.7078 mL 21.4156 mL 42.8311 mL 53.5389 mL
5 mM 0.4283 mL 2.1416 mL 4.2831 mL 8.5662 mL 10.7078 mL
10 mM 0.2142 mL 1.0708 mL 2.1416 mL 4.2831 mL 5.3539 mL
50 mM 0.0428 mL 0.2142 mL 0.4283 mL 0.8566 mL 1.0708 mL
100 mM 0.0214 mL 0.1071 mL 0.2142 mL 0.4283 mL 0.5354 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Loteprednol etabonate

Loteprednol Etabonate is an anti-inflammatory corticosteroid used in optometry and ophthalmology.

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References on Loteprednol etabonate

Comparison of the Safety and Efficacy of Loteprednol Etabonate 0.5%/Tobramycin 0.3% with Dexamethasone 0.1%/Tobramycin 0.3% Following Strabismus Surgery.[Pubmed:28149143]

Eurasian J Med. 2016 Oct;48(3):186-188.

OBJECTIVE: To compare the anti-inflammatory efficacy and safety of 0.5% Loteprednol etabonate/0.3% tobramycin (LE/T) and 0.1% dexamethasone/0.3% tobramycin (DM/T) ophthalmic suspensions following strabismus surgery. MATERIALS AND METHODS: The records of 40 patients who were treated with either LE/T or DM/T following strabismus surgery were retrospectively reviewed. The recorded signs and symptoms of inflammation and intraocular pressure of the patients at 1 day, 1 week, and 3 weeks after the surgery were evaluated and compared between the groups. RESULTS: In both groups, reduced inflammation was noted during the follow-up visits. There was no statistically significant difference between the LE/T and DM/T groups with regard to the postoperative scores or measurements, including discomfort, chemosis, secretion, conjunctival hyperemia, and conjunctival gap size (p>0.05), during the follow-up visits. Allergic reactions to the medications were not reported in any patient. Intraocular pressures were within normal limits in both groups. CONCLUSION: LE/T was found to be as effective as DM/T in reducing inflammation after strabismus surgery. LE/T, as a new-generation steroid combination product, could be used as a safe and effective anti-inflammatory agent for the treatment of inflammation following strabismus surgery.

Development of loteprednol etabonate-loaded cationic nanoemulsified in-situ ophthalmic gel for sustained delivery and enhanced ocular bioavailability.[Pubmed:27689408]

Drug Deliv. 2016 Nov;23(9):3712-3723.

A novel cationic nanoemulsified in-situ ophthalmic gel of Loteprednol etabonate (LE) was developed to improve the permeability and retention time of formulations for overall improvement of drug's ocular bioavability. Capryol 90 (oil phase), tween 80 (surfactant) and transcutol P (cosurfactant) was selected as formulation excipients to construct pseudoternary phase diagrams and nanoemulsion region was recognized from diagrams. Spontaneous emulsification method was used to manufacture LE nanoemulsion and it was optimized using 3(2) factorial design by considering the amount of oil and the ratio of surfactant to cosurfactant (Smix) as independent variables and evaluated for various physicochemical properties. Optimized NE was dispersed in Poloxamer 407 and 188 solution to form nanoemulsified sols that were predictable to transform into in-situ gels at corneal temperature. Drug pharmacokinetics of sterilized optimized in situ NE gel, NE-ISG2 [0.69% w/w Capryol 90, 0.99%w/w Smix (3:1), 13% Poloxamer 407, 4% w/w Poloxamer 188] and marketed formulation were assessed in rabbit aqueous humor. The in-situ gels were clear, shear thinning in nature and displayed zero-order drug release kinetics. NE-ISG2 showed the minimum ocular irritation potential and significantly (p < 0.01) higher Cmax and AUC(0-10 h), delayed Tmax, extended mean residence time and improved (2.54-fold times) bioavailability compared to marketed formulation.

Dose Uniformity of Topical Corticosteroids: A Simulated Trial of Fluorometholone Acetate 0.1% and Loteprednol Etabonate Gel 0.5.[Pubmed:28140772]

J Ocul Pharmacol Ther. 2017 Mar;33(2):111-114.

PURPOSE: The purpose of the study was to determine the concentrations of Flarex((R)) and Lotemax((R)) when shaken and not shaken. Many patients fail to shake or inappropriately shake suspensions of corticosteroids before instillation as directed. This study was designed to help determine what concentration of corticosteroid these patients are receiving. In addition, independent confirmation of Loteprednol etabonate ophthalmic gel dose uniformity was determined and compared as a possible alternative. METHODS: Drug concentrations of shaken versus unshaken Flarex and Lotemax were determined over a 20-day simulated tapered course in our institutional laboratory. Collected samples were analyzed by reversed-phase high-performance liquid chromatography with photodiode array detection at 240 nm. RESULTS: Flarex had a mean concentration of 93.7% of the declared concentration when shaken and 7.25% when not shaken. The difference between these groups was statistically significant (P = 0.0001). Lotemax had a mean concentration of 96.74% of the declared concentration when shaken and a mean concentration of 98.97% when not shaken. The difference between these groups was not statistically significant (P = 0.194). CONCLUSIONS: Flarex maintains dose uniformity when shaken. When not shaken, it has poor dose uniformity. Lotemax was consistent whether shaken or not in our study and can be considered to eliminate the variability of poor patient compliance with shaking. The manufacturers of both drugs recommend shaking before application.

Efficacy of olopatadine hydrochloride 0.1%, emedastine difumarate 0.05%, and loteprednol etabonate 0.5% for Chinese children with seasonal allergic conjunctivitis: a randomized vehicle-controlled study.[Pubmed:27869354]

Int Forum Allergy Rhinol. 2017 Apr;7(4):393-398.

BACKGROUND: Allergic conjunctivitis (AC) is a disease of various agents that affects the physical and mental health of children. Although the most effective therapy has not been found so far, it is essential to explore the considerable therapeutic method. We compared the clinical efficacy of olopatadine, emedastine, Loteprednol etabonate (LE), and vehicle for treating seasonal allergic conjunctivitis (SAC) in Chinese children. METHODS: Eighty cases of 160 eyes aged from 5 to 10 years with SAC were available and those subjects were randomly distributed into 4 groups. Both their eyes received olopatadine hydrochloride 0.1% twice a day, emedastine difumarate 0.05% twice a day, or LE 0.5% 4 times a day, respectively, whereas those of the control group received artificial tears (AT) 0.5% 3 times a day. This study was conducted successfully and the observations were collected before treatment and on day 8 (+/-1 day) and day 15 (+/-2 days) afterward. The principal measurement of efficacy was focused on the signs and symptoms of the subjects, evaluated before and after treatment, in addition to visual acuity (VA) and fundus oculi. RESULTS: On day 8 (+/-1 day) and day 15 (+/-2 days), all the antiallergic agents were found to be more effective than vehicle (p < 0.05) in terms of all the symptoms and signs. However, there was no statistical significance (p >/= 0.05) shown among the treatment groups. There were no evident changes in VA and no clinically significant changes were observed in fundus oculi. CONCLUSION: After the treatment, the efficacy presented a similar distribution among the trial groups.

Description

Loteprednol etabonate (LE) is an orally active "soft" steroid belonging to a unique class of glucocorticoids. Loteprednol etabonate (LE) exhibits anti-inflammatory activity and has been used in optometry and ophthalmology.

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