Ophthalmic compositions
By using a mixture of castor oil and medium-chain triglycerides to promote corneal and conjunctival re-epithelialization and mucin expression, the shortcomings of existing ocular disease treatments are addressed, resulting in better ocular surface lubrication and protection.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- LAB SALVAT SA
- Filing Date
- 2017-07-07
- Publication Date
- 2026-06-09
AI Technical Summary
Existing technologies are unable to effectively promote corneal and conjunctival reepithelialization and mucin production, especially the expression of MUC5AC, making it difficult to effectively treat various eye diseases such as dry eye, conjunctivitis, and keratitis.
A mixture of castor oil and medium-chain triglycerides was used as an ophthalmic composition, combined with a suitable pH and surfactant, to promote the expression and re-epithelialization of mucins, especially MUC1 and MUC5AC.
It significantly improves the reepithelialization process of the cornea and conjunctiva, alleviates symptoms of eye diseases such as dry eye, conjunctivitis, and keratitis, and provides better ocular surface lubrication and protection.
Smart Images
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Figure BDA0001344669660000331
Abstract
Claims
1. The use of a sterile ophthalmic composition in the preparation of a medicament for treating eye diseases, wherein the sterile ophthalmic composition comprises a) an oil phase including castor oil and medium-chain triglycerides, b) one or more surfactants and c) an aqueous phase, wherein the composition has a pH of 5.0 to 9.
0. The active ingredient of the composition consists solely of the castor oil and the medium-chain triglycerides. The medium-chain triglyceride mentioned above is caprylic / capric triglyceride. The weight ratio of castor oil to the medium-chain triglyceride is 1.5:1 to 1:1.5, and The eye diseases mentioned therein are selected from the group consisting of the following diseases: dry eye, conjunctivitis and keratitis.
2. The application according to claim 1, wherein the weight ratio of the castor oil to the medium-chain triglyceride is 1:
1.
3. The application according to claim 1, wherein the total amount of castor oil and medium-chain triglycerides is 0.05 to 70 wt% relative to the total weight of the composition.
4. The application according to claim 1, wherein the composition further comprises one or more oils other than the castor oil and the medium-chain triglycerides.
5. The use according to claim 4, wherein the one or more oils other than the castor oil and the medium chain triglyceride are selected from the group consisting of ethyl oleate, isopropyl myristate, isopropyl palmitate, isopropyl isostearate, isostearyl isostearate, myristyl lactate, ethylhexyl hydroxystearate, ethylhexyl nonanoate, triethylhexanoic acid, isohexadecane, mineral oil, vegetable oil, triisononyl, C 12-15 alkyl benzoate esters and mixtures thereof.
6. The application according to claim 1, wherein the hydrophilic-lipophilic balance value of the one or more surfactants is 10 to 16.
7. The application according to claim 6, wherein the one or more surfactants are selected from the group consisting of polyoxyethylene 35 castor oil, polyoxyethylene 20 sorbitol monooleate, sorbitol laurate, and mixtures thereof.
8. The application according to claim 1, wherein the total amount of the surfactant is 0.1 to 40 wt% relative to the total weight of the composition.
9. The application according to claim 1, wherein the composition further comprises one or more muscle elasticity modifiers.
10. The application according to claim 9, wherein the one or more muscle elasticity modifiers are selected from the group consisting of sodium chloride, glycerol, propylene glycol, and mixtures thereof.
11. The application according to claim 1, wherein the composition further comprises one or more pH adjusters.
12. The application according to claim 11, wherein the one or more pH adjusters are selected from the group consisting of tris(hydroxymethyl)aminomethane, tris(hydroxymethyl)aminomethane hydrochloride, potassium dihydrogen phosphate, disodium hydrogen phosphate, and mixtures thereof.
13. The application according to claim 1, wherein the composition further comprises 0.1 to 10 wt% of one or more tackifiers relative to the total weight of the composition, said one or more tackifiers being selected from the group consisting of sodium alginate, polyvinylpyrrolidone, gellan gum, chitosan or derivatives thereof, and mixtures thereof.
14. The application according to claim 1, wherein the composition comprises at least 80 wt% water relative to the total weight of the composition.
15. The application according to claim 1, wherein the composition is in the form of a nanoemulsion.
16. The application according to claim 1, wherein the dry eye syndrome is selected from the group consisting of keratoconjunctivitis sicca, xerophthalmia, xerostomia, and Schogren's syndrome. The conjunctivitis was selected from the group consisting of allergic conjunctivitis, vernal keratoconjunctivitis, atopic keratoconjunctivitis, bullous pemphigoid, Stephens-Johnson syndrome, toxic epidermal necrolysis, viral keratoconjunctivitis, and marginal keratoconjunctivitis. The keratitis referred to is selected from the group consisting of interstitial necrotizing keratitis, Cogan's syndrome, erosive corneal ulcer, neurotrophic keratitis, exposure keratitis, crystalline infectious keratitis, Singerson superficial punctate keratitis, filamentous keratitis, recurrent corneal epithelial erosion, epithelial dystrophy, and Meissmann's dystrophy.