Water-based in-situ gel ophthalmic preparation for treating xerophthalmia

An in-situ gel and ophthalmic preparation technology, applied in the field of medicine, can solve the problem of not specifying thickeners and the like, and achieve the effects of reducing the frequency of frequent medication, reducing systemic absorption, and improving bioavailability

Active Publication Date: 2021-01-08
IVEW THERAPEUTICS (ZHUHAI) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Likewise, common thickeners do not exhibit the thixotropic characteristics of in situ gels, nor have thickeners (such as sodium hyaluronate) been shown to act as artificial tears for the treatment of dry eye

Method used

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  • Water-based in-situ gel ophthalmic preparation for treating xerophthalmia
  • Water-based in-situ gel ophthalmic preparation for treating xerophthalmia
  • Water-based in-situ gel ophthalmic preparation for treating xerophthalmia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: the mensuration of gel matrix concentration

[0046] The gel matrix solution samples containing 0.1% diclofenac sodium and 0.5% sodium hyaluronate at different concentrations are shown in Table 2-5:

[0047] Table 2: Concentration of Gel Matrix DGG

[0048]

[0049]

[0050] Table 3: Concentration of Xanthan Gum in Gel Matrix

[0051]

[0052] Table 4: Gel Matrix Carrageenan Concentrations

[0053]

[0054] Table 5: Concentration of Sodium Alginate in Gel Matrix

[0055]

[0056] Preparation method of gel solution

[0057] Accurately weigh a certain amount of sodium chloride, and slowly add 85 grams of deionized water. Stir until the sodium chloride is completely dissolved, and slowly add the gel base and sodium hyaluronate to the above mixture with continuous stirring. The solution was placed in a 90°C water bath and stirred for 1 hour. The mixture was then cooled to room temperature. Weigh 0.1 g of diclofenac sodium, and slowly add ...

Embodiment 2

[0073] Embodiment 2: the aqueous in situ gel ophthalmic preparation of the present embodiment

[0074] The instant ophthalmic gel containing 0.1% diclofenac sodium and 0.5% sodium hyaluronate, the specific prescription is as follows:

[0075] Diclofenac Sodium 0.1wt%, Sodium Hyaluronate 0.5%wt%, Deacetylated Gellan Gum 0.4wt%, Polyoxyethylene 35 Castor Oil 5.0wt%, Vitamin E Macrogol Succinate 0.5%, Mannitol 4.0wt% %, 0.02wt% butyl p-hydroxybenzoate, add an appropriate amount of tromethamine hydrochloride buffer solution, add water for injection to 100g, and make 100g specifications of ophthalmic instant gel containing 0.1% diclofenac sodium and 0.5% sodium hyaluronate glue. (Table 10)

[0076]

[0077] In Table 10, Sample 1 is a formulation in which a combination of polyoxyethylene 35 castor oil and vitamin E polyethylene glycol succinate was added as a solubilizer. Sample 2 is a formulation with pH adjusted to a strongly alkaline solution (pH 8.5) without a solubilizer,...

Embodiment 3

[0106] Example 3: Aqueous in situ gel ophthalmic formulations composed of different pH

[0107] Different pH in situ gel solutions containing 0.1% diclofenac sodium and 0.5% sodium hyaluronate, specific prescriptions are as follows:

[0108] Diclofenac Sodium 0.1wt%, Sodium Hyaluronate 0.5%wt%, Deacetylated Gellan Gum 0.4wt%, Polyoxyethylene 35 Castor Oil 5.0wt%, Vitamin E Macrogol Succinate 0.5%, Mannitol 4.0wt% , butyl p-hydroxybenzoate 0.02wt%, add an appropriate amount of tromethamine hydrochloride buffer or hydrochloric acid, and water for injection, make 100g ophthalmic in situ gel containing 0.1% diclofenac sodium and 0.5% sodium hyaluronate ( Table 16).

[0109]

[0110] Stability Study: Samples 1 / 2 / 3 / 4 were prepared and divided into multi-dose eye drop bottles and stored in a stability room at 25°C. Samples were taken on days 0, 3, 6, and 10, respectively.

[0111] Features: traits, pH, content of diclofenac sodium.

[0112] Table 17: Stability test results for...

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Abstract

The present invention discloses a water-based in-situ gel ophthalmic preparation. Thewater-based in-situ gel ophthalmic preparation comprises the following components: non-steroidal anti-inflammatorydrugs, polysaccharide polymers with in-situ gel characteristics, artificial tears and water, in-situ gel containing the non-steroidal anti-inflammatory drugs and the artificial tears is formed under physiological conditions of eyes, and instantaneous viscosity is increased when the drug solution is dripped into the eyes. The water-based in-situ gel ophthalmic preparation can be used for treating xerophthalmia caused by corneal injury, can supplement lacrimal secretion insufficiency during treatments, increases retention and bioavailability of the drug in the eyes, improves compliance of patients, and reduces stimulation of the drug to eyes of the patients and use frequency of the drug.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an aqueous in-situ gel ophthalmic preparation for treating dry eye. Background technique [0002] Dry eye, also known as keratoconjunctivitis sicca, is an abnormal tear quality or quantity or fluid dynamics caused by multiple factors and complex reasons, resulting in decreased tear film stability, accompanied by ocular discomfort and / or ocular surface tissue An umbrella term for a variety of disorders characterized by lesions that result in severe immune inflammation of the ocular surface and other ocular surface disorders. If timely and effective treatment is not taken, it is easy to develop intractable dry eye, form keratitis and corneal ulcer, and even cause blindness. [0003] With the widespread use of video terminals and the popularization of air-conditioning facilities in residential and office environments, dry eye syndrome has become a global epidemic. Due to the lack of suffic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K45/06A61K31/196A61K31/728A61K47/36A61K47/44A61K47/22A61K47/10A61P27/02A61P29/00A61P27/04
CPCA61K9/06A61K9/0048A61K45/06A61K31/196A61K31/728A61K47/36A61K47/44A61K47/22A61K47/10A61P27/02A61P29/00A61P27/04A61K2300/00
Inventor 波·梁彭海洲
Owner IVEW THERAPEUTICS (ZHUHAI) CO LTD
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