Ophthalmic cetirizine hydrochloride liposome, in-situ gel and preparation method of ophthalmic cetirizine hydrochloride liposome

A technology of cetirizine hydrochloride and ophthalmic liposomes, which is applied in the field of pharmaceutical preparations, can solve the problems of short residence time, poor compliance of semi-solid dosage forms, and difficult acceptance by patients, so as to delay drug release and improve bioavailability degree of effect

Active Publication Date: 2022-04-26
CHENGDU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] The purpose of the present invention is to overcome the short residence time of cetirizine hydrochloride eye drops in the prior art in the conjunctival sac, which causes its low eye bioavailability, poor compliance of semi-solid dosage forms, and is difficult to be accepted by patients. and other defects, provide a preparation that delays drug release, increases its residence time in the eye, improves corneal permeability, and improves bioavailability

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  • Ophthalmic cetirizine hydrochloride liposome, in-situ gel and preparation method of ophthalmic cetirizine hydrochloride liposome
  • Ophthalmic cetirizine hydrochloride liposome, in-situ gel and preparation method of ophthalmic cetirizine hydrochloride liposome
  • Ophthalmic cetirizine hydrochloride liposome, in-situ gel and preparation method of ophthalmic cetirizine hydrochloride liposome

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Effect test

Embodiment 1

[0169] Prescription and ratio: cetirizine hydrochloride 28.5mg, egg yolk lecithin 356.3mg, cholesterol 41.8mg, sodium chloride: 13mg, ethyl p-hydroxybenzoate: 10mg, ultrapure water to 10mL.

[0170] Preparation method: Weigh the prescribed amount of egg yolk lecithin and cholesterol, dissolve in 5mL ethanol, stir and ultrasonically dissolve as the oil phase; add 8mL of 59.39mg / mL ammonium sulfate solution to another beaker, keep the temperature in a water bath at 50°C, as Water phase: Use a disposable 5mL syringe to slowly inject the oil phase below the liquid level of the water phase, stir magnetically (1200 rpm) while adding, continue to stir at 50°C for 50min to evaporate ethanol, and then rotate at 50°C and 200rpm Remove ethanol by evaporation; then ultrasonically smooth the inner wall of the round bottom flask, put it into a pre-treated dialysis bag, place it in 500mL 0.9% NaCl solution for dialysis for 24 hours (change the dialysate every 2 hours for the first 6 hours, an...

Embodiment 2

[0252] The best prescription (10mL) of cetirizine hydrochloride lipothermal gel containing 0.298%: cetirizine hydrochloride: 29.8mg, egg yolk lecithin: 372.5mg, cholesterol: 43.67mg, F127: 2.55g, F68 : 0.6g, sodium chloride: 13mg, ethyl p-hydroxybenzoate: 10mg and ultrapure water to 10mL.

[0253] Weigh the prescribed amount of egg yolk lecithin and cholesterol and dissolve in 5mL of ethanol, stir and ultrasonically dissolve as the oil phase; add 8mL of 59.39mg / mL ammonium sulfate solution to another beaker and keep the temperature in a water bath at 50°C as the water phase; Use a disposable 5mL syringe to slowly inject the oil phase below the liquid level of the water phase, stir magnetically (1200 rpm) while adding, continue stirring at 50°C for 50 minutes to evaporate the ethanol, and then remove the ethanol by rotary evaporation at 50°C and 200rpm Then ultrasonically smooth the inner wall of the round-bottomed flask, put it into a pre-treated dialysis bag, place it in 500m...

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Abstract

The invention discloses cetirizine hydrochloride ophthalmic liposome, in-situ gel and a preparation method of cetirizine hydrochloride ophthalmic liposome, and belongs to the technical field of pharmaceutical preparations. In order to overcome the defects that existing cetirizine hydrochloride eye drops are short in residence time, poor in compliance of semi-solid dosage forms, low in bioavailability, not easy to accept by patients and the like, an ethanol injection method is combined with an ammonium sulfate gradient method to obtain the liposome, and the liposome comprises 0.28-0.30% of cetirizine hydrochloride, 1.4-6.0% of phospholipid, 0.14-1.8% of cholesterol, 0.1-0.15% of an osmotic pressure regulator, 0.05-0.1% of a bacteriostatic agent and the balance of water. And a solvent. The invention further provides the cetirizine hydrochloride liposome-in-situ gel and a preparation method thereof. By optimizing the prescription and the process, the obtained liposome and in-situ gel can delay the drug release, increase the retention time of eyes, improve the cornea permeability and improve the bioavailability.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a cetirizine hydrochloride ophthalmic liposome, a corresponding liposome-in-situ gel and a preparation method thereof. Background technique [0002] Allergic conjunctivitis mainly refers to a kind of ocular inflammatory disease caused by hypersensitivity reaction of conjunctiva due to contact with certain atopic substances, and is one of the most common diseases in ophthalmology. For nearly half a century, the incidence of the disease has continued to increase, accounting for about 20% of the total population. There are many ways to treat allergic conjunctivitis clinically, including the use of histamines, mast cell stabilizers, short-term corticosteroids, subcutaneous or sublingual immunotherapy, and for severe and refractory patients with allergic conjunctivitis. Use immunosuppressants such as cyclosporine eye drops, etc. [0003] Cetirizine hy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/495A61K47/28A61K9/06A61P27/02A61P37/08
CPCA61K31/495A61K9/0048A61K9/1277A61K9/06A61P27/02A61P37/08Y02A50/30
Inventor 张颖王兰张静张斌陈金鑫郭雨虹
Owner CHENGDU UNIV
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