Eye drops containing tafluprost and preparation method thereof

A technology of tafluprost and eye drops, applied to medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., which can solve the problem of unstable intraocular pressure effects, inaccurate doses, and increased risks of inducing toxic and side effects And other issues

Active Publication Date: 2015-05-20
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The existing dosage form on the market is water-based eye drops. The solution-type eye drops have the advantages of simple production process and easy operation, but there are the following disadvantages: 1) The dosage is not accurate, and the amount of each instillation of the patient is different. , lead to differences in the outflow of uveoscleral aqueous humor, which makes the effect of lowering intraocular pressure unstable, and there are safety risks; The average blood concentration of prostaglandin acid is lower than the detection limit (10pg/mL) in bioanalytical test; 3) in the non-stop blinking of eyelid and the non-stop secret...

Method used

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  • Eye drops containing tafluprost and preparation method thereof
  • Eye drops containing tafluprost and preparation method thereof
  • Eye drops containing tafluprost and preparation method thereof

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Embodiment Construction

[0011] The inventors have found in their research that using the hydrophilic polymer polycarbophil AA-1 or carbomer as an eye drop sustained-release material, which is in the form of an aqueous solution in an in vitro environment, when dripped into the conjunctival sac, Affected by the temperature, pH or ionic strength of the eye, it quickly forms a gel and attaches to the surface of the eyeball, forming a very thin layer of drug storage, which can not only increase the retention time of the drug in the eye, avoid the rapid loss of the drug, and The formed drug depot has the effect of slowly releasing the drug, avoiding the rapid elimination of the drug, and improving the bioavailability.

[0012] The invention provides an eye drop containing tafluprost, which comprises the active ingredient tafluprost and a hydrophilic polymer, wherein the hydrophilic polymer is selected from polycarbophil or carbomer.

[0013] In some embodiments, according to the total weight percentage, th...

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Abstract

The invention provides eye drops containing tafluprost. The eye drops comprise tafluprost and a hydrophilic polymer, wherein the hydrophilic polymer is selected from polycarbophil or carbomer and the content of the hydrophilic polymer is 0.4-1.0%. Medicament storage formed by the eye drops plays a role of slowly releasing medicaments, prevents medicaments from being rapidly eliminated, and improves the bioavailability. The preparation method of the eye drops is simple and feasible and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an eye drop containing tafluprost and a preparation method thereof. Background technique [0002] The structure of Tafluprost is as follows: [0003] [0004] It is a new generation of prostaglandin derivative anti-glaucoma drugs, which can increase the outflow of aqueous humor through the uveoscleral pathway, achieve the effect of lowering intraocular pressure, and play a role in the treatment of glaucoma. Tafluprost was first developed by Santen Pharmaceutical Co., Ltd. in Japan. It is a colorless or light yellow viscous liquid, almost insoluble in water, sensitive to heat, and needs to be frozen for storage. [0005] The existing dosage form on the market is water-based eye drops. The solution-type eye drops have the advantages of simple production process and easy operation, but there are the following disadvantages: 1) The dosage is not accurate, and the amount...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/216A61P27/06
Inventor 赵玉姣
Owner SUNSHINE LAKE PHARM CO LTD
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