A kind of eye drop containing tafluprost and preparation method thereof

Abstract

The invention provides an eye drop containing tafluprost, comprising tafluprost and a hydrophilic polymer, wherein the hydrophilic polymer is selected from polycarbophil or carbomer, and the hydrophilic polymer The content of the substance is 0.4 to 1.0%. The drug depot that can be formed by the eye drops of the present invention has the effect of slowly releasing drugs, avoids rapid elimination of drugs, and improves bioavailability; the preparation method of the eye drops is simple and easy, and is 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...

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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 secretion process of tear fluid in conjunctiva, more than about 95% of the medicinal liquid is absorbed by tear fluid It is taken away through the nasolacrimal duct, resulting in extremely low bioavailability (less than 1%), and a large amount of drugs enter the nasal cavity or digestive tract through the nasolacrimal duct and are finally absorbed by the whole body, which increases the risk of inducing toxic and side effects. 4) In order to achieve effective The lowering effect of intraocular pressure, patients with long-term drug use to increase the number and frequency of drug administration, and this will bring greater economic and physiological burden

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