JP2827295B2 - Eye drops containing vitamin A - Google Patents

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an eye drop containing vitamin A palmitate or vitamin A acetate, and more particularly to an eye drop prepared by stabilizing vitamin A palmitate or vitamin A acetate in the eye drop. .

BACKGROUND ART Vitamin A is a fat-soluble vitamin and hardly dissolves in water. Therefore, in order to make this an ophthalmic agent,
An ophthalmic ointment was prepared by mixing it with an oil component, or solubilized by using a nonionic surfactant in eye drops based on sterilized purified water.

Problems to be Solved by the Invention However, in the former case, there is a problem that the usability is poor, and in the latter case, there is a problem that the vitamin A is unstable with time.

Means for Solving the Problems As a result of intensive research, the present inventors have studied the formulation of a small amount of liquid paraffin in an ophthalmic solution based on sterilized purified water and the formulation of a nonionic surfactant. By doing so, the inventors have found that the above-mentioned problem is solved, and completed the present invention.

That is, the present invention is an eye drop containing vitamin A palmitate or vitamin A acetate, 1 to 4% by weight of liquid paraffin, and 0.1 to 0.5% by weight of a nonionic surfactant.

In the present invention, as the nonionic surfactant, polyoxyethylene sorbitan mono-fatty acid esters such as polyoxyethylene sorbitan monooleate (polysorbate 80), polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monolaurate; Polyoxyethylene monofatty acid esters such as polyoxyethylene monostearate, polyoxyethylene monooleate, polyoxyethylene monopalmitate, polyoxyethylene alcohol ethers such as polyoxyethylene lauryl ether, polyoxyethylene hydrogenated castor oil, etc. And these may be used alone or as a mixture of two or more. The degree of polymerization of polyoxyethylene is desirably 10 or more from the viewpoint of usability.

In addition, there is no problem in using liquid paraffin with light liquid paraffin.

 Sterile purified water is used as a base for eye drops.

In the present invention, if the amount of the liquid paraffin is less than 1% by weight, the stabilization of vitamin A is not sufficiently performed. On the other hand, when the content exceeds 4% by weight, the feeling of use of the eye drops is deteriorated.

If the amount of the nonionic surfactant is less than 0.1% by weight, the emulsifiability of oil components such as liquid paraffin and vitamin A in water deteriorates. If it exceeds 0.5% by weight, the stabilization of vitamin A is not sufficiently performed.

The compounding amount of vitamin A palmitate or vitamin A acetate is 100,000 IU / 100 ml.

In the eye drops of the present invention, in addition to the above essential components, if necessary, vitamin E acetate, dipotassium glycyrrhizinate, sodium flavin adenine dinucleotide, neostigmine methyl sulfate, cyanocobalamin, taurine,
Drugs such as sodium chondroitin sulfate, pyridoxine hydrochloride, epsilon-aminocaproic acid, chlorpheniramine maleate, allantoin, naphazoline hydrochloride, phenylephrine hydrochloride, tetrahydrozoline hydrochloride, magnesium potassium L-aspartate, sodium chloride,
Isotonic agents such as potassium chloride, stabilizers such as disodium ethylenediaminetetrahydrochloride, benzalkonium chloride,
Preservatives such as methylparaben, propylparaben, and sorbic acid; buffers such as citric acid, sodium citrate, boric acid, and borax; and polyhydric alcohols, polyvinyl alcohol, polyvinylpyrrolidone, hydroxypropylmethylcellulose, and high-performance such as methylcellulose and hydroxyethylcellulose. A molecular additive or the like may be blended.

 The eye drop of the present invention is produced as follows.

That is, an oil layer composed of vitamin A palmitate or vitamin A acetate, liquid paraffin, and an aqueous layer composed of sterilized purified water, a nonionic surfactant, etc., are emulsified using a homomixer or a microfluidizer, and filled in an ophthalmic container. Alternatively, the solution is filled into an ophthalmic container so as to form a two-layer liquid in the order of an aqueous layer and an oil layer (in this case, the ophthalmic solution is shaken before use to emulsify).

Test Example An eye drop having the formulation shown in Table 1 was prepared and filled into ampoules. These samples were examined for the residual ratio of vitamin A acetate after storage at 50 ° C. for one month. In addition,
The content of vitamin A acetate was determined by high performance liquid chromatography (column: TSK-Gel LS410, moving bed; methanol: water: phosphoric acid = 98: 2: 0.1, measurement wavelength; 280 nm).

 Table 1 shows the results.

Effect of the Invention According to the present invention, it has become possible to provide a vitamin A-containing eye drop having excellent stability. Moreover, the eye drops of the present invention have a good feeling in use.

Examples Hereinafter, the present invention will be described in more detail with reference to examples.

Example 1 Ingredients Compounding amount Vitamin A palmitate (1.7 million IU / g) 0.04 g Liquid paraffin 1.96 g Dipotassium glycyrrhizinate 0.1 g Taurine 1.0 g Sodium chondroitin sulfate 0.5 g Benzalkonium chloride 0.01 g Sodium chloride Appropriate amount of ethylenediaminetetraacetic acid Sodium 0.003 g Polyoxyethylene (60) hydrogenated castor oil 0.1 g Sterile purified water was added to the above components to make a total volume of 100 ml.
Next, the mixture was emulsified using a homomixer and a microfluidizer, and then filled in a polyester eye drop container to prepare an eye drop.

Example 2 Ingredients Compounding amount Vitamin A acetate (500,000 IU / g) 0.04 g Vitamin E acetate 0.03 g Light liquid paraffin 3.93 g Pyridoxine hydrochloride 0.1 g Magnesium potassium L-aspartate 1.0 g Polyvinylpyrrolidone 1.0 g Methyl paraben 0.03 g Propyl Paraben 0.01 g Sodium chloride 0.1 g Boric acid 1.0 g Borax Suitable amount Disodium ethylenediaminetetraacetate 0.003 g Polysorbate 80 0.1 g Polyester made by adding sterilized purified water to the water-soluble components of the above components so that the total volume becomes 100 ml The mixture was filled in an eye drop container, and then the oil component was filled so as to float above the aqueous layer to prepare an eye drop consisting of two layers.

Claims (1)

(57) [Claims] An eye drop containing vitamin A palmitate or vitamin A acetate, 1 to 4% by weight of liquid paraffin and 0.1 to 0.5% by weight of a nonionic surfactant.