JPH0338519A - Eye drops containing vitamin A - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention relates to eye drops containing vitamin A palmitate or vitamin A acetate, and more particularly to eye drops containing stabilized vitamin A palmitate or vitamin A acetate in the eye drops. .

Conventional technology Vitamin A is a fat-soluble vitamin and hardly dissolves in water. Therefore, in order to use it as an ophthalmic preparation, it must be mixed with an oil component and made into an eye ointment, or it must be mixed with sterile purified water. eye drops based on the drug were solubilized using a nonionic surfactant.

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

Means for Solving the Problems As a result of intensive research, the present inventors formulated a small amount of liquid paraffin into an eye drop based on sterile purified water.
Furthermore, the inventors have found that the above problem can be solved by examining the amount of nonionic surfactant added, and have 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 monooleate (polysorbate 80), polyoxyethylene sorbitan monooleate
Polyoxyethylene sorbitan monofatty acid esters such as polyoxyethylene sorbitan monolaurate, polyoxyethylene monofatty acid esters such as polyoxyethylene monostearate, polyoxyethylene monooleate, and polyoxyethylene monopalmitate , polyoxyethylene alcohol ether such as polyoxyethylene lauryl ether, polyoxyethylene hydrogenated castor oil, etc., and these may be used alone or in combination of two or more types. The degree of polymerization of ethylene is desirably 10 or more from the viewpoint of feeling in use.

Furthermore, as for liquid paraffin, there is no problem in using light liquid paraffin.

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

In the present invention, if the amount of liquid paraffin is less than 1% by weight, vitamin A will not be sufficiently stabilized.
Moreover, if it exceeds 4% by weight, the feeling of use of the eye drops becomes worse.

If the amount of the nonionic surfactant is less than 0.1% by weight, the emulsifying properties of oil components such as liquid paraffin and vitamin A in water will deteriorate. Moreover, if it exceeds 0.5% by weight, vitamin A will not be stabilized sufficiently.

The amount of vitamin A palmitate or vitamin A acetate is 1 to 100,000 I, U, /100ml! It is.

In addition to the above-mentioned essential ingredients, the eye drops of the present invention optionally contain vitamin E acetate, dipotassium glycyrrhizinate,
Sodium flavin adenine dinucleotide, neostigmine methyl sulfate, dianocobalamin, taurine, sodium fundroitin sulfate, pyridoxine hydrochloride, epsilon-aminocaproic acid, chlorpheniramine maleate, allantoin, naphazoline hydrochloride, phenylephrine hydrochloride, tetrahydrozoline hydrochloride, magnesium L-aspartate Drugs such as potassium, tonicity agents such as sodium chloride, potassium chloride, stabilizers such as disodium ethylenediaminetetraacetate, preservatives such as benzalkonium chloride, methylparaben, propylparaben, sorbic acid, citric acid, Buffers such as sodium, boric acid, borax, polyhydric alcohol, polyvinyl alcohol,
Polymer additives such as bonovinylpyrrolidone, hydroxypropylmethylcellulose, methylcellulose, and hydroxyethylcellulose can also be blended.

The eye drops of the present invention are manufactured as follows.

That is, an oil layer consisting of vitamin A pal, mitate or vitamin A acetate, liquid paraffin, etc. and an aqueous layer consisting of sterile purified water, a nonionic surfactant, etc. are emulsified using a homomixer or a microfluidizer to form an eye drop container. or fill it into an eye drop container so that it becomes a two-layer solution, consisting of an aqueous layer and an oil layer (in this case, the eye drops should be shaken and emulsified before use).

Test Example Eye drops having the formulation shown in Table 1 were prepared and filled into ampoules. For these samples, the residual rate of vitamin A acetate after storage at 50° C. for one month was investigated. The content of vitamin A acetate was determined by high performance liquid chromatography (column: TSK-Gel LS410. Mobile phase: methanol:water diphosphoric acid-98:2:o,t
, measurement wavelength; 280 nm).

The results are shown in Table 1.

Table 1 Note: Vitamin A palmitate O, 04w75% is 6.8
Just in case. U, / corresponds to concave -.

Effects of the Invention The present invention has made it possible to provide vitamin A-containing eye drops with excellent stability. Moreover, the eye drops of the present invention have a good feeling of use.

Example Hereinafter, the present invention will be explained in more detail with reference to Examples.

Example 1 Ingredients Blend amount Vitamin A palmitate (1.7 million I”, U, 7g) 0.04g
Liquid paraffin 1.96g Dipotassium glycyrrhizinate 0.1g Taurine
1. Og fundroitin sulfate sodium 0.5g benzalkonium chloride
0.01 g sodium chloride
Appropriate amount Disodium ethylenediaminetetraacetate 0.003 g Polyoxyethylene (60) Hydrogenated castor oil 0.1 g Sterilized purified water was added to the above ingredients to make the total amount IOM.Next, emulsification was performed using a homomixer and a microfluidizer. Thereafter, the mixture was filled into polyester eye drop containers to prepare eye drops.

Example 2 Ingredients Blend amount Vitamin A acetate (500,001.U, 7 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 1.0g Methylparaben
0.03 g propylparaben
0.01 g sodium chloride
0.1g boric acid
1.0g borax
Appropriate amount Disodium ethylenediaminetetraacetate 0.003 g Polysorbate 80 Q, l
g Sterilized purified water is added to the water-soluble components of the above components so that the total amount is IOM, and the mixture is filled into a polyester eye drop container.Then, the oil component is filled so as to float on top of the water layer, and the two-layer An eye drop consisting of the following was prepared.

Claims (1)

[Claims] (1) Eye drops 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.