KR0153855B1 - Visual acuity protective agent - Google Patents

Abstract

The present invention relates to an eye care agent which improves the absorption rate by increasing the dissolution rate of pharmacologically active ingredients, and includes, as a main component, barkinium myrutilus extract, L-citrulline, N-acetyl-L-aspartic acid, retinol acetate, tocopherol acetate and hydrochloric acid. It contains pyridoxine, it contains soybean oil, coconut oil, sulfur and soybean phospholipid as excipients, it contains 4: 1 parts by weight of a mixture of methyl paraoxybenzoate and propyl paraoxybenzoate as a preservative, and contains other fragrances, colorants and light-shielding agents. One gelatin soft capsule vision protectant.

In the preparation method, the main component is dissolved and suspended in the excipient, a mixture of 4: 1 parts by weight of paraoxybenzoic acid methyl and paraoxybenzoic acid propyl is added as a preservative, and these contents are encapsulated with gelatin to prepare a soft capsule.

Description

Eyesight protector with improved absorption rate and preparation method thereof

1 is a dissolution degree graph of the soft capsule and the tablet of the present invention.

The present invention relates to an eye care agent having improved absorption rate, and a method for manufacturing the same. The present invention relates to a pharmaceutical composition for eye protection and a method for preparing the same having excellent stability and excellent dissolution ability of an active ingredient.

Currently, many eye-protective agents such as chondroitin (chondroitin) are introduced. Among them, the main ingredients are Bakinium, Vaccinium myrtillus ext., L-citrulline, and N-citrulline. Tablet-type formulations containing acetyl-L-aspartic acid, retinol acetate, tocopherol acetate and pyridoxine hydrochloride have been developed, but spots are formed on the tablet surface due to the wettability of the main ingredient, resulting in a poorly prepared product and in question of stability. There has always been a problem to be improved.

Therefore, the present invention was able to solve the drawbacks of the tablet formulation by formulating into a soft capsule during the study to solve such defects, and furthermore to improve the dissolution of the drug to improve the absorption rate of high quality soft capsule drug After confirming that it can be obtained, it is filed as a patent.

An object of the present invention is to provide an eye protector having improved absorption and a method of manufacturing the same.

The eye protectant of the present invention contains barkinium myrutilus extract, L-citrulline, N-acetyl-L-aspartic acid, retinol acetate, tocopherol acetate and pyridoxine hydrochloride as main components, and as an excipient, soybean oil, coconut oil, sulfur wax, soybean, It is a gelatin soft capsule vision-protective agent containing phospholipid and containing 4: 1 parts by weight of paraoxybenzoic acid methyl and paraoxybenzoic acid propyl as a preservative, and a fragrance, a coloring agent and a light shielding agent. In a homogeneously mixed medium of hardened oil, lead and soybean phospholipid, Bakinium mirutilose extract, L-citrulline, N-acetyl-L-aspartic acid, retinol acetate, tocopherol acetate and pyridoxine hydrochloride are suspended and paraoxygen is suspended in the suspension contents. A mixture of 4: 1 parts by weight of methyl benzoate and paraoxybenzoic acid propyl was dissolved in purified water and added, followed by gelatin, concentrated glycerin, and D-sorbitol. It is a method for producing a soft capsule for eyesight protection, characterized in that the liquid is heated and dissolved, and then homogenized with a homogenizer to form a capsule film and to contain it.

That is, the ophthalmic protective agent pharmaceutical composition of the present invention contains, as a main component, bakinium myrutilus extract, L-citrulline, N-acetyl-L-aspartic acid, retinol acetate, tocopherol acetate and pyridoxine hydrochloride. First, the method for preparing the composition of the present invention is an excipient such as soybean oil, coconut oil, wax, and soybean phospholipid. The main ingredient is barkinium mirutilus extract, L-citrulline, N-acetyl-L-aspartic acid, retinol acetate, acetic acid Suspended tocopherol and pyridoxine hydrochloride to prepare the suspension contents, and then the suspension contents were mixed and homogenized by gelatin, concentrated glycerin, and D-sorbitol liquid, and then paraoxybenzoic acid methyl and paraoxybenzoic acid propyl as preservatives. A film is formed from a soft capsule base added by mixing at a weight ratio of 4: 1 to produce a soft capsule encapsulated.

Titanium oxide may be included as the light-shielding agent in the production method, and may contain a fragrance such as ethylvanillin and other colorants. It may also contain cyclodextrins to stabilize the formulation, but is not necessary.

The soft capsule of the present invention was subjected to the same composition tablet and dissolution comparison test. As can be seen from Table 2, the elution of the tablet after 15 minutes was 17.6%, while that of the soft capsule was 52.4%. The dissolution degree is 72.4%, whereas the soft capsule dissolution degree of the present invention is 97.9%, and it can be seen that it is a much superior drug due to its higher dissolution rate than the tablet of the same composition.

Example 1

1. Composition: In soft capsule

2. Manufacture

Soybean oil 28.83Kg, coconut oil 7.875Kg, 2.625Kg of sulfur and 1.5Kg of soybean phospholipid were mixed well while warming to 65 ℃, and then 15Kg of Bakinium Myrutilus extract, 1.5Kg of L-citrulline, N-acetyl-L- Aspartic acid 1.5Kg, 0.75Kg retinol acetate, 3.7Kg tocopherol acetate and 3.7Kg pyridoxine hydrochloride are mixed and homogenized with homogenizer to prepare the suspension contents.

Separately, 14.55Kg of gelatin, 4.2Kg of concentrated glycerin, and 6Kg of D-soribitol solution were added to the purified water dissolved in advance by adding an appropriate amount of paraoxybenzoic acid methyl 40.5g, propyl paraoxybenzoic acid propyl, and equvanillin, a pigment, and a pigment. It is made into a capsule base by adjusting so that it may have a moderate roughness under 15 mmHg pressure reduction at 70 degreeC.

After molding with a capsule base, the prepared suspension contents are filled and molded (capacity 615 mg × 150,000 soft caps), cooled, and rolled to obtain a finished product.

Example 2-8

The amount of paraoxybenzoic acid methyl and paraoxybenzoic acid propyl preservatives in the suspension contents prepared according to Example 1 was adjusted as shown in Table 1 below.

According to the test results, paraoxybenzoic acid methyl and paraoxybenzoic acid propyl showed stable state when mixed at a weight ratio of 3: 1 to 5: 1, and among them, 4: 1 showed the optimal preservation effect. .

Experimental Example 1 (Dissolution Test Data)

The three batches prepared according to Example 1 (batch no. SC 130, SC 131, SC 132) and the main ingredients were the same as in Example 1 and the three batches prepared by conventional purification methods (batch no. T61, T62) , T63) was tested.

1. Test Equipment

1) Dissolution Tester

2) Spectrophotometer

2. Test Sample

1) Preparation of soft capsule according to Example 1 of the present invention

SC 130 (manufactured on 10/15/93)

SC 131 (manufactured on October 16, 1993)

SC 132 (manufactured on October 17, 1993)

2) Manufacture of tablets according to conventional methods for comparative testing

T 61 (manufactured by 93.10.5)

T 62 (manufactured by 93.10.6)

T 63 (manufactured by 93.10.7)

3. Dissolution test of Bakinium Myrutilus X

1) Test solution

20 g of sodium chloride is added to 8.1 ml of hydrochloric acid (35%) and water to make 1 l (PH 1.2).

Add 667 ml (6: 4) of ethanol to this solution and mix.

2) Preparation of Test Solution

Place 900 ml of test solution in the tester and warm it to 37 ± 0.5 ° C. Then, put 1 capsule (tablet, comparative test) into the formulation that passed the weight deviation test, and set the number of revolutions to 100 RPM. Test according to Method 2 of the test method (Paddle method).

15 minutes after the start of the test, take 10 ml of the solution with Pippet, add 10 ml of the test solution warmed to 37 ° C. in the tester, and after 15 minutes, take 10 ml of the solution, add each test solution to make 100 ml, and filter with 0.45 μm membrane filter paper. 15 minutes later and 30 minutes later.

3) Preparation of Standard Solution

Accurately weigh 110mg of Barkinium Myrtilus extract, add 170ml of anhydrous ethanol, add 30ml of 1.5N hydrochloric acid to make 200ml, and filter. Take 2 ml of this filtrate, add test solution to make 100 ml, and use this standard solution.

4) Condition (absorbance measurement)

Device: UV / VISIBLE SPECTROPHOTOMETER

Control solution: Test solution Wavelength: 535 nm

4. Dissolution Test Result

As shown in Table 2 below, as shown in the test results, the elution after 15 minutes was an average of 17.6% for tablets, whereas 52.4% for soft capsules, and 74.2% for tablets after 30 minutes. In the case of, the elution rate was 97.7%, much better than that of tablets, which showed the improvement of absorption rate of pharmacologically active ingredient.

This is shown graphically and attached to FIG.

Experimental Example 2 (Stability Line Test)

Stability test was performed with three batches of soft capsules prepared according to Example 1.

1. Test Equipment

1) Thermo-hygrostat 2) HPLC 3) UV-Spectrophotometer

2. Test Sample

Soft capsule prepared according to Example 1 of the present invention

SC-135 (manufactured on October 22, 2008)

SC-136 (manufactured on October 23, 2009)

SC-137 (manufactured on October 24, 2008)

3. Test condition

1) Acceleration test

Storage condition: 40 ℃, 75% RH

Test period: '93 .10.26 ~ '94 .4.27

Test equipment: start of test and 2, 4, 6 months

Test Items: Appearance, Identification, Disintegration, Content

2) Severity Test

Storage condition: 60 ℃

Test period: '93 .10.26 ~ '94 .4.27

-Test period: Test start and 2, 4, 6 months

Test Items: Appearance, Identification, Disintegration, Content

4. Test score

Accelerated test results are shown in Table 3 below, and severe test results are shown in Table 4 below.

5. Test result

From the test it was confirmed that the stability was secured during the three years of use.

Claims (2)

It contains Bachinium Myrutilus X, L-Citrulline, N-acetyl-L-aspartic acid, Retinol acetate, Tocopherol Acetate, and Pyridoxine Hydrochloride as main ingredients, and contains soybean oil, coconut oil, coconut oil, soybean phospholipid as excipients, and as a preservative A gelatin soft capsule vision care agent comprising a 4: 1 parts by weight mixture of paraoxybenzoic acid methyl and paraoxybenzoic acid propyl and a fragrance, colorant, and light-shielding agent. Suspension of barkinium mirutilus extract, L-citrulline, N-acetyl-L-aspartic acid, retinol acetate, tocopherol acetate and pyridoxine hydrochloride in a homogeneous mixture of soybean oil, coconut oil, lead and soybean phospholipids. After adding 4: 1 parts by weight of a mixture of paraoxybenzoic acid methyl and paraoxybenzoic acid in dissolved water in purified water, gelatin, concentrated glycerin, and D-sorbitol solution were heated and dissolved, and homogenized with a homogenizer. Formation, manufacturing method of a soft capsule for eyesight protection, characterized in that the inclusion.