Ebastine oral solution and preparation method thereof

Abstract

The invention provides an ebastine oral solution and a preparation method thereof, and belongs to the technical field of medicines. The ebastine oral solution comprises the following components in percentage by mass: 1-5% of ebastine, 5-10% of a composite dispersant, 5-10% of a sweetening agent, 0.5-1% of a defoaming agent and the balance of water, the composite dispersing agent is formed by mixing Tween 80, povidone and Arabic gum. According to the ebastine oral solution and the preparation method thereof, the composite dispersing agent is prepared from the Tween 80, the povidone and the Arabic gum, and the ebastine oral solution is prepared from the composite dispersing agent, so that the stability of the oral solution is remarkably improved, and the problem of layering after long-time storage is avoided.

Description

TECHNICAL FIELD

[0001] The application provides an ebastine oral solution and a preparation method thereof, and belongs to the technical field of medicines. BACKGROUND

[0002] The ebastine oral solution is a commonly used antihistamine in clinic and is mainly used for relieving allergic symptoms. Ebastine is a peripheral histamine H1 receptor antagonist and can be metabolized into active carbastine in the body after oral administration. By selectively blocking peripheral histamine H1 receptors, the allergic reaction mediated by histamine is reduced, and the specific effect is concentrated on relieving the symptoms of allergic diseases. Ebastine is mainly applied to relieve the symptoms of allergic rhinitis, relieve the symptoms of chronic urticaria, and relieve other mild and moderate allergic symptoms mediated by histamine such as allergic conjunctivitis and allergic dermatitis. At present, the ebastine oral solution has the defect of poor stability, and there is a serious delamination problem after long storage, resulting in unsatisfactory use effect. SUMMARY

[0003] Based on this, the application provides an ebastine oral solution and a preparation method thereof. The ebastine oral solution is prepared by using a composite dispersing agent, which avoids the delamination problem after long storage and significantly improves the use effect of the ebastine oral solution.

[0004] An ebastine oral solution comprises the following components in mass percentage:

[0005] 1-5% of ebastine, 5-10% of a composite dispersing agent, 5-10% of a sweetening agent, 0.5-1% of an antifoaming agent, and the rest of water.

[0006] The composite dispersing agent is a mixture of Tween 80, povidone and gum arabic.

[0007] Preferably, the mass ratio of Tween 80, povidone and gum arabic in the composite dispersing agent is 1:2:1-3.

[0008] Preferably, the povidone is at least one of povidone K30 or povidone K12.

[0009] Preferably, the sweetening agent comprises at least one of sucrose, glucose, sorbitol, maltitol, mannitol, mogroside, steviol glycoside and sucralose.

[0010] Preferably, the antifoaming agent is a mixture of soybean oil and polyglycerol fatty acid ester.

[0011] Further preferably, the mass ratio of the soybean oil and the polyglycerol fatty acid ester is 5-8:1.

[0012] Preferably, 1-1.5% of a fragrance is further included, the fragrance including any one of strawberry essence, vanilla essence, honey peach essence, and cantaloupe essence.

[0013] Preferably, 1-2% of a preservative is further included, the preservative being potassium sorbate.

[0014] The preparation method of the ebastine oral solution is that the above ingredients are weighed and mixed in proportion, a pH adjuster is added to adjust the pH of the solution to 4.5-5, and the ebastine oral solution is obtained after uniform mixing.

[0015] Preferably, the pH adjuster is one or more of a phosphate buffer solution, an acetate buffer solution, citric acid, and malic acid.

[0016] Compared with the prior art, the present application has the following beneficial effects:

[0017] The present application provides an ebastine oral solution, which is prepared by using a composite dispersing agent made of Tween 80, povidone, and acacia gum, so that the stability of the oral solution is significantly improved, and the problem of stratification after long storage is avoided. DETAILED DESCRIPTION

[0018] In order to make the purpose, technical scheme and advantages of the present application more clear, the preferred embodiments of the present application are further described in detail below in combination with examples. All other examples obtained by those skilled in the art without creative labor on the basis of the examples in the present application belong to the scope of protection of the present application.

[0019] Example 1

[0020] An ebastine oral solution includes the following ingredients in mass percentage:

[0021] 3% of ebastine, 8% of a composite dispersing agent, 5% of a sweetening agent, 0.5% of an antifoaming agent, 1.0% of a fragrance, 1.0% of a preservative potassium sorbate, and the rest water;

[0022] The composite dispersing agent is mixed by Tween 80, povidone, and acacia gum in a mass ratio of 1:2:1, wherein the povidone is povidone K30; the sweetening agent is sucrose. The antifoaming agent is mixed by soybean oil and polyglycerol fatty acid ester in a mass ratio of 8:1. The fragrance is strawberry essence.

[0023] The preparation method of the ebastine oral solution in the present example is that the above ingredients are weighed and mixed in proportion, a pH adjuster is added to adjust the pH of the solution to 4.5, and the ebastine oral solution is obtained after uniform mixing, wherein the pH adjuster is a phosphate buffer solution.

[0024] Example 2

[0025] An ebastine oral solution comprising the following ingredients by mass percentage:

[0026] ebastine 3%, composite dispersant 8%, sweetener 5%, antifoaming agent 0.5%, flavoring agent 1.0%, preservative potassium sorbate 1.0%, and the rest water;

[0027] The composite dispersant is a mixture of Tween 80, povidone, and acacia gum in a mass ratio of 1:2:2, wherein the povidone is povidone K30. The sweetener is sucrose. The antifoaming agent is a mixture of soybean oil and polyglycerol fatty acid ester in a mass ratio of 8:1. The flavoring agent is strawberry flavor.

[0028] The preparation method of the ebastine oral solution in this example is to weigh the above ingredients in proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 4.5, and mix uniformly to obtain the ebastine oral solution, wherein the pH adjuster is a phosphate buffer solution.

[0029] Example 3

[0030] An ebastine oral solution comprising the following ingredients by mass percentage:

[0031] ebastine 3%, composite dispersant 8%, sweetener 5%, antifoaming agent 0.5%, flavoring agent 1.0%, preservative potassium sorbate 1.0%, and the rest water;

[0032] The composite dispersant is a mixture of Tween 80, povidone, and acacia gum in a mass ratio of 1:2:3, wherein the povidone is povidone K30. The sweetener is sucrose. The antifoaming agent is a mixture of soybean oil and polyglycerol fatty acid ester in a mass ratio of 8:1. The flavoring agent is strawberry flavor.

[0033] The preparation method of the ebastine oral solution in this example is to weigh the above ingredients in proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 4.5, and mix uniformly to obtain the ebastine oral solution, wherein the pH adjuster is a phosphate buffer solution.

[0034] Example 4

[0035] An ebastine oral solution comprising the following ingredients by mass percentage:

[0036] ebastine 5%, composite dispersant 10%, sweetener 5%, antifoaming agent 1%, flavoring agent 1.5%, preservative potassium sorbate 2%, and the rest water;

[0037] The composite dispersant is composed of Tween 80, povidone, and gum arabic in a mass ratio of 1:2:1, wherein the povidone is povidone K12. The sweetener is sucralose; the defoamer is composed of soybean oil and polyglycerol fatty acid esters in a mass ratio of 5:1. The flavoring agent is vanilla extract.

[0038] The method for preparing the ebastine oral solution described in this embodiment is to weigh the above-mentioned components according to the proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 5, and mix them evenly to obtain the ebastine oral solution, wherein the pH adjuster is an acetate buffer solution.

[0039] Example 5

[0040] An ebastine oral solution comprising the following components by weight percentage:

[0041] Ebastine 5%, compound dispersant 10%, sweetener 5%, defoamer 1%, fragrance 1.5%, potassium sorbate preservative 2%, the remainder is water;

[0042] The composite dispersant is composed of Tween 80, povidone, and gum arabic in a mass ratio of 1:2:2, wherein the povidone is povidone K12. The sweetener is sucralose; the defoamer is composed of soybean oil and polyglycerol fatty acid esters in a mass ratio of 5:1. The flavoring agent is vanilla extract.

[0043] The method for preparing the ebastine oral solution described in this embodiment is to weigh the above-mentioned components according to the proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 5, and mix them evenly to obtain the ebastine oral solution, wherein the pH adjuster is an acetate buffer solution.

[0044] Example 6

[0045] An ebastine oral solution comprising the following components by weight percentage:

[0046] Ebastine 5%, compound dispersant 10%, sweetener 5%, defoamer 1%, fragrance 1.5%, potassium sorbate preservative 2%, the remainder is water;

[0047] The composite dispersant is composed of Tween 80, povidone, and gum arabic in a mass ratio of 1:2:3, wherein the povidone is povidone K12. The sweetener is sucralose; the defoamer is composed of soybean oil and polyglycerol fatty acid esters in a mass ratio of 5:1. The flavoring agent is vanilla extract.

[0048] The method for preparing the ebastine oral solution described in this embodiment is to weigh the above-mentioned components according to the proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 5, and mix them evenly to obtain the ebastine oral solution, wherein the pH adjuster is an acetate buffer solution.

[0049] Example 7

[0050] An ebastine oral solution comprising the following components by weight percentage:

[0051] Ebastine 2%, compound dispersant 10%, sweetener 5%, defoamer 0.5%, fragrance 1.5%, preservative potassium sorbate 1%, the remainder is water;

[0052] The composite dispersant is a mixture of Tween 80, povidone, and gum arabic in a mass ratio of 1:2:1, wherein the povidone is povidone K30. The sweetener is steviol glycoside. The defoamer is a mixture of soybean oil and polyglycerol fatty acid esters in a mass ratio of 7:1. The flavoring agent is cantaloupe flavoring.

[0053] The method for preparing the ebastine oral solution described in this embodiment is to weigh the above-mentioned components according to the proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 4.5, and mix evenly to obtain the ebastine oral solution, wherein the pH adjuster is citric acid.

[0054] Example 8

[0055] An ebastine oral solution comprising the following components by weight percentage:

[0056] Ebastine 2%, compound dispersant 10%, sweetener 5%, defoamer 0.5%, fragrance 1.5%, preservative potassium sorbate 1%, the remainder is water;

[0057] The composite dispersant is a mixture of Tween 80, povidone, and gum arabic in a mass ratio of 1:2:2, wherein the povidone is povidone K30. The sweetener is steviol glycoside. The defoamer is a mixture of soybean oil and polyglycerol fatty acid esters in a mass ratio of 7:1. The flavoring agent is cantaloupe flavoring.

[0058] The method for preparing the ebastine oral solution described in this embodiment is to weigh the above-mentioned components according to the proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 4.5, and mix evenly to obtain the ebastine oral solution, wherein the pH adjuster is citric acid.

[0059] Example 9

[0060] An ebastine oral solution comprising the following components by weight percentage:

[0061] Ebastine 2%, compound dispersant 10%, sweetener 5%, defoamer 0.5%, fragrance 1.5%, preservative potassium sorbate 1%, the remainder is water;

[0062] The composite dispersant is composed of Tween 80, povidone, and gum arabic in a mass ratio of 1:2:3, wherein the povidone is povidone K30. The sweetener is steviol glycoside. The defoamer is composed of soybean oil and polyglycerol fatty acid esters in a mass ratio of 7:1. The flavoring agent is cantaloupe flavoring.

[0063] The method for preparing the ebastine oral solution described in this embodiment is to weigh the above-mentioned components according to the proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 4.5, and mix evenly to obtain the ebastine oral solution, wherein the pH adjuster is citric acid.

[0064] Example 10

[0065] An ebastine oral solution comprising the following components by weight percentage:

[0066] Ebastine 5%, compound dispersant 5%, sweetener 5%, defoamer 1%, fragrance 1%, preservative potassium sorbate 2%, the remainder is water;

[0067] The composite dispersant is composed of Tween 80, povidone, and gum arabic in a mass ratio of 1:2:3, wherein the povidone is povidone K30. The sweetener is mannitol. The defoamer is composed of soybean oil and polyglycerol fatty acid esters in a mass ratio of 6:1. The flavoring agent is strawberry flavoring.

[0068] The method for preparing the ebastine oral solution described in this embodiment is to weigh the above-mentioned components according to the proportion and mix them, then add a pH adjuster to adjust the pH of the solution to 5, and mix evenly to obtain the ebastine oral solution, wherein the pH adjuster is malic acid.

[0069] The embodiments described above are some, but not all, embodiments of the present invention. The detailed description of the embodiments of the present invention is not intended to limit the scope of the claimed invention, but merely to illustrate selected embodiments. All other embodiments obtained by those skilled in the art based on the embodiments of the present invention without inventive effort are within the scope of protection of the present invention.

Claims

1. An ebastine oral solution, characterized in that, Including the following components by mass percentage: Ebastine 1-5%, compound dispersant 5-10%, sweetener 5-10%, defoamer 0.5-1%, the remainder is water; The composite dispersant is a mixture of Tween 80, povidone, and gum arabic.

2. The ebastine oral solution according to claim 1, characterized in that, The mass ratio of Tween 80, polyvinyl ketone, and gum arabic in the composite dispersant is 1:2:1~3.

3. The ebastine oral solution according to claim 1, characterized in that, Povidone is at least one of povidone K30 or povidone K12.

4. The ebastine oral solution according to claim 1, characterized in that, The sweetener includes at least one of sucrose, glucose, sorbitol, maltitol, mannitol, mogrosides, steviol glycosides, and sucralose.

5. The ebastine oral solution according to claim 1, characterized in that, The defoamer is a mixture of soybean oil and polyglycerol fatty acid esters.

6. The ebastine oral solution according to claim 5, characterized in that, The mass ratio of soybean oil to polyglycerol fatty acid ester is 5~8:

1.

7. The ebastine oral solution according to claim 1, characterized in that, It also includes 1 to 1.5% of a fragrance, which includes any one of strawberry flavoring, vanilla flavoring, peach flavoring, and cantaloupe flavoring.

8. The ebastine oral solution according to claim 1, characterized in that, It also includes 1-2% preservative, which is potassium sorbate.

9. The method for preparing the ebastine oral solution according to any one of claims 1 to 8, characterized in that, Weigh the above ingredients according to the proportions and mix them. Add a pH adjuster to adjust the pH of the solution to 4.5-5. After mixing evenly, you will get an ebastine oral solution.

10. The preparation method according to claim 9, characterized in that, The pH adjuster is one or more of phosphate buffer solution, acetate buffer solution, citric acid, and malic acid.