Preparation method of ebastine oral solution

Abstract

The invention discloses an ebastine oral solution preparation method, which comprises: 1, weighing 5-20 parts by mass of ebastine, 50-100 parts by mass of a thickening agent, 10-18 parts by mass of a bacteriostatic agent, 1800-2000 parts by mass of a thickening agent, 0.1-0.2 part by mass of a defoaming agent, 600-700 parts by mass of a sweetening agent, adjusting the pH value to 3.5-4.5 by using a pH value adjusting agent, and carrying out a proper amount of water; 2, adjusting the temperature to 35 DEG C, adding ebastine into the thickening agent, and stirring to completely disperse the ebastine; 3, adding part of purified water, an acidity regulator and a thickening agent, and stirring until the materials are completely dissolved; 4, adding the sweetening agent, the bacteriostatic agent and the defoaming agent, and stirring until the materials are completely dissolved; 5, cooling after complete dissolution, and adjusting the pH value to 4 by using an alkaline regulator; step 6, fixing the volume; by optimizing the preparation process, efficient dissolution of the ebastine oral solution is realized, the problems of clinical application pain points of tablets and low solubility of raw material medicines of the oral solution are solved, and a safer and more convenient treatment choice is provided for special crowds.

Description

Technical Field

[0001] The present invention relates to the technical field of preparation of ebastine oral solution, in particular to a preparation method of ebastine oral solution. Background Art

[0002] Ebastine is a potent, highly selective, and specific H1 receptor blocker. The original Ebastine oral solution was first launched in Spain in 1989. It is primarily indicated for the symptomatic treatment of allergic rhinitis (seasonal and perennial) with or without allergic conjunctivitis and chronic idiopathic urticaria.

[0003] Ebastine is a BCS Class II (low solubility, high permeability) drug. Due to its low solubility, tablets are currently the primary marketed dosage form for ebastine. However, tablets have drawbacks such as poor patient compliance, slow onset of action, and complex manufacturing processes. To address the shortcomings of existing technologies, a precise, easy-to-take oral solution for ebastine needs to be developed. However, the formulation process for commercially available ebastine oral solutions has a long dissolution time, often exceeding 4 hours, making preparation challenging. Summary of the Invention

[0004] The purpose of the present invention is to provide a method for preparing ebastine oral solution. By optimizing the preparation process, efficient dissolution of ebastine oral solution is achieved, solving the pain points of clinical application of tablets and the low solubility of oral solution raw materials, providing a safer and more convenient treatment option for special populations.

[0005] To achieve the above object, the present invention provides the following technical solution: a method for preparing ebastine oral solution, comprising the following steps:

[0006] Step 1: Weigh 5-20 parts of ebastine, 50-100 parts of thickener, 10-18 parts of antibacterial agent, 1800-2000 parts of thickener, 0.1-0.2 parts of defoaming agent, 600-700 parts of sweetener, pH regulator to adjust the pH value to 3.5-4.5, and water in appropriate amounts;

[0007] Step 2: Adjust the temperature to 35°C, add Ebastine to the thickener and stir until it is completely dispersed;

[0008] Step 3: Add some purified water, acidity regulator, and thickener, and stir until completely dissolved;

[0009] Step 4: Add sweetener, antibacterial agent, and defoamer and stir until completely dissolved;

[0010] Step 5: After the solution is completely dissolved, cool it down and adjust the pH to 4 using an alkaline regulator.

[0011] Step 6: Adjust the volume.

[0012] Preferably, in step 1, 10 parts of ebastine, 100 parts of thickener, 15 parts of antibacterial agent, 2000 parts of thickener, 0.2 parts of defoaming agent, 700 parts of sweetener, pH regulator to adjust the pH value to 4, and an appropriate amount of water are weighed in parts by mass.

[0013] Preferably, the thickener is one or both of polyoxyethylene 40 hydrogenated castor oil and Tween 80.

[0014] Preferably, the antibacterial agent is one or more of sodium methylparaben, sodium propylparaben, benzoic acid, and sodium benzoate.

[0015] Preferably, the thickener is one or both of propylene glycol and glycerol.

[0016] Preferably, the defoaming agent is dimethicone, and the sweetener is one or more of saccharin sodium, sucralose, xylitol, and sorbitol.

[0017] Preferably, the pH adjuster is one or more of citric acid, sodium citrate, lactic acid, hydrochloric acid, and sodium hydroxide.

[0018] Compared with the prior art, the present invention has the following beneficial effects:

[0019] The present invention achieves efficient dissolution of ebastine oral solution by optimizing the preparation process, solves the pain points of clinical application of tablets and the problem of low solubility of oral solution raw materials, and provides a safer and more convenient treatment option for special populations. DETAILED DESCRIPTION

[0020] The following will be combined with the embodiments of the present invention to clearly and completely describe the technical solutions in the embodiments of the present invention. Obviously, the embodiments described are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative efforts are within the scope of protection of the present invention.

[0021] The present invention provides a method for preparing ebastine oral solution, comprising the following steps:

[0022] Step 1: Weigh 5-20 parts of ebastine, 50-100 parts of thickener, 10-18 parts of antibacterial agent, 1800-2000 parts of thickener, 0.1-0.2 parts of defoaming agent, 600-700 parts of sweetener, pH regulator to adjust the pH value to 3.5-4.5, and water in appropriate amounts;

[0023] Step 2: Adjust the temperature to 35°C, add Ebastine to the thickener and stir until it is completely dispersed;

[0024] Step 3: Add some purified water, acidity regulator, and thickener, and stir until completely dissolved;

[0025] Step 4: Add sweetener, antibacterial agent, and defoamer and stir until completely dissolved;

[0026] Step 5: After the solution is completely dissolved, cool it down and adjust the pH to 4 using an alkaline regulator.

[0027] Step 6: Adjust the volume.

[0028] The thickener is one or both of polyoxyethylene 40 hydrogenated castor oil and Tween 80.

[0029] The antibacterial agent is one or more of sodium methylparaben, sodium propylparaben, benzoic acid and sodium benzoate.

[0030] The thickener is one or both of propylene glycol and glycerin.

[0031] The defoaming agent is preferably dimethicone, and the sweetener is one or more of saccharin sodium, sucralose, xylitol, and sorbitol.

[0032] The pH regulator is one or more of citric acid, sodium citrate, lactic acid, hydrochloric acid, and sodium hydroxide.

[0033] Example 1:

[0034] A method for preparing ebastine oral solution comprises the following steps:

[0035] Step 1: Prepare ingredients according to 1L of ebastine oral solution as 1 batch: 1g of ebastine, 1.2g of sodium methylparaben, 0.3g of sodium propylparaben, 200g of glycerin, 0.02g of dimethicone, 2g of sucralose, 68g of sorbitol, 9g of lactic acid, sodium hydroxide to adjust the pH to 4, 10g of polyoxyethylene 40 hydrogenated castor oil, and 1g of cantaloupe essence. Add purified water to the remainder to 1L;

[0036] Step 2: Adjust the temperature to 35°C, add Ebastine to polyoxyethylene 40 hydrogenated castor oil and stir until it is completely dispersed;

[0037] Step 3: Add 60% of the total amount of purified water, lactic acid, and glycerol and stir until completely dissolved;

[0038] Step 4: Add sorbitol, sucralose, sodium methylparaben, sodium propylparaben, and dimethicone and stir until completely dissolved;

[0039] Step 5: After the solution is completely dissolved, cool it down and adjust the pH to 4 using sodium hydroxide;

[0040] Step 6: Adjust the volume to the total amount.

[0041] The ebastine oral solution prepared by this process is clear and transparent, and the production process only takes about 1 hour, which greatly improves the production efficiency of the ebastine oral solution.

[0042] Ebastine only takes 10 minutes to disperse and dissolves quickly in an acidic aqueous solution, with the entire preparation process taking only about an hour. This significantly reduces the time it takes to dissolve Ebastine and the risk of drug content.

[0043] Example 2:

[0044] A method for preparing ebastine oral solution comprises the following steps:

[0045] Step 1: Prepare ingredients for 1 L of ebastine oral solution: 1.5 g of ebastine, 1.6 g of sodium benzoate, 180 g of propylene glycol, 0.01 g of dimethicone, 65 g of sodium saccharin, 9 g of hydrochloric acid, citric acid to adjust the pH to 4, 8 g of Tween, and 1 g of cantaloupe essence. Add the remainder of the mixture to 1 L with purified water.

[0046] Step 2: Adjust the temperature to 35°C, add Ebastine to Tween and stir to fully disperse;

[0047] Step 3: Add 60% of the total amount of purified water, hydrochloric acid, and propylene glycol and stir until completely dissolved;

[0048] Step 4: Add sodium benzoate, sodium saccharin, and dimethicone and stir until completely dissolved;

[0049] Step 5: After the solution is completely dissolved, cool it down and adjust the pH to 4 using sodium hydroxide;

[0050] Step 6: Adjust the volume to the total amount.

[0051] In summary, through the specific operating steps of Example 1 and Example 2, the feasibility and efficiency of the method for preparing the oral solution of ebastine provided by the present invention can be clearly seen. In Example 1, polyoxyethylene 40 hydrogenated castor oil was used as a thickener, glycerin was used as a thickener, dimethicone was used as a defoaming agent, sucralose and sorbitol were used as sweeteners, lactic acid and sodium hydroxide were used as pH regulators, and sodium methylparaben and sodium propylparaben were used as antibacterial agents to successfully prepare a clear and transparent oral solution of ebastine. In Example 2, Tween was used as a thickener, propylene glycol was used as a thickener, sodium saccharin was used as a sweetener, hydrochloric acid and citric acid were used as pH regulators, and sodium benzoate was used as an antibacterial agent to prepare an oral solution of ebastine that met the requirements. Both examples demonstrate that the method provided by the present invention can effectively improve the dissolution efficiency of ebastine, reduce the content risk in the production process, and provide a safer and more convenient treatment option for special populations.

[0052] Although the present invention has been described in detail with reference to the aforementioned embodiments, it is still possible for those skilled in the art to modify the technical solutions described in the aforementioned embodiments, or to make equivalent substitutions for some of the technical features therein. Any modifications, equivalent substitutions, improvements, etc. made within the spirit and principles of the present invention should be included in the scope of protection of the present invention.

Claims

1. A method for preparing ebastine oral solution, characterized in that: The following steps are involved: Step 1: Weigh 5-20 parts of ebastine, 50-100 parts of thickener, 10-18 parts of antibacterial agent, 1800-2000 parts of thickener, 0.1-0.2 parts of defoaming agent, 600-700 parts of sweetener, pH regulator to adjust the pH value to 3.5-4.5, and water in appropriate amounts; Step 2: Adjust the temperature to 35°C, add Ebastine to the thickener and stir until it is completely dispersed; Step 3: Add some purified water, acidity regulator, and thickener, and stir until completely dissolved; Step 4: Add sweetener, antibacterial agent, and defoamer and stir until completely dissolved; Step 5: After the solution is completely dissolved, cool it down and adjust the pH to 4 using an alkaline regulator. Step 6: Adjust the volume.

2. The method for preparing an ebastine oral solution according to claim 1, wherein: Preferably, in step 1, 10 parts of ebastine, 100 parts of thickener, 15 parts of antibacterial agent, 2000 parts of thickener, 0.2 parts of defoaming agent, 700 parts of sweetener, pH regulator to adjust the pH value to 4, and an appropriate amount of water are weighed in parts by mass.

3. The method for preparing an ebastine oral solution according to claim 1, wherein: The thickener is one or both of polyoxyethylene 40 hydrogenated castor oil and Tween 80.

4. The method for preparing an ebastine oral solution according to claim 1, wherein: The antibacterial agent is one or more of sodium methylparaben, sodium propylparaben, benzoic acid and sodium benzoate.

5. The method for preparing an ebastine oral solution according to claim 1, wherein: The thickener is one or both of propylene glycol and glycerol.

6. The method for preparing an ebastine oral solution according to claim 1, wherein: The defoaming agent is preferably dimethicone, and the sweetener is one or more of saccharin sodium, sucralose, xylitol, and sorbitol.

7. The method for preparing an ebastine oral solution according to claim 1, wherein: The pH regulator is one or more of citric acid, sodium citrate, lactic acid, hydrochloric acid, and sodium hydroxide.