Silybin meglumine oral liquid and preparation method thereof

Abstract

The invention discloses a silybin meglumine oral liquid and a preparation method thereof. The method comprises the following steps: preparing silybin meglumine powder, a sweetening agent, an acidulant and purified water as raw materials; under the conditions that the stirring speed is 250 rpm and the water temperature is 25-30 DEG C, silybin meglumine powder is slowly scattered into the purified water to be stirred for 45 minutes until the silybin meglumine powder is completely dissolved; adding a sweetening agent and an acidulant, continuously stirring for 10 minutes, and then filtering through a 0.22 mu m microfiltration membrane to obtain a sterile and transparent solution; and subpackaging the solution into sterile oral liquid bottles, and sealing and packaging. The silybin meglumine oral liquid prepared by the method has the advantages of high dissolution efficiency, optimized taste, sterility, safety, stable quality and the like, is suitable for industrial large-scale production, and can remarkably improve the medication compliance of patients. The method is simple in process, easy to operate and low in cost, and has wide popularization and application values.

Description

Technical Field

[0001] The invention relates to the field of preparation of silybin meglumine, and more specifically to a silybin meglumine oral liquid and a preparation method thereof. Background Art

[0002] Silybin meglumine is a drug commonly used to protect liver function, which has good water solubility and pharmacological activity. However, most of the drugs with silybin meglumine as the main ingredient on the market are sold in the form of tablets and capsules. Although this dosage form has the advantages of good stability, easy storage and transportation, it has exposed some problems in actual application, especially when facing the elderly patient group.

[0003] First, middle-aged and elderly patients are the main users of silybin meglumine drugs. However, as they age, elderly patients generally have deteriorating swallowing functions, and often find it difficult to swallow solid preparations such as tablets and capsules, which may even cause aspiration or other adverse reactions. Secondly, the gastrointestinal function of elderly patients gradually declines, and the dissolution and absorption efficiency of tablets and capsules is relatively low, which may affect the efficacy of the drug. These problems have, to a certain extent, limited the clinical use of silybin meglumine drugs and the patients' medication compliance.

[0004] Therefore, developing a silybin meglumine oral solution and proposing a corresponding preparation method to solve the deficiencies of existing dosage forms has important practical significance and broad application prospects. Summary of the invention

[0005] In order to solve the problems existing in the prior art, the present invention provides a silybin meglumine oral solution, and the specific scheme is as follows:

[0006] A method for preparing silybin meglumine oral solution, the method comprising the following steps:

[0007] S1. Raw material preparation: prepare silybin methylglucamine, flavoring agent and purified water;

[0008] S2, dissolving: placing purified water in a stirring container, starting the stirrer, and setting the stirring speed to 200-300 rpm; slowly adding silybin meglumine powder, ensuring that it is evenly sprinkled into the purified water; continuing stirring for 30-60 minutes until the silybin meglumine is completely dissolved to form a uniform, transparent solution;

[0009] S3, adding flavoring agent: adding flavoring agent, the flavoring agent includes sweetener and acidulant; continuing stirring for 10 to 15 minutes to make the flavoring agent completely dissolved and evenly distributed in the solution;

[0010] S4, filtration treatment: the prepared solution is sterile filtered through a 0.22 μm microporous filter membrane to remove particles and other impurities;

[0011] S5. Filling and packaging: The filtered solution is dispensed into special oral liquid bottles under a sterile environment; after dispensing, the bottle mouth is immediately sealed with a sealing device to prevent contamination; each bottle of oral liquid is labeled and packaged, indicating the drug name, ingredients, dosage and storage conditions.

[0012] Furthermore, the mass volume ratio of silybin meglumine to purified water is 1:20.

[0013] Furthermore, the temperature of the S2 solution is controlled at 25-30°C.

[0014] Furthermore, the sweetener is one or a combination of erythritol, maltitol, aspartame or steviol glycosides; the added amount of the sweetener is 0.5-2%.

[0015] Furthermore, the acidulant is citric acid; the added amount of the acidulant is 0.1-0.3%.

[0016] Furthermore, the stirring time in S2 is 45 min.

[0017] Furthermore, the added amount of the sweetener is 1%.

[0018] Furthermore, the added amount of the sour agent is 0.2%.

[0019] The silybin meglumine oral solution is prepared by the above preparation method.

[0020] Beneficial effects:

[0021] The present invention provides a silybin meglumine oral solution and a preparation method thereof, which has the following beneficial effects:

[0022] (1) The present invention effectively avoids powder agglomeration by optimizing the stirring speed, controlling the water temperature at 25-30°C, and evenly sprinkling the powder. The present invention uses sweeteners such as maltitol, steviol glycosides, or erythritol to replace traditional sucrose, and adds citric acid as an acidulant to make the oral liquid have a fresh and palatable flavor. Sweeteners can not only effectively mask the bitterness and astringency of the drug, but also have the characteristics of low calories or zero calories, which are suitable for diabetic patients and groups that need to control blood sugar, and significantly improve the compliance of patients.

[0023] (2) Filtration through a 0.22μm microporous membrane combined with strict aseptic operation ensures that the preparation is free of particles and contamination, meeting the quality requirements of drugs. At the same time, the filling process uses aseptic packaging and aluminum foil sealing, which effectively improves the safety and stability of the product.

[0024] (3) The present invention simplifies the operation steps in the process design, reduces the production difficulty, and the process is suitable for large-scale industrial production. It has low preparation cost, high product quality, and has wide practical application value. BRIEF DESCRIPTION OF THE DRAWINGS

[0025] Figure 1 The invention discloses a flow chart of a method for preparing silybin meglumine oral solution. DETAILED DESCRIPTION

[0026] In order to deepen the understanding of the present invention, the present invention will be further described in detail below in conjunction with examples. The examples are only used to explain the present invention and do not constitute a limitation on the protection scope of the present invention.

[0027] Figure 1 The present invention is a flow chart of a method for preparing silybin meglumine oral solution, such as Figure 1 As shown, the process comprises the following steps: raw material preparation, dissolution, adding flavoring agents, filtering, filling and packaging.

[0028] Example:

[0029] Step S1: Raw material preparation

[0030] Prepare the following ingredients:

[0031] Silybin meglumine powder: weigh 5 g;

[0032] Sweetener: Weigh 1 gram of erythritol and 0.5 gram of maltitol, and use them in combination at a mass ratio of 2:1. The total amount of sweetener used is 1% of the mass of the solution.

[0033] Acidulant: Weigh 0.1 g of citric acid to ensure that the acidity is evenly adjusted.

[0034] Purified water: Accurately measure 100 ml. The water quality must meet the purified water standards specified in the Chinese Pharmacopoeia.

[0035] Step S2: Dissolution

[0036] Place purified water in a stainless steel stirring container, start the stirrer, and set the stirring speed to 250 rpm to ensure that the water flow is evenly distributed, which is conducive to powder dispersion.

[0037] The water temperature was controlled at 25-30°C (the water temperature measured in actual operation was 27°C) to optimize the dissolution rate and avoid the influence of excessive temperature on the stability of silybin meglumine.

[0038] Slowly sprinkle in the Silybin Meglumine powder, ensuring even dispersion and avoiding powder lumps.

[0039] Stirring was continued for 45 minutes until silybin meglumine was completely dissolved to form a uniform transparent solution. No insoluble particles were found in the solution and the transparency met the preparation requirements.

[0040] Step S3: Flavoring agent addition

[0041] Add sweetener and acidulant in the above proportions:

[0042] Add the combined sweetener of sucrose and maltitol first and sprinkle slowly into the solution.

[0043] Then, citric acid was added, and the amount of the acidulant was 0.2% of the total mass of the solution.

[0044] Stirring was continued for 10 minutes at a stirring speed of 250 rpm to ensure that the flavoring agent was evenly dissolved and distributed in the solution.

[0045] The final result is a basic solution with a balanced and refreshing taste, which ensures the palatability of the oral solution.

[0046] Step S4: Filtering

[0047] The solution was sterile filtered using a 0.22 μm microporous filter membrane and the operation was completed under sterile conditions.

[0048] The filtrate flow rate was controlled at 0.5 L / min to ensure thorough filtration, removal of all particles and impurities, and a clear, transparent solution.

[0049] Step S5: Filling and packaging

[0050] Transfer the filtered solution to a sterile filling device and fill it into special oral liquid bottles, with each bottle containing 10 ml.

[0051] After packaging, seal immediately with an aluminum foil sealer to prevent external contamination or oxidation.

[0052] Label the product according to the drug specification requirements, indicating the drug name, ingredients, dosage and storage conditions. The final product should be stored in a cool and dry place.

[0053] Effect analysis

[0054] ① High dissolution efficiency: By controlling the stirring speed to 250rpm and the solution temperature to 25-30℃, combined with the method of evenly sprinkling powder, powder agglomeration is effectively avoided, the dissolution of silybin meglumine is accelerated, and the operating efficiency and product quality are significantly improved.

[0055] ② Taste optimization: The sweetener and sour agent are matched in proportion to make the oral solution taste refreshing and non-greasy, which is easy for patients to accept and improves drug compliance. The sweetener dosage is 1% and the sour agent dosage is 0.2%. The precise ratio avoids taste imbalance.

[0056] ③ Sterility assurance: Use 0.22μm microporous filter membrane and strict aseptic operation to ensure the safety and stability of the preparation, avoid microbial contamination, and meet drug quality standards.

[0057] ④Easy to operate and high stability: Through precise raw material ratio and operating parameter control (such as stirring time of 45 minutes), the obtained product is transparent and uniform and has a long storage stability period.

[0058] As a further improvement, the above is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions, improvements, etc. made within the spirit and principles of the present invention should be included in the protection scope of the present invention.

Claims

1. A method for preparing silybin meglumine oral solution, characterized in that: The preparation method comprises the following steps: S1. Raw material preparation: prepare silybin methylglucamine, flavoring agent and purified water; S2, dissolving: placing purified water in a stirring container, starting the stirrer, and setting the stirring speed to 200-300 rpm; slowly adding silybin meglumine powder, ensuring that it is evenly sprinkled into the purified water; continuing stirring for 30-60 minutes until the silybin meglumine is completely dissolved to form a uniform, transparent solution; S3, adding flavoring agent: adding flavoring agent, the flavoring agent includes sweetener and acidulant; continuing stirring for 10 to 15 minutes to make the flavoring agent completely dissolved and evenly distributed in the solution; S4, filtration treatment: the prepared solution is sterile filtered through a 0.22 μm microporous filter membrane to remove particles and other impurities; S5. Filling and packaging: The filtered solution is dispensed into special oral liquid bottles under a sterile environment; after dispensing, the bottle mouth is immediately sealed with a sealing device to prevent contamination; each bottle of oral liquid is labeled and packaged, indicating the drug name, ingredients, dosage and storage conditions.

2. The method for preparing silybin meglumine oral solution according to claim 1, characterized in that: The mass volume ratio of silybin meglumine to purified water is 1:

20.

3. The method for preparing silybin meglumine oral solution according to claim 1, characterized in that: The temperature of S2 solution is controlled at 25-30°C.

4. The method for preparing silybin meglumine oral solution according to claim 1, characterized in that: The sweetener is one or a combination of erythritol, maltitol, aspartame or steviol glycoside; the added amount of the sweetener is 0.5-2%.

5. The method for preparing silybin meglumine oral solution according to claim 1, characterized in that: The acidulant is citric acid; the added amount of the acidulant is 0.1-0.3%.

6. The method for preparing silybin meglumine oral solution according to claim 1, characterized in that: The stirring time in S2 is 45 min.

7. The method for preparing silybin meglumine oral solution according to claim 4, characterized in that: The added amount of the sweetener is 1%.

8. The method for preparing silybin meglumine oral solution according to claim 5, characterized in that: The added amount of the sour agent is 0.2%.

9. Silybin meglumine oral solution prepared by the preparation method according to any one of claims 1 to 8.

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