Kaixin powder preparation and preparation method thereof

Abstract

The invention relates to the field of traditional Chinese medicine preparations, in particular to a Kaixin powder preparation and a preparation method. The invention provides a Kaixin powder preparation which comprises the following raw materials in parts by weight: a main drug: 800-1000 parts by weight of Kaixin powder; an auxiliary material: 4-5 parts by weight of a sweetening agent; and / or 16-20 parts by weight of an aromatic agent; and / or 32-40 parts by weight of a thickening agent; due to the fact that Kaixin powder mixed powder is slightly bitter and astringent in mouth, obvious in throat stabbing feeling after swallowing, lasting in throat stabbing feeling, poor in taste and low in patient medication compliance, the research finds that by adding a sweetening agent, an aromatic and a thickening agent, the main medicine prescription composition, the preparation method and the dosage form of classic famous formula Kaixin powder can be reserved, the overall taste of the preparation can be improved, and the preparation cost is reduced. Bad tastes such as bitter taste, pungent smell and throat pricking feeling of the medicine are covered, and the medication compliance of a patient is improved.

Description

Technical Field

[0001] The present invention relates to the field of traditional Chinese medicine preparations, and particularly relates to a Kāixīn Sǎn preparation and a preparation method thereof. Background Art

[0002] Kāixīn Sǎn (the 33rd formula in the first batch of ancient classic formulas) was first recorded in the "Essential Prescriptions for Emergencies Worth a Thousand Gold Pieces" by Sun Simiao, and is composed of four herbs: Poria cocos, Acorus tatarinowii, Ginseng, and Polygala tenuifolia, and is mainly used to treat "forgetfulness", and is a representative formula for tonifying qi to nourish the heart and calming the mind. Among them, Polygala tenuifolia is bitter and slightly pungent, and chewing it has a feeling of pricking the throat, resulting in the mixed powder of Kāixīn Sǎn being slightly bitter and astringent in the mouth, with an obvious pricking throat feeling after swallowing, and the pricking throat feeling is persistent, with a poor taste, and the compliance of patients taking the medicine is low.

[0003] In order to mask the bitter and astringent taste of the medicine and reduce the pricking throat feeling, the formation of taste is intervened through flavoring technology. Currently, the intervention is mainly achieved through the following several methods: ① interfering with the perception of bad taste by taste buds, such as adding sweeteners (aspartame, stevioside), umami substances (sodium glutamate); taste blockers (adenosine monophosphate) or taste paralyzants (menthol), etc.; ② reducing the direct contact between the medicine and taste buds through preparation means, such as coating, inclusion, solid dispersion, ion exchange, etc.; ③ modifying the molecular structure of the medicine, such as making prodrugs, enzyme treatment, etc.

[0004] In the actual flavoring process, flavoring is generally carried out by adopting the method of processing, such as using the method of processing with licorice to reduce the bad taste of the medicine; or, pretreating the medicinal materials to add other synergistic medicinal materials; or, obtaining the active ingredients through extraction and separation, and formulating with other medicinal excipients through a certain preparation process to obtain a new dosage form. However, using the above methods to flavor Kāixīn Sǎn requires changing the main drug prescription composition, preparation method, and dosage form of the classic formula Kāixīn Sǎn. Summary of the Invention

[0005] Therefore, the technical problem to be solved by the present invention is to overcome the defect in the prior art that flavoring Kāixīn Sǎn requires changing the main drug prescription composition, preparation method, and dosage form of the classic formula Kāixīn Sǎn, so as to provide a Kāixīn Sǎn preparation and a preparation method thereof. The Kāixīn Sǎn preparation and the preparation method can, on the basis of retaining the main drug prescription composition, preparation method, and dosage form of the classic formula Kāixīn Sǎn, mask the bitter and astringent taste of the medicine, especially Polygala tenuifolia, reduce the pricking throat feeling and other adverse reactions, thereby improving the overall taste of the preparation, increasing the palatability, and improving the compliance of patients taking the medicine.

[0006] For this purpose, the present invention provides the following technical solutions: An embodiment of the present invention provides a Kāixīn Sǎn preparation, including the following raw materials in parts by weight: Main drug: Kāixīn Sǎn, 800 - 1000 parts by weight; Excipients: sweetener, 4 - 5 parts by weight; and / or, flavoring agent, 16 - 60 parts by weight; and / or, thickening agent, 32 - 60 parts by weight.

[0007] In some embodiments, the sweetener is selected from at least one of aspartame, stevioside or mannitol; Optionally, the sweetener is aspartame.

[0008] In some embodiments, the flavoring agent is selected from at least one of wheat flavor essence, cocoa flavor essence, peanut flavor essence or red date flavor essence.

[0009] In some embodiments, the flavoring agent is wheat flavor essence and / or cocoa flavor essence; Optionally, the flavoring agent is wheat flavor essence, with a dosage of 16 - 20 parts by weight; Optionally, the flavoring agent is cocoa flavor essence, with a dosage of 48 - 60 parts by weight.

[0010] In some embodiments, the thickening agent is selected from at least one of xanthan gum, sorbitol or gelatin.

[0011] In some embodiments, the thickening agent is xanthan gum and / or sorbitol; Optionally, the thickening agent is xanthan gum, with a dosage of 32 - 40 parts by weight; Optionally, the thickening agent is sorbitol, with a dosage of 48 - 60 parts by weight.

[0012] In some embodiments, the raw materials of the Anshen Buxin Pills include raw materials in parts by weight: Poria cocos 320 - 400 parts by weight, Acorus tatarinowii 160 - 200 parts by weight, Ginseng 160 - 200 parts by weight, Polygala tenuifolia 160 - 200 parts by weight.

[0013] In some embodiments, the raw materials of the Anshen Buxin Pills include raw materials in parts by weight: The mass ratio of Poria cocos, Acorus tatarinowii, Ginseng, and Polygala tenuifolia is 2:1:1:1.

[0014] In some embodiments, the main drug is Anshen Buxin Pills powder; the Anshen Buxin Pills are obtained by mixing the raw materials after crushing them together or separately and then mixing; Optionally, the particle size of the Anshen Buxin Pills powder does not exceed 0.15 mm.

[0015] The embodiments of the present invention provide a preparation method of the Anshen Buxin Pills, which is characterized by weighing the raw materials according to the raw material formula and then mixing them.

[0016] The technical solution of the present invention has the following advantages: 1. A Kāixīn Sǎn preparation provided by the present invention comprises raw materials in the following parts by weight: main drug: Kāixīn Sǎn, 800 - 1000 parts by weight; auxiliary materials: sweetener, 4 - 5 parts by weight; and / or, flavoring agent, 16 - 60 parts by weight; and / or, thickening agent, 32 - 60 parts by weight. Since the mixed powder of Kāixīn Sǎn is slightly bitter and astringent in the mouth, has an obvious throat-irritating feeling after swallowing, and the throat-irritating feeling lasts for a long time, with poor taste, the compliance of patients taking the medicine is low. The present invention has found through research that by using a sweetener, a flavoring agent and a thickening agent in combination, the taste-improving effect can be enhanced. And when the Kāixīn Sǎn preparation is prepared by mixing with water, the thickening agent can increase the viscosity of the liquid, delay the release of bad taste molecules or block their contact with taste buds, thereby playing a role in masking bad taste. At the same time, the viscosity of xanthan gum solution will temporarily decrease under shear action (such as swallowing action), but the viscosity will quickly recover after the shear stops. This property can interfere with the continuity of taste perception and confuse the brain's judgment of bitterness through dynamic viscosity changes. In summary, the above Kāixīn Sǎn preparation can not only retain the main drug prescription composition, preparation method and dosage form of the classic famous prescription Kāixīn Sǎn, but also improve the overall taste of the preparation, cover up the bitter and astringent taste, pungent smell and throat-irritating feeling and other bad tastes of the drug, and improve the compliance of patients taking the medicine.

[0017] 2. A Kāixīn Sǎn preparation provided by the present invention, wherein the flavoring agent is wheat fragrance essence, and the dosage is 16 - 20 parts by weight. When the flavoring agent is selected as wheat fragrance essence, the dosage of the flavoring agent can be significantly reduced, the usage amount of auxiliary materials can be saved, and the cost can be significantly reduced.

[0018] 3. A Kāixīn Sǎn preparation provided by the present invention, wherein the thickening agent is xanthan gum, and the dosage is 32 - 40 parts by weight; when the thickening agent is selected as xanthan gum, the dosage of the thickening agent can be significantly reduced, the usage amount of auxiliary materials can be saved, and the cost can be significantly reduced. Detailed implementation manners

[0019] The following embodiments are provided to better further understand the present invention, which are not limited to the best implementation manner, and do not constitute a limitation to the content and protection scope of the present invention. Any product that is the same as or similar to the present invention obtained by anyone under the inspiration of the present invention or by combining the features of the present invention with other prior art features falls within the protection scope of the present invention.

[0020] For those not specifying specific experimental steps or conditions in the embodiments, the operations or conditions of the conventional experimental steps described in the literature in this field can be followed. For the reagents or instruments not specifying the manufacturer, they are all conventional reagent products that can be obtained through commercial purchase.

[0021] The aspartame in the following embodiments is purchased from Jiangsu Weiduo Co., Ltd.

[0022] The wheat fragrance essence is purchased from Yilun (Shanghai) Flavor & Fragrance Co., Ltd.

[0023] The cocoa essence was purchased from Yilun (Shanghai) Flavor & Fragrance Co., Ltd.

[0024] Stevioside was purchased from Shandong Aojing Biotechnology Co., Ltd.

[0025] Mannitol was purchased from Roquette France.

[0026] The strawberry essence was purchased from Yilun (Shanghai) Flavor & Fragrance Co., Ltd.

[0027] The peanut essence was purchased from Henan Wanbang Industrial Co., Ltd.

[0028] Sorbitol was purchased from Shijiazhuang Ruixue Pharmaceutical Co., Ltd.

[0029] Gelatin was purchased from Jiangxi Fumeitai Biotechnology Co., Ltd.

[0030] Xanthan gum was purchased from Hubei Gedian Humanwell Pharmaceutical Excipients Co., Ltd., xanthan gum GRINDSTED® XANTHAN80PRM was purchased from IFF Pharmaceutical Solutions, and xanthan gum GRINSTED XANTHAN 200PRM was purchased from IFF Pharmaceutical Solutions.

[0031] Example 1 This example provides a Kāixīn Sǎn preparation, the prescription of which consists of the following raw materials: Kāixīn Sǎn powder (the mass ratio of Poria cocos, Acorus tatarinowii, Panax ginseng, and Polygala tenuifolia is 2:1:1:1, and the powder particle size does not exceed 0.15 mm), 1000 g; Sweetener: Aspartame, 5 g; Fragrance: Wheat essence, 20 g; Thickener: Xanthan gum (xanthan gum GRINDSTED® XANTHAN 80PRM), 40 g.

[0032] Preparation method: Weigh the raw materials according to the prescription, and then mix them evenly to obtain the product.

[0033] Example 2 This example provides a Kāixīn Sǎn preparation, the prescription of which consists of the following raw materials: Kāixīn Sǎn powder (the mass ratio of Poria cocos, Acorus tatarinowii, Panax ginseng, and Polygala tenuifolia is 2:1:1:1, and the powder particle size does not exceed 0.15 mm), 1000 g; Sweetener: Aspartame, 5 g; Fragrance: Cocoa essence, 60 g; Thickener: Xanthan gum (xanthan gum GRINDSTED® XANTHAN 80PRM), 40 g.

[0034] Preparation method: Weigh the raw materials according to the prescription, and then mix them evenly to obtain the product.

[0035] Example 3 This example provides a Kāixīn Sǎn preparation, the prescription of which consists of the following raw materials: Kāixīn Sǎn powder (the mass ratio of Poria cocos, Acorus tatarinowii, Ginseng, and Polygala tenuifolia is 2:1:1:1, and the particle size of the powder does not exceed 0.15 mm), 1000 g; Sweetener: Aspartame, 4 g; Fragrance: Wheat fragrance essence, 16 g; Thickener: Xanthan gum (Xanthan gum GRINDSTED® XANTHAN 200PRM), 40 g.

[0036] Preparation method: Weigh the raw materials according to the prescription, and then mix them evenly to obtain the product.

[0037] Example 4 The difference between this example and Example 1 is that the sweetener is replaced with steviol glycoside in equal mass.

[0038] Example 5 The difference between this example and Example 1 is that the sweetener is replaced with mannitol in equal mass.

[0039] Example 6 The difference between this example and Example 1 is that the fragrance is replaced with red date essence in equal mass.

[0040] Example 7 The difference between this example and Example 1 is that the fragrance is replaced with peanut essence in equal mass.

[0041] Example 8 The difference between this example and Example 1 is that the thickener is replaced with sorbitol in equal mass, and the dosage is 60 g.

[0042] Example 9 The difference between this example and Example 1 is that the thickener is replaced with gelatin in equal mass.

[0043] Example 10 The difference between this example and Example 1 is that the thickener is replaced with domestic xanthan gum (purchased from Hubei Gedian Humanwell Pharmaceutical Excipients Co., Ltd.) in equal mass.

[0044] Comparative Example 1 Preparation by co-grinding process Take 2 portions of 10.0 g of Kāixīn Sǎn powder (from Example 1) and place them in a mortar. Add 0.20 g and 0.50 g of silicon dioxide (SYLOID) respectively, and manually grind for 30 min to obtain the product.

[0045] Comparative Example 2: Preparation by co-spray drying process Dissolve 8.0 g of hydroxypropyl methylcellulose powder in 400 mL of water to obtain a hydroxypropyl methylcellulose solution; uniformly disperse 100.0 g of Kaixin San powder in the hydroxypropyl methylcellulose solution, stir for 10 min, and then spray dry. The instrument parameters are: inlet air temperature 150℃, inlet air volume 35 m³ / min. 3 / h, atomization pressure 75 kPa, liquid inlet rate 9 mL / min, to obtain spray-dried powder 1. Take 100.0 g of Kaixin San powder and evenly disperse it in 400 mL of purified water, stir for 10 min, and then spray dry it with the same instrument parameters as above to obtain spray-dried powder 2. Calculate the powder yield using the following formula: ; Where m1 is the mass (g) of the powder obtained after spray drying, and m0 is the total amount of powder (g) before spray drying.

[0046] The yield of spray-dried powder 1 was 80.42%, and the yield of spray-dried powder 2 was 60.20%. Both spray-dried powders 1 and 2 had the following taste: slightly bitter and astringent upon entry, almost no irritating odor, and almost no throat irritation upon swallowing. This indicates that co-spraying effectively improves the throat irritation of the powder.

[0047] However, the high temperature and humidity conditions during the spray-drying process may cause the loss of active ingredients in Kaixin San, such as volatile oils. Following the method 2204B of General Chapter IV of the 2020 edition of the Pharmacopoeia of the People's Republic of China, the volatile oil content of the original Kaixin San powder and spray-dried powder 1 was determined by steam distillation. The results are as follows: the volatile oil content of the original Kaixin San powder was 0.2% (mL / g), and the volatile oil content of spray-dried powder 1 was 0%. Although the throat-irritating sensation of Kaixin San was improved after spray-drying, the volatile oil components in the powder were completely lost, therefore this method is not recommended.

[0048] Experimental Example The taste of Kaixin San preparation was evaluated manually, and the specific evaluation method is as follows: Eleven volunteers were selected to taste each Kaixin San preparation; eleven volunteers were selected for each Kaixin San preparation. The scoring criteria for the tasting evaluation method were as follows: Bitterness levels: 1 point - weak, 2 points - slightly weak, 3 points - medium, 4 points - strong, 5 points - very strong.

[0049] Corresponding throat irritation: 1 point - weak, 2 points - slightly weak, 3 points - moderate, 4 points - strong, 5 points - intense.

[0050] The scores for each indicator are the sum of the scores given by the 11 volunteers after tasting the food.

[0051] Evaluation of the sample: Take 3.075g of the sample and add it to 60mL of drinking water at room temperature, and stir well.

[0052] The evaluation results are shown in the table below: Table 1. Evaluation Results

[0053] As shown in the table above, the bitterness and throat irritation scores of Examples 1-3 are low, indicating that the excipients in both Kaixin San preparations can effectively mask the bitterness and throat irritation, improving patient compliance. Further comparison of the aromatics in Examples 1 and 2 shows that the amount of aromatics used in Example 1 is only 33.3% of that in Example 2, significantly reducing the amount of excipients used. The bitterness and throat irritation scores of Examples 4-5 are higher than those of Example 1, indicating that the sweetener in Example 1 works better with other excipients to mask the bitterness and throat irritation. The bitterness and throat irritation scores of Examples 6-7 are higher than those of Example 1, indicating that the aromatics in Example 1 work better with other excipients to mask the bitterness and throat irritation. The bitterness and throat irritation scores of Examples 8-10 are higher than those of Example 1, indicating that the thickener in Example 1 works better with other excipients to mask the bitterness and throat irritation. The bitterness and throat irritation scores of Examples 1-10 were significantly lower than those of Comparative Example 1, indicating that the excipients in the Kaixin San preparations of both examples can better mask the bitterness and throat irritation, thereby improving patient compliance.

[0054] Obviously, the above embodiments are merely illustrative examples for clear explanation and are not intended to limit the implementation. Those skilled in the art will recognize that other variations or modifications can be made based on the above description. It is neither necessary nor possible to exhaustively list all possible implementations here. However, obvious variations or modifications derived therefrom are still within the scope of protection of this invention.

Claims

1. A Kaixin San (a traditional Chinese medicine formula), characterized in that, Including the following parts by weight of raw materials: Main ingredient: Kaixin San (a traditional Chinese medicine), 800-1000 parts by weight; Excipients: sweetener, 4-5 parts by weight; and / or flavoring agent, 16-60 parts by weight; and / or thickener, 32-60 parts by weight.

2. The Kaixin San preparation according to claim 1, characterized in that, The sweetener is selected from at least one of aspartame, steviol glycosides or mannitol; Optionally, the sweetener is aspartame.

3. The Kaixin San preparation according to any one of claims 1-2, characterized in that, The flavoring agent is selected from at least one of wheat flavoring, cocoa flavoring, peanut flavoring, or jujube flavoring.

4. The Kaixin San preparation according to claim 3, characterized in that, The flavoring agent is wheat flavoring and / or cocoa flavoring; Optionally, the fragrance is wheat flavoring, and the amount used is 16-20 parts by weight; Optionally, the flavoring agent is cocoa flavoring, used in an amount of 48-60 parts by weight.

5. The Kaixin San preparation according to any one of claims 1-4, characterized in that, The thickener is selected from at least one of xanthan gum, sorbitol, or gelatin.

6. The Kaixin San preparation according to claim 5, characterized in that, The thickener is xanthan gum and / or sorbitol; Optionally, the thickener is xanthan gum, and the dosage is 32-40 parts by weight; Optionally, the thickener is sorbitol, used in an amount of 48-60 parts by weight.

7. The Kaixin San preparation according to any one of claims 1-6, characterized in that, The raw materials of the Kaixin San include the following components by weight: Poria cocos 320-400 parts by weight, Acorus tatarinowii 160-200 parts by weight, Ginseng 160-200 parts by weight, Polygala tenuifolia 160-200 parts by weight.

8. The Kaixin San preparation according to claim 7, characterized in that, The raw materials of the Kaixin San include the following components by weight: The mass ratio of Poria cocos, Acorus tatarinowii, ginseng, and Polygala tenuifolia is 2:1:1:

1.

9. The Kaixin San preparation according to any one of claims 1-8, characterized in that, The main ingredient is Kaixin San powder; Kaixin San is obtained by mixing and pulverizing the raw materials or by pulverizing the raw materials separately and then mixing them. Optionally, the particle size of the Kaixin powder is no more than 0.15 mm.

10. A method for preparing the Kāixīn Sǎn preparation according to any one of claims 1-9, characterized in that, Weigh the raw materials according to the formula, and then mix them.

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