Exocarpium citri grandis effervescent tablet and preparation method thereof

Abstract

The present application relates to effervescent tablet preparation technical field, specifically disclose a kind of fructus aurantii immaturi effervescent tablet and its preparation method.The fructus aurantii immaturi effervescent tablet contains the following weight parts of raw material component: fructus aurantii immaturi freeze-dried powder 4~8 parts;Acid source 50~70 parts;Alkali source 50~70 parts;Sweetener 20~40 parts;Additive 1~3 parts.The preparation method of the fructus aurantii immaturi effervescent tablet contains the following steps: in raw material, 1 / 2 dosage of sweetener, 1 / 2 dosage of fructus aurantii immaturi freeze-dried powder and acid source are sequentially taken, mixed and then uniformly, then granulated by anhydrous ethanol to obtain acidic granules;In raw material, 1 / 2 dosage of sweetener, 1 / 2 dosage of fructus aurantii immaturi freeze-dried powder and alkali source are sequentially taken, mixed and then uniformly, then granulated by anhydrous ethanol to obtain basic granules;Additive is melted, then mixed uniformly with acidic granules and basic granules to be compressed into tablets, i.e.the fructus aurantii immaturi effervescent tablet.The effervescent tablet fructus aurantii immaturi effervescent tablet of the present application disintegrates rapidly, and has good effervescent effect.

Description

TECHNICAL FIELD

[0001] The present application relates to effervescent tablet preparation technical field, specifically relates to a fructus aurantii immaturi effervescent tablet and a preparation method thereof. BACKGROUND

[0002] Fructus aurantii immaturus, also known as Maojuhong, Huazhouchenpi, and orange peel, is the dried outer pericarp of immature or nearly mature fruit of Citrus grandis (L.) Osbeck; it is a very common local Guangdong traditional Chinese medicine, according to the Pharmacopoeia, it has the effects of regulating qi, broadening the middle, drying dampness, and resolving phlegm, and is commonly used for cough with much phlegm, food accumulation and injury by alcohol, and vomiting with distention. Traditional Chinese medicine is known as "natural medicine", "green medicine", etc., and plays a significant role in preventing and treating diseases, and is increasingly attracting the attention of scholars.

[0003] Effervescent tablets are a new dosage form that is convenient to take and has rapid effect, which are prepared by using organic acid and basic carbonate (hydrogen) salt as effervescent disintegrants, and then placed in water to generate and release a large amount of carbon dioxide gas immediately, which is like boiling, hence the name effervescent tablets.

[0004] Therefore, it has important application value to provide an effervescent tablet of fructus aurantii immaturus by using fructus aurantii immaturus as a raw material. SUMMARY

[0005] In order to overcome at least one of the technical problems in the prior art, the present application provides a preparation method of rape bee pollen enzyme.

[0006] The above technical problems to be solved by the present application are solved by the following technical solutions:

[0007] An effervescent tablet of fructus aurantii immaturus comprises the following raw material components by weight:

[0008] Fructus aurantii immaturus freeze-dried powder 4-8 parts; acid source 50-70 parts; base source 50-70 parts; sweetening agent 20-40 parts; additive 1-3 parts.

[0009] The present application provides a fructus aurantii immaturus effervescent tablet with a completely new composition, which has rapid disintegration and good effervescence effect.

[0010] Preferably, the fructus aurantii immaturus effervescent tablet comprises the following raw material components by weight:

[0011] Fructus aurantii immaturus freeze-dried powder 4-6 parts; acid source 55-65 parts; base source 55-65 parts; sweetening agent 30-35 parts; additive 1-2 parts.

[0012] Most preferably, the fructus aurantii immaturus effervescent tablet comprises the following raw material components by weight:

[0013] Wuweizi freeze-dried powder 5 parts; acid source 60 parts; base source 60 parts; sweetener 34 parts; additive 1 part;

[0014] Preferably, the acid source is citric acid.

[0015] Preferably, the base source is sodium bicarbonate.

[0016] Preferably, the sweetener is selected from erythritol; or the sweetener is selected from a combination of erythritol and white granulated sugar.

[0017] Preferably, the additive is PEG.

[0018] Preferably, the wuweizi freeze-dried powder is prepared by the following method:

[0019] Take wuweizi, then use solvent to heat reflux extraction, after the end of extraction, the extract liquid is concentrated and freeze-dried to obtain the wuweizi freeze-dried powder.

[0020] Further preferably, the solvent is selected from water or a 10% to 50% volume fraction of ethanol aqueous solution.

[0021] More preferably, the solvent is a mixed solvent consisting of a 10% to 50% volume fraction of ethanol aqueous solution and 1,3-propanediol.

[0022] Most preferably, the solvent is a mixed solvent consisting of a 40% volume fraction of ethanol aqueous solution and 1,3-propanediol.

[0023] Preferably, the weight amount of the solvent is 5 to 15 times the weight of wuweizi.

[0024] Most preferably, the weight amount of the solvent is 10 times the weight of wuweizi.

[0025] Preferably, the volume ratio of the 10% to 50% volume fraction of ethanol aqueous solution and 1,3-propanediol is 4 to 6:1.

[0026] Most preferably, the volume ratio of the 40% volume fraction of ethanol aqueous solution and 1,3-propanediol is 5:1.

[0027] The inventors surprisingly found in the research that the preparation method of wuweizi freeze-dried powder plays a decisive role in whether a large amount of foam will be generated after the effervescent reaction of the prepared wuweizi effervescent tablets and the dissipation time of the foam.

[0028] The inventors found in a large number of studies that the addition of the freeze-dried powder of Citrus aurantium L. prepared by using water or a 10% to 50% ethanol aqueous solution to the Citrus aurantium L. effervescent tablets can produce a large amount of foam after the effervescent reaction of the Citrus aurantium L. effervescent tablets, and the dissipation time of the foam is long. In order to solve this problem, the inventors surprisingly found in the research that the addition of the freeze-dried powder of Citrus aurantium L. prepared by using a mixed solvent composed of a 10% to 50% ethanol aqueous solution and 1,3-propanediol to the Citrus aurantium L. effervescent tablets can significantly reduce the amount of foam produced after the effervescent reaction of the Citrus aurantium L. effervescent tablets, and can also significantly shorten the dissipation time of the foam.

[0029] Further preferably, the freeze-dried powder of Citrus aurantium L. is prepared by the following method:

[0030] (1) Citrus aurantium L. is taken, and then extracted by heating reflux using a solvent. After the extraction is completed, the Citrus aurantium L. extract liquid is concentrated and dried to obtain a Citrus aurantium L. extract;

[0031] (2) The Citrus aurantium L. extract is subjected to macroporous resin column, and then eluted with a 30% to 35% ethanol aqueous solution to obtain an eluate. The eluate is concentrated and freeze-dried to obtain the freeze-dried powder of Citrus aurantium L.

[0032] The inventors further surprisingly found in the research that the freeze-dried powder of Citrus aurantium L. prepared by further extracting Citrus aurantium L. using a mixed solvent composed of a 10% to 50% ethanol aqueous solution and 1,3-propanediol and then subjecting the extract to the above-mentioned macroporous resin elution conditions can further significantly reduce the amount of foam produced after the effervescent reaction of the Citrus aurantium L. effervescent tablets, and can also further significantly shorten the dissipation time of the foam.

[0033] Here, the inventors need to point out that the elution conditions of the macroporous resin are very critical. Only the freeze-dried powder of Citrus aurantium L. prepared by further extracting Citrus aurantium L. using a mixed solvent composed of a 10% to 50% ethanol aqueous solution and 1,3-propanediol and then subjecting the extract to the above-mentioned macroporous resin elution conditions can further significantly reduce the amount of foam produced after the effervescent reaction of the Citrus aurantium L. effervescent tablets, and can also further significantly shorten the dissipation time of the foam. The freeze-dried powder of Citrus aurantium L. prepared by using other macroporous resin elution conditions cannot further significantly reduce the amount of foam produced after the effervescent reaction of the Citrus aurantium L. effervescent tablets, and cannot further significantly shorten the dissipation time of the foam.

[0034] Preferably, the solvent in step (1) is a mixed solvent composed of a 10% to 50% ethanol aqueous solution and 1,3-propanediol.

[0035] Preferably, the volume ratio of the 10% to 50% ethanol aqueous solution and 1,3-propanediol is 4 to 6:1.

[0036] Most preferably, the volume ratio of 40% ethanol aqueous solution and 1,3-propanediol is 5:1.

[0037] Preferably, the weight amount of the solvent is 5-15 times of the weight of Fructus aurantii.

[0038] Most preferably, the weight amount of the solvent is 10 times of the weight of Fructus aurantii.

[0039] The application also provides a preparation method of the effervescent tablet of Fructus aurantii, which comprises the following steps:

[0040] Preparation of the acidic granules: in the raw materials, 1 / 2 amount of the sweetening agent, 1 / 2 amount of the freeze-dried powder of Fructus aurantii and 1 / 2 amount of the acid source are sequentially taken, mixed, uniformly mixed, then granulated by using anhydrous ethanol to obtain the acidic granules.

[0041] Preparation of the basic granules: in the raw materials, 1 / 2 amount of the sweetening agent, 1 / 2 amount of the freeze-dried powder of Fructus aurantii and 1 / 2 amount of the alkali source are sequentially taken, mixed, uniformly mixed, then granulated by using anhydrous ethanol to obtain the basic granules.

[0042] Mixing and tabletting step: the additives are melted, then mixed with the acidic granules and the basic granules to obtain the effervescent tablet of Fructus aurantii.

[0043] Beneficial effects: the application provides a brand new effervescent tablet of Fructus aurantii; the effervescent tablet of Fructus aurantii provided by the application has rapid disintegration and good effervescent effect. DETAILED DESCRIPTION

[0044] The application will be further explained in combination with specific examples, but the examples do not limit the application in any form.

[0045] Example 1: preparation of the effervescent tablet of Fructus aurantii

[0046] The raw material of the effervescent tablet of Fructus aurantii comprises: 5 parts of the freeze-dried powder of Fructus aurantii, 60 parts of citric acid, 60 parts of sodium bicarbonate, 30 parts of erythritol, 4 parts of white sugar and 1 part of PEG6000.

[0047] The freeze-dried powder of Fructus aurantii is prepared by the following method:

[0048] The freeze-dried powder of Fructus aurantii is prepared by the following method:

[0049] Preparation method of the effervescent tablet of Fructus aurantii:

[0050] (1) Preparation of acidic granules: 15 parts of erythritol, 2.5 parts of dried Wampee powder, 60 parts of citric acid and 2 parts of white sugar were taken in sequence, mixed and made uniform, and then granulated with anhydrous ethanol to obtain the acidic granules;

[0051] (2) Preparation of basic granules: 15 parts of erythritol, 2.5 parts of dried Wampee powder, 60 parts of sodium bicarbonate and 2 parts of white sugar were taken in sequence, mixed and made uniform, and then granulated with anhydrous ethanol to obtain the basic granules;

[0052] Mixing and tabletting step: 1 part of additive was melted, then mixed with the acidic granules and the basic granules prepared in steps (1) and (2) to make uniform, and then tabletted to obtain the Wampee effervescent tablet.

[0053] Preparation of Wampee effervescent tablet in Example 2

[0054] The raw material weight composition and preparation method of the Wampee effervescent tablet are the same as in Example 1; the difference is in the preparation method of the dried Wampee powder;

[0055] The dried Wampee powder in Example 2 is prepared by the following method:

[0056] The dried Wampee powder is obtained by taking Wampee, heating and refluxing with 10 times the weight of 40% ethanol aqueous solution at 78°C for 2h, concentrating and freeze-drying the extract.

[0057] Preparation of Wampee effervescent tablet in Example 3

[0058] The raw material weight composition and preparation method of the Wampee effervescent tablet are the same as in Example 1; the difference is in the preparation method of the dried Wampee powder;

[0059] The dried Wampee powder in Example 3 is prepared by the following method:

[0060] The dried Wampee powder is obtained by taking Wampee, heating and refluxing with 10 times the weight of a mixed solvent at 78°C for 2h, concentrating and freeze-drying the extract;

[0061] The mixed solvent refers to a mixed solvent composed of 40% ethanol aqueous solution and 1,3-propanediol in a volume ratio of 5:1.

[0062] Preparation of Wampee effervescent tablet in Example 4

[0063] The raw material weight composition and preparation method of the Wampee effervescent tablet are the same as in Example 1; the difference is in the preparation method of the dried Wampee powder;

[0064] The Citrus grandis (L.) Osbeck freeze-dried powder described in Example 4 is prepared by the following method:

[0065] (1) Citrus grandis (L.) Osbeck is taken, and then heated and refluxed with 10 times the weight of a mixed solvent at 78°C for 2 h. After the extraction is completed, Citrus grandis (L.) Osbeck extract liquid is obtained. The Citrus grandis (L.) Osbeck extract liquid is concentrated and dried to obtain Citrus grandis (L.) Osbeck extract. The mixed solvent refers to a mixed solvent composed of 40% ethanol aqueous solution and 1,3-propanediol in a volume ratio of 5:1.

[0066] (2) The Citrus grandis (L.) Osbeck extract is loaded onto a D101 macroporous resin column, and then eluted with 5 times the column volume of 33% ethanol aqueous solution to obtain an eluate. The eluate is concentrated and freeze-dried to obtain the Citrus grandis (L.) Osbeck freeze-dried powder.

[0067] Preparation of Citrus grandis (L.) Osbeck effervescent tablets in Comparative Example 1

[0068] The raw material weight composition and preparation method of the Citrus grandis (L.) Osbeck effervescent tablets are the same as in Example 4. The difference is that the elution conditions of the macroporous resin in the preparation method of the Citrus grandis (L.) Osbeck freeze-dried powder are different.

[0069] The Citrus grandis (L.) Osbeck freeze-dried powder described in Comparative Example 1 is prepared by the following method:

[0070] (1) Citrus grandis (L.) Osbeck is taken, and then heated and refluxed with 10 times the weight of a mixed solvent at 78°C for 2 h. After the extraction is completed, Citrus grandis (L.) Osbeck extract liquid is obtained. The Citrus grandis (L.) Osbeck extract liquid is concentrated and dried to obtain Citrus grandis (L.) Osbeck extract. The mixed solvent refers to a mixed solvent composed of 40% ethanol aqueous solution and 1,3-propanediol in a volume ratio of 5:1.

[0071] (2) The Citrus grandis (L.) Osbeck extract is loaded onto a D101 macroporous resin column, and then eluted with 5 times the column volume of 33% ethanol aqueous solution to obtain an eluate. The eluate is concentrated and freeze-dried to obtain the Citrus grandis (L.) Osbeck freeze-dried powder.

[0072] Preparation of Citrus grandis (L.) Osbeck effervescent tablets in Comparative Example 2

[0073] The raw material weight composition and preparation method of the Citrus grandis (L.) Osbeck effervescent tablets are the same as in Example 4. The difference is that the elution conditions of the macroporous resin in the preparation method of the Citrus grandis (L.) Osbeck freeze-dried powder are different.

[0074] The Citrus grandis (L.) Osbeck freeze-dried powder described in Comparative Example 2 is prepared by the following method:

[0075] (1) taking the Citrus aurantium fruit and then extracting at 78°C for 2 hours by heating reflux with 10 times the weight of a mixed solvent to obtain a Citrus aurantium fruit extract liquid, and then concentrating and drying the Citrus aurantium fruit extract liquid to obtain a Citrus aurantium fruit extract; the mixed solvent refers to a mixed solvent composed of 40% ethanol aqueous solution and 1,3-propanediol in a volume ratio of 5:1;

[0076] (2) loading the Citrus aurantium fruit extract onto a D101 macroporous resin column, and then eluting with 5 times the column volume of 20% ethanol aqueous solution to obtain an eluate, and then concentrating and freeze-drying the eluate to obtain the freeze-dried Citrus aurantium fruit powder.

[0077] The Citrus aurantium fruit effervescent tablets prepared in Examples 1-4 and Comparative Examples 1-2 were respectively placed in 200 ml of water for effervescent reaction, and the disintegration time, foam production amount and foam dissipation time were recorded; the results are shown in Table 1.

[0078] Table 1. Results of effervescent experiment of Citrus aurantium fruit effervescent tablets of the present application

[0079] Disintegration time Foam volume Foam dissipation time Citrus aurantium effervescent tablets prepared in Example 1 125 seconds Very much 210 seconds Citrus aurantium effervescent tablets prepared in Example 2 120 seconds Very much 203 seconds Citrus aurantium effervescent tablets prepared in Example 3 123 seconds Little 116 seconds Citrus aurantium effervescent tablets prepared in Example 4 121 seconds Very little 31 seconds Citrus aurantium effervescent tablets prepared in Comparative Example 1 122 seconds Little 109 seconds Citrus aurantium effervescent tablets prepared in Comparative Example 2 125 seconds Little 104 seconds

[0080] As can be seen from the results in Table 1, the Citrus aurantium fruit effervescent tablets prepared in Examples 1 and 2 produced a large amount of foam, and the foam dissipation time was long; while the foam amount of the Citrus aurantium fruit effervescent tablets prepared in Example 3 was significantly reduced, and the foam dissipation time was greatly shortened. This shows that, compared with adding the freeze-dried Citrus aurantium fruit powder prepared using water or 40% ethanol aqueous solution, adding the freeze-dried Citrus aurantium fruit powder prepared using a mixed solvent composed of 40% ethanol aqueous solution and 1,3-propanediol can significantly reduce the foam production amount after effervescent reaction of the Citrus aurantium fruit effervescent tablets, and can also significantly shorten the foam dissipation time.

[0081] As can also be seen from the results in Table 1, the foam amount of the Citrus aurantium fruit effervescent tablets prepared in Example 4 was further significantly reduced compared with Example 3, and the foam dissipation time was also further greatly shortened; this shows that, after the Citrus aurantium fruit is extracted using a mixed solvent composed of 40% ethanol aqueous solution and 1,3-propanediol, and then the freeze-dried Citrus aurantium fruit powder is prepared by the macroporous resin elution conditions of the present application, the freeze-dried Citrus aurantium fruit powder can further significantly reduce the foam production amount after effervescent reaction of the Citrus aurantium fruit effervescent tablets, and can also further greatly shorten the foam dissipation time.

[0082] However, the effervescence amount of the effervescent tablets of Citrus aurantium L. prepared by Comparative Examples 1 and 2 is not further obviously reduced, and the foam dissipation time is not further greatly shortened, as compared with Example 3; this indicates that: after the Citrus aurantium L. is extracted by the mixed solvent composed of the ethanol aqueous solution with a volume fraction of 40% and 1,3-propanediol, only the Citrus aurantium L. freeze-dried powder prepared by the macroporous resin elution condition (i.e. elution is carried out by using the ethanol aqueous solution with a volume fraction of 33%) can further obviously reduce the effervescence amount of the effervescent tablets of Citrus aurantium L. after effervescent reaction, and can further greatly shorten the foam dissipation time; and the Citrus aurantium L. freeze-dried powder prepared by other macroporous resin elution conditions cannot further obviously reduce the effervescence amount of the effervescent tablets of Citrus aurantium L. after effervescent reaction, and cannot further greatly shorten the foam dissipation time.

Claims

1. A fructus aurantii effervescent tablet, characterized in that, The raw material components comprise the following weight parts: The lyophilized powder of Fructus aurantii 4~6 parts; acid source 55~65 parts; base source 55~65 parts; sweetener 30~35 parts; additive 1~2 parts. The lyophilized powder of Fructus aurantii is prepared by the following method: (1) Take Fructus aurantii, then heat and reflux extraction with solvent, and obtain the extract liquid after the extraction is completed, and then concentrate and dry the extract liquid to obtain the extract of Fructus aurantii; the solvent is a mixed solvent composed of 10%~50% (volume fraction) ethanol aqueous solution and 1,3-propanediol; (2) load the extract of Fructus aurantii on a macroporous resin column, then elute with 30~35% (volume fraction) ethanol aqueous solution to obtain an eluate; concentrate and lyophilize the eluate to obtain the lyophilized powder of Fructus aurantii.

2. The Wuzhifen effervescent tablet according to claim 1, characterized in that, The raw material components comprise the following weight parts: The lyophilized powder of Fructus aurantii 4~6 parts; acid source 55~65 parts; base source 55~65 parts; sweetener 30~35 parts; additive 1~2 parts.

3. The effervescent tangerine peel tablets according to claim 1, characterized in that, The acid source is citric acid.

4. The effervescent tangerine peel tablets according to claim 1, characterized in that, The base source is sodium bicarbonate.

5. The effervescent tangerine peel tablets according to claim 1, characterized in that, The sweetener is selected from erythritol; or the sweetener is a combination of erythritol and white sugar.

6. The effervescent citrus peel tablets according to claim 1, characterized in that, The volume ratio of 10%~50% (volume fraction) ethanol aqueous solution and 1,3-propanediol is 4~6:

1.

7. The Wuzhifen effervescent tablet according to claim 6, characterized in that, The volume ratio of 10%~50% (volume fraction) ethanol aqueous solution and 1,3-propanediol is 5:

1.

8. The preparation method of the Exocarpium Citri Grandis effervescent tablets according to any one of claims 1-7, characterized in that, The steps comprise: Preparation of acidic granules: in the raw materials, take 1 / 2 dosage of sweetener, 1 / 2 dosage of lyophilized powder of Fructus aurantii and acid source in sequence, mix and homogenize, then granulate with anhydrous ethanol to obtain acidic granules; Preparation of basic granules: in the raw materials, take 1 / 2 dosage of sweetener, 1 / 2 dosage of lyophilized powder of Fructus aurantii and base source in sequence, mix and homogenize, then granulate with anhydrous ethanol to obtain basic granules; Mixing and tabletting step: melt the additive, then mix and homogenize with the acidic granules and the basic granules, and then tablet to obtain the effervescent tablet of Fructus aurantii.