阅读说明：本技术 一种苦杏仁苷含片及其应用 (Amygdalin buccal tablet and application thereof ) 是由 唐秀全 唐牧驰 于 2021-08-13 设计创作，主要内容包括：本发明属于医药技术领域,具体涉及一种苦杏仁苷含片及其应用。苦杏仁苷含片由苦杏仁苷、消化酶和辅料按照1:1-10:100-1000的质量比例混合后,压片而成。患者通过口含的方式使用苦杏仁苷含片后,苦杏仁苷水解产生的氢氰酸等物质通过消化系统和呼吸系统进入体内,具有抗菌和抗癌效果,可以防止疾病的发生,提高机体免疫力。(The invention belongs to the technical field of medicines, and particularly relates to an amygdalin buccal tablet and application thereof. The amygdalin buccal tablet is prepared by mixing amygdalin, digestive enzyme and auxiliary materials according to the mass ratio of 1:1-10:100-1000, and tabletting. After the patient uses the amygdalin buccal tablet in a buccal mode, hydrocyanic acid and other substances generated by amygdalin hydrolysis enter the body through a digestive system and a respiratory system, and the amygdalin buccal tablet has antibacterial and anticancer effects, can prevent diseases and improve the immunity of the organism.)

1. The amygdalin buccal tablet is characterized by being prepared by mixing amygdalin, digestive enzyme and auxiliary materials according to the mass ratio of 1:1-10:100-1000 and tabletting.

2. The amygdalin lozenge of claim 1, wherein the digestive enzyme is amylase, pepsin or trypsin.

3. The amygdalin buccal tablet of claim 2, wherein the excipient comprises powdered sugar.

4. The amygdalin buccal tablet of claim 3, wherein the excipient further comprises a flavoring agent.

5. The amygdalin buccal tablet of claim 4, wherein the flavoring agent is a sweetener or a flavoring agent.

6. The amygdalin lozenge of claim 5, wherein the sweetener is sucrose, glucose or malto-oligosaccharide.

7. The amygdalin buccal tablet of claim 5, wherein the flavoring agent is strawberry flavor.

8. Use of an amygdalin buccal tablet as claimed in any one of claims 1 to 7 in the preparation of a microbial inhibitor.

9. Use according to claim 8, characterized in that the microorganism is Escherichia coli ATCC35401, Staphylococcus aureus ATCC6538, Candida albicans ATCC10231 or Streptococcus pyogenes ATCC 19615.

10. Use of amygdalin buccal tablets as claimed in any one of claims 1 to 7 in the preparation of cancer cell activity inhibitors.

Technical Field

The invention belongs to the technical field of medicines, and particularly relates to an amygdalin buccal tablet and application thereof.

Background

Amygdalin is a compound existing in nature, mostly exists in leaves and fruit kernels of some plants, is extracted by people and then used as a medicine, but has poor effect in practical application, so that the practical use amount is small. It is known that amygdalin is decomposed by enzyme to produce hydrocyanic acid, the boiling point of hydrocyanic acid is 27 ℃, hydrocyanic acid is decomposed into gas quickly after enzymolysis in human body, and hydrocyanic acid has inhibition effect on respiration of cells, so amygdalin has treatment effect through hydrocyanic acid finally.

At present, amygdalin is prepared into oral medicines or injections. After the oral medicine enters the digestive tract, amygdalin is enzymolyzed into hydrocyanic acid in the digestive tract, and the hydrocyanic acid produced only acts on the digestive system. The injection is prepared by injecting amygdalin into blood, and the blood lacks enzymes for degrading amygdalin, so that hydrocyanic acid cannot be produced, and the treatment effect of hydrocyanic acid cannot be achieved.

Therefore, it is necessary to develop a amygdalin drug acting on the whole body of the human body, so as to utilize hydrocyanic acid decomposed by amygdalin to achieve therapeutic effects.

Disclosure of Invention

In order to solve the technical problems, the invention provides an amygdalin buccal tablet and application thereof.

The invention aims to provide an amygdalin buccal tablet which is prepared by mixing amygdalin, digestive enzyme and auxiliary materials according to the mass ratio of 1 (1-10) to 100 (1000) and tabletting.

Preferably, in the amygdalin buccal tablet, the digestive enzyme is amylase, pepsin or trypsin.

Preferably, the amygdalin buccal tablet comprises sugar powder as an auxiliary material.

Preferably, the amygdalin buccal tablet comprises the auxiliary materials and a flavoring agent.

Preferably, the amygdalin buccal tablet is characterized in that the flavoring agent is a sweetening agent or a flavoring agent.

Preferably, in the amygdalin buccal tablet, the sweetener is sucrose, glucose or malto-oligosaccharide.

Preferably, in the amygdalin buccal tablet, the flavoring agent is strawberry essence.

The invention also provides an application of the amygdalin buccal tablet in preparation of a microbial inhibitor.

Preferably, in the above application, the microorganism is escherichia coli ATCC35401, staphylococcus aureus ATCC6538, candida albicans ATCC10231, or streptococcus pyogenes ATCC 19615.

The invention also provides an application of the amygdalin buccal tablet in a cell activity inhibitor.

Compared with the prior art, the invention has the following beneficial effects:

the amygdalin buccal tablet provided by the invention has antibacterial and anticancer effects, can prevent diseases and improve the immunity of organisms. Such as:

(1) after a patient uses the amygdalin buccal tablet in a buccal mode, hydrocyanic acid and other substances generated by amygdalin hydrolysis enter the body through a digestive system and a respiratory system, harmful bacteria such as candida albicans and the like in the body are killed, the occurrence of infection is reduced, and the chance of virus parasitism is reduced after the harmful bacteria are killed, so that the occurrence probability of body diseases is greatly reduced.

(2) The amygdalin buccal tablet has antibacterial effect, and can reduce the accumulation of harmful bacteria in body, provide opportunity for the growth of beneficial bacteria, and improve immunity.

(3) The amygdalin buccal tablet provided by the invention has an anticancer effect and can inhibit the proliferation of cancer cells LNCaP.

Detailed Description

In order that those skilled in the art will better understand the technical solutions of the present invention to practice, the present invention will be further described with reference to the following specific examples.

In the description of the present invention, reagents used are commercially available and methods used are conventional in the art, unless otherwise specified. The amygdalins described in the examples below were purchased from Hibiscus Biotech, Inc., wherein the amygdalin content was 98%.

The invention provides an amygdalin buccal tablet which is prepared by mixing amygdalin, digestive enzyme and auxiliary materials according to the mass ratio of 1 (1-10) to 100 (1000) and tabletting. The digestive enzyme is amylase, pepsin or trypsin. The auxiliary materials comprise powdered sugar and flavoring agents, and the flavoring agents are sweetening agents or flavoring agents. The sweetener is sucrose, glucose or malto-oligosaccharide. The flavoring agent is strawberry essence.

Example 1

A amygdalin buccal tablet is prepared by mixing amygdalin, digestive enzyme and adjuvants at a mass ratio of 1:1:100, and tabletting. The digestive enzyme is amylase, and the auxiliary material is powdered sugar. The tabletting method adopts a tabletting machine for pharmacy to tablet.

Example 2

A amygdalin buccal tablet is prepared by mixing amygdalin, digestive enzyme and adjuvants at a mass ratio of 1:1:1000, and tabletting. The digestive enzyme is pepsin, and the auxiliary material is powdered sugar. The tabletting method adopts a tabletting machine for pharmacy to tablet.

Example 3

A amygdalin buccal tablet is prepared by mixing amygdalin, digestive enzyme and adjuvants at a mass ratio of 1:1:500, and tabletting. The digestive enzyme is trypsin, and the auxiliary material is powdered sugar. The tabletting method adopts a tabletting machine for pharmacy to tablet.

Example 4

A amygdalin buccal tablet is prepared by mixing amygdalin, digestive enzyme and adjuvants at a mass ratio of 1:1:200, and tabletting. The digestive enzyme is amylase, and the auxiliary materials are sugar powder and glucose which are mixed according to a ratio of 200:1 to form a mixture. The tabletting method adopts a tabletting machine for pharmacy to tablet.

Example 5

A amygdalin buccal tablet is prepared by mixing amygdalin, digestive enzyme and adjuvants at a mass ratio of 1:1:800, and tabletting. The digestive enzyme is amylase, and the auxiliary materials are powdered sugar and strawberry essence which are mixed according to a ratio of 2000:1 to form a mixture. The tabletting method adopts a tabletting machine for pharmacy to tablet.

The amygdalin buccal tablet has the following effects:

first, a bactericidal action

The amygdalin buccal tablet provided by the invention can generate hydrocyanic acid under the action of water and digestive enzyme, and has a sterilization effect, and the specific experimental method is as follows:

activating Escherichia coli ATCC35401 with LB slant culture medium, picking activated thallus under aseptic condition, placing in 0.85g/100mL sodium chloride solution, diluting to 10%⁶The cell concentration of each/mL order of magnitude, and the test bacterial liquid of the escherichia coli is obtained.

Test bacterial liquids of staphylococcus aureus ATCC6538, candida albicans ATCC10231 and streptococcus pyogenes ATCC19615 were prepared according to the above-described methods, respectively, and were used.

The amygdalin buccal tablet in the embodiment 1 is ground into powder of 100 meshes, 0.5g of the amygdalin buccal tablet is taken to be dissolved in sodium chloride solution with the concentration of 0.85g/100mL to be respectively prepared into suspensions with the concentrations of 3g/L, 10g/L and 15g/L, the suspensions with the concentrations are respectively mixed with different test bacterial liquids according to equal proportion, and the sterilization rate is counted after 15 min. A blank was prepared from 0.85g/100mL sodium chloride solution. Each test was performed in triplicate, viable bacteria were counted using viable bacteria counting method, and the average value was calculated and reported in table 1.

The bactericidal ratio was 1- (2X concentration of bacterial liquid after test/concentration of bacterial liquid before test)

The results are shown in table 1, and the results in table 1 show that the amygdalin buccal tablet of the present invention has a good bactericidal effect.

TABLE 1 Bactericidal effect of amygdalin buccal tablets with different concentrations

Second, anticancer effects

The experimental object of the invention is a human prostate epithelial cancer cell strain LNCaP. The cell line LNCaP was cultured in RPMI-1640 cell culture medium in 96-well plates. The culture medium is added with fetal calf serum with volume fraction of 10% and double antibodies, wherein the double antibodies are penicillin with final concentration of 10kU/mL and streptomycin with final concentration of 10mg/mL respectively. The culture conditions were 37 ℃ and 5% CO₂When the cells are attached to the culture dishAfter the growth is finished, adding the medicine, and continuously incubating for 72h after adding the medicine.

The experimental groups were as follows: (1) in the control group, the amygdalin buccal tablet powder is replaced by sterile water with equal mass;

(2) in the experimental group 1, 100-mesh amygdalin buccal tablet powder of the example 1 was added, and the final concentration was 10 mg/mL;

(3) experiment group 2, 100 mesh amygdalin buccal tablet powder of example 1 was added to a final concentration of 15 mg/mL;

each group of experiments is provided with 3 multiple wells, and the average value of each experiment is taken when calculating the cell activity.

After 72h incubation, the medium was removed, washed with 0.1M, pH ═ 7.2 in PBS, and 5mg/ml MTT was added to each well, 5% CO at 37 ℃₂Incubate for 5h, add 0.4mL of 10g/100mL SDS/well, 37 ℃/5% CO₂Culturing for 12 h. After the culture is finished, the sample is taken out, placed at room temperature for 25min, the absorbance value of the culture solution at 570nm is measured, and the cell activity is calculated.

Cell activity ═ (absorbance of experimental group)/(absorbance of control group) × 100%.

The cell survival rate calculation results are shown in table 2, the experiment data in table 2 are averaged, the test data of the control group is set as a reference value of 100, the relative activity of the experiment group is calculated, and the results show that the amygdalin buccal tablet has an anti-proliferative effect on LNCaP cells.

TABLE 1 measurement of cell Activity

It should be noted that, when the present invention relates to a numerical range, it should be understood that two endpoints of each numerical range and any value between the two endpoints can be selected, and since the steps and methods adopted are the same as those in the embodiment, in order to prevent redundancy, the present invention describes a preferred embodiment. While preferred embodiments of the present invention have been described, additional variations and modifications in those embodiments may occur to those skilled in the art once they learn of the basic inventive concepts. Therefore, it is intended that the appended claims be interpreted as including preferred embodiments and all such alterations and modifications as fall within the scope of the invention.

It will be apparent to those skilled in the art that various changes and modifications may be made in the present invention without departing from the spirit and scope of the invention. Thus, if such modifications and variations of the present invention fall within the scope of the claims of the present invention and their equivalents, the present invention is also intended to include such modifications and variations.