Bursting bead capsule containing arecoline and areca polyphenol and application thereof

Abstract

The invention belongs to the field of medicines and tobaccos, and particularly relates to a blasting bead capsule containing arecoline and areca polyphenol and application of the blasting bead capsule. The blasting bead capsule containing the arecoline and the areca polyphenol is prepared from 0.5%-8.5% of the arecoline, 1%-10% of the areca polyphenol and water. The blast bead is developed by combining arecoline and areca polyphenol, can be applied to the fields of medicines and tobaccos, and explores the effect of the blast bead in drugs for expelling parasites and the like.

Description

Technical Field

[0001] The invention belongs to the field of medicine and tobacco, and particularly relates to a bursting bead capsule containing arecoline and areca nut polyphenol and application thereof. Background Art

[0002] The information disclosed in this background technology section is only intended to enhance the understanding of the overall background of the invention, and should not necessarily be regarded as an admission or any form of suggestion that the information constitutes the prior art already known to a person skilled in the art.

[0003] The chemical formula of arecoline is C 7 H 13 N, belongs to the alkaloid compound, usually white crystals or crystalline powder, with a slightly bitter taste and irritation. Arecoline, as a cholinergic receptor agonist, can enhance the activity of the neurotransmitter acetylcholine, thereby improving alertness and attention. It can also have an excitatory effect on the central nervous system, temporarily increase energy levels and improve mood. From a health perspective, arecoline may help improve attention and cognitive function, has certain antioxidant effects, and has potential benefits for health. However, arecoline is addictive, and long-term use may lead to dependence. Studies have found that it is associated with oral cancer and other oral diseases. Long-term chewing of betel nut increases these health risks, especially when used with tobacco. Therefore, arecoline is a compound with complex biological activity. Although it may have benefits in some aspects, its potential health risks cannot be ignored. Therefore, caution should be taken when using betel nut, especially considering the long-term health effects. Future research will help to more fully understand the mechanism of action of arecoline and its application in medicine. Areca nut polyphenols have significant antioxidant effects, which can prevent cell damage and reduce the risk of chronic diseases. Studies have shown that areca nut polyphenols may have the ability to inhibit inflammatory responses and help prevent chronic inflammatory-related diseases. In addition, it may protect cardiovascular health by lowering cholesterol and improving blood circulation. Areca nut polyphenols are widely used in medicines and are being studied and developed as functional ingredients.

[0004] So far, there is no report on the development of arecoline and areca nut polyphenols in combination. Summary of the invention

[0005] The shortcomings of the prior art are overcome, and the present invention provides a bursting bead capsule containing arecoline and areca nut polyphenols, and provides the application of the capsule in medicine and tobacco.

[0006] The components of the bursting bead capsule containing arecoline and areca nut polyphenols of the present invention are as follows: 0.5% to 8.5% of arecoline, 1% to 10% of areca nut polyphenols, and the rest is water. The bursting bead capsule shell is composed of ergosterol, sodium alginate, glycerin, gelatin, and water in a mass ratio of 0.1 to 0.3: 0.2 to 0.5: 0.7 to 1.4: 0.3 to 0.4: 1.

[0007] The present invention provides use of the explosive bead capsule containing arecoline and areca nut polyphenol in preparing anthelmintics and antiallergic drugs.

[0008] The present invention provides application of the explosive bead capsule containing arecoline and areca nut polyphenol in preparing tobacco products.

[0009] Compared with the prior art, the technical effects of the present invention are: The present invention combines arecoline and areca nut polyphenols to develop a bursting bead, which can be used in the fields of medicine and tobacco, and explores its role in anthelmintics and anti-allergic drugs.

[0010] The invention optimizes the formula of the bead-bursting capsule shell, reasonably combines ergosterol with raw materials such as sodium alginate, and obtains a bead-bursting capsule shell that is tough, elastic, can be isolated from the outside world, and is anti-oxidative, thereby ensuring the stability of arecoline and areca nut polyphenols in the bead-bursting capsule. BRIEF DESCRIPTION OF THE DRAWINGS

[0011] Figure 1 : Example 1 to Example 3 Changes in the arecoline content in the accelerated test of the bursting capsule containing arecoline and areca nut polyphenols.

[0012] Figure 2 : Example 1, Comparative Examples 1 to 3 Changes in the arecoline content in the accelerated test of the bursting bead capsules containing arecoline and areca nut polyphenols.

[0013] Figure 3 : Example 1, Comparative Example 1 to Comparative Example 3 Changes in the content of areca nut polyphenols in the accelerated test of the bursting bead capsules containing arecoline and areca nut polyphenols.

[0014] Figure 4 : The levels of IgE in serum of rats in each group.

[0015] Figure 5 : ALP content in serum of rats in each group. DETAILED DESCRIPTION

[0016] In order to make the purpose and technical solution of the present invention clearer, the present invention is further described below in conjunction with embodiments, but the protection scope of the present invention is not limited to these embodiments, and the embodiments are only used to explain the present invention. It should be understood by those skilled in the art that any changes or equivalent substitutions that do not deviate from the concept of the present invention are included in the protection scope of the present invention.

[0017] Example 1 Explosive bead capsule containing arecoline and areca nut polyphenols Contents: Arecoline 2.5%, areca nut polyphenols 6.5%, and the rest is water.

[0018] Bead-bursting capsule shell: ergosterol, sodium alginate, glycerin, gelatin, and water in a mass ratio of 0.2:0.3:1.1:0.35:1.

[0019] Preparation method: prepare the content solution and the bursting bead capsule shell solution according to the formula, and use the dripping method to encapsulate the content.

[0020] Example 2 Explosive bead capsules containing arecoline and areca nut polyphenols Contents: Arecoline 0.5%, Areca nut polyphenols 1%, the rest is water Bursting bead capsule shell: ergosterol, sodium alginate, glycerol, gelatin, and water in a mass ratio of 0.1:0.2:0.7:0.3:1.

[0021] Preparation method: prepare the content solution and the bursting bead capsule shell solution according to the formula, and use the dripping method to encapsulate the content.

[0022] Example 3 Explosive capsules containing arecoline and areca nut polyphenols Contents: Arecoline 8.5%, areca nut polyphenols 10%, and the rest is water.

[0023] Bead-bursting capsule shell: ergosterol, sodium alginate, glycerol, gelatin, and water in a mass ratio of 0.3:0.5:1.4:0.4:1.

[0024] Preparation method: prepare the content solution and the bursting bead capsule shell solution according to the formula, and use the dripping method to encapsulate the content.

[0025] Comparative Example 1: Explosive bead capsule containing arecoline and areca nut polyphenols Contents: Arecoline 2.5%, areca nut polyphenols 6.5%, and the rest is water.

[0026] Bead-bursting capsule shell: sodium alginate, glycerol, gelatin, and water in a mass ratio of 0.3:1.1:0.35:1.

[0027] Preparation method: prepare the content solution and the bursting bead capsule shell solution according to the formula, and use the dripping method to encapsulate the content.

[0028] Comparative Example 2: Explosive capsules containing arecoline and areca nut polyphenols Contents: Arecoline 2.5%, areca nut polyphenols 6.5%, and the rest is water.

[0029] Bead-bursting capsule shell: cholesterol, sodium alginate, glycerol, gelatin, and water in a mass ratio of 0.2:0.3:1.1:0.35:1.

[0030] Preparation method: prepare the content solution and the bursting bead capsule shell solution according to the formula, and use the dripping method to encapsulate the content.

[0031] Comparative Example 3: Explosive capsule containing arecoline and areca nut polyphenols Contents: Arecoline 2.5%, areca nut polyphenols 6.5%, and the rest is water.

[0032] Bead-bursting capsule shell: ergosterol, sodium alginate, glycerin, gelatin, and water in a mass ratio of 0.6:0.1:1.1:0.35:1.

[0033] Preparation method: prepare the content solution and the bursting bead capsule shell solution according to the formula, and use the dripping method to encapsulate the content.

[0034] Stability of bursting bead capsules containing arecoline and areca nut polyphenols After packaging, the bursting bead capsules containing arecoline and areca nut polyphenols of Examples 1 to 3 and the bursting bead capsules containing arecoline and areca nut polyphenols of Comparative Examples 1 to 3 were placed under conditions of 40°C±2°C and 75%±5% relative humidity for accelerated testing, and samples were taken on the first day, at the end of the second month, at the end of the third month, and at the end of the sixth month for testing.

[0035] The content of arecoline is determined according to the high performance liquid chromatography method (General Rule 0512) in the 2020 edition of the Chinese Pharmacopoeia. Chromatographic conditions and system suitability test: strong cation exchange bonded silica gel is used as the filler (SCX-strong cation exchange resin column); acetonitrile-phosphoric acid solution (2→1000, concentrated ammonia test solution adjusts the pH value to 3.8) (55:45) is used as the mobile phase; the detection wavelength is 215nm. The number of theoretical plates calculated based on the arecoline peak should not be less than 3000. Preparation of reference solution: Take an appropriate amount of arecoline hydrobromide reference substance, accurately weigh it, add the mobile phase to make a solution containing 0.1 mg per 1 ml, and obtain (arecoline weight = arecoline hydrobromide weight / 1.5214). Preparation of test solution: Take about 0.3g of the powder of this product (pass through a No. 5 sieve), weigh accurately, place in a stoppered conical flask, add 50ml of ether, and then add 3ml of carbonate buffer (take 1.91g of sodium carbonate and 0.56g of sodium bicarbonate, add water to dissolve to 100ml, and then place for 30 minutes, shaking from time to time; heat and reflux for 30 minutes, take the ether solution, and add it to an evaporating dish containing 1ml of phosphoric acid solution (5→1000); add ether to the residue and heat and reflux and extract twice (30ml, 20ml), each time for 15 minutes, combine the ether solution and place it in the same evaporating dish, evaporate the ether, dissolve the residue in 50% acetonitrile solution, transfer to a 25ml volumetric flask, add 50% acetonitrile to the scale; shake well, filter, and take the filtrate to obtain. Determination method: Accurately aspirate 10μl of the reference solution and the test solution, inject into the liquid chromatograph, and determine to obtain.

[0036] Table 1 Areca nut polyphenol content (%) Figure 1 The changes in the arecoline content in the accelerated test of the bursting bead capsules containing arecoline and areca nut polyphenols in Examples 1 to 3. Figure 2 The changes of arecoline content in the accelerated test of the bursting bead capsules containing arecoline and arecoline polyphenols in Example 1 and Comparative Examples 1 to 3. Arecoline polyphenols were determined by high performance liquid chromatography. Figure 3 The changes in the content of areca nut polyphenols in the accelerated test of the bursting bead capsules containing arecoline and areca nut polyphenols in Example 1 and Comparative Examples 1 to 3. As shown in Table 1, the bursting bead capsules containing arecoline and areca nut polyphenols in the accelerated test of Examples 2 to 3 optimize the shell formula of the capsule, add a certain proportion of ergosterol and sodium alginate, improve the isolation ability, and make the bursting bead capsules containing arecoline and areca nut polyphenols more stable.

[0037] Pharmacodynamics experiment of Baozhu capsule containing arecoline and areca nut polyphenols in treating allergy SD rats, SPF grade, 180-220 g, were fed adaptively under standard conditions for 1 week before the experiment, and the OVA sensitization method was used to model the model. Rats were subcutaneously injected with 100 μg of OVA and adjuvant Al(OH) 3 5mg PBS solution 200μL, sensitize the rats; on the 7th, 14th and 21st days, intraperitoneal injection of 200μL PBS solution containing OVA 100μg was used to strengthen sensitization. The rats with successful modeling were divided into model group, Example 1 group, Example 2 group, Example 3 group and positive drug group, with 10 rats in each group, and 10 normal rats in the blank group. Rats in each group were given equal doses of corresponding drugs (in terms of arecoline, 0.01mg / kg), rats in the positive drug group were given commercially available cetirizine hydrochloride (purchased from Lu** Co., Ltd., 0.9mg / kg), and the blank group and model group were gavaged with normal saline, and the drugs were administered for 3 consecutive days, once a day.

[0038] Behavioral scoring of rats Sneezing, runny nose, redness and swelling of hands and feet, and number of times of scratching nose were used as scoring indicators. Each indicator was divided into a score range of 0 to 5 as a standard for judging the severity and statistics were performed.

[0039] Table 2 Behavioral scores of rats in each group Compared with the model group, *P<0.01.

[0040] Compared with the positive drug group, *P<0.01.

[0041] As shown in the behavioral scores of rats in each group in Table 2, the explosive bead capsules containing arecoline and areca nut polyphenols in Examples 1 to 3 of the present invention can alleviate allergic reactions and effectively relieve symptoms such as scratching the nose, sneezing, runny nose, and swollen hands and feet caused by allergies in rats.

[0042] IgE and ALP levels in rat serum Figure 4 is the IgE content in the serum of rats in each group, Figure 5 The ALP content in the serum of rats in each group is significantly different from that in the model group and the positive drug group in Example 1 to Example 3, P < 0.05.

[0043] In summary, the explosive bead capsule containing arecoline and areca nut polyphenols of the present invention can be used to treat allergic diseases and has excellent therapeutic effect in anti-allergic effect.

[0044] The anthelmintic effect of the explosive bead capsule containing arecoline and areca nut polyphenols of the present invention A chicken farmer had a case of sick chickens, with symptoms such as drooping wings, depression, diarrhea, and bloody mucus in the loose feces. After investigation, more than 300 laying hens were found to be infected with roundworms and tapeworms. The sick chickens were then isolated and the site and environment were strictly disinfected. The 300 sick chickens were divided into three test groups, namely, group 1, group 2, and group 3, with 100 chickens in each group. The corresponding drugs were given at 0.01 mg / kg in terms of arecoline for 7 days, and the treatment effect was statistically analyzed.

[0045] The cure rate, effective rate and mortality rate are determined based on the clinical symptoms of the chickens after treatment. Cure rate = number of cured chickens / total number × 100%, effective rate = (number of cured chickens + number of effective chickens) / total number × 100%.

[0046] Table 3 The anthelmintic effect of the explosive bead capsule containing arecoline and areca nut polyphenols of the present invention As shown in Table 3, the anthelmintic effect results of the Baozhu capsule containing arecoline and areca nut polyphenols show that the present invention can exert a significant anthelmintic effect, and the effective rate of treating laying hens infected with ascaris and tapeworms is higher than 90%.

[0047] Popping Bead Cigarettes According to the formula and preparation method of Examples 1 to 3, popping beads with a diameter of 2.6 to 4.6 mm are made. When preparing tobacco, they are placed in the filter tip of a cigarette. Smokers can pinch the beads to make the liquid in the beads flow out during smoking, making the cigarette taste richer and more fragrant.

Claims

1. A capsule containing arecoline and areca nut polyphenols, characterized in that: The arecoline content is 0.5% to 8.5%, and the areca nut polyphenol content is 1% to 10%.

2. The explosive bead capsule containing arecoline and areca nut polyphenols according to claim 1, characterized in that: The components of the bursting bead capsule are as follows: 0.5% to 8.5% of arecoline, 1% to 10% of areca nut polyphenols, and the rest is water.

3. The explosive bead capsule containing arecoline and areca nut polyphenols according to claim 1, characterized in that: The components of the bursting bead capsule are as follows: 2.5% of arecoline, 6.5% of areca nut polyphenols, and the rest is water.

4. The explosive bead capsule containing arecoline and areca nut polyphenols according to claim 1, characterized in that: The components of the bursting bead capsule are as follows: 0.5% of arecoline, 1% of areca nut polyphenols, and the rest is water.

5. The explosive bead capsule containing arecoline and areca nut polyphenols according to claim 1, characterized in that: The components of the bursting bead capsule are as follows: 8.5% of arecoline, 10% of areca nut polyphenols, and the rest of water.

6. The explosive bead capsule containing arecoline and areca nut polyphenols according to claim 1, characterized in that: The shell of the bursting bead capsule is composed of ergosterol, sodium alginate, glycerol, gelatin and water in a mass ratio of 0.1-0.3:0.2-0.5:0.7-1.4:0.3-0.4:

1.

7. The explosive bead capsule containing arecoline and areca nut polyphenols as claimed in claim 1, characterized in that: The bursting capsule containing arecoline and areca nut polyphenol is used for preparing anthelmintic medicine.

8. The explosive bead capsule containing arecoline and areca nut polyphenols as claimed in claim 1, characterized in that: The bursting bead capsule containing arecoline and areca nut polyphenol is used for preparing tobacco products.

9. The explosive bead capsule containing arecoline and areca nut polyphenols as claimed in claim 1, characterized in that: The bursting bead capsule containing arecoline and areca nut polyphenol is used for preparing antiallergic drugs.

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