CN103191070A - Oral tablet of superoxide dismutase and preparation method thereof - Google Patents

Abstract

The invention provides a superoxide dismutase oral buccal tablet and a preparation method thereof. The buccal tablet includes superoxide dismutase and food additives, and each gram of oral buccal tablet contains 14,000-45,000 U active superoxide dismutase . During preparation, an appropriate amount of superoxide dismutase dry powder with an activity of 10 U/g to 500,000 U/g is used, mixed with food additives, and compressed into tablets. When the buccal tablet of the present invention is taken, the SOD gradually releases its activity through the slow dissolution of saliva, thereby avoiding the phenomenon that the SOD enters the stomach and is inactivated in the gastric acid environment. Moreover, the SOD dry powder in the present invention is extracted from corn, and the cost of the SOD dry powder is greatly reduced in addition to retaining the activity to the greatest extent.

Description

A kind of superoxide dismutase oral buccal tablet and its preparation method

technical field

The invention relates to an oral biological preparation and a preparation method, in particular to a superoxide dismutase oral buccal tablet and a preparation method.

Background technique

Superoxide dismutase (English abbreviation "SOD") is internationally recognized as the "scavenger", "anti-aging king", and "beauty favorite" of human waste. most powerful substance. Supplementing the SOD needed by the human body through exogenous sources can improve human immunity and delay aging; effectively reduce blood lipids, cholesterol, and blood pressure; resist fatigue and radiation; inhibit cardiovascular and cerebrovascular diseases, etc.

There are a large number of very popular SOD health products on the market today, including SOD capsules, SOD oral liquid, SOD liquid medicine and so on. According to the characteristics of SOD, we know that SOD is a metalloenzyme that is very sensitive to pH. When SOD is taken as a tablet or liquid reagent, it will directly enter the stomach of the human body, and the gastric acid of the human body will destroy the three-dimensional structure of SOD. , and decompose it into peptide chains and amino acids, completely destroying the activity of SOD, so it is difficult to guarantee the function of SOD. In order to avoid this problem, SOD enteric-coated tablets and enteric-coated capsules have appeared in the world. These enteric-coated tablets or capsules will avoid the decomposition of gastric acid and directly reach the small intestine, then disintegrate, absorb through the inner wall of the small intestine, and enter the human blood to exert the effect of SOD. However, in the complex environment in the small intestine, it is difficult to determine whether SOD can be fully absorbed and play its role.

Contents of the invention

The present invention aims to provide an oral superoxide dismutase lozenge that can be fully absorbed through the oral cavity and esophageal mucosa and has obvious efficacy, and provides a method for preparing the lozenge with low cost. The present invention realizes by following scheme:

A superoxide dismutase oral lozenge comprises superoxide dismutase and a food additive, and each gram of the oral lozenge contains 14,000-45,000 U active superoxide dismutase.

In order to enhance the taste, the total amount of food additives accounts for 80% to 90% of the total mass of the lozenge.

These food additives are conventional additives for oral lozenges, including: lubricants, mold release agents (such as magnesium stearate, sodium stearate, etc.), anti-caking, moisture-absorbing additives (such as silicon dioxide) , disintegrants (such as microcrystalline cellulose), binders (such as hydroxypropyl cellulose, hydroxypropionamide, etc.) and sweeteners (such as xylitol, mannitol, etc.). The purity of all additives is food grade, that is, the main component content is above 99%. The addition amount of each of the above-mentioned food additives gets final product according to the amount of ordinary preparation oral buccal tablet.

The preparation method of the above-mentioned superoxide dismutase oral buccal tablet is to take an appropriate amount of superoxide dismutase dry powder with an activity of 10 U/g to 500,000 U/g, mix it with food additives, and press it into tablets; the superoxide dismutase added during preparation The mass of oxide dismutase dry powder accounts for 8%-15% of the total mass.

The above-mentioned superoxide dismutase dry powder is prepared by the following steps:

The first step: pretreating the corn to obtain corn slurry;

The second step: adding water-soluble copper salt to the corn slurry to maintain the pH value of 7-9, and then separating the solid and liquid to obtain the superoxide dismutase stock solution;

The third step: the superoxide dismutase stock solution obtained in the second step is filtered through more than two stages of membranes to remove impurities with a molecular weight of >120,000 and a molecular weight of <10,000 in sequence to obtain a concentrated superoxide dismutase solution;

Step 4: adding a water-miscible organic liquid to the concentrated superoxide dismutase solution, separating to obtain a precipitate, and freeze-drying the precipitate.

In order to further improve the purity of superoxide dismutase, the dry powder obtained in the fourth step above can be dissolved in water again, and then add a water-miscible organic liquid to separate to obtain a precipitate, and freeze-dry the above precipitate.

The water-miscible organic liquid is generally preferred for industrial applications such as acetone, absolute ethanol or methanol.

In order to enhance the mouthfeel, 8% to 15% of the total mass of the superoxide dismutase dry powder is added during preparation, and the rest is the total amount of food additives added.

Compared with the prior art, the present invention has the following advantages:

1. SOD is a metalloenzyme that is very sensitive to pH and will be inactivated in an acidic environment. It is readily soluble in water and readily absorbed through mucous membranes. The SOD dry powder of the present invention is made into SOD buccal tablets. When the buccal tablets are taken, the SOD gradually releases its activity through the slow dissolution of saliva, and then is fully absorbed by the oral mucosa and esophageal mucosa, thereby preventing SOD from entering the stomach and dissolving in gastric acid. The phenomenon of inactivation in the environment directly enters the human body and fully exerts its special effects.

2, SOD dry powder among the present invention is to extract from corn. During the extraction process, no chemical substances harmful to human health are added to maximize the retention of SOD in corn. It is well known that the purer a substance is extracted, the higher its cost. The price of pure SOD in the international market is 10,000 to 15,000 US dollars/gram, and the price of pure SOD in the domestic market is 59,000 to 120,000 RMB/gram. Due to the high cost of SOD, its comprehensive promotion is largely limited. The price of the SOD buccal tablets made from corn SOD dry powder in the present invention is far lower than that of products produced by using pure SOD products, and can be accepted by the majority of consumer groups.

Detailed ways

Example 1

A superoxide dismutase oral lozenge, composed of superoxide dismutase and food additives, each lozenge has a net weight of 680 mg, and each lozenge contains 24,000 U of active superoxide dismutase, that is, each gram contains The tablet contains about 35,000 U of active superoxide dismutase; food additives include xylitol, hydroxypropyl cellulose, magnesium stearate, silicon dioxide and microcrystalline fiber, and the total amount of additives accounts for about 84% of the total mass of the lozenge .

Example 2

The preparation method of the superoxide dismutase oral buccal tablet of embodiment 1, with 25g, activity is the superoxide dismutase dry powder of 300,000 U/g and the food additive of following food-grade purity: 75g xylitol, 28g hydroxypropyl Fiber, 11g of magnesium stearate, 9g of silicon dioxide, and 63g of microcrystalline fiber are fully mixed, then divided into buccal tablets with a tablet press, so that the quality of each buccal tablet is 680 mg, and then aseptically packaged.

Example 3

The superoxide dismutase dry powder in embodiment 2 adopts the following steps to make:

Step 1: Take 120Kg of dry corn kernels, wash them, soak them in warm water (30°C) for 24 hours, take them out and drain them to obtain 140Kg of wet corn. The corn was refined with 180L of water to obtain 350L of corn slurry containing superoxide dismutase.

Step 2: Add 24.5 g of anhydrous copper sulfate to the above corn slurry, adjust the pH to 7-9 with ammonia water, and perform solid-liquid separation by pressure filtration to obtain 210 L of an enzyme stock solution with a superoxide dismutase activity of 468 U/mL.

The third step: the superoxide dismutase stock solution obtained in the previous step is sequentially filtered through a ceramic membrane and concentrated by an ultrafiltration membrane. Oxide dismutase concentrate, the activity of superoxide dismutase in the concentrate is 9691U/mL, the volume is 10L, and the activity retention rate is 98.6%.

The fourth step: adding acetone to the superoxide dismutase concentrated solution obtained in the previous step, separating the precipitate to obtain the precipitate, and freeze-drying the above precipitate to obtain the desired dry powder.

Example 4

A superoxide dismutase oral lozenge, composed of superoxide dismutase and food additives, each lozenge has a net weight of 680 mg, and each lozenge contains 15,000 U of active superoxide dismutase, that is, each gram contains The tablet contains about 22,000 U of active superoxide dismutase; food additives include mannitol, hydroxypropionamide, sodium stearate, silicon dioxide and microcrystalline fiber, and the total amount of additives accounts for about 93% of the total mass of the lozenge.

Example 5

The preparation method of the superoxide dismutase oral lozenge of embodiment 4, with 25g, activity is the superoxide dismutase dry powder of 300,000 U/g and the food additive of following food-grade purity: 150g xylitol, 56g hydroxypropyl Fiber, 18g of magnesium stearate, 6g of silicon dioxide, and 82g of microcrystalline fiber are fully mixed, then divided into buccal tablets with a tablet press, so that the quality of each buccal tablet is 680 mg, and then aseptically packaged.

Example 6

A superoxide dismutase oral lozenge, composed of superoxide dismutase and food additives, each lozenge has a net weight of 680 mg, and each lozenge contains 31,000 U active superoxide dismutase, that is, each gram contains The tablet contains about 45,000 U of active superoxide dismutase; food additives include mannitol, hydroxypropionamide, sodium stearate, silicon dioxide and microcrystalline fiber, and the total amount of additives accounts for about 93% of the total mass of the lozenge.

Example 7

The preparation method of the superoxide dismutase oral lozenge of embodiment 6, with 30g, activity is the superoxide dismutase dry powder of 500,000 U/g and the food additive of following food-grade purity: 150g xylitol, 56g hydroxypropyl Fiber, 18g of magnesium stearate, 6g of silicon dioxide, and 82g of microcrystalline fiber are fully mixed, then divided into buccal tablets with a tablet press, so that the quality of each buccal tablet is 680 mg, and then aseptically packaged.

Example 8

The superoxide dismutase dry powder in embodiment 7 adopts following steps to make:

Step 1: Take 120Kg of dry corn kernels, wash them, soak them in warm water (30°C) for 24 hours, take them out and drain them to obtain 140Kg of wet corn. The corn was refined with 180L of water to obtain 350L of corn slurry containing superoxide dismutase.

Step 2: Add 24.5 g of anhydrous copper sulfate to the above corn slurry, adjust the pH to 7-9 with ammonia water, and perform solid-liquid separation by pressure filtration to obtain 210 L of an enzyme stock solution with a superoxide dismutase activity of 468 U/mL.

The third step: the superoxide dismutase stock solution obtained in the previous step is sequentially filtered through a ceramic membrane and concentrated by an ultrafiltration membrane. Oxide dismutase concentrate, the activity of superoxide dismutase in the concentrate is 9691U/mL, the volume is 10L, and the activity retention rate is 98.6%.

The fourth step: adding acetone to the superoxide dismutase concentrated solution obtained in the previous step, separating to obtain a precipitate, and freeze-drying the above precipitate to obtain a primary dry powder.

The fifth step: after dissolving the primary dry powder obtained in the fourth step in water, adding acetone, obtaining a precipitate through separation, and freeze-drying the above precipitate to obtain a superoxide dismutase dry powder.

Claims (8)

1. a superoxide dismutase oral buccal tablet comprises superoxide dismutase and food additive, it is characterized in that: contain 1.4～4.5 ten thousand U active superoxide dismutase in the oral buccal tablet of every gram.

2. superoxide dismutase oral buccal tablet as claimed in claim 1, it is characterized in that: food additive accounts for 80%～90% of buccal tablet gross mass.

3. the preparation method of a superoxide dismutase oral buccal tablet as claimed in claim 1 or 2, it is characterized in that: getting an amount of activity is the superoxide dismutase dry powder of 10U/g～500,000 U/g, after food additive is mixed, compression molding.

4. the preparation method of superoxide dismutase oral buccal tablet as claimed in claim 3 is characterized in that: described superoxide dismutase dry powder adopts following steps to make,

The first step: Semen Maydis is carried out pretreatment obtain the Semen Maydis serosity;

Second step: in the Semen Maydis serosity, add water the dissolubility mantoquita, keep pH value 7～9, afterwards through solid-liquid separation, obtain superoxide dismutase stock solution;

The 3rd step: with the superoxide dismutase stock solution membrane filtration more than two-stage again of the second step gained, remove molecular weight successively〉120,000 and the impurity of molecular weight＜10,000, obtain the superoxide dismutase concentrated solution;

The 4th step: in the superoxide dismutase concentrated solution, add and to obtain precipitate with the Organic substance liquid that water dissolves each other through separating, the described precipitate of lyophilization.

5. the preparation method of superoxide dismutase oral buccal tablet as claimed in claim 4, it is characterized in that: after described the 4th step gained dry powder is water-soluble again, add again and can obtain precipitate with the Organic substance liquid that water dissolves each other through separating, the described precipitate of lyophilization.

6. as the preparation method of claim 4 or 5 described superoxide dismutase oral buccal tablets, it is characterized in that: the described preferred acetone of Organic substance liquid, dehydrated alcohol or the methanol that can dissolve each other with water.

7. as the preparation method of claim 4 or 5 described superoxide dismutase oral buccal tablets, it is characterized in that: add the ratio 8%～15% that described superoxide dismutase dry powder accounts for gross mass during preparation.

8. the preparation method of superoxide dismutase oral buccal tablet as claimed in claim 6 is characterized in that: add the ratio 8%～15% that described superoxide dismutase dry powder accounts for gross mass during preparation.