CN1981855A - Self-emusified composition containing diamond vine extract - Google Patents

Abstract

The invention discloses a self-emulsifying composition containing King Kong vine extract. The components and the weight content include: 20-60% of King Kong vine extract, 10-80% of surfactant, and 0-70% of co-emulsifier. In the present invention, under the condition of mild stirring or gastrointestinal peristalsis, due to the existence of the surfactant, the emulsion is spontaneously emulsified to form milk droplets, and the appearance is clear. Carry out dissolution test by the dissolution determination method that Chinese Pharmacopoeia stipulates, take commercially available syrup as contrast, take distilled water as dissolution medium, take diosgenin as detection index, the result shows that King Kongteng Capsules of the present invention has good dissolution performance, and the dissolution rate Both the degree of concentration and the degree have increased significantly, indicating that it has the characteristics of fast absorption and high bioavailability in the body. The accelerated test results show that the disintegration time limit of the Jingangteng capsules of the present invention meets the requirements of the Pharmacopoeia.

Description

Self-emulsifying composition containing King Kong vine extract

technical field

The invention relates to a composition containing an extract of vine vine.

Background technique

King Kongteng is the rhizome of Liliaceae Smilax, which has the effects of clearing away heat and detoxification, reducing swelling and dispelling stagnation. It is mainly used clinically to treat lower abdominal pain, lumbago, and irregular menstruation caused by adnexal inflammation, adnexal inflammatory mass, and various gynecological inflammations. It is also used to treat rheumatic joint pain, bruises, cellulitis, gastroenteritis, etc.

However, the preparation products currently on the market are mainly syrups, and there are also tablets, capsules, etc., due to the slow and incomplete dissolution rate of active ingredients, resulting in poor absorption and insignificant curative effect.

Contents of the invention

The purpose of the present invention is to disclose a kind of self-emulsifying composition that contains King Kong vine extract, to overcome the above-mentioned defect that the prior art exists.

The components and weight content of the self-emulsifying composition containing the King Kong vine extract of the present invention include:

Vajra Rattan Extract 20～60%

Surfactant 10～80%

Co-emulsifier 0～70%

Preferred components and weight content:

Vajra Rattan Extract 30～50%

Surfactant 20～60%

Co-emulsifier 10～50%

Said King Kong vine extract can be prepared by known methods, such as the methods disclosed in CN03114644.9 patents.

Said surfactant is preferably a nonionic surfactant with lower toxicity, selected from polysorbate 20, polysorbate 80, sorbitan oleate, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, One or more of polyoxyethylene lauryl ether, polyoxyethylene cetyl ether, polyoxyethylene monolaurate or glyceryl caprate; preferably polyoxyethylene hydrogenated castor oil or polysorbate 20 ;

The main function of surfactant is to increase the hydrophilicity of King Kongteng extract and promote its absorption in the body. The greater the hydrophilic-lipophilic balance value HLB value of the surfactant, the greater the hydrophilicity, and the greater the effect. stronger.

The reason why surfactants can increase the solubility of poorly soluble drugs in water is generally believed to be the result of the formation of micelles (micelles) by surfactants in water. The micelle is a tiny oil droplet (non-polar central area) formed by the lipophilic group of the surfactant inward, while the hydrophilic group is outward (the non-ionic hydrophilic group is formed from the oil droplet). The surface extends into the water phase like waves) into a spherical body. It is now believed that the micelles can insert the slightly polar molecules of the solute into the oil droplets in the micelles with the non-polar part of the molecules, and the polar parts extend between the hydrophilic groups of the surfactant in the water resulting in solubilization.

Surfactants have the effect of dissolving lipids at low concentrations, and can dissolve phospholipids in the mucosa of the digestive tract to change the permeability of epithelial cells and reduce the barrier effect of lipid bodies in the intestinal mucosa. Therefore, many drugs that are difficult to absorb by passive diffusion are added with surfactants to increase the absorption. Therefore, the surfactant with a higher HLB value can not only increase the solubility of the extract in water, but also reduce the barrier effect of the intestinal mucosal lipid body and increase its absorption in the body.

Said co-emulsifier is selected from one or more of polyethylene glycol 400, polyethylene glycol 600, ethanol, propylene glycol, glycerin; preferably glycerin, polyethylene glycol 400 or polyethylene glycol 600. The addition of co-emulsifier can further promote the dissolution of the drug, reduce the interfacial tension, increase the fluidity of the interfacial film, and adjust the HLB value.

The preparation method of the self-emulsifying composition containing the extract of King Kong vine is very simple, and the conventional physical mixing method can be used to stir and mix the extract of King Kong vine, the surfactant and the co-emulsifier.

The present invention also relates to a capsule preparation containing a therapeutically effective amount of the above-mentioned self-emulsifying composition containing the extract of King Kong vine;

The capsule preparation of the present invention is prepared as follows: quantitatively mix the components according to the above ratio, stir at a certain temperature until the solution is clear, use a colloid mill or a high-pressure milk homogenizer to make the preparation easier, degas, and then use The capsule making machine can be used to fill the liquid medicine into the gelatin rubber, and it can also be filled into the hard capsule by the liquid capsule filling machine.

The self-emulsifying composition of King Kongteng of the present invention can be used to treat adnexitis, adnexal inflammatory mass and various gynecological inflammations caused by lower abdominal pain, lumbago, irregular menstruation, dysmenorrhea, yellow and thick leucorrhea, etc. Rheumatic joint pain, bruises, cellulitis, gastroenteritis and other diseases.

In the present invention, under the condition of mild stirring or gastrointestinal peristalsis, due to the existence of the surfactant, the emulsion is spontaneously emulsified to form milk droplets, and the appearance is clear.

Carry out test by the dissolution rate method that Chinese Pharmacopoeia stipulates, take the HCL of distilled water and 0.1mol/L respectively as medium, compare the dissolubility of King Kongteng Capsules of the present invention and commercially available syrup, the result shows that King Kongteng Capsules dissolution performance of the present invention Good, the dissolution rate and degree are significantly increased compared with the commercially available syrup, indicating that it has the characteristics of fast absorption and high bioavailability in the body. The accelerated test results show that the disintegration time limit of the Jingangteng capsules of the present invention meets the requirements of the Pharmacopoeia.

Detailed ways

Example 1

Preparation of King Kongtaw Extract:

Add 5 times the amount of 75% ethanol to the vine and soak it for 24 hours, extract it under reflux for 3 times, each time for 1 hour, combine the extracts, filter, concentrate the filtrate, dry it in vacuum, and crush it into a fine powder.

Example 2

Mix 100 grams of King Kong vine extract, 400 grams of polyethylene glycol, 200 grams of polyethylene glycol, 50 grams of glycerin, and 150 grams of polyoxyethylene hydrogenated castor oil, heat at 65 ° C, and stir at a speed of 500 rpm until the solution is clear and degassed. Compressed into 1000 capsules with a rotary mode capsule manufacturing machine, the content of the vine extract is 0.1 g/granule.

Example 4

Mix 200 grams of King Kong vine extract, 200 grams of capric laurate glyceride, and 400 to 300 grams of polyethylene glycol. After stirring evenly, grind it with a colloid mill until the solution is clear, degas, and press it into a gel with a rotary mode capsule making machine Pills 1000 capsules, the content of King Kongteng extract is 0.2 grams per capsule.

Example 5

Mix 300 grams of King Kong vine extract, 20 to 200 grams of polysorbate, 150 grams of glycerin capric acid laurate, and 100 grams of glycerin. After stirring evenly, grind it with a colloid mill until the solution is clear, degas, and press it with a rotary mode capsule making machine 1000 gelatinized pills, the content of King Kongteng extract is 0.3 g/capsule.

Example 6

Antibacterial effect in vitro

Prepare a range of concentrations (0.25, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 10.0, 15.0%) containing drug medium, nutrient agar medium for Staphylococcus aureus and Escherichia coli, and Neisseria gonorrhoeae for Neisseria gonorrhoeae Medium, Bengal red agar medium for Candida albicans. Take the commercially available syrup as the control group, compare the antibacterial effect with the capsule of the present invention, and inoculate the flat plate without medicine at the same time as the growth control. The result shows, does not contain drug flat plate bacterium growth is good, and the minimum inhibitory concentration (MIC) of King Kong rattan syrup to staphylococcus aureus is 1.0%, is 3.0% to the MIC of escherichia coli, and is 4.0% to the MIC of Neisseria gonorrhoeae , the antibacterial effect to Candida albicans is not obvious, and MIC is greater than 15.0%; The minimum inhibitory concentration (MIC) of staphylococcus aureus to the minimum inhibitory concentration (MIC) of the King Kong rattan capsule content of the present invention is 0.5%, and the MIC to escherichia coli is 1.0 %, the MIC for Neisseria gonorrhoeae is 3.0%, and the MIC for Candida albicans is 15.0%. Therefore the bacteriostasis of King Kongteng capsule of the present invention is much stronger than commercially available King Kongteng granules.

Example 7

anti-inflammatory effect

1. Effect of p-xylene on mouse ear swelling 50 mice, half male and half male, were randomly divided into 5 groups: normal saline group (negative control group); King Kongteng syrup group, 60g (crude drug)/kg; King Kongteng Capsule large, medium and small dose groups, 60g (crude drug)/kg, 40g/kg, 20g/kg. Each group was intragastrically administered for three days, and 1 hour after the last administration, the left ear of each mouse was smeared with 100% xylene (0.02mL/only), and it was executed after 15 minutes. Put a round ear piece on the same part and weigh it. The difference in weight between the two ear pieces is the degree of swelling. The results are shown in the following table, the Jingangteng capsules of the present invention have significantly better inhibitory effect on mouse ear swelling than the syrup group.

Table 1 King Kong rattan preparation on the impact of mouse ear swelling

group Dose (g/kg) Degree of swelling (mg) control / 2.1±3.0 Vajra Rattan Syrup 60 3.4±2.5 Vajra Rattan Capsules 60 3.0±1.9 40 5.3±2.7 20 6.1±1.2

2. 50 SD rats, half male and half male, were randomly divided into 5 groups: normal saline group (negative control group); King Kongteng syrup group, 60g (crude drug)/kg; King Kong rattan capsule large, medium and small dose groups, 60g (crude drug)/kg, 40g/kg, 20g/kg. The syrup group was fed with 2 mL/100g twice a day, and the other groups were fed with 1.2 mL/100g once a day for three consecutive days. 1h after the last administration, subcutaneously inject 1% carrageenan (0.1mL/rat) into the right hind foot of each rat, and measure the concentration of the rats before administration and 30, 60, and 120 minutes after the injection of carrageenan by volumetric method. The volume of the right hind paw was used to obtain the degree of swelling (volume after administration - volume before administration). The results are shown in the table below. The Jingangteng capsules of the present invention are significantly better than the syrup group in inhibiting effect on rat paw swelling.

Table 2 The effect of King Kongteng preparation on carrageenan-induced paw swelling in rats

group Dose (g/kg) 30min 60min 120min control / 0.45±0.12 0.54±0.21 0.75±0.27 Vajra Rattan Syrup 60 0.25±0.09 0.31±0.05 0.48±0.13 Vajra Rattan Capsules 60 0.20±0.15 0.27±0.06 0.45±0.11 40 0.26±0.06 0.31±0.15 0.50±0.24 20 0.30±0.14 0.35±0.08 0.52±0.18

Example 8

Analgesic effect

100 mice, half male and half male, were randomly divided into 5 groups, 20 in each group: normal saline group (negative control group); King Kongteng syrup group, 60g (crude drug)/kg; King Kongteng capsule large, medium and small dose groups , 60g (crude drug)/kg, 40g/kg, 20g/kg. It was fed once a day for a total of three days. One hour after the last feeding, 0.2 mL of 0.6% glacial acetic acid solution was injected intraperitoneally to the mice in each group, and the writhing reaction of the mice was observed within 20 minutes. Result is as following table, it can be seen that King Kong Teng capsule of the present invention is much stronger than the analgesic effect of syrup.

The analgesic effect of table 3 King Kong rattan preparation

group Dose (g/kg) Number of animals (only) Number of writhing reactions (only) Analgesic percentage (%) control group / 20 20 0 Vajra Rattan Syrup 60 20 8 60 Vajra Vine Capsules 60 20 4 80 40 20 9 55 20 20 14 30

Claims (4)

1. a kind of self-emulsifying composition containing King Kong vine extract, it is characterized in that, component and weight content comprise: Vajra Rattan Extract 20～60% Surfactant 10～80% Co-emulsifier 0～70% Said surfactant is selected from polysorbate 20, polysorbate 80, sorbitan oleate, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, polyoxyethylene lauryl ether, polyoxyethylene cetyl ether , one or more of polyoxyethylene monolaurate or capric laurate; preferably polyoxyethylene hydrogenated castor oil or polysorbate 20; Said co-emulsifier is selected from one or more of polyethylene glycol 400, polyethylene glycol 600, ethanol, propylene glycol or glycerin. 2. The self-emulsifying composition containing the radula vine extract according to claim 1, wherein said surfactant is selected from glycerin, polyethylene glycol 400 or polyethylene glycol 600. 3. the self-emulsifying composition containing the King Kong vine extract according to claim 1 and 2, is characterized in that, component and weight content are: Vajra Rattan Extract 30～50% Surfactant 20～60% Co-emulsifier 10-50%. 4. A capsule preparation containing a therapeutically effective amount of the self-emulsifying composition containing an extract of King Kong vine according to any one of claims 1 to 3.