A kind of endoscopy spasmolysis defoaming agent and preparation method thereof
Technical field
The invention belongs to endoscopy formulation art, in particular to a kind of endoscopy spasmolysis defoaming agent and its preparation.
Background technique
Medically the lesion situation in gastrointestinal tract is checked commonly using high definition scope, however mucus and foam in gastrointestinal tract
The visual field for usually influencing scope, leads to that minimal disease recall rate is low, the review time extends;Then the excess shrinkage of gastrointestinal tract also can
It prevents correctly to diagnose and can make the cancer site of small damage such as small size that can be missed.
In order to solve problem above present in endoscopic procedures, CN1893982A discloses a kind of containing menthol
Preparation, said preparation are emulsion, and containing l-menthol, surfactant and defoaming agent, said preparation is used to inhibit smooth muscle contraction,
And stability can be kept for a long time, shows high light transmittance.But antifoam content present in the emulsion is low, if
The content of defoaming agent is increased, the dissolubility of defoaming agent is reduced, can be precipitated from emulsion, and defoaming agent present in the emulsion is only
Bubble present in elimination emulsion use process, cannot eliminate existing bubble in gastric juice, clinically, better in order to reach
Defoaming effect, the emulsion also need in addition to be used together with defoaming agent, and defoaming effect is poor.
Summary of the invention
In order to solve the above technical problem, the present invention provides a kind of defoaming agents for being exclusively used in endoscopy, which can
To be used alone, while there is defoaming effect, also there is good light transmittance.
Specific technical solution of the present invention is as follows:
The present invention provides a kind of endoscopy spasmolysis defoaming agent, which includes each ingredient of following parts by weight:
L-menthol 1-3 surfactant 0.5-1
Defoaming component 0.05-0.1 pure water 65-75.
Further to improve, the defoaming component is 0.02-0.04 parts of sodium taurocholate and 0.03-0.06 parts of poly dimethyl
The mixture of siloxanes.
Further to improve, the sodium taurocholate and dimethyl silicone polymer form dispersion, the preparation side of the dispersion
Method are as follows: sodium taurocholate is placed in mortar, dimethyl silicone polymer is slowly added under grinding, grinds 20-30min, revolving speed is
500rmp reversely continues to grind 20-30min, revolving speed 500rmp, take out, cross 120 meshes, dispersion is made.
Further to improve, the surfactant includes each ingredient of following parts by weight:
Polyethylene glycol 1500 0.05-0.2 octadecyltrimethylammonium chloride 0.35-0.5
Sodium lactate 0.1-0.3.
Further to improve, the defoaming agent further includes the glycyrrhizin that parts by weight are 1-3 parts.
Another aspect of the present invention provides a kind of preparation method of endoscopy spasmolysis defoaming agent, which includes as follows
Step: surfactant being added in pure water, 7min is stirred at 500rmp, stands, l-menthol and defoaming component are added
Enter in above-mentioned solution, defoaming agent is made in ultrasound.
Preferably, the condition of the ultrasound are as follows: 15-20 DEG C, ultrasonic power 65-75w, ultrasonic time 3-5s, interval time
4-5s accumulates ultrasonic time 30-35min.
The present invention provides a kind of endoscopy spasmolysis defoaming agent, which has extraordinary suppression in gastrointestinal tract environment
Bubble ability, antifoaming speed is fast, and light transmittance is significantly better than existing emulsion and defoaming agent.
Specific embodiment
Embodiment 1
Embodiment 2
The sodium taurocholate and dimethyl silicone polymer form dispersion, the dispersion the preparation method comprises the following steps: by sodium taurocholate
It is placed in mortar, dimethyl silicone polymer is slowly added under grinding, grind 20min, revolving speed 500rmp reversely continues to grind
20min, revolving speed 500rmp take out, and cross 120 meshes, and dispersion is made.
Embodiment 3
The endoscopy spasmolysis defoaming agent the preparation method comprises the following steps:
Polyethylene glycol 1500, octadecyltrimethylammonium chloride and sodium lactate are added in pure water, stirred at 500rmp
7min to be mixed, is stood, l-menthol and sodium taurocholate and dimethyl silicone polymer are added in above-mentioned solution, defoaming agent is made in ultrasound,
The condition of ultrasound are as follows: 15 DEG C of ultrasonic temperature, ultrasonic power 65w, ultrasonic time 5s, interval time 4s, accumulate ultrasonic time
35min。
Embodiment 4
The sodium taurocholate and dimethyl silicone polymer form dispersion, the dispersion the preparation method comprises the following steps: by sodium taurocholate
It is placed in mortar, dimethyl silicone polymer is slowly added under grinding, grind 30min, revolving speed 500rmp reversely continues to grind
30min, revolving speed 500rmp take out, and cross 120 meshes, and dispersion is made.
The endoscopy spasmolysis defoaming agent the preparation method comprises the following steps:
Polyethylene glycol 1500, octadecyltrimethylammonium chloride and sodium lactate are added in pure water, stirred at 500rmp
7min is mixed, is stood, l-menthol and dispersion are added in above-mentioned solution, defoaming agent, ultrasonic condition is made in ultrasound are as follows: super
20 DEG C of sound temperature, ultrasonic power 75w, ultrasonic time 3s, interval time 4s, accumulate ultrasonic time 30min.
Embodiment 5
Embodiment 6
Embodiment 7
The endoscopy spasmolysis defoaming agent the preparation method comprises the following steps:
Polyethylene glycol 1500, octadecyltrimethylammonium chloride and sodium lactate are added in pure water, stirred at 500rmp
7min is mixed, is stood, l-menthol, sorbierite, polyacrylic acid, carbomer, sodium taurocholate and dimethyl silicone polymer are added above-mentioned
In solution, defoaming agent, ultrasonic condition is made in ultrasound are as follows: and 17 DEG C of ultrasonic temperature, ultrasonic power 70w, ultrasonic time 4s, interval
Time 5s accumulates ultrasonic time 35min.
Embodiment 8
The sodium taurocholate and dimethyl silicone polymer form dispersion, the dispersion the preparation method comprises the following steps: by sodium taurocholate
It is placed in mortar, dimethyl silicone polymer is slowly added under grinding, grind 30min, revolving speed 500rmp reversely continues to grind
30min, revolving speed 500rmp take out, and cross 120 meshes, and dispersion is made.
The endoscopy spasmolysis defoaming agent the preparation method comprises the following steps:
Polyethylene glycol 1500, octadecyltrimethylammonium chloride and sodium lactate are added in pure water, stirred at 500rmp
7min is mixed, is stood, l-menthol, sorbierite, polyacrylic acid, carbomer, dispersion are added in above-mentioned solution, ultrasound is made
Defoaming agent, ultrasonic condition are as follows: 16 DEG C of ultrasonic temperature, ultrasonic power 68w, ultrasonic time 4s, interval time 5s, when accumulation is ultrasonic
Between 35min.
Embodiment 9
The sodium taurocholate and dimethyl silicone polymer form dispersion, the dispersion the preparation method comprises the following steps: by sodium taurocholate
It is placed in mortar, dimethyl silicone polymer is slowly added under grinding, grind 30min, revolving speed 500rmp reversely continues to grind
30min, revolving speed 500rmp take out, and cross 120 meshes, and dispersion is made.
The endoscopy spasmolysis defoaming agent the preparation method comprises the following steps:
Polyethylene glycol 1500, octadecyltrimethylammonium chloride and sodium lactate are added in pure water, stirred at 500rmp
7min is mixed, is stood, l-menthol and dispersion and glycyrrhizin are added in above-mentioned solution, defoaming agent, ultrasonic item is made in ultrasound
Part are as follows: 20 DEG C of ultrasonic temperature, ultrasonic power 75w, ultrasonic time 3s, interval time 4s, accumulate ultrasonic time 30min.
Embodiment 10
Preparation method is the same as embodiment 9.
Embodiment 11
Preparation method is the same as embodiment 9.
Reference examples 1
Emulsion disclosed in the embodiment 1 of CN1893982A.
Reference examples 2
The preparation method of endoscopy spasmolysis defoaming agent is the same as embodiment 3.
Reference examples 3
The preparation method of endoscopy spasmolysis defoaming agent is the same as embodiment 3.
Reference examples 4
The preparation method of endoscopy spasmolysis defoaming agent is the same as embodiment 3.
Reference examples 5
The preparation method of endoscopy spasmolysis defoaming agent is the same as embodiment 3.
Reference examples 6
The preparation method of endoscopy spasmolysis defoaming agent is the same as embodiment 3.
Reference examples 7
The preparation method of endoscopy spasmolysis defoaming agent is the same as embodiment 5.
Reference examples 8
The preparation method of endoscopy spasmolysis defoaming agent is the same as embodiment 5.
Reference examples 9
The preparation method of endoscopy spasmolysis defoaming agent is the same as embodiment 5.
Reference examples 10
Preparation method is the same as embodiment 9.
Reference examples 11
Preparation method is the same as embodiment 9.
Reference examples 12
Preparation method is the same as embodiment 9.
The experiment of 1 defoaming capacity of experimental example
According to the method configuration simulated gastric fluid and simulated intestinal fluid in 2,010 2 annex XA of Chinese Pharmacopoeia:
Simulated gastric fluid: taking dilute hydrochloric acid 16.4mL, and water about 800mL and pepsin 10g is added to be diluted with water into after shaking up
1000mL to get.
Simulated intestinal fluid: i.e. phosphate buffer (containing pancreatin) (pH6.8).
30mL bottle is taken, is divided into four groups, first group and second group of each bottle and places simulated gastric fluid 10mL;Third group and
Four groups of each bottle places simulated intestinal fluid 10mL, and then first group and third group are put into the embodiment of the present invention and reference examples in 25 DEG C
The defoaming agent 10mL of offer, second group and the 4th group is put into the defoaming agent that the embodiment of the present invention and reference examples provide at 37 DEG C
10mL, each group keep temperature, vibrate 1min on oscillator (200r/min), after 1min, measure foam vanishing time T and light transmission
Rate Y, the results are shown in Table 1.
The defoaming capacity experimental result of each embodiment of table 1 and reference examples
As can be seen from the table, endoscopy spasmolysis defoaming agent provided by the invention is in simulated gastric fluid, simulated intestinal fluid, and
25 DEG C or 37 DEG C are detected, and light transmittance is significantly better than control group, and foam time is significantly lower than control group, and from control
The experimental data of example 1 can be seen that reference examples 1 offer emulsion pH be 7, and temperature be 25 DEG C when, with fine light transmission
Rate, and foam time is short, and in 37 DEG C or simulated gastric fluid, light transmittance is significantly lower than defoaming agent provided by the present application, and
Foam time significantly extends.And as can be seen from the above table, defoaming component significantly affects foam time, the significant shadow of surfactant
Ring light transmittance.
Obtain as a result, endoscopy spasmolysis defoaming agent provided by the invention for carry out gastrointestinal endoscopy when, Ke Yixian
It writes and improves gastrointestinal endoscopy light transmittance, and significantly shorten foam time.
2 adsorption experiment of experimental example
The protein solution for being 1.0mg/mL with phosphate buffer (pH6.8) configuration gastrointestinal tract protein concentration, incite somebody to action this respectively
Defoaming agent (microspheres amount 0.3g) addition for inventing the embodiment and reference examples that provide is placed in containing protein solution (0.3mL)
In test tube, (120r/min) 4h is vibrated in 37 DEG C of constant temperature oscillator, then measures protein content in solution.Before absorption
The amount of albumen calculates the protein adsorption quantity on microballoon, protein adsorption rate=(protein content after starting protein content -4h)/starting albumen afterwards
Amount * 100%, each group is shown in Table 2 to the adsorption rate of albumen.
The Adsorption experimental results of table 2 each embodiment and reference examples
Sample |
Adsorption rate (%) |
Embodiment 7 |
45.6 |
Reference examples 7 |
0 |
Reference examples 8 |
2.3 |
Reference examples 9 |
8.3 |
As can be seen from the table, defoaming agent provided by the invention has certain suction-operated to gastrointestinal tract albumen, thus
It can be concluded that defoaming agent provided by the invention can have the effect of certain adhesion protein, can will adhere in intestinal wall
In protein adsorption to defoaming agent, the clarity to gastrointestinal examination is further improved, improves the accuracy of inspection.
Experimental example 3 inhibits spasm experiment
SD rat, weight 200-250g, male;
Rat is divided into 6 groups, is respectively administered 1 group, is administered 2 groups, compares 1 group, 2 groups of control, control 3 groups and blank control
Group after fasting 12h, is administered as follows:
The defoaming agent 5mL of 1 group of gastric infusion embodiment of the present invention 1 is administered;
The defoaming agent 5mL of 2 groups of gastric infusion embodiment of the present invention 9 is administered;
Compare the defoaming agent 5mL of 1 group of gastric infusion reference examples 10 of the present invention;
Compare the defoaming agent 5mL of 2 groups of gastric infusions reference examples 11 of the present invention;
Compare the defoaming agent 5mL of 3 groups of gastric infusions reference examples 12 of the present invention;
Blank control group gives isometric physiological saline.
=(mean tension after being administered to mean tension one after KCl)/is calculated, inhibiting rate (%) using existing method (gives KCl
One rest tension of mean tension afterwards) × 100%, each group inhibiting rate the results are shown in Table 3.
The spasm inhibition assay result of 3 each group of table
Group |
Inhibiting rate (%) |
Blank control group |
7.56±1.23 |
It is administered 1 group |
65.94±2.37 |
It is administered 2 groups |
90.68±5.66 |
Compare 1 group |
22.38±2.82 |
Compare 2 groups |
60.32±1.57 |
Compare 3 groups |
61.55±2.96 |
As can be seen from the table, defoaming agent provided in an embodiment of the present invention there is significant inhibition to make the spasm of colon
With as can be seen from the table, glycyrrhizin and l-menthol have synergistic effect.