CN110327471A - A kind of endoscopy spasmolysis defoaming agent and preparation method thereof - Google Patents

A kind of endoscopy spasmolysis defoaming agent and preparation method thereof Download PDF

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Publication number
CN110327471A
CN110327471A CN201910677597.6A CN201910677597A CN110327471A CN 110327471 A CN110327471 A CN 110327471A CN 201910677597 A CN201910677597 A CN 201910677597A CN 110327471 A CN110327471 A CN 110327471A
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defoaming agent
endoscopy
spasmolysis
parts
preparation
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CN110327471B (en
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李苏
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Beijing Yiliya Medical Technology Co.,Ltd.
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Beijing Gefei Medical Devices Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention provides a kind of endoscopy spasmolysis defoaming agent and preparation method thereof, the defoaming agent is made of the l-menthol of 1-3,0.5-1 parts of surfactant, 0.05-0.1 parts of defoaming agent and 65-75 parts of pure water, endoscopy spasmolysis defoaming agent provided by the invention can have extraordinary foam inhibition ability in gastrointestinal tract environment, antifoaming speed is fast, and light transmittance is significantly better than existing emulsion.

Description

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.

Claims (8)

1. a kind of endoscopy spasmolysis defoaming agent, which is characterized in that the defoaming agent 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.
2. endoscopy spasmolysis defoaming agent as described in claim 1, which is characterized in that the defoaming component is 0.02-0.04 The sodium taurocholate of part and the mixture of 0.03-0.06 parts of dimethyl silicone polymer.
3. endoscopy spasmolysis defoaming agent as claimed in claim 2, which is characterized in that the sodium taurocholate and polydimethylsiloxanes Alkane forms dispersion, the dispersion the preparation method comprises the following steps: sodium taurocholate is placed in mortar, be slowly added to poly dimethyl under grinding Siloxanes grinds 20-30min, revolving speed 500rmp, reversely continues to grind 20-30min, revolving speed 500rmp, take out, crosses 120 Dispersion is made in mesh.
4. endoscopy spasmolysis defoaming agent as described in claim 1, which is characterized in that the surfactant includes following weight Measure each ingredient of part:
Polyethylene glycol 1500 0.05-0.2 octadecyltrimethylammonium chloride 0.35-0.5 sodium lactate 0.1-0.3.
5. endoscopy spasmolysis defoaming agent as described in claim 1, which is characterized in that the defoaming agent further includes that parts by weight are 0.01-0.05 parts of sorbierite, 0.2-0.4 parts of polyacrylic acid and 0.7-1.2 parts of carbomer.
6. endoscopy spasmolysis defoaming agent as described in claim 1, which is characterized in that the defoaming agent further includes that parts by weight are 1-3 parts of glycyrrhizin.
7. a kind of preparation method of endoscopy spasmolysis defoaming agent described in claim 1, which is characterized in that the method includes Following steps: surfactant being added in pure water, 7min is stirred at 500rmp, is stood, by l-menthol and defoaming group Divide and be added in above-mentioned solution, defoaming agent is made in ultrasound.
8. preparation method as claimed in claim 7, which is characterized in that the condition of the ultrasound are as follows: 15-20 DEG C of ultrasonic temperature, Ultrasonic power 65-75w, ultrasonic time 3-5s, interval time 4-5s accumulate ultrasonic time 30-35min.
CN201910677597.6A 2019-01-24 2019-07-25 Antispasmodic agent for endoscopy and preparation method thereof Active CN110327471B (en)

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1893982A (en) * 2003-06-30 2007-01-10 日本制药株式会社 Menthol-containing preparation
US20070148099A1 (en) * 2005-12-27 2007-06-28 Burke Susan E Use of aroma compounds as defoaming agents for ophthalmic solutions with high concentrations of surfactants
CN103110961A (en) * 2012-11-30 2013-05-22 江苏唯德康医疗科技有限公司 Preparation method of high-definition endoscope mucus-removal defoaming composite preparation
CN106177971A (en) * 2016-07-20 2016-12-07 贵州理工学院 Potato starch capsule shells containing menthol

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1893982A (en) * 2003-06-30 2007-01-10 日本制药株式会社 Menthol-containing preparation
CN102038963A (en) * 2003-06-30 2011-05-04 日本制药株式会社 Method for preparing a stabilised menthol emulsion
US20070148099A1 (en) * 2005-12-27 2007-06-28 Burke Susan E Use of aroma compounds as defoaming agents for ophthalmic solutions with high concentrations of surfactants
CN103110961A (en) * 2012-11-30 2013-05-22 江苏唯德康医疗科技有限公司 Preparation method of high-definition endoscope mucus-removal defoaming composite preparation
CN106177971A (en) * 2016-07-20 2016-12-07 贵州理工学院 Potato starch capsule shells containing menthol

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
H.-G. GRIGOLEIT ET AL: ""Pharmacology and preclinical pharmacokinetics of peppermint oil"", 《PHYTOMEDICINE》 *
曾玉兰: ""多效内窥镜乳的制备及质量控制"", 《北方药学》 *

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