Anti-flocculation defoaming agent for digestive tract mucosa in gastroscopy and preparation method of anti-flocculation defoaming agent

Abstract

The invention discloses an anti-flocculation defoaming agent for digestive tract mucosa in gastroscopy and a preparation method of the anti-flocculation defoaming agent, and relates to the technical field of medicines, and the anti-flocculation defoaming agent comprises simethicone emulsion, sodium bicarbonate and sterilized water for injection. 80mg of simethicone emulsion is combined with 40ml of 2.5% sodium bicarbonate solution (containing 1000mg of sodium bicarbonate) to be used for preparation before gastroscopy, flocculent precipitation can be prevented and the gastric mucosa cleaning effect can be improved by using a small dose of simethicone emulsion, and the simethicone emulsion is simple to use, can be rapidly prepared, is low in cost and high in cost performance, and reduces the medical cost.

Description

Technical Field

[0001] The present invention relates to the technical field of medicine, and in particular to a digestive tract mucosa anti-flocculation and anti-foaming agent for gastroscopy and a preparation method thereof. Background Art

[0002] Gastroscopy is an important tool for diagnosing upper gastrointestinal diseases. Besides the physician's experience, competence, meticulousness, examination time, patient cooperation, endoscope performance, and image quality, endoscopic visual clarity significantly impacts the accuracy of endoscopic diagnosis. Foam and mucus adhering to the surface of the normal gastric mucosa can hinder mucosal observation and the detection of early lesions. Therefore, removing foam and mucus from the gastric mucosa before endoscopy is a crucial measure to ensure clear endoscopic vision. Simethicone, a nonionic surfactant, reduces the surface tension of bubbles, promoting their collapse. Orally administered, it is not absorbed and is a commonly used defoaming agent in preoperative preparation. International guidelines recommend oral administration of simethicone or acetylcysteine ​​before endoscopy. Domestically, the use of simethicone is also recommended, but there are no clear recommendations on dosage and method. However, clinical practice has shown that simethicone can cause flocculation, significantly impairing endoscopic visualization of the esophageal and gastric mucosa. In the research reports on the use of simethicone, most domestic literature recommends the use of combined pronase. The research methods are mostly to compare the effects of simethicone combined with pronase with the use of simethicone alone. The dosage of simethicone used is usually too high. Clinical work has found that larger doses will produce flocculent precipitates. Pronase is a proteinase produced by Streptomyces griseus. Its working principle is to cut the peptide bonds of glycoproteins in gastric mucus, reduce its viscosity, and then dissolve it to improve the clarity of gastroscopy.

[0003] With reference to the prior art publication number CN115400228A, a Chinese invention patent discloses "a gastrointestinal mucosal anti-flocculation and defoaming agent for gastroscopy and its preparation method, comprising 400 mg of simethicone, 20,000 U-24,000 U of pronase, 1.6 g-2.0 g of a weakly alkaline substance such as sodium bicarbonate, 30 ml of water at 30°C-35°C, and 1.0 g-1.3 g of xylitol. This formula has a wider range of applications. After all patients undergoing gastroscopy took the defoaming agent of this formula 5-30 minutes before the operation, no case of defoaming agent flocculating and agglomerating in the esophagus and stomach occurred. The static time of this formula can reach 3 hours without changing the pH value. Nurses can centrally configure it according to the number of patients, effectively saving the manpower and time required for the configuration process and procedure. Compared with the prior art, this formula has a normal and appropriate gastroscopy operation time, avoiding the gastroscopy caused by the flocculation and agglomeration of white flocculent precipitates in the stomach and the need for repeated flushing. Compared with existing technologies, this formulation enhances endoscopic gastric mucosal visibility, with 90% of cases receiving a Grade A endoscopic visibility score and no cases receiving a Grade C or D score. This improves the screening rate for microscopic lesions in the esophageal and gastric mucosa, as well as the detection rate for precancerous lesions and early cancer. The aforementioned protocol discloses the combined use of simethicone, pronase, a weakly alkaline substance, and xylitol. While this approach can prevent flocculation and agglomeration in the stomach, it uses a large number of pharmaceutical ingredients, is complex to prepare, and is costly. Pronase granules cost approximately 70 yuan, increasing patient medical costs. Regarding the combined use of pronase granules with simethicone, please refer to the relevant protocol ("Study on the Effectiveness of Pronase Combined with Simethicone Emulsion for Preoperative Preparation for Gastroscopy," Chen Jing et al., Chinese Journal of Hospital Drug Evaluation and Analysis, Vol. 19, No. 6, pp. 708-710).

[0004] Reference can also be made to the prior art publication number CN107441508B, which discloses "a simethicone composition, characterized in that the composition comprises simethicone and acetylcysteine, wherein, in terms of weight percentage, simethicone: acetylcysteine ​​= 65:1000 to 95:1000. The ratio of the composition is more reasonable, and it can maximize its defoaming and mucus removal functions, and it has strong light transmittance after being dissolved in water, which improves the clarity of the clinician's field of view during endoscopic examination and reduces missed or misdiagnosed cases." This method uses a combination of simethicone and acetylcysteine. Acetylcysteine ​​is a mucolytic agent. The thiol group in its molecular structure breaks the disulfide bonds between mucin molecular complexes, and has a good dissolving effect on mucus in the respiratory tract and digestive tract. However, according to the preparation method, there are requirements for temperature and carrier materials, and the particles must be prepared and dried, and cannot be quickly prepared during gastroscopy. In addition, the cost is still relatively high, which increases medical costs. Summary of the Invention

[0005] The purpose of the present invention is to provide a gastrointestinal mucosal anti-flocculation and anti-foaming agent for gastroscopy and a preparation method thereof in order to solve the above problems.

[0006] The present invention achieves the above-mentioned purpose through the following technical solutions:

[0007] The invention discloses an anti-flocculation and anti-foaming agent for the digestive tract mucosa during gastroscopy, comprising simethicone emulsion, sodium bicarbonate and sterile water for injection.

[0008] Furthermore, it contains 80 mg of simethicone emulsion and 40 ml of 2.5% sodium bicarbonate solution containing 1000 mg of sodium bicarbonate.

[0009] The present application also provides a method for preparing a gastrointestinal mucosal anti-flocculation and anti-foaming agent for gastroscopy.

[0010] S1: Add 25g of sodium bicarbonate tablets to 1000ml of sterile water for injection to prepare a 2.5% sodium bicarbonate dilution solution;

[0011] S2: Take 40 ml of the prepared 2.5% sodium bicarbonate diluted solution, containing 1000 mg of sodium bicarbonate, add 80 mg of simethicone emulsion, mix well, and obtain an anti-flocculation and defoaming agent.

[0012] The beneficial effect is that: this application uses 80 mg of simethicone emulsion combined with 40 ml of 2.5% sodium bicarbonate solution (containing 1000 mg of sodium bicarbonate) for preparation before gastroscopy. A small dose can prevent flocculent precipitation and improve the cleaning effect of gastric mucosa. It is simple to use, can be quickly prepared, has low cost, high cost performance, and reduces medical costs. BRIEF DESCRIPTION OF THE DRAWINGS

[0013] Figure 1 This is a picture of the gastric mucosa of the first group of experimental patients of the present invention (no foam on the surface of the gastric mucosa, and grayish white flocculent precipitation can be seen in the gastric body of all three cases);

[0014] Figure 2 This is a picture of the gastric mucosa of the second group of experimental patients of the present invention (off-white flocculent precipitation can be seen on the surface of the gastric mucosa);

[0015] Figure 3 This is a picture of the gastric mucosa of the third group of experimental patients of the present invention (the gastric mucosal surface is clean, without foam or flocculent precipitation);

[0016] Figure 4 This is a picture of the gastric mucosa of the fourth group of experimental patients of the present invention (the gastric mucosal surface is clean, without foam or flocculent precipitation). DETAILED DESCRIPTION

[0017] To make the objectives, technical solutions, and advantages of the present invention more apparent, the technical solutions of the present invention will be described in detail below. Obviously, the embodiments described are only some of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other implementations obtained by those of ordinary skill in the art without inventive effort are within the scope of protection of the present invention.

[0018] The invention provides a gastrointestinal mucosal anti-flocculation and anti-foaming agent for gastroscopy, comprising simethicone emulsion, sodium bicarbonate and sterile water for injection.

[0019] Furthermore, it includes 80 mg of simethicone emulsion and 40 ml of 2.5% sodium bicarbonate solution containing 1000 mg of sodium bicarbonate.

[0020] The present application also provides a method for preparing a gastrointestinal mucosal anti-flocculation and anti-foaming agent for gastroscopy.

[0021] S1: Add 25g of sodium bicarbonate tablets to 1000ml of sterile water for injection to prepare a 2.5% sodium bicarbonate dilution solution;

[0022] S2: Take 40 ml of the prepared 2.5% sodium bicarbonate diluted solution, containing 1000 mg of sodium bicarbonate, add 80 mg of simethicone emulsion, mix well, and obtain an anti-flocculation and defoaming agent.

[0023] Using the above scheme, simethicone can reduce the surface tension of bubbles and promote the collapse of bubbles. Different doses of simethicone can improve the visibility of the mucosa under gastroscopy. The larger the dose, the better the effect. However, if the amount of sodium bicarbonate used cannot be accurately controlled, the agglomeration of white flocs will also increase significantly. Currently, many schemes often use 1.6g-2.0g of sodium bicarbonate per person to neutralize the gastric acid secreted in the human body, especially in the fasting state. The increased gastric acid secretion makes the pH value in the human body reach 5-8, which also provides conditions for the action environment of pronase. However, what is always thought of in current research is that simethicone should be used in combination with pronase or acetylcysteine ​​under alkaline conditions to reduce the chance of white flocs agglomerating in the mucosa. It has not been thought that simethicone emulsion and sodium bicarbonate can be used alone to prevent the formation of white flocs. In this application, a 2.5% sodium bicarbonate solution containing 1000 mg of sodium bicarbonate is used, 40 ml of 2.5% sodium bicarbonate solution is taken and evenly mixed with 80 mg of simethicone emulsion, and the mixture is taken at room temperature to neutralize the gastric acid in the human body to a condition of about neutrality. Then the simethicone emulsion acts to produce a significant cleaning effect in the digestive tract.

[0024] The present application provides the following examples and comparative examples:

[0025] (1) Materials used: Simethicone emulsion, sterile water for injection, sodium bicarbonate tablets, and acetylcysteine ​​solution for inhalation.

[0026] Among them, simethicone emulsion: 30ml / bottle, containing 1200mg of simethicone, Yuanda Life Sciences (Wuhan) Co., Ltd., approval number H20223383, product batch number 72307251; sterile water for injection: 500ml / bottle, Shijiazhuang Siyao Co., Ltd., national medicine standard number H20046572, production batch number 2306133202; sodium bicarbonate tablets: 100 tablets / bottle, 0.5g / tablet, Fuzhou Ocean Pharmaceutical Co., Ltd., national medicine standard number H35021110, product batch number 23063020; acetylcysteine ​​solution for inhalation, 3ml: 300mg / ampoule, Hainan Star Pharmaceutical Co., Ltd., national medicine standard number H20183005, product batch number 2307115B. The main instruments used are: Olympus GI F-H290Z gastroscope, Fuji EG-600WR gastroscope, and all gastroscopes used have the function of supplying water.

[0027] (2) Select multiple clinical trials:

[0028] Group 1: 40 mL of sterile water, added with 80 mg (2 mL) of simethicone emulsion;

[0029] Group 2: 40 mL of sterile water, added with 80 mg (2 mL) of simethicone emulsion and 600 mg (6 mL) of acetylcysteine ​​solution for inhalation (light pink liquid);

[0030] Group 3: 40 mL of 2.5% sodium bicarbonate solution (containing 1000 mg of sodium bicarbonate) plus 80 mg of simethicone emulsion;

[0031] Group 4: 2.5% sodium bicarbonate solution (containing 1000 mg of sodium bicarbonate) 40 mL, added with 80 mg of simethicone emulsion and 600 mg of acetylcysteine ​​(light pink liquid)

[0032] (III) Instructions: Patients should abstain from food and water for at least 6-8 hours before the gastroscopy. 10-30 minutes before the gastroscopy, the dispensing nurse will measure and prepare the liquid medication in a special opaque container and instruct the patient to take it orally. After taking the medication, the nurse will instruct the patient to bend over and shake their body, and to turn 360 degrees in bed.

[0033] Professional anesthesiologists administered intravenous anesthesia (using propofol or etomidate), along with routine nasal cannula oxygenation and ECG monitoring. Four senior endoscopists, who had undergone a week of training, performed gastroscopy procedures, and nursing staff recorded the procedures and observed indicators.

[0034] (IV) Observational Indicators: The primary endpoint was endoscopic visual clarity. The Crema Stomach Cleaning Score (CSCS) was used to grade the cleanliness of the gastric antrum, body, and fundus based on the presence of foam, mucus, or flocculent deposits in the endoscopic observation area, as well as the number of endoscopic water flushes required. The stomach was divided into the antrum, body, and fundus for cleanliness assessment, with each area scored on a scale of 1 to 3. The sum of the scores for the three areas formed the overall score, with a score of ≥6 indicating satisfactory endoscopic visual clarity and a score of <6 indicating unsatisfactory endoscopic visual clarity. A secondary endpoint was the presence of flocculent deposits in the gastric cavity, defined as the presence of grayish-white floccules under the microscope.

[0035] (V) Statistical methods: SPSS 20.0 statistical software was used for statistical analysis. x The data were expressed as ±s. The comparisons between the two groups were performed with t-test or analysis of variance. The enumeration data were expressed as cases (%) and were performed with χ2 test or Fisher's exact test. P < 0.05 indicated statistically significant differences.

[0036] (VI) Case selection: A total of 342 patients were included, including 77 patients in group 1 (34 males and 43 females, with a mean age of (57.06±11.34) years); 80 patients in group 2 (37 males and 43 females, with a mean age of (56.84±11.94) years); 90 patients in group 3 (42 males and 48 females, with a mean age of (55.96±10.92) years); and 95 patients in group 4 (41 males and 54 females, with a mean age of (56.03±12.05) years. There was no statistically significant difference in gender among the four groups (P>0.05), indicating that the four groups were comparable.

[0037] (VII) Comparison of gastroscopic visual field clarity:

[0038] The mean CSCS scores for endoscopic visual clarity in the four groups were 5.52±1.54, 5.56±1.51, 7.53±1.34, and 7.82±1.15, respectively. There was no significant improvement in gastric mucosal cleanliness in Group 2 compared with Group 1, and no statistically significant difference in endoscopic visual clarity scores between the two groups was observed (Table 1).

[0039] The gastric mucosal cleanliness of Groups 1 and 2 without sodium bicarbonate was poor, and the difference was statistically significant compared with Groups 3 and 4 with sodium bicarbonate, as shown in Table 1.

[0040] The gastric mucosal surface cleanliness of patients in groups 3 and 4 was good, and no flocculent precipitation occurred. The patients in group 4 who added acetylcysteine ​​had the highest CSCS score for gastroscopic visual clarity, but there was no statistically significant difference between the two groups (see Table 1).

[0041] Table 1: Comparison of CSCS scores of gastroscopic visual field clarity among four groups of patients

[0042]

[0043] The proportion of patients with a gastroscopic visual field clarity score of 9 points in Group 3 and Group 4 was observed. In Group 3, there were 26 patients with a score of 9 points, accounting for 28.89%; in Group 4, there were 36 patients with a score of 9 points, accounting for 37.89%. The proportion of patients with a score of 9 points increased significantly after adding acetylcysteine, but the difference was not statistically significant.

[0044] Reference Attachment Figure 1 As shown:

[0045] Observe the formation of flocculent precipitation in the gastric cavity after oral administration of simethicone emulsion: obvious flocculent precipitation was observed in most of the groups 1 and 2, which affected gastroscopy observation; flocculent precipitation was rarely observed in the groups 3 and 4 containing sodium bicarbonate. Figure 1 Because it is difficult to strictly distinguish between flocculent precipitates, mucus patches, and thick foam, this study did not perform quantitative data analysis. During the observation process, the number of times and time required for physicians to flush the visual field decreased significantly, and satisfaction with visual clarity increased significantly, facilitating the observation of subtle mucosal lesions.

[0046] Compared with the existing technology, this application uses 80 mg of simethicone emulsion and 40 ml of 2.5% sodium bicarbonate solution (containing 1000 mg of sodium bicarbonate) for use before gastroscopy. It can achieve the purpose of cleaning the digestive tract, provide a clear field of vision, and facilitate the observation of subtle mucosal lesions. This solution is low in cost, simple to use, and cost-effective.

[0047] Based on the observation results of the experiment in this application, 80 mg of simethicone combined with 1000 mg of sodium bicarbonate can be used for preparation before gastroscopy to prevent flocculent precipitation and improve the cleaning effect of gastric mucosa.

[0048] The above description is merely a specific embodiment of the present invention, but the scope of protection of the present invention is not limited thereto. Any modifications or substitutions that can be easily conceived by a person skilled in the art within the technical scope disclosed in the present invention should be included within the scope of protection of the present invention. Therefore, the scope of protection of the present invention should be based on the scope of protection of the claims.

Claims

1. A gastrointestinal mucosal anti-flocculation and anti-foaming agent for gastroscopy, characterized in that: Includes simethicone emulsion, sodium bicarbonate and sterile water for injection.

2. The anti-flocculation and anti-foaming agent for the digestive tract mucosa in gastroscopy according to claim 1, characterized in that: Includes 80 mg of simethicone emulsion and 40 ml of 2.5% sodium bicarbonate solution containing 1000 mg of sodium bicarbonate.

3. A method for preparing a gastrointestinal mucosal anti-flocculation and anti-foaming agent for gastroscopy, characterized in that: S1: Add 25g of sodium bicarbonate tablets to 1000ml of sterile water for injection to prepare a 2.5% sodium bicarbonate dilution solution; S2: Take 40 ml of the prepared 2.5% sodium bicarbonate dilution solution, containing 1000 mg of sodium bicarbonate, add 80 mg of simethicone emulsion, mix well, and obtain an anti-flocculation and defoaming agent.

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