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CN118903170A - Application of trachelospermin in preparation of diarrhea treatment medicine - Google Patents

Application of trachelospermin in preparation of diarrhea treatment medicine Download PDF

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Publication number
CN118903170A
CN118903170A CN202410905072.4A CN202410905072A CN118903170A CN 118903170 A CN118903170 A CN 118903170A CN 202410905072 A CN202410905072 A CN 202410905072A CN 118903170 A CN118903170 A CN 118903170A
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diarrhea
group
mice
glycoside
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柯仲成
程小玲
程子洋
李长江
程旭
牛怡敏
杨惠敏
叶婷
万芳瑶
朱紫彤
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Huangshan University
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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
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61P1/12Antidiarrhoeals
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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Abstract

The invention discloses application of trachelospermi glycoside in preparation of a medicament for treating diarrhea. Compared with the prior art, the invention discovers that the trachelospermi glycoside can treat diarrhea for the first time. Proved by experimental study, the trachelospermi glycoside can effectively reduce the loose stool rate and the diarrhea rate of diarrhea mice, and improve the weight, the feed intake and the water intake of the diarrhea mice. Therefore, the trachelospermine glycoside can be used for treating diarrhea, and has remarkable effect. In conclusion, the trachelospermi glycoside can be used for preparing the medicine for treating diarrhea, and has good market potential and value.

Description

络石苷在制备治疗腹泻药物中的应用Application of trachelosidin in the preparation of drugs for treating diarrhea

技术领域Technical Field

本发明属于药物新用途技术领域,特别涉及络石苷在制备治疗腹泻药物中的应用。The invention belongs to the technical field of new drug applications, and particularly relates to the application of trachelosidoside in the preparation of drugs for treating diarrhea.

背景技术Background Art

腹泻是一种常见的消化系统疾病,其定义为每日排便次数超过正常频率,并且粪质稀薄、水分增加,可能含有未消化的食物或脓血、黏液。腹泻可以分为急性腹泻和慢性腹泻,急性腹泻通常与肠道感染有关,而慢性腹泻则可能由多种原因引起,包括肠道疾病、消化和吸收不良、肿瘤等。Diarrhea is a common digestive system disease, which is defined as more bowel movements per day than normal, and the stool is thin and has increased water content, which may contain undigested food or pus, blood, and mucus. Diarrhea can be divided into acute diarrhea and chronic diarrhea. Acute diarrhea is usually related to intestinal infection, while chronic diarrhea may be caused by a variety of reasons, including intestinal diseases, malabsorption and digestion, tumors, etc.

腹泻的症状包括腹痛、腹泻次数增加、发热和消瘦等。腹痛通常出现在腹泻开始时,排便后可能有所缓解。急性腹泻可能导致每日排便次数显著增加,粪便稀薄,有时可能伴有血和脓液。腹泻还可能引起发热,这在急性细菌性痢疾等感染性腹泻中尤为常见。慢性腹泻,如由胃肠道恶性肿瘤引起,可能影响营养吸收,导致消瘦。Symptoms of diarrhea include abdominal pain, increased frequency of diarrhea, fever, and weight loss. Abdominal pain usually occurs at the beginning of diarrhea and may be relieved after a bowel movement. Acute diarrhea may cause a significant increase in the number of bowel movements per day, with loose stools that may sometimes contain blood and pus. Diarrhea may also cause fever, which is especially common in infectious diarrhea such as acute bacillary dysentery. Chronic diarrhea, such as caused by gastrointestinal malignancies, may affect nutrient absorption and lead to weight loss.

腹泻的原因多种多样,包括疾病因素、药物因素、遗传因素、环境因素和生活方式等。疾病因素中,食物中毒、急性肠道感染、炎症性肠病。治疗腹泻需要根据病因进行。对于急性腹泻,补充液体和电解质以预防脱水是关键。对于由感染引起的腹泻,可能需要使用抗感染药物。对于慢性腹泻,治疗主要针对具体的病因,同时保障病人的营养摄入。此外,保持良好的卫生习惯、注意食水安全、避免滥用药物等也有助于预防腹泻的发生。There are many causes of diarrhea, including disease factors, drug factors, genetic factors, environmental factors and lifestyle. Among the disease factors, there are food poisoning, acute intestinal infection, and inflammatory bowel disease. Treatment of diarrhea needs to be based on the cause. For acute diarrhea, replenishing fluids and electrolytes to prevent dehydration is key. For diarrhea caused by infection, anti-infective drugs may be required. For chronic diarrhea, treatment is mainly targeted at the specific cause while ensuring the patient's nutritional intake. In addition, maintaining good hygiene habits, paying attention to water safety, and avoiding drug abuse can also help prevent the occurrence of diarrhea.

总之,腹泻是一种常见的消化系统疾病,其症状多样,原因复杂。对于腹泻的治疗和预防,需要综合考虑病因、症状和个人情况,采取针对性的措施。目前并未发现络石苷能够治疗腹泻的相关研究。In short, diarrhea is a common digestive system disease with diverse symptoms and complex causes. For the treatment and prevention of diarrhea, it is necessary to comprehensively consider the cause, symptoms and personal situation and take targeted measures. At present, no relevant research has been found that trachelosyl glycoside can treat diarrhea.

发明内容Summary of the invention

发明目的:为了解决现有技术的缺陷,本发明提供了络石苷在制备治疗腹泻药物中的应用。Purpose of the invention: In order to solve the defects of the prior art, the present invention provides the use of trachelosidone in the preparation of drugs for treating diarrhea.

技术方案:为达到上述发明目的,本发明采用以下技术方案:Technical solution: In order to achieve the above-mentioned invention object, the present invention adopts the following technical solution:

第一方面,本发明提供了络石苷在制备治疗腹泻药物中的应用。In a first aspect, the present invention provides the use of trachelosidoside in the preparation of a drug for treating diarrhea.

具体地,所述腹泻为大肠杆菌感染所引起的腹泻。Specifically, the diarrhea is diarrhea caused by Escherichia coli infection.

作为优选方案,所述络石苷作为唯一活性成分在制备治疗腹泻药物中的应用。As a preferred embodiment, the trachelosidoside is used as the sole active ingredient in the preparation of a drug for treating diarrhea.

作为具体实施方案,所述治疗腹泻药物为口服药物或者注射药物。As a specific embodiment, the drug for treating diarrhea is an oral drug or an injectable drug.

第二方面,本发明提供了包含络石苷的组合物在制备腹泻药物中的应用。In a second aspect, the present invention provides use of a composition comprising trachelosyl glycoside in the preparation of a diarrhea drug.

具体地,所述腹泻为大肠杆菌感染所引起的腹泻。Specifically, the diarrhea is diarrhea caused by Escherichia coli infection.

作为优选方案,所述组合物中,络石苷作为唯一活性成分。As a preferred embodiment, in the composition, trachelosidoside is the only active ingredient.

作为具体实施方案,所述组合物包括络石苷以及药物上可接受的辅料。As a specific embodiment, the composition comprises trachelosidoside and pharmaceutically acceptable excipients.

作为具体实施方案,所述组合物的剂型选自片剂、胶囊剂、粉剂、颗粒剂、口服液或注射液。As a specific embodiment, the dosage form of the composition is selected from tablets, capsules, powders, granules, oral liquids or injections.

本发明中所述络石苷,其分子式为C27H34O12,CAS号为33464-71-0,其化学结构式如下所示:The trachelosidin described in the present invention has a molecular formula of C 27 H 34 O 12 , a CAS number of 33464-71-0, and a chemical structural formula as shown below:

有益效果:与现有技术相比,本发明公开了络石苷在制备治疗腹泻药物中的应用。本发明试验研究证实,络石苷能有效降低腹泻小鼠稀便率和腹泻率,提高腹泻小鼠体重、采食量和饮水量。因此,络石苷可以用来治疗腹泻,且效果显著。综上,络石苷能够用于制备治疗腹泻的药物,具备良好的市场潜力和价值。Beneficial effects: Compared with the prior art, the present invention discloses the use of trachelosidone in the preparation of drugs for treating diarrhea. The experimental study of the present invention confirms that trachelosidone can effectively reduce the loose stool rate and diarrhea rate of diarrheal mice, and increase the body weight, food intake and water intake of diarrheal mice. Therefore, trachelosidone can be used to treat diarrhea, and the effect is significant. In summary, trachelosidone can be used to prepare drugs for treating diarrhea, and has good market potential and value.

具体实施方式DETAILED DESCRIPTION

下面将对本发明实施例中的技术方案进行清楚、完整地描述。实施例中未注明具体条件者,按照常规条件或制造商建议的条件进行。所用试剂或仪器未注明生产厂商者,均为可以通过市售购买获得的常规产品。The technical scheme in the embodiments of the present invention will be described clearly and completely below. If the specific conditions are not specified in the embodiments, the conventional conditions or the conditions recommended by the manufacturer are followed. If the manufacturer of the reagents or instruments used is not specified, they are all conventional products that can be purchased commercially.

实施例Example

1、主要实验材料1. Main experimental materials

络石苷(MCE),氯化钠,蒸馏水,大肠杆菌CMCC44108。MCE, sodium chloride, distilled water, Escherichia coli CMCC44108.

SPF级昆明小鼠由上海斯莱克斯实验动物有限公司/中国科学院上海动物实验中心提供,体重20±2g。SPF Kunming mice were provided by Shanghai SLEX Laboratory Animal Co., Ltd./Shanghai Animal Experimental Center, Chinese Academy of Sciences, with a body weight of 20±2g.

2、实验方法2. Experimental methods

试验选取健康昆明种小鼠50只,待其适应一周后,按体重相近随机分组,空白组10只,模型组50只。模型组腹腔注射0.02mL/g(3×108CFU)的大肠杆菌CMCC44108菌悬液,空白组注射等剂量无菌生理盐水,连续5d后,将模型组再次分为模型对照组和络石苷治疗组,治疗组分别为络石苷高剂量组(400mg/kg)、中剂量组(200mg/kg)和低剂量组(100mg/kg),10只/组,5只/笼,按上述剂量灌胃治疗。空白组和模型对照组小鼠灌胃等体积生理盐水,各组小鼠投喂饲料是55g/笼/d,水是150mL/笼/d,连续治疗6d。Fifty healthy Kunming mice were selected for the experiment. After one week of adaptation, they were randomly divided into blank group and model group according to similar body weight, with 10 mice in blank group and 50 mice in model group. The model group was intraperitoneally injected with 0.02mL/g (3×10 8 CFU) of Escherichia coli CMCC44108 suspension, and the blank group was injected with the same dose of sterile saline. After 5 consecutive days, the model group was divided into model control group and trachelosyl glycoside treatment group again. The treatment groups were trachelosyl glycoside high-dose group (400mg/kg), medium-dose group (200mg/kg) and low-dose group (100mg/kg), 10 mice/group, 5 mice/cage, and gavage treatment according to the above doses. The blank group and model control group mice were gavaged with the same volume of saline, and the mice in each group were fed with 55g/cage/d of feed and 150mL/cage/d of water, and the treatment was continued for 6 days.

3、实验动物临床记录及观察3. Clinical records and observations of experimental animals

观察各组小鼠稀便情况,并记录小鼠的体重、采食量、排便总数和稀便数,计算体重增长率和稀便率。The loose stools of mice in each group were observed, and the body weight, food intake, total number of defecation and number of loose stools were recorded, and the body weight growth rate and loose stool rate were calculated.

体重增长率=[(最终体重-治疗0d时体重)/治疗0d时体重]×100%;Weight growth rate = [(final weight - weight at treatment day 0) / weight at treatment day 0] × 100%;

采食量(g)=当天投放饲料总量(55g)-第二天剩余量;Feed intake (g) = total amount of feed put in on the day (55g) - remaining amount on the second day;

稀便率(%)=稀便数/排便总数×100%。Loose stool rate (%) = number of loose stools/total number of defecation × 100%.

4、统计学分析4. Statistical analysis

各分组所得计量数据采用平均值±标准差(x±s)表示,用DPSv7.05软件处理数据,两组间均数比较用t检验,P<0.05有统计学意义。The measurement data obtained from each group were expressed as mean ± standard deviation (x ± s), and the data were processed using DPSv7.05 software. The means between the two groups were compared using t-test, and P < 0.05 was considered statistically significant.

5、结果5. Results

5.1络石苷对腹泻小鼠体重的影响5.1 Effect of trachelosidol on body weight of mice with diarrhea

统计各组小鼠治疗后0d、2d、4d和6d的体重变化情况,并且计算体重增长率,结果如下表1所述。The weight changes of mice in each group at 0d, 2d, 4d and 6d after treatment were counted, and the weight growth rate was calculated. The results are shown in Table 1 below.

表1各组小鼠体重变化情况(n=10)Table 1 Body weight changes of mice in each group ( n=10)

注:与空白组相比,*P<0.05;与模型组相比,#P<0.05。Note: Compared with the blank group, *P<0.05; compared with the model group, #P<0.05.

由上表1结果可得,与空白组相比,治疗0d时,模型对照组,络石苷高剂量组、中剂量组和低剂量组的小鼠体重均显著降低,表明造模成功。与模型组相比,治疗6d后,络石苷高剂量组、中剂量组和低剂量组小鼠的体重增长率均显著提高,尤其是络石苷高剂量组,其体重增长率与空白组接近。From the results in Table 1 above, it can be seen that compared with the blank group, at 0 days of treatment, the body weight of mice in the model control group, the high-dose group, the medium-dose group and the low-dose group of trachelosidone was significantly reduced, indicating that the model was successfully established. Compared with the model group, after 6 days of treatment, the body weight growth rate of mice in the high-dose group, the medium-dose group and the low-dose group of trachelosidone was significantly increased, especially in the high-dose group of trachelosidone, whose body weight growth rate was close to that of the blank group.

5.2络石苷对腹泻小鼠采食量影响5.2 Effect of trachelosidol on food intake in mice with diarrhea

按照上述方法,统计各组小鼠每天的饲料投放总量,以及剩余量,计算治疗后0d、2d、4d和6d的采食量,结果如下表2所示。According to the above method, the total amount of feed given to each group of mice per day and the remaining amount were counted, and the food intake at 0d, 2d, 4d and 6d after treatment was calculated. The results are shown in Table 2 below.

表2各组小鼠采食量情况(n=10)Table 2 Food intake of mice in each group ( n=10)

注:与空白组相比,*P<0.05;与模型组相比,#P<0.05。Note: Compared with the blank group, *P<0.05; compared with the model group, #P<0.05.

由上表2结果可得,与空白组相比,治疗0d时,模型对照组,络石苷高剂量组、中剂量组和低剂量组的小鼠采食量均显著降低,表明造模成功。与模型组相比,治疗2d后,络石苷高剂量组采食量显著提高,治疗4d后,络石苷中剂量组采食量也显著提高,治疗6d后,络石苷高剂量组、中剂量组和低剂量组小鼠的采食量均显著提高,尤其是络石苷高剂量组,其采食量与空白组接近。From the results in Table 2 above, it can be seen that compared with the blank group, at 0 days of treatment, the food intake of mice in the model control group, the high-dose group, the medium-dose group and the low-dose group of trachelosidone was significantly reduced, indicating that the model was successfully established. Compared with the model group, after 2 days of treatment, the food intake of the high-dose group of trachelosidone increased significantly, after 4 days of treatment, the food intake of the medium-dose group of trachelosidone also increased significantly, and after 6 days of treatment, the food intake of mice in the high-dose group, the medium-dose group and the low-dose group of trachelosidone increased significantly, especially the high-dose group of trachelosidone, whose food intake was close to that of the blank group.

5.3络石苷对腹泻小鼠稀便率的影响5.3 Effect of trachelosyl glycosides on the loose stool rate in mice with diarrhea

按照上述方法,统计各组小鼠每天的排便总数和稀便数,计算稀便率,结果如下表3所示。According to the above method, the total number of defecation and loose stools of each group of mice per day were counted, and the loose stool rate was calculated. The results are shown in Table 3 below.

表3各组小鼠稀便率情况(n=10)Table 3 The loose stool rate of mice in each group ( n=10)

注:与空白组相比,*P<0.05;与模型组相比,#P<0.05。Note: Compared with the blank group, *P<0.05; compared with the model group, #P<0.05.

由上表3结果可得,与空白组相比,治疗0d时,模型对照组,络石苷高剂量组、中剂量组和低剂量组的小鼠稀便率均显著升高,表明造模成功。与模型组相比,治疗2d后,络石苷高剂量组小鼠稀便率显著降低,治疗4d和6d后,络石苷高剂量组、中剂量组和低剂量组小鼠的稀便率均显著降低。From the results in Table 3 above, it can be seen that compared with the blank group, at 0 days of treatment, the loose stool rates of mice in the model control group, the high-dose group, the medium-dose group and the low-dose group of trachelosidone were significantly increased, indicating that the model was successfully established. Compared with the model group, after 2 days of treatment, the loose stool rate of mice in the high-dose group of trachelosidone was significantly reduced, and after 4 and 6 days of treatment, the loose stool rates of mice in the high-dose group, the medium-dose group and the low-dose group of trachelosidone were significantly reduced.

以上所述实施例仅表达了本发明的几种实施方式,其描述较为具体和详细,但并不能因此而理解为对发明专利范围的限制。应当指出的是,对于本领域的普通技术人员来说,在不脱离本发明构思的前提下,还可以做出若干变形和改进,这些都属于本发明的保护范围。因此,本发明专利的保护范围应以所附权利要求为准。The above-mentioned embodiments only express several implementation methods of the present invention, and the descriptions thereof are relatively specific and detailed, but they cannot be understood as limiting the scope of the invention patent. It should be pointed out that, for ordinary technicians in this field, several variations and improvements can be made without departing from the concept of the present invention, and these all belong to the protection scope of the present invention. Therefore, the protection scope of the patent of the present invention shall be subject to the attached claims.

Claims (9)

1.络石苷在制备治疗腹泻药物中的应用。1. The application of trachelosyl glycoside in the preparation of drugs for treating diarrhea. 2.根据权利要求1所述的应用,其特征在于,所述腹泻为大肠杆菌感染所引起的腹泻。2. The use according to claim 1, characterized in that the diarrhea is diarrhea caused by Escherichia coli infection. 3.根据权利要求1所述的应用,其特征在于,所述络石苷作为唯一活性成分在制备治疗腹泻药物中的应用。3. The use according to claim 1, characterized in that the trachelosidoside is used as the sole active ingredient in the preparation of a drug for treating diarrhea. 4.根据权利要求1所述的应用,其特征在于,所述治疗腹泻药物为口服药物或者注射药物。4. The use according to claim 1, characterized in that the drug for treating diarrhea is an oral drug or an injectable drug. 5.包含络石苷的组合物在制备治疗腹泻药物中的应用。5. Use of a composition comprising trachelosyl glycoside in the preparation of a drug for treating diarrhea. 6.根据权利要求5所述的应用,其特征在于,所述腹泻为大肠杆菌感染所引起的腹泻。6. The use according to claim 5, characterized in that the diarrhea is diarrhea caused by Escherichia coli infection. 7.根据权利要求5所述的应用,其特征在于,所述组合物中,络石苷作为唯一活性成分。7. The use according to claim 5, characterized in that in the composition, trachelosidoside is the only active ingredient. 8.根据权利要求5所述的应用,其特征在于,所述组合物包括络石苷以及药物上可接受的辅料。8. The use according to claim 5, characterized in that the composition comprises trachelosidoside and pharmaceutically acceptable excipients. 9.根据权利要求5所述的应用,其特征在于,所述组合物的剂型选自片剂、胶囊剂、粉剂、颗粒剂、口服液或注射液。9. The use according to claim 5, characterized in that the dosage form of the composition is selected from tablets, capsules, powders, granules, oral liquids or injections.
CN202410905072.4A 2024-07-08 2024-07-08 Application of trachelospermin in preparation of diarrhea treatment medicine Pending CN118903170A (en)

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