Differences Between the Concentrations in Rabbit Body Fluid of Berberine Hydrochloride, Chlorogenic Acid, Baicalin, and Their Minimal Inhibitory Concentrations

To explore the relationship between the heat-clearing and detoxicating functions and the bacteriostatic actions of berberine hydrochloride （Ber. H）, chlorogenic acid （Chlo. A）, and baicalin （Bai）, their concentrations in rabbit body fluid were compared with their minimal inhibitory concentrations （MICs）. Their concentrations in rabbit blood and tissue fluid were determined by reversed-phase high performance liquid chromatography, and their MICs to Escherichia coli were determined by tube dilution method. The results showed that the peak concentrations of Ber. H, Chlo. A, and Bai in rabbit blood were 3.2, 5.03, and 7.63 μg mL^-1, and in rabbit tissue fluid were 0.12, 0.11, and 0.12 μg mL^-1, respectively. Their MICs to E. coli were, respectively, 1.0×10^3, 3.75 × 10^3, and 6.75 ×10^3μg mL^-1, which were far higher than the concentrations in rabbit body fluids. This study indicates that Ber. H, Chlo. A, and Bai have weak bacteriostatic actions and do not reach their effective inhibitory concentrations in rabbit body fluids, and their heat-clearing and detoxicating functions are independent on the bacteriostatic actions.

Detection of Berberine Hydrochloride in Jin Weng Zhili Particle Using TLC and HPLC

[Objectives]To screen optimum conditions of HPLC and TLC for qualitative discrimination of berberine hydrochloride contained in Jin Weng Zhili Particle,thus providing basis for quality standard. [Methods]According to the method described in Chinese Veterinary Pharmacopoeia,thin layer chromatography and high performance liquid chromatography were used respectively for qualitative and quantitative identification of berberine hydrochloride contained in Jin Weng Zhili Particle by improving the conditions of extraction and purification. [Results]After optimizing TLC conditions of Jin Weng Zhili Particle,the separation effect of TLC of test samples was favorable. The spot color was clear,reproducibility was good,and precision was high. Under the conditions of mobile phase constituted by acetonitrile-water-glacial acetic acid-triethylamine( 28∶ 70∶ 1∶ 1),detection wavelength of 265 nm,flow rate of 1. 0 m L min^(-1)and column temperature of 35℃,the resolution of berberine hydrochloride was good; the injection volume in the range of 3. 15-50 μg· m L^(-1)had good linear relationship with the peak area( R^2= 0. 998); the average sample recovery rate(n=6) was 5. 672%,and RSD was 0. 864%; the content of berberine hydrochloride contained in Jin Weng Zhili Particle was 4. 023 mg. [Conclusions]The method was of good feasibility,reproducibility and specificity,and could be used for qualitative and quantitative detection of berberine hydrochloride contained in Jin Weng Zhili Particle.

JAK2 and MAPK pathways are involved in the inhibitory effect of berberine hydrochloride on gastric cancer cell proliferation and IL-8 secretion

Acknowledgements This work was supported by Educational Commission of Shanghai of China （2012JW19）; Key Research Innovation Project （13ZZ099）; Key Project from Department of Education of China （20123107130002）; Shanghai Eastern Scholar Program （2013-59） and Shanghai E-research Institute of Bioactive Constituent in TCM plan. Abstract： Aim This investigation was to identify whether Janus-activated kinase 2 （JAK2） and mitogen-activated protein kinase （MAPK） pathways were involved in the inhibitory effect of berberine hydrochloride （BER） on gastric cancer cell proliferation and IL-8 expression in vitro and in vivo. Methods CCK- 8 assay was used to assess the cell proliferation. IL-8 production was determined by ELISA and qPCR assay. Mo- lecular pathways involved were evaluated by ELISA and western-blotting methods. Results BER time- and dose- dependently inhibited the proliferation of MGC 803 and AGS cells. It also suppressed tumor growth in nude mice xenografted with MGC 803 cells. In addition, BER reduced interleukin-8 （IL-8） secretion of AGS cells as well as MGC 803 cells both in vitro and in vivo. Further study disclosed that inactivation of JAK2, p38 MAPK, ERK1/2 and JNK by BER contributed to the decreased proliferation and tumor growth as well as IL-8 expression in gastric cancer. Although there was no significantly synergistic inhibitory effect between BER and evodiamine on gastric cancer cell proliferation and tumor growth, BER could counteract the up-regulation of IL-8 induced by evodiamine in vitro and vivo. Conclusions Our results suggested that BER might be an efficient and safe drug candidate for treating gastric cancer through JAK2 and MAPK pathways.

A meta-analysis of berberine hydrochloride in adjuvant treatment of ulcerative colitis and its influence on inflammatory factors

Objective:To evaluate the clinical efficacy of berberine hydrochloride in the treatment of ulcerative colitis and its influence on inflammatory factors.Methods:We searched VIP Chinese Journal Database(VIP),China Biomedical Literature Database(CBM),Wanfang Data,China Knowledge Network(CNKI),and searched English databases including:PubMed,Embase,Web of Science,and Cochrane Library for randomized controlled studies of berberine hydrochloride in the treatment of ulcerative colitis.The retrieval time was from the establishment of the database to April 28,2021.After the quality evaluation of the selected literature,the RevMan5.3 software was used for statistical analysis.Results:Eight studies were included,involving 658 patients with ulcerative colitis.Meta analysis showed that the effective rate of the treatment group was higher than that of the control group,and the difference was statistically significant[OR=6.41,95%CI(3.25,12.65),Z=5.36,P<0.00001];IL-6[MD=-13.64,95%CI(-14.88,-12.41),Z=3.99,P<0.00001],IL-8[MD=-13.41,95%CI(-15.11,-11.71),Z=15.46,P<0.00001],tumor necrosis factor[MD=-5.62,95%CI(-8.35,-2.89),Z=4.03,P<0.0001],and disease activity index[MD=-2.34,95%CI(-2.55,-2.14),Z=22.37,P<0.00001]in the treatment group were lower than the control group,the difference was statistically significant;IL-10[MD=6.49,95%CI(5.64,7.35),Z=14.86,P<0.00001]in the treatment group was higher than the control group,and the difference was statistically significant;abdominal pain relief time[MD=-3.41,95%CI(-4.02,-2.79),Z=10.84,P<0.00001],diarrhea relief time[MD=-2.5,95%CI(-2.86,-2.15),Z=13.87,P<0.00001],pus and blood stool remission time[MD=-2.44,95%CI(-2.87,-2.00).Z=10.87,P<0.00001]in the treatment group were shorter than the control group,and the difference was statistically significant.Conclusion:Berberine hydrochloride can assist in the treatment of ulcerative colitis by reducing the level of inflammatory factors.

Preparation of berberine hydrochloride long-circulating liposomes by ionophore A23187-mediated ZnSO_(4)gradient method

The aim of the study was to prepare berberine hydrochloride long-circulating liposomes and optimize the formulation and process parameters,and investigate the influence of different factors on the encapsulation efficiency.Berberine hydrochloride liposomes were prepared in response to a transmembrane ion gradient that was established by ionophore A23187.Free and liposomal drug were separated by cation exchange resin,and then the amount of intraliposomal berberine hydrochloride was determined by UV spectrophotometry.The optimized encapsulation efficiency of berberine hydrochloride liposomes was 94.3%
2.1%when the drug-to-lipid ratio was 1:20,and the mean diameter was 146.9 nm
3.2 nm.As a result,the ionophore A23187-mediated ZnSO_(4)gradient method was suitable for the preparation of berberine hydrochloride liposomes that we could get the desired encapsulation efficiency and drug loading.

Determination of Berberine Hydrochloride Content in Qingwen Baidu Granule by HPLC

The paper was to establish a simple and sensitive HPLC method for determination of berbefine hydrochloride content in Qingwen Baidu granule. The HPLC system consisted of Stable Bond - C18 column （4.6 × 150 mm, 5um） and with a mobile phase of acetonitrile -0.05mol/L potassium dihydrogen phosphate solution （50：50,v：v） mixture. Berberine hydrochloride was detected at the wavelength of 345 nm, with a flow rate of 1.0 ml/min and a column temperature of 30 ℃. The excipients and solvents in the granule could be well separated from the drug under such a designated chromatogram condition and did not interfere with the assay. A good linear relationship was found between peak area and the concentration of berberine hydrochloride in the range of 16.0 -48.0 I^g/mL. The average recovery of berberine hydrochloride was 99.09%. The established approach was specific, accurate, reliable, prompt, sensitive and applicable, and could be used to control the quality of Qingwen Baidu granule.

Semi-quantitative analysis on the content of berberine hydrochloride in compound berberine tablets with the fluorescence spectral imaging method

The content of berberine hydrochloride(BH)in compound berberine tablets(CBTs)is subject to strict requirements.Its content is usually measured based on chemical analysis.In this paper,the fluorescence spectral imaging method was used to study the relative content of BH from a physics perspective.By comparing the relative fluorescence intensity of self-made CBTs with di®erent mass percentages of BH,a linear positive relationship was observed between the BH content and the relative fluorescence intensity,and accordingly the quality of CBTs of different brands was evaluated.The results indicate that the fluorescence spectral imaging method can be a simple,fast and nondestructive semi-quantitative analysis method to determine the content of BH in CBTs,and this method has great potential in the quality control of CBTs.

HPLC法测定肾康灵胶囊中盐酸小檗碱的含量

目的 建立肾康灵胶囊中盐酸小檗碱的HPLC含量测定方法,为质量控制提供依据。方法 采用HPLC法,色谱柱:Sapphire-C_(18)柱(4.6×250 mm, 5μm);流动相:乙腈-0.1%磷酸溶液(梯度洗脱);流动相流速:1.0 mL·min^(-1);检测波长:265 nm;柱温:30℃,进样量:10μL。结果 盐酸小檗碱含量在0.0584~0.5840μg范围内与峰面积值呈良好线性关系(R^(2)=0.9981),精密度和重复性试验的RSD均<2.0%(n=6),稳定性试验(18 h内)的RSD为1.11%,平均加样回收率为98.24%,RSD=1.43%(n=6)。结论 该方法快速简便、稳定性好,专属性强,重复性良好,可为肾康灵胶囊的质量控制提供依据。

黄连解毒汤6种主要成分高效液相色谱检测方法的建立和应用

目的建立检测黄连解毒汤中6种主要成分的高效液相色谱(HPLC)方法。方法采用Zorbax Eclipse Plus C18色谱柱(250 mm×4.6 mm,5μm),以0.03 mg·mL-1磷酸二氢钾-乙腈(V∶V=7∶3)为流动相,等度洗脱,流速为1.0 mL·min-1,检测波长为345 nm,柱温为37℃,进样量为20μL,建立检测黄连解毒汤6种主要成分(京尼平苷、小檗碱、黄连碱、药根碱、黄芩苷、巴马汀)的HPLC方法。绘制HPLC检测6种成分的标准曲线,并进行方法学评价(线性、加样回收率、准确度和精密度、稳定性)。采用建立的HPLC方法检测黄连解毒汤样本。结果HPLC检测京尼平苷、小檗碱、黄连碱、药根碱、黄芩苷、巴马汀的线性范围分别为25.00~800.00、32.00~1024.00、20.00~640.00、20.30~650.00、13.13~420.00、25.00~800.00μg·mL-1,精密度和准确度均<2%,加样回收率分别为105.30%、102.88%、103.51%、107.76%、96.29%、99.34%。稳定性实验结果显示,室温放置24 h、反复冻融3次、2~8℃保存1周、-80℃冻存1个月,京尼平苷、小檗碱、黄连碱、药根碱、黄芩苷、巴马汀的峰面积相对标准偏差(RSD)均<2%,检测结果均稳定。采用HPLC检测黄连解毒汤的主要成分,浓度从高到低依次为药根碱(2799.00μg·mL-1)、小檗碱(2358.03μg·mL-1)、京尼平苷(1793.34μg·mL-1)、巴马汀(945.30μg·mL-1)、黄连碱(192.00μg·mL-1)、黄芩苷(171.00μg·mL-1)。结论建立的同时检测黄连解毒汤6种主要成分的HPLC方法快速、简便、重复性好、准确度高,可为后续黄连解毒汤的相关研究和临床应用奠定基础。

黄芩苷与盐酸小檗碱自沉淀理化性质及抑菌作用机制研究

目的 以黄芩苷和盐酸小檗碱产生的自沉淀为研究对象,探究其理化性质,对其抑菌作用及其机制展开研究,为中药自沉淀现象产生的物质深入研究提供参考。方法 采用差示热量扫描法、红外光谱扫描和紫外光谱扫描测定黄芩苷和盐酸小檗碱的自沉淀理化性质;采用牛津杯法探索黄芩苷、盐酸小檗碱及自沉淀对大肠埃希菌、金黄色葡萄球菌的抑菌活性;采用二倍稀释法进一步研究黄芩苷、盐酸小檗碱、自沉淀对大肠埃希菌和金黄色葡萄球菌的最小抑菌浓度(MIC)和最小杀菌浓度(MBC),并通过测定菌体的生长曲线、胞外核酸相对含量、胞外可溶性蛋白质含量和电导率研究黄芩苷、盐酸小檗碱及自沉淀对大肠埃希菌、金黄色葡萄球菌的抗菌机制,分析对比黄芩苷、盐酸小檗碱反应前后抑菌作用机制是否发生改变。结果 差示热量扫描法结果显示盐酸小檗碱与黄芩苷反应前后存在热量变化,该自沉淀是一种不同于盐酸小檗碱、黄芩苷的新物质或复合物,其官能团、紫外吸收均发生了变化。盐酸小檗碱对大肠埃希菌的MIC为0.9375 mg/mL,MBC为7.5 mg/mL;对金黄色葡萄球菌的MIC为0.9375 mg/mL,MBC为7.5 mg/mL。黄芩苷对大肠埃希菌的MIC为1.875 mg/mL,MBC为7.5 mg/mL;对金黄色葡萄球菌的MIC为3.75 mg/mL,MBC为15 mg/mL。自沉淀对大肠埃希菌的MIC为3.75 mg/mL,MBC为3.75 mg/mL;对金黄色葡萄球菌的MIC为3.75 mg/mL,MBC为3.75 mg/mL。3种物质对大肠埃希菌和金黄色葡萄球菌菌体生长均有显著的抑制效果,但作用机制有所差异。结论 3种物质对大肠埃希菌和金黄色葡萄球菌显示出较好的抑菌活性,由强到弱为盐酸小檗碱、黄芩苷、自沉淀,均通过对细菌细胞膜造成损伤改变其通透性,影响细菌生长,从而起到抑制细菌生长的目的。三种物质虽能使菌体内容物大量渗出,但对胞内物质泄出作用存在差异,研究成果为进一步探究中药自沉淀提供参考。

复方三黄凝胶薄层色谱鉴别方法研究

目的建立复方三黄凝胶的薄层色谱(TLC)鉴别方法。方法采用TLC考察不同展开剂、不同温度、不同薄层板厂家对复方三黄凝胶中大黄、黄芩、黄柏鉴别的影响,确定最佳TLC条件。结果大黄采用硅胶H薄层板,以甲苯-醋酸乙酯-甲酸(7∶3∶0.1)为展开剂,取出,晾干,置365 nm紫外光灯下检视,置氨蒸气中熏后,斑点显色清晰;黄芩采用聚酰胺薄膜,以甲苯-醋酸乙酯-甲醇-甲酸(10∶3∶1∶2)为展开剂,展开,取出,晾干,置365 nm紫外光灯下检视,斑点显色清晰;黄柏采用硅胶G薄层板,以甲苯-甲醇-醋酸乙酯-异丙醇-浓氨试液(6∶1.5∶3∶1.5∶0.5)为展开剂,展开,取出,晾干,置365 nm紫外光灯下检视,斑点显色清晰,三味药的TLC图特征明显,分离度好且无阴性干扰。结论所用TLC方法专属性强,耐用性好,可作为复方三黄凝胶的质量控制方法。

奇白消软膏的定性鉴别与定量检测

目的:建立奇白消软膏的定性鉴别与含量测定方法,加强奇白消软膏的质量控制。方法:采用薄层色谱(TLC)法对制剂中的黄连和人工牛黄进行定性鉴别;采用高效液相色谱法(HPLC)测定制剂中黄连有效成分盐酸小檗碱的含量。结果:奇白消软膏的TLC斑点清晰、阴性无干扰、分离度好;盐酸小檗碱在1.28~38.4μg;回归方程为Y=49873.84X-554.74(r=1)。精密度、稳定性、重复性试验的RSD分别为0.41%、0.38%、1.8%;加样回收率为98.88%~101.23%,RSD为0.95%(n=6)。结论:本研究建立的TLC和HPLC简便易行,准确、重复性好,可用于奇白消软膏的质量控制。

乳酸菌素片联合盐酸小檗碱片治疗成人急性肠炎的效果

目的:探究乳酸菌素片联合盐酸小檗碱片治疗成人急性肠炎的临床效果。方法:选择广东省人民医院赣州医院2022年1月—2023年6月收治的90例急性肠炎患者为研究对象,随机将其分为对照组和观察组,每组45例。在常规治疗基础上,对照组加服乳酸菌素片,观察组在对照组基础上联合盐酸小檗碱片进行治疗,两组均连续治疗7 d。对比两组的临床治疗效果、胃肠功能恢复情况、不良反应发生情况、临床症状评分。结果:观察组的临床治疗效果和不良反应发生情况均优于对照组(P<0.05)。观察组的腹痛、腹泻和恶心呕吐消失时间均早于对照组(P<0.05)。治疗前,两组的临床症状评分比较,差异均无统计学意义(P>0.05);治疗后,观察组的临床症状评分均低于对照组(P<0.05)。结论:乳酸菌素片联合盐酸小檗碱片可显著增强成人急性肠炎的整体治疗效果,促进患者临床症状及胃肠功能改善,使患者尽快恢复,且临床安全性较高。

盐酸小檗碱联合蒙脱石散灌肠治疗小儿急性细菌性肠炎的临床效果

目的:分析在小儿急性细菌性肠炎治疗中应用盐酸小檗碱联合蒙脱石散灌肠治疗的效果。方法:选取2019年8月—2022年8月江苏省宝应县人民医院收治的94例急性细菌性肠炎患儿为研究对象,采用抛硬币法将其分为试验组和对照组,各47例。对照组给予抗生素、补液等基础治疗,试验组在对照组基础上给予盐酸小檗碱及蒙脱石散灌肠治疗,比较两组治疗效果、症状改善时间、体液免疫检测指标、生活质量。结果:试验组总有效率高于对照组,差异有统计学意义(P<0.05)。试验组退热、腹泻缓解、呕吐改善、大便常规恢复正常时间均短于对照组,差异有统计学意义(P<0.05)。治疗前,两组体液免疫检测指标水平比较,差异无统计学意义(P>0.05);治疗后,试验组IgG、IgM及IgA水平均高于对照组,差异有统计学意义(P<0.05)。治疗前,两组生活质量评分比较,差异无统计学意义(P>0.05);治疗后,试验组生理、精神、认知评分均高于对照组,差异有统计学意义(P<0.05)。结论:在小儿急性细菌性肠炎治疗中应用盐酸小檗碱和蒙脱石散灌肠的效果显著,能够缩短患儿症状缓解时间,提高其免疫功能及生活质量。

中医药调控巨噬细胞改善急性肺损伤

中医药可通过调控肺泡巨噬细胞的吞噬、极化等,提高肺部代谢水平及免疫功能,加速体内毒素排出,减轻肺组织炎性损伤,缓解急性肺损伤(acute lung injury,ALI)的症状。中医药治疗ALI的单味药多以大黄、黄芩、白头翁、青蒿、白芍、甘草等为主,其中药活性成分主要有大黄素、黄芩苷、白头翁皂苷B4、双氢青蒿素、白芍苷、甘草酸等。中药复方常以清金化痰汤、黄连解毒汤、大承气汤、芪冬活血饮等加减为主。目前,研究存在的问题是,中医药治疗ALI的机制尚不明确,缺乏大样本量及循证研究,研究与临床应用结合不够充分,缺乏系统全面的总结;中药的配伍、使用剂量等依赖医生的个人经验总结,难以精准用药。今后,需基于网络药理学、细胞学、病理学及免疫学等,进一步加强中医药治疗ALI的机制研究及以调控巨噬细胞改善AIL为中心的大样本随机对照研究,寻找高效、安全治疗ALI及预防其并发症的中医药治疗方法。

小儿清热止咳口服液高效液相色谱指纹图谱的建立及8种成分含量测定

目的建立小儿清热止咳口服液的高效液相色谱(HPLC)指纹图谱,并测定其中8种主要成分的含量。方法色谱柱为Agilent Infinity Lab Poroshell 120 EC-C18柱(150 mm×4.6 mm,2.7μm),流动相为乙腈-甲醇(89∶11,V/V)-0.01 mol/L磷酸二氢钾溶液(pH 3.2),梯度洗脱,流速为1.0 mL/min,检测波长为210 nm(0~31 min)、270 nm(31~75 min),柱温为30℃,进样量为10μL。结果共得到28个共有峰,其中26个可找到归属,各批样品间相似度均大于0.99。盐酸麻黄碱、黄芩苷、苦杏仁苷、甘草酸铵、盐酸伪麻黄碱、黄芩素、甘草苷、(R,S)-告依春质量浓度分别在2.05~41.06μg/mL、38.42~768.48μg/mL、9.00~179.93μg/mL、3.23~64.61μg/mL、1.09~21.90μg/mL、1.49~29.80μg/mL、1.94~38.87μg/mL、0.69~13.71μg/mL范围内与峰面积线性关系良好(r≥0.9994),检测限为0.0686~0.8576μg/mL,定量限为0.3284~1.6152μg/mL;稳定性、重复性、中间精密度试验结果的RSD均小于3.0%;平均加样回收率为97.90%~101.44%,RSD为0.45%~1.85%(n=6)。结论该方法灵敏、简便、准确,可用于小儿清热止咳口服液的质量控制。

基于含量测定和指纹图谱评价电子束辐照灭菌对藏药小檗膏耳用散剂质量的影响

目的 评价电子束辐照灭菌对藏药小檗膏耳用散剂质量的影响。方法 分别采用0、2、4、6、8、10 kGy剂量的电子束辐照处理小檗膏耳用散剂,研究不同剂量电子束辐照对其性状、指纹图谱、生物负载及指标成分盐酸小檗碱、没食子酸和西红花苷-Ⅰ含量的影响。结果 电子束辐照剂量增加时,粉末颜色略有加深,各组之间无明显变化,均为棕黄色粉末;电子束辐照能够有效降低小檗膏耳用散剂中细菌和霉菌、酵母菌菌落总数,随着辐照剂量增大,其存活数显著降低(P<0.05);电子束辐照对小檗膏耳用散剂中主要成分盐酸小檗碱、没食子酸和西红花苷-Ⅰ 的含量无显著影响(P>0.05)。不同剂量电子束辐照处理的小檗膏耳用散剂指纹图谱的相似度均大于0.958,表明经电子束辐照处理的样品与未辐照样品相比无显著变化。结论 10 kGy以下电子束辐照灭菌对藏药小檗膏耳用散剂的多个指标成分的含量无明显影响,而6 kGy以下电子束辐照灭菌即可符合《中国药典》2020年版微生物限度标准的规定。电子束辐照适用于小檗膏耳用散剂的灭菌,为电子束辐照技术在小檗膏耳用散剂灭菌中的应用提供了科学依据。

HPLC法测定骨伤跌打康复凝胶贴膏剂中7种成分含量

目的 建立测定骨伤跌打康复凝胶贴膏剂中7种主要成分质量分数的HPLC法。方法 色谱柱为Agilent ZORBA×SB-C18S tableBond Analytical柱(4.6 mm×250 mm, 5μm);测定波长为290 nm,流动相为乙腈-0.1%甲酸水梯度洗脱;流速为1.0 mL/min;柱温为35℃;进样量为10μL。结果 骨伤跌打康复凝胶贴膏剂中的原儿茶酸、咖啡酸、阿魏酸、盐酸小檗碱、大黄酸、大黄素、大黄酚7种主要有效成分在浓度线性范围内与色谱峰面积的标准曲线线性关系良好;原儿茶酸、咖啡酸、阿魏酸、盐酸小檗碱、大黄酸、大黄素、大黄酚的平均回收率分别为93.79%、95.86%、96.12%、95.31%、96.58%、107.43%、97.12%,7种成分的平均回收率均在93.79%~107.43%范围内。结论 建立的方法适合作为骨伤跌打康复凝胶贴膏剂质量控制的方法。

美沙拉秦联合盐酸小檗碱片治疗溃疡性结肠炎患者的临床效果

目的:探究美沙拉秦联合盐酸小檗碱片治疗溃疡性结肠炎(ulcerative colitis,UC)患者的临床效果。方法:选取2021年3月—2023年3月盐城市第一人民医院收治的100例UC患者作为研究对象。根据随机数表法将其分为对照组和观察组,各50例。两组入院后均采取对症治疗,对照组给予美沙拉秦,观察组在对照组基础上给予盐酸小檗碱片。比较两组临床疗效,症状改善时间,治疗前及治疗3个月后肠道黏膜屏障功能、炎症因子。结果:观察组治疗总有效率为98.00%,显著高于对照组的82.00%,差异有统计学意义(P<0.05)。观察组腹痛、腹泻、脓血便改善时间均早于对照组,差异有统计学意义(P<0.05)。治疗3个月后,两组二胺氧化酶(diamine oxidase,DAO)和D-乳酸(D-lactic acid,D-LA)水平均下降,观察组DAO和D-LA水平均低于对照组,差异有统计学意义(P<0.05)。治疗3个月后,两组C反应蛋白(C-reactive protein,CRP)、白细胞介素-1β(interleukin-1β,IL-1β)水平均显著降低,白细胞介素-10(interleukin-10,IL-10)水平明显升高,观察组CRP、IL-1β水平均低于对照组,IL-10水平明显高于对照组,差异有统计学意义(P<0.05)。结论:美沙拉秦联合盐酸小檗碱片治疗UC效果显著,有效改善肠道黏膜屏障功能,降低炎症因子水平。

盐酸小檗碱结晶水及其稳定性研究

目的研究盐酸小檗碱原料药中的结晶水类型及含水量,以及盐酸小檗碱片制剂工艺对原料药结晶水的影响,为完善盐酸小檗碱片制剂质量控制提供依据。方法采用热重分析法(TGA)、差示扫描量热法(DSC)、X-射线粉末衍射法(XRPD)对盐酸小檗碱原料药中的结晶水进行研究,并考察盐酸小檗碱片生产过程及稳定性考察期间结晶水的变化情况。结果盐酸小檗碱以二水物为主,并含有少量的四水物和游离水;盐酸小檗碱片生产过程及稳定性考察期间原料药结晶水基本无明显变化。结论明确了盐酸小檗碱原料药中的结晶水,并做好盐酸小檗碱片生产过程质量控制,有助于确保其制剂质量均一、稳定、可控。