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.

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.

Berberine hydrochloride alleviates chronic prostatitis/chronic pelvic pain syndrome by modifying gut microbiome signaling

Chronic prostatitis/chronic pelvic pain syndrome(CP/CPPS)is highly prevalent worldwide and poses a significant threat to men’s health,particularly affecting young men.However,the exact causes and mechanisms behind CP/CPPS remain unclear,leading to challenges in its treatment.In this research,a CP/CPPS rat model was established with complete Freund’s adjuvant(CFA),and berberine hydrochloride was administered through daily gavage to assess its therapeutic effects.The alterations in the gut microbiome induced by CP/CPPS and berberine hydrochloride were investigated through 16S ribosomal RNA sequencing of cecum content and colonic epithelial cells.To investigate the impact of the gut microbiome on CP/CPPS,a pseudo germ-free rat model was established,and fecal microbiome transplantation(FMT)was performed on these rats.In all,berberine hydrochloride demonstrated effective reduction of inflammation and oxidative stress in the prostate,offering significant therapeutic advantages for CP/CPPS.Through analysis of the gut microbiome using 16S ribosome RNA sequencing,distinct differences were observed between CP/CPPS rats and control rats,and Clostridium butyricum was identified as a key bacteria.Pseudo germ-free rats that underwent FMT from CP/CPPS rats or rats treated with berberine hydrochloride displayed varying levels of inflammatory cytokine production,oxidative stress,and activity of associated signaling pathways.In conclusion,the therapeutic potential of berberine hydrochloride in addressing CP/CPPS is highly significant.The gut microbiome has emerged as a critical factor in the development of CP/CPPS and plays a pivotal role in mediating the therapeutic effects of berberine hydrochloride.

Comparison of dissolution profile characteristics of 11 berberine hydrochloride tablet brands in different dissolution media

Berberine hydrochloride is commonly used to treat bacterial dysentery,gastroenteritis and other diseases.Many manufacturers are available on the market today,while the production process and formulation are quite different,which may directly affect the therapeutic effect of the drug.To this end,11 different production producers of berberine hydrochloride tablets were collected according to the pharmacopeia berberine hydrochloride dissolution method(basket method).In addition the dissolution process was carried out in four elution media with different pH,and the difference was similar(f2).Factors were calculated to evaluate in vitro dissolution requirements,and in vitro dissolution of different manufacturers of berberine hydrochloride tablets was determined by high performance liquid chromatography(HPLC).The method was verified by linearity,precision,stability and robustness.Based on the f2 value,there was a significant difference in the dissolution behavior of the formulations of most berberine hydrochloride tablet brands.This research provided the basis for further in-depth research in the later period.Although the drug specifications(0.1 g)were the same,the dissolution curve was different.This phenomenon may be attributed to the fact that the excipients and crystal form of the tablets affected the release and dissolution of the tablets in vitro.

Synergistic Antimicrobial Activity of Berberine Hydrochloride, Baicalein and Borneol against Candida albicans

Objective To determine the synergistic effects of berberine hydrochloride, baicalein,and borneol in different combinations on Candida albicans. Methods The broth microdilution method was used to determine the minimal inhibitory concentration（MIC） and minimal bactericidal concentration（MBC） of the three agents, and the checkerboard method was simultaneously used to determine the MIC and fractional inhibitory concentration index（FICI） of the combination of three antimicrobial agents to study their extracorporeal effects. Results Berberine hydrochloride was the most potent inhibitor of C. albicans（MIC and MBC of 0.160 and 0.640 mg/mL）, followed by borneol（MIC and MBC of 0.320 and 0.640 mg/mL） and baicalein（MIC and MBC of 1.28 and 20.48 mg/mL）. Moreover, the antifungal effect of the combination was significantly stronger than that tested alone. Further in vivo study showed that the mortality rate of tainted mice reduced over 50% compared with the control group. Conclusion The results of experiments in vitro and in vivo indicate the synergistic effect of the combination of three antimicrobial agents on C. albicans, which can make reference for the future clinical treatment.

Quality Standard of Compound Quanchangning Capsule

[ Objective] The research aimed to study the quality standard of Compound Quanchangning Capsule. [ Method] Coptis, Phelledendron, Pulsatilla and Astragalus in Compound Quanchangning Capsule were indentified qualitatively by thin layer chromatography （ TLC）, and the content of berberine hydrochloride was determined by high performance liquid chromatography （HPLC）, to study the quality standard of Compound Quanchangning Capsule. [ Result] TLC identification showed that the tested product was clear and well-separated with no interference. Berberine hydrechloride showed a good linear relationship with peak area at the injection volume of 10.92 - 163.74 ~Lg/mL, and the regression equation was Y = 39 611X -2 387. 9 （R2 = 0. 999 8） ; the average recovery was 97.60%, and the relative standard deviation was 1.64% （n =6）. [ Conclusion] The standard is simple in operation and good in specificity, stability and repeatability, which is prompted as a favorable method for quality control of Compound Quanchangning Capsule.

Anti-hemorrhoidal activity of Lian-Zhi-San,a traditional Chinese medicine,in an experimental hemorrhoidal model in rats

Objective:Hemorrhoidal disease(HD)is the most common proctological disease,with an estimated prevalence rate of 4.4%,and a peak in individuals between 45 and 65 years of age.This study was done to evaluate whether Lian-Zhi-San(LZS),a clinically used anti-hemorrhoidal ointment could alleviate the inflammatory injury,with its associated changes of inflammatory cytokines and morphology of anorectal tissues,in an experimental model of HD in rats.Methods:HD was induced by croton oil preparation(COP)applied to the anorectal region.Rats were then treated with cotton swabs soaked in LZS ointment,water or white vaseline,twice a day for 7 d.At the end of the experiment,HD was evaluated by measuring hemorrhoidal and biochemical parameters along with histopathological observations.Results:In this study,COP induced a significant increase in the macroscopic severity score,anorectal coefficient and Evans blue extravasation,compared to normal rats.Additionally,it greatly enhanced the expression and secretion levels of some important inflammation-related cytokines along with marked histological damage,compared to normal rats.Rats treated with LZS ointment experienced significantly ameliorated Evans blue extravasation(P<0.05),decreased macroscopic severity score(0.86±0.14 vs.1.65±0.16)and the anorectal coefficient(P<0.01);its use also attenuated tissue damage and inhibited the expression and secretion levels of inflammation-related cytokines(interleukin-1 b,interleukin-6 and tumor necrosis factor-a).Conclusion:This study validates a preliminary understanding of the use of LZS ointment to treat inflammatory factors and tissue damage in an experimental model of HD in rats.