ABSTRACT
Objective To prepare berberine hydrochloride nanoemulsion, optimize its formulation composition and preparation process, and investigate its in vitro characteristics. Methods BBR-NE was prepared by water drop addition and pseudo-ternary phase diagram was drawn. The formulation of NE was optimized by central composite design-response surface methodology to choose the optimal formulation composition. The particle size, potential and appearance of the prepared BBR-NE were characterized. Results The optimal prescription of BBR-NE was determined as the oil phase Capryol 90 accounted for 32.84% of the system, the surfactant Tween-80 accounted for 33.90%, the co-surfactant 1,2-propylene glycol accounted for 16.95%, and water relative system accounted for 15.25%. The prepared NE was clear and transparent in appearance, regular in shape and uniform in size, with an average particle diameter of (68.85±8) nm, polydiseperse index of (0.245±0.03) and drug loading of 0.83 mg/g. The in vitro drug release results of NE showed that the in vitro drug release behavior was passive diffusion, which had a certain slow releasing effect and met the first-order release equation. Conclusion The BBR-NE can provide a new dosage form for the clinical use of berberine.
ABSTRACT
ObjectiveTo investigate the efficacy and mechanism of berberine hydrochloride （BBH） against lung cancer cells through the mevalonate （MVA） pathway. MethodHuman lung cancer A549 cells and mouse Lewis lung carcinoma （LLC） cells were used as research subjects. Cell proliferation and cell counting kit-8 （CCK-8） assay were performed to detect the inhibitory effect of BBH （10， 20， 30， 40， 50 μmol·L-1） on the proliferation of the two kinds of cells （48 h）. Then cell scratch assay was used to explore the influence of BBH （40 μmol·L-1） on the migration of A549 and LLC cells （24， 48 h）， and colony formation assay was conducted to compare the colony formation ability of the cells under different concentrations of BBH （10， 20， 40 μmol·L-1）. Moreover， the effects of BBH （40 μmol·L-1） on the content of acetyl-coenzyme A （A-CoA） and total cholesterol （TC） in A549 and LLC cells were determined by kit assay. AutoDock Vina was used for the dock of BBH and MVA pathway regulatory protein， sterol regulatory element-binding protein 2 （SREBP2）. Real-time fluorescence quantitative polymerase chain reaction （Real-time PCR） was used to observe the effects of BBH （40 μmol·L-1） on the mRNA expression of nine genes related to the MVA pathway in A549 and LLC cells： hydroxymethylglutaryl-CoA synthase 1 （HMGCS1）， hydroxymethylglutaryl-CoA Reductase （HMGCR）， mevalonate kinase （MVK）， phosphomevalonate kinase （PMVK）， mevalonate 5-pyrophosphate decarboxylase （MVD）， farnesyl diphosphate synthase （FDPS）， squalene epoxidase （SQLE）， farnesyl-diphosphate farnesyltransferase 1 （FDFT1）， and geranylgeranyl diphosphate synthase 1 （GGPS1）. Western blot was performed to clarify the effects of BBH （40 μmol·L-1） on the expression of three key proteins of the MVA pathway： HMGCS1， HMGCR， and FDFT1. The Cancer Genome Atlas （TCGA） database was searched to analyze the relationship between HMGCS1， HMGCR， FDFT1 and transcription gene SREBF2 in non-small cell lung cancer （NSCLC）. ResultCompared with the conditions in the control group， the proliferation， migration， and colony formation of A549 and LLC cells in the BBH group were decreased （P<0.01）， while the cell apoptosis rate was increased （P<0.01）. Molecular docking showed that BBH had good binding activity with SREBP2. In addition， the content of A-CoA and TC of the MVA pathway was reduced （P<0.01）. BBH down-regulated the mRNA expression of HMGCS1， HMGCR， MVK， PMVK， MVD， FDPS， SQLE， FDFT1， and GGPS1 in A549 and LLC cells （P<0.01）， and lowered the levels of HMGCS1， HMGCR， and FDFT1 proteins （P<0.05， P<0.01）. In NSCLC patients， HMGCS1， HMGCR， and FDFT1 were highly correlated with SREBF2 （R=0.54， R=0.57， and R=0.48）. ConclusionBBH can inhibit the proliferation， migration， and colony formation of A549 and LLC cells and promote cell apoptosis， which may be related to the regulation of MVA pathway by BBH binding to SREBP2.
ABSTRACT
The present study aims to investigate the effects of the main components(aesculin, berberine hydrochloride, and anemoside B4) in the butyl alcohol extract of Baitouweng Decoction(BAEB) on the chemotaxis of neutrophils induced by dimethyl sulfoxide(DMSO). HL60 cells were cultivated in RPMI-1640 complete medium, and transferred into a 6-well plate(2 × 10~5 per mL) with 4 mL in each well, followed by incubation with DMSO at 1.3% for five days. The morphologic changes of cells were observed under an inverted microscope. The CD11 b expression after DMSO induction was analyzed by flow cytometry. The effects of aesculin, berberine hydrochloride, and anemoside B4 on the cell proliferation and migration were detected by CCK8 assay and Transwell assay, respectively. The effects of the main components on the production and polarization of F-actin protein were also examined by flow cytometry and laser confocal microscopy. PI3 K/Akt signaling pathway was checked by Western blot. As revealed by the results, neutrophil-like HL60 cells were observed after DMSO induction. The CD11 b expression in these cells increased significantly as indicated by the flow cytometry. Additionally, 100 μg·mL~(-1) aesculin, 8 μg·mL~(-1) berberine hydrochloride, and 80 μg·mL~(-1) anemoside B4 were potent in inhibiting the migration of neutrophils and reducing F-actin expression. Berberine hydrochloride was verified to be capable of diminishing phosphorylated PI3 K/Akt protein expression. The findings indicate that aesculin, anemoside B4, and especially berberine hydrochloride in the BAEB can inhibit the chemotaxis of neutrophils, which is possibly achieved by the inhibition of F-actin and PI3 K/Akt signaling pathway.
Subject(s)
1-Butanol , Berberine/pharmacology , Chemotaxis , Drugs, Chinese Herbal/pharmacology , NeutrophilsABSTRACT
The object of this study is to preparate the berberine hydrochloride (BBH) resin compound with taste masking effect. We took the BBH as the model drug and Amberlite IRP69 as the drug carriers, uncovered the curve of solubility of BBH in different cosolvent with a certain range of temperature, and then used it to calculate the parameters during the preparation of the complex such as adding quantity of BBH and the reaction temperature. Afterwards, the characteristic and in vitro release experiments were studied to verify the formation and predict the in vivo release behavior of the complex. The results showed that in the condition of using 60% ethanol as a cosolvent and stirring at 50 ℃ for 1 h, the drug loading and drug availability of the complex are at about 35% and 64%, respectively, and has a better taste-masking effect. In this study, a method was provided for preparing a taste-masking preparation of BBH.
ABSTRACT
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-1β, interleukin-6 and tumor necrosis factor-α).@*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.
ABSTRACT
The aim of this paper was to investigate the effect of berberine hydrochloride on the cell wall integrity of Candida albicans hypha. The minimal inhibitory concentration(MIC) of berberine hydrochloride against clinical and standard C. albicans strains was detected by micro liquid-based dilution method; the effect of berberine hydrochloride on the colony formation of C. albicans SC5314 was investigated by spot assay; the effect of berberine hydrochloride on the metabolism of C. albicans SC5314 hypha was checked by XTT reduction assay, and the viability of C. albicans SC5314 hypha was tested by fluorescent staining assay. The effect of berberine hydrochloride on the morphology of C. albicans SC5314 hypha was examined by scanning electron microscope. The changes in the cell wall of C. albicans SC5314 hypha after berberine hydrochloride treatment were detected by transmission electron microscopy. The effect of berberine hydrochloride on β-glucan from C. albicans SC5314 was detected by flow cytometry. The effect of berberine hydrochloride on hypha-specific gene ECE1 and β-glucan synthase genes FKS1 and FKS2 in C. albicans was examined by qRT-PCR. The results showed that berberine hydrochloride showed a strong inhibitory effect on both clinical and standard strains of C. albicans, and the MIC was 64-128 μg·mL~(-1). Spot assay, XTT redunction assay and fluorescent staining assay showed that with the increase of berberine hydrochloride concentration, the viability of C. albicans SC5314 gradually decreased. The transmission electron microscopy scanning assay showed that this compound could cause cell wall damage of C. albicans. The flow cytometry analysis showed the exposure degree of C. albicans β-glucan. The qRT-PCR further showed that berberine hydrochloride could significantly down-regulate hypha-specific gene ECE1 and β-glucan synthase-related gene FKS1 and FKS2. In conclusion, this compound can down-regulate C. albicans and β-glucan synthase-related gene expressions, so as to destroy the cell wall structure of C. albicans, expose β-glucan and damage the integrity of the wall.
Subject(s)
Antifungal Agents/pharmacology , Berberine/pharmacology , Candida albicans/genetics , Cell Wall , Hyphae , Microbial Sensitivity TestsABSTRACT
Objective: Comparing the differences between dispensing granule decoction (DGD), standard decoction (SD) and traditional decoction (TD) of Phellodendri Chinensis Cortex (PCC) prescription to evaluate the quality of commercially available dispensing granule (DG), and establish the relevant standards for SD, TD and evaluative methods for DG. Methods: Fingerprint was established by HPLC. A comprehensive comparative study was conducted on 35 samples of DGD (three batches from each of the five A-E manufacturers), SD (10 batches) and TD (10 batches) in seven categories from five aspects of chemical composition type, representative index component content, fingerprint similarity, total peak area sum and principal component analysis (PCA); Clinically recommended equivalent corrections were performed for DGD. Results: ① Twenty-one common peaks in SD and TD were preserved in the DGD fingerprint. ② The content of magnoflorine in manufacturer A of DGD was 34.3% lower than that of SD (P < 0.05); The content of magnoflorine in manufacturer C was 35.6% lower than SD (P < 0.01), and 37.0% lower than TD (P < 0.05); The content of phellodendrine hydrochloride in D manufacturer was 22.0% lower than SD (P < 0.05), and 27.5% lower than TD (P < 0.05), The content of berberine hydrochloride in D manufacturer was 20.8% lower than SD (P < 0.05), and 23.8% lower than TD (P < 0.05). There were no significant differences between the other manufacturers' components. ③ The average similarity of each DGD and SD was greater than 0.992 6, and the average similarity of each DGD and TD was greater than 0.991 2, with high component similarity. Using the normalization method, the total peak area of the 21 common peaks of SD was 1 unit, and the ratios of the seven types of samples were 0.90, 1.03, 0.69, 0.77, 0.73, 1.00, and 1.06. ⑤ PCA showed that the distance between the B manufacturer and SD and TD was close, and the difference was small. Using the 21 common peak information of SD as the standard, the peak area plus method was used to correct the clinical recommended equivalent of DG. It was recommended that manufacturers A, C, D, and E could be reduced from 1 g equivalent to 12 g of the original decoction pieces to 10.7, 8.3, 9.2, and 8.8 g, respectively. B manufacturer was not needed to be corrected, and still 1 g was equivalent to 10 g of the original decoction pieces. Conclusion: There are differences in the content of components between DGD, SD, and TD in the real world. There is no significant difference in the proportion of components and components. These overall basically consistent differences can be adjusted by correcting the clinical recommended equivalent, thus promoting clinical rational drug use.
ABSTRACT
Objective: To prepare berberine hydrochloride dry powder inhalation, and investigate its pharmacological effect on Staphylococcus aureus pneumonia after pulmonary administration. Methods: Berberine hydrochloride dry powder by spray drying and the experimental conditions was optimized by orthogonal experiment. The lung deposition, fluidity and appearance were characterized. The pharmacodynamic effects of the preparations on S. aureus pneumonia were performed with SD rats. Results: A berberine hydrochloride dry powder was prepared at an inlet temperature of 130 ℃ with a gas volume flow of 610 L/h and a feed volume flow of 3 mL/min. The berberine hydrochloride dry powder had a lung deposition rate (FPF) of 76.4% and an aerodynamic diameter of 4.61 μm. The stability index (SI) ≈ 1, the aeration energy ratio (AR) = 1.76 > 1, and the inflation energy (AE10) = 2.1 mJ < 10 mJ. Through the pharmacodynamic evaluation of S. aureus, we can know that the berberine hydrochloride dry powder inhalation effectively improved the pathological state of pneumonia rats, and significantly reduced (P < 0.05) the number of WBC, neutrophils, and the expression of inflammatory factors (TNF-α, IL-1β, and IL-6) in pneumonia rats. Conclusion: Berberine hydrochloride dry powder inhalation can directly reach the lesion site through pulmonary administration, so it has significant therapeutic effect on S. aureus pneumonia.
ABSTRACT
Objective: To optimize Bletilla striata polysaccharide (BSP)/polyvinylalcohol (PVA) wet spinning process by Box- Behnken response surface method and prepare the composite fiber and performe their structural characterization and performance evaluation. Methods: Taking the OD value of three types of mechanical property data (breaking force, breaking strength and elongation at break) of the fiber as the evaluation index, five factors (BSP mass fraction, PVA mass fraction, volumetric mix ratio of BSP/PVA, coagulation time and spinning speed) were investigated by single factor experiments. On the basis of the results of single factor experiments, three factors (BSP mass fraction, volumetric mix ratio of BSP/PVA, coagulation time) were investigated by response surface method to optimize BSP/PVA composite fiber wet spinning process. The morphology, structure, thermal property, and absorption property of the fibers were characterized and analyzed by SEM, IR, DSC, and water absorption test. Berberine hydrochloride (BH) was used as model drug to evaluate the drug loading property of the composite fiber and antibacterial activity of the drug loading fiber. Results: The optimal spinning process of composite fiber were as follows: BSP mass fraction was 7.5%, volume mixing ratio of BSP/PVA was 1:1 and coagulation time was 3 min. The composite fiber had a dense surface and formed a three-dimensional network structure inside, generated intermolecular forces, which enhanced the thermal and mechanical properties, and exhibited excellent water absorption capacity. The encapsulation efficiency of the composite fiber reached 70.2%. And the drug loading fiber formed obvious inhibition zone in the bacteriostatic zone test, which presented excellent antibacterial effect against E. coli and S. aureus. Conclusion: The optimized spinning process is feasible and low cost. The prepared composite fiber has better physical property and certain coating ability, and its application in the field of biomedical textiles is worth further study.
ABSTRACT
OBJECTIVE：To evaluate the quality of inflorescence of Coptis chinensis from different altitude with different growth years and drying processing methods ，and to provide reference for its utilization and quality control. METHODS ：The contents of total flavonoids and berberine hydrochloride in 24 batches of inflorescence of C. chinensis （S1-S24）from different altitude with different growth years and drying processing methods were determined by UV-Vis spectrophotometry and HPLC. Using the contents of total flavonoids and berberine hydrochloride as indexes ，and taking the short drying time as the best ，the weight ratios of total flavonoids content ，berberine hydrochloride content and standardized value of drying time were 30，40 and 30，respectively；comprehensive score was calculated ，then the quality of 24 batches of samples was evaluated. Using the contents of total flavonoids and berberine hydrochloride as variables ，systematic cluster analysis was performed for 24 batches of samples by using SPSS 19.0 statistical software. RESULTS ：For inflorescence of C. chinensis with altitude about 1 200 m and the growing years of 4 years and above ，the higher the comprehensive score （84-94 score）and the better the quality were. The comprehensive score of inflorescence of C. chinensis procesed by gradient drying method was generally higher than samples processed by other methods. Results of cluster analysis showed that S 1-S4，S9，S10，S13-S18 were clustered into one category ，and other 12 batches were clustered into one category ， which were basically consistent with the results of comprehensive scoring method. CONCLUSIONS：Different altitude ，different growth years and different drying processing methods have certain effects on the quality of inflorescence of C. chinensis ，among which the samples processed by gradient drying method with growth altitude of 1 200 m，growth years of 4 years and above are the best.
ABSTRACT
The objective of the present investigation was to design and optimize lipid-based floating multiparticulate of Berberinehydrochloride (BERH), so as to increase its solubility and to reduce P-Glycoprotein mediated efflux in the intestine,hence to improve oral bioavailability. Solid dispersions were prepared using hydrophilic carriers gelucire 44/14and gelucire 50/13 in different ratio. The prepared solid dispersion of BERH was further formulated into sustainrelease gastroretentive floating pellets using hydrophobic lipid carrier gelucire 43/01 as release retardant, sodiumbicarbonate (NaHCO3) and hydroxylpropyl methyl cellulose K4M (HPMC K4M) as gas former and matrix polymer,respectively. The effect of amount of gelucire 43/01 and NaHCO3: HPMC K4M were studied and optimized using a3-level, 2-factor, factorial design. Solid dispersion of BERH compared to pure drug showed 4-fold enhancement inaqueous solubility. The optimum system could float for more than 8 hours and showed 88.46% drug release in 8 hours.The pharmacokinetic study conducted in male Wistar rats indicated 2.32-fold increase in relative bioavailability ofoptimized formulation compare to the marketed tablet. The lipid-based floating pellets of BERH were obtained andcould be an applicable choice to deliver BERH with improved bioavailability in effective use for various clinicalapplications.
ABSTRACT
OBJECTIVE: To explore the masking efficiency and regularity of bitterness suppressants (BS) to a representative bitterness substance berberine hydrochloride (BBR). METHODS: Some quantitative evaluation methods of BS efficiency were established based on relevant literature and our previous research. Efficiency of respectively added into eight kinds of BS such as acesulfame, on bitter degree 3 BBR solution (0.05 mg•mL-1) were evaluated using the established methods. Bitterness masking regularity of BS on BBR solution were explained by respectively establishing the relationships between tongue tasted bitter decreased value (ΔI), electronic tongue tasted bitter decreased value (ΔIe) with BS concentration (ρ). RESULTS: ①Five tongue taste bitter masking efficiency (calibrated masking rate, bitterness revised standard half effect index and so on), two electronic tongue bitter masking efficiency(first taste reduce and aftertaste reduce) were established. ②Seven kinds of bitterness suppressants efficacy indicators can be used to compare the bitterness suppressants efficacy of BS to BBR solution, and the maximum bitterness reduction of 8 kinds of BS to BBR solution is above 1.8. ③ΔI-ρ Weibull regularity models of eight BS and nine ΔIe-ρ models of six BS were brlilt.HP-β-CD, glycine and crystalline fructose had good response to two sensor, stevioside, soluble soybean polysaccharide and acesulfame had a good response to one sensor and xanthan gum and aspartame had no response to any sensor. CONCLUSION: Seven evaluation indexes and methods are built based on human tongue and electronic tongue taste method. Max standard capability index of BS is suitable for the development of bitterness suppressants in taste method and two indicators of electronic tongue are also can be used as indicative indicators. Masking regularity of BS to BBR solution is exposed which could provide reference for the development and application of more BS.
ABSTRACT
OBJECTIVE: To compare the limits of detection ( LODs) of TLC obtained with three evaluation approaches in Chinese Pharmacopoeia 2015, and facilitate selection of LOD evaluation approach in TLC method validation. METHODS: After development, the spots of strychnine, berberine hydrochloride, and ten chemical dyes were first detected by human eyes and then scanned by thin layer scanner to obtain the LODs based on visual evaluation, signal-to-noise, and standard deviation of the response and the slope. RESULTS: The LODs obtained by the three approaches showed no significant difference. For strychnine and 10 chemical dyes, the LODs based on the three approaches were close to each other. For berberine hydrochloride, the LOD obtained by visual evaluation was slightly lower than those obtained by the other two approaches. CONCLUSION: All the three approaches are feasible to determine LOD in TLC. The approach based on visual evaluation is rapid and reliable, which might be the first choice for LOD determination in TLC.
ABSTRACT
Objective: To establish an Angong Niuhuang Pills (ANP) characteristic spectrum analysis method, and to comprehensively characterize the quality properties and characteristics of ANP, and then to apply it to the quality detection and analysis of 10 batches of ANP, and to find out the specificity of the quality characterization of ANP. Methods: The UPLC-PDA multi-wavelength was used in the method, and a Waters Cortecs shields RP18 Column (100 mm × 2.1 mm, 1.6 μm) was used, the mobile phase was acetonitrile and 0.3% phosphoric acid solution, the detection wavelength was set at 240, 262, 330, 360, 274, and 440 nm, the column temperature was kept at 38 ℃, and the flow rate was 0.2 mL/min. Results: The results showed that the established analytical method can simultaneously determine 13 index components (including geniposide, genipin1-gentiobioside, crocin I, crocin II, berberine hydrochloride, coptis hydrochloride, palmatine chloride, epiberberine, baicalin, wogonoside, baicalein, wogonin and curcumin) in ANP, and a total of 35 characterstic peaks were identified in ANP. It included natural musk characteristic peak and natural bovis calculus characteristic peak which can identify the natural properties of raw materials. The mean values of the 13 index components in 10 batches of ANP were 2.87, 1.14, 0.40, 0.03, 3.17, 0.94, 0.74, 0.58, 10.01, 1.62, 0.34, 0.17, 0.05 mg/g, respectively. The RSD values ranged from 4.19% to 20.81%. All the 10 batches of ANP could be detected with 35 characteristic peaks, the average area values of natural musk and natural bovis calculus characteristic peaks were 0.031 and 0.003, and the RSD values ranged from 1.5% to 26.79%. Conclusion: According to the analysis of characteristic spectrum, the quality of finished products of 10 batches of ANP was relatively stable, and all showed the specific quality characterization of raw materials of natural musk, natural bovis calculus and Curcumae Radix; According to the analysis of the content of index components, the large fluctuation of the index components in 10 batches of samples mainly comes from Scutellaria baicalensis and Curcumae Radix, while the content of crocin I in Gardeniae Fructus and four alkaloids in Coptidis Rhizoma were relatively stable.
ABSTRACT
Objective To investigate the effects of the three methods of decocting with deslag, decocting without deslag, and double decocting on the content of nine ingredients baicalin, baicalein, ginsenoside Re, ginsenoside Rb1, monoammonium glycyrrhizinate hydrate, liquiritin, 6-gingerol, berberine hydrochloride, palmatine hydrochloride, and total flavonoids in Banxia Xiexin Decoction (BXD). Methods Nine index components were determined by HPLC. The HPLC analysis was performed on Welch Ultimate XB-C18 column (250 mm × 4.6 mm, 5 μm) with mobile phase of acetonitrile-0.1% phosphate aqueous solution for gradient elution; And carried out at column temperature of 28 ℃, volume flow of 0.9 mL/min, and detection wavelength of 203, 252, 280, and 355 nm. The total flavonoids were determined by colorimetry. Results Nine kinds of ingredients and total flavonoids could be detected in three different decoctions. In the method of decocting with deslag, baicalin, baicalein, ginsenoside Rb1, monoammonium glycyrrhizinate hydrate, and liquiritin increased by 10.01%, 12.88%, 29.09%, 16.75%, and 15.02%, respectively, compared with decocting without deslag; It decreased by 5.54%, 4.15%, 14.49%, 7.85%, and 9.18%, respectively compared with double decocting; Ginsenoside Re, 6-gingerol, berberine hydrochloride, and palmatine hydrochloride increased by 37.90%, 3.78%, 5.33%, and 5.99% compared with decocting without deslag, respectively; compared to the double decocting methods, it increased by 1.07%, 11.57%, 3.41%, and 1.93%. The total flavonoids increased 22.61% higher than decocting without deslag and 6.54% higher than double decocting. Conclusion: The results can effectively reflect the quality difference of different decocting methods. Among the three methods of decoction, the method of decocting without deslag has significantly improved the dissolution of the active ingredients of each component in the decoction, and improve the clinical efficacy of BXD to a certain extent. It provides a good experimental basis for the decocting without deslag method used in Zhang Zhongjing’s Treatise on Febrile Diseases.
ABSTRACT
Objective: To establish HPLC method for the simultaneous determination of saikosaponin a, naringin, paeoniflorin, calycosin-7-glucoside, tanshinone IIA, cinnamaldehyde, schisandrin, syringin, berberine hydrochloride, chrysophanol and hesperidin in Yigan Yiqi Jieyu Granules (YYJG), and conduct a quality assessment using principal component analysis. Methods: The chromatographic separation was achieved on an Caprisil AQ-C18 (150 mm × 4.6 mm, 5.0 μm) column with mobile phase consisted of 0.1% phosphate-acetonitrile for gradient elution, at the flow rate of 0.8 mL/min; The column temperature was 45 ℃. The results of the content were then combined with the principal component analysis to achieve the scientific assessment of the different batches of drugs. Results: The content of saikosaponina, naringin, paeoniflorin, calycosin-7-glucoside, tanshinone IIA, cinnamaldehyde, schisandrin, syringin, berberine hydrochloride, chrysophanol and hesperidin in YYJG had good linear relationship in the ranges of 1.6-80.0, 14-700, 10-500, 1.6-80.0, 1.6-80.0, 2.4-120.0, 1.2-60.0, 1.2-60.0, 8.0-400.0, 2.0-100.0, and 2.0-100.0 μg/mL, respectively; The average sample recovery rate range were 98.3%, 99.2%, 98.8%, 99.3%, 101.9%, 97.5%, 99.8%, 101.7%, 101.1%, 102.5%, and 100.9% (RSD < 2.0%); The content of 11 active ingredients in 16 batches of samples respectively were 0.233-0.322, 3.007-3.142, 2.201-2.273, 0.320-0.355, 0.317-0.399, 0.451-0.523, 0.265-0.297, 0.209-0.226, 1.848-1.873, 0.380-0.425, and 0.615-0.647 mg/g, respectively. Conclusion: The established method is simple, accurate and reproducible, and can provide the reference for the quality control of YYJG.
ABSTRACT
Objective: To optimize purification process of total alkaloid extract of Berberis dictyophylla cortex by macroporous resin,and to establish its quality standard. Method: Acid dye colorimetry was used to investigate the purification process of total alkaloid extract of B. dictyophylla cortex,the process parameters included concentration of sample solution,speed of sampling,diameter-height ratio of resin column,water washing amount,concentration and dosage of eluent,flow rate of elution,etc.In order to determine the optimum process,HPLC was employed to determine the contents of four alkaloids(magnoflorine,jatrorrhizine hydrochloride,palmatine hydrochloride,and berberine hydrochloride) with mobile phase of acetonitrile-0.1% phosphoric acid aqueous solution for gradient elution and detection wavelength at 270 nm.After being purified,quality standard of total alkaloid extract of B. dictyophylla cortex was investigated according to the requirements in the 2015 edition of Chinese Pharmacopoeia. Result: Optimal purification conditions were as following:10 g of HPD100 macroporous adsorption resin with a column diameter-height ratio of 1:8,sampling solution concentration of 11 g·L-1,the loading flow rate of 1 mL·min-1,sampling solution volume of 50 mL,washed with 4 BV of water(1 BV=15 mL) and added 9 BV of 30% ethanol,after being purified,the transfer rate of total alkaloids was>80%,and its purity was>65%.The quality standard of total alkaloid extract of B. dictyophylla cortex was established,there were 19 common peaks in the characteristic chromatogram,and the overall similarity was>0.99. Conclusion: This optimized purification process is stable and feasible, and the established quality standard is controllable.
ABSTRACT
Objective: To investigate the effect of berbamine hydrochloride on the absorption characteristics of berberine hydrochloride in different intestinal segments of rats in normal environment and high calcium environment. Method: Taking rat everted intestinal sac model,the content of berberine hydrochloride in absorbent solution of everted intestinal sac from different compatibility groups was determined by HPLC,and the uptake per unit area in different groups was analyzed by One-way ANOVA. Result: Compared with the normal J70 group(in normal environment,the concentration of berberine hydrochloride was 70 mg·L-1) at the same time point,the uptake per unit area of the normal J70+Ver100 group(in normal environment,the concentration of berberine hydrochloride was 70 mg·L-1,adding verapamil hydrochloride to a concentration of 100 mg·L-1) was significantly increased in the ileum(P-1,adding berbamine hydrochloride to a concentration of 35 mg·L-1) were significantly increased in the duodenum(P-1,adding berbamine hydrochloride to a concentration of 70 mg·L-1) were significantly increased in the ileum(PConclusion: Berbamine hydrochloride can promote the absorption of berberine hydrochloride in intestine to a certain extent,especially in the high calcium environment.
ABSTRACT
OBJECTIVE： To study the effects of berberine hydrochloride on the pharmacokinetics of tacrolimus in rats after single or multiple administration， and to provide reference for clinical combination therapy. METHODS： 30 rats were randomly divided into 5 groups， with 6 rats in each group： group one was treated with single administration of tacrolimus； group two was treated with tacrolimus intragastrically， twice a day， for consecutive 1 week； group three was treated with single administration of berberine hydrochloride， 5 min later given single administration of tacrolimus； group four was treated with tacrolimus intragastrically， twice a day， for consecutive 1 week， and then given tacrolimus intragastrically once 5 min after intragastric administration of berberine hydrochloride on the 8th day； group five was treated with berberine hydrochloride intragastrically， twice a day， and given tacrolimus intragastrically every 5 min， for consecutive 8 d. The doses of berberine hydrochloride and tacrolimus were 200 mg/kg and 0.945 mg/kg. The blood samples 0.3 mL were collected from posterior orbital venous plexus of rats 0， 5， 15， 30 min and 1， 2， 3， 4， 6， 8， 12 h after last intragastric administration of tacrolimus. The concentration of tacrolimus in rat whole blood was determined by LC-MS/MS. DAS 2.0 software was used for pharmacokinetic study. RESULTS： Compared with group one， the pharmacokinetic parameters AUC0-12 h， AUC0-∞ and MRT0-12 h of tacrolimus in rats were decreased significantly in group three （P＜0.05），while there was no statistical significance in all pharmacokinetic parameters of tacrolimus in group four （P＞0.05）. Compared with group two， AUC0-12 h of tacrolimus was decreased significantly while CLz was increased significantly in group four （P＜0.05）； there was no statistical significance in all pharmacokinetic parameters of tacrolimus in group five （P＞0.05）. CONCLUSIONS： Single and multiple intragastric administration of berberine hydrochloride has a certain effect on the pharmacokinetics of tacrolimus in rats， it shows that there is a downward trend in blood drug concentration and needs to be used with caution.
ABSTRACT
Objective: To optimize the optional extraction process parameters of Modified Simiao Granule (MSG). Methods: HPLC was employed to determine the content of rhodoglycoside, chlorogenic acid, ammonium glycyrrhizate, berberine hydrochloride, and glycyrrhizin, using the extraction ratio, dried cream yield, and fingerprint similarity of which as comprehensive evaluation indexes, orthogonal test was used to investigate effects of solid-liquid ratio, extraction time and times on extraction process. Information entropy method was used to determine the objective weight of each index to achieve orthogonal test optimization of extraction process. Results: According to the result of comprehensive score, the optimal extraction conditions of this preparation were as follows: extracted twice with 10 times of water quantity, each for 30 min. The mean of the three batches of comprehensive evaluation was 88.91 and the RSD value was 0.61%. Conclusion: The optimized technologies are stable, repeatable, feasible and suitable for the industrial production of MSG.