Glycyrrhizic Acid and Its Derivatives: Promising Candidates for the Management of Type 2 Diabetes Mellitus and Its Complications.

Type 2 diabetes mellitus (T2DM) is a chronic metabolic disease, which is characterized by hyperglycemia, chronic insulin resistance, progressive decline in ß-cell function, and defect in insulin secretion. It has become one of the leading causes of death worldwide. At present, there is no cure for T2DM, but it can be treated, and blood glucose levels can be controlled. It has been reported that diabetic patients may suffer from the adverse effects of conventional medicine. Therefore, alternative therapy, such as traditional Chinese medicine (TCM), can be used to manage and treat diabetes. In this review, glycyrrhizic acid (GL) and its derivatives are suggested to be promising candidates for the treatment of T2DM and its complications. It is the principal bioactive constituent in licorice, one type of TCM. This review comprehensively summarized the therapeutic effects and related mechanisms of GL and its derivatives in managing blood glucose levels and treating T2DM and its complications. In addition, it also discusses existing clinical trials and highlights the research gap in clinical research. In summary, this review can provide a further understanding of GL and its derivatives in T2DM as well as its complications and recent progress in the development of potential drugs targeting T2DM.

Long-Lasting Anti-Inflammatory and Antinociceptive Effects of Acute Ammonium Glycyrrhizinate Administration: Pharmacological, Biochemical, and Docking Studies.

The object of the study was to estimate the long-lasting effects induced by ammonium glycyrrhizinate (AG) after a single administration in mice using animal models of pain and inflammation together with biochemical and docking studies. A single intraperitoneal injection of AG was able to produce anti-inflammatory effects in zymosan-induced paw edema and peritonitis. Moreover, in several animal models of pain, such as the writhing test, the formalin test, and hyperalgesia induced by zymosan, AG administered 24 h before the tests was able to induce a strong antinociceptive effect. Molecular docking studies revealed that AG possesses higher affinity for microsomal prostaglandin E synthase type-2 compared to type-1, whereas it seems to locate better in the binding pocket of cyclooxygenase (COX)-2 compared to COX-1. These results demonstrated that AG induced anti-inflammatory and antinociceptive effects until 24-48 h after a single administration thanks to its ability to bind the COX/mPGEs pathway. Taken together, all these findings highlight the potential use of AG for clinical treatment of pain and/or inflammatory-related diseases.

Prolong the shelf-life of the Pakchoi seedlings through the ammonium glycyrrhizinate.

Pakchoi seedlings (Brassica chinensis L.) is susceptible to damage and spoilage during harvest and transport, leading to significant quality deterioration and financial losses. This study explored the use of ammonium glycyrrhizinate (AG) to address these issues. AG self-assembles into macromolecules at room temperature, blocking stomata and regulating respiration rates in Pakchoi seedlings. Additionally, it disrupts bacterial cell biofilm and inhibits its synthesis. While AG has been used in medicine, its application in the food industry remains limited. The study found that incorporating AG in Pakchoi seedlings preserves water content and total soluble solids (TSS), while preventing declines in catalase (CAT), Vitamin C (VC), and chlorophyll during storage. AG also reduced malondialdehyde (MDA) levels and maintained peroxidase (POD) and superoxide dismutase (SOD) activities. At a concentration of 4.25 g L-1, AG enhanced radical scavenging ability and extended the shelf life of Pakchoi seedlings by inhibiting bacteria and postponing senescence.

Ammonium Glycyrrhizinate and Bergamot Essential Oil Co-Loaded Ultradeformable Nanocarriers: An Effective Natural Nanomedicine for In Vivo Anti-Inflammatory Topical Therapies.

Bergamot essential oil (BEO) and Ammonium glycyrrhizinate (AG), naturally derived compounds, have remarkable anti-inflammatory properties, thus making them suitable candidates for the treatment of skin disorders. Despite this, their inadequate physicochemical properties strongly compromise their topical application. Ultradeformable nanocarriers containing both BEO and AG were used to allow their passage through the skin, thus maximizing their therapeutic activity. Physicochemical characterization studies were performed using Zetasizer Nano ZS and Turbiscan Lab®. The dialysis method was used to investigate the release profile of the active compounds. In vivo studies were performed on human healthy volunteers through the X-Rite spectrophotometer. The nanosystems showed suitable features for topical cutaneous administration in terms of mean size, surface charge, size distribution, and long-term stability/storability. The co-delivery of BEO and AG in the deformable systems improved both the release profile kinetic of ammonium glycyrrhizinate and deformability properties of the resulting nanosystems. The topical cutaneous administration on human volunteers confirmed the efficacy of the nanosystems. In detail, BEO and AG-co-loaded ultradeformable vesicles showed a superior activity compared to that recorded from the ones containing AG as a single agent. These results are promising and strongly encourage a potential topical application of AG/BEO co-loaded nanocarriers for anti-inflammatory therapies.

Micelle Formation of Monoammonium Glycyrrhizinate.

Monoammonium glycyrrhizinate is produced by the neutralization of glycyrrhizic acid from plant licorice with ammonia. In this study, the physicochemical properties of aqueous monoammonium glycyrrhizinate were investigated from the viewpoint of surface chemistry. The structure of the amphiphilic molecule is bola type, comprising two glucuronic acid moieties having two carboxylic acids groups and an aglycone part having a carboxylic acid at the opposite end of the molecule from the glucuronic acids. We found that the physicochemical properties of aqueous monoammonium glycyrrhizinate are dependent on the ionization of the carboxylic acid groups. The solubility of monoammonium glycyrrhizinate gradually increased above pH 4 in the buffer solution. The critical micelle concentration (CMC) and surface tension at the CMC (γCMC) of monoammonium glycyrrhizinate were determined by the surface tension method to be 1.5 mmol L-1 and 50 mN m-1 in pH 5 buffer and 3.7 mmol L-1 and 51 mN m-1 in pH 6 buffer, respectively. The surface tension gradually decreased with increasing concentration of monoammonium glycyrrhizinate in the pH 7 buffer, but the CMC was not defined by the curve. Light scattering measurements also did not reveal a clear CMC in the pH 7 buffer. The ionization of the carboxylic acid groups in the bola-type amphiphilic molecule with increasing pH is disadvantageous for micelle formation. Cryo-transmission electron microscopy showed that monoammonium glycyrrhizinate forms rod-like micelles in pH 5 buffer, and small angle X-ray scattering experiments confirmed that the average micellar structure was rod-like in pH 5 buffer. Thus, it was found that monoammonium glycyrrhizinate can form micelles only in weakly acidic aqueous solutions.

Topical Unsaturated Fatty Acid Vesicles Improve Antioxidant Activity of Ammonium Glycyrrhizinate.

Linoleic and oleic acids are natural unsaturated fatty acids involved in several biological processes and recently studied as structural components of innovative nanovesicles. The use of natural components in the pharmaceutical field is receiving growing attention from the scientific world. The aim of this research work is to design, to perform physico-chemical characterization and in vitro/in vivo studies of unsaturated fatty acids vesicles containing ammonium glycyrrhizinate, obtaining a new topical drug delivery system. The chosen active substance is well known as an anti-inflammatory compound, but its antioxidant activity is also noteworthy. In this way, the obtained nanocarriers are totally natural vesicles and they have shown to have suitable physico-chemical features for topical administration. Moreover, the proposed nanocarriers have proven their ability to improve the in vitro percutaneous permeation and antioxidant activity of ammonium glycyrrhizinate on human keratinocytes (NCTC 2544 cells). In vivo studies, carried out on human volunteers, have demonstrated the biocompatibility of unsaturated fatty acid vesicles toward skin tissue, indicating a possible clinical application of unsaturated fatty acid vesicles for the treatment of topical diseases.

Ammonium Glycyrrhizinate Prevents Apoptosis and Mitochondrial Dysfunction Induced by High Glucose in SH-SY5Y Cell Line and Counteracts Neuropathic Pain in Streptozotocin-Induced Diabetic Mice.

Glycyrrhiza glabra, commonly known as liquorice, contains several bioactive compounds such as flavonoids, sterols, triterpene, and saponins; among which, glycyrrhizic acid, an oleanane-type saponin, is the most abundant component in liquorice root. Diabetic peripheral neuropathy is one of the major complications of diabetes mellitus, leading to painful condition as neuropathic pain. The pathogenetic mechanism of diabetic peripheral neuropathy is very complex, and its understanding could lead to a more suitable therapeutic strategy. In this work, we analyzed the effects of ammonium glycyrrhizinate, a derivate salt of glycyrrhizic acid, on an in vitro system, neuroblastoma cells line SH-SY5Y, and we observed that ammonium glycyrrhizinate was able to prevent cytotoxic effect and mitochondrial fragmentation after high-glucose administration. In an in vivo experiment, we found that a short-repeated treatment with ammonium glycyrrhizinate was able to attenuate neuropathic hyperalgesia in streptozotocin-induced diabetic mice. In conclusion, our results showed that ammonium glycyrrhizinate could ameliorate diabetic peripheral neuropathy, counteracting both in vitro and in vivo effects induced by high glucose, and might represent a complementary medicine for the clinical management of diabetic peripheral neuropathy.

Simultaneous determination of seven constituents in Chenxiang Lubailu tablet by HPLC / 药学实践与服务

Objective To establish the method for the simultaneous determination of liquiritin, ammonium glycyrrhizinate, hesperidin, nobiletin;tangeretin;costunolide, dehydrocostuslactone in Chenxiang Lubailu tablet by HPLC. Methods ZORBAX Eclipse XDB-C18 chromatographic column (4.6 mm×250 mm, 5 μm) was used. The mobile phase was methanol-0.1% phosphoric acid solution. Gradient elution with flow rate of 1.0 ml/min was used. Column temperature was 35 ℃. Detection wavelength for liquiritin, ammonium, tangeretin, and costunolide was at 237 nm. Detection wavelength for glycyrrhizinate was at 283 nm. Detection wavelength for hesperidin and nobiletin was at 330 nm. Injection volume was 10 μl. 16 batches of samples were tested. Results The linear ranges for the detection of liquiritin, ammonium, glycyrrhizinate, hesperidin, nobiletin, tangeretin, and costunolide were 1.110 - 55.72 (r=0.9992), 22.15 - 1108 (r=0.9999), 6.140 - 307.2 (r=0.9995), 1.130 - 56.25 (r=0.9997), 0.3700 - 18.75 (r=0.9982), 0.5200 - 26.01 (r=0.9991), and 1.180 - 58.95 (r=0.9999) μg/ml respectively. The average recoveries were 98.71%, 98.12%, 98.44%, 98.22%, 99.17%, 99.18%, and 97.93%, and the RSDs were 0.16%, 0.67%, 0.57%, 0.62%, 0.48%, 0.56%, and 0.58% respectively. The contents of the seven components in 16 batches of samples were 0.1250 - 1.174, 2.354 - 7.426, 1.822 - 27.21, 0.0370 - 1.399, 0.0723 - 0.4433, 0.0140 - 0.1990, and 0.2207 - 1.407 mg/g respectively. Conclusion The method is accurate, reproducible and durable, which could be used to the quality control and evaluation of Chenxiang Lubailu tablet.

Kegan Liyan oral liquid ameliorates lipopolysaccharide-induced acute lung injury through inhibition of TLR4-mediated NF-κB signaling pathway and MMP-9 expression.

ETHNOPHARMACOLOGICAL RELEVANCE: Kegan Liyan oral liquid (KGLY), a Chinese prescription modified from classic formulas Yin-Qiao-San (from TCM classic Wenbing Tiaobian) and Shen-Jie-San (first mentioned in Shanghan Wenyi Tiaobian), has been reported to exert heat-clearing and detoxifying effects and used extensively for the treatment of severe pulmonary diseases in clinics including influenza, cough and pneumonia. AIM OF THIS STUDY: The purpose of this study was to investigate the protective effect of KGLY on lipopolysaccharide (LPS) induced acute lung injury (ALI) in mice and to illuminate the underlying mechanisms. MATERIALS AND METHODS: Mice were orally administrated with KGLY (50, 100 and 150mg/kg) before intratracheal instillation of LPS. 24h post LPS challenge, lung tissues and the bronchoalveolar lavage fluid (BALF) were collected for lung wet/dry (W/D) weight ratio, histopathological examinations and biochemical analyses. The cell counts, protein concentration, interleukin-1ß (IL-1ß), interleukin-6 (IL-6), necrosis factor-α (TNF-α), macrophage inflammatory protein-2 (MIP-2) in BALF, superoxide dismutase (SOD), glutathione (GSH), myeloperoxidase (MPO) and malondialdehyde (MDA) levels were detected. Meanwhile, the activation of toll-like receptor 4 (TLR4), nuclear factor kappa B (NF-κB), as well as matrix metalloproteinases 9 (MMP-9) were determined by western blot assay. RESULTS: KGLY significantly prolonged mice survival time and ameliorated LPS-induced edema, thickening of alveolar septa and inflammatory cell infiltration in a dose-dependent manner. Additionally, KGLY markedly attenuated LPS-induced acute pulmonary inflammation via decreasing the expressions of cytokines and chemokines (IL-1ß, IL-6, TNF-α, and MIP-2), enhanced the activities of anti-oxidative indicators (SOD and GSH), suppressed the levels of MPO and MDA, and down-regulated the expressions of TLR4, NF-κB and MMP9. CONCLUSIONS: The results suggested that the relieving effect of KGLY against LPS-induced ALI might be partially due to suppression of oxidative stress and inflammatory response, inhibition of TLR4-mediated NF-κB activation, and down-regulation of MMP9 expression, indicating it may be a potential therapeutic agent for ALI.

Quality control of Tibetan medicine Baimai Ointment based on multi-component determination, fingerprint and multivariate statistical analysis / 中草药

Objective: To establish a fingerprint method of Baimai Ointment (BO) and determine the content of its main components. The BO of 14 batches from two production areas was scientifically and comprehensively evaluated based on multivariate statistical analysis, which provided the basis for the quality control. Methods: HPLC method was used to determine the content of liquiritin, ammonium glycyrrhizinate, nardosinone and curcumin in BO, and the fingerprint of BO was established. The fingerprint similarity analysis, cluster analysis, principal component analysis (PCA) and factor analysis were performed to comprehensively evaluate the different batches of BO in two producing areas. Results: The methodological determination of liquiritin, ammonium glycyrrhizinate, nardosinone and curcumin met the requirements, and the content was 0.051-0.200 mg/g, 0.136-0.622 mg/g, 0.030-0.345 mg/g, 0.001-0.069 mg/g, respectively. The established fingerprints of BO were calibrated with 17 common peaks. Three chromatographic peaks of liquiritin, ammonium glycyrrhizinate and nardosinone were identified by reference. The similarity of 14 batches of sample was greater than 0.975. In the cluster analysis, 14 batches of BO from two producing areas can be divided into four categories, among which batches S1-S11 produced by Linzhi City of Tibet were grouped into one category. And S12 produced in Lanzhou City of Gansu Province was clustered into one class, and S13 was clustered into one class, S14 was grouped into one class. The results of PCA and factor analysis showed that the comprehensive scores of the three batches of S12-S14 produced in Lanzhou City of Gansu Province were higher than the 11 batches of S1-S11 produced by Linzhi City of Tibet, presumably because of the changes in production conditions or sources of medicinal materials. The result was consistent with cluster analysis. Conclusion: This study is the first to establish a scientific and reliable quality control method of Tibetan medicine BO based on multi-component determination, fingerprint and multivariate statistical analysis. It can be used not only for the quality control of Baimai Ointment, but also for the comprehensive evaluation of batch quality consistency. It provides reference for the improvement of the quality standard of BO and the quality evaluation among Chinese medicine batches.

Cardioprotective effect of ammonium glycyrrhizinate against doxorubicin-induced cardiomyopathy in experimental animals.

OBJECTIVE: The objective of this study was to evaluate the cardioprotective effect of herbal bioactive compound ammonium glycyrrhizinate against doxorubicin-induced cardiomyopathy, in experimental animals. MATERIALS AND METHODS: Ammonium glycyrrhizinate (50, 100, 200 mg/kg, p.o.) was administered for four weeks in albino rats. Cardiomyopathy was induced with a dose of 2.5 mg/kg i.p. of doxorubicin on 1(th), 7(th), 14(th), 21(th), 28(th) day in the experimental animals. At the end of the experiment, on 29(th) day, serum and heart tissues were collected and hemodynamic, biochemical and histopathological studies were carried out. RESULTS: Administration of doxorubicin in normal rats showed significant (P < 0.001) changes in body weight, feed intake, urine output, hemodynamic parameters like (blood pressure, heart rate, cardiac output) and in lipid profile (cholesterol, triglyceride, high density lipoprotein, low density lipoprotein, very low density lipoprotein) indicating cardiomyopathy symptoms. Animals treated with ammonium glycyrrhizinate significantly (P < 0.05) decreased triglyceride, cholesterol, low density lipoprotein (LDL) and very low density lipoprotein (VLDL) levels. Moreover, high density lipoprotein (HDL) levels increased in rats treated with ammonium glycyrrhizinate as compared with the normal group. CONCLUSION: Ammonium glycyrrhizinate is effective in controlling serum lipid profile and cardiac complications in experimentally induced cardiomyopathy in animals.

Ammonium glycyrrhizinate-loaded niosomes as a potential nanotherapeutic system for anti-inflammatory activity in murine models.

BACKGROUND: Liquorice extracts demonstrate therapeutic efficacy in treating dermatitis, eczema, and psoriasis when compared with corticosteroids. In this work, nonionic surfactant vesicles (niosomes, NSVs) containing polysorbate 20 (Tween 20), cholesterol, and cholesteryl hemisuccinate at different molar concentrations were used to prepare monoammonium glycyrrhizinate (AG)-loaded NSVs. The anti-inflammatory properties of AG-loaded NSVs were investigated in murine models. METHODS: The physicochemical properties of the NSVs were characterized using dynamic light scattering. The fluidity of the lipid bilayer was evaluated by measuring the fluorescence intensity of diphenylhexatriene. The drug entrapment efficiency of AG was assessed using high-performance liquid chromatography. The physicochemical stability of the NSVs was evaluated as a function of time using dynamic light scattering combined with Turbiscan Lab Expert analysis. Serum stability was determined by incubating the NSVs with 10% v/v fetal bovine serum. The cytotoxic effects of the NSVs were investigated in human dermal fibroblasts using the Trypan blue dye exclusion assay (for cell mortality) and an MTT assay (for cell viability). Release profiles for the AG-loaded NSVs were studied in vitro using cellulose membranes. NSVs showing the most desirable physicochemical properties were selected to test for in vivo anti-inflammatory activity in murine models. The anti-inflammatory activity of the NSVs was investigated by measuring edema and nociception in mice stimulated with chemical agents. RESULTS: NSVs showed favorable physicochemical properties for in vitro and in vivo administration. In addition, they demonstrated long-term stability based on Turbiscan Lab Expert analysis. The membrane fluidity of the NSVs was not affected by self-assembling of the surfactants into colloidal structures. Fluorescence anisotropy was found to be independent of the molar ratios of cholesteryl hemisuccinate and/or cholesterol during preparation of the NSVs. The anti-inflammatory AG drug showed no effect on the stability of the NSVs. In vivo experiments demonstrated that AG-loaded NSVs decreased edema and nociceptive responses when compared with AG alone and empty NSVs. In vitro and in vivo results demonstrated that pH sensitive and neutral NSVs show no statistical significant difference. CONCLUSION: NSVs were nontoxic and showed features favorable for potential administration in vivo. In addition, neutral NSVs showed signs of increased anti-inflammatory and antinociceptive responses when compared with AG.

Establishment of HPLC fingerprint and determination of three components of classical Linggui Zhugan Decoction / 中草药

Objective: To establish an HPLC fingerprint of classical named Linggui Zhugan Decoction and determination method of the content of three compounds, and provide reference for the study of the material basis of the classical Linggui Zhugan Decoction. Methods: The method was performed by high performance liquid chromatography with CNW Athena C18 (250 mm × 4.6 mm, 5 μm) and gradient elution with acetonitrile (A)-0.1% phosphoric acid (B) as the mobile phase, gradient elution: 0-10 min, 5%-10%; 10-20 min, 10%-15% A; 20-50 min, 15%-30% A; 50-75 min, 30%-40% A; 75-95 min, 40%-50% A; 95-111 min, 50%-95% A. The flow rate was 1.0 mL/min, the injection volume was 10 μL, and the column temperature is 30 ℃. The fingerprint and the detection wavelength of glycyrrhizin and ammonium glycyrrhizinate were 230 nm, and cinnamic aldehyde was 290 nm. The chromatographic fingerprint evaluation system published by the State Pharmacopoeia Commission (2012 Edition) was used to establish the fingerprint of 10 batches of Lingguizhugan decoction, and the content of three kinds of index components were determined simultaneously by the established HPLC method. Results: The research on the 10 batches of Lingguizhugan soup showed that the fingerprint similarity was greater than 0.9, and 24 common peaks were calibrated, and the peak resolution was good. The content determination results showed that the content of glycyrrhizin and ammonium glycyrrhizinate was high. According to the methodological investigation, the three components showed a good linear relationship within a certain concentration range; The precision RSD values were all less than 1.0%; The average recovery rates of glycyrrhizin, cinnamaldehyde and ammonium glycyrrhizinate were 98.35%, 101.51%, and 102.59%, respectively. The RSD is less than 2.5%; The sample is stable within 48 h, and the method has good repeatability. Conclusion: The fingerprint method and the determination method of three components in the traditional Chinese medicine classical prescription named Linggui Zhugan Decoction established in this study are simple, stable, accurate and reliable, and can be used for the quality control of the Linggui Zhugan Decoction.

Aqueous extract of Glycyrrhiza inflata inhibits aggregation by upregulating PPARGC1A and NFE2L2-ARE pathways in cell models of spinocerebellar ataxia 3.

Spinocerebellar ataxia (SCA) types 1, 2, 3, 6, 7, and 17 and dentatorubropallidoluysian atrophy, as well as Huntington disease, are a group of neurodegenerative disorders caused by a CAG triplet-repeat expansion encoding a long polyglutamine (polyQ) tract in the respective mutant proteins. The cytoplasmic and nuclear aggregate formation, a pathological hallmark of polyQ diseases, is probably the initial process triggering the subsequent pathological events. Compromised oxidative stress defense capacity and mitochondrial dysfunction have emerged as contributing factors to the pathogenesis of polyQ diseases. The roots of licorice (Glycyrrhiza species) have long been used as an herbal medicine. In this study, we demonstrate the aggregate-inhibitory effect of Glycyrrhiza inflata herb extract and its constituents licochalcone A and ammonium glycyrrhizinate (AMGZ) in both 293 and SH-SY5Y ATXN3/Q75 cells, SCA3 cell models. The reporter assay showed that G. inflata herb extract, licochalcone A, and AMGZ could enhance the promoter activity of peroxisome proliferator-activated receptor γ, coactivator 1α (PPARGC1A), a known regulator of mitochondrial biogenesis and antioxidative response genes. G. inflata extract, licochalcone A, and AMGZ upregulated PPARGC1A expression and its downstream target genes, SOD2 and CYCS, in the 293 ATXN3/Q75 cell model. The expression of nuclear factor erythroid 2-related factor 2 (NFE2L2), the principal transcription factor that binds to antioxidant-responsive elements (AREs) to promote ARE-dependent gene expression when the cells respond to oxidative stress, and its downstream genes, HMOX1, NQO1, GCLC, and GSTP1, was also increased by G. inflata herb extract, licochalcone A, and AMGZ. Knockdown of PPARGC1A increased aggregates in ATXN3/Q75 cells and also attenuated the aggregate-inhibiting effect of the tested compounds. G. inflata extract and its constituents significantly elevated GSH/GSSG ratio and reduced reactive oxidative species in ATXN3/Q75 cells. The study results suggest that the tested agents activate PPARGC1A activity and NFE2L2-ARE signaling to increase mitochondrial biogenesis, decrease oxidative stress, and reduce aggregate formation in SCA3 cellular models.

Difference of chemical constituents and efficacy between crude and processed Pinelliae Rhizoma / 中草药

Objective To study the chemical constituents and effects of crude and processed Pinelliae Rhizoma. Methods The contents of inosine, guanosine, adenosine, succinic acid, ephedrine hydrochloride, liquiritin, glyeyrrhizie acid, and 6-gingerol of Pinelliae Rhizoma, Pinelliae Rhizoma Praeparatum cum Alumine, Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine, and Pinelliae Rhizoma Praeparatum were detected by HPLC. The pharmacodynamics of the traditional efficacy of expectorant and cough relieving was studied by stimulating mice with phenol red and concentrated ammonia in the trachea of mice. Results The contents of inosine, guanosine, adenosine, succinic acid, and ephedrine hydrochloride decreased significantly after processing, and inosine was not detected in Pinelliae Rhizoma Praeparatum cum Alumine. Compared with the three processed products, the content of inosine, guanosine, adenosine and succinic acid was the highest in the Pinelliae Rhizoma Praeparatum cum Alumine, the lowest was in Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine, and in consistent with the effect of resolving phlegm. The four components were the active components of resolving phlegm effect. Adding alumen during Pinelliae Rhizoma Praeparatum cum Alumine processing has also enhanced its effectiveness. Pinelliae Rhizoma Praeparatum has the strongest antitussive effect, followed by Pinelliae Rhizoma, Pinelliae Rhizoma Praeparatum cum Alumine and Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine. Adding licorice and lime water during Pinelliae Rhizoma Praeparatum processing, licorice (peak 6: liquiritin, peak 7: ammonium glycyrrhizinate) had a powerful antitussive effect and enhanced its antitussive effect. After processing by ginger and white peony, ginger (peak 8: 6-gingerol) is good at warming middle energizer to arrest vomiting, thus enhance antiemetic effect and weaken phlegm, cough effect of Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine. Conclusion The chemical composition and efficacy of Pinelliae Rhizoma have changed after being processed, and different processing methods have different effects on its chemical composition and efficacy.

Quaily Analysis of Weiling Granules / 中国药师

Objective: To analyze 167 batches of Weiling granules according to the quality standard and exploratory research, and evaluate the overall quality and standard condition of the preparation. Methods: A TLC method was established for the identification of Atractylodis macrocephalae Rhizoma;an HPLC method was established for the fingerprint and the content determination of paeoniflorin, tetrahydropalmatine and ammonium glycyrrhizinate. An Agilent Poroshell120,SB-C18analytical column (100 mm×4. 6 mm, 2. 7 μm) was employed with gradient elution of acetonitrile-0. 1% phosphoric acid as the mobile phase at the flow rate of 1. 8 ml·min-1, and the sample size was 3 μl. Acid base titration method was used for measuring acid-neutralizing capacity. Results: No interference from the negative controls was shown to the TLC identification of Atractylodis macrocephalae Rhizoma. The fingerprint exhibited better separation of each peak. The precision, reproducibility and stability of the method were good,and the RSDs of the relative retention time and rela-tive peak area were less than 3. 0% . The linear range of paeoniflorin, tetrahydropalmatine and ammonium glycyrrhizinate was 0. 057-0. 568 μg(r=0. 999 9), 0. 035-0. 353 μg(r=0. 999 9)and 4. 244×10 -3-42. 44×10 -3μg(r=0. 999 9), respectively, and the av-eragerecoverywas99.3%(RSD=1.0%,n=6),100.0%(RSD=0.8%,n=6) and99.8%(RSD=1.2%,n=6),respectively. The average recovery of acid-neutralizing capacity was 99. 5% (RSD=0. 5% ,n=6). Conclusion: Exploratory research increases the specificity, controllability and safety of the standards, which provides reference for the further drug standards revision and the drug quality control.

Research on HPLC Fingerprint of Jinsangqi Kangdu Dropping Pills / 中国中医药信息杂志

Objective To establish fingerprint of Jinsangqi Kangdu Dropping Pills by HPLC; To control the quality of the preparation. Methods Waters XSELECT CSH-C18 chromatographic column (4.6 mm × 150 mm, 5 μm) was used and eluted with acetonitrile - 0.1% phosphoric acid solution gradient at the flow rate of 1.0 mL/min. The detection wavelength was 260 nm with column temperature of 30 ℃. Using calycosin-7-O-β-D-glucopyranoside, rutin, liquiritin, hyperoside, quercetin and ammonium glycyrrhizinate as the object references, ten batches of Jinsangqi Kangdu Dropping Pills were tested and analyzed by similarity comparison.Results Fringerprint spectrum of Jinsangqi Kangdu Dropping Pills had 24 common peaks in total, and characteristic spectrums of Hypericum Perforatum, Mori Cortex, Astragali Radix and Glycyrrhizae Radix et Rhizoma had been found, while similarity of HPLC fingerprint was more than 0.9 among those batches of samples. Conclusion Using HPLC fingerprint can evaluate the Jinsangqi Kangdu Dropping Pills quality totality,which can provide references for improving the quality control of the preparation.

Simultaneous Determination of 5 Constituents in Xiao'er Magan Granule by HPLC-QAMS / 中国药师

Objective:To develop a method of quantitative analysis of multi-components by single marker(QAMS)for the determi-nation of five constituents(ephedrine hydrochloride,amygdalin,liquiritin, baicalin and ammonium glycyrrhizinate)in Xiao'er Magan granule. Methods:Amygdalin was used as the internal reference substance, and the relative correlation factors(RCF) of ephedrine hydrochloride,liquiritin,baicalin and ammonium glycyrrhizinate to amygdalin were calculated and evaluated. The contents of the five constituents were determined by the external standard method(ESM) and QAMS,respectively. The content results determined by the two methods were compared and the feasibility of QAMS method was verified. Results:The RCF between amygdalin and the other con-tents was 1.237,1.318,1.327 and 0.884,respectively. There were no significant differences in the results between QAMS and ESM with the relative errors less than 0.3%. Conclusion:The QAMS method is accurate and feasible for the simultaneous determination of Xiao'er Magan granule.

Simultaneous Determination of 3 Components in Xiaoer Huadu Powder by HPLC / 中国药房

OBJECTIVE:To establish a method for simultaneous determination of paeoniflorin,berberine hydrochloride and ammonium glycyrrhizinate in Xiaoer huadu powder.METHODS:HPLC method was adopted.The separation was performed on Waters SunFireTM-C18 column with mobile phase consisted of acetonitrile-0.1％ phosphoric acid (gradient elution) at the flow rate of 1.0 mL/min.The detection wavelength was set at 238 nm,and column temperature was 25 ℃.The sample size was 10 μL.RESULTS:The linear ranges of paeoniflorin,berberine hydrochloride and ammonium glycyrrhizinate were 8.808-88.08 μg/mL(r=0.999 8),1.778-17.78 μg/mL(r=0.999 6),2.533-25.33 μg/mL(r=0.999 9),respectively.LOQ were 4.404,0.889,2.533 μg/mL;LOD were 1.101,0.445,1.267 μg/mL.RSDs of precision,stability and reproducibility tests were all lower than 2％.The recoveries were 95.08％-99.61％ (RSD=1.77％,n =9),96.93％-99.94％ (RSD=0.92％,n=9),98.33％-102.05％ (RSD=1.27％,n=9).CONCLUSIONS:The method is simple,accurate and reproducible,and can be used for simultaneous determination of paeoniflorin,berberine hydrochloride and ammonium glycyrrhizinate in Xiaoer huadu powder.

Establishment of Quality Standard for Extractum Glycyrrhizae Capsules / 中国药师

Objective:To establish the quality standard for two effective components in extractum glycyrrhizae capsules. Methods:Radix glycyrrhizae was identified by a TLC method. The contents of liquiritin and ammonium glycyrrhizinate in extractum glycyrrhizae capsules were determined by HPLC. An Inertsil C18 (150 mm × 4. 6 mm, 5μm) column was used. The mobile phase consisted of ace-tonitrile (A)-0. 2％ phosphoric acid (B) (0-8 min: 20％A-20％A;8-34 min: 20％A-50％A;34-35 min: 50％A-100％A;35-40 min:100％A-20％A) at a flow rate of 1. 0 ml·min-1 . The detection wavelength was at 237 nm under 25℃. Results: The spots in TLC were clear. Liquiritin showed a good linear relationship within the range of 0. 0020-0. 1000 mg·ml-1(r=0. 9995). The aver-age recovery was 100. 29％, and the RSD was 2. 94％(n=6). Ammonium glycyrrhizinate showed a good linear relationship within the range of 0. 0020-0. 1000 mg·ml-1(r=0. 9998). The average recovery was 101. 46％, and the RSD was 2. 33％(n=6). Conclu-sion:The method is simple,reliable and reproducible, which can be used for the quality control of the preparation.