Journal of Chinese Pharmaceutical Sciences

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2012, 21(3): 201-204.

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Drug management of hypertension in hemodialysis patients

Kong-Cai Zhu, Guo-Ying Cao^*, Xin Hu

2012, 21(3): 205-210. DOI: 10.5246/jcps.2012.03.026

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Hypertension is believed to be a major risk factor that causes cardiovascular disease in patients on hemodialysis (HD). Removing of excess water during HD, accurate assessment of dry weight and anti-hypertension therapeutics are the most commonly used measures to lower blood pressure in patients on HD.

Determination of metformin in diabetic rat plasma by an improved ion-pair high-performance liquid chromatography: application to a pharmacokinetic study

Ye Chen, Han-Qing Li, Jiao-Jiao Xu, Xiang-Fei Jiu, Chen-Hui Deng, Xin-Gang Li, Liang Li, Xiao-Qing Xu, Tian-Yan Zhou^*, Wei Lu^*

2012, 21(3): 211-218. DOI: 10.5246/jcps.2012.03.027

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An efficient and sensitive ion-pair HPLC-UV method using atenolol as internal standard (IS) was developed and validated for the determination of metformin in the plasma of diabetic rats. Plasma samples were deproteinated with 10% (v/v) perchloric acid. Separation was achieved on a Ultimate^TM AQ-C18 column (250 mm×4.6 mm, 5 μm) with a mobile phase (pH 5.05) composed of acetonitrile-water (31:69, v/v, containing 0.002 M sodium dodecyl sulfate, 0.0125 M potassium dihydrogen phosphate, 0.015 M triethylamine) at a flow rate of 1.0 mL/min. The calibration curve was linear (r>0.994) between 7.5 and 4000 ng/mL. The lower limit of quantification (LLOQ) was 7.5 ng/mL. The precision was validated and the relative standard deviation was in the range of 1.87% to 15.70%; the accuracy was between 93.98%-106.89%. The mean recoveries were 95.40% and 95.31% for metformin and IS, respectively. The relative error (RE) of stability at different storage conditions was within ±9.00%. This method was used to determine the concentration-time profile of metformin in diabetic rat plasma following an oral administration of metformin at the dose of 10 mg/kg. Our results indicated that ion-pair HPLC-UV method using Ultimate^TM AQ-C18 column was effective for the pharmacokinetic studies of high polarity compounds like metformin.

Rapid determination of quercetin-3'-O-glucoside in rat plasma by high
performance liquid chromatography-tandem mass spectrometry

Hui-Lian Huang, Ke-Lan Liu, Feng Shao, Gang Ren, Yao-Hui Ye, Shou-Wen Zhang, Rong-Hua Liu^*

2012, 21(3): 219-225. DOI: 10.5246/jcps.2012.03.028

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A method for the quantification of quercetin-3'-O-glucoside in rat plasma by high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was developed and validated. Along with internal standard (carbamazepine), quercetin-3'-O-glucoside was extracted from plasma samples by simple liquid-liquid extraction with ethyl acetate. The mass spectrometry detection was set in multiple reaction monitoring (MRM) mode via positive electrospray ionization (ESI). The chromatographic run time was 3.5 min per sample. The calibration curves were linear (r² = 0.9992) with a lower limit of quantification (LLOQ) of 10.625 ng/mL, and the limit of detection (LOD) was 4.25 ng/mL. The intra- and inter- day precision and accuracy, in terms of relative standard deviation (RSD), were all lower than 10.44%. The recovery rate of the analyte and internal standard were higher than 66.80%. After intravenous administration of 10 mg/kg quercetin-3'-O-glucoside, the t1/2 and AUC were (0.02±0.01) h and (1.22±0.28)×10⁴μg/L·h. The method is accurate, stable and sensitive, which is suitable for the pharmacokinetic study of quercetin-3'-O-glucoside in rats.

Preparation and property of mPEG-PLA/pluronic mixed micelles and their role in solubilization of propofol

Gui-Ling Li, Xin-Ru Li, Ya-Ting Fan, Yan-Hui Zhang, Mei Li, Yan Liu^*

2012, 21(3): 226-233. DOI: 10.5246/jcps.2012.03.029

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Novel mixed polymeric micelles formed by biocompatible polymers, mPEG-PLA and Pluronic P105, were fabricated and used as a nanocarrier to solubilize the poorly soluble anesthetic drug propofol. Propofol was added directly to an aqueous solution of mPEG-PLA/Pluronic P105 mixed micelles and stirred into a micellar solution. The average particle size and size distribution of micelles were evaluated by the dynamic light scattering technology. Drug loading content, encapsulation efficiency and free drug concentration were determined by using ultracentrifugation and lyophilization. In vitro release characteristic of propofol formulation was investigated by dialysis method. The physical stability of mixed micelles was also assessed under storage condition (4 ºC) after six months. Sleep-recovery studies in male Sprague-Dawley rats, at a dose of 10 mg/kg were performed to compare the pharmacodynamic profiles of propofol in mixed micelles with that of commercial lipid emulsion (CLE). The results indicated that solubilization of propofol in the mixed micelles was more efficient than that in mPEG-PLA alone. Micelles with the optimized composition of mPEG-PLA/Pluronic P105/Propofol (10:4:5, w/w/w) had particle size of about 90 nm with narrow distribution (polydispersity index of about 0.2). The content of free propofol in the aqueous phase of mixed micelles was significantly lower than that in CLE (P<0.05). There was no remarkable differences for particle size, polydispersity index, and free drug concentration when the mix micelles were stored at 4 ºC for six months, suggesting that the propofol-loaded mixed micelles were stable for at least six months. The accumulative release of mixed micelles was significantly higher than that of CLE at the corresponding time points, suggesting that quick release rate for mixed micelles might produce favorable pharmacological effect. No significant differences in the unconsciousness time and recovery time of righting reflex were observed between the mixed micelles and CLE (P>0.05). In conclusion, the mixed micelle of mPEG-PLA and pluronic copolymer may be a promising candidate for intravenous delivery of propofol in clinic.

Curative effect of novel oral carbon microspheres on streptozotocin-induced
diabetes mellitus in rats

Qing Shen, Shan-Shan Gao, Yi-Ni Xie, Li-Cheng Ling, Feng Gao^*

2012, 21(3): 234-241. DOI: 10.5246/jcps.2012.03.030

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A kind of novel pitch-based activated carbon microsphere (ACM) characterized by its controlled porous structure was developed in this study, the curative effect of this ACM on diabetes mellitus in rats was investigated. ACM 0.2-0.3 mm in diameter was prepared by modified method. The optimal ACM was screened by its adsorption ability for glucose. Diabetes mellitus model was established by streptozotocin injection in male Sprague-Dawley rats. Two groups of rats were orally administrated with ACM twice a day for 30 d. Intestinal glucose transport was determined in vitro using everted rat intestinal sacs technique. Compared with the diabetic mellitus group, the ACM treated group showed significant lower blood glucose level and improved glucose tolerance after two-week treatment. If ACM was applied in the mucosal side, glucose permeation clearance in the ACM treated group was significantly higher than that of the control group, especially at high glucose concentration (10 mg/mL) on the serosal side. The selected ACM possessed a BET specific surface of 1566 m²/g and high volume of micropores (0.478 cm³/g) with fine spherical morphology, and showed more significant adsorption capacity for glucose. As oral microsphere preparations, ACM presented the curative effect on streptozotocin-induced diabetes mellitus in rats.

Preparation and in vitro evaluation of gelatin microspheres for embolization

Ya-Nan Wu, Wen-Jing Meng, Ying-Ying Liu, Tong Guo, Tian-Yuan Fan^*

2012, 21(3): 242-250. DOI: 10.5246/jcps.2012.03.031

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The objective of this research was to develop gelatin microspheres (GMSs) and study their properties for embolization. The GMSs were prepared by emulsion chemical crosslinking method. The morphology and particle size of GMSs were observed under an optical microscope. The ratio of water absorption and GMSs swelling ratio were measured. The elasticity of GMSs was studied by TMS-Pro food texture analyzer. The deliverability of GMSs through catheter was investigated with a new device designed in this study. Finally, the acetone residue was determined by headspace capillary gas chromatography. The dried GMSs were elliptic with corrugated surface and the wet GMSs were round with smooth surface. The average diameter of dried GMSs was 430.5 μm with a range of 100-1000 μm, and that of wet GMSs was 601.2 μm with a range of 150-1425 μm. The maximum ratio of water absorption was 590.7% and the average swelling ratio was 103.0%. The elasticity of GMSs was proven to be appropriate for embolization. Three subgroups of wet GMSs (100-450 µm, 450-700 µm and 700-940 µm) were delivered through catheter with acceptable pressure. The content of residual acetone in GMSs was less than the minimum limit in the Chinese Pharmacopoeia 2010. Therefore, we concluded that the GMSs were suitable for embolization according to the applicable properties in vitro. And the methods for assessing the properties of GMSs in this study were going to be useful in the evaluation of embolic microspheres.

Effects of 4-amino-2-methyl-cantharidinimide on GABAC receptors

Yan-Xin Zhang, Yu-Fang Liao, Ming-Zheng Wang^*, Yan-Ting Gu, Yi Xiao, Xin-Feng Wang

2012, 21(3): 251-258. DOI: 10.5246/jcps.2012.03.032

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The antiepileptic effect of 4-amino-2-methyl-cantharidinimide (AMC) was reported, but its mechanism remains unknown. In this study, we investigated the effects of AMC on a rat model of penicillin-induced epilepsy. The doses of 88 and 22 mg/kg AMC and the dose of 154 mg/kg sodium valproate (VPA) were administered intragastrically (i.g.) 30 min before penicillin injection, respectively. The epileptiform activity was verified by electrocorticographic (ECoG) recordings. The levels of GABA and GABAC receptors in hippocampus were determined by immunohistochemistry, and real-time polymerase chain reaction (RT-PCR) technique was used to detect the mRNA expression of GABAC receptor ρ2. The mean frequency and amplification of spike epileptiform activity were significantly decreased in AMC and VPA-pretreated rats compared with those of non-pretreated penicillin-induced epilepsy (PIE) group. The levels of GABA, GABAC receptors and the mRNA expression of GABAC receptors ρ2 in AMC and VPA-pretreated rats were significantly increased as compared with PIE group. These findings indicate that AMC and VPA have an antiepileptic effect on PIE in rats, and the antiepileptic effect of AMC may be mediated by the GABAC receptors and GABA.

Polymorphisms in ghrelin and heparan sulfate proteoglycan genes and their association with diabetic nephropathy in Pakistani population

Khuram Shehzad, Maria Rasool, Mahjabeen Saleem^*, Mamoona Naz

2012, 21(3): 259-264. DOI: 10.5246/jcps.2012.03.033

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Diabetic nephropathy (DN), a long term complication of diabetes, is the most common cause of end-stage renal disease, increasing the risk of death. Genetic predispositions play an important role in determining the susceptibility of the development of DN. Heparan sulphate proteoglycan (HSPG) and ghrelin (GH) gene polymorphisms are associated with the risk of DN. T allele frequency of the HSPG gene determined by BamHI polymorphism located in intron 6 may be a risk factor for the development of renal dysfunction in DN (Fisher two tailed test, CI = 95%, d.f. = 29, P = 0.016). The ghrelin gene polymorphism is caused by a cytosine-to-adenine transition in exon 2 of the preproghrelin gene forming Leu72Met variant. In Pakistani population, the preproghrelin Leu72Met polymorphism was observed to be not associated with diabetic nephropathy in patients as indicated by statistical analysis (CI = 95%, d.f. = 29, P = 0.691). The allelic frequencies of HSPG genetic polymorphism has the potential to be used as diagnostic markers for diabetic nephropathy disease.

Synthesis and antimycobacterial activity of ternatolide

Xing-Yue Ji⁺, Si-Yang Li⁺, Shuai Meng, Chun-Ling Xiao, Xue-Fu You, Zhuo-Rong Li^*

2012, 21(3): 265-268. DOI: 10.5246/jcps.2012.03.034

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Ternatolide isolated from Radix Ranuncoli Ternati is considered as the active ingredient against Mycobacterium tuberculosis. Herein, ternatolide was synthesized in four steps in 32.7% overall yield by using Yamaguchi esterification as the key step, and its antimycobacterial activity was investigated in vitro using a rapid direct susceptibility assay. It was reported that ternatolide killed the Mycobacterium tuberculosis possibly by enhancing the expression of GLS in PBLs indirectly, and our results indicated that ternatolide was weakly active against MTB H37Rv ATCC 27294 directly. Therefore, it can be concluded that its mechanism of action was possibly related to the cellular factors.

Selective acetylation of puerarin by Rhodococcus sp.

Ya-Guang Ding, De-Wu Zhang, Shu-Min Liu, Jun-Gui Dai^*

2012, 21(3): 269-272. DOI: 10.5246/jcps.2012.03.035

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Among 39 species of microbial strains, Rhodococcus sp. AS 4.1147 possessed the ability to selectively acetylate puerarin (1) at C-6 position of the glucosyl moiety. The structure of the acetylated product, 6''-O-acetylpuerarin (2) was determined by the analysis of MS, NMR spectroscopic data. The isolated yield of 2 was 22.2%.

Triterpenoids from the stems of Casearia velutina Bl.

Fei-Fei Li, Zhi-Qin Guo, Xing-Yun Chai, Peng-Fei Tu^*

2012, 21(3): 273-277. DOI: 10.5246/jcps.2012.03.036

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To investigate the chemical components from the stems of Casearia velutina Bl., the constituents were isolated by repeated chromatography with silica gel, Sephadex LH-20, and ODS columns. The structures were elucidated by spectroscopic analysis. Eleven triterpenoids and its glycosides were isolated from the crude extract of C. velutina, and their structures were identified as friedelin-2,3-lactone (1), friedelane (2), epifriedelanol (3), friedelin (4), 2α,3α,19α-trihydroxy-urs-12-en-28-oic acid (5), 2α,3β,19α-trihydroxy-urs-12-en-28-oic acid (6), 2α,3α,23-trihydroxy-urs-12-en-28-oic acid (7), 2α,3α,23-trihydroxy-olean-12-en-28-oic acid (8), 2α,3α,19α,23-tetrahydroxy-urs-12-en-28-oic acid (9), 2α,3α,19α,23-tetrahydroxy-urs-12-en-28-oic acid-28-O-β-D-glucopyranosyl ester (10), and 3β,19α-dihydroxy-urs-12-en-28-oic acid 3-O-α-L-arabinopyranoside (11). All the compounds described above were isolated from this species for the first time. Compound 1 is a rarely occurred seco-friedelolactone in Flacourtiaceae.

Antibacterial activities of some selected plant extracts of local herbal
medicines in Lahore-Pakistan

Fouzia Noreen^*, Naqi Hussain, Muhammad Zaheer, Salma Rahman

2012, 21(3): 278-282. DOI: 10.5246/jcps.2012.03.037

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The antibacterial activity of methanol and acetone extracts of five plant extracts being utilized for the cure of different ailments in Pakistan was studied. The extracts of Curcuma zedoaria, Ipomea turpethum, Sphaeranthus indicus, Terminalia chebula and Tricholepis glaberrima were tested against seven different bacterial strains by well diffusion method and microdilution methods. The pattern of zone of inhibition varied with the plant extracts, the solvent used for extraction and organisms tested. Plant extracts (20 mg/mL) were used to evaluate antibacterial activities. The zone of inhibition exhibited by methanol extracts varied between 11 mm and 32 mm while those of acetone extracts varied between 9 mm and 25 mm respectively. The minimum inhibitory concentration (MIC) exhibited by methanol extracts ranged between (18.4-51.1) mcg/mL. Overall methanolic extracts showed more activity than the acetone extracts against tested organisms except for S. indicus. The plants were also analyzed for their elemental composition using atomic absorption spectrophotometer to explore natural sources of essential elements that can be utilized for medicinal purposes.

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