Interaction study between Ocimum sanctum and Glimepiride(sulfonylurea derivative) in diabetic rats

The present study was intended to discover the interaction between Ocimum sanctum(O. sanctum) and Glimepiride, a sulfonylurea derivative used in the treatment of type-2 diabetes, in diabetic rats to suggest an alteration in the dose of Glimepiride in case of hypoglycaemia. LD50 studies for the aqueous extract of O. sanctum leaf were carried out in albino mice up to the dose level of 2000 mg/kg. O. sanctum at low, medium and high doses(100, 200 and 400 mg/kg, per oral), respectively and Glimepiride ?(half) therapeutic dose, therapeutic dose and 2 time therapeutic dose(0.036, 0.072 and 0.144 mg/200 g, per oral) were selected. After the treatment with O. sanctum and Glimepiride as single doses and in various combinations of these two drugs in streptozotocin-induced diabetic rats serum glucose levels in all the groups were analysed by the glucose oxidase-peroxidase method. When administered alone as single doses both aqueous extract of O. sanctum leaf and Glimepiride produced a significant anti-diabetic effect in diabetic rats. The anti-diabetic effect observed with combination of aqueous extract of O. sanctum leaf and Glimepiride was significant and more when compared to either of the drugs given alone. There was a definite interaction that necessitates dose readjustment of Glimepiride and further glucose levels are to be frequently monitored to avoid complication of hypoglycemic condition with aqueous extract of O. sanctum leaf and Glimepiride combination.     

The Preparation of Salbutamol Sulfate Controlled Release TabletsCoated with Cellulose Acetate Aqueous Dispersion

In this study, emulsion-solvent evaporation method was applied to prepare the cellulose acetate(CA) aqueous dispersion. Upon the analyzing of the character of the aqueous dispersion, a controlled releaseformulation of salbutamol sulfate coated with cellulose acetate aqueous dispersion was prepared through orthogonalexperiment design. The factors that control the drug release character of the tablets were investigated. The drugrelease mechanism of the formulation was also studied. The experimental results indicated that CA aqueousdispersion had excellent film-forming ability under the effect of plasticizer. The drug release profile of the controlledrelease tablets coated with CA aqueous dispersion exhibited zero-order release character and the drug release rate wasmodulated by the osmotic pressure of the dissolution medium.     

Formulation of self-nanoemulsifying drug delivery systems containing monoacyl phosphatidylcholine and Kolliphor® RH40 using experimental design

 The development of self-nanoemulsifying drug delivery systems (SNEDDS) to enhance the oral bioavailability of lipophilic drugs is usually based on traditional one-factor-at-a-time approaches. These approaches may be inadequate to analyse the effect of each excipient and their potential interactions on the emulsion droplet size formed when dispersing the SNEDDS in an aqueous environment. The current study investigates the emulsion droplet sizes formed from SNEDDS containing different levels of the natural surfactant monoacyl phosphatidylcholine to reduce the concentration of the synthetic surfactant polyoxyl 40 hydrogenated castor oil (Kolliphor? RH40). Monoacyl phosphatidylcholine was used in the form of Lipoid S LPC 80 (LPC, containing approximately 80% monoacyl phosphatidylcholine, 13% phosphatidylcholine and 4% concomitant components).The investigated SNEDDS comprised of long-chain or medium-chain glycerides (40% to 75%), Kolliphor? RH40 (5% to 55%), LPC (0 to 40%) and ethanol (0 to 10%). D-optimal design, multiple linear regression, and partial least square regression were used to screen different SNEDDS within the investigated excipient ranges and to analyse the effect of each excipient on the resulting droplet size of the dispersed SNEDDS measured by dynamic light scattering. All investigated formulations formed nano-emulsions with droplet sizes from about 20 to 200 nm. The use of mediumchain glycerides was more likely to result in smaller and more monodisperse droplet sizes compared to the use of long-chain glycerides. Kolliphor? RH40 exhibited the most significant effect on reducing the emulsion droplet sizes. Increasing LPC concentration increased the emulsion droplet sizes, possibly because of the reduction of Kolliphor? RH40 concentration. A higher concentration of ethanol resulted in an insignificant reduction of the emulsion droplet size. The study provides different ternary diagrams of SNEDDS containing LPC and Kolliphor? RH40 as a reference for formulation developers.     

In vivo and in vitro chondrotoxicity of ciprofloxacin in juvenile rats

AIM: To study the relationship between chondrotoxicity and toxicokinetics of ciprofloxacin (CPFX). METHODS: Rats, 4-week old, were treated with CPFX 0, 400, 800, and 1200 mg/kg ig once daily on seven consecutive days. The knee joint cartilage was examined histopathologically. The concentration of CPFX in venous blood and knee joint cartilage samples were determined by a microbioassay using Escherichia coli 44102. The effects of CPFX on proliferation of chondrocytes and secretion of soluble proteoglycans were determined with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and 1,9-dimethylmethylene blue (DMB) assay, respectively. RESULTS: Cartilage was severely lesioned after treatment with CPFX 800 or 1200 mg/kg for 7 d, such as matrix swelling and loss of chondrocytes. The thickness of cartilage was significantly decreased compared with the control group. The maximum serum concentration (Cmax), the area under the plasma concentration-time curve (AUC0-∞2), and concentration in cartila     

Therapeutic efficacy of charcoal hemoperfusion in patients with acute severe dichlorvos poisoning

AIM: To assess the efficacy of hemoperfusion (HP) in the treatment of the patients with acute severe dichlorvos (DDVP) poisoning. METHODS: One hundred and eight patients with acute severe DDVP poisoning in the two teaching hospitals were enrolled. Sixty-seven patients were treated with HP (HP group) and forty-one patients accepted traditional treatment only as the control. Serum concentration of DDVP was determined by gas chromatography. RESULTS: The duration of coma, impaired consciousness, ICU stay, and mechanical ventilation     

Tissue distribution of bitespiramycin and spiramycin in rats

AIM: To investigate the tissue distribution of bitespiramycin (BSPM) and spiramycin (SPM) in rats. METHODS: Liquid chromatographic-mass spectrometric assay was applied for the determination of three major components (isovalerylspiramycins, ISV-SPMs) of BSPM and their major active metabolites (SPMs) in rat tissues and plasma after an oral dose of bitespiramycin, as well as SPMs. RESULTS: High levels of drug concentrations were observed in most tissues, especially in the liver, stomach, intestine, spleen, lung, womb, and pancreas. BSPM persisted long time in many rat tissues such that the drug concentration in spleen was 69.4 nmol/g at 60 h post-dose and it was still above the minimum inhibitory concentration of many susceptible pathogens. At 2.5 h post-dose, the total concentrations of ISV-SPMs and SPMs achieved in tissues were from 6 to 215 times higher than the corresponding concentrations in plasma. At 2.5 h post-dose, the mean Ct/CP of BSPM appeared to be 2- or 3-fold those of SPM in most tissues. The     

Pharmacokinetic studies of meloxicam following oral and transdermal administration in Beagle dogs

Aim： The potential for topical delivery of meloxicam was investigated by examining its pharmacokinetic profiles in plasma and synovial fluid following oral and transdermal administration in Beagle dogs.
Methods： The experiment was a two-period, crossover design using 6 Beagle dogs. Meloxicam tablets were administered orally at a dose of 0.31 mg/kg, and meloxicam gel was administered transdermally at a dose of 1.25 mg/kg. Drug concentrations in plasma and synovial fluid were determined by liquid chromatography-tandem mass spectrometry （LC/MS/MS）. The pharmacokinetic parameters were calculated using the Topfit 2.0 program. Results： The pharmacokinetic results showed that AUC0-t （23.9±8.26 pg·h·mL^-1） in plasma after oral administration was significantly higher than after transdermal delivery （1.00±0.43 pg·h·mL^-1）. In contrast, the ratio of the average concentration in synovial fluid to that in plasma following transdermal administration was higher than that for an oral delivery. The synovial fluid concentration in the treated leg was much higher than that in the untreated leg, whereas the synovial fluid concentration in the untreated leg was similar to the plasma concentration.
Conclusion： The high concentration ratio of synovial fluid to plasma indicates direct penetration of meloxicam following topical administration to the target tissue. This finding is further supported by the differences observed in meloxicam concentrations in synovial fluid in the treated and untreated joints at the same time point. Our results suggest that transdermal delivery of meloxicam is a promising method for decreasing its adverse systemic effects.     

吉非替尼治疗老年人晚期非小细胞肺癌30例临床分析

Objective To investigate the efficacy and adverse reactions of gefitinib in treatment of elderly patients with advanced non-small-cell lung cancer.Methods 30 elderly patients with advanced non-small cell lung cancer were treatment with oral gefitinib,250mg/d,every 4 weeks for a treatment period.The efficacy,adverse reactions,quality of life were observed.Results Of 30 cases,the rate of complete response(CR) ,partial response(PR), stability of disease(SD) .progression of disease(PD) and disease control was 0.0% ,26.6% ,26.6% ,49.6% ,53.3% ,respectively;The disease control rate( 84.0% ) in adenocarcinoma was significantly higher than that in squamous cell carcinoma( 20.0% ) (x2 = 9.125, P < 0.01) ; The disease control rate (100.0% ) in stage- Ⅲ was significantly higher than that in stage Ⅳ(77.8%)(x2 =3.879,P<0.05);The median progression-free survival was 3.8 months, and median survival was 5.2 months;The most common toxicity was skin toxicity, hematologic toxicity was not observed.Conclusion As the first-line treatment for advanced NSCLC, gefitinib was effective and tolerable for the elderly.     

Effect of Complexation with Hydroxylpropyl-β-Cyclodextrin on Solubility, Dissolution Rate and Chemical Stability of Prostaglandin E1

Aim To study the effect of complexation with hydroxylpmpyl-β-cycledextrin (HP-β-CD) on the solubility, dissolution rate and chemical stability of pmstaglandin E1 (PGE1), thereby providing a basis for preparing a stable solid or aqueous preparation of PGF1 formulated with HP-β-CD. Methods The effect of HP-β-CD on the solubility of PGF1 was studied by phase solubility method. The formation of inclusion complexes of PGE1 with HP-β-CD in the aqueous solution was confirmed by UV spectra, circular dichroism spectroscopy, and that in the solid state by IR spectra and X-ray diffractometry. An solid inclusion complex of PGF1 with HP-β-CD was prepared by lyophilization. The dissolution rate and stability of the inclusion complex were determined and compared with those of PGE1 alone. Meanwhile, the stability of PGF1 aqueous solutions in the presence of HP-β-CD was studied under different pH conditions. Results The solubility of PGF1 increased linearly with increasing HP-β-CD concentration in various pH buffered solutions, showing typical AL-type phase solubility diagrams. The stability and dissolution rate of the solid inclusion complex of PGE1 were significantly increased, compared with those of pure PGE1 . The stability of PGEI in HP-β-CD solutions was also obviously improved under acidic and basic conditions, but the stabilizing effect was absent under neutral conditions. Conclulsions The solubility, dissolution rate and chemical stability of PGE1 are markedly improved by complexation with HP-β-CD. It is quite possible to prepare a stable PGE1 inclusion complex-containing solid dosage forms, but almost impossible to obtain a stable aqueous preparation of PGE1 formulated with HP-β-CD.     

Pharmacokinetics of recombinant human basic fibroblast growth factor in rabbits and mice serum and rabbits aqueous humor

AIM: To study the pharmacokinetics of recombinant human basic fibroblast growth factor (rhbFGF) in rabbits and mice after iv and postocular administration, and the changes of rhbFGF in rabbits aqueous humor after postocular administration. METHODS: After iv or postocular administration three doses of rhbFGF in rabbits and mice, rhbFGF concentration in serum and rabbit aqueous humor was determined by enzyme-linked immunosorbent assay. RESULTS: Serum concentration-time data of rabbits after iv administration of rhbFGF 1, 2, and 4 μg/kg were fitted to bi-exponential equations with half-lives of 0.9, 0.9, and 0.6 min for T1/2α and 7, 8, and 4.7 min for T1/2β. Plasma concentration-time data of mice after iv administration of rhbFGF 2.5, 5 and 10 μg/kg were fitted to bi exponential equations with half-lives of 0.4, 0.6, and 0.9 min for T1/2α　and 6, 5, and 7 min for T1/2β.The AUCs were linearly correlated to doses in both cases (rrabbit=0.997, rmouse=0.999). The serum concentrations of rhbFGF were very l     

子宫中隔切除术后预防粘连方法探讨

目的 探讨子宫中隔并不孕患者宫腔镜术后不同处理方法预防宫腔粘连的效果.方法 55例子宫中隔并不孕患者行腹腔镜监护下宫腔镜子宫中隔切除术(TCRS),术后针对不同患者采用不同术后处理措施,包括宫腔放置与不放IUD,是否进行人工周期治疗,部分患者术后使用GnRH-a类药物治疗术后第1、3个月行宫腔镜检查随访,宫内放置IUD的患者;于术后第3个月取环.结果 54例患者术后进行宫腔镜检查随访,其中40例分别于术后第1、3个月完成了术后2次宫腔镜检查,另14例只完成一次检查.宫腔术后放环与否对术后宫腔形态影响无差异(P>0.05),术后使用人工周期治疗患者较未使用者子宫内膜厚,此两者术后第3个月宫腔镜检查发现宫底创面均已有内膜覆盖.使用GnRH-a类药物患者术后官腔形态满意.结论 TCRS术后宫腔放置IUD无助于预防术后粘连的发生;术后人工周期治疗应更个体化并有针对性的使用GnRH-a类药物治疗.术后及时进行宫腔镜检查随访可防止术后宫底新粘连的形成.     

欧洲药典适用性认证介绍

目的介绍欧洲药典适用性认证程序,为国内药品监管机构和原料药生产企业提供信息,促进我国原料药生产企业的国际化。方法通过查阅调研欧盟相关药品法规和与EDQM同行面对面的交流,详细了解欧洲药典适用性认证的组织机构和具体程序。结果与结论欧洲药典适用性认证程序在对原料药的质量控制有重要作用,加强了药典的监管力度,进一步保证了原料药的质量、安全性和有效性。     

住院患者精神用药情况调查分析

目的：了解目前住院精神患者的药物使用情况。方法：采用一日法调查西安市精神卫生中心403例住院精神患者诊断和治疗情况，并与上海市精神卫生中心2004年调查结果相比较。结果：①传统精神药物使用显著减少，新型精神药物使用占据首位；②抗精神病药物使用趋向小剂量化；③本组联用丙戊酸盐类药物显著增多；④我院精神药物使用情况与上海精神卫生中心比较有显著差异。结论：近年来精神药物使用情况已发生了显著变化，与新型精神药物疗效好，副作用少，患者依从性高有关。     

不同方法治疗慢性宫颈炎的疗效分析

目的慢性宫颈炎是妇科最常见的疾病之一,可引起盆腔脏器炎症,并且与宫颈癌的发生关系密切。本文诣在探讨不同方法在慢性宫颈炎中的疗效。方法回顾性分析新乡市中心医院收治的210例宫颈炎患者,采用药物保妇康栓、聚焦超声治疗及宫腔镜下宫颈电切术的临床效果进行统计分析。结果宫颈电切术治疗有效率为97.9%,明显高于另外两组,差异有统计学意义。结论宫腔镜下宫颈电切术治愈慢性宫颈炎,并且切除宫颈移行带,减少宫颈癌发生。     

槲皮素代谢产物定性检出条件研究

目的:研究给予大鼠槲皮素后血浆中代谢产物的定性检出条件。方法:给予大鼠槲皮素单体(100mg.kg-1)后腹腔静脉取血,血浆样品经2mol.L-1盐酸(甲醇-水溶液)水解,采用高效液相色谱法对血浆样品中代谢产物进行定性分析。结果:大鼠给药后3h内取血、血浆样品经盐酸水解处理4h,可稳定检测槲皮素和异鼠李素,样品在—20℃条件下贮存稳定。结论:血浆样品采集时间、盐酸水解时间及贮存方式等不同均可影响代谢产物的有效检出。     

片剂溶出度影响因素分析

目的:考察片剂溶出度的影响因素,提高片剂溶出度,从而提高产品质量。方法:通过实验,研究各种参数对片剂溶出度的影响,选择出最佳工艺条件,如改进处方、控制颗粒硬度和大小、控制压力等工艺参数,用于指导大型生产,提高片剂溶出度。结论:崩解剂及润滑剂的用量对片剂溶出度影响较大,颗粒的硬度及大小、粘合剂的温度,压片压力对片剂的溶出度亦有影响;片剂直径大小对片剂溶出度影响不大。     

甲泼尼龙佐治毛细支气管炎疗效观察

目的探讨甲泼尼龙与布地奈德治疗毛细支气管炎的疗效。方法将182例毛细支气管炎患儿随机分成三组,三组均采用综合治疗,A组62例用甲泼尼龙静脉滴注,B组60例雾化吸入布地奈德,C组60例用静滴氢化可的松,观察三组喘憋、哮鸣音消失和住院时间。结果A组喘憋、哮鸣音消失时间及住院时间均比B,C组缩短（P〈0.05）。结论甲泼尼龙静滴治疗毛细支气管炎有效、安全、方便,明显加快治愈过程,优于布地奈德与氢化可的松。     

新疆维吾尔自治区基层医院平均住院日调查分析

目的 通过对新疆维吾尔自治区14个县乡级医疗机构住院患者平均住院日及影响因素进行分析,为县乡级医疗机构进一步提高医疗管理质量提供依据.方法 将2009-2010年1504例县乡级医院住院患者平均住院天数,按性别、年龄、院别、付费方式、疾病分类进行描述性统计和秩和检验分析.结果 不同性别间及院别间平均住院日差异均有统计学意义(均P＜0.05),男性平均住院日为10.39 d,女性为8.69d,乡级医院为9.27d,县级医院为9.50 d.不同年龄间平均住院日差异有统计学意义(P＜0.05),小于15岁组、15 ～24岁组、25～44岁组、45 ～65岁组、大干65岁组平均住院日分别为8.10 d、7.66d、8.83 d、10.26 d和11.33 d.自费患者平均住院日为8.39 d,新农合组为9.10 d,商业保险组10.17 d,社会基本医疗保险患者则为11.08 d.不同疾病分类间平均住院日差异明显,妊娠类平均住院日最短,为6.73 d,而肿瘤患者则为14.26 d.结论 不同性别、不同年龄段、不同疾病分类及不同付费方式间平均住院日存在差异,县级医疗机构和乡级医疗机构住院患者平均住院日也存在差异.     

住院患者抗菌药物不合理使用分析

目的了解该院住院患者不合理使用抗菌药物情况。方法随机抽取2009年住院使用抗菌药物病历544份。依据《抗菌药物临床使用原则》等相关规定进行评价,统计、分析抗菌药物不合理使用现象。结果该院住院患者抗菌药物不合理使用率为31.8%,不合理现象主要表现有选药不当、高起点用药、用法用量不当等。结论该院住院患者抗菌药物不合理使用现象严重,医院应采取措施加强监管,促进抗菌药物合理使用。     

对天津市北辰医院医务人员药品不良反应认知度调查分析

药品不良反应(ADR)监测工作是对上市药品安全性的再评价,是公众安全合理用药的保障,是药品监督管理工作的重要组成部分。本中心对天津市北辰医院103名医务人员进行了药品不良反应相关知识认知度调查,并对调查结果进行统计分析,为相关部门的药品监管工作提供依据和参考。