苦碟子联合低分子肝素钙治疗急性脑梗死疗效观察

Objective:  to evaluate combinative effect of Kudiezi Injection and low molecular weight heparin calcium in the treatment of acute cerebral infarction. Methods:  72 cases of acute cerebral infarction were randomly divided into two groups, the treatment group of 36 cases were treated with the combination of Kudiezi Injection and low molecular heparin calcium; the other 36 cases in the control group were treated with the combination of Xuesaitong injection and low molecular weight heparin calcium. The degree of neurological deficit score and clinical outcome were respectively evaluated before and after treatment. Results:  There are significant differences between the treatment group and the control group in results efficiency. Conclusion:  It can improve the curative effect and the prognosis of the patients in the acute stage of cerebral infarction in the combinative treatment of Kudiezi Injection and low molecular weight heparin.目的 评价苦碟子注射液联合低分子肝素钙治疗急性脑梗死的临床效果及护理方法。方法 将72例急性脑梗死患者随机分为两组，治疗组36例用苦碟子联合低分子肝素钙治疗；对照组36例用血塞通注射液联合低分子肝素钙治疗。治疗前后分别进行神经功能缺损程度评分以及临床疗效评定[5]。结果 治疗组显效率与对照组比较差异有非常显著性(P=0.009)。结论 对急性期脑梗死患者在常规治疗基础上加用苦碟子及低分子肝素钙可显著提高疗效，改善患者预后。

Preparation and characterization of solid lipid nanoparticles loaded with frankincense and myrrh oil

The aim of the present study was to prepare solid lipid nanoparticles (SLNs) for the oral delivery of frankincense and myrrh essential oils (FMO). Aqueous dispersions of SLNs were successfully prepared by a high-pressure homogenization method using Compritol 888 ATO as the solid lipid and soybean lecithin and Tween 80 as the surfactants. The properties of the SLNs such as particle size, zeta potential (ZP), and drug encapsulation efficiency (EE) were investigated. The morphology of SLNs was observed by transmission electron microscopy (TEM). The crystallinity of the formulation was analyzed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). In addition, drug evaporation release and antitumor activity were also studied. Round SLNs with a mean size of 113.3 ± 3.6 nm, a ZP of −16.8 ± 0.4 mV, and an EE of 80.60% ± 1.11% were obtained. DSC and XRD measurements revealed that less ordered structures were formed in the inner cores of the SLN particles. Evaporation loss of the active components in FMO could be reduced in the SLNs. Furthermore, the SLN formulation increased the antitumor efficacy of FMO in H22-bearing Kunming mice. Hence, the presented SLNs can be used as drug carriers for hydrophobic oil drugs extracted from traditional Chinese medicines

In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion

Yong-Tai Zhang, Zhe-Bin Huang, Su-Juan Zhang, Ji-Hui Zhao, Zhi Wang, Ying Liu, Nian-Ping FengDepartment of Pharmaceutics, Shanghai University of Traditional Chinese Medicine, Shanghai, The People's Republic of ChinaObjective: To investigate the cellular uptake of evodiamine and rutaecarpine in a microemulsion in comparison with aqueous suspensions and tinctures.Materials and methods: A microemulsion was prepared using the dropwise addition method. Mouse skin fibroblasts were cultured in vitro to investigate the optimal conditions for evodiamine and rutaecarpine uptake with different drug concentrations and administration times. Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions. Rhodamine B labeling and laser scanning confocal microscopy (LSCM) were used to explore the distribution of fluorochrome transferred with the microemulsion in fibroblasts. Cellular morphology was also investigated, using optical microscopy to evaluate microemulsion-induced cellular toxicity.Results: The maximum cellular drug uptake amounts were obtained with a 20% concentration (v/v) of microemulsion and an 8 hour administration time. Drug uptake by mouse skin fibroblasts was lowest when the drugs were loaded in microemulsion. After incubation with rhodamine B-labeled microemulsion for 8 hours, the highest fluorescence intensity was achieved, and the fluorochrome was primarily distributed in the cytochylema. No obvious cellular morphologic changes were observed with the administration of either the microemulsion or the aqueous suspension; for the tincture group, however, massive cellular necrocytosis was observed.Conclusion: The lower cellular uptake with microemulsion may be due to the fact that most of the drug loaded in the microemulsion vehicle was transported via the intercellular space, while a small quantity of free drug (released from the vehicle) was ingested through transmembrane transport. Mouse skin fibroblasts rarely endocytosed evodiamine and rutaecarpine with a microemulsion as the vehicle. The microemulsion had no obvious effect on cellular morphology, suggesting there is little or no cellular toxicity associated with the administration of microemulsion on mouse skin fibroblasts.Keywords: mouse skin fibroblasts, evodiamine, rutaecarpine, microemulsion, cellular uptake, in vitr

Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion

Yong-Tai Zhang, Ji-Hui Zhao, Su-Juan Zhang, Yang-Zi Zhong, Zhi Wang, Ying Liu, Feng Shi, Nian-Ping FengSchool of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of ChinaObjective: The purpose of this study was to improve skin permeation of evodiamine and rutaecarpine for transdermal delivery with microemulsion as vehicle and investigate real-time cutaneous absorption of the drugs via in vivo microdialysis.Methods: Pseudoternary phase diagrams were constructed to evaluate microemulsion regions with various surfactants and cosurfactants. Nine formulations of oil in water microemulsions were selected as vehicles for assessing skin permeation of evodiamine and rutaecarpine in ex vivo transdermal experiments. With a microdialysis hollow fiber membrane implanted in the skin beneath the site of topical drug administration, dialysis sampling was maintained for 10 hours and the samples were detected directly by high performance liquid chromatography. Real-time concentrations of the drugs in rat skin were investigated and compared with those of conventional formulations, such as ointment and tincture. Furthermore, the drugs were applied to various regions of the skin using microemulsion as vehicle.Results: In ex vivo transdermal experiments, cutaneous fluxes of evodiamine and rutaecarpine microemulsions were 2.55-fold to 11.36-fold and 1.17-fold to 6.33-fold higher, respectively, than those of aqueous suspensions. Different drug loadings, microemulsion water content, and transdermal enhancers markedly influenced the permeation of evodiamine and rutaecarpine. In microemulsion application with in vivo microdialysis, the maximum concentration of the drugs (evodiamine: 18.23 ± 1.54 ng/mL; rutaecarpine: 16.04 ± 0.69 ng/mL) were the highest, and the area under the curve0–t of evodiamine and rutaecarpine was 1.52-fold and 2.27-fold higher than ointment and 3.06-fold and 4.23-fold higher than tincture, respectively. A greater amount of drugs penetrated through and was absorbed by rat abdominal skin than shoulder and chest, and a reservoir in the skin was found to supply drugs even after the microemulsion was withdrawn.Conclusion: Compared to conventional formulations, higher cutaneous fluxes of evodiamine and rutaecarpine were achieved with microemulsion. Based on this novel transdermal delivery, the transdermal route was effective for the administration of the two active alkaloids.Keywords: microemulsion, evodiamine, rutaecarpine, transdermal delivery, microdialysi

Assessment of changes in lipid profile and related enzymes in children with asthma

Purpose: To investigate the influence of the lipid profile and related parameters on the development of asthma in children aged 10 to 15 years.Methods: Peripheral blood samples were collected from a group diagnosed with asthma as well as from a healthy control group. The lipid profile parameters measured were total cholesterol (TC), triglycerides (TG), low-density lipoprotein (LDL), very-low-density lipoprotein (VLDL), high-density lipoprotein (HDL), serum total antioxidant capacity (TAC), reduced glutathione (GSH), and malondialdehyde (MDA), and the activities of lecithin–cholesterol acyltransferase (LCAT) and cholesteryl ester transfer protein (CETP).Results: TC, TG, LDL, and VLDL levels were significantly (p ≤ 0.05) higher in the asthma group compared with the controls, while HDL level was lower. Total TAC and GSH were lower in the asthma group, while MDA level, and LCAT and CETP activities were higher.Conclusion: There is a link between an elevated lipid profile and increased antioxidant capacity in asthmatic children

Clinical analysis of 1 case of solitary brain metastases misdiagnosed as cerebral infarction

目的  通过报告1例误诊为脑梗死的单发性脑转移瘤患者的诊断过程，总结单发性脑转移瘤的临床、影像学特征及诊断治疗方法。方法  回顾性分析1例单发性脑转移瘤患者的诊断过程，并复习有关文献。结果  脑转移瘤常多发，单发者仅占25%，发病年龄以40～60岁多见，原发病灶以肺最常见。脑转移瘤常位于脑叶灰白质交界处，不同部位的肿瘤可出现不同的临床表现，影像学上常表现为“小病灶、大水肿”，与颅内原发肿瘤不易区分，头颅CT或 MRI增强检查并查到其他部位的原发肿瘤病灶后可确定诊断。目前主张单发性脑转移瘤应进行手术切除，术后辅以立体定向放射治疗和全脑放射治疗。结论  15%的脑转移瘤患者既往无肿瘤病史，因此诊断脑瘤后须在身体其他部位查找有无原发病灶，避免误诊、漏诊。对于中老年肺癌或其他恶性肿瘤患者，无论有无中枢神经系统症状，均应积极进行头颅CT甚至MRI检查，以发现较小的早期脑转移瘤病灶。对于易患肺癌人群，应该每年体检，进行胸部X线检查或低剂量CT筛查，以便早期发现肺癌病灶，早期治疗，防止肿瘤转移。Objective: To report 1 case was misdiagnosed as cerebral infarction solitary brain metastases (SBM) in patients with diagnosis process, and to summarize the clinical and imaging features of the SBM and its treatment. Methods: To retrospectively analyze the diagnostic process of 1 case of SBM patients, and to have literature review. Results: Patients with solitary and multiple brain metastases accounted for only 25%, the onset age was 40 ~ 60 years old, and the most common primary lesion is in lung. Brain metastases are often on the border, in between lobes grey matter. Different parts of the tumors can present different clinical manifestations. The diagnostic imaging is often shown as "small lesions, large edema", and intracranial primary tumor is not easy to distinguish, Head CT or MRI examination of tumors in other parts could confirm the diagnosis. Now that SBM should undergo surgery resection, postoperative supplemented by stereotactic radiotherapy and whole brain radiotherapy. Conclusions: 15% of the patients with brain metastases haven’t got previous medical history, the doctor is therefore must look for presence of primary lesions in other parts of the body for accurate diagnosis, to avoid the misdiagnosis and missed diagnosis. Middle-aged and elderly patients with lung cancer or other malignant tumor, regardless of the presence of the central nervous system symptoms, should carry on the head CT or MRI examination, and find smaller early brain metastatic lesions. People who are susceptible to lung cancer should have annual physical examination, chest X-ray or low dose CT screening for early detection of lung cancer lesions, early treatment and prevention of tumor metastasi

Anticonvulsant activities of α-asaronol ((E)-3'-hydroxyasarone), an active constituent derived from α-asarone.

BACKGROUND: Epilepsy is one of chronic neurological disorders that affects 0.5-1.0% of the world's population during their lifetime. There is a still significant need to develop novel anticonvulsant drugs that possess superior efficacy, broad spectrum of activities and good safety profile. METHODS: α-Asaronol and two current antiseizure drugs (α-asarone and carbamazepine (CBZ)) were assessed by in vivo anticonvulsant screening with the three most employed standard animal seizure models, including maximal electroshock seizure (MES), subcutaneous injection-pentylenetetrazole (PTZ)-induced seizures and 3-mercaptopropionic acid (3-MP)-induced seizures in mice. Considering drug safety evaluation, acute neurotoxicity was assessed with minimal motor impairment screening determined in the rotarod test, and acute toxicity was also detected in mice. RESULTS: In our results, α-asaronol displayed a broad spectrum of anticonvulsant activity (ACA) and showed better protective indexes (PI = 11.11 in MES, PI = 8.68 in PTZ) and lower acute toxicity (LD50 = 2940 mg/kg) than its metabolic parent compound (α-asarone). Additionally, α-asaronol displayed a prominent anticonvulsant profile with ED50 values of 62.02 mg/kg in the MES and 79.45 mg/kg in the sc-PTZ screen as compared with stiripentol of ED50 of 240 mg/kg and 115 mg/kg in the relevant test, respectively. CONCLUSION: The results of the present study revealed α-asaronol can be developed as a novel molecular in the search for safer and efficient anticonvulsants having neuroprotective effects as well as low toxicity. Meanwhile, the results also suggested that α-asaronol has great potential to develop into another new aromatic allylic alcohols type anticonvulsant drug for add-on therapy of Dravet's syndrome