家犬单剂量和多剂量口服阿昔莫司缓释制剂的药代动力学和生物等效性研究

目的研究阿昔莫司缓释片在家犬体内单剂量和多剂量的药代动力学和生物等效性。方法测定6只家犬单剂量和多剂量口服缓释片和普通胶囊后的血药浓度。结果阿昔莫司的药-时曲线符合非隔室模型。单剂量给药后，缓释片和普通胶囊的AUC分别为(158±30)和(147±37) μg·h·mL^-1；T_max分别为(4.3±0.8)和(2.6±1.3) h；C_max分别为(29±6)和(42±10) μg·mL^-1；T_1/2分别为(2.3±0.7)和(1.60±0.10) h；MRT分别为(6.0±0.8)和(3.9±0.7) h；F_r为(108±16)%。多剂量给药后，缓释片和普通胶囊的AUC分别为(209±23)和(195±26) μg·h·mL^-1；T_max分别为(6.3±0.8)和(3.4±1.5) h；C_max分别为(27±4)和(36±5) μg·mL^-1；Cmin分别为(2.2±1.0)和(0.20±0.20) μg·mL^-1；C_av分别为(8.7±1.0)和(8.1±1.1) μg·mL^-1；FI分别为(293±73)%和(448±91)%；F_r为(114±19)%。结论单剂量实验的双单侧检验结果表明：缓释片和普通胶囊生物等效；缓释片具有良好的缓释效果。多剂量实验结果表明：缓释片和普通胶囊生物等效；缓释片的波动系数优于普通胶囊。     

Multi-constituent synergism is responsible for anti-inflammatory effect of Azadirachta indica leaf extract

Context: Azadirachta indica A. Juss. (Meliaceaes) leaves have been used traditionally to treat swelling and rheumatism in Indian cultures.

Objective: To fractionate A. indica leaf extracts using bioactivity guided manner for identification of the active anti-inflammatory principles.

Materials and methods: Polarity-gradient sequential extracts (petroleum ether, chloroform, methanol, and water) of A. indica leaves were screened for their anti-inflammatory potential using the carrageenan-induced rat paw edema model (1?g/kg). The chloroform extract was sequentially fractionated to obtain n-hexane (F-1), n-hexane-chloroform (F-2), and chloroform (F-3) fractions and their inhibitory effect on rat paw edema was evaluated (500?mg/kg). Inhibitory effect of F-2 on granuloma formation, plasma interleukin (IL-1), and tumor necrosis factor (TNF-α) was assessed at the doses of 100, 200, and 400?mg/kg using the cotton pellet assay in rats. Three sub-fractions (SF-1, SF-2, and SF-3) were obtained upon chromatography of F-2, and their inhibitory effect on cyclooxygenase was assessed at 200?µg/mL concentration. The sub-fractions were subjected to gas chromatography–mass spectrometry (GC-MS).

Results: All the extracts showed significant anti-inflammatory effect; however, chloroform extract was the most effective against paw edema (53.25% inhibition). The three fractions of chloroform extract showed significant effect, while F-2 being the most potent (51.02%). F-2 demonstrated dose-dependent inhibition of granuloma and cytokines. Interestingly, all the sub-fractions of F-2 inhibited COX-1 and COX-2 with almost equal potential. GC-MS revealed that chemically the sub-fractions were totally different from each other.

Discussion and conclusion: Anti-inflammatory effect of A. indica is a result of cumulative and synergistic effects of diversified constituents with varying polarities that collectively exert the effect via suppression of cyclo-oxygenases and cytokines (IL-1 and TNF-α).     

自体颗粒脂肪移植在丰唇中的应用研究

目的:观察自体颗粒脂肪移植丰唇在上下唇的临床效果。方法:局部肿胀麻醉后,利用注射器抽吸腹部或大腿内侧皮下脂肪颗粒,进行离心后,注射填充在上下红唇部。结果,采用自体颗粒脂肪移植治疗薄唇36例,其中5例进行2次填充。其余31例填充1次,均达到理想效果。结论:利用自体颗粒脂肪移植丰唇是一种理想并有效的方法,值得临床推广应用。     

醋酸戈舍瑞林缓释植入剂联合腹腔镜手术治疗子宫内膜异位症效果

目的:探讨醋酸戈舍瑞林缓释植入剂联合腹腔镜手术治疗子宫内膜异位症的临床疗效。方法:选择本院就诊的子宫内膜异位症患者80例,随机分为两组各40例,根据r-AFS分期进行腹腔镜手术,在术后1周内观察组醋酸戈舍瑞林缓释植入剂3.6mg皮下注射,每4周1次,连用6个月;对照组口服孕三烯酮2.5mg,每周2次,连用6个月。比较两组临床疗效,术前和术后6个月测定血清血管内皮生长因子(VEGF)、基质金属蛋白酶-9/组织金属蛋白酶抑制物-1(MMP-9/TIMP-1),评定患者视觉模拟评分法(VAS)和健康生活质量调查问卷(SF-36),随访3年术后不良反应和复发情况。结果:治疗有效率对照组(75.0%)低于观察组(92.5%)(P<0.05)。术后6个月时,对照组和观察组血清VEGF(158.41±56.28 ng/L、119.63±47.13ng/L),MMP-9/TIMP-1(1.35±0.25、1.14±0.23),生理健康评分(64.20±12.81分、78.53±13.23分),心理健康评分(69.14±13.26分、80.35±14.59分),VAS评分(1.21±0.46分、0.84±0.39分)比较均有差异(P<0.05);观察组无不良反应发生,术后3年复发率对照组(27.5%)高于观察组(10.0%)(P<0.05)。结论:醋酸戈舍瑞林缓释植入剂联合腹腔镜手术治疗子宫内膜异位症疗效确切,可降低术后血管侵袭指标及复发率,提高生活质量,安全性高。     

紫外分光光度法测定阿替洛尔缓释微囊含量

目的：建立以紫外分光光度法测定阿替洛尔缓释微囊含量的方法。方法：将阿替洛尔缓释微囊研磨破碎,转移至容量瓶中,稀释后,在224nm处进行含量测定。结果：阿替洛尔在224nm处有最大吸收,辅料对测定无干扰。标准曲线方程：A=0.0355C+0.0014,线性范围为2.5～20.0μg·ml-1。回收率98.81%～99.36%,精密度和稳定性RSD均在2%以内,符合《中国药典》的要求。     

混悬液上药法制备非诺贝特微丸的处方研究

目的:采用流化床混悬液上药法制备非诺贝特速释微丸。方法:以上药效率、脆碎度、粘连率为评价指标,考察并优化混悬液上药法制备非诺贝特速释微丸的处方。结果:确定FNBT/HPMC-E5/SDS=160∶20∶1.6为最佳配比处方,选定固含量为20%,上药效率为95%,溶出度为15 min达90%。结论:流化床混悬液上药法制备非诺贝特微丸,上药效率高,方法简便可靠,溶出迅速。     

喹硫平与丙戊酸钠缓释片在双相情感障碍躁狂发作治疗中的疗效比较

目的 对比分析喹硫平与丙戊酸钠缓释片在双相情感障碍躁狂发作治疗中的临床疗效。方法 52例双相情感障碍躁狂发作患者,采用随机数字表法分为A组和B组,每组26例。A组患者采用喹硫平治疗, B组患者采用丙戊酸钠缓释片治疗。比较两组患者临床疗效及贝克-拉范森躁狂量表(BRMS)评分降低1/2时间、治疗前后炎症因子水平、不良反应发生情况。结果 A组患者总有效率为96.15%,与B组的92.31%比较差异无统计学意义(χ^2=0.354, P=0.552>0.05)。A组患者BRMS评分降低1/2时间为(2.32±0.57)周,短于B组的(3.87±0.67)周,差异具有统计学意义(t=8.985, P=0.000<0.05)。治疗前,两组患者白细胞介素-1(IL-1)、白细胞介素-10(IL-10)、肿瘤坏死因子-α(TNF-α)水平比较差异无统计学意义(P>0.05);治疗后,两组患者IL-1、TNF-α水平低于本组治疗前, IL-10水平高于本组治疗前,且A组患者IL-1、TNF-α水平低于B组, IL-10水平高于B组,差异具有统计学意义(P<0.05)。A组患者不良反应发生率为3.85%,低于B组的30.77%,差异具有统计学意义(χ^2=6.584, P=0.010<0.05)。结论 喹硫平与丙戊酸钠缓释片治疗双相情感障碍躁狂发作疗效相当,但喹硫平的起效时间更快,能够显著改善炎症因子水平,且不良反应更少,这对于控制病情发展具有更高的临床应用价值。     

头孢氨苄胃漂浮缓释片的制备与质量评价

目的制备头孢氨苄胃漂浮缓释片,并考察其漂浮延迟时间及体外药物释放度。方法采用粉末直接压片工艺制备头孢氨苄胃漂浮缓释片,采用单因素实验方法筛选得到影响头孢氨苄胃漂浮缓释片体外漂浮延迟时间、漂浮时间和释放度的关键性辅料用量范围,最终以羟丙甲纤维素(HPMC K15M)用量、碳酸氢钠用量以及压片主压力作为考察因素,以头孢氨苄胃漂浮缓释片的漂浮延迟时间和1,4和8 h时间点的药物释放度作为评价指标,通过Box-Behnken实验设计优化得到头孢氨苄胃漂浮缓释片处方设计空间,并在设计空间任取一点连续制备3批头孢氨苄胃漂浮缓释片,评价其漂浮延迟时间及体外释放度。结果优化得到头孢氨苄胃漂浮缓释片的处方设计空间,每片HPMC K15M用量为260 mg,碳酸氢钠用量为60 mg,压片主压力为8 kN,制备的头孢氨苄胃漂浮缓释片漂浮延迟时间仅为12.1±0.5 min,在12 h内药物释放平缓,无药物突释。结论通过Box-Behnken实验设计优化得到的头孢氨苄胃漂浮缓释片处方,漂浮延迟时间较短,12 h维持漂浮状态,药物释放平稳。     

An ultrasound examination of tongue movement during swallowing

Six female adults were studied during the production of four single swallows each, using real-time ultrasound. A pellet was affixed to the tongue at the junction between the (calculated) anterior third and posterior two-thirds of the tongue surface. Direction, rate, and extent of pellet movement were measured and used to create stages of tongue blade movement during swallowing. Pellet movement was then compared to the three stages of hyoid movement (ascent, steady, descent). Anterior-posterior and superior-inferior components of pellet movement were examined and discussed.     

大黄缓释膜对大鼠牙周炎的治疗作用

目的：探讨大黄缓释膜对大鼠牙周炎的治疗作用。方法48只Wistar大鼠,随机分为空白对照组、模型对照组、复方奥硝唑大黄缓释膜组和大黄缓释膜组。各组大鼠均采用左上颌第一磨牙钢丝结扎、注射细菌内毒素并配以高糖饮食的方法建立牙周炎模型。空白对照组大鼠用生理盐水进行处理。各组大鼠造模2h后给予药物进行治疗,第8天处死。检查大鼠龈出血指数、探针深度、牙槽骨吸收。结果与模型对照组比较,给药组大鼠的龈出血指数、探针深度、牙槽骨吸收均降低（P<0.001）。结论大黄缓释膜对实验性牙周炎有明显的治疗作用。