益心酮滴丸对急性心肌梗塞犬心肌细胞超微结构的影响

目的:观察益心酮滴丸对急性心肌梗塞犬心肌细胞超微结构及心肌酶的影响。方法：健康成年杂种犬30只，分为对照组、吉罗益心酮片组及益心酮滴丸25、50和100 mg•kg^-1组，每组6只。采用麻醉开胸结扎犬的冠状动脉前降支（LAD）制备急性心肌梗塞模型，取静脉血检测血清中天门冬氨酸转氨酶（AST）、磷酸肌酸激酶（CK）和乳酸脱氢酶（LDH）活性；应用透射电子显微镜观察心肌细胞超微结构的改变。 结果：与对照组比较，益心酮滴丸各剂量组AST、CK及LDH的活性明显降低（P<0.05P<0.001）；与吉罗益心酮片组比较差异无显著性（P>0.05）。益心酮滴丸各剂量组心肌细胞超微结构基本正常。结论 ：益心酮滴丸对急性心肌梗塞犬的心肌细胞具有一定的保护作用。     

泮托拉唑钠肠溶微丸胶囊的处方工艺研究

目的：研制泮托拉唑钠肠溶微丸胶囊。方法采用流化床包衣法制备泮托拉唑钠肠溶微丸,将制备好的微丸装入胶囊即得泮托拉唑钠肠溶微丸胶囊。结果胶囊在人工胃液中耐酸良好,在人工肠液中能够迅速溶出。结论该工艺简单易行、重现性良好、生产周期短、成本低、适合工业化生产。     

丹参素缓释微丸的制备及家兔体内药动学研究

目的:制备丹参素24 h缓释微丸并研究其在家兔体内的药动学行为。方法:采用挤出滚圆法制备丹参素含药丸芯,以尤特奇水分散体为缓释包衣材料进行流化床包衣制备缓释微丸,研究制剂在家兔体内药动学行为。结果:所得丹参素缓释微丸圆整度好,包衣均匀,体外达到24 h缓慢释放。家兔口服相同剂量的丹参素速释微丸和缓释微丸后,Cmax分别为(1.45±0.24)μg·mL-1和(0.67±0.13)μg·mL-1,Tmax分别为(2.00±0.30)h和(8.00±0.50)h,MRT分别为(3.50±0.25)h和(10.93±0.26)h。与丹参素速释微丸相比缓释微丸的相对生物利用度为111.28%±1.28%。结论:丹参素缓释微丸可以达到24 h缓释,以AUC为评价指标时,与丹参素速释微丸生物等效。     

Control of drug release by incorporation of sorbitol or mannitol in microcrystalline-cellulose-based pellets prepared by extrusion-spheronization

Mixtures of microcrystalline cellulose (MCC) with sorbitol (up to 50%) or mannitol (up to 80%) were investigated as major excipients for controlled accelerated release of the model poorly water-soluble drug hydrochlorothiazide from pellets prepared by extrusion/spheronization. Optimal wetting volume decreased with increasing polyol content and was always less than the volume required for maximum wet mass consistency. All pellet formulations had satisfactory morphological, mechanical and flow properties, although sorbitol/MCC pellets were rougher than mannitol/MCC pellets. Together they presented a wide range of drug release profiles in 0.1?M HCl, allowing the rate of drug release into aqueous media to be controlled by manipulation of sorbitol or mannitol content. Pellets with a 50% sorbitol content released hydrochlorothiazide faster than pellets with a 50% mannitol content because of their greater porosity and the greater solubility of sorbitol in water. Fastest release was from pellets with an 80% mannitol content, which rapidly underwent complete disintegration.     

Antiinflammatory activity of a polyherbal formulation

The antiinflammatory activity of the polyherbal formulation Entox^® was investigated in rats for acute and sub acute models of inflammation using carrageenan-induced rat paw edema and cotton pellet granuloma methods respectively at a dose of 300 mg/kg and 600 mg/kg administered orally. The formulation in doses of 300 mg/kg and 600 mg/kg showed 51.61% and 54.84% inhibition of paw edema, respectively at the end of 3 h. The percent inhibition of granuloma by cotton pellet method was 27.92% and 53.17%, respectively. The formulation showed a significant antiinflammatory activity in both the experimental models and the activity was comparable to that of the standard drug, indomethacin.     

Polyamines: Potential anti-inflammatory agents and their possible mechanism of action

Objective:

To evaluate the anti-inflammatory activity of exogenously administered polyamines on experimentally induced acute and chronic inflammation in wistar rats and to elucidate their possible mechanism of action.

Materials and Methods:

The in vivo anti-inflammatory activity of polyamines was studied using acute (carrageenin paw edema), sub-acute (cotton pellet granuloma) and chronic (Freund''s adjuvant induced arthritis) models of inflammation. The biochemical parameters like liver lipid peroxides, SGOT and SGPT were also measured.

Results:

Polyamines exhibited significant anti-inflammatory activity in acute, sub-acute and chronic models of inflammation. Polyamines treatment inhibited the increase in lipid peroxides in liver and the serum concentration of marker enzymes (glutamate oxaloacetate transferase and glutamate pyruvate transferase) during inflammation.

Conclusion:

Polyamines possess anti-inflammatory activity in acute and chronic inflammation which can be attributed to their anti-oxidant and /or lysosomal stabilization properties.     

结核丸联合常规抗结核方案治疗老年肺结核合并颈部淋巴结核的临床研究

目的：评价结核丸联合常规抗结核方案治疗老年肺结核合并颈部淋巴结核的临床疗效。方法2012年1月－2014年1月共纳入河北省胸科医院胸三科103例合并颈部淋巴结核老年肺结核患者,并按随机数字表法将患者随机分为常规抗结核方案组（对照组）51例和结核丸联合常规抗结核方案组（治疗组）52例。对照组采用常规抗结核方案（2HRZE/4HR）治疗;治疗组在对照组治疗基础上加服结核丸治疗。2组均先采用标准化抗结核药物治疗4周后,行颈淋巴结结核病灶摘（清）除术,脓肿性结节行切开引流术。2组均治疗6个月后检测痰涂片,流式细胞术检测外周血CD8细胞上自然杀伤（NK）T细胞表面受体NKG2D和NKG2A表达及血清白细胞介素（IL）-6、IL-10、肿瘤坏死因子-α（TNF-α）水平变化,并进行临床疗效评价。结果治疗组病灶吸收率为78.85%（41/52）,显著高于对照组的58.82%（30/51）（χ2＝4.439,P＜0.05）;空洞闭合率为62.86%（22/35）,也显著高于对照组的35.48%（11/31）（χ2＝3.893, P＜0.05）。治疗组2、4、6个月末累计痰菌阴转率显著高于对照组（χ2值分别为5.343、5.067和4.118, P均＜0.05）。治疗组治疗后表达 NKG2A的CD8细胞显著低于同组治疗前和对照组治疗后（t值分别为9.510、9.832,P均＜0.01）;表达NKG2D的CD8细胞显著高于同组治疗前和对照组治疗后（t值分别为10.622、10.433,P均＜0.01）。2组血清IL-6、TNF-α水平均较同组治疗前下降（治疗组t值分别为17.344、21.142,对照组t值分别为10.984、12.203,P均＜0.01）,且治疗组治疗后低于对照组治疗后（t值分别为7.832、5.478,P均＜0.01）。2组血清IL-10水平均明显高于同组治疗前（t 治疗组＝12.454、t 对照组＝7.934, P均＜0.01）,且治疗组治疗后高于对照组治疗后（t＝4.720,P＜0.01）。治疗组淋巴结核有效率（46/52,88.5%）高于对照组（33/51,64.7%）（χ2＝6.855,P＜0.01）。结论结核丸联合常规抗结核方案治疗可提高患者的免疫功能及痰菌阴转率,促进病灶吸收。     

Development of multiple-unit pellet system tablets by employing the SeDeM expert diagram system II: pellets containing different active pharmaceutical ingredients

The SeDeM Expert Diagram System (SeDeM EDS) was originally developed to provide information about the suitability of powders to produce direct compressible tablets. Multiple-unit pellet systems (MUPS) are dosage forms consisting of pellets compressed into tablets or loaded into hard gelatin capsules. The aim of this study was to apply the SeDeM EDS to different size pellets (i.e. 0.5, 1.0, 1.5, 2.0, and 2.5?mm) containing different APIs (i.e. doxylamine, ibuprofen or paracetamol) to determine which properties should be corrected to yield MUPS tablet formulations. The SeDeM parameter tests were conducted on the pellets, selected excipients, intermediate blends, and final blends. The study showed that the properties of the pellets depended on the active ingredient and pellet size. The SeDeM compressibility indices indicated that the final pellet blends should be suitable for compression into MUPS tablets. MUPS tablets were prepared from the final blends and evaluated in terms of physico-chemical properties and dissolution profiles. Only three of the MUPS tablet formulations containing ibuprofen and one MUPS tablet formulation containing paracetamol failed content uniformity. The water solubility of the APIs as well as the pellet size (surface area exposed to the dissolution medium) attributed to the difference in drug dissolution rate.     

Prenatal diclofenac sodium administration increases the number of Purkinje cells in female rats: a stereological study

Diclofenac sodium (DS) may affect the number of Purkinje cells in the developing cerebellum since DS can easily be transported from the maternal to the fetal physiological system during the pregnancy. In the present study, the effects of prenatal exposure to DS on the number of Purkinje cells in the cerebellum of 4-week-old (4W-old) and 20-week-old (20W-old) female rats were investigated. There were two main groups: the drug-treated group (DTG) and the control group (CG). Beginning from the 5th day after mating for a period of 15 days, a daily dose of 1 mg/kg of DS (Voltaren, 75 mg/3 ml ampul, Novartis, Mefar Ilaç Sanayi A.S., Kartal, ?stanbul, Turkey) was intraperitoneally injected in the DTG of pregnant rats. In contrast, a daily dose of 1 ml/kg of isotonic saline was intraperitoneally administered to the CG of pregnant rats during the same period. After spontaneous delivery, female offspring were obtained, and the main groups’ offspring were divided into two subgroups as a 4W-old group and a 20W-old group. Therefore, there were four groups at the end of the experiment: the 4W-old DTG and the CG, and the 20W-old DTG and the CG. At the end of 4W and 20W, offspring were perfused, their brains were dissected, and the number of cells estimated via the optical fractionator technique. Our results showed that while the total number of Purkinje cells in the cerebellum of offspring of DT 20W-old female rats was significantly higher than that of the CG, there was no significant difference between the 4W-old DTG and the control groups. Therefore, it could be suggested that DS administration during the prenatal period increases the number of Purkinje cells in the cerebellum of a developing female rat throughout postnatal 20W.     

TRH-03肠溶微丸的制备及其处方优化

目的研究TRH-03肠溶微丸的处方优化及制备工艺。方法采用流化床包衣法,以载药量及释放量为考察指标,对TRH-03肠溶微丸的处方、上药和包衣工艺进行了优化。结果制得的3批肠溶微丸圆整度好,其载药率分别为35.63%、35.04%、35.64%;在人工胃液中保持不释药,人工肠液中45min内释放率分别为89.58%、88.96%、88.36%,载药量稳定且重现性好,体外释放度符合中国药典2010年版二部的要求。结论本方法制备工艺简单易行,重复性好,适合进一步的工业化生产。