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.     

玳玳黄酮自微乳化微丸含量测定及HPLC特征图谱分析

目的:建立玳玳黄酮自微乳化微丸中柚皮苷、新橙皮苷HPLC含量测定方法和HPLC特征图谱,为玳玳黄酮自微乳化微丸的质量控制提供有效的方法。方法:含量测定采用Agilent-C18色谱柱(250 mm×4.6 mm,5μm),流动相为乙腈-0.1%磷酸水溶液(22∶78),流速为1.0 mL.min-1,柱温为室温。HPLC特征图谱测定采用250-4 Lichrocart C18色谱柱(250 mm×4.0mm,5μm),流动相为甲醇-乙腈-0.1%的磷酸水溶液,梯度洗脱,流速1.0 mL.min-1,柱温30℃。检测波长均为283 nm。结果:柚皮苷浓度在4.48～17.92μg.mL-1范围内线性关系良好(r=0.9998),平均加样回收率为97.5%(RSD=1.0%);新橙皮苷浓度在5.92～23.68μg.mL-1范围内线性关系良好(r=0.9997),平均加样回收率为98.8%(RSD=0.82%)。在此条件下所建立的特征图谱中各成分得到有效分离,各批玳玳黄酮自微乳化微丸的相似度在0.900～1.000间。结论:HPLC法同时测定玳玳黄酮自微乳化微丸中柚皮苷和新橙皮苷含量的方法简便、准确,建立的HPLC特征图谱可用于评价微丸的物质组成及有效物质群的质量变化,可作为玳玳黄酮自微乳化微丸质量控制的依据。     

Characterization and evaluation of self-microemulsifying sustained-release pellet formulation of puerarin for oral delivery

The present study aims to develop self-microemulsifying drug delivery systems (SMEDDS) in sustained-release pellets of puerarin to enhance the oral bioavailability of puerarin. The performances of puerarin-SMEDDS including oils, emulsifiers, and co-emulsifiers were evaluated. Pseudo-ternary phase diagrams shows that the optimized formulation consisted of castor oil as the oil phase, Cremophor EL as the emulsifier, and 1,2-propanediol as the co-emulsifier. SMEDDS sustained-release pellets were prepared via extrusion-spheronization. The particle size distributions of the formulations were determined using transmission electron microscopy and scanning electronic microscopy. The mean particle size was 50 ± 8 nm. The pharmacokinetics and bioavailability of the puerarin-SMEDDS sustained-release pellets and puerarin tablets were evaluated and compared in beagle dogs. The absolute bioavailability of the puerarin-SMEDDS sustained-release pellets was enhanced by approximately 2.6-fold compared with that of the puerarin tablet. The relative bioavailability (F(rel)) of the SMEDDS pellets was 259.7% compared with the tablet group. The results demonstrated that the puerarin-SMEDDS sustained-release pellets had a sustained-release effect, and could remarkably improve the oral bioavailability of puerarin.     

盐酸坦索罗辛缓释微丸胶囊的制备及处方工艺考察

目的:制备盐酸坦索罗辛缓释微丸胶囊。方法:采用苏丽丝、雅克宜、欧巴代II作为包衣材料,用流化床底喷溶液上药法制备载药微丸,并进行缓释包衣。结果:以释放度为指标,通过对包衣工艺及处方影响因素的考察,确定了包衣处方工艺。结论:本研究处方工艺简便,重现性良好,可能适合工业化生产。     

酮洛芬微丸缓释片的制备及体外释放度考察

目的:制备一种酮洛芬缓释片剂。方法:采用挤出-滚圆法制备酮洛芬微丸,用Eudragit?RS 30D和Eudragit?RL30D包衣。再将包衣微丸与酮洛芬原药压片,最终制成酮洛芬缓释片。结果:体外释放度实验显示,制备的酮洛芬缓释片在2h内能释药30%,剩余70%药物在随后的10 h内缓慢释放。结论:用本方法制备酮洛芬缓释片,工艺简便,易于操作。     

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.     

Inhibition of the adhesive ability of Streptococcus mutans on hydroxyapatite pellet using a toothbrush equipped with TiO2 semiconductor and solar panel

TiO₂ has an antibacterial effect against Streptococcus mutans (S. mutans). The objective of this study was to show the Inhibition of the adhesive ability of S. mutans on hydroxyapatite pellet using a toothbrush equipped with TiO₂ semiconductor and solar panel. Gradual brushing of 9 hydroxyapatite pellets was done by the same person using a solar toothbrush under 750/LUX light source in water. As a control, pellets brushed with a placebo toothbrush were done using the same procedure by the same person. All the pellets were inoculated in 10 ml Brain Heart Infusion (BHI) broth containing 100μl of 10⁸ CFU/ml S. mutans and 1% sucrose and then incubated at 37°C for 12 hours. After incubation, the adherence conditions of S. mutans on each pellet were checked. The bacterial count of S. mutans on the brushed pellets using solar toothbrush were fewer than those using placebo toothbrush. The quantities of adherence of S. mutans decreased according to number of brushing and adhesion on pellets brushed more than 50 times could not be recognized. However, adhesion of S. mutans on the pellets brushed using placebo toothbrush were recognized and the adhesive quantities were visually the same. These results occurred because of some electronic charges on the brushed pellets using solar toothbrush. Soladey-3 toothbrush prevented S. mutans adhesion to the hydroxyapatite pellet under a light source.