奇奥心血丹滴丸对麻醉犬血流动力学的作用

目的观察奇奥心血丹滴丸对麻醉犬血流动力学的作用.方法3%戊巴比妥钠静脉麻醉,颈总脉插管及左心室插管,测量血压、心率、心输出量、左室内压、左室舒张末压、±dp/dtmax等血流动力学指标.结果奇奥心血丹滴丸可明显降低血压、心率、心输出量、左室内压、±dp/dtmax.结论奇奥心血丹丸具有负性频率、负性肌力及降低血压等作用.     

双氯酚酸钠米索前列醇片的抗炎作用研究

双氯酚酸钠米索前列醇片（ＤＳＭＴ）（２０,１０ｍｇ／ｋｇ）连续２ｄ灌胃给药可显著地抑制二甲苯所致鼠耳肿胀（Ｐ〈０．０１,Ｐ〈０．０５）;ＤＳＭＴ（１５,７．５ｍｇ／ｋｇ）灌胃给药均可非常显著抑制角叉菜胶至炎后３ｈ内大鼠足肿胀;ＤＳＭＴ高、低剂量组（１５,７．５ｍｇ／ｋｇ）灌胃给药７ｄdisplay structure     

KD306型耐硫甲烷化催化剂有效扩散系数的测定

基于开发的计算机取样系统,采用ＳＰＳＲ法脉冲动态测试ＫＤ３０６型耐硫甲烷化催化剂的有效扩散系数。线性化和参数估值的结果吻合较好,证实：线性化简化是合理的,参数估值是可用于有效扩散系数。ＫＤ３０６型耐硫甲烷化催化剂的曲折因子为７．２。     

细辛油的抗炎作用

腹腔注射细辛油0.24 ml/kg对角叉菜胶引起的大鼠足肿胀有抑制作用。此作用在切除肾上腺的大鼠亦能看到。细辛油能降低炎症组织及其渗出液中组胺含量,对组胺或PGE₂引起的大鼠足肿胀有抑制作用,并能对抗组胺或PGE₂引起的毛细血管通透性增加,本品能抑制大鼠胸腔因注射角叉菜胶后引起的白细胞游走;对大鼠棉球肉芽肿有抑制作用,并使胸腺萎缩,还降低正常大鼠肾上腺内维生素C含量。     

Drug release from reservoir pellets compacted with some excipients of different physical properties

The aim of the present study was to investigate the influence of the size and the porosity of excipient microcrystalline cellulose (MCC) particles on the densification and the deformation during compaction and the consequent effect on the drug release from reservoir pellets. Drug pellets consisting of salicylic acid and microcrystalline cellulose were prepared by extrusion-spheronisation and spray-coated with ethyl cellulose (ethanol solution). Excipient pellets of different size and porosity were prepared by extrusion-spheronisation or direct spheronisation. Five binary mixtures of reservoir pellets and excipient particles were prepared in the proportion 1:7 and lubricated. After compaction the reservoir pellets were retrieved and analysed to determine the intragranular porosity, surface area, shape and drug release. The reservoir pellets were shown to undergo extensive deformation and densification during compaction, resulting in a preserved or even prolonged drug release time. The mode of deformation of the reservoir pellets seems to be critical for the compression-induced change in drug release. Formation of large indents has a negative effect on the release time, while the use of small particles or small deformable agglomerates has a protective effect. We also hypothesize that the coating structure changes during compaction and the final structure of the coating is the net effect of two parallel processes, one reducing and one prolonging the drug transport time across the coating.     

Effect of intragranular porosity on compression behaviour of and drug release from reservoir pellets

In this study, reservoir pellets were prepared and their compression behaviour as well as the importance of their porosity for compression-induced changes in drug release was investigated. Pellets of three different porosities, consisting of microcrystalline cellulose and salicylic acid, were prepared by extrusion–spheronisation and spray-coated with ethyl cellulose (ethanol solution). Lubricated reservoir pellets were compressed and retrieved by deaggregation of the tablets. The retrieved pellets were analysed regarding porosity, thickness, surface area, shape and drug release. It was found that the coating did not significantly affect their compression behaviour. Compaction of pellets of high original porosity considerably affected densification and degree of deformation, whereas the effect on drug release was minor. For low porosity pellets the influence of compaction on drug release was appreciable, but only slight regarding densification and degree of deformation. In conclusion, the porosity of pellets is a potential factor that the formulator can use to optimize drug release and one that can affect the robustness of a formulation during manufacture. Moreover, the coating may be able to adapt to the densification and deformation of the pellets.     

中药浸膏微丸制备研究

目的:制备圆整度好、含药量较高的中药浸膏微丸.方法:用挤出滚圆制粒法制备微丸,并考察微丸的部分物理性质.结果:微丸中浸膏含量达40%,成品收率达80%,微丸物理性能稳定.结论:用挤出滚圆法制备的中药浸膏微丸具有产率高、物理性能优良的特点,挤出滚圆法在中药制粒领域具有巨大的应用潜力.     

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。     

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。