水杨酸软膏与乳膏的制备及质量检查

目的:探讨以水杨酸乳膏取代软膏的可行性.方法:用软膏基质和乳膏基质分别制备水杨酸软膏和乳膏,并以刺激性试验、稳定性试验、释放度试验和临床试验进行比较.结果:以乳膏基质制备的成品在释放度和外观上好于软膏基质.结论:水杨酸乳膏可以取代软膏.     

及胶软膏的体外释放度考察

目的:考察及胶软膏的体外释放度,为优化处方、制备工艺、合理用药提供依据。方法:用无水葡萄糖为对照品,以白及多糖为指标,生理盐水为释放介质,0.2%蒽酮-硫酸试液为染色剂,采用透析袋法研究及胶软膏的体外释药特性。结果:4 h内白及多糖累积释放度为61.8%,为速释期;在12 h以后药物的释放度为38.2%,为缓释期;48 h内累积释放度为97.8%。结论:及胶软膏具有缓释性,每12 h使用一次可保持疗效。该方法用于及胶软膏的体外释放度考察,操作便利、方法稳定、结果可靠。     

水杨酸软膏与乳膏的比较

用软膏基质和乳膏基质分别将水杨酸制成水杨酸软膏和水杨酸乳膏,并用刺激性试验、稳定性试验、释放度试验和临床试验进行比较,结果是乳膏基质的成品在释放度和外观上好于软膏基质.     

不同厂家复方酮康唑乳膏释放度的比较

目的以不同厂家复方酮康唑乳膏释放度的比较数据为例,论证建立释放度的重要性。方法采用流通池法进行体外释放度实验,以HPLC法测定酮康唑含量,计算累计释放百分率,并以威布尔方程拟合释放参数,用方差分析对组间溶出参数进行统计学分析。比较5个厂家复方酮康唑乳膏的体外释放度。结果5个厂家复方酮康唑乳膏体外释放度拟合参数m,T50,Td和T80均存在显著性差异（P〈0.01）。结论说明不同厂家复方酮康唑乳膏的释放度存在差异,乳膏的体外释放度能够评价其质量。     

氢定乳膏制备工艺的优化及体外释放度考察

目的:优化氢定乳膏的制备工艺,测定其体外释放速率.方法:以乳膏的均匀度和粒度为考察指标,采用正交设计优化制备工艺;采用高效液相色谱法测定氢定乳膏在释放介质中的含量及释放速率.结果:最佳制备工艺为三乙醇胺和聚山梨醇酯-80加入水相中,乳化温度85℃,变速搅拌,乳化40 min.氢化可的松和醋酸氯已定的释放速率分别为13.9,137.1 μg·cm-2·h-1/2,r=0.983 5,r=0.996.结论:以最优工艺制备的3批制剂释放参数无明显变化,质量稳定.     

湿疮清乳膏治疗亚急性湿疹的Ⅱ期临床试验

目的:观察中药湿疮清乳膏治疗亚急性湿疹(湿热留滞、血虚风证)的疗效及安全性。方法:采用随机、双盲、多中心、阳性药平行对照的Ⅱ期临床试验方法。共入组203例,实际完成201例,其中试验组101例,对照组100例。试验组用湿疮清乳膏,对照组用冰黄肤乐软膏,bid,疗程为2周,每周复诊1次。结果:试验组总有效率与对照组比较,差异无统计学意义(83.2%vs 79.0%,P>0.05)。两组在症状的改善上疗效相当。两组均未发现不良反应。结论:中药湿疮清软膏治疗亚急性湿疹(湿热留滞、血虚风证)安全、有效,疗效与冰黄肤乐软膏相当。     

冰黄肤乐软膏体外抗炎抗菌及皮肤毒性评价研究

目的探讨冰黄肤乐软膏体外抗炎抗菌作用及皮肤毒性评价。方法评估冰黄肤乐软膏抗炎作用:SD大鼠和KM小鼠,随机分为模型组、基质组、皮炎平组、冰黄肤乐软膏低、中、高剂量组,测定足趾肿胀度、耳肿胀度和白细胞水平;评估冰黄肤乐软膏抗菌作用:将冰黄肤乐软膏样品进行梯度稀释,分别加入细菌或真菌50μl,确定该药物的最小抑菌浓度(MIC);皮肤刺激性及组织病理学:采用家兔皮肤自体对照方式,连续给药7 d,观察药物刺激强度,在观察期结束时取皮肤进行组织病理学检查。结果冰黄肤乐软膏在低、中、高剂量组各个时间点对大鼠足趾肿胀的影响与基质组和模型组比较,差异有统计学意义(P 0.01);冰黄肤乐软膏低、中、高剂量组对小鼠耳肿胀和白细胞水平的影响与基质组和模型组比较,差异有统计学意义(P 0.05);冰黄肤乐软膏对金黄色葡萄球菌、绿脓杆菌及白色念珠菌的MIC分别为:3.12～6.25、3.12～6.25、1.56～3.12 mg/ml,有显著抑制作用;冰黄肤乐软膏不具有皮肤刺激性。结论冰黄肤乐软膏具有很好的抗炎抗菌作用,同时无皮肤刺激性,证实其在临床用药中的有效性和安全性。     

盐酸特比萘芬乳膏的释放度考察

目的:建立盐酸特比萘芬乳膏释放度检查法。方法:采用改良的桨碟法进行盐酸特比萘芬乳膏的体外释放度试验,以超高效液相色谱法测定其释放度;并用f2相似因子法评价自制乳膏与兰美抒体外释放曲线的相似性。结果:乳膏基质及释放介质对测定无干扰,平均回收率为101.1%,RSD值为0.33%(n=9)。f2因子分别为45.5,37.8,58.7。结论:本法简便、重现性好,为建立盐酸特比萘芬乳膏的体外释放度检查法提供依据。自制乳膏中有一批与兰美抒释放行为相似。     

浓乳稀释法制备水包油型乳膏的研究

目的:探讨浓乳稀释法制备水包油(O/W)型乳膏基质的工艺及其特点。方法:以尿素乳膏为模型,以乳膏稳定性的各项参数为指标,考察参与乳化的不同水相比例对浓乳稀释法制备O/W型乳膏基质的影响,并与混合乳化法制备的乳膏基质比较;采用扩散法考察所制乳膏释放度。结果:当参与乳化的水相与油相质量之比为1.1∶1时,浓乳稀释法制备的O/W型乳膏基质稳定性较好,并优于混合乳化法制备的乳膏,2种方法制备的尿素乳膏释放度分别为6.542、3.621。结论:本法与制备O/W型乳膏常用方法相比节能、节时、低耗,值得推广应用。     

琥珀酸美托洛尔缓释片的制备及体外释放度考察

目的制备与倍他乐克释放行为一致的琥珀酸美托洛尔缓释片。方法采用正交试验优化琥珀酸美托洛尔缓释片的处方工艺,通过高效液相色谱法测定体外释放度,并考察处方工艺的重复性,并与市售片进行F2相似因子比较。结果自制片3批次各取样点释放度的SD值均小于2%,F2值分别为92.6、91.5、87.2。结论本处方工艺稳定且释放行为与市售片相似。     

五种阿昔洛韦软膏释放与透皮性质比较

目的：探讨不同的软膏基质对阿昔洛韦（ＡＣＶ）透皮性能的影响。方法：设计四种不同基质的处方,测定ＡＣＶ从处方中的释放与经皮渗透性质,并与商品ＡＣＶ软膏进行比较。结果：四种软膏基质中ＡＣＶ的释放速率与透皮速率均大于商品ＡＣＶ软膏,乳膏基质、Ⅰ号凝胶基质、ＰＥＧ基质、Ⅱ号凝胶基质中药物的透皮速率分别是商品软膏的２．４７,４．９８,１２．７９与１７．８５倍。结论：由卡巴浦、月桂氮苷卓酮、丙二醇、薄荷油及辅助促透剂组成的ＡＣＶ软膏为较好的处方。     

Effect of Plant Extracts Formulated in Different Ointment Bases on MDR Strains

Extracts of Aloe vera whole plant, Eucalyptus globulus leaves, Ficus infectoria bark, Ficus religiosa bark and Piper betel leaves were studied for antibacterial activity on resistant and sensitive strains, isolated from skin and soft tissue infections. A combination of hot alcoholic extracts of Ficus infectoria, Ficus religiosa and Piper betel were found to be more effective against all the isolates. The combined extract was formulated in different ointment bases such as polyethylene glycol, gelatin, sodium alginate, carbopol, cream base and honey. These were then evaluated to find a suitable base for preparation of an ointment. In vitro study of the release of antimicrobials and kill-time studies of the herbal ointments was carried out against multi-drug resistant isolate of Pseudomonas. The ointment showed bactericidal activity within 2 h against the resistant strain of Pseudomonas spp.     

瑰及乳膏中白及多糖的体外释放度考察

目的考察瑰及乳膏的体外释放度,为合理用药提供依据。方法以无水葡萄糖为对照品、白及多糖为指标、生理盐水为释放介质、0.2%蒽酮-硫酸试液为染色剂,采用透析袋法研究瑰及乳膏的体外释药特性。结果 10 h内白及多糖累积释放度为84.2%,为速释期;在12 h以后其释放度为15.8%,为缓释期;48 h内累积释放度为97.9%。结论瑰及乳膏具有缓释特性,每10 h使用一次可保持疗效。透析袋法用于瑰及乳膏的体外释放度考察,操作便利、方法稳定、结果可靠。     

Percutaneous absorption of ketoprofen. I. In vitro release and percutaneous absorption of ketoprofen from different ointment bases

Ketoprofen (KP) is a potent non-steroidal anti-inflammatory drug which is used for the treatment of rheumatoid arthritis. The oral administration of KP can cause gastric irritation and renal adverse effects. Topical application of the drug can bypass gastrointestinal disturbances and provide relatively consistent drug levels at the site of action. Since the efficacy of an ointment depends on the type of ointment base and the concentration of the drug, four different bases (white petrolatum, cold cream, hydrophilic ointment and Carbopol 940 gel) were used at 1, 3, 5, 7 and 10% concentrations of KP to evaluate the effect of ointment base and concentration. The general rank order of the drug release was found to be: Carbopol gel > hydrophilic ointment > cold cream > white petrolatum. There was a positive correlation between the concentration of KP and release rate for all bases except Carbopol gel. The in vivo percutaneous absorption of KP from different ointment bases at 3% concentration was studied by carrageenan-induced paw edema in mice. The rank order of the percent edema inhibition was as follows: Carbopol gel ≥ hydrophilic ointment > cold cream > white petrolatum. There was a good correlation between the in vitro and in vivo results.     

Pharmaceutical availability of betamethasone dipropionate and gentamicin sulfate from cream and ointment

Kinetics of drug release from both compared preparations occuring as a cream and ointment, was in vitro studied. A reversed-phase HPLC method was developed for the determination of betamethasone dipropionate in lipophylic bases. Analyses were performed using a PLRP column with a mobile phase of methanol-acetonitrile-water and ultraviolet detection at lambda = 254 nm. The calibration curve was constructed for concentration (.0-50.0 microg/ml. The method is simple, accurate and precise. For the determination of gentamicin sulfate the FPIA method was used.     

In vitro skin absorption and drug release - a comparison of six commercial prednicarbate preparations for topical use.

Reconstructed human epidermis is a useful tool for in vitro skin absorption studies of chemical compounds. If this may hold true also for topical dermatics, we investigated the glucocorticoid prednicarbate applied by two sets (innovator and generic) of cream, ointment and fatty ointment using the commercially available EpiDerm model. Moreover, stability and local tolerability of the preparations as well as drug release were studied, to estimate an influence on prednicarbate absorption and metabolism. While release ranked in the order cream相似文献   

正交试验法优化祖师麻凝胶膏组方及其体外透皮特性研究

目的采用正交试验优化祖师麻凝胶膏的组方,并研究其体外透皮吸收行为。方法以初黏度、膏体强度和释放度为考察指标,综合评分,采用L18(37)正交试验对空白基质辅料的用量进行优化,确定最佳处方组合并进行验证试验。采用改良的Franz扩散池,通过体外透皮试验,采用HPLC法同时测定最佳处方中瑞香苷、瑞香素-8-O-β-D-葡萄糖苷、祖师麻甲素的体外透皮渗透量。结果优选出祖师麻凝胶膏黏合剂最佳组方为卡波姆980、聚维酮K30、二氧化硅、阿拉伯胶、聚维酮K90、明胶、聚乙二醇400比例为8∶3∶4∶12∶8∶10∶8,体外透皮行为符合零级动力学过程。结论采用优选的黏合剂组方制备的凝胶膏剂的黏附性、膏体强度、释药性能等均良好,具有较好的使用舒适度,可作为祖师麻凝胶膏的基础制剂组方使用,并可以为新型凝胶膏剂的开发提供技术参考。     

Pharmaceutical availability of clobetasol-17-propionate from cream and ointment

Kinetics of drug release from both compared preparations available as a cream and an ointment, was in vitro studied. A reversed-phase HPLC method was developed for the determination of clobetasol-17-propionate in lipophylic bases using clobetasol-17-butyrate as an internal standard. Analyses were performed using a C18 reversed-phase column with a mobile phase of methanol-water and ultraviolet detection at lambda=254 nm. The calibration curve was constructed for the concentration range 0.5-40.0 microg/ml. The method is simple, accurate and precise.     

特益乳膏的制备及稳定性考察

目的:研制盐酸特比萘芬硝酸益康唑乳膏(特益乳膏)并考察该制剂的稳定性。方法:采用单因素法优化处方制得特益乳膏并对其在市售包装条件下进行稳定性试验(影响因素试验、加速试验和长期试验)。结果:优化处方组成包括盐酸特比萘芬10g、硝酸益康唑2.5g、白凡士林30g、十八醇10g、硬脂酸60g、三乙醇胺5.4g等(总量1000g),所制样品均匀、细腻、涂展性好;其稳定性各项指标未见明显变化。结论:所制特益乳膏处方合理,在市售包装条件下稳定性良好。     

Liberation of hydrocortisone acetate from different commercial formulations

Liberation of hydrocortisone acetate from different commercial formulations In this article the release of hydrocortisone acetate (HC-acetate) from three commercial semisolid formulations (Ebeno-ointment, Soventol HC cream and Fenistil hydrocortisone ointment) was measured by means of a multilayer membrane system (MLMS) described in the literature. The formulations are different regarding rate and extent of the release of HC-acetate. The release of HC-acetate form the Soventol HC cream is very fast and results in high topical availability. In contrast, HC-acetate shows a sustained release from the Fenistil hydrocortisone ointment. The release of HC-acetate from the Ebenol-ointment is between that of the Soventol HC cream and that of the Fenistil-ointment. In summary, HC-acetate shows a shorter mean liberation time (MDT) and a higher topical availability from Soventol HC cream in comparison to the other formulations studied.