三种不同基质的苯巴比妥栓在家兔体内的药物动力学研究

研制了三种不同基质的苯巴比妥栓剂，并对其在家兔体内的药物动力学与市售片剂进行了比较。结果表明，三种栓剂的释药性具有显著性差异，以水溶性基质脂肪酸聚氧乙烯醚（Ｓ－４０型）制成的栓剂最好，其ＣｍａｘＡＵＣ值等均明显高于片剂和其它两种栓剂。     

盐酸异丙嗪栓的研制及其家兔体内生物药剂学评价

本文报告了盐酸异丙嗪栓剂的研究及其与片剂在家兔体内生物利用度的比较。试验采用双波长分光光度法测定盐酸异丙嗪的血药浓度。结果表明栓剂比片剂的达峰时间快，Ｔｐ之间有非常显著性差异（Ｐ〈０．０１）。Ｃｐ和ＡＵＣ没有显著性差异（Ｐ〉０．０５），栓剂的相对生物利用度为９８．０７％。     

高效液相色谱法测定异烟肼固体制剂血药浓度

本文应用高效液相色谱法对异烟肼栓剂、片剂的血药浓度监测方法进行了研究，用Ｃ１８，以２０％甲醇－水（含十二烷基硫酸钠）为流动相在２５４ｎｍ测定，用外标法定量。     

奥硝唑不同剂型药理分析及在妇科滴虫性阴道炎中的应用研究

目的总结奥硝唑栓剂与片剂的药理作用,探讨奥硝唑栓剂局部用药与奥硝唑片剂口服用药治疗滴虫性阴道炎的临床疗效。方法将200例滴虫性阴道炎患者随机分为观察组及对照组各100例,对两组患者分别进行奥硝唑栓剂与片剂治疗,观察比较两组的临床疗效。结果观察组和对照组的总有效率分别为94.00%和72.00%,两组比较有显著性差异（P〈0.05）。观察组患者的临床症状治疗后改善明显（P均〈0.05）;对照组患者的临床症状治疗后也改善明显（P均〈0.05）;观察组治疗后与对照组治疗后比较,观察组显著优于对照组（P〈0.05）。对照组不良反应发生率19/50（38.00%）;观察组不良反应发生率9/50（18.00%）,两组有显著性差异（P〈0.05）。结论奥硝唑栓剂局部用药与片剂口服相比,具有显效快、疗效强、不良反应少等优点,值得在临床上推广和应用。     

三种不同基质的苯巴比妥栓在家兔体内的药物动力学研究

研制了三种不同基质的苯巴比妥(phenobarbital,PBT)栓剂,并对其在家兔体内的药物动力学与市售片剂进行了比较.结果表明,三种栓剂的释药性具有显著性差异,以水溶性基质脂肪酸聚氧乙烯醚(S-40型)制成的栓剂最好,其Cmax、AUC值等均明显高于片剂和其它两种栓剂(P＜0.001).     

比较氧氟沙星两种片剂在健康志愿者体内的药物动力学

本实验采用反相高效液相荧光分析法，比较了８名健康志愿者单剂量口服两种氧氟沙星片剂后的药物动力学和生物利用度。血药浓度经时过程用ＣＡＰＰ程序包在计算机上拟合为二房室模型，试验片的相对生物利用度Ｆ为１００．１２％，经统计分析，二种片剂的Ｔｍａｘ，Ｃｍａｘ和ＡＵＣ均无显著性差异（Ｐ＞０．０５），可认为二种片剂具有生物等效性。     

美沙拉秦治疗溃疡性结肠炎的多中心研究

目的：观察美沙拉秦对我国溃疡性结肠炎病人的疗效。方法：溃疡性结肠炎病人１００例，其中４１例单纯溃疡性直肠炎为栓剂组，其他５９例为片剂组。栓剂组（男性２４例，女性１７例，年龄４３±ｓ１１ａ）予美沙拉秦栓剂１．０ｇ纳肛，ｂｉｄ，疗程８ｗｋ；片剂组（男性２９例，女性３０例，年龄４４±１４ａ）予美沙拉秦缓释片０．５～１．０ｇ，ｐｏ，ｔｉｄ～ｑｉｄ，疗程８ｗｋ；疗程结束后复查肠镜并作活检。结果：２组病人治疗后肠镜及组织学所见均显著改善，栓剂组总有效率为９８％，片剂组为９５％，前者无不良反应，后者不良反应轻微。结论：美沙拉秦治疗我国溃疡性结肠炎疗效显著而又安全。     

国家非处方药目录（第一批）

１　西药部分１－１　解热、镇痛药活性成分序号药品名称剂型１布洛芬Ｉｂｕｐｒｏｆｅｎ片剂、缓释片、缓释胶囊剂、颗粒剂、口服溶液剂、乳膏剂、栓剂、搽剂２双氯芬酸（二乙胺盐）Ｄｉｃｌｏｆｅｎａｃ凝（乳）胶剂、乳膏剂３阿司匹林（包括阿司匹林钙脲、锌、赖氨酸阿司匹林）Ａｓｐｉｒｉｎ片剂、水溶片、肠溶片、缓释片、泡腾片、胶囊剂、栓剂、散剂４吲哚美辛（消炎痛）Ｉｎｄｏｍｅｔａｃｉｎ软膏剂、搽剂、乳膏剂、栓剂、贴膏剂５对乙酰氨基酚（扑热息痛）Ｐａｒａｃｅｔａｍｏｌ片剂、咀嚼片、缓释片、泡腾片、分散片、胶囊剂、…     

国家非处方药目录(第一批)西药部分

一、解热、镇痛药活性部分序号药品名称剂型注１布洛芬Ｉｂｕｐｒｏｆｅｎ片剂、缓释片、缓释胶囊剂、颗粒剂、口服溶液剂、乳膏剂、栓剂、搽剂受限２双氯芬酸（二乙胺盐）Ｄｉｃｌｏｆｅｎａｃ凝（乳）胶剂、乳膏剂受限３阿司匹林（包括阿司匹林钙脲、锌、赖氨酸阿司匹林）Ａｓｐｉｒｉｎ片剂、水溶片、肠溶片、缓释片、泡腾片、胶囊剂、栓剂、散剂受限４吲哚美辛（消炎痛）Ｉｎｄｏｍｅｔａｃｉｎ软膏剂、搽剂、乳膏剂、栓剂、贴膏剂受限５对乙酰氨基酚（扑热息痛）Ｐａｒａｃｅｔａｍｏｌ片剂、咀嚼片、缓释片、泡腾片、分散片、胶囊…     

布洛芬栓剂、片剂解热作用的比较

布洛芬在解热镇痛方面，具有比阿斯匹林或扑热息痛作用更强、更安全的优点，目前是世界上销售量最大的抗风湿解热镇痛药。国内市场上常见的有片剂、缓释胶囊，根据临床需要，我们采用国产栓剂基质，试制成布洛芬小儿退热栓，将栓剂与片剂进行动物体内降温试验比较，结果表明栓剂的退热效果明显优于片剂，临床试用疗效良好，现将试验结果报告如下：1实验器材SHARPMT-20数字显示测温计，兔固定架、磅秤、注射器、家兔灌胃导管、兔开口器。2实验药品布洛芬（山东新华制药厂），布洛芬栓（自制）、空白基质检（自制）、布洛芬片（安徽淮南制…     

Relative bioavailability of a paracetamol suppository

Summary The relative bioavailability of a new paracetamol suppository (Panodil) and tablets in doses of 0.5 and 1 g was investigated in eight healthy subjects. The tablets were absorbed faster and higher peak plasma concentrations were obtained than after the suppositories. The bioavailability of the suppositories was approximately 80% of that of the tablets at both dose levels. There was no indication of capacity-limited elimination at either the two doses investigated.     

4种给药方案治疗滴虫性阴道炎的成本-效果对比研究

目的:探讨4种给药方案治疗滴虫性阴道炎所产生的经济学效果.方法:选择我院门诊滴虫性阴道炎患者120例,随机分为4组,分别给予保妇康栓加奥硝唑片(A组)、双唑泰栓加奥硝唑片(B组)、甲硝唑栓加奥硝唑片(C组)、奥硝唑片(D组),运用药物经济学方法进行成本-效果分析.结果:4组方案成本分别为:116.4元、128.8元、85.1元、63.8元;有效率分别为:90%、93.3%、93.3%、86.6%;成本-效果比分别为:1.29、1.38、0.91、0.73;A、B、C方案相对于D方案的增量成本-效果比分别为:15.4、9.7、3.2.结论:甲硝唑栓加奥硝唑片治疗滴虫性阴道炎疗效好、成本低,并且不良反应最少.     

氟康唑片与达克宁栓治疗念珠菌性阴道炎的随机对照研究

目的 比较氟康唑口服片与达克宁栓两种不同方法治疗念珠菌性阴道炎的疗效.方法 将98例念珠菌性阴道炎患者随机分为两组,分别予氟康唑片和达克宁栓治疗(氟康唑片组48例,达克宁栓组50例).治疗两周后观察疗效及做阴道分泌物检查.结果 氟康唑片组有效率为95.83%,达克宁栓组有效率为80%,有显著性差异.结论 氟康唑口服片安全有效,疗效优于达克宁栓剂.     

尼美舒利栓药代动力学及相对生物利用度研究

目的　以市售的尼美舒利普通片为参比制剂 ,评价自制尼美舒利直肠栓的生物利用度和生物等效性。方法　采用随机交叉分组实验设计 ,5只新西兰家兔分别给予剂量 5 0 mg.kg- 1 的尼美舒利栓和普通片剂 ,栓剂直肠给药 ,片剂口服 ;按设计采集 2 4h内动态血标本 ;以 HPLC法测定血浆药物浓度 ;以二室模型计算两种制剂在动物体内的药动学参数和相对生物利用度。结果　参比制剂和受试制剂的 Tmax 分别为 ( 6.96± 1 .69) h和( 2 .0 3± 1 .0 7) h,Cmax 分别为 ( 65 .5 1± 2 8.0 9) mg.L- 1和 ( 65 .99± 1 2 .1 3 ) mg.L- 1 ,AUC0 - inf 分别为 ( 5 1 9.3 4±1 5 1 .0 5 ) mg.h.L- 1和 ( 4 40 .1 2± 72 .89) mg.h.L- 1 ,t1 / 2α分别为 ( 0 .63± 0 .1 3 ) h和 ( 2 .2 9± 0 .82 ) h,t1 / 2β分别为( 1 .72± 0 .95 ) h和 ( 1 .76± 0 .2 1 ) h,MRT分别为 ( 9.0 0± 1 .1 6) h和 ( 6.2 4± 0 .62 ) h,滞后时间分别为 ( 5 .42±1 .63 ) h和 ( 0 .0 7± 0 .0 9) h,以市售 NIM普通片为参比制剂 ,NIM直肠栓的相对生物利用度为 84.75 %。结论　统计结果显示 ,各主要药动学参数均有显著性差异。尼美舒利栓具有明显的速释特征 ,与尼美舒利普通片生物不等效。     

Investigation of hypoglycemic properties of rectal suppositories with chlorpropamide

Rectal suppositories with chlorpropamide and suppositories with chlorpropamide in the dispersion system with urea were prepared. Witepsol H15 and H19 and a polyoxyethyleneglycol mixture were used as bases. Rabbits were tested for blood-glucose level. The animals have been administered with prepared suppositories and commercial tablets. It was found that the suppositories prepared on the basis Witepsol H 15 with the dispersed chlorpropamide caused a much higher decrease of blood-glucose level than commercial tablets.     

Studying the bioavailability of fenozan acid in various medicinal forms

The bioavailability of fenozan acid as an antioxidant from tablets and rectal suppositories was studied in vitro and in vivo (rabbits). The complete release of fenozan acid from tablets in vitro takes 45 min, while 75% of the drug content is released from tablets within 21 min. The absolute bioavailability of fenozan acid from tablets and rectal suppositories in vivo amounts to 46.8 and 51.4%, respectively. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 40, No. 1, pp. 3–5, January, 2006.     

反复发作外阴阴道炎患者的临床处理

目的探讨克霉唑栓和伊曲康唑联合用药治疗反复发作念珠菌性外阴阴道炎的临床疗效。方法选取2009年3月-2011年7月到本院治疗的120例反复发作念珠菌性外阴阴道炎患者,随机分成对照组和治疗组各60例,两组患者在年龄、病情、病程等一般资料差异无统计学意义,具有可比性。治疗组患者给予克霉唑栓500mg／片,阴道给药,洗净后将栓剂置于阴道深处,每晚1次,1次1粒,连续7d为1个疗程,此外,治疗组患者再口服伊曲康唑200mg／片,每日1次,疗程为3d。对照组患者给予克霉唑栓500mg／片,阴道给药,洗净后将栓剂置于阴道深处,每晚1次,1次1粒,连续7d为1个疗程。观察并对比治疗组和对照组患者用药后的临床疗效。结果经治疗后,治疗组患者60例,治愈59例,治愈率为98．3％;对照组患者60例,治愈45例,治愈率为75．0％。两组比较可见,治疗组治愈率明显高于对照组,两组患者差异有统计学意义（P〈0．05）。结论克霉唑栓和伊曲康唑联合用于反复发作念珠菌性外阴阴道炎的治疗,可以显著提高念珠菌性外阴阴道炎的治疗效果,值得临床推广使用。     

The role of various surfactants on the release of salbutamol from suppositories

Salbutamol is a selective beta(2)-adrenoreceptor agonist with different pharmacological effects. In this research because of the simplicity of suppository application in elderly and its higher plasma concentration than tablets as well as its particular indication in premature labour, salbutamol suppositories were prepared. The suppositories were formulated containing 10 mg of the drug and Witepsol H15, the oleaginous soluble base using melting method. To optimize the release rate of drug, different surfactants namely, sodium lauryl sulphate (SLS) as an ionic surfactant and Tween 80 as well as Arlacel 60 as non-ionic surfactants with different HLBs were chosen. The effect of surfactant concentration on the release rate of salbutamol from suppositories were also investigated. All prepared formulations fulfilled the specifications set down in British Pharmacopoeia. The results showed that Tween 80 (2%w/w) and SLS (0.75%w/w) caused an increase in dissolution rate of salbutamol from suppositories. As anionic surfactants, such as SLS, cause greater damage on mucosa than non-ionic surfactant, such as Tween 80, this study recommended that Tween 80 could be added in suppository formulation in order to increase the dissolution rate of salbutamol. It was also shown that the release rate of salbutamol altered linearly with the amount of Tween 80 in suppository formulations.     

Pharmacokinetic evaluation of ethionamide suppositories.

The absorption and elimination of ethionamide (ETA) after oral tablets and rectal suppositories were determined in 12 healthy, adult male volunteers. A randomized, double-blind, double-dummy, crossover design was used. Treatments compared 250-mg ETA tablets and a placebo suppository to a 500-mg ETA suppository and two placebo tablets, given 7 days apart. Blood samples were collected at predetermined intervals for 12 hours after the dose. Serum concentrations of ETA were determined using high-performance liquid chromatography. The area under the serum concentration-time curve was used to compare the relative bioavailability of ETA from the two preparations. Relative bioavailability after rectal administration was 57.3% of that after oral administration. The maximum serum concentration after rectal administration was 33% of that after oral administration. Higher doses of ETA and serum concentration monitoring are recommended whenever the suppositories are used.     

Comparison of bioavailability in man of tamoxifen after oral and rectal administration

The bioavailability of tamoxifen from 40 mg suppositories was tested in six male volunteers and compared with that of tamoxifen (Nolvadex) tablets. Plasma concentrations of tamoxifen and its major metabolites, 4-hydroxytamoxifen and N-desmethyltamoxifen, were measured by extraction from plasma obtained at different times after administration, separated by HPLC, converted on-line to fluorescent phenanthrene derivatives and quantified with a fluorescence detector. The mean relative bioavailability from the suppositories was 28%; the addition of a surfactive agent diminished the bioavailability to 13%. Simulation of repeated administration of 40 mg suppositories suggests a mean steady state plasma concentration for tamoxifen of approximately 70 ng ml-1, i.e. 30% of the steady state value after simulated oral administration. Rectal administration of tamoxifen leads to a lower bioavailability than that by oral administration and therefore cannot be recommended when used in equivalent doses.