阿丹三滴眼液的制备及临床应用

目的：研制阿丹三滴眼液，建立质量控制方法，观察其临床疗效。方法：对主要成份阿托品采用可见分光光度法测定。结果：工艺简单，易控制，质量基本稳定，定性、定量方法准确，专属性强。结论：本制剂工艺合理，质量可控，临床疗效良好。     

鱼腥草滴眼液的特性及临床疗效

目的:观察鱼腥草滴眼液的特性和临床疗效。方法:以鱼腥草为主药,用水蒸气蒸馏法制备鱼腥草滴眼液,对其质量进行鉴别,并与病毒唑滴眼液进行临床疗效对照研究。结果:鱼腥草滴眼液组结膜炎治疗总有效率为95.24%,病毒唑滴眼液组治疗总有效率为74.60%,两组间差异具有统计学意义。结论:鱼腥草滴眼液为纯中药制剂,毒副作用小,临床治疗结膜炎疗效高。     

针对春季卡他性结膜炎的联合用药疗效观察分析

目的:针对春季卡他性结膜炎使用0.1%盐酸奥洛他定滴眼液联合那素达滴眼液治疗对临床疗效予以观察分析.方法:对春季卡他性结膜炎的169例患者使用盐酸奥洛他定滴眼液进行每日两次治疗,持续时间45~90d;使用那素达滴眼液进行每天三次的治疗,治疗时间一个月.在治疗后的三天、一星期、两星期、四星期、八星期、十二星期观察疗效.结果:联合用药一个星期后有77.85%的患者结膜充血症状消失,两个星期后79.75%的患者眼痒、灼烧、流泪等症状消失,十二个星期后,总治愈率高达98.73%.结论:将盐酸奥洛他定与那素达滴眼液配合使用,有助于快速稳定、控制由春季卡他性结膜炎引起的症状及体征.     

利奈唑胺滴眼液的制备、质量控制和眼刺激性实验

目的:制备利奈唑胺滴眼液,并对其进行质量控制和眼刺激性考察。方法:以玻璃酸钠、氯化钠、泊洛沙姆407和依地酸二钠为辅料,采用新型眼用释药系统纳米分子罩系统α(NMHSα)制备利奈唑胺滴眼液,采用高效液相色谱法测定滴眼液中利奈唑胺的含量,考察滴眼液的兔眼刺激性和稳定性。结果:所制滴眼液为类白色黏稠液体,规格为10 ml∶20 mg,含药量为0.2%;利奈唑胺检测质量浓度的线性范围为0.025⁰.8 mg/ml(r=0.999 9),平均回收率为101.08%,RSD=0.71%(n=3)。该滴眼液对兔眼无刺激性,室温环境下12个月内稳定性良好。结论:本制剂制备方法简单、可行,质量可控,无眼刺激性。     

芦氟沙星滴眼液的研制及临床应用

目的 :研制芦氟沙星滴眼液。方法 :采用HPLC法测定滴眼液芦氟沙星含量 ;对150例门诊眼部重症感染患者应用该滴眼液后进行疗效观察。结果 :芦氟沙星平均回收率为100 12 % ,RSD为1 18 % (n=5) ;治疗后痊愈130例 ,有效16例 ,无效4例 ,总有效率为97 33 %。结论 :HPLC法测定含量简便、快速、准确 ,不需要特殊试剂 ;该滴眼液疗效确切     

用晶体混浊分类系统Ⅲ探讨复方水蛭滴眼液防治老年性白内障的临床研究

目的 :用晶体混浊分类系统Ⅲ (lensopacitiesclassificationsystemⅢ ,LOCSⅢ )探讨复方水蛭 (shuizhi,SZ)滴眼液对老年性白内障的防治作用。方法 :采用以民间验方为基础、以SZ为主要成分、富含锌和维生素C的复方SZ滴眼液 ,并以进口抗白内障药物吡诺克辛钠滴眼液 (吡诺克辛 )为对照组 ,应用LOCSⅢ晶体混浊分类系统观察和比较两种滴眼液对老年性白内障的防治作用。结果 :复方SZ滴眼液组视力提高率 (76 % )、晶体混浊减低率 (5 9% )、有效率 (6 6 % )均明显优于吡诺克辛滴眼液对照组(2 .0 %、0 %和 2 .0 % )。且无明显的不良反应。结论 :复方SZ滴眼液是一种安全、有效的抗白内障药物 ,疗效优于进口抗白内障药物吡诺克辛滴眼液。     

硝酸毛果芸香碱滴眼液含量测定方法比较

目的评价医院制剂室中硝酸毛果芸香碱滴眼液含量测定的三种常用方法。方法采用紫外分光光度法、旋光法、中合法对不同批号1%、2%硝酸毛果芸香碱滴眼液制剂的含量进行测定。结果测定方法不同,所测制剂含量结果有一定差异。结论三种方法均符合质量标准要求,紫外分光光度法对硝酸毛果芸香碱滴眼液含量测定的方法较为准确。     

0.2%布洛芬滴眼液的制备及临床应用

目的:制备0.2%布洛芬滴眼液,并对其稳定性、刺激性进行观察.方法:以非甾体类药物布洛芬为主药,以生理上所允许的镁盐为刺激缓冲剂.结果:0.2%布洛芬滴眼液室温(20℃)贮存期约为2年,对家兔眼睛无刺激作用;对168例患各种类型结膜炎及内眼手术后患者的临床总有效率为97.0%,未发现明显的毒副作用.结论:0.2%布洛芬滴眼液制备工艺简单、合理,临床疗效较好.     

氟康唑滴眼液的研制及质量控制

目的 :制备氟康唑滴眼液并控制其质量。方法 :采用高效液相色谱法测定滴眼液中氟康唑含量 ,依据《中国药典》对滴眼液进行质量控制。结果 :含量测定平均回收率为100 41 % ,RSD=0 54% (n=5)。结论 :该制剂处方合理 ,制备工艺简便 ,质量易于控制。     

甲磺酸培氟沙星滴眼液的研制及临床应用

:目的 :研制甲磺酸培氟沙星滴眼液。方法 :采用紫外分光光度法测定含量。对170例门诊眼部重症感染患者应用该滴眼液后进行疗效观察。结果 :线性范围为2～14μg/ml,回归方程为A=0.1018C,r=0.9999(n=7)。该方法测得平均回收率为99 64 % ,RSD为0 43 %。经治疗痊愈150例 ,有效16例 ,无效4例 ,总有效率达97 6 %。结论 :该滴眼液疗效确切 ,紫外分光光度法测定含量方法简便、快速、准确 ,不需要特殊试剂     

Biliary excretion of olsalazine sodium in humans

The biliary excretion of Olsalazine sodium (ADS) was studied by three different methods in healthy volunteers and in patients. 1 g ADS in a 2% solution was infused during 1 h into jejunum in six healthy volunteers via a three lumen sond. The bile was collected, during 2.5-6 h, proximal of an occlusive balloon on the three lumen sond. 10 mg ADS was given i.v. to five healthy volunteers and the bile was collected during 3-4.5 h with the same type of three lumen sond as used in the first experiment. 1 g ADS was given orally to three patients, with a T-tube inserted into coleducus at surgery. The bile was collected via the T-tube for 24 h. The mean biliary excretion of the jejunal dose was 0.41% (0.22% if one subject, who probably had a beckflow of the instillation fluid, is omitted). In patients, the mean excretion with bile of ADS was 0.35% and of ac-5-ASA 0.17%. Due to the short collection time after jejunal infusion and the probably incomplete collection of bile in both enteral studies the biliary excretion was estimated to be less than 2% as ADS and less than 1% as ac-5-ASA. The biliary excretion of an i.v. dose showed large individual variations (0.16-12.2%) which were not correlated to the length of the collection time. The total excretion was estimated to be less than 20% as ADS. No metabolites were detected after the i.v. dose.     

Higher anticholinergic drug scale (ADS) scores are associated with peripheral but not cognitive markers of cholinergic blockade. Cross sectional data from 21 Norwegian nursing homes

AimThis study evaluated a presumed gradual decline in cognitive function in nursing home residents when the anticholinergic drug scale (ADS) score increased above 3.MethodThe study population was recruited from 21 nursing homes in Norway. Criteria for inclusion were ADS score ≥ 3 and no severe dementia, defined as Clinical Dementia Rating (CDR) score < 3. Primary cognitive end points were CERAD 10‐word lists for recall and Mini Mental State Examination (MMSE). Secondary end points were activity of daily living (ADL), mouth dryness and serum anticholinergic activity (SAA). The patients were stratified into subgroups according to ADS score, i.e. a reference group with score 3 and test groups with scores 4, 5 or ≥6. End points were compared by analyses of covariance (ancova).ResultsOverall, 230 of the 1101 screened nursing home residents (21%) had an ADS score ≥3. After exclusion 101 residents were recruited and among these, 87 managed to participate in the study. No significant differences were detected in cognitive function or ADL when ADS increased above 3 (P > 0.10), but in vivo (mouth dryness) and in vitro (SAA) measures of peripheral anticholinergic activity were significantly higher in patients with an ADS score ≥6 (P < 0.01).ConclusionThe present study does not support a progressive decline in cognitive function with ADS score above 3. This might indicate that the ADS score model has limited potential to predict the clinical risk of central anticholinergic side effects in frail elderly patients receiving multiple anticholinergic drugs.     

Prevention of Alcohol Dependence: Strategies for Selective,Indicated, and Universal Prevention

ABSTRACT

Study of the chronology of criteria of dependence in alcohol dependence syndrome (ADS) can enable us to design strategies for the prevention for ADS, which takes into account primary prevention (indicated, selective, and universal prevention) approaches and aims at reducing the occurrence of ADS. The objective of this work is to study the age-wise and order-wise chronologies of International Classification of Diseases Tenth Revision Diagnostic Criteria for Research (ICD-10 DCR) dependence criteria in individuals with ADS. Consecutively admitted and consenting inpatients with ICD-10 DCR diagnosis of ADS were evaluated in a structured interview after detoxification using Semi-Structured Assessment for the Genetics of Alcoholism (SSAGA)-II. The total sample size was 81. The mean ages at the first onset of alcohol use, development of the first criterion, and ICD-10 dependence was 18.72 years (SD: 6.84), 24.33 years (SD: 9.21), and 27.51 years (SD: 9.28), respectively. In age-wise chronology, tolerance, loss of control, and craving were present in 97.53%, 80.24%, and 79%, respectively, of our study sample. In order-wise chronology, either craving (16%) or tolerance (71.6%) was present as the first criterion and the presence of craving (16%), tolerance (21%), or loss of control (18.5%) was observed as the first criterion in 55.5% of the subjects. Indicated prevention may be attempted by enquiring about craving, tolerance, and loss of control and use of anticraving medications or behavioral strategies. Selective prevention by using naltrexone for those genetically inclined and universal prevention by use of “clinical” labeling on alcoholic beverages can also be attempted.     

An item response analysis of the Alcohol Dependence Scale in treatment-seeking alcoholics

OBJECTIVE: In this study we use methods based on Item Response Theory to examine in depth the psychometric properties of the Alcohol Dependence Scale (ADS). In particular, we examine the ability of each ADS item to discriminate among individuals across the continuum of alcohol dependence severity and also examine the extent to which item-response options provide useful and reliable information about the level of alcohol dependence. METHOD: Participants were 166 alcohol-dependent patients with elevated depressive symptoms. We conducted a maximum likelihood common factors analysis on the ADS, and then used a nonparametric kernel smoothing method to create Item Characteristic Curves (ICC) and Option Characteristic Curves (OCC) for each ADS item. On the basis of these curves, we identified items showing at least fair discrimination and modified the scoring of response options where indicated. We then created an empirically derived ADS score and correlated it with the original ADS and with other measures of alcohol involvement. RESULTS: Replicating previous studies, our results indicated a primarily unidimensional factor structure. A total of 12 of the 25 ADS items showed good discrimination, and examination of the OCC indicated that dichotomous scoring was most appropriate for these items. This 12-item abbreviation of the ADS was highly correlated with the original scale (r = 0.91), and showed similar patterns of correlations with other measures of alcohol involvement. CONCLUSIONS: Results suggest potential gains in measurement efficiency using methods based on Item Response Theory and indicate potential ordering of dependence symptoms based on item severities.     

九节龙皂苷Ⅰ聚合物载药胶束的制备及体外表征

目的制备九节龙皂苷Ⅰ普朗尼克F127载药胶束。方法采用成膜-水化法制备该胶束体系,通过正交实验优化处方,用透射电镜和激光粒子测定仪对胶束的粒径分布和形态进行表征,用透析法考察体外释药特征。结果最优处方制备的九节龙皂苷Ⅰ普朗尼克F127载药胶束的粒径为18.74nm,外观呈圆球形,包封率大于90%,较九节龙皂苷Ⅰ(ADS-Ⅰ)纯药具有显著的缓释效果。结论九节龙皂苷Ⅰ普朗尼克F127载药胶束的粒径小,包封率高,可显著增加所载药物的溶解性,且具有显著缓释作用,是1种具有应用前景的抗肿瘤药物给药系统。     

穿心莲内酯磺化物体外抗流感病毒药效学研究

目的探讨穿心莲内酯磺化物（andrographolide sulfonated,ADS）体外对甲型流感病毒H1N1、H3N2以及乙型流感病毒（B）的抑制作用及最佳浓度。方法采用细胞病变观察法（CPE）、四甲基偶氮唑蓝（MTT）比色法,观察药物对狗肾传代细胞（MDCK）的毒性作用,计算半数有毒浓度（TC50）和最大无毒浓度（TC0）;3种流感病毒分别接种于MDCK,观察不同浓度的药物对病毒致CPE的影响,测定药物对病毒的增殖抑制率,Probit回归法计算药物的半数有效浓度（EC50）和治疗指数（TI）;红细胞血凝素滴定法测定ADS对流感病毒血凝素抑制作用。结果 CPE、MTT法测得ADS对MDCK的TC0≤0.781 3 mg.mL-1,TC50为2.280 8 mg.mL-1。ADS对H1N1、H3N2、B流感病毒的EC50分别为0.072 6、0.152 7、0.158 5 mg.mL-1,TI分别为31.42、14.93、14.39,此外ADS对不同流感病毒血凝素抑制作用,最低抑制浓度分别为0.048 9、0.097 8、0.097 8 mg.mL-1,且呈现出量效关系。结论 ADS体外抗H1N1、H3N2以及B型流感病毒感染作用,可能是通过药物抑制流感病毒表面的血凝素的活性而实现的。     

Additive effects of lithium and antidepressants in the forced swimming test: further evidence for involvement of the serotoninergic system

In the mouse forced swimming test (FST) pretreatment with a subactive dose of lithium (1 mEq/kg), given IP 45 min before the test, facilitated the antidepressant activity of iprindole, fluoxetine, and moclobemide (given IP 30 min before the test). These antidepressants (ADS) were not active alone in the FST in this study. Moreover, when subactive lithium was combined with a wide range of ADS, each given at subactive doses, those ADS with serotoninergic properties (e.g. imipramine, citalopram, paroxetine, fluoxetine, trazodone, mianserin, and moclobemide) significantly reduced immobility times. ADS acting primarily on noradrenaline (NA) or dopamine (DA) systems (desipramine, maprotiline, viloxazine, and bupropion) did not significantly decrease immobility when given in combination with lithium. This was also the case for RO 16 6491 [a reversible, B specific monoamine oxidase inhibitor (MAOI)], nialamide, and pargyline (both irreversible, mixed MAOIs). The anti-immobility effect of iprindole in combination with lithium suggests either a direct or indirect action on the serotonin (5HT) system by this ADS whose mechanism of action remains obscure. These results, using an animal behavioral model of depression and combining our present knowledge of the acute action of various ADS, support the hypothesis that the potentiation by lithium of ADS is via direct 5HT mechanisms,indirectly via a NA/5HT link, and/or by second messenger systems. Lithium may also facilitate the expression of antidepressant activity of ADS not active by themselves in the FST.     

The Anticholinergic Drug Scale as a measure of drug-related anticholinergic burden: associations with serum anticholinergic activity

Anticholinergic Drug Scale (ADS) scores were previously associated with serum anticholinergic activity (SAA) in a pilot study. To replicate these results, the association between ADS scores and SAA was determined using simple linear regression in subjects from a study of delirium in 201 long-term care facility residents who were not included in the pilot study. Simple and multiple linear regression models were then used to determine whether the ADS could be modified to more effectively predict SAA in all 297 subjects. In the replication analysis, ADS scores were significantly associated with SAA (R2 = .0947, P < .0001). In the modification analysis, each model significantly predicted SAA, including ADS scores (R2 = .0741, P < .0001). The modifications examined did not appear useful in optimizing the ADS. This study replicated findings on the association of the ADS with SAA. Future work will determine whether the ADS is clinically useful for preventing anticholinergic adverse effects.     

Item functioning of the alcohol dependence scale in a high-risk sample

We conducted in-depth analyses of the functioning of items from the alcohol dependence scale (ADS) in a sample of high-risk alcohol drinkers, specifically 101 men and 93 women mandated to a domestic violence intervention program. We first conducted a maximum likelihood common factors analysis on the ADS, which indicated a primarily unidimensional factor structure. We then used a nonparametric kernel smoothing method to create item characteristic curves (ICC) and option characteristic curves (OCC) for each ADS item. Based on these curves, we identified nine of the 25 ADS items as reliably discriminating between those with no or minimal alcohol problems and those with symptoms of excessive or abusive drinking. Dichotomous scoring appeared most appropriate for these items. No differential item functioning (DIF) by gender was detected, indicating that these items assess alcohol problems similarly in both men and women. This nine-item empirically-derived abbreviation of the ADS appeared to be an efficient and effective measure in this sample; it was highly correlated with the original scale (r(s)=0.96) yet had superior distributional properties. Retained items reflected primarily excessive or hazardous drinking rather than alcohol dependence per se, suggesting that items targeting these types of symptoms may be most useful in high-risk samples. Combined with previous work with the ADS in treatment-seeking alcoholics, mapping of ADS item severities suggests a continuum of alcohol problem severity from heavy drinking to severe withdrawal that may be reliably tapped with dichotomous items.