蒲地蓝消炎口服液联合利巴韦林泡腾颗粒治疗手足口病普通型的疗效观察

目的探讨蒲地蓝消炎口服液联合利巴韦林泡腾颗粒治疗儿童手足口病普通型的临床疗效。方法 150例手足口病普通型患儿随机分为治疗组和对照组,治疗组应用蒲地蓝消炎口服液及利巴韦林泡腾颗粒治疗,对照组采用利巴韦林泡腾颗粒治疗。结果观察两组临床症状及体征改善时间,治疗组热退时间、疱疹结痂及消退时间、开始进食时间、痊愈天数均明显短于对照组(t=21.64、44.56、13.52、3.263、8.71,P<0.05或P<0.01);治疗组总有效率亦高于对照组(χ2=5.95,P<0.05),差异具有统计学意义。结论蒲地蓝消炎口服液联合利巴韦林治疗手足口病普通型疗效确切,值得推广应用。     

复方珍珠粉泡腾颗粒处方筛选及溶出度考察

目的:筛选复方珍珠粉泡腾颗粒处方并考察其在不同介质中的体外溶出度。方法:以乙二胺四乙酸消耗量为指标,兼顾发泡高度和pH值,用均匀设计法筛选处方中无水柠檬酸、碳酸氢钠、乳糖的量;考察并比较复方珍珠粉泡腾颗粒、自制碳酸钙片、自制珍珠粉片中碳酸钙在蒸馏水和盐酸中的溶出度。结果:处方中无水柠檬酸、碳酸氢钠、乳糖的量分别为10.0、2.5、5.0g;3种制剂间的溶出度有明显差异。结论:制备的复方珍珠粉泡腾颗粒释药速度快、药物溶出完全,溶液呈酸性,适合特定人群使用。     

乙酰半胱氨酸泡腾片合用噻托溴铵吸入剂对50例COPD合并肺气肿的临床疗效研究

目的：观察和评估乙酰半胱氨酸泡腾片合用噻托溴铵吸入剂对COPD合并肺气肿患者的肺功能和临床症状的影响。方法：随机选取我院2013年2月—2014年12月收治的COPD合并肺气肿患者共100例,按治疗方式分为观察组和对照组,观察组用乙酰半胱氨酸泡腾片联合噻托溴铵吸入剂治疗,对照组单纯口服乙酰半胱氨酸泡腾片治疗。对两组患者CRP及IL-18水平,肺功能指标以及临床症状评分,SGRQ的症状分,活动分,影响分的分值等指标进行对比分析。结果：观察组患者CRP及IL-18水平,临床症状评分, SGRQ的症状分,活动分,影响分的分值明显低于对照组(P<0.01);观察组肺功能指标明显优于对照组(P<0.01)。结论：采用乙酰半胱氨酸泡腾片合用噻托溴铵吸入剂临床疗效显著,具有一定的抗炎作用,可以明显降低COPD合并肺气肿患者的CRP及IL-18水平,有效改善患者的肺功能和临床症状,提高患者的生活质量。     

黄芪颗粒治疗复发性阿弗他溃疡的远期疗效观察

目的:评价黄芪颗粒治疗复发性阿弗他溃疡的远期疗效和安全性.方法:将80例复发性阿弗他溃疡患者随机分为治疗组和对照组,每组各40例.治疗组在常规药物消炎止痛治疗的基础上再给予口服黄芪颗粒3个月;对照组仅给予常规药物消炎止痛治疗.治疗组在口服黄芪颗粒3个月后与对照组一同进行为期6个月的疗效跟踪评定.结果:治疗组6个月内的溃疡复发次数、溃疡总数、溃疡平均愈合天数分别为(6.71±2.58)次、(10.09±2.92)个、(4.94±1.63)d,均优于对照组[(13.53±5.77)次、(27.97±8.14)个、(12.35±4.28 d)],差异有统计学意义(P<0.05).未发现治疗组有任何毒副作用.结论:黄芪颗粒治疗复发性阿弗他溃疡具有远期疗效肯定、使用方便、安全性高等优点,值得在临床上推广应用.     

碳酸钙泡腾颗粒的人体生物利用度研究

目的：评价碳酸钙泡腾颗粒的人体生物利用度。方法：以原子吸收光谱法测定１０名健康志愿者口服碳酸钙泡腾颗粒与进口碳酸钙片后的尿钙浓度，以尿钙总排泄量与尿钙增量为指标评价两种制剂吸收差异。结果：口服１．２ｇ碳酸钙泡腾颗粒与碳酸钙片后４ｈ尿钙总排泄量分别为０．１４３ｍｇ·（ｍｇＣｒ）－１与０．１０９ｍｇ·（ｍｇＣｒ）－１；尿钙增量分别为０．０５１ｍｇ·（ｍｇＣｒ）－１与０．０３１ｍｇ·（ｍｇＣｒ）－１，前者均显著高于后者（Ｐ＜０．０５和Ｐ＜０．０１）。结论：碳酸钙泡腾颗粒的口服生物利用度高于碳酸钙片。     

康妇炎胶囊联合甲硝唑阴道泡腾片治疗细菌性阴道病180例疗效观察

目的：观察康妇炎胶囊联合甲硝唑阴道泡腾片治疗细菌性阴道病临床疗效。方法将180例患者随机分为两组,对照组单纯使用甲硝唑阴道泡腾片阴道放药治疗。治疗组在上述治疗基础上同时给予康妇炎胶囊口服,对两组治疗结果进行疗效观察。结果对照组和治疗组治愈率分别为：78%、100%,差异有统计学意义（P〈0.05）。结论采用康妇炎胶囊联合甲硝唑阴道泡腾片治疗细菌性阴道病,增强疗效,防止复发、简便易行。     

Process to manufacture effervescent tablets: air forced oven melt granulation

In the present study we apply melt granulation in an air forced oven, called "are forced oven melt granulation" to the single-stage manufacture of effervescent granules consisting of anhydrous citric acid (43.2%) and sodium bicarbonate (56.8%) in order to make tablets. This study established that process parameters such as concentration of PEG 6000, residence time in the air forced oven, fineness of PEG 6000, fineness of the initial effervescent mix and efficiency of two lubricants markedly influenced several granule and tablet characteristics. The granules ready to be compressed into tablets were stable for 7 days at 60% RH/18 degrees C. It is a dry, simple, rapid, effective, economical, reproducible process particularly well suited to the manufacture of effervescent granules which are easily compressed into effervescent tablets. Of all the formulations tested, only formulations B2 and E2 melt granulated for 30 minutes gave tablets which had optimum compression characteristics without processing problems during compression.     

Systemic Availability of Acetylsalicylic Acid in Human Subjects after Oral Ingestion of Three Different Formulations

Abstract: Systemic availability of acetylsalicylic acid (ASA) in normal human subjects after oral ingestion of 1 g in three different formulations was determined by using high-pressure liquid chromatography for ASA assay. For an effervescent, a plain and a sustained release preparation systemic availabilities expressed in percent of the ingested dose were 16.9±3.2, 8.6±1.2 and 2.6±0.4%, respectively. All subjects had clearly measureable amounts of ASA in plasma after oral intake of a sustained release preparation with an average peak concentration of 15 μmol/1. Peak concentration after an effervescent and plain formulation was on the average 80 and 40 μmol/1, respectively. Half-life of ASA in plasma was 18.1±1.2 min. for the effervescent and 28.7±5.3 min. for the plain preparation, while the elimination phase was too ill defined for the sustained release formulation. Average plasma half-life of salicylic acid (SA) was similar after the three different administration forms with values between 3.0 and 3.7 hrs. Further, no difference in SA distribution volumes or amounts of SA absorbed was found. The present study demonstrates that oral ingestion of ASA in effervescent, plain and sustained release formulations gives rise to significant amounts of ASA in plasma. Concentrations found indicate that long-term antithrombotic therapy with ASA in a sustained release formulation may be possible.     

Effect of Sodium Acid Pyrophosphate on Ranitidine Bioavailability and Gastrointestinal Transit Time

During development of a ranitidine effervescent oral solution dosage form, a marked decrease was observed in the extent of ranitidine absorption relative to the conventional oral tablet. Two studies were conducted in healthy volunteers to confirm the involvement of an excipient, SAPP (sodium acid pyrophosphate), and the mechanism of interaction, altered gastrointestinal transit. The first study (n = 12) involved single-dose crossover comparisons of (A) 150 mg ranitidine with 1132 mg SAPP versus (B) 150 mg ranitidine and (C) 150 mg ranitidine with all the effervescent tablet excipients except SAPP versus (D) a 150-mg ranitidine effervescent tablet, all administered as oral solutions. Serum ranitidine AUC, C _max, and t _max were compared using two one-sided t test 90% confidence intervals (CI). Comparing treatments A to B and D to C, all 90% CI were below the 80–120% range, indicating significantly less extensive ranitidine absorption (54% based on AUC) from the oral solutions containing SAPP. The second study (n = 12) was a single-dose crossover comparing 50 µCi ¹¹¹InCl solutions with and without 1132 mg SAPP. Gastrointestinal transit times, determined by scintigraphic imaging, were compared between treatments. Gastric emptying time was unchanged, but small intestinal transit time was decreased to 56% in the presence of SAPP. More rapid small intestinal transit associated with an excipient of a solution dosage form apparently resulted in a decreased extent of ranitidine absorption. This observation contradicts the conventional wisdom that oral solutions are unlikely to fall short of bioequivalence relative to solid oral formulations.     

Bioequivalence and bioavailability after single administration of effervescent ranitidine tablets]

An open two-way cross-over study in 12 healthy male volunteers was performed in order to determine the relative bioavailability of a 150 mg ranitidine (Zantic, CAS 66357-35-5) effervescent tablet sweetened with saccharine in comparison to the 150 mg standard ranitidine dispersible tablet (Trinkette). On two occasions separated by a wash-out period of 1 week volunteers received a single oral dose of both formulations. On each administration day blood samples were collected at predetermined time points in order to investigate the pharmacokinetic parameters. Single oral doses of ranitidine were very well tolerated by healthy male volunteers. The non-parametric 95% confidence intervals for AUC and Cmax were 87 to 116% and 84 to 107%, respectively. The relative bioavailability of the ranitidine effervescent tablet was 99% compared to the dispersible tablet. The mean of the Cmax ratio was 95%. The ranitidine effervescent tablet could thus be claimed to be bioequivalent to the dispersible tablet.     

舒利通颗粒的镇痛抗炎作用研究

目的:研究舒利通颗粒的镇痛抗炎作用。方法:采用醋酸建立小鼠疼痛扭体模型;采用二甲苯致小鼠耳廓肿胀和大鼠棉球肉芽肿形成模型;分别观察舒利通颗粒的镇痛及抗炎作用。结果:舒利通颗粒可显著降低小鼠扭体反应次数(P<0.01);减轻小鼠耳廓肿胀(P<0.05);减少大鼠肉芽肿形成(P<0.01)。结论:舒利通颗粒对疼痛和炎症具有明显的镇痛和抗炎作用。     

菌毒清颗粒镇痛、抗炎作用研究

目的:探讨菌毒清颗粒的镇痛、抗炎作用。方法:采用醋酸扭体、热板法观察菌毒清的镇痛作用,采用毛细血管通透性及耳廓肿胀实验研究其抗炎作用。结果:菌毒清低、中、高剂量组小鼠出现扭体反应的次数均明显减少(P<0.01);菌毒清中、高剂量组均能降低小鼠腹腔毛细血管通透性(P<0.05或0.01);菌毒清中、高剂量组均能减轻小鼠耳廓肿胀度(P<0.01);但对热板至痛小鼠无明显影响。结论:菌毒清具有明显的镇痛抗炎作用。     

盐酸雷尼替丁泡腾颗粒剂的血药浓度的测定及其药物动力学的研究

目的 :测定 10个男性健康者 11个时间点盐酸雷尼替丁泡腾颗粒剂的血药浓度及其药物动力学参数。方法 :10名男性健康志愿者口服盐酸雷尼替丁泡腾颗粒剂 ,采用HPLC法测定人血清中药物浓度并进行其药物动力学的研究。以ALLTIMAC18为固定相 ,0 .0 2mol·L 1磷酸二氢钾溶液 甲醇 (70 :30 )为流动相 ,检测波长为 32 0nm。结果 :泡腾颗粒剂血药浓度曲线均符合二室模型。其主要药物动力学参数 :Tpeak为 (1.96± 0 .5 5 )h ,Cmax为 (6 6 5± 2 13) μg·L 1,AUC为 (345 2± 6 0 1)h·μg·L 1。结论 :结果表明本法提取简便 ,灵敏度高 ,准确度高     

槐角颗粒的主要药效学研究

目的观察槐角颗粒的主要药理作用.方法采用断尾凝血法、体外凝血法、扭体法、热板致痛法、耳廓肿胀法、腹腔毛细血管通透性观察法、棉球肉芽肿法、体内外抑菌试验等方法.结果槐角颗粒可明显缩短小鼠断尾后的出血时间及血管内凝血时间;对抗0.6%冰醋酸所致小鼠的扭体次数增加,提高小鼠的痛阈值;抑制致炎液所致小鼠耳廓的肿胀度;抑制冰醋酸所致小鼠腹腔毛细血管通透性的增加;抑制大鼠棉球肉芽肿的增长;并具有明显的抑菌作用.结论槐角颗粒与原丸剂型一样具有明显的止血、凝血及镇痛、抗炎、抗菌等药理作用.     

夏莲颗粒剂抗甲状腺肿作用的实验研究

要目的：探讨夏莲颗粒剂的抗炎及对甲状腺肿的拮抗作用。方法：采用大鼠角叉菜胶性足趾肿胀和棉球植入法致炎症模型，观测药物的抗炎作用；以甲巯咪唑诱发大鼠甲状腺肿为模型，观测药物抗甲状腺肿的作用。结果：夏莲颗粒剂不仅能明显减轻急、慢性炎症反应，且对甲状腺肿有明显的抑制作用。结论：夏莲颗粒剂具有明显的抗炎及抗甲状腺肿的作用。     

The dental implications of chronic use of acidic medicines in medically compromised children

Objective: Liquid oral medicines form a significant proportion (11%) of the medicines used by the population as a whole, either prescribed or over the counter. The active agent, as well as some of the other ingredients, can pose a threat to oral health. Method: Eight liquid oral medicines and two effervescent preparations routinely prescribed for longterm use by paediatric renal patients were assessed for titratable acidity and pH values. Results: All of the medicines tested were acidic and the majority were well below the critical pH of 5.5 at which enamel demineralisation takes place. The titratable acidity values, at a pH of 6.7, ranged between 0.01 and 1.54 for the liquid preparations but were 8.4 and 10.6 for the two effervescent tablets tested. Conclusion: Surplus acid in effervescent preparations while ensuring palatability of medicines and thus compliance, may produce unwanted dental side effects in children who are already medically compromised.     

清肺消咳颗粒抑菌、抗炎作用的研究

目的研究清肺消咳颗粒的体内外抑菌与抗炎作用.方法采用体外抗菌及病原菌感染小鼠造模,评价清肺消咳颗粒的抑菌作用;采用二甲苯致小鼠耳廓肿胀、大鼠棉球肉芽肿与角叉菜胶致大鼠足跖肿胀等炎性模型,研究清肺消咳颗粒的抗炎作用.结果清肺消咳颗粒对肺炎双球菌、甲/乙型溶血性链球菌、金黄色葡萄球菌均有较明显的抑制或灭活作用,对大肠杆菌和绿脓杆菌的抑制作用较弱,对肺炎双球菌感染小鼠的死亡保护率分别为40%,35%,10%,生命延长率为57.14%,45.45%,14.29%;清肺消咳颗粒可显著抑制二甲苯致小鼠耳廓肿胀、大鼠棉球致肉芽组织增生和大鼠足跖肿胀并明显减少炎症组织内PGE2含量.结论清肺消咳颗粒具有较好的体内、外抑菌与抗炎作用.     

盐酸多奈哌齐口崩片的处方优选及稳定性研究

目的:优选盐酸多奈哌齐口崩片处方并考察其稳定性。方法:采用正交试验确定最佳处方,并与普通薄膜衣片进行体外溶出度比较。在不同条件下留样进行稳定性研究。结果:筛选后最佳处方为崩解剂用量10%、填充剂用量20%、泡腾剂用量5%,所制制剂崩解迅速,几乎在30s内崩解完全,并能通过内径为710μm的筛,其溶出速度快于普通片剂,稳定性均合格。结论:所得口崩片质量稳定,有效期定为2y。     

The effect of metoclopramide on the absorption of effervescent aspirin in migraine.

1 The absorption of effervescent aspirin was studied in two groups of patients during attacks of migraine. The first group received effervescent aspirin alone whilst the second group received intramuscular metoclopramide before effervescent aspirin. 2 After effervescent aspirin alone there was significant impairment in the rate of aspirin absorption during migraine attacks compared with the rate of aspirin absorption in normal volunteers and in the same patients when headache-free. 3 When metoclopramide was given before effervescent aspirin the rate of aspirin absorption during migraine attacks was not significantly different from that obtained in normal volunteers given effervescent aspirin alone or from that obtained in the patients themselves when given both metoclopramide and effervescent aspirin when headache-free. 4 It is concluded that the impairment of absorption of effervescent aspirin during migraine attacks is related to impaired gastro-intestinal motility with delayed gastric emptying and that this impaired motility can be overcome by parenteral metoclopramide.     

Pharmacology of benzydamine

Benzydamine is a topical anti-inflammatory drug which is widely available and used topically for the treatment of the mouth. It is also used as a gel for application to inflamed joints. It has physicochemical properties and pharmacological activities which differ markedly from those of the aspirin-line non-steroidal anti-inflammatory drugs. Benzydamine is a weak base unlike the aspirin-like drugs which are acids or metabolized to acids. A major contrast with the aspirin-like drugs is that benzydamine is a weak inhibitor of the synthesis of prostaglandins but it has several properties which may contribute to its anti-inflammatory activity. These properties include inhibition of the synthesis of the inflammatory cytokine, tumour necrosis factor-α (EC₅₀, 25 μmol/L). Inhibition of the oxidative burst of neutrophils occurs under some conditions at concentrations of 30 to 100 μmol/L, concentrations which may be produced within oral tissues after local application. A further activity of benzydamine is a general activity known as membrane stabilization which is demonstrated by several actions including inhibition of granule release from neutrophils at concentrations ranging from 3 to 30 μmol/L and stabilization of lysosomes. Lack of knowledge of the tissue concentrations of benzydamine limit the correlation between pharmacological activities in vitro and in vivo. The concentration of benzydamine in the mouthwash is 4 mmol/L but the concentrations in oral tissues have not been studied adequately. Limited data in the rat indicates that concentrations of benzydamine in oral tissues are approximately 100 μmol/L.