Solid State Characterization of Domperidone: Hydroxypropyl-��-Cyclodextrin Inclusion Complex

The purpose of the present study was to prepare inclusion complex of domperidone with hydroxylpropyl-β-cyclodextrin in order improved the solubility and hence to increase dissolution of domperidone. An effect of concentration of hydroxylpropyl-β-cyclodextrin on the aqueous solubility of domperidone was determined by phase-solubility method. The aqueous solubility of domperidone increased as a function of hydroxylpropyl-β-cyclodextrin concentration, showing AL type diagram. Solid domperidone/hydroxylpropyl-β-cyclodextrin complex was prepared in ratio 1:1 by ultrasonication and kneading method. Solid state inclusion complex was characterized by FTIR, powder X-ray diffraction and differential-scanning calorimetry techniques. FTIR studies showed intactness of drug in complex whereas powder diffraction studies showed that hydroxylpropyl-β-cyclodextrin complex was amorphous. Solubility studies showed that complexation increased domperidone solubility as compared to pure drug in 0.1M hydrochloric acid and distilled water. Drug content confirms that ultrasonication is one of the efficient methods to prepare inclusion complex. Dissolution data of inclusion complexes also indicated that there is 1.4 folds increase in dissolution as compared to pure drug and was observed in case of inclusion complexes prepared by ultrasonication.     

多潘立酮片在健康男性受试者中的生物等效性研究

目的：研究多潘立酮片在健康男性受试者中的相对生物利用度,评价两种多潘立酮片剂的生物等效性。方法：18名男性健康志愿者随机交叉、单剂量口服试验制剂多潘立酮片和参比制剂多潘立酮片,剂量为20mg,用LC—MS法检测多潘立酮的血药浓度。利用DAS Ver2．0进行药动学参数计算和统计分析。结果：试验制剂和参比制剂主要药代动力学参数Cmax分别为（36±8）和（38±9）μg／L,tmax分别为（0．6±0．2）和（0．7±0．3）h,t1/2分别为（10±8）和（9±3）h,AUC0-24分别为（138±34）和（144±31）μg·L^-1·h,AUC0-∞分别为（168±68）和（166±37）μg·L^-1·h.多潘立酮片试验制剂相对于参比制剂的相对生物利用度F（以AUC0-24作为评价依据）为：（97±20）％。结论：两种多潘立酮片剂在健康人体中具有生物等效性。     

多潘立酮缓解消化不良症状的疗效观察

目的 探讨多潘立酮对缓解消化不良症状的效果及安全性.方法 选择2010年12月～2012年12月在本医务室治疗的消化不良症状患者80例,给予多潘立酮10 mg,3次/d,餐前15～30 min服用,持续2周,于治疗1、2周时进行消化不良症状评分,记录不良反应.结果 患者就诊时的临床症状积分为（14.32±6.51）分,治疗1周后的临床症状积分为（5.69±4.75）分,治疗2周后的临床症状积分为（1.83±0.95）分;治疗1周后的显效率为26.25％（21/80）,治疗2周后的显效率为67.50％（54/80）,治疗2周后的总有效率为93.75％（75/80）;上腹胀发生率最高,为88.75％（71/80）,且以中、重度居多,其次为嗳气,占62.50％（50/80）,以轻、中度居多,其次分别为早饱、上腹痛、食欲不振、恶心、呕吐,均以轻度居多;患者主要临床症状消失时间为4～8 d,恶心、呕吐为4d,其余依次为食欲不振、上腹痛、早饱、嗳气、上腹胀;共出现不良反应2例,占2.50％,其中不良事件1例.结论 多潘立酮能有效改善消化不良症状,治疗有效率高,且安全性良好,值得临床推广.     

香砂六君丸治疗糖尿病胃轻瘫随机平行对照研究

[目的]观察香砂六君丸治疗糖尿病胃轻瘫疗效。[方法]使用随机平行对照方法,将100例住院患者按随机数字表法分为两组。对照组50例多潘立酮,10mg/次,3次/d,口服。治疗组50例香砂六君丸,4.5g/次,3次/d,口服。连续治疗7d为1疗程。观测临床症状、中医证候积分、不良反应。连续治疗4疗程,判定疗效。[结果]治疗组痊愈10例,显效14例,有效23例,无效3例,总有效率94.00%。对照组痊愈5例,显效12例,有效20例,无效13例,总有效率74.00%。治疗组疗效优于对照组(P0.05)。中医证候积分两组均有改善(P0.05),治疗组改善优于对照组(P0.05)。[结论]香砂六君丸治疗糖尿病胃轻瘫效果显著,值得推广。     

十三味和中丸治疗老年肝胃不和型功能性消化不良疗效观察

目的:观察十三味和中丸治疗老年肝胃不和型功能性消化不良(Functional DyspepsiaFD)的临床疗效。方法:将60例符合纳入标准的FD患者随机分为治疗组与对照组。治疗组给予十三味和中丸治疗,对照组给予多潘立酮治疗。疗程4周,观察4周后患者主要症状、证候疗效及钡条胃排空率。结果:2组内患者治疗前后主要症状、钡条胃排空率比较,差异均有统计学意义(P<0.05);2组间患者治疗后上腹部疼痛、烧灼感等症状及证候积分总有效率改善优于对照组,差异有统计学意义(P<0.05),钡条胃排空率比较,疗效相当,差异无统计学意义(P>0.05);且未见不良反应。结论:十三味和中丸治疗老年肝胃不和型FD安全有效,值得临床推广。     

多潘立酮联合复方消化酶治疗功能性消化不良的临床疗效

目的：分析功能性消化不良实施药物联合治疗的效果。方法随机选取该院2015年1—12月收治的80例功能性消化不良患者作为研究对象,随机分为两组,对照组（多潘立酮治疗)、试验组（多潘立酮+复方消化酶治疗)各40例。观察临床疗效,比较症状积分和改善时间。结果试验组治疗有效38例（95.0%),高于对照组的32例（80.0%);试验组治疗后症状积分、改善时间为(3.5±1.4)min、(5.4±1.2)d,对照组为(6.0±1.8)min、(7.6±1.5)d。 P﹤0.05,差异有统计学意义。结论多潘立酮、复方消化酶联合治疗功能性消化不良疗效确切,有利于改善临床症状,值得推广。     

Domperidone improves gallbladder emptying function in patients with irritable bowel syndrome

AIM: To investigate the pathogenesis of abnormal gallbladder (GB) emptying and the effect of domperidone (Dom) on GB emptying in patients with irritable bowel syndrome (IBS). METHODS: The effects of DOM on GB emptying were studied in 20 IBS patients and 18 healthy controls by real time ultrasonography, using randomized, double-blind, and controlled methods. RESULTS: Fasting GB volume was significantly higher in IBS patients than in controls (24.136 ± 1.38 cm³vs 19.793 ± 1.487 cm³, x^-± s_x-, p < 0.01). In controls, 30 min after 10 mg Dom orally, the GB ejection fraction (GBEF) was decreased significantly (p < 0.005), and the magnitude of this decrease was greater after 20 mg Dom. The difference between these two doses was not significant (p > 0.05). In IBS patients, GBEF was significantly increased 15 min after 10 mg Dom orally (p < 0.01), and the magnitude of this increase was greater with 20 mg Dom (p < 0.001). This difference was even more marked with prolongation of time after oral Dom. The GBEF in IBS patients with segmental contraction was significantly less than that with hypermotility (p < 0.01), and the increase of GBEF was more marked after oral Dom in IBS patients with segmental contraction than those with hypermotility (p < 0.01). CONCLUSION: GB emptying function is abnormal in patients with IBS. The feeble contractility of the GB and/or the incomplete relaxation of Oddi sphincter may be factors that directly affect GB emptying in IBS patients. Dom can significantly improve GB emptying function and may decrease the risk of forming GB stones in these patients.     

多潘立酮治疗功能性消化不良的临床观察

目的　观察多潘立酮对功能性消化不良 (FD)的疗效及安全性。方法　 70例 FD患者随机分为治疗组36例 ,对照组 34例。治疗组予多潘立酮 (西安杨森制药有限公司生产 ) 1 0 mg,3次 / d,对照组予胃复安 1 0 m g,3次 / d,每月为 1疗程。治疗中每周门诊复诊 1次 ,记录上腹痛、饱胀、嗳气、恶心、呕吐、纳差 6大症状变化及不良反应。结果　有效率 :治疗组为 80 .6 % ,对照组为 5 8.8% ,差异有显著性 (P<0 .0 5 )。不良反应的发生率 :治疗组为 5 .6 % ,对照组为2 6 .5 % ,差异有显著性 (P<0 .0 5 )。复发率 :治疗组为 1 6 .1 % ,对照组 32 .0 % ,差异无显著性 (P>0 .0 5 )。结论　多潘立酮治疗 FD安全有效 ,依从性好 ,无严重不良反应     

多潘立酮口腔崩解片的制备及质量控制

目的：制备多潘立酮口腔崩解片并对其崩解时限、溶出度、有关物质和含量进行测定。方法：采用直接压片法制备,紫外分光光度法测定其溶出度和含量,HPLC法测定其有关物质。结果：制备的多潘立酮口腔崩解片崩解时间不超过30s,标示含量达到99．45％以上,有关物质在0．10％以下,5min内溶出93％以上。结论：多潘立酮口腔崩解片制备过程简单,质量可控,适用于工业大生产。     

吗丁啉预防化疗所致呕吐的临床研究

 吗丁啉为多巴胺－D2受体阻滞剂，极少中枢神经系统副作用。我们以口服负荷量加舌下含化维持量吗丁啉作为化疗呕吐的预防剂，对含中剂量DDP（40mg×3天）化疗方案呕吐的完全控制率为74.3%，对不含DDP化疗方案的呕吐完全控制率为81.8%，同期枢复宁对合中剂量DDP（40mg×3天）化疗方案的呕吐完全控制率为74.0%。本研究表明，吗丁啉预防化疗呕吐有效，无明显毒副作用，价廉，用法简便，值得进一步研究。