Single and Dual Drug Release Patterns from Shellac Wax-Lutrol Matrix Tablets Fabricated with Fusion and Molding Techniques

The objective of this investigation was to prepare the shellac wax matrix tablets by fusion and molding technique incorporated with Lutrol in different ratios to modify the hydrophobicity of matrix tablet. The matrix tablets with single drug were loaded either with propranolol hydrochloride or hydrochlorothiazide as hydrophilic and hydrophobic model drugs, and a dual drug formula was also prepared. The single and dual drug release patterns were studied in a dissolution apparatus using distilled water as medium. Propranolol hydrochloride released from matrix was easier than hydrochlorothiazide. Drug release from shellac wax matrix could be enhanced by incorporation of Lutrol. However retardation of drug release from some matrix tablets was evident for the systems that could form dispersion in the dissolution medium. The gel network from high content of Lutrol was hexagonal which was a dense and more compact structure than the other structures found when low amounts of Lutrol were present in the formula. Therefore, the formulae with high content of Lutrol could prolong drug release more efficiently than those containing low content of Lutrol. Hence shellac wax matrix could modulate the drug release with the addition of Lutrol. Sustainable dual drug release was also obtained from these developed matrix tablets. Thus shellac wax-Lutrol component could be used as a potential matrix tablet prepared with fusion and molding technique with excellent controlled drug release.     

桑生除痹合剂治疗增生性脊柱炎临床研究

目的：观察桑生除痹合剂治疗增生性脊柱炎的临床疗效。方法：将228例患者按随机数字表法随机分为治疗组120例和对照组108例,治疗组采用桑生除痹合剂治疗,对照组采用抗骨增生片治疗,1个月为1个疗程,治疗1个疗程后判定临床疗效。结果：治疗组有效率为91.7%,对照组有效率为71.3%,两组比较有极显著性差异（P〈0.01）。结论：桑生除痹合剂治疗增生性脊柱炎有较好的临床疗效。     

8.5%甲嘧·高氯氟泡腾片及其应用研究

目的研究8.5%甲嘧·高氯氟卫生杀虫泡腾片剂的加工工艺、药效及其质量控制。方法选用广谱性的杀虫有效成分甲基嘧啶磷和高效氯氟氰菊酯混配组成,计量后压片。结果研制了8.5%甲嘧.高氯氟卫生杀虫泡腾片,适用于背负式、手动储压式、机动喷雾器、水雾机,可广泛用于宾馆、饭店等有卫生要求的场所防治蚊蝇和蟑螂等害虫,1L水加2片。结论 8.5%甲嘧·高氯氟卫生杀虫泡腾片剂作为一种新剂型具有高效、便捷、量化的特点。     

二甲双胍联合炔雌醇环丙孕酮片对多囊卵巢综合征患者性激素和胰岛素水平的影响

目的:研究二甲双胍联合炔雌醇环丙孕酮片对多囊卵巢综合征(Polycystic ovarian syndrome,PCOS)患者性激素和胰岛素水平的影响。方法:选取2018年3月至2019年10月于我院就诊的PCOS患者135例,按照随机数字表法分为两组,对照组患者67例予以炔雌醇环丙孕酮片(每天1片)口服,研究组68例在对照组的基础上增加二甲双胍(每天0.85 g)口服。治疗3个疗程后,观察两组患者临床疗效、性激素水平、胰岛素水平、自然受孕率、不良反应。结果:研究组患者治疗后的临床有效率、受孕率明显高于对照组(P<0.05)。治疗后研究组黄体生成素(Luteinizing hrmone,LH)、睾酮(Testosterone,T)、卵泡刺激素(Follicle-stimulating Hormone,FSH)、胰岛素抵抗指数(Homeostasis model assessment insulin resistance,HOMA-IR)、空腹胰岛素(Fasting serum insulin,FINS)、空腹血清葡萄糖(Fasting plasma glucose,FPG)均显著低于对照组(P<0.05),雌二醇(Estradiol,E2)显著高于对照组(P<0.05)。两组患者不良反应发生率无显著差异(P>0.05)。结论:二甲双胍联合炔雌醇环丙孕酮片应用于PCOS患者可通过纠正性激素紊乱、改善胰岛素抵抗来提高临床疗效及自然受孕率,可临床推广。     

凉血散瘀方对肾虚血瘀型 IgA 肾病患者的疗效观察

〔摘 要〕 目的：分析凉血散瘀方加减辅助雷公藤多苷、醋酸泼尼松片治疗肾虚血瘀型 IgA 肾病患者的临床效果。 方法：选取三明市中西医结合医院 2019 年 6 月至 2020 年 6 月期间收治的 70 例肾虚血瘀型 IgA 肾病患者，依照治疗方案不同分为 观察组与对照组，各35例。对照组给予西药治疗；观察组在对照组基础上加用凉血散瘀方加减治疗。比较两组治疗效果。 结果：观察组患者治疗总有效率为 91.43 %，高于对照组的 71.43 %，差异具有统计学意义（P ＜ 0.05）。治疗前两组患者的尿红细 胞个数、血清肌酐（Scr）、血尿酸（SUA）、24 h 尿蛋白定量、Ⅳ 型胶原（C–Ⅳ）、基质金属蛋白酶组织抑制物 –1（TIMP–1） 及层粘连蛋白（LN）比较，差异无统计学意义（P ＞ 0.05）；治疗后两组患者的尿红细胞个数、Scr、SUA、24 h 尿蛋白 定量、C–Ⅳ、TIMP–1 及 LN 均低于治疗前，且观察组患者的尿红细胞个数、Scr、SUA、24 h 尿蛋白定量、C–Ⅳ、TIMP–1 及 LN 均低于对照组，差异具有统计学意义（P ＜ 0.05）。观察组患者不良反应发生率为 2.86 %，与对照组的 8.57 % 比较，差异无统计学意义（P ＞ 0.05）。 结论：凉血散瘀方联合雷公藤多苷、醋酸泼尼松片治疗肾虚血瘀型 IgA 肾病患者， 可进一步改善患者病情，调节血脂水平，改善肾脏纤维化，且安全性不受影响。     

银杏叶片治疗轻度认知功能损害对照研究

目的 探讨银杏叶片治疗轻度认知功能损害患者的临床疗效和安全性.方法 将110例轻度认知功能损害患者随机分为两组,每组55例,研究组口服银杏叶片治疗,对照组口服丹参片治疗,观察3个月.于治疗前后采用简易智力状态检查量表和日常生活能力量表评定临床疗效,及时记录各种不良反应.结果 治疗后研究组简易智力状态检查量表评分较治疗前显著升高(P＜0.01),日常生活能力量表评分较治疗前显著下降(P＜0.05);对照组简易智力状态检查量表评分较治疗前有升高趋势,日常生活能力量表评分较治疗前有下降趋势,但差异均无显著性(P＞0.05).治疗后研究组简易智力状态检查量表评分显著高于对照组(P＜0.01).两组均未见明显不良反应.结论 银杏叶片与丹参片治疗轻度认知功能损害患者均有效,且安全性高,依从性好,但银杏叶片疗效显著优于丹参片.     

Understanding the in vivo performance of enteric coated tablets using an in vitro-in silico-in vivo approach: Case example diclofenac

Individual pharmacokinetics after administration of enteric coated tablets are often highly variable and this has been ascribed to the interaction of the dosage form with the physiology of the gastrointestinal tract. This research aimed to explore the influence of interactions between enteric coated tablets and physiological factors such as gastric and intestinal pH as well as gastric emptying on the release of drug from the dosage form and the subsequent plasma profile, using diclofenac as a case example.A physiologically based pharmacokinetic (PBPK) model for monolithic enteric coated dosage forms was designed and coupled with biorelevant dissolution results to predict PK profiles of diclofenac from Voltaren® tablets in both fasted and fed humans. The paddle method was used to obtain the dissolution profiles of diclofenac in biorelevant media. The Noyes–Whitney model was employed to describe the dissolution kinetics. The PBPK model was set up using STELLA® software. A single unit enteric coated tablet was assumed to be emptied from stomach only with the house-keeping wave. Timing of the emptying was simulated using a random number generator to statistically estimate gastric emptying times after ingestion. The lag times and the dissolution rate used as input parameters in the STELLA® model were adjusted according to the pre-exposure period. The oral PK profiles were predicted for each virtual subject individually, and then the mean profiles and standard deviations were calculated.The dissolution profiles were highly affected by the period of pre-exposure in FaSSGF. A long period of pre-exposure of the tablet prolonged the lag time and decreased the dissolution rate. The results of the pharmacokinetic simulations showed that not only the mean profiles in the fasted state but also the variability could be predicted successfully using data generated for the individual virtual subjects. The results emphasize the importance of accounting for the range of pH profiles and gastrointestinal transit in the target population when predicting plasma profiles of enteric coated dosage forms and point to problems in demonstrating bioequivalence for dosage forms of this type.     

多潘立酮片门诊用药评价及智能化知识库的作用

背景　多潘立酮为胃肠促动力药，自2012年起连续载入《国家基本药物》。鉴于2012-2014年加拿大、美国、英国等指出多潘立酮有导致心源性猝死及突发室性心律失常的风险，特别是年龄超过60岁、每天用药超过30 mg的患者。2016年9月，我国原国家食品药品监督管理总局（CFDA）发布了《关于修订多潘立酮制剂说明书的公告》，提出对多潘立酮说明书内容进行重新修订的要求。此后，多潘立酮生产厂家对多潘立酮说明书“不良反应、禁忌、注意事项、用法用量”等项进行修订，更新后的药品说明书载入了相关警示及风险提示内容。目的　了解多潘立酮片门诊治疗各种疾病的情况，为临床安全、合理用药提供参考。方法　选取2019年3-8月上海市闵行区吴泾社区卫生服务中心门诊医师开具的单一诊断，使用多潘立酮片的处方515张，统计患者的性别、年龄、临床诊断、用法用量等。构建契合社区医疗卫生机构用药特点的知识库智能管理系统。结果　515例使用多潘立酮片患者中，男197例（38.3%），女318例（61.7%）；年龄26~98岁，平均年龄（72.0±12.4）岁，以60 岁及以上的老年患者为主〔86.0%（443/515）〕。单一诊断涉及的疾病有19种，其中消化不良、消化性溃疡、慢性胃炎、胃食管反流病居前4位，占81.4%（419/515）。所有患者的每日剂量符合药品说明书规定。结论　门诊多潘立酮片使用基本合理。借助知识库利用信息技术能为患者用药“保驾护航”。