复方丹参片薄膜包衣工艺研究

目的将复方丹参片糖衣片改为薄膜衣片。方法以羟丙基甲基纤维素为主要成膜材料包衣,将生产的复方丹参薄膜衣片与糖衣片同时进行稳定性考察、比较。结果复方丹参薄膜衣片在抗湿性、硬度、稳定性、外观等方面均优于糖衣片。结论所用方法简单、工艺成熟。     

丙戊酸钠薄膜衣片的制备及稳定性研究

目的研究丙戊酸钠薄膜衣片的制备方法。方法分别用全水型和醇溶型薄膜包衣预混剂对该素片进行包衣,与该品种同规格糖衣片同时进行稳定性考察比较。结果用全水型和醇溶型薄膜包衣预混剂对该产品素片进行包衣后,当增重达到（3．5±0．3）％时,本品6个月时的水分含量分别为6.3％、6．6％,糖衣片为8．9％,其他项目比糖衣片也显出一定的优势,且均符合规定。结论按该工艺生产的丙戊酸钠薄膜衣片符合质量标准要求,工艺稳定可靠,适合大生产需要。     

金胆片全水型薄膜包衣的生产工艺研究

目的:对金胆片包衣生产工艺进行研究,降低包衣片的顶裂、剥落现象,同时优化包衣的生产工艺条件.方法:通过崩解、耐温湿试验比较醇溶型薄膜包衣及全水型薄膜包衣对金胆片理化性质的影响,通过正交试验摸索出全水型薄膜包衣的最佳工艺条件.结果:全水型薄膜包衣可显著减少金胆片项裂、剥落现象,提高贮存期稳定性,在优选的金胆片工艺条件下各项质量指标均合格.结论:金胆片可采用全水型薄膜包衣.     

陈香露白露薄膜衣片的研制

目的:制备陈香露白露薄膜衣片,提高药物稳定性。方法:选用不同的粘合剂制备片芯,再选用不同的包衣材料进行包衣,比较陈香露白露薄膜衣片与糖衣片的稳定性。结果:采用10%聚乙烯吡咯烷酮乙醇液为粘合剂制备片芯,用隔离材料玉米阮将片芯保护,采用上海卡乐康公司的黄色或红棕色胃溶性包衣粉制备的陈香露白露薄膜衣片在外观质量上优于其它材料制备的成品,尤其是防渗油和防潮性方面优势明显;薄膜衣片稳定性优于糖衣片。结论:陈香露白露薄膜衣片质量稳定,制备工艺简单。     

冠心丹参片薄膜包衣生产工艺研究

目的：将冠心丹参片改为薄膜衣片,提高冠心丹参片质量。方法：以胃溶型全水防潮性包衣剂为包衣料,将生产的冠心丹参薄膜衣片与冠心丹参糖衣片同时进行稳定性考察、比较。结果：冠心丹参薄膜衣片在抗湿性、硬度、稳定性、外观等均优于糖衣片。结论：操作方法简单,工艺成熟、可行。     

刺五加黄芪片薄膜包衣的制备与质量控制

目的改进刺五加黄芪片包衣的质量和稳定性。方法采用羟丙甲基纤维素、丙烯酸树脂Ⅱ号为薄膜包衣主材对刺五加黄芪片进行薄膜包衣，并将其薄膜衣片与糖衣片进行质量和稳定性比较。结果薄膜包衣制备工艺可行，薄膜衣片外观、硬度、崩解时限、水分、稳定性、抗热性等均优于糖衣片。结论薄膜包衣可以改进刺五加黄芪片的质量。     

复方利血平氢氯噻嗪片薄膜包衣工艺研究

目的通过薄膜包衣工艺条件的筛选，提高复方利血平氢氯噻嗪片的稳定性。方法通过试验摸索薄膜包衣的最佳工艺条件，并通过影响因素试验、加速试验和长期稳定性试验，比较薄膜衣片及糖衣片对复方利血平氢氯噻嗪片理化性质的影响。结果薄膜包衣片的稳定性优于糖衣片。结论复方利血平氢氯噻嗪片采用包薄膜衣比包糖衣稳定。     

青霉素V钾片包衣处方研究及稳定性考察

目的：通过研究不同包衣处方对青霉素V钾片进行包衣,并考察稳定性。方法：采用水溶性防潮包衣材料和醇溶性防潮包衣材料分别对青霉素V钾片进行包衣,并就其质量稳定性进行对比。结果：采用醇溶防潮包衣的青霉素V钾片,具有较佳的防潮性能和稳定性。结论：利用醇溶防潮包衣材料进行青霉素V钾片薄膜包衣,产品质量稳定,值得广泛应用。     

右旋糖酐铁糖衣片改为薄膜衣片生产工艺探讨

目的提高右旋糖酐铁糖衣片的溶出度和防潮性能,使其在有效期内能够保持质量稳定,符合中国药典规定。方法将右旋糖酐铁片由糖衣片改为薄膜衣片。结果薄膜衣片溶出度和防潮性能明显提高,在留样考察期内,薄膜衣片溶出度和防潮性能无明显改变,产品在有效期内质量始终满足中国药典要求。结论按该工艺生产的右旋糖酐铁片质量稳定可靠,改进的薄膜包衣工艺适合大生产要求。     

宣肺止咳薄膜衣片的制备及其稳定性研究

目的研究宣肺止咳薄膜衣片的制备及考察其稳定性。方法采用丙烯酸树脂制备薄膜衣片,应用加速试验进行稳定性研究,并与糖衣片进行比较。结果宣肺止咳薄膜衣片的包衣合格率、崩解时限、防潮性、微生物限度检查等指标均优于糖衣片,加速试验稳定性良好。结论制备宣肺止咳薄膜衣片的方法简单可行,质量稳定。     

冰片内加法对复方丹参薄膜包衣片素片的影响

目的比较冰片的加入方式以寻找制备复方丹参薄膜包衣片的最佳工艺。方法考察冰片外加法和内加法两种复方丹参薄膜包衣片片芯制备工艺对粉体的物理性质、片芯物理性质、片剂外观以及片剂中冰片的加速试验的影响。结果两种方法制备的样品颗粒流动性、片芯物理性状无明显差异。冰片外加法制备的片芯加速试验后表面含有较多的孔洞,不光滑,冰片下降较快,而采用冰片内加法制备的片芯无明显孔洞,外观细腻,冰片挥发较慢。结论冰片内加法为制备复方丹参薄膜包衣片片芯的优化方法。     

Detrimental Effect of the Film Coat Chemistry and Thickness on the Physical Stability of Amorphous Solid Dispersions in Tablet Formulations

Amorphous solid dispersions (ASDs) have been widely utilized to enhance the bioavailability of pharmaceutical drugs with poor aqueous solubility. The role of various excipients on the amorphous drug to crystalline form conversion in ASDs has been widely documented. However, there has been no published study to investigate the role of film coating material on the physical stability of an ASD based tablet formulation, to the best of our knowledge. Here we show that the film coating can potentially have a detrimental impact on the physical stability of spray dried intermediates (SDI) in tablet formulations. The impact of the film coating on the physical stability of SDI was found to be related to the film coat material composition, and an increase in the film coating thickness led to a reduction in the physical stability of SDI in tablets. Oral compressed tablets in which the film coat material was “mixed-in” with the formulation blend showed a similar or worse physical stability than film coated tablets, further underscoring the film coat material impact on physical stability, independent of the film coating process. This study demonstrates a need for careful consideration of the film coat material selection for ASD based pharmaceutical product development.     

复方丹参滴丸联合阿司匹林防治短暂性脑缺血发作的疗效观察

目的观察复方丹参滴丸联合阿司匹林肠溶片防治短暂性脑缺血发作的疗效和安全性。方法 120例TIA患者随机分为治疗组和对照组,每组60例。治疗组服用复方丹参滴丸及阿司匹林肠溶片,对照组只服用阿司匹林肠溶片。观察治疗两个疗程内TIA复发或进展为脑梗死的例数、胃肠道反应、出血等不良反应,并比较两组疗效。结果两组治疗后两个疗程内的脑梗死发生率差异无统计学意义(P>0.05),治疗组TIA复发率较对照组低,差异有统计学意义(P<0.05),治疗组疗效优于对照组,差异有统计学意义(P<0.05),但出血和胃肠道不良反应的发生率与对照组比较,差异无统计学意义(P>0.05)。结论复方丹参滴丸联合阿司匹林肠溶片对TIA防治效果优于单用阿司匹林肠溶片,其机制可能与改善血液变学指标有关。     

Development of an enteric coating formulation and process for tablets primarily composed of a highly water-soluble, organic acid.

The purpose of this study was to define coating conditions for the enteric coating of a highly water soluble, acidic tablet core. Acidic tablet cores containing a marker drug were separated into three groups and seal coated to coverage levels of 0% (uncoated, white), 1% (yellow), and 3% (tan) weight gains. By employing a 'color coding' scheme, the different seal coated tablets could be coated simultaneously to reduce the number of experiments and eliminate potential differences that may exist during separate coating processes. In addition, an allotment of each coded tablet type was sequentially numbered with a marker pen, weighed, and recorded in order to identify the precise level of enteric coating as well as to monitor the variability of a given coating operation. The tablets were coated with five Eudragit((R)) L30D-based enteric formulations containing different amounts of plasticizer (10-20 parts) and talc (10-50 parts). During each enteric coating process, a predetermined amount of labeled tablets were removed after attaining 6, 8, and 10% weight gains. The labeled tablets were re-weighed, sorted, and then tested using USP disintegration and dissolution methods. Weight gain measurements of individual tablets indicated low coating variability (6.2% RSD) during the enteric coating processes. Dissolution results revealed that all enteric coat formulations inhibited drug release for 2 h in 0.1 N HCl. In contrast, it was found that tablets without a seal coat failed the USP disintegration test. In addition, seal coated tablets exhibited ca. 1.5-5 fold greater drug release at most intermediate sampling time points in phosphate buffer, pH 6.8, than tablets without a seal coat, suggesting that the dissolution of the latter was delayed by the generation of an acidic microenvironment at the interface of the enteric coat/acidic tablet core. Prior to enteric coating an acidic, highly water soluble substrate, a seal coat barrier should be applied to prevent retardation in drug release. A simple strategy utilizing color coding and tablet marking can be employed to test the effect of a seal coat, evaluate enteric coating formulations and process with minimal experimentation and analyses.     

Film coated tablets (ColoPulse technology) for targeted delivery in the lower intestinal tract: Influence of the core composition on release characteristics

The design of a film coating technology which allows a tablet to deliver the drug in the ileocolonic segment would offer new treatment possibilities. The objective is to develop a platform technology that is suitable for a broad range of drug compounds. We developed a coated tablet with a delayed, pulsatile release profile based on a pH-sensitive coating technology (ColoPulse). The production process was validated, and the effect of core composition on the in vitro release and water uptake investigated. The release profile of the standard tablet core composition, based on the use of cellulose as a filler, was independent of the coat thickness in a range of 9.0–13.2?mg/cm². The release profile of a coated tablet was strongly influenced when cellulose was partly replaced by the model substance glucose (loss of sigmoidal release), citric acid (stabilization), sodium bicarbonate (destabilization) or sodium benzoate (destabilization). The film coating takes up water when below the pH-threshold. However, this did not cause early disintegration of the coating. The ColoPulse technology is successfully applied on tablets. The in vitro release characteristics of the coated tablets are influenced by the composition of the core.     

Film coated tablets (ColoPulse technology) for targeted delivery in the lower intestinal tract: influence of the core composition on release characteristics

The design of a film coating technology which allows a tablet to deliver the drug in the ileocolonic segment would offer new treatment possibilities. The objective is to develop a platform technology that is suitable for a broad range of drug compounds. We developed a coated tablet with a delayed, pulsatile release profile based on a pH-sensitive coating technology (ColoPulse). The production process was validated, and the effect of core composition on the in vitro release and water uptake investigated. The release profile of the standard tablet core composition, based on the use of cellulose as a filler, was independent of the coat thickness in a range of 9.0-13.2?mg/cm(2). The release profile of a coated tablet was strongly influenced when cellulose was partly replaced by the model substance glucose (loss of sigmoidal release), citric acid (stabilization), sodium bicarbonate (destabilization) or sodium benzoate (destabilization). The film coating takes up water when below the pH-threshold. However, this did not cause early disintegration of the coating. The ColoPulse technology is successfully applied on tablets. The in vitro release characteristics of the coated tablets are influenced by the composition of the core.     

片剂薄膜包衣过程激光共聚焦成像及近红外光谱建模分析

目的 研究薄膜包衣的微观成膜过程，实现对包衣质量无损检测模型的构建。方法 采用聚乙烯吡咯烷酮为包衣材料对微晶纤维素片进行包衣，在包衣材料中加入罗丹明为示踪剂。测定包衣过程不同时间包衣增重和衣膜厚度，并通过激光共聚焦显微镜成像系统和近红外光谱技术分别测定包衣片衣膜的微观结构和宏观图谱，最后采用化学计量学的方法关联近红外图谱与衣膜质量，构建包衣过程的控制模型。结果 衣膜在片芯表面呈现非均匀分布，先分布于片芯两侧表面，后分布于片芯曲面，这种差异随包衣的进行逐渐降低，且在衣膜表面存有微小的孔隙结构。多元散色矫正预处理后的近红外光谱图形能够构建包衣质量的精确控制和预测模型。结论 激光共聚焦成像及近红外光谱技术能够分别从微观和宏观角度增进对薄膜包衣过程的理解和控制，有助于促进薄膜包衣技术的进一步开发利用。