全水型薄膜包衣预混剂在复方丹参片生产中的应用研究

目的研究全水型薄膜包衣技术在复方丹参片生产中的应用,提高复方丹参片的质量稳定性。方法进行加速试验,比较复方丹参片全水型薄膜衣片与醇溶性薄膜衣片的综合质量和稳定性。结果全水型薄膜包衣片外观明显优于醇溶性薄膜衣片,在稳定性考察过程中含量测定和崩解时限均无明显变化。结论全水型薄膜包衣预混剂可用于复方丹参片的包衣生产。     

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.     

薄膜包衣提高含浸膏中药片剂稳定性研究

目的通过薄膜包衣片、糖衣片和素片的对比试验,研究分析薄膜包衣对提高含浸膏中药片剂稳定性的作用。方法取一种含浸膏的中药片剂的素片、糖衣片、薄膜衣片,在一定条件下进行加速试验,并对试验结果进行统计分析。结果薄膜包衣的片剂无论是在外观还是引湿等方面的变化均比糖衣片和素片小。结论薄膜包衣技术能显著提高含浸膏中药片剂的稳定性,值得在该领域推广使用。     

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。     

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。     

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。     

水性薄膜包衣技术在骨仙片生产的工艺研究

目的确定骨仙片水性薄膜包衣工艺方法。方法采用水性薄膜包衣技术,考察骨仙薄膜衣片和骨仙糖衣片包衣工艺,比较其外观、水分、崩解时限、抗热性、抗湿性及抗磨性等质量因素。结果实验结果表明,骨仙薄膜衣片,其外观、崩解时限、抗热性、抗湿性、抗磨性均优于其糖衣片。结论骨仙片水性薄膜包衣工艺可替代其糖衣工艺。     

秦息痛糖衣片改薄膜衣片的成型工艺研究

目的探索秦息痛糖衣片改为薄膜衣片的生产工艺。方法采用正交实验探索秦息痛薄膜衣片的最佳生产工艺参数,采用HPLC法,以片剂中青藤碱的含量为指标对正交实验结果进行验证。结果青藤碱质量浓度在1.032~10.88μg·mL-1范围内呈良好线性关系,平均回收率为99.49%,RSD值为2.79%(n=6)。秦息痛薄膜衣片最佳生产工艺:雾化气压0.4 MPa,包衣液喷速0.16~0.18kg·min-1,素片温度40℃,包衣液浓度10%。该工艺条件下生产的秦息痛薄膜衣片外观色泽均匀,表面平滑,崩解时限为29~31min,包衣合格率高于99.58%。HPLC法测得秦息痛薄膜衣片中青藤碱含量在10.48~10.55mg,符合标准要求。结论该制备工艺稳定,可为秦息痛薄膜衣片的工业化生产奠定基础。     

木香顺气丸薄膜包衣工艺研究

目的研究用薄膜包衣技术改进木香顺气丸的质量稳定性。方法采用薄膜包衣工艺技术,选取3种包衣液处方对本品素丸进行包衣,考察包衣前后丸子的相关质量指标。结果本品素丸包薄膜衣对溶散时限影响较小,对含量测定几无影响,稳定性试验表明包衣丸比未包衣素丸的吸湿率低。结论本品可以采用胃溶型薄膜包衣预混剂进行包衣,对提高其防吸湿性有明显效果,且工艺操作简单。     

美扑伪麻薄膜衣片与素片的稳定性对比研究

美扑伪麻薄膜衣片与素片在温度40±2℃、相对湿度为75±5%的条件下放置6个月,通过美扑伪麻薄膜衣片与素片的稳定性对照试验,考察薄膜包衣技术能否提高该制剂的稳定性及对药物溶出的影响。结果表明美扑伪麻薄膜衣片较美扑伪麻素片对潮湿稳定,溶出度也未发生明显变化。     

Development and evaluation of the tablets coated with the novel formulation termed thin-layer sugarless coated tablets

The purpose of this study was to develop and evaluate the thin-layer sugarless coated tablets containing Vitamin C, Vitamin E, Vitamin B2, calcium pantothenate, and L-cysteine. As a result of the formulation study, three coating layers, 2% under coating (UC), 38% build-up coating (BC), and 5% syrup coating (SC) were necessary for sufficient impact toughness, elegant appearance, and improvement of appearance stability after storage at 25 degrees C/75% RH for 6 months under open conditions. We demonstrated that the thin-layer sugarless coated tablets are superior to the sugar-coated tablets in terms of small tablet size and stability of calcium pantothenate. It was due to the coating method, the continuous spray mist method, which can minimize the thicknesses of coating layers and the moisture content in the tablets. We also demonstrated that the thin-layer sugarless coated tablets are superior to the film-coated tablets in terms of masking ability of the unpleasant odor and the appearance, stability of the appearance, and low hygroscopicity. It was due to the dense, opaque, and stable coating layers mainly consist of erythritol. We revealed that thin-layer sugarless coated tablets have both advantages of film-coated tablets and sugar-coated tablets.     

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.     

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.     

氯化钾缓释片的处方工艺研究

目的尝试用骨架与膜衣相结合的方法对水易溶性药物释放速度的控制 ,调整体外释药行为 ,应用EUDRAGIT系列辅料进行氯化钾控释片的研究。方法用RSPO和NE 30D与KCl压制成水不溶蚀性骨架片 ,再用RL10 0 ,RS10 0包衣制得。结果体外释放度研究表明其释药行为是 :第2 ,4 ,6h的溶出量分别为标示量的 2 0 %～ 4 0 % ,30 %～ 6 0 % ,75 %以上。结论水易溶性药物 ,通过骨架和膜衣双重控制 ,体外释药行为效果较好     

Influence of processing parameters and formulation factors on the drug release from tablets powder-coated with Eudragit L 100-55.

The aim of this study was to develop a dry powder coating process for chlorpheniramine maleate (CPM) tablets using Eudragit L 100-55 as the delayed release polymer. Powder coating, a water and organic solvent-free process, was investigated as a method to prevent the migration of an ionizable, highly water soluble model drug into the polymeric film during the coating process. Eudragit L 100-55 was pre-plasticized with triethyl citrate (TEC) using hot-melt extrusion at levels of 20%, 30%, and 40%, based on the polymer weight. The extrudate was subsequently cut into pellets and cryogenically ground into a fine powder. Talc was incorporated into the coating powder as an anti-tack agent. PEG 3350 was used as a primer for the powder coating of tablets with pre-plasticized Eudragit L 100-55. The addition of polyethylene glycol 3350 (PEG 3350) to the pre-plasticized Eudragit L 100-55 was necessary to enhance the adhesion of the coating powder to the tablet cores. PEG 3350 also improved film formation and coalescence of the polymeric particles due to its plasticization effects on the acrylic polymer. For comparison, theophylline tablets were also coated with pre-plasticized Eudragit L 100-55. Theophylline was selected as a less water soluble model drug. The powder coating process was performed in a modified laboratory scale spheronizer. The drug release rate was dependent both on TEC content and the coating level. The stability of the powder-coated CPM tablets was confirmed at 25 degrees C/60% RH over a storage time of 12 weeks.     

Study of triethyl citrate migration from coating polymers to tablet cores

Migration of plasticizers from film coating polymers towards the core and to the storage medium could result in serious changes in the mechanical properties and permeability of coatings thus greatly influencing rate and extent of drug release. The purpose of the present study was to follow the migration of water soluble triethyl citrate applied as a plasticizer in Acryl-Eze coating by Gas Chromatography/Mass Spectrometry (GC/MS). 20%w/w Acryl-Eze dispersions containing triethyl citrate of different concentrations were prepared. Placebo tablets were compressed and coated with the prepared dispersions. The coated tablets were stored under different relative humidity conditions for different time intervals. Considerable migration of triethyl citrate towards the tablet cores was found. The extent of the triethyl citrate migration was influenced by the relative humidity of the storage medium.     

Evaluation of a novel sugar coating method for moisture protective tablets

A novel method of manufacturing one-step dry-coated (OSDRC) tablets, which we recently invented, was used to produce sugar-coated tablets protected from moisture without the need for a conventional complicated sugar coating process. Amorphous sucrose was selected for the outer layer of the OSDRC tablets as sugar-coated layer. The isothermal crystallization behavior and characteristics such as water vapor permeability, tensile strength, and disintegration time of compressed amorphous sucrose were investigated. Water vapor adsorption measurements showed the crystallization behavior of amorphous tablets to be similar to that of amorphous powder, although it was affected by compression pressure. We found that the crystallized amorphous sucrose after compression at 200 MPa was moisture protective, and the water vapor permeability coefficient was decreased to 1/2000 or less compared with a tablet prepared with a lactose-microcrystalline cellulose (MCC) mixture, hydroxypropylmethylcellulose (HPMC), and sucrose crystal. The water vapor permeability and physicochemical characteristics were influenced by the amorphous content or additive content. It was confirmed that a new sugar-coated tablet using amorphous sucrose and OSDRC technology was moisture protective, therefore, it was concluded that the novel sugar coating method was very useful to obtain a moisture protective tablet.     

新型水性胃溶薄膜包衣预混辅料的制备及防潮防裂性能研究

目的研究新型水性胃溶薄膜包衣预混辅料。方法制备一种新型水性胃溶薄膜包衣预混辅料，对其处方结构和制备工艺特点进行分析。将用该预混辅料配制的包衣液分别对复方丹参片、花红片、普乐安片和钙尔奇D片进行包衣，在温度（40±2）℃、相对湿度（75±5）％的条件下进行裸片加速试验7d，考察其防潮防裂性能；通过对该预混辅料中镁元素含量及100目筛余率的测定，考察其均匀度和粒度。结果该预混辅料粒度小于100目，混合均匀度不低于99．5％，并具有较强的防潮、防裂性能。结论制备得到了一种粒度细、均匀度高、防潮防裂性能强的水性胃溶薄膜包衣预混辅料。