薄膜颗粒压片工艺应用于氟灭酸片等生产

薄膜包衣工艺目前在国内仅用于片剂包衣方面,我们进行了一些探索性的试验,使这一工艺得到了更广泛的应用。我厂生产的氟灭酸、无味氯霉素、安妥明铝三个品种常产生粘冲、滞冲等问题,经试用薄膜液制粒压片取得了较好的成果,现已用于生产。薄膜颗粒压片系指将主辅料混合均匀后加入优选确定的薄膜液,使药物粉末或微粉完整的被薄膜包裹起来,再经常规片剂生产的程序压片的方法。现将我们生产的情况简介如下: 一、氟灭酸片氟灭酸原料系短纤维状质轻的微绿色粉末,固相附着力强,采用一般常用的辅料如淀粉、滑石粉、微晶纤维素等组方制粒,当压片时,开车仅10～20分钟就产生了难以排除的粘冲现象致使不能生产。经采用薄膜颗粒压片获得了解决。     

酚氨咖敏片制备工艺研究

目的研究适合酚氨咖敏片的制备工艺。方法考察组成酚氨咖敏片主要物料间的相互作用，采用分别制粒与筛除细粉工艺进行小试及中试，考察粘冲情况及压片质量。结果该工艺能解决压片过程中的粘冲难题，产品符合质量标准要求。结论所用工艺可行，对类似的由物料间相互作用而形成易溶盐、易粘冲的品种，有一定借鉴作用。     

无糖型复方庆大霉素普鲁卡因颗粒的研制

目的:研制无糖型复方庆大霉素普鲁卡因颗粒.方法:以制粒收率为指标,用正交试验法优选制粒工艺.结果:按优化后的新工艺制粒,制粒收率达到92.4%.结论:优化后的新工艺可行并可应用于大生产.     

布洛芬片制备工艺改进

目的：对布洛芬片制备工艺进行改进。方法：采用内加部份预胶化淀粉、15％预胶化淀粉浆制粒;应用新辅料HPMC60RT50和丙烯酸树酯Ⅳ号作包衣材料对布洛芬片薄膜包衣。结果：解决布洛芬压片时粘冲,提高其溶出度;薄膜包衣后,增加产品的抗热、抗湿性,提高产品质量。结论：该制备工艺操作简单、工艺成熟。     

清热感冒颗粒流化床制粒工艺研究

目的 探索研究清热感冒颗粒流化床制粒的最佳工艺.方法 采用正交试验法,以制粒收得率和颗粒水分为指标,探索清热感冒颗粒流化床制粒的最佳工艺条件.结果 清热感冒颗粒流化床制粒的最佳工艺条件为:进风量2000m3/h,进风温度78℃、进液速度20rpm.结论 本试验为清热感冒颗粒的工艺改进提供了依据.     

消炎利胆片工艺优化及其制备

目的:解决消炎利胆片处方有黄色成分析出造成包装药瓶发黄质量问题。方法:优化制粒、压片工艺;筛选合适的薄膜包衣剂和包衣工艺。结果:采用一步制粒法工艺,颗粒能顺利进行高速压片,片芯硬度适中。片芯选用雅克宜包隔离层,欧巴代85G进行薄膜包衣,片剂外观优良,崩解性能良好,留样稳定性考察,未发生黄色成分析出现象。结论:该制备工艺可操作性强,产品质量稳定。     

影响ATP片质量稳定性的工艺探讨

目的对影响ATP片质量稳定性的工艺进行探讨。方法采用制空白颗粒工艺与原湿法制粒工艺对比,采用包薄膜衣与包糖衣工艺对比。结果经实验对比,两种新工艺的方法减少了含量的降解,提高了质量稳定性。结论探索ATP片生产新工艺,对提高质量稳定性尤为重要。     

保精片一步制粒法工艺研究

目的:改进保精片制粒工艺,使其适合压片和薄膜包衣.方法:采用一步制粒法制备保精片用颗粒,确定其一步制粒的最佳工艺条件.结果:最佳制粒工艺条件是将一定量的保精片用干膏10 ～0.12 MPa中,开启风机并加热,使物料在流化状态下均匀升温至50℃,以速度25～32 r·min-1喷入黏合剂,雾化压力0.10～0.12 MPa,进风温度75～90℃,物料温度随后控制在43～ 47℃,密切观察物料流化状态,直至黏合剂全部喷入,继续干燥8～10 min,降温出料.结论:一步制粒法颗粒可压性提高,所压片芯硬度好、片重差异幅度缩小、崩解时限符合规定.且一步制粒法比摇摆式制粒法更易控制,生产效率也更高.     

棕榈氯霉素（B型）片工艺研究

目的：对棕榈氯霉素（B型）片处方及工艺进行研究,解决该产品颗粒流动性差、压片粘冲、崩解时间长等问题。方法：通过处方的重新设计、制粒工艺的改进和实际操作过程的精细化控制及细节管理来实现。结果和结论：通过处方工艺的改进,彻底解决了棕榈氯霉素（B型）片生产过程中的质量问题,也为其他类似产品的工艺改进提供了借鉴作用。     

乳块消片一步制粒法工艺研究

目的：薄膜衣片中确定制粒工艺及其参数，以解决颗粒所压片芯硬度和崩解时限问题。方法：颗粒采用一步制粒法。结果：一步制粒法所生产的颗粒，可压性提高，所压片芯硬度好、崩解时间缩短、片重差异幅度缩小。结论：颗粒采用一步制粒法生产的可操作性强，产品质量稳定并得到提高，适合高速压片和薄膜包衣。     

薄膜包衣技术常见问题解决方法探索

目的讨论研究薄膜包衣中常见问题及解决方法.方法针对薄膜包衣过程中出现色差、粘片等技术问题,采用不同的方法进行解决.结果及结论通过调整片芯质量、调节包衣处方和操作可以保证薄膜包衣外观质量达到规定要求.     

布洛芬微晶体在口腔崩解片中的应用

目的：改善口腔崩解片干粉压片工艺中药物的可压性、流动性、黏冲性，提高崩解片的崩解速度。方法：以布洛芬为模型药物，利用溶剂-非溶剂法改变其结晶形态，获得5种不同的微晶体，并用扫描电镜（SEM）和X衍射仪（XRD）表征。通过各晶体的压片工艺性能测试及压片后的崩解实验，优选出性能良好的晶体，并对其压制的崩解片进行了体外洛出性能的测定。结果：优选出的微晶体具有良好的可压性、流动性和抗黏冲性能，压片后崩解时限大大缩短，溶出度也有一定的提高。结论：优选出的布洛芬微晶体改善了口腔崩解片的整体性能。     

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。     

How suitable is the measurement of take-off forces for detection of sticking during direct compression of various ibuprofen tablet formulations?

Sticking of tablet formulations to punch surfaces is one of the most common problems observed during tablet manufacture. An inline method proposed for detection of sticking during compression is the measurement of take-off forces, which occur when tablets are detached from the lower punch surface. It has been postulated that the tablet take-off force is a direct indicator of the sticking tendency of a tablet formulation. In the present study, the take-off forces measured during direct compression of sticking ibuprofen tablet formulations were evaluated and compared to the sticking extent of these tablets quantified by HPLC analysis of ibuprofen. As expected, sticking to the lower punch was increased with an increase of the ibuprofen content in the investigated tablet formulations. However, data obtained from take-off force measurements did not correlate with the quantified amount of sticking. Although pronounced sticking was observed, the measured tablet take-off forces remained low even at high drug contents. These results indicate that the tablet take-off force is not a direct indicator of the sticking tendency of ibuprofen tablet formulations. It is suggested that the evaluation of take-off force data requires a differentiated approach. A new interpretation of take-off force data is presented in this paper.     

Effects of surface roughness and chrome plating of punch tips on the sticking tendencies of model ibuprofen formulations

The sticking of three model ibuprofen-lactose formulations with respect to compaction force and the surface quality of the upper punch were assessed. Compaction was performed at 10, 25 or 40 kN using an instrumented single-punch tablet press. Two sets of 12.5-mm flat-faced punches were used to evaluate the influence of surface quality. A third set of chrome-plated tooling was also used. Surface profiles (Taylor Hobson Talysurf 120) of the normal tooling upper punches indicated a large difference in quality. The punches were subsequently classified as old (Ra = 0.33 microm) or new (Ra = 0.04 microm) where Ra is the mean of all positive deviations from zero. Surface profiles of sample tablets were also obtained. Following compaction, ibuprofen attached to the face was quantified by spectroscopy. Punch surface roughness, compaction force and the blend composition were all significant factors contributing to sticking. Chrome plating of punch faces increased sticking at a low compaction force but decreased sticking at higher forces. Surface roughness of the tablets did not correlate with the corresponding data for sticking, indicating that this is not a suitable method of quantifying sticking.     

Controlling individual steps in the production process of paracetamol tablets by use of NIR spectroscopy

Various physical and chemical parameters of interest to the pharmaceutical industry were determined by NIR spectroscopy with a view to assessing the potential of this technique as an effective, expeditious alternative to conventional methods for this purpose. To this end, the following two steps in the production process of tablets containing 1 g of paracetamol were studied: (1) intermediate granulation, which was characterized in terms of Active Principle Ingredient (API) content, average particle size and particle size distribution and (2) manufactured tablet, which was examined in relation to compaction pressure and API content of the tablets. The ultimate aim was to identify critical attributes of the process influencing the quality of the end-product. Based on the results, a new method for determining the API in the end-product was developed and validated for its quality control.     

布洛芬片工艺改进

硅胶粉可以避免布洛芬片压片过程中的粘冲问题,以薄膜包衣代替糖衣制片,工艺简单,过程较短,稳定性符合要求。     

Pharmacokinetics of ibuprofen in man IV: absorption and disposition

Fifteen normal male volunteers received 400, 800, and 1200 mg doses of ibuprofen as 1, 2, or 3 tablets, respectively, in crossover fashion, then 420 mg in solution form during the fourth week. Plasma concentration of ibuprofen was measured by an HPLC method. Individual subject concentration-time (C,t) data following the solution were analyzed by two different methods, and results unequivocally indicated the open two compartment model with first order absorption. However, the computer fitting of both arithmetic and geometric mean concentrations led to a different model. A method was developed to obtain absorption data (fraction of drug absorbed, Fa, versus time) for a multicompartmental system from oral data alone, without intravenous data. The method assumes that Vp is constant intrasubject and that absorption is complete following administration of both the solution and tablets. The method was successfully applied to the ibuprofen tablet data. It was shown also that such a method is necessary to obtain ibuprofen absorption data since intrasubject variation of the microscopic rate constants k12, k21, and kel (as reflected by the intrasubject variation of the hybrid rate parameters lambda 1 and lambda 2 or beta and alpha) is of the same order of magnitude as intersubject variation. Absorption of ibuprofen from tablets was shown not to be simple first order as for the solution. The absorption profiles following one tablet were S-shaped, while those following 2 or 3 tablets had partial linear segments indicating zero order absorption.     

Effect of lubricant type and concentration on the punch tip adherence of model ibuprofen formulations

A model formulation, comprising ibuprofen and direct compression lactose (Tablettose 80) was used to assess the influence of two lubricants, magnesium stearate and stearic acid, on punch tip adherence. Lubricant concentrations were varied from 0.25% to 2% w/w. Formulations in the presence and absence of 0.5% w/w colloidal silica (Aerosil 200) were examined, to assess the influence of the glidant on the anti-adherent effects of the lubricants. Differential scanning calorimetry (DSC) was used to examine the effect of the lubricants on the melting temperature of ibuprofen. Tablets were compacted using a single punch tablet press at 10 kN using hard chrome-plated punches or at 40 kN using uncoated steel punches, tooling was 12.5-mm diameter in each case. The upper punch faces were characterized by obtaining Taylor Hobson Talysurf surface profiles. Following compaction, ibuprofen attached to the face was quantified by spectroscopy. At low concentrations of each lubricant, the levels of sticking observed were similar. Whilst sticking increased at magnesium stearate concentrations above 1%, sticking with stearic acid remained relatively constant at all concentrations. DSC revealed that the melting temperature of ibuprofen was lowered by the formation of eutectic mixtures with both lubricants. However, the onset temperature of melting and melting point were lowered to a greater extent with magnesium stearate compared with stearic acid. When using uncoated tooling at 40 kN, the deleterious effects of magnesium stearate on the tensile strength of the tablets also contributed to sticking. When using chrome-plated punches at 10 kN, the tensile strength reduction by the presence of magnesium stearate was less pronounced, as was the level of sticking.     

布洛芬缓释片的生产及体外释药性能研究

目的:研究布洛芬骨架缓释片从研试处方到生产处方的放大过程中,工艺参数对药物释放性能的影响.方法:通过测定不同时间点药物累积释药量,考察布洛芬缓释片的释药机制;并考察了致孔剂、制粒工艺和压片设备等因素对药物释放的影响,还对骨架片进行了6个月的加速试验.结果:布洛芬不溶性骨架缓释片的药物释放规律符合Higuchi方程;致孔剂羟丙甲纤维素(HPMC)的加入可以提高药物释放速率;不同制粒工艺和压片设备对药物释放的均匀性有一定影响;在一定压力范围内,药物释放对压力敏感.结论:布络芬缓释片的大生产中,制粒工艺、致孔剂用量和压片设备对药物释放有影响,可以通过优化上述工艺参数来提高产品质量.