Scheiffele S, Kolter K, Schepky G
Fachhochschule, Pharmatechnik Dept., Sigmaringen, Germany.
Drug Dev Ind Pharm. 1998 Sep;24(9):807-18. doi: 10.3109/03639049809088525.
The products that are processed in aqueous form, such as Aqoat MF (suspension), Aquateric (pseudolatex), HP 55 (ammonia-based solution), and Kollicoat MAE 30 D (latex), were compared (in the form of spray dispersions, isolated films prepared from the dispersions, and caffeine-film-coated tablets with 5.5, 8.0, and 11.0 mg film/cm2) with one another and with ethanolic HP 55 S solution. The addition of pigments to all of the liquid preparations, with the exception of the ammoniacal solution of HP 55, led to a slight increase in pH. In each case, the viscosity of both solutions was well above that of the other formulations. The minimum film-forming temperature was decidedly reduced by the addition of pigment. Kollicoat MAE was the undissolved film-former that had the smallest particle size and particle size distribution. The next smallest were those of Aqoat MF. The latex and the suspension were the only products that were sensitive to shear and heat. The isolated films did not display any tack. The strongest films and the films most impermeable to water vapor were obtained from solutions, and this can be ascribed to the fine distribution of the film-former. None of the isolated films showed signs of dissolving at pH 4.5. At pH 5.5, only the HP 55 was dissolved. This was because HP 55 was processed in ammonia-based solution; as a result of which, films that were not very resistant to gastric juice were obtained. The other formulations did not dissolve until the pH reached 6.0. As the pH rose, the rate of dissolution increased for all of the films. The permeability to protons was similar to that of caffeine-film-coated tablets to gastric juice. The resistance increased in the following sequence: HP 55 (ammonia-based) < Aquateric < Aqoat MF < HP 55 S (organic) and Kollicoat MAE. As a result of the temperature treatment and the rate of spraying, the production time on a 5-kg scale was twice as long for 5.5 mg Aqoat MF/cm2 as it was for Kollicoat MAE. This amount of film sufficed for Kollicoat MAE and HP 55 S solution to achieve adequate resistance to gastric juice. Aqoat MF did not attain the same resistance until a thickness of 11 mg film/cm2 was reached. Film tablets with Aquateric and ammonia-based HP 55 solution absorbed more than 20% of gastric juice at this film thickness.
对以水性形式加工的产品进行了比较，这些产品包括Aqoat MF（悬浮液）、Aquateric（假乳胶）、HP 55（氨溶液）和Kollicoat MAE 30 D（乳胶），比较形式为喷雾分散体、由分散体制备的分离膜以及含5.5、8.0和11.0mg膜/cm²的咖啡因薄膜包衣片，它们之间相互比较，并与乙醇性HP 55 S溶液比较。除HP 55的氨溶液外，向所有液体制剂中添加颜料均导致pH略有升高。在每种情况下，两种溶液的粘度均远高于其他制剂。添加颜料后，最低成膜温度明显降低。Kollicoat MAE是粒径和粒径分布最小的不溶性成膜剂。其次是Aqoat MF的粒径和粒径分布。乳胶和悬浮液是仅对剪切和热敏感的产品。分离膜未表现出任何粘性。从溶液中获得的薄膜强度最高且对水蒸气最具阻隔性，这可归因于成膜剂的精细分布。在pH 4.5时，没有分离膜显示出溶解迹象。在pH 5.5时，只有HP 55溶解。这是因为HP 55是在氨溶液中加工的；因此，获得的薄膜对胃液的耐受性不强。其他制剂直到pH达到6.0才溶解。随着pH升高，所有薄膜的溶解速率均增加。质子渗透性与咖啡因薄膜包衣片对胃液的渗透性相似。耐受性按以下顺序增加：HP 55（氨溶液）<Aquateric<Aqoat MF<HP 55 S（有机溶液）和Kollicoat MAE。由于温度处理和喷雾速率的原因，5kg规模下5.5mg Aqoat MF/cm²的生产时间是Kollicoat MAE的两倍。对于Kollicoat MAE和HP 55 S溶液，该量的薄膜足以获得对胃液的足够耐受性。Aqoat MF直到达到11mg膜/cm²的厚度才获得相同的耐受性。在此薄膜厚度下，含Aquateric和氨溶液型HP 55的薄膜片吸收了超过20%的胃液。
