Imai T, Kimura S, Iijima T, Miyoshi T, Ueno M, Otagiri M
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
J Pharm Pharmacol. 1990 Sep;42(9):615-9. doi: 10.1111/j.2042-7158.1990.tb06618.x.
Rapidly absorbed oral dosage forms of ibuprofen using water-soluble gelatin (hydrolysate of common gelatin: mean mol. wt: 6000) have been studied and compared with tablets prepared with common gelatin (mean mol. wt: 100,000) and commercial tablets. Spray-dried and speed-kneaded powders, two types of granules and tablets were prepared with water-soluble gelatin. The in-vitro dissolution rates of water-soluble gelatin preparations were significantly faster than those of commercial tablets, whereas the tablets prepared using common gelatin had slower dissolution rates than commercial tablets. Water-soluble gelatin enhanced the dissolution rate of ibuprofen by improving the wettability of the drug particle surface by water, without any interaction in solution and the solid state. The absorption behaviour of various preparations was evaluated in four beagle dogs. The peak concentration time (tmax) of the water-soluble gelatin preparations was significantly shorter than that of tablets prepared with common gelatin and commercial tablets. The maximum concentration (cmax) and the area under the serum concentration-time curve (AUCo-10 h) were similar in all cases. The serum concentration profiles of water-soluble gelatin solid preparations were almost the same as those of the solutions. On the other hand, the profiles of the common gelatin tablets were similar to those of the commercial tablets. The mean absorption time (MAT) from water-soluble gelatin preparations was about 0.7 h, while the MAT from commercial tablets and common gelatin tablets was about 1.2 h. The differences in the MAT of water-soluble gelatin preparations and commercial tablets or common gelatin tablets were the same as the differences in mean dissolution time (MDT) in gastrointestinal fluid.(ABSTRACT TRUNCATED AT 250 WORDS)
对使用水溶性明胶（普通明胶水解产物：平均分子量6000）的布洛芬速吸收口服剂型进行了研究，并与用普通明胶（平均分子量100,000）制备的片剂及市售片剂进行了比较。用水溶性明胶制备了喷雾干燥粉末、快速捏合粉末、两种颗粒剂和片剂。水溶性明胶制剂的体外溶出速率明显快于市售片剂，而用普通明胶制备的片剂溶出速率比市售片剂慢。水溶性明胶通过改善药物颗粒表面被水的润湿性来提高布洛芬的溶出速率，在溶液和固态中均无相互作用。在四只比格犬中评估了各种制剂的吸收行为。水溶性明胶制剂的达峰浓度时间（tmax）明显短于用普通明胶制备的片剂和市售片剂。在所有情况下，最大浓度（cmax）和血清浓度-时间曲线下面积（AUCo-10 h）相似。水溶性明胶固体制剂的血清浓度曲线与溶液的几乎相同。另一方面，普通明胶片剂的曲线与市售片剂相似。水溶性明胶制剂的平均吸收时间（MAT）约为0.7小时，而市售片剂和普通明胶片剂的MAT约为1.2小时。水溶性明胶制剂与市售片剂或普通明胶片剂在MAT上的差异与胃肠液中平均溶出时间（MDT）的差异相同。（摘要截短于250字）
