药学学报, 2001, 36(7): 535-538
引用本文:
金一;大熊英树;汪成发;夏目秀视;杉林坚次;森本雍宪. 尼可地尔口腔速溶片的研究[J]. 药学学报, 2001, 36(7): 535-538.
JIN Yi; Ohkuma Hideki; WANG Cheng-fa; Natsume Hideshi Sugibayashi Kenj; Morimoto Yasunori. PHARMACEUTICAL EVALUATION OF FAST-DISINTEGRANT TABLET CONTAINING NICORANDIL-LOADED PARTICLES[J]. Acta Pharmaceutica Sinica, 2001, 36(7): 535-538.

尼可地尔口腔速溶片的研究
金一;大熊英树;汪成发;夏目秀视;杉林坚次;森本雍宪
1.浙江大学药学院,浙江杭州310031; 2.城西大学药学部,日本坂户350-0295; 3.横店集团康裕制药有限公司,浙江东阳322118; 4.株式会社TTS技术研究所,日本坂户350-0295
摘要:
目的 制备尼可地尔口腔速溶片以提高其生物利用度和改善药物的苦味。方法 用croscarmellosesodium ,D-甘露醇和乳糖制备直径为6mm(崩解时限为12s)和10 mm(崩解时限为23s)的尼可地尔口腔速溶片。对其崩解性能、硬度、药物释放度、体内吸收及口感性能进行了考察。结果 压力在1.37×108 Pa以上,甘露醇-乳糖比为9∶1,croscarmellosesodium的添加量为1% - 4%时,口腔速溶片的崩解时间较市售片缩短了1/3,且能达到一定的硬度。对Beagle犬经口服给药后,测得血药浓度与市售片相同,AUC ,Cmax,Tmax值无明显差异。口腔速溶片有长效和掩盖药物苦味的作用,同时甜味剂对掩盖药物苦味有相加作用。结论 口腔速溶片为快速崩解型片剂,与市售片等效,适合老龄和小儿患者服用
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PHARMACEUTICAL EVALUATION OF FAST-DISINTEGRANT TABLET CONTAINING NICORANDIL-LOADED PARTICLES
JIN Yi; Ohkuma Hideki; WANG Cheng-fa; Natsume Hideshi Sugibayashi Kenj; Morimoto Yasunori
Abstract:
AIM To improve the bioavailability and taste of fast-disintegrating tablet (FD tablet) containing nicorandil loaded particles. METHODS A FD tablet containing nicorandil loaded particles with 1%-4% croscarmellose sodium in addition of D-mannitol and lactose (9∶1) was prepared and the dissolution and absorption characteristics were examined, in comparison with FD tablet and commercial tablets of nicorandil. In vivo absorption of nicorandil from FD tablet was evaluated in beagle dogs. RESULTS The disintegration time of FD tablets containing 1% croscarmellose sodium with 6 mm and 10 mm in diameter were about 12 and 23 seconds, respectively. When nicorandil loaded particles consist of myristyl alcohol and stearyl alcohol were put in FD tablet, nicorandil release from FD tablet continued until 6 h while nicorandil release from Sigmart and FD tablet containing nicorandil crystals finished within 5 min. In vivo absorption of nicorandil from Sigmart and FD tablet containing nicorandil crystals was very similar after oral administration in beagle dogs and no statistic difference in AUC, Tmax, Cmax was observed between these tablets. However pharmacokinetics parameters of nicorandil after oral administration of FD tablet containing nicorandil loaded particles showed that nicorandil was delivered into the body at a suitable absorption rate with similar AUC, delayed Tmax and lower Cmax. CONCLUSION The reports suggest that the modification of properties of myristyl alcohol and stearyl alcohol released from the drug-loaded particles system would lead to more acceptable bioavailability of the system. However, The formulation of particles and may have a masking effect against the bitter taste and irritation of the drug.
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