Nasir S S, Wilken L O, Akhtar B
J Pharm Sci. 1977 Mar;66(3):370-9. doi: 10.1002/jps.2600660316.
Gluconolactone was evaluated as an excipient for tablets prepared by direct compression using various drugs known to be difficult to compress. The physical properties of the tablets were evaluated after compression and after storage and were satisfactory. Comparative studies were conducted between gluconolactone and anhydrous lactose, a common direct compression diluent, for development of static charges during blending, flow, drug distribution, drug stratification, color distribution, compressibility, and preservation against mold growth. Gluconolactone possesses those properties necessary to produce high quality tablets by the direct compression process. Separate powdered mixtures of aspirin USP with gluconolactone, anhydrous lactose, spray-dried lactose, mannitol, and sorbitol were stored at various humidities and temperatures for specified periods and tested for the integrity of aspirin. Gluconolactone contributed least to the degradation of the drug as compared to other excipients studied. A preliminary in vivo study also was conducted on the bioavailability of aspirin from separate and similar mixtures with gluconolactone, anhydrous lactose, and starch. Gluconolactone did not show any inhibitory effect on aspirin absorption.
葡萄糖酸内酯被评估为一种辅料，用于通过直接压片法制备片剂，所使用的各种药物已知难以压片。压片后及储存后的片剂物理性质令人满意。对葡萄糖酸内酯和无水乳糖（一种常见的直接压片稀释剂）进行了对比研究，涉及混合过程中的静电产生、流动性、药物分布、药物分层、颜色分布、可压性以及防霉生长等方面。葡萄糖酸内酯具备通过直接压片法生产高质量片剂所需的特性。将美国药典阿司匹林与葡萄糖酸内酯、无水乳糖、喷雾干燥乳糖、甘露醇和山梨醇的单独粉末混合物在不同湿度和温度下储存特定时间，并对阿司匹林的完整性进行测试。与所研究的其他辅料相比，葡萄糖酸内酯对药物降解的影响最小。还对阿司匹林与葡萄糖酸内酯、无水乳糖和淀粉的单独且类似混合物的生物利用度进行了初步体内研究。葡萄糖酸内酯对阿司匹林吸收未显示任何抑制作用。
