RTI International, 3040 Cornwallis Road, Research Triangle Park, NC 27709, United States.
AustarPhama, LLC 18 Mayfield Ave, Edison, NJ 08837, United States.
J Pharm Sci. 2023 Mar;112(3):830-836. doi: 10.1016/j.xphs.2022.11.002. Epub 2022 Nov 8.
Hydroxychloroquine sulfate (HCQS) was granted US-FDA approval in 1955 for the prevention and treatment of malaria. Since then, its uses have expanded to treat systemic lupus erythematosus and rheumatoid arthritis. For each indication, HCQS is a crucial option for the treatment of pediatric, juvenile, adult, and elderly populations. Existing currently on the market are only 200-mg strength tablets exclusively for adult administration. To facilitate weight-based administration for pediatric and juvenile patients, an HCQS suspension is made by compounding a 200-mg HCQS tablet and suspending the crushed granules into water and Ora-Plus®. The Ora-Plus® suspension does not alter the extreme bitterness of HCQS such that it facilitates oral administration. Additional research has been executed to affirm that a slightly buffered, ion-pairing system, reduces the bitterness of HCQS. The buffered, ion-pairing system can be interwoven into an immediate-release tablet formulation likely without compromising tablet performance. With the taste-masking system embedded, the tablet could be more easily be compounded and suspended in water to generate a palatable oral suspension. Such a novel HCQS 200-mg tablet would be tailored for adult usages wherein the interwoven task-masking system could be utilized to facilitate weight-based administration for pediatric and juvenile patients. The dual quality target product profile of the tablet and the tablet compounded for suspension in water would make the tablet formulation applicable to a wide patient population ranging from pediatric to elder adults to facilitate in improving compliance and overall health outcomes.
硫酸羟氯喹(HCQS)于 1955 年获得美国食品药品监督管理局(US-FDA)批准,用于预防和治疗疟疾。此后,其用途已扩展到治疗系统性红斑狼疮和类风湿关节炎。对于每种适应症,HCQS 都是治疗儿科、青少年、成年和老年人群的重要选择。目前市场上仅有的 200mg 片剂仅适用于成人使用。为了便于儿科和青少年患者进行基于体重的给药,通过将 200mg HCQS 片剂粉碎并悬浮在水中和 Ora-Plus®中制成 HCQS 混悬剂。Ora-Plus®混悬剂不会改变 HCQS 的极端苦味,从而便于口服给药。已经进行了额外的研究来证实,略微缓冲的离子配对系统可以降低 HCQS 的苦味。缓冲的离子配对系统可以编织到速释片剂配方中,而不会影响片剂的性能。通过嵌入掩味系统,片剂可以更容易地在水中复合和悬浮,以生成可口服的混悬液。这种新型的 200mg HCQS 片剂将专门用于成人使用,其中编织的掩味系统可用于为儿科和青少年患者进行基于体重的给药。片剂和用于混悬在水中的片剂的双重质量目标产品特性将使该片剂配方适用于广泛的患者群体,从儿科到老年人,以提高顺应性和整体健康结果。