Development of an Immediate-Release Prototype Tablet Formulation of Hydroxychloroquine Sulfate with an Interwoven Taste-Masking System.

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.

Evaluation of an Immediate-Release Formulation of Hydroxychloroquine Sulfate With an Interwoven Pediatric Taste-Masking System.

Hydroxychloroquine sulfate (HCQ) is a quinoline used for the prevention and treatment of uncomplicated malaria, lupus erythematosus, and rheumatoid arthritis. For each indication, HCQ is an option for treatment of pediatric and juvenile patients on a weight basis; however, no tailored pediatric product is available on the market. Preliminary research confirmed that a slightly buffered, ion-pairing system significantly reduces the bitterness of HCQ, suggesting a high likelihood that a pediatric taste-masking system could be interwoven into an adult immediate-release formulation allowing the creation of a palatable suspension with water using common excipients. Because HCQ is a Biopharmaceutics Classification System Class 1 drug, the pharmacokinetics for an adult immediate-release formulation would not be altered by embeding a taste-masking system. Embedding the taste-masking and suspension agents within the adult tablet formulation would remove the need for aqueous-based vehicles and simplify the creation of a water-based suspension formulation to support improved compliance, dosing accuracy, and health outcomes in pediatric patients who are weight-base dosed with HCQ.