New Formulations Benefit Special Populations

About 40% of American adults cannot or will not swallow solid forms of medications.¹

There are many different types of oral formulations or solid dosage forms, such as capsules and tablets, which are preferred, because of the cost-effectiveness, dosing convenience, and high physicochemical stability.² However, certain solid formulations can be difficult for elderly patients and infants with dysphasia. This difficulty encouraged development of a new medication with liquid and sprinkle formulations.³

Sprinkle formulations are drugs that contain granules or pallets that can be mixed with soft food prior to administration. These formulations provide the same dosing flexibility and ease of ingestion as liquid formulations. Sprinkle formulations can be sprinkled on applesauce or yogurt, which can mask the unpleasant smell and taste of a drug. Sprinkle formulations have a higher stability of drugs compared with liquid formulations during storage. Numerous drugs that have been previously available as tablet formulations have now been approved as sprinkles, including Drizalma (duloxtine), Ezallor (rosuvastatin), and Kapspargo (metoprolol succinate). Other drugs approved as a liquid formulation are Carospir (spironolactone) and Riomet ER (metformin hydrochloride for extended-release oral suspension).

Carospir (spironolactone) oral suspension is an aldosterone approved by the FDA on August 7, 2017 and is manufactured by CMP Pharmaceutical Industries. Carospir is indicated for the treatment of NYHA Class III-IV heart failure and reduced election fraction to increase survival, manage edema and to reduce hospitalization for heart failure. It is also used as an add-on therapy for the treatment of hypertension and management of edema in adult patients with cirrhosis. Carospir is a stable, ready to use, and consistent liquid treatment option for adult patients who have difficulty swallowing, or who cannot swallow tablets.⁴

Drizalma Sprinkle (duloxetine delayed-release capsules) is a serotonin and norepinephrine reuptake inhibitor (SNRI) that the FDA approved on July 19, 2019, and it is manufactured by Sun Pharmaceutical Industries. Drizalma is indicated for chronic musculoskeletal pain in adults, diabetic peripheral neuropathic pain in adults, generalized anxiety disorder in adults and pediatric patients ages 7 to 17 years, and major depressive disorder in adults. It is available in 20-, 30-, 40-, and 60 mg. Drizalma provides a controlled and predictable release, and the ability to be administered via a nasogastric tube, and it can be sprinkled over applesauce.⁵

Ezallor Sprinkle (rosuvastatin capsules) is a HMG-Co-A reductase inhibitor indicated for adult patients with hypertriglyceridemia, primary dysbetalipoproteinemia (Type III hyperlipoproteinemia), and homozygous familial hypercholesterolemia (HoFH) to reduce LDL-C, total-C, and ApoB. Ezallor was FDA-approved on December 18, 2018 and is manufactured by Sun Pharmaceutical Industries. It is available in 5 mg, 10 mg, 20 mg, and 40 mg. Ezallor can be administered as a single dose at any time of day, with or without food. For patients who are unable to swallow capsules, the capsules can be opened for administration.⁶

Kaspargo Sprinkle (metoprolol succinate capsules) is a β₁-selective adrenoceptor blocking agent approved by the FDA on January 26, 2018 and is manufactured by Sun Pharmaceutical Industries. Kaspargo is indicated for hypertension (to lower blood pressure), angina pectoris, and heart failure (to reduce the risk of cardiovascular mortality and hospitalization). It is administered once daily and is available in 25mg, 50mg, 100mg, and 200mg. The benefit of Kaspargo is that it provides a controlled and predictable release, can be sprinkled over applesauce, and the ability to be administered via a nasogastric tube.⁷

Riomet ER (metformin hydrochloride for extended-release oral suspension) is a biguanide that the FDA approved on August 29, 2019, that is manufactured by Sun Pharmaceutical Industries. Riomet ER is indicated to improve glycemic control in adults and pediatric patients age 10 years and older with type 2 diabetes mellitus. Riomet ER is available in 16-oz. bottles and comes in grape and strawberry flavors. The extended-release liquid formulation allows for once-daily dosing without the need to break, chew, or crush a tablet. The starting dose is 500 mg (5 mL) orally once daily with the evening meal; the dose can be increased in increments of 500 mg (5 mL) weekly, up to a maximum dose of 2000 mg (20 mL), once daily with the evening meal.⁸

Oral delivery is a desirable route of administration for many patients. These new formulations of drugs are intended to help patients who are in long-term-care facilities and residents who cannot or will not swallow solid medication form. Liquid and sprinkle formulations can help improve adherence to medications.

Saro Arakelians, PharmD, is the vice president of pharmacy operations at BioScrip Infusion in Burbank, California.

Sagar Shah is a PharmD candidate at West Coast University School of Pharmacy in Los Angeles, California.

REFERENCES

• Center for Drug Evaluation & Research. Size, shape, and other physical attributes of generic tablets and capsules: guidance for industry. FDA. June 2015. Accessed July 20, 2020. https://www.fda.gov/media/87344/download
• Tahaineh L, Wazaify M. Difficulties in swallowing oral medications in Jordan. Int J Clin Pharm. 2017;39(2):373-379. doi: 10.1007/s11096-017-0449-z
• Logrippo S, Ricci G, Sestili M, et al. (2017, January 31). Oral drug therapy in elderly with dysphagia: between a rock and a hard place! Clin Interv Aging. 2017;12:241-251. doi: 10.2147/CIA.S121905
• Carospir oral suspension [prescribing information]. Farmville, NC; CMP Pharma, Inc: 2017. Accessed August 11, 2020. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209478s000lbl.pdf
• Drizalma Sprinkle [prescribing information]. Cranbury, NJ; Sun Pharmaceutical Industries, Ltd: 2019. Accessed August 11, 2020. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212516s000lbl.pdf
• Ezallor Sprinkle [prescribing information]. Gujarat, India; Sun Pharmaceutical Industries, Ltd: 2020. Accessed August 11, 2020. https://www.healthgrades.com/drugs/ezallor-sprinkle
• Kapspargo Sprinkle [prescribing information]. Cranbury, NJ; Sun Pharmaceutical Industries, Ltd: 2018. Accessed August 11, 2020. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210428s001lbl.pdf
• Riomet Sprinkle [prescribing information]. Cranbury, NJ; Sun Pharmaceutical Industries, Ltd: 2019. Accessed August 11, 2020. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212595s000lbl.pdf