Formulation and Optimization of Modified Release Capsules for the Treatment of Rosacea

Abstract

Rosacea is a commonly occurring chronic inflammatory disease in the area of dermatology. Approved topical and systemic treatments are available for the treatment purpose. For severe rosacea light and laser surgeries are also accessible. Oral tetracycline derivatives are the most often used systemic drugs for rosacea, even though a lack of a curative treatment. A conventional dose of Drug X is known to cause gastric disturbance to overcome this side effect of Drug X modified-release capsule is required. This modified-release capsule of Drug X contains 75% immediate-release pellets and 25% delayed-release pellets to achieve the desired pharmacological action for a longer period to reduce the frequency and dose of the drug. For drug loading and delayed release layer coating fluidized bed equipment was used. For immediate release, HPMC E15 was selected as a binder to achieve entrapment efficiency of the drug. Delayed release polymer Eudragit L30D 55 is responsible for dissolving the drug over the pH 5.5 in the duodenum and not at acidic pH bypassing the stomach. To achieve the desired drug release profile different percentages of weight gain of the delayed release layer batches were formulated and optimized. The findings seem to indicate that modifiedrelease capsules may have promise as a stomach and duodenal delivery method.