Water dispersible mini-tablets comprising Enalapril for treatment of hypertension in a pediatric population and method of preparation thereof
Inventors
Karavas, Evangelos • KOUTRIS, EFTHYMIOS • SAMARA, VASILIKI • Koutri, Ioanna • Kalaskani, Anastasia • Kalantzi, Lida • KAKOURIS, ANDREAS • Diakidou, Amalia • GOTZAMANIS, GEORGE • GEORGOUSIS, ZAHARIAS • Konstanti, Louiza
Assignees
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Publication Number
US-11318114-B2
Publication Date
2022-05-03
Expiration Date
Abstract
The present invention relates to water dispersible mini-tablets of Enalapril or a pharmaceutically acceptable salt thereof for use in the treatment of hypertension in a pediatric population. The pediatric population is defined as 0 to 18 years of age. The water dispersible mini-tablets of Enalapril further include a disintegrant, a diluent, a lubricant and a glidant. The active ingredient is distributed evenly in the mini-tablet and the disintegrant comprises Crospovidone. The mini-tablet has a diameter of 3 mm and disintegrates in less than 15 seconds in water.
Core Innovation
The invention relates to water-dispersible minitablets comprising Enalapril or pharmaceutically acceptable salts thereof as an active ingredient, with a disintegrant, a diluent, a lubricant and a glidant. The active ingredient is distributed evenly in the minitablet, and the minitablet has a diameter of 3 mm with Crospovidone as the disintegrant.
The minitablet disintegrates in less than 15 seconds in water, providing rapid dispersion for pediatric use. Crospovidone is described as the preferred disintegrant, and the formulation includes excipients including a diluent, a lubricant and a glidant.
The core formulation is developed in the context of direct compression for pediatric patients 0 to 18 years. The document provides a dosing strategy using a weight-based approach, including a dosing amount per minitablet, and reports formulation development examples evaluating hardness, disintegration performance, and stability/impurity trends for a selected trial formulation.
Claims Coverage
The independent claim set is grounded in a single independent claim directed to a specific pediatric water-dispersible Enalapril minitablet, with the main inventive coverage defined by five core inventive features.
Evenly distributed active ingredient in the minitablet
The active ingredient is distributed evenly in the minitablet.
3 mm diameter water-dispersible minitablet
The minitablet has a diameter of 3 mm.
Crospovidone as the disintegrant
The disintegrant comprises Crospovidone.
Less than 15 seconds water disintegration
The minitablet disintegrates in less than 15 seconds in water.
Disintegrant, diluent, lubricant and glidant formulation set
The minitablet comprises a disintegrant, a diluent, a lubricant and a glidant, together with Enalapril or pharmaceutically acceptable salts thereof as an active ingredient.
Overall claim coverage centers on a water-dispersible 3 mm minitablet with evenly distributed Enalapril, Crospovidone as the disintegrant, and rapid water disintegration in less than 15 seconds, while employing a formulation set including disintegrant, diluent, lubricant and glidant.
Stated Advantages
Provides water disintegration in less than 15 seconds.
Supports even distribution of the active ingredient in the minitablet.
Described as suitable without sweeteners, including neutral taste.
Addresses dissolution and stability effects via disintegrant hydration and glidant moisture capture.
Documented Applications
Pediatric administration for patients 0 to 18 years.
Water-dispersible use of Enalapril minitablets that disintegrate rapidly in water.
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