Pediatric powder for oral suspension containing antiviral agent and method for the preparation thereof
Inventors
Karavas, Evangelos • KOUTRIS, EFTHYMIOS • SAMARA, VASILIKI • Koutri, Ioanna • Kalaskani, Anastasia • Kalantzi, Lida • KAKOURIS, ANDREAS • Diakidou, Amalia • GOTZAMANIS, GEORGE • GEORGOUSIS, ZAHARIAS • FOUSTERIS, MANOLIS
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-11969429-B2
Publication Date
2024-04-30
Expiration Date
Abstract
The present invention relates to a pediatric powder for reconstitution as suspension for oral administration comprising a therapeutically effective amount of an antiviral agent or pharmaceutical acceptable salt or derivative thereof, in particular Valaciclovir in complex with an ion exchange resin in a specific ratio in order to obtain a palatable and child-friendly product. It also relates to a process for the preparation thereof.
Core Innovation
The invention relates to a pediatric-reconstitution powder for oral suspension containing valaciclovir as a drug complexed with an ion exchange resin to form Drug-Resin complex (DRC) particles. In the DRC particles, valaciclovir is described as being complexed such that hydrogen bonds are formed between the ion exchange resin and a cationic center of valaciclovir, with the Drug:Resin ratio fixed at 1:0.8.
The powder further includes a suspending agent and a pH agent, and the suspending agent is described as forming a film around each DRC particle. This film decreases interparticle attraction, and the powder is configured to be reconstituted with an aqueous diluent as a suspension for oral administration.
The formulation is characterized by a dissolution profile in which more than 95% of valaciclovir is released from complexation with the ion exchange resin at 10 minutes when suspended in 900 ml of HCl 0.1N. The document discusses selection of excipients and resin types, including weak and strong cation resins tested and examples using INDION™ 204 and PUROLITE™ C100CaMR.
Claims Coverage
The document provides two independent claims. Across these claims, the inventive coverage centers on valaciclovir-ion exchange resin Drug-Resin complex (DRC) particles at a fixed 1:0.8 drug-to-resin ratio, combined with a suspending agent, a pH component, and defined dissolution-release performance for oral reconstitution.
Drug-resin complex drc particles with hydrogen bonding at fixed ratio
Valaciclovir, or a pharmaceutical acceptable salt or derivative, is in complex with an ion exchange resin forming DRC particles, each DRC particle comprises hydrogen bonds between the ion exchange resin and a cationic center of Valaciclovir, and the ratio of Valaciclovir to the ion exchange resin is 1:0.8.
Film-forming suspending agent around drc particles for reduced interparticle attraction
The powder further comprises a suspending agent that forms a film around each DRC particle, and the film decreases interparticle attraction.
Reconstitutable powder for oral suspension with dissolution release criterion in hcl 0.1n
The powder is configured to be reconstituted with an aqueous diluent as suspension for oral administration, and more than 95% of Valaciclovir is released from complexation with the ion exchange resin at 10 minutes when suspended in 900 ml HCl 0.1N.
Valaciclovir-only active pharmaceutical ingredient at fixed ratio with suspending and pH adjusting agents
A powder for oral suspension comprises Valaciclovir or a pharmaceutical acceptable salt thereof in complex with an ion exchange resin, a suspending agent and a pH adjusting agent, the ratio of Valaciclovir to the ion exchange resin is 1:0.8, and Valaciclovir is the only active pharmaceutical ingredient.
Overall, the independent claims are directed to powders in which valaciclovir forms DRC particles with an ion exchange resin at a fixed 1:0.8 ratio, supported by hydrogen bonding and combined with suspending and pH components. One claim additionally requires a suspending agent film that decreases interparticle attraction and a defined dissolution-release performance in HCl 0.1N, while another limits the composition to valaciclovir as the only active pharmaceutical ingredient.
Stated Advantages
Taste masking and child-friendly palatability for pediatric use.
More than 95% Valaciclovir released from complexation at 10 minutes in HCl 0.1N.
Documented Applications
Pediatric-reconstitution powder configured to be reconstituted with an aqueous diluent as a suspension for oral administration.
Powder for oral suspension comprising Valaciclovir complexed with an ion exchange resin, including dissolution release performance when suspended in HCl 0.1N.
Interested in licensing this patent?