Dry processed surface coated engineering excipients
Inventors
Assignees
New Jersey Institute of Technology
Publication Number
US-10751288-B2
Publication Date
2020-08-25
Expiration Date
2037-08-23
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Abstract
Pharmaceutical blends are disclosed herein. In some embodiments, a pharmaceutical blend includes a cohesive active pharmaceutical ingredient (API) and a dry coated pharmaceutical excipient. The dry coated pharmaceutical excipient is present in an amount of about 1 wt % to 99 wt %, based on the total weight of the pharmaceutical blend. The dry coated pharmaceutical excipient includes a core and a shell surrounding the core, wherein the shell partially covers the core of the pharmaceutical excipient.
Core Innovation
The invention described relates to pharmaceutical blends that incorporate a cohesive active pharmaceutical ingredient (API) and a specially engineered dry coated pharmaceutical excipient. The excipient features a core surrounded by a shell, where the shell at least partially covers the core but does not fully encapsulate it. The shell consists of a plurality of discrete particles—such as nano-sized silica or similar agents—ranging from about 5 nanometers to 35 nanometers in average size. These excipients are designed to be present in the blend in amounts from about 1 wt% to 99 wt% based on the total blend weight.
The background section identifies a significant problem in pharmaceutical tablet formulation: fine or cohesive APIs typically exhibit poor flow, packing density, and compaction properties, which make direct tablet formation challenging, especially at high drug loadings (e.g., above 10 wt%). Traditionally, this results in a need for wet granulation or additional processing steps, limiting efficiency and flexibility in tablet manufacturing. Moreover, while fine excipients can improve tablet strength by increasing bonding areas, their small particle size leads to cohesiveness and poor flow, complicating blend handling and compaction.
The core innovation solves these issues by providing a dry processed, surface coated excipient that dramatically improves flowability and bulk density of pharmaceutical blends containing highly cohesive APIs. The dry coated excipient allows blends to achieve high drug loadings (30 wt% to 99 wt%) with desirable mechanical properties for direct compression, thereby eliminating or reducing the need for traditional wet granulation. The method employs simplified manufacturing using dry coating technology, without requiring the use of liquids, and can result in blends that possess sufficient flow, density, and compaction (tensile) strength for tablet formation.
Claims Coverage
There is one independent claim defining the inventive features of the pharmaceutical blend.
Pharmaceutical blend of non-coated cohesive API and dry coated excipient
The inventive feature is a pharmaceutical blend consisting essentially of: - A non-coated cohesive active pharmaceutical ingredient (API) present in an amount from about 30 wt% to about 99 wt%, resulting in a high drug loading. - A dry coated pharmaceutical excipient present in an amount of about 1 wt% to 70 wt% (based on total blend weight), which includes a core and a shell that does not fully cover the core but provides partial coverage by discrete particles. - The excipient's shell consists of discrete particles, such as nano-silica, with average particle size from about 5 nm to 35 nm, disposed on the core surface. The excipient has a particle size in the range of about 20 to 40 microns, enabling elimination of wet granulation at high drug loading. - The pharmaceutical blend provides improvement in bulk density (above 0.41 g/mL) and flow function coefficient (FFC of about 3.7 to 8.0), addressing poor flow and density characteristics of the non-coated cohesive API (which itself has bulk density of about 0.05 g/mL to 0.40 g/mL and FFC of about 0.10 to 3.5). - The dry coating is only disposed on the excipient, not the API, and the addition of the coated excipient in presence of the non-coated API results in improved bulk density, FFC, and tensile strength relative to blends using non-coated excipient.
The claim coverage is focused on a pharmaceutical blend comprising a high loading of a non-coated cohesive API and a specifically engineered dry coated excipient, characterized by a core-shell structure with discrete nanoparticulate shell, yielding improved blend properties to enable direct compression tablet formation and eliminating the need for wet granulation.
Stated Advantages
Provides pharmaceutical blends at high drug loadings with improved flowability and bulk density, enabling direct compression without the need for wet granulation.
Facilitates the use of fine, cohesive APIs in blends by overcoming their inherent poor flow and compaction problems.
Yields tablets with sufficient mechanical strength and tensile properties even at high API loadings, compared to blends with uncoated or conventionally processed excipients.
Enables simplified, liquid-free manufacturing of excipients, reducing environmental footprint and process complexity.
Documented Applications
Application in formation of pharmaceutical tablets using direct compression or roller compaction, especially for blends with high loadings of fine or cohesive APIs.
Use in manufacturing pharmaceutical blends and tablets which require improved flow, packing density, and compaction properties without wet granulation.
Interested in licensing this patent?