Rivaroxaban Capsule Composition Without Wet Granulation
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing processes for preparing rivaroxaban compositions are lengthy, expensive, and unsuitable for industrial scale due to the use of costly chemicals and require wet granulation, leading to stability and bioavailability issues.
Innovation Solution
A pharmaceutical capsule composition using tricalcium citrate as a pharmaceutically acceptable excipient, combined with micronized rivaroxaban and hydroxpropyl methylcellulose capsules, eliminating the need for wet granulation and enhancing dissolution and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If wet granulation is used in the preparation process, then the capsule composition can be formed, but stability and bioavailability decrease due to crosslinking and agglomeration
Solution Approach 1:
The invention extracts and eliminates the wet granulation step from the preparation process. By using a direct compression method with hydroxpropyl methylcellulose capsules, the patent removes the source of crosslinking and agglomeration problems while still achieving proper capsule formation through a simplified process.
Solution Approach 2:
The invention uses hydroxpropyl methylcellulose capsules as a disposable, single-use formulation vehicle that eliminates the need for complex granulation processes. These capsules provide the necessary structure for drug delivery without causing the stability issues associated with gelatin-based systems that require wet granulation.
2Manufacturing precision
If conventional preparation processes are used, then rivaroxaban composition can be prepared, but the process is lengthy and expensive with poor industrial feasibility
Solution Approach 1:
The invention implements a continuous, streamlined preparation process where micronized rivaroxaban is directly mixed with excipients and filled into hydroxpropyl methylcellulose capsules without intermediate wet granulation steps. This continuous process eliminates downtime and reduces overall manufacturing time while maintaining composition quality.
Solution Approach 2:
The patent extracts and removes the expensive and time-consuming wet granulation step from the conventional process. By using direct compression with pre-formed hydroxpropyl methylcellulose capsules, the invention significantly reduces both process time and chemical costs while maintaining manufacturing precision.
3Ease of manufacture
If gelatin capsules are used, then capsule formulation is achieved, but crosslinking and agglomeration occur reducing dissolution and bioavailability
Solution Approach 1:
The invention replaces traditional gelatin capsules with hydroxpropyl methylcellulose capsules that do not cause crosslinking or agglomeration. These alternative capsules serve the same formulation purpose but eliminate the harmful interactions with rivaroxaban, thereby improving dissolution and bioavailability without compromising ease of manufacture.
Solution Approach 2:
The patent uses hydroxpropyl methylcellulose, a composite material with superior properties compared to traditional gelatin. This material provides the necessary capsule structure while being chemically compatible with rivaroxaban, preventing crosslinking and agglomeration issues that plague gelatin-based formulations.
Data Source
AI summary
This invention relates to a novel pharmaceutical capsule composition comprising rivaroxaban with at least one pharmaceutically acceptable excipient and its process.