Cariprazine Hydrochloride Oral Composition for Stability and Dissolution
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Solution Overview
Problem
Existing formulations of cariprazine hydrochloride face challenges in achieving both stability and dissolution profile simultaneously, particularly due to hydrolytic degradation caused by excipients with high water activity, and there is a need for formulations that provide better results.
Innovation Solution
A solid oral composition comprising cariprazine hydrochloride with a specified particle size d (0.9) between 30 µm and 1 µm, combined with pharmaceutically acceptable excipients like microcrystalline cellulose, hydroxypropyl cellulose, and magnesium stearate, is developed to enhance stability and dissolution profile.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If cariprazine is formulated in aqueous suspension with excipients to achieve stability, then stability is improved, but the formulation complexity and manufacturing difficulty increase
Solution Approach 1:
The patent changes the physical-chemical parameters of cariprazine by converting it to the hydrochloride salt form and controlling particle size distribution (d(0.9) between 1-30 microns). This parameter change allows the drug to be formulated in solid oral composition without requiring complex aqueous suspension systems, thereby achieving stability while reducing formulation complexity
Solution Approach 2:
The patent creates a composite formulation system combining cariprazine hydrochloride with specific excipients (microcrystalline cellulose, hydroxypropyl cellulose, magnesium stearate) in optimized ratios. This composite approach achieves stable drug delivery in solid form, eliminating the need for complex aqueous suspension systems while maintaining or improving stability
2Stability of the object's composition
If cariprazine is formulated with excipients having high water activity to improve dissolution profile, then dissolution is improved, but hydrolytic degradation increases causing poor stability
Solution Approach 1:
The patent changes the particle size parameter of cariprazine hydrochloride to a controlled range (d(0.9) between 1-30 microns), which increases surface area and improves dissolution rate without requiring excipients with high water activity. This eliminates the trade-off between dissolution and stability
Solution Approach 2:
The patent converts the potential harm of cariprazine's sensitivity to water activity into a benefit by using the hydrochloride salt form with controlled particle size. This allows the drug to achieve both rapid dissolution and enhanced stability, turning the stability challenge into a formulation advantage
3Ease of manufacture
If cariprazine particle size is reduced to improve dissolution profile, then dissolution is improved, but manufacturing complexity and cost increase
Solution Approach 1:
The patent establishes a specific particle size range (d(0.9) between 1-30 microns) that optimizes dissolution profile while remaining achievable through conventional pharmaceutical manufacturing techniques. This parameter range balances dissolution improvement with manufacturing feasibility, avoiding the need for complex nanosizing processes
Data Source
AI summary
The present invention relates to a solid oral composition comprising cariprazine hydrochloride and at least one pharmaceutically acceptable excipient, wherein cariprazine hydrochloride has a d (0.9) particle size between 30 µm and 1 µm. The present invention also relates to a simple, rapid, cost effective, time-saving and industrially convenient method of preparing the formulation.