Lumateperone Formulation Without Mannitol
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Solution Overview
Problem
Existing pharmaceutical compositions of Lumateperone require high amounts of mannitol and disintegrating agents to achieve desired pharmaceutical attributes like dissolution and stability, making them costly and complex to manufacture.
Innovation Solution
A solid oral pharmaceutical composition of Lumateperone or its pharmaceutically acceptable salts, free of mannitol and disintegrating agents, with a weight ratio of Lumateperone to diluent ranging from 1:2 to 1:25, using excipients like microcrystalline cellulose and sucrose, which ensures adequate drug dissolution without mannitol or disintegrating agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If mannitol is used as diluent and disintegrating agent in Lumateperone pharmaceutical composition, then dissolution and stability attributes are improved, but manufacturing complexity and cost increase due to high amounts required
Solution Approach 1:
The patent removes mannitol from the formulation entirely, extracting the problematic substance that causes processing issues and requires high amounts of lubricant and disintegrating agent. The invention replaces mannitol with alternative diluents like microcrystalline cellulose and sucrose, eliminating the need for excessive lubricant and disintegrating agent while maintaining dissolution and stability attributes.
Solution Approach 2:
The patent changes the formulation parameters by replacing mannitol with alternative diluents (microcrystalline cellulose, sucrose) and adjusting the ratio of excipients. This parameter change allows achieving the same pharmaceutical attributes with simpler manufacturing processes and lower costs.
2Ease of manufacture
If high amount of lubricant is used to reduce processing problems with mannitol, then manufacturing ease is improved, but cost and formulation complexity increase
Solution Approach 1:
The patent eliminates mannitol from the formulation, which removes the cause of processing problems that required high amounts of lubricant. By using alternative diluents like microcrystalline cellulose and sucrose, the formulation achieves ease of manufacture without requiring excessive lubricant quantities.
3Reliability
If high amount of disintegrating agent is used to achieve disintegration time with mannitol, then dissolution performance is improved, but formulation complexity and cost increase
Solution Approach 1:
The patent removes mannitol from the formulation, eliminating the need for high amounts of disintegrating agent. The alternative diluents (microcrystalline cellulose, sucrose) provide sufficient disintegration performance without requiring excessive disintegrating agent, thereby reducing formulation complexity.
4Reliability
If mannitol is used in Lumateperone formulation, then dissolution profile is improved, but manufacturing cost increases
Solution Approach 1:
The patent replaces expensive mannitol with more cost-effective alternative diluents like microcrystalline cellulose and sucrose. These alternatives provide comparable dissolution profiles at lower manufacturing costs, making the formulation more economically viable.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition achieves over 80% dissolution within 30 minutes in 0.1N Hydrochloric acid and demonstrates stability, bioavailability, and cost-effectiveness, comparable to commercially marketed formulations like CAPLYTA®, while simplifying the manufacturing process.
Implementation Method 1
The composition achieves over 80% dissolution within 30 minutes in 0.1N Hydrochloric acid
Data Source
AI summary
The present disclosure relates to pharmaceutical composition comprising Lumateperone or pharmaceutically acceptable salt form and, processes for manufacture thereof.