Pimavanserin Capsule Formulation for Swallowability
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Solution Overview
Problem
Current formulations of pimavanserin for treating Parkinson's disease psychosis are challenging due to large tablet size and poor physical properties, leading to compliance issues and manufacturing difficulties, particularly in administering a single daily dose.
Innovation Solution
Development of capsules containing 5-34 mg of pimavanserin or its pharmaceutically acceptable salt, combined with fillers and lubricants, using a process involving granulation, drying, and encapsulation in size 3 or 4 capsules, which improves bulk density and flowability without the need for binders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If conventional tablet formulations of pimavanserin are used, then the drug can be administered, but the tablet size becomes too large and patient compliance deteriorates
Solution Approach 1:
The patent segments the large tablet into smaller capsule units containing lower doses of pimavanserin (5mg, 10mg, 15mg, 20mg, or 25mg). This allows patients to take smaller, more manageable doses that are easier to swallow, directly addressing the compliance issue while maintaining therapeutic effectiveness.
Solution Approach 2:
The patent changes the dosage form parameters from large tablets to smaller capsules with reduced drug content per unit. By formulating capsules with 5-25mg of pimavanserin instead of larger tablet equivalents, the physical dimensions and swallowability are improved while preserving the therapeutic dose through appropriate selection of capsule strength.
2Ease of manufacture
If conventional manufacturing techniques are used for pimavanserin tablets, then the drug can be produced, but the bulk density and flowability deteriorate leading to manufacturing difficulties
Solution Approach 1:
The patent applies granulation technology to change the physical parameters of pimavanserin powder, transforming it into granules with improved bulk density and flow characteristics. This parameter change enables accurate filling of small capsules at high production speeds, directly resolving the manufacturing precision and ease of manufacture contradiction.
Solution Approach 2:
The patent introduces granulation as an intermediary processing step between powder preparation and capsule filling. The granulation process acts as a mediator that improves the flow and packing properties of pimavanserin, enabling subsequent accurate and efficient capsule filling without requiring binders or other additives.
3Stability of the object's composition
If binders and other agents are added to improve tablet properties, then the dosage form can be manufactured, but the finished dosage size increases
Solution Approach 1:
The patent extracts or eliminates the need for binders and other size-increasing agents by using granulation technology that works directly with pimavanserin powder. This removal of unnecessary components maintains dosage form stability and integrity while keeping the final capsule size small and patient-friendly.
Solution Approach 2:
The granulation process enables pimavanserin to self-form stable granules with appropriate flow and packing properties without requiring external binders or additives. The material essentially serves itself, forming stable dosage forms through the granulation process alone, thereby avoiding size increase from additional agents.
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
This approach enables reproducible and accurate filling of small-sized capsules at high production speeds, enhancing patient compliance and manufacturing efficiency while maintaining product quality and stability.
Implementation Method 1
adding water to pimavanserin or a pharmaceutically acceptable salt thereof, and granulating pimavanserin or a pharmaceutically acceptable salt thereof with the water
Implementation Method 2
drying the granulated pimavanserin or a pharmaceutically acceptable salt thereof
Data Source
AI summary
Provided herein are capsules containing pimavanserin, processes for manufacturing said capsule, and pharmaceutical compositions containing pimavanserin.