Lurasidone Hydrochloride Tablet Composition for Fast Dissolution
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Solution Overview
Problem
Existing lurasidone hydrochloride pharmaceutical compositions face challenges with low solubility and disintegration, particularly when using high concentrations, and are not suitable for lactose-intolerant patients due to high lactose content, with processing issues arising from its sticky nature.
Innovation Solution
A solid oral pharmaceutical composition comprising lurasidone hydrochloride with specific ratios of pregelatinized starch, polyvinylpyrrolidone, microcrystalline cellulose, croscarmellose sodium, mannitol, and magnesium stearate, along with a film coating, to enhance dissolution and disintegration profiles and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If high concentration of lurasidone hydrochloride is used in the pharmaceutical composition, then the therapeutic efficacy is improved, but the solubility and dissolution profile deteriorate
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by using micronized lurasidone hydrochloride (reducing particle size), adjusting pH with buffers (phosphate, citrate, acetate), and optimizing excipient ratios to improve solubility and dissolution at high drug concentrations
Solution Approach 2:
The patent creates a composite pharmaceutical formulation combining lurasidone hydrochloride with multiple excipients including pregelatinized starch, croscarmellose sodium, microcrystalline cellulose, and various buffers to achieve both high drug concentration and improved dissolution profile
2Reliability
If pregelatinized starch is used as binder and disintegrant, then the disintegration and dissolution profiles are improved, but the tablet weight and volume increase
Solution Approach 1:
The patent optimizes the ratio of pregelatinized starch to other excipients and adjusts its particle size distribution to achieve maximum disintegration efficiency at lower concentrations, reducing the overall tablet weight while maintaining improved disintegration profile
3Strength
If lactose monohydrate is used as binder, then the tablet integrity is improved, but the suitability for lactose-intolerant patients deteriorates
Solution Approach 1:
The patent removes lactose monohydrate from the formulation and replaces it with lactose-free alternatives such as pregelatinized starch, microcrystalline cellulose, and crosslinked polyvinyl pyrrolidone, thereby maintaining tablet integrity while making the product suitable for lactose-intolerant patients
Solution Approach 2:
The patent uses excipients like pregelatinized starch and microcrystalline cellulose that can serve multiple functions (binder, disintegrant, filler) without containing lactose, making the formulation universally suitable for all patients including those with lactose intolerance
4Reliability
If micronized lurasidone hydrochloride is used to improve solubility, then the dissolution profile is improved, but the processing difficulty increases due to sticky nature
Solution Approach 1:
The patent uses spray-dried micronized lurasidone hydrochloride as an intermediary form that maintains the solubility benefits of micronization while the spray-drying process removes moisture that causes stickiness, facilitating easier processing
Solution Approach 2:
The patent changes the moisture content and physical state of micronized lurasidone hydrochloride through spray-drying, transforming it from a sticky wet powder to a free-flowing dry powder that is easier to process while retaining the enhanced dissolution properties
Data Source
AI summary
The present invention relates to pharmaceutical compositions, which provide a better dissolution and disintegration profile, comprising lurasidone hydrochloride with at least one binder and one or more other pharmaceutically acceptable excipient.