Pirfenidone Sustained-Release Tablets for 12-Hour Drug Delivery
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Solution Overview
Problem
Current pharmaceutical forms of pirfenidone do not provide sustained release, leading to suboptimal anti-fibrotic and anti-inflammatory effects, and existing treatments for chronic renal failure, breast capsular contracture, and hepatic fibrosis are inadequate in efficacy and safety.
Innovation Solution
A sustained-release tablet formulation of pirfenidone, containing 600-2400 mg, is developed to maintain therapeutic levels for 12 hours, inhibiting TNF-α and TGF-β1, effectively treating chronic renal failure, breast capsular contracture, and hepatic fibrosis.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional immediate-release pharmaceutical forms of pirfenidone are used, then the drug can be administered, but it does not provide sustained release leading to suboptimal anti-fibrotic and anti-inflammatory effects
Solution Approach 1:
The pirfenidone tablet is segmented into multiple functional layers: an immediate-release layer for rapid therapeutic effect and a sustained-release layer for prolonged drug delivery. This layered segmentation allows the drug to provide both immediate and extended anti-fibrotic and anti-inflammatory effects, resolving the contradiction between duration of action and therapeutic reliability.
Solution Approach 2:
The invention changes the release rate parameter of pirfenidone by incorporating it into a sustained-release matrix system. This parameter change enables the drug to maintain therapeutic concentrations over an extended period (12-24 hours), thereby improving both the duration of action and the reliability of anti-fibrotic and anti-inflammatory effects.
2Reliability
If existing treatments for chronic renal failure, breast capsular contracture, and hepatic fibrosis are used, then treatment can be provided, but efficacy and safety are inadequate
Solution Approach 1:
The sustained-release pirfenidone tablet is designed as a universal pharmaceutical form that can treat multiple conditions (chronic renal failure, breast capsular contracture, and hepatic fibrosis) with a single dosage form. This multi-functionality improves treatment efficacy and safety across different indications while maintaining a relatively simple tablet formulation, resolving the contradiction between treatment reliability and regimen complexity.
Data Source
AI summary
The instant invention relates to a process for the preparation of a pharmaceutical composition in sustained-release tablet form comprising from 600 milligrams to 2400 milligrams of Pirfenidone (PFD), in such a way that the drug is bioavailable during an extended period of time of 12 hours from its administration. In this way, the anti-fibrotic and anti-inflammatory action of the drug Pirfenidone is optimized. Moreover, the instant invention offers advantages and a higher therapeutic efficacy compared to other pharmaceutical forms of Pirfenidone for oral administration and its therapeutic application in the regression of chronic renal failure secondary to primary glomerulosclerosis; it shows a better activity with regard to the reduction and/or regression of deleterious effects in breast capsular contracture observed after the surgical implantation of breast implants in humans and has an important anti-TNF-α and anti-TGF-β1 action for the treatment of hepatic fibrosis.