Biphasic Oseltamivir Formulation for Sustained Plasma Concentration

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Solution Overview

Problem

Conventional oseltamivir phosphate formulations face challenges with time delays in absorption and reduced bioavailability, leading to poor clinical efficacy and patient compliance due to the need for frequent dosing and potential adverse reactions from burst releases.

Innovation Solution

A biphasic or multiphase oseltamivir formulation with a combination of immediate-release and sustained-release components, optimized to maintain effective plasma concentrations for at least 24 hours, using materials like cellulose acetate and methacrylic acid-ethyl acrylate copolymers to control release rates and minimize peak-to-valley fluctuations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If immediate-release formulation is used, then rapid absorption and quick onset of action are achieved, but frequent dosing is required which reduces patient compliance

Engineering Contradiction:

Improveabsorption speedVSAvoiddosing frequency

Core Design Contradiction:

SpeedVSEase of operation

Solution Approach 1:

The formulation is segmented into multiple functional components: an immediate-release portion containing oseltamivir phosphate and a sustained-release portion containing oseltamivir phosphate combined with a sustained-release material. This segmentation allows the immediate-release portion to provide rapid absorption for quick onset of action, while the sustained-release portion maintains effective plasma concentrations over extended periods, thereby reducing dosing frequency and improving patient compliance.

Inventive Principle:

Principle #1Segmentation

2Ease of operation

If sustained-release formulation is used, then dosing frequency is reduced, but time delay in absorption occurs which may miss optimal treatment window

Engineering Contradiction:

Improvedosing frequencyVSAvoidabsorption time delay

Core Design Contradiction:

Ease of operationVSLoss of time

Solution Approach 1:

Inventive Principle:

Principle #1Segmentation

3Ease of operation

If sustained-release formulation is used, then dosing frequency is reduced, but bioavailability is reduced leading to poor therapeutic effect

Engineering Contradiction:

Improvedosing frequencyVSAvoidtherapeutic efficacy

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The formulation employs composite materials by combining oseltamivir phosphate with specific sustained-release materials such as ethyl cellulose, cellulose acetate, or methacrylic acid-ethyl acrylate copolymers. These composite materials enable controlled release kinetics that maintain bioavailability while extending the duration of action, ensuring reliable therapeutic efficacy with reduced dosing frequency.

Inventive Principle:

Principle #40Composite materials

4Speed

If sustained-release formulation is used to achieve rapid onset, then burst release occurs which prevents long-term therapeutic effect

Engineering Contradiction:

Improveonset of actionVSAvoidtherapeutic duration

Core Design Contradiction:

SpeedVSDuration of action of stationary object

Solution Approach 1:

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The formulation utilizes parameter changes by controlling the release rate through specific sustained-release materials and their combinations. The release rate is optimized to prevent burst release while maintaining rapid onset of action, ensuring both quick therapeutic effect and long-term sustained concentrations through controlled release kinetics.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20220354816A1Oseltamivir formulation

Publication Date: 2022.11.10 SUNSHINE LAKE PHARMA CO LTD

AI summary

An oseltamivir formulation and a preparation method of the formulation, the method being simple to operate, having good reproducibility, and being suitable for manufacture. The oseltamivir formulation includes oseltamivir or a salt thereof and a sustained-release material. The formulation may be a single-phase release formulation, a dual-phase release formulation, a three-phase release formulation, or a multi-phase release formulation having more than three phases. The formulation is administered once-daily and can achieve sustained release of at least 24 hours or longer, which can reduce the times of administration and avoid peak-to-valley fluctuations, thereby improving the compliance and safety of patients.