Pancreatic Lipase Inhibitor Composition with Natural Extracts

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Solution Overview

Problem

Current pancreatic lipase inhibitors, such as tetrahydrolipostatin, have significant gastrointestinal side effects and potential organ toxicity, along with diminishing efficacy over time and increased appetite, leading to tachyphylaxis and compromised weight loss potential.

Innovation Solution

A composition comprising Coleus forskohlii extract, Salacia reticulata extract, and Sesamum indicum extract, which safely and effectively inhibits pancreatic lipase, administered in nutritionally and pharmacologically effective amounts to control digestive fatty acid accumulation and body weight.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If tetrahydrolipostatin is used to inhibit pancreatic lipase, then weight loss is achieved, but gastrointestinal side effects occur

Engineering Contradiction:

Improveweight lossVSAvoidgastrointestinal side effects

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent uses a composite formulation combining orlistat with multiple natural extracts (Salacia reticulata, Caralluma fimbriata, Gymnema sylvestre, and/or Trigonella foenum-graecum) to create a synergistic composition that maintains weight loss efficacy while reducing gastrointestinal side effects through the complementary properties of each component

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The natural extracts serve as intermediaries that modulate the action of orlistat, providing gastroprotective effects and reducing direct irritation to the gastrointestinal tract while maintaining the lipase inhibition mechanism for weight loss

Inventive Principle:

Principle #24Intermediary (Mediator)

2Productivity

If tetrahydrolipostatin is used to inhibit pancreatic lipase, then dietary fat digestion is blocked, but organ toxicity occurs

Engineering Contradiction:

Improvefat digestion blockingVSAvoidorgan toxicity

Core Design Contradiction:

ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent formulates orlistat with multiple natural extracts that have hepatoprotective and nephroprotective properties, creating a composite composition that reduces organ toxicity while maintaining fat digestion blocking capability

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent converts the potentially harmful effect of complete lipase inhibition into a beneficial controlled inhibition by using natural extracts that modulate the intensity and duration of lipase blocking, preventing excessive fat malabsorption that leads to organ toxicity

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

3Productivity

If tetrahydrolipostatin is used for prolonged treatment, then initial weight loss is achieved, but efficacy diminishes due to tachyphylaxis

Engineering Contradiction:

Improveweight lossVSAvoiddrug efficacy duration

Core Design Contradiction:

ProductivityVSDuration of action of moving object

Solution Approach 1:

The patent creates a formulation where the natural extracts provide sustained modulation of lipase inhibition, ensuring continuous effective action without tachyphylaxis by maintaining optimal inhibition levels throughout prolonged treatment periods

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The patent uses natural extracts that dynamically adjust lipase inhibition based on physiological conditions, providing adaptive control that prevents tolerance development and maintains efficacy throughout prolonged treatment

Inventive Principle:

Principle #15Dynamics

4Productivity

If tetrahydrolipostatin is used to inhibit pancreatic lipase, then caloric intake is reduced, but appetite increases

Engineering Contradiction:

Improvecaloric intake reductionVSAvoidincreased appetite

Core Design Contradiction:

ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent combines orlistat with natural extracts that have appetite suppressant properties, creating a composite formulation that simultaneously reduces caloric intake through lipase inhibition and controls appetite through the additional components

Inventive Principle:

Principle #40Composite materials

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 safely inhibits pancreatic lipase, reducing visceral and liver fat, body weight, appetite, and caloric intake, while preventing tachyphylaxis, without the side effects associated with existing inhibitors.

Implementation Method 1

Blocking the mechanisms of dietary fat digestion and absorption has been utilized in management of obesity. Inhibition of PTL activity with tetrahydrolipostatin (Orlistat/Xenical)

Methodology Applied

Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS9278117B2Composition and method for the safe and effective inhibition of pancreatic lipase in mammals

Publication Date: 2016.03.08 BIO ACTIVES JAPAN

AI summary

Provided are a composition and method for the safe and effective inhibition of pancreatic lipase in humans and other mammals. Provided is a composition which contains extracts of one or more of Coleus forskohlii, Salacia reticulata, and Sesamum indicum, and which is administered orally to humans and other mammals in a nutritionally or pharmacologically effective amount. Further provided is a method for producing said composition.