Sodium Butyrate Tablets with Gastroprotective Coating
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current formulations of butyric acid tablets face issues such as unpleasant odor, rapid absorption in the upper gastrointestinal tract, and inadequate delivery to the colon, where it is needed for therapeutic and preventive action, along with challenges in industrial production due to hydrolysis and residual synthetic polymers.
Innovation Solution
A tablet design featuring a gastroprotective coating comprising an intermediate layer of hydroxypropyl cellulose, polyvinyl alcohol, and calcium carbonate, followed by an outer layer of ethyl cellulose and medium chain triglycerides, which prevents butyrate release in the stomach and ensures controlled release in the intestine, using a nebulization process in ethanol to minimize core disintegration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional gastro-resistant coating based on anionic polyacrylates is applied by spraying aqueous solution, then gastroprotection is achieved, but the sodium butyrate core disintegrates during coating application releasing butyric acid
Solution Approach 1:
The patent changes the solvent parameter from aqueous to alcoholic solution for coating application. This parameter change prevents butyric acid release during coating because the alcoholic solution does not trigger hydrolysis of sodium butyrate, eliminating the harmful odor and core disintegration while maintaining gastroprotective functionality.
Solution Approach 2:
The patent introduces an intermediary substance (alcoholic solution) to transfer the coating polymer onto the core without causing hydrolysis. The alcoholic solution acts as a mediator that allows coating application without triggering the harmful chemical reaction that occurs with aqueous solutions.
2Productivity
If butyric acid tablets are administered without controlled release coating, then the tablets dissolve rapidly in the stomach, but the active ingredient is absorbed in the upper gastrointestinal tract instead of reaching the colon
Solution Approach 1:
The patent segments the dissolution process into two distinct phases: rapid disintegration of the tablet core in the stomach to release the coated granules, followed by controlled dissolution of the gastro-resistant coating in the intestine. This segmentation ensures the active ingredient is released at the right location (colon) while maintaining appropriate dissolution kinetics.
Solution Approach 2:
The patent uses a flexible gastro-resistant coating film that remains intact in the acidic stomach environment but dissolves in the more neutral intestinal environment. This thin film acts as a selective barrier that protects the core during gastric passage while allowing release in the target location.
3Manufacturing precision
If aqueous solution is used for coating application, then the coating can be applied uniformly, but sodium butyrate hydrolyzes releasing butyric acid causing bad odor and equipment contamination
Solution Approach 1:
The patent changes the solvent parameter from water to alcohol in the coating solution. This parameter change maintains the ability to apply uniform coating while eliminating the hydrolysis reaction that produces butyric acid, thus preventing bad odor and equipment contamination during manufacturing.
4Reliability
If conventional coating materials are used, then gastroprotection is provided, but the synthetic polymers are difficult to remove from the body and can accumulate in liver and kidneys
Solution Approach 1:
The patent uses coating materials (cellulose derivatives and fats/oils) that are homogeneous with natural bodily substances. These materials are biocompatible and can be naturally metabolized and eliminated by the body, eliminating the harmful accumulation effect associated with synthetic polymers while maintaining gastroprotective function.
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 coating effectively prevents butyrate release in gastric conditions, allowing for complete dissolution at intestinal pH within 8 hours, ensuring effective therapeutic action while reducing equipment contamination and production time.
Implementation Method 1
The coating effectively prevents butyrate release in gastric conditions, allowing for complete dissolution at intestinal pH within 8 hours
Implementation Method 2
using a nebulization process in ethanol to minimize core disintegration
Implementation Method 3
using a nebulization process in ethanol to minimize core disintegration
Implementation Method 4
ensures controlled release in the intestine
Implementation Method 5
allowing for complete dissolution at intestinal pH within 8 hours
Data Source
AI summary
Coated tablets containing as active ingredient butyric acid, a pharmaceutically acceptable salt thereof, or a mixture of both, comprising a core in which said active ingredient is dispersed and a gastroprotective coating wherein said gastroprotective coating comprises or consists of: A) An intermediate coating or pre-coating that wraps the core and is in contact with the latter and said coating A) comprises or consists of: a) A film-forming polymer selected from hydroxypropyl cellulose and polyvinyl alcohol; b) A plasticizer chosen from polyethylene glycol, glycerol; c) An opacifying agent selected from calcium carbonate, titanium dioxide; d) An antiadhesive agent selected from talc, magnesium stearate, calcium stearate, stearic acid, microcrystalline cellulose; B) An outer coating wrapping said intermediate coating or pre-coating A) comprising or consisting of the following components: e) A film-forming polymer selected from ethyl cellulose or shellac; f) A plasticizer selected from: triglycerides of medium chain fatty acids, triethyl citrate g) A thickening agent selected from: sodium alginate, corn starch; h) A lubricating agent selected from oleic acid, stearic acid or salts thereof.