Magnesium Lactate Granules for High-Loading Controlled Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Conventional magnesium oral dosage forms face challenges in achieving high bioavailability, high drug load, and controlled release characteristics, leading to inadequate magnesium absorption in patients with deficiencies, particularly due to poor compressibility and inadequate targeting of magnesium release in the digestive tract.
Innovation Solution
Development of high-loading, controlled-release dosage forms comprising magnesium lactate as 80-95% of the formulation, with additional components like hydroxypropyl cellulose and cross-linked acrylic acid-based polymers, which are compressed to form tablets with specific dissolution profiles ensuring sustained release, targeting the distal small intestine for optimal absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If compressibility aids are included to improve compressibility, then the material can be compressed into solid dosage forms, but the dosage level is limited
Solution Approach 1:
The patent changes the physical and chemical parameters of magnesium lactate through granulation processes, transforming it from a free-flowing powder to cohesive granules with improved compressibility. This allows high dosage levels (80-95% magnesium lactate) to be compressed into solid tablets without requiring large amounts of compressibility aids, thereby resolving the contradiction between manufacturability and dosage level.
Solution Approach 2:
The patent creates composite granules by combining magnesium lactate with specific excipients in controlled ratios. The composite structure leverages the properties of each component: magnesium lactate provides the active ingredient and bulk, while the excipients (present in optimized amounts) provide cohesion and compressibility. This composite approach enables high drug loading while maintaining manufacturability.
2Duration of action of moving object
If controlled release materials are included to delay release, then magnesium release is controlled, but the dosage level is limited
Solution Approach 1:
The patent modifies the release characteristics of magnesium lactate by controlling the physical state and surface properties of the granules. Through granulation and coating processes, the patent creates a controlled release profile where magnesium is released gradually over time. This allows high dosage levels to be maintained while achieving controlled release, as the release rate is controlled by the granule structure rather than by diluting the active ingredient.
3Reliability
If magnesium salts with high bioavailability are used to improve absorption, then intracellular magnesium levels can be achieved, but the materials exhibit poor compressibility
Solution Approach 1:
The patent applies granulation technology to change the physical parameters of high-bioavailability magnesium salts like magnesium lactate. The granulation process creates cohesive granules with improved compressibility while preserving the high bioavailability properties of the magnesium salt. This parameter transformation allows the material to be manufactured into solid dosage forms without sacrificing absorption efficacy.
Solution Approach 2:
The patent introduces granulation excipients as intermediaries that facilitate the transformation of magnesium lactate from a difficult-to-compress powder to a compressible granular form. These intermediaries act as binders and structure-building agents, enabling the high-bioavailability magnesium salt to be processed into manufacturable solid dosage forms while maintaining its therapeutic properties.
4Quantity of substance
If conventional magnesium dosage forms are used to treat deficiencies, then magnesium supplementation is provided, but absorption is inadequate in patients with deficiencies
Solution Approach 1:
The patent optimizes the physical parameters of magnesium lactate through granulation, creating granules with controlled surface area, porosity, and dissolution characteristics. These parameter changes enhance the bioavailability and absorption of magnesium in patients with deficiencies. The controlled release profile ensures sustained magnesium supplementation, improving absorption reliability while maintaining adequate magnesium levels in the body.
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 described dosage forms achieve a therapeutically effective magnesium release profile, with at least 50% of magnesium released within 6 hours and 85% by 10 hours, significantly improving magnesium absorption and addressing magnesium deficiencies effectively.
Implementation Method 1
The inclusion of controlled release materials can delay release of a drug from the tablet
Implementation Method 2
controlled-release dosage forms comprising magnesium lactate as 80-95% of the formulation... ensuring sustained release
Implementation Method 3
targeting the distal small intestine for optimal absorption
Data Source
AI summary
Disclosed are high loading, controlled-release dosage forms for oral administration of magnesium salts. For example, an oral dosage form can comprise from about 80% to about 95% magnesium lactate and one or more components. As another example, an oral dosage form can comprise at least about 50% magnesium salt and exhibit a controlled release dissolution profile. Also disclosed are methods for making controlled release dosage forms for oral administration of a therapeutically effective amount of magnesium salt to a mammal. Also disclosed are methods for treating a disorder characterized by magnesium deficiency and methods for preventing or alleviating low magnesium levels.