Controlled-Release Vitamin D Therapy for Secondary Hyperparathyroidism

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Solution Overview

Problem

Current Vitamin D supplements for treating secondary hyperparathyroidism in CKD patients are ineffective due to rapid surges in blood Vitamin D levels, leading to decreased systemic bioavailability, aberrations in calcium and phosphorus homeostasis, and over suppression of PTH secretion, which are not adequately addressed by existing therapies.

Innovation Solution

Administering both Vitamin D repletion and Vitamin D hormone replacement therapies in controlled release formulations to maintain blood concentrations of 25-hydroxyvitamin D above 30 ng/mL and 1,25-dihydroxyvitamin D within normal physiological ranges, using predominantly 25-hydroxyvitamin D3 to prevent hypercalcemia and hyperphosphatemia, and manage plasma iPTH levels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If Vitamin D supplements are administered to treat secondary hyperparathyroidism, then blood Vitamin D levels increase, but rapid surges occur leading to decreased systemic bioavailability and aberrations in calcium and phosphorus homeostasis

Engineering Contradiction:
Improveblood Vitamin D levelsVSAvoidsystemic bioavailability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent employs periodic, controlled-release administration of Vitamin D compounds to deliver sustained low-dose therapy rather than single high-dose bolus administration. This periodic action maintains stable blood concentrations over time, preventing the rapid surges that cause decreased bioavailability and metabolic aberrations.

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The invention uses dynamic controlled-release formulations that adjust the release rate of Vitamin D to maintain optimal blood concentrations. This dynamic approach allows the therapy to adapt to the patient's metabolic needs, ensuring reliable systemic bioavailability while avoiding toxic accumulation.

Inventive Principle:
Principle #15Dynamics

2Quantity of substance

If high doses of Vitamin D are administered to raise blood levels, then 25-hydroxyvitamin D concentrations increase, but this causes over suppression of PTH secretion and hypercalcemia

Engineering Contradiction:
Improve25-hydroxyvitamin D concentrationVSAvoidover suppression of PTH and hypercalcemia
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The patent changes the dosing parameters from high single doses to lower frequent doses, and modifies the release kinetics parameter of Vitamin D administration. This parameter optimization achieves the desired 25-hydroxyvitamin D concentration threshold (>30 ng/mL) while maintaining PTH suppression within therapeutic ranges and preventing hypercalcemia.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The controlled-release formulations incorporate feedback mechanisms where the release rate of Vitamin D is regulated based on maintaining target blood concentration ranges. This feedback control prevents both under-dosing (ineffective PTH suppression) and over-dosing (hypercalcemia and excessive PTH suppression).

Inventive Principle:
Principle #23Feedback

3Quantity of substance

If conventional Vitamin D therapy is used, then PTH levels may be suppressed, but calcium and phosphorus homeostasis becomes aberrant

Engineering Contradiction:
ImprovePTH suppressionVSAvoidcalcium and phosphorus homeostasis
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The sustained periodic administration of controlled-release Vitamin D formulations maintains stable blood concentrations that reliably suppress PTH while simultaneously maintaining normal calcium and phosphorus homeostasis. The periodic low-dose delivery prevents the metabolic disruptions caused by intermittent high-dose therapy.

Inventive Principle:
Principle #19Periodic action

Data Source

PatentUS11452734B2Method of treating and preventing secondary hyperparathyroidism
Publication Date: 2022.09.27 EIRGEN PHARMA LTD

AI summary

The method of treating elevated blood levels of iPTH by increasing or maintaining blood concentrations of both 25-hydroxyvitamin D and 1,25-dihydroxyvitamin D in a patient by administering, as necessary, both Vitamin D repletion and Vitamin D hormone replacement therapies, is disclosed. The blood concentrations of 25-hydroxyvitamin D are increased to and maintained at or above 30 ng/mL, and blood concentrations of 1,25-dihydroxyvitamin D are increased to or maintained within a patient's normal historical physiological range for 1,25-dihydroxyvitamin D without causing substantially increased risk of hypercalcemia, hyperphosphatemia or over suppression of plasma iPTH in the patient. The blood levels of 25-hydroxyvitamin D are maintained at or above 30 ng/mL between doses of Vitamin D repletion therapies, and the blood levels of 1,25-dihydroxyvitamin D are maintained in the patient's normal historical physiological range between doses of Vitamin D hormone replacement therapies. In one aspect, the disclosure includes methods wherein the blood concentration of 25-hydroxyvitamin D during treatment comprises predominantly 25-hydroxyvitamin D3, and/or wherein the method includes administering predominantly or solely 25-hydroxyvitamin D3 for 25-hydroxyvitamin D repletion and/or maintenance.