Lanthanum Carbonate Capsule Formulation for CKD

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Solution Overview

Problem

Patients with chronic kidney disease (CKD) face challenges with existing lanthanum carbonate formulations, including difficulty in administration and variability in dissolution rates, which affect phosphate binding consistency and patient compliance.

Innovation Solution

Development of oral pharmaceutical capsules and powders containing lanthanum carbonate or lanthanum carbonate hydrate with a gelatin shell and additional excipients like talc, which maintain consistent dissolution rates and pharmacokinetic properties, allowing for flexible administration and improved compliance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If lanthanum carbonate chewable tablets are used to treat hyperphosphatemia, then phosphate binding effect is achieved, but patient compliance deteriorates due to difficulty in chewing and unpalatable taste

Engineering Contradiction:

Improvephosphate binding effectVSAvoidpatient compliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent transforms the physical form of lanthanum carbonate from chewable tablets to capsule formulations, changing the administration parameters to eliminate chewing requirements and improve palatability while preserving the phosphate binding therapeutic effect

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces capsule shells and excipients as intermediary carriers to deliver lanthanum carbonate in a form that is easier to administer, mediating between the active ingredient and patient acceptance

Inventive Principle:

Principle #24Intermediary (Mediator)

2Duration of action of stationary object

If lanthanum carbonate formulations are stored, then shelf life is extended, but dissolution rate variability increases affecting phosphate binding consistency

Engineering Contradiction:

Improveshelf lifeVSAvoiddissolution rate consistency

Core Design Contradiction:

Duration of action of stationary objectVSStability of the object's composition

Solution Approach 1:

The patent performs preliminary encapsulation of lanthanum carbonate in gelatin shells with specific excipients before storage, preparing the formulation in advance to maintain dissolution rate consistency throughout the shelf life period

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent creates composite capsule formulations combining lanthanum carbonate with gelatin shells and specific excipients (such as talc and magnesium stearate), where the composite structure protects the active ingredient and maintains consistent dissolution properties during storage

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS9023397B2Capsule and powder formulations containing lanthanum compounds

Publication Date: 2015.05.05 TAKEDA PHARMA CO LTD

AI summary

The present invention includes an oral pharmaceutical capsule comprising a shell, lanthanum carbonate or lanthanum carbonate hydrate, and a lubricant such as talc, wherein the shell encapsulates the lanthanum carbonate or its hydrate and the lubricant. Capsule shells comprise, for example, gelatin. The present invention also includes an oral pharmaceutical powder comprising lanthanum carbonate or lanthanum carbonate hydrate and a pharmaceutically acceptable excipient. The oral pharmaceutical capsules and powders of the present invention can be administered to treat a patient at risk of or suffering from hyperphosphatemia, at risk of or suffering from chronic kidney disease (CKD), at risk of or suffering from soft tissue calcification associated with CKD, or at risk of or suffering from secondary hyperparathyroidism.