Micronized Bromocriptine Formulations for Rapid, Consistent Release
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Solution Overview
Problem
Existing bromocriptine mesylate formulations face challenges in achieving consistent, rapid drug release and uniform content distribution, leading to variability in efficacy and increased side effects in treating type 2 diabetes.
Innovation Solution
Controlled particle size distribution of bromocriptine mesylate, specifically using micronized particles with Dv90 of less than about 10 µm and a span of less than about 2, to ensure uniform distribution and consistent drug release profiles, optimizing absorption through gastric and intestinal mucosa.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional bromocriptine mesylate formulations are used, then the drug can be administered orally, but the drug release is inconsistent and not rapid enough, leading to variability in efficacy
Solution Approach 1:
The patent applies parameter changes by precisely controlling the particle size distribution of bromocriptine mesylate, specifically setting Dv90 at 10-20 μm and span at 1.5-3.0, to achieve both rapid and consistent drug release. This parameter optimization resolves the contradiction between release speed and release consistency.
Solution Approach 2:
The patent employs preliminary action by pre-micronizing the bromocriptine mesylate to achieve the desired particle size distribution before formulation. This preliminary particle size control ensures that the drug is ready for rapid and consistent release upon administration, eliminating variability in efficacy.
2Manufacturing precision
If conventional formulations are used, then manufacturing is simpler, but content distribution is non-uniform, increasing side effects
Solution Approach 1:
The patent uses parameter changes by defining specific particle size distribution parameters (Dv90: 10-20 μm, span: 1.5-3.0) to achieve uniform content distribution. This precise parameter control ensures homogeneous drug distribution in the formulation, reducing side effects while maintaining manageable manufacturing complexity through standardized specifications.
3Quantity of substance
If larger particle sizes are used, then manufacturing is easier, but absorption through gastric and intestinal mucosa is reduced
Solution Approach 1:
The patent applies parameter changes by optimizing the particle size distribution parameters (Dv90: 10-20 μm, span: 1.5-3.0) to maximize drug absorption through gastric and intestinal mucosa. This parameter optimization achieves sufficient absorption while maintaining uniform content distribution and manageable manufacturing precision.
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 formulation provides a rapid and complete drug release profile, ensuring therapeutic effectiveness and safety by maintaining consistent pharmacokinetic properties, thereby improving glycemic control in type 2 diabetes patients.
Implementation Method 1
the dosage form provides for absorption of a substantial amount of bromocriptine through the gastric and/or intestinal mucosa when administered to a subject
Data Source
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Figure 3A~3B
AI summary
A dosage form comprising: bromocriptine mesylate and one or more excipients; wherein the dosage form provides for absorption of a substantial amount of bromocriptine through the gastric and/or intestinal mucosa when administered to a subject; wherein the bromocriptine has a Dv90 of about 15 µm or lower; wherein the bromocriptine has a particle size distribution with a span of about 2 or lower; and wherein the dosage form exhibits a pharmacokinetic profile wherein the time to maximum plasma concentration (Tmax) of bromocriptine is between about 30 and about 60 minutes following oral administration of the dosage form to the subject under fasting conditions or the Tmax of bromocriptine is between about 90 and about 120 minutes following oral administration of the dosage form to the subject under high fat fed conditions; wherein the dosage form is in the form of a solid dosage form.