Cefdinir Capsule Formulation for Enhanced Dissolution Rate
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Solution Overview
Problem
Cefdinir's low solubility and dissolution rate limit its bioavailability due to its water-insoluble nature, requiring improved formulations to enhance solubility and dissolution rates.
Innovation Solution
A pharmaceutical formulation of cefdinir or its pharmaceutically acceptable salt with an average particle size of 10 µm, using calcium carboxymethyl cellulose, polyoxyethylene stearate, colloidal silicone dioxide, and magnesium stearate, prepared through wet granulation and encapsulation, optimizing the weight proportions of cefdinir to calcium carboxymethyl cellulose within specific ranges.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If cefdinir is used in conventional formulations, then the formulation is stable and manufacturable, but the dissolution rate and bioavailability are low due to water-insolubility
Solution Approach 1:
The cefdinir is ground into fine particles with an average size of 10 µm or less, dividing the drug into smaller segments that increase the total surface area available for dissolution, thereby improving the dissolution rate while maintaining stability
Solution Approach 2:
The patent changes the particle size parameter of cefdinir from conventional larger sizes to 10 µm or less, and optimizes the ratio of calcium carboxymethyl cellulose to cefdinir (3:17 to 5:12 by weight), transforming the physical parameters to achieve improved dissolution rate and bioavailability
2Speed
If cefdinir particle size is reduced to improve dissolution rate, then the dissolution rate increases, but the manufacturing complexity increases due to wet granulation requirements
Solution Approach 1:
Calcium carboxnymethyl cellulose is used as a binder and intermediary material in the wet granulation process, facilitating the formation of uniform granules from fine cefdinir particles while maintaining the benefits of reduced particle size and improving manufacturability
Solution Approach 2:
The patent creates a composite formulation combining cefdinir (3-85% by weight) with calcium carboxymethyl cellulose (15-97% by weight) in specific ratios, where the composite structure provides both the dissolution rate benefits of fine particles and the manufacturing advantages of granulated formulations
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 significantly enhances the solubility and dissolution rate of cefdinir, leading to improved bioavailability and effective treatment of various infections, with optimal results achieved using 44.25 to 60 mg of calcium carboxymethyl cellulose.
Implementation Method 1
a method for preparing a pharmaceutical formulation, this method comprising the steps of a. adding calcium carboxymethyl cellulose and polyoxyethylene stearate to cefdinir and mixing the resulting mixture, b. forming wet granulation with alcohol and water
Implementation Method 2
A preferred embodiment according to the present invention further comprises polyoxyethylene stearate, as a surface active agent
Implementation Method 3
A preferred embodiment according to the present invention further comprises colloidal silicone dioxide, as a glidant
Implementation Method 4
A preferred embodiment according to the present invention further comprises magnesium stearate, as a lubricant
Data Source
AI summary
The present invention relates to formulations of cefdinir or a pharmaceutically acceptable salt of cefdinir. The present invention provides a pharmaceutically formulation in the form of a capsule, comprising a pharmaceutically acceptable salt or polymorph of cefdinir, which is wet-granulated and has an average particle size of 10 µm at most, and calcium carboxymethyl cellulose.