Abstract
Purpose: The quasi-emulsion solvent diffusion (QESD) has evolved into an effective technique to manufacture agglomerates of API crystals. Although, the proposed technique showed benefits, such as cost effectiveness, that is considerably sensitive to the choice of a stabilizer, which agonizes from a absence of systemic understanding in this field. In the present study, the combination of different solvents and stabilizers were compared to investigate any connections between the solvents and stabilizers. Methods: Agglomerates of celecoxib were prepared by QESD method using four different stabilizers (Tween 80, HPMC, PVP and SLS) and three different solvents (methyl acetate, ethyl acetate and isopropyl acetate). The solid state of obtained particles was investigated by differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectroscopy. The agglomerated were also evaluated in term of production yield, distribution of particles and dissolution behavior. Results: The results showed that the effectiveness of stabilizer in terms of particle size and particle size distribution is specific to each solvent candidate. A stabilizer with a lower HLB value is preferred which actually increased its effectiveness with the solvent candidates with higher lipophilicity. HPMC appeared to be the most versatile stabilizer because it showed a better stabilizing effect compared to other stabilizers in all solvents used. Conclusion: This study demonstrated that the efficiency of stabilizers in forming the celecoxib agglomerates by QESD was influenced by the HLB of the stabilizer and lipophilicity of the solvents.
Highlights
Spherical crystallization technology which has been used to enlarge the size of the particles, has attracted the attention of pharmaceutical industry in the last decades, where small crystals are often produced by crystallization but their handing out is very difficult and costly
The results showed that the effectiveness of stabilizer in terms of particle size and particle size distribution is specific to each solvent candidate
In order to cut down the number of experiments, the emulsions were manufactured at a constant phase ratio using pure water as continuous phase and 0.1 % stabilizer in identical condition, while the influence of different stabilizers was investigated
Summary
Spherical crystallization technology which has been used to enlarge the size of the particles, has attracted the attention of pharmaceutical industry in the last decades, where small crystals are often produced by crystallization but their handing out is very difficult and costly. The technology has the capability to agglomerates the crystals directly inside the reactor where the properties of agglomerates can be controlled.[1,2,3] this method is still not widely employed in pharmaceutical industry. On shifting a temporary O/W emulsion into water, droplets solidify promptly as a result of the diffusion of the organic solvent out of the droplets to the external phase. In this method, the intermediate step of agglomeration is establishing an emulsion, which is turned into agglomerates. The combinations of 2 commonly used stabilizers (HPMC and PVP), 2 surfactants (Tween 80 and SLS) and 3 solvents (methyl acetate, ethyl acetate and isopropyl acetate) were investigated under constant processing and characterization conditions
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