scholarly journals Use of supercritical CO2 -aided and conventional melt extrusion for enhancing the dissolution rate of an active pharmaceutical ingredient

2011 ◽  
Vol 23 (5) ◽  
pp. 909-918 ◽  
Author(s):  
Zsombor Kristóf Nagy ◽  
Martial Sauceau ◽  
Katalin Nyúl ◽  
Elisabeth Rodier ◽  
Balázs Vajna ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Supercritical Co2 ◽  
Active Pharmaceutical Ingredient ◽  
Melt Extrusion

scholarly journals Preparation of Hot-Melt Extruded Dosage Form for Enhancing Drugs Absorption Based on Computational Simulation

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 757
Author(s):  
Sung-Min Choi ◽  
Sung-Hoon Lee ◽  
Chin-Yang Kang ◽  
Jun-Bom Park
Keyword(s):  
Gastrointestinal Tract ◽  
Dissolution Rate ◽  
Computational Simulation ◽  
Active Pharmaceutical Ingredient ◽  
Hot Melt Extrusion ◽  
Optimization Approach ◽  
Melt Extrusion ◽  
Hot Melt ◽  
Pbpk Simulation

The aim of this study was to control the dissolution rate and permeability of cilostazol. To enhance the dissolution rate of the active pharmaceutical ingredient (API), hot-melt extrusion (HME) technology was applied to prepare a solid dispersion (SD). To control permeability in the gastrointestinal tract regardless of food intake, the HME process was optimized based on physiologically based pharmacokinetic (PBPK) simulation. The extrudates were produced using a laboratory-scale twin-screw hot-melt extruder with co-rotatory screws and a constant feeding rate. Next, for PBPK simulation, parameter-sensitive analysis (PSA) was conducted to determine the optimization approach direction. As demonstrated by the dissolution test, the solubility of extrudate was enhanced comparing cilostazol alone. Based on the PSA analysis, the surfactant induction was a crucial factor in cilostazol absorption; thus, an extrudate with an even distribution of lipids was produced using hot-melt extrusion technology, for inducing the bile salts in the gastrointestinal tract. In vivo experiments with rats demonstrated that the optimized hot-melt extruded formulation was absorbed more rapidly with lower deviation and regardless of the meal consumed when compared to marketed cilostazol formulations.

scholarly journals Improving Nefiracetam Dissolution and Solubility Behavior Using a Cocrystallization Approach

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 653 ◽  
Author(s):  
Xavier Buol ◽  
Koen Robeyns ◽  
Camila Caro Garrido ◽  
Nikolay Tumanov ◽  
Laurent Collard ◽  
...  
Keyword(s):  
Citric Acid ◽  
Oxalic Acid ◽  
Dissolution Rate ◽  
Zinc Chloride ◽  
Active Pharmaceutical Ingredient ◽  
Water Soluble ◽  
Solubility Behavior

In this work, we are the first to identify thirteen cocrystals of Nefiracetam, a poor water-soluble nootropic compound. Three of which were obtained with the biocompatible cocrystallization agents citric acid, oxalic acid, and zinc chloride. These latter have been fully structurally and physically characterized and the solubility, dissolution rate, and stability were compared to that of the initial Active Pharmaceutical Ingredient (API).

scholarly journals Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide

Crystals ◽  
2018 ◽  
Vol 8 (9) ◽  
pp. 336 ◽  
Author(s):  
Muhammad Inam ◽  
Jiajia Wu ◽  
Jie Shen ◽  
Chi Phan ◽  
Guping Tang ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Dissolution Rate ◽  
Acidic Medium ◽  
Active Pharmaceutical Ingredient ◽  
Free Drug ◽  
Crystalline Material ◽  
In Vitro Dissolution ◽  
Crystallization Method

Two new co-crystals, Ticagrelor with Nicotinamide, have been prepared with improved solubility. Because Ticalegor has a poor solubility and dissolution rate, a novel co-crystallization method with structurally homogenous crystalline material, an active pharmaceutical ingredient (API), and co-former indefinite stoichiometric amount has been made to improve Ticagrelor’s solubility. The co-crystal of Ticagrelor (TICA) with Nicotinamide (NCA) was prepared in ratio (1:1) and confirmed by FTIR, DSC, and XRD characterization. Furthermore, the single crystal structure of TICA-NCA hydrate was analyzed. The solubility of co-crystals was investigated in pH 2 acidic medium, which was a significant improvement as compared to the solubility of a free drug. The in vitro dissolution rate of co-crystal was larger than that of the commercial product.

scholarly journals Experimental study on the dissolution of supercritical CO2 in PS under different agitators

e-Polymers ◽  
2021 ◽  
Vol 21 (1) ◽  
pp. 443-452
Author(s):  
Long Wang ◽  
Xingyuan Huang ◽  
Haifeng Liang
Keyword(s):  
Experimental Study ◽  
Dissolution Rate ◽  
Supercritical Co2 ◽  
Polymer Melt ◽  
Static Condition ◽  
Bubble Nucleation ◽  
Homogeneous Body ◽  
Different Temperatures ◽  
Short Time ◽  
Nucleation Bubble

Abstract In the continuous molding of microporous plastics, the polymer/CO2 homogeneous body needs to be formed in a very short time, which affects the subsequent bubble nucleation, bubble pore distribution, and growth, and is the key to the molding. It is known that the formation time of homogeneous body is shortened during the continuous molding of microporous plastics because of the agitator’s effect. However, different agitators have different effects on the dissolution rate. So, it is necessary to study not only the dissolution of gas in polymer melt under static condition but also the dissolution under the action of the agitator. In this article, the solubility and dissolution rate of supercritical CO2 in polymer melt PS at different temperatures and pressures were experimentally investigated under conical and screw agitators, and the numerical solution was also carried out.

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