Manufacturing strategies to develop amorphous solid dispersions: An overview

Abstract

Since the past several decades, poor water solubility of existing and new drugs in the pipeline have remained a challenging issue for the pharmaceutical industry. Literature describes several approaches to improve the overall solubility, dissolution rate, and bioavailability of drugs with poor water solubility. Moreover, the development of amorphous solid dispersion (SD) using suitable polymers and methods have gained considerable importance in the recent past. In the present review, we attempt to discuss the important and industrially scalable thermal strategies for the development of amorphous SD. These include both solvent (spray drying and fluid bed processing) and fusion (hot melt extrusion and KinetiSol®) based techniques. The current review also provides insights into the thermodynamic properties of drugs, their polymer miscibility and solubility, and their molecular dynamics to develop stable and more efficient amorphous SD.

Direct Powder Extrusion 3D Printing of Praziquantel to Overcome Neglected Disease Formulation Challenges in Paediatric Populations

“…This proves that 3DP can be a highly valuable technology for producing personalised pharmaceutical dosage forms to improve physical and sensory properties necessary for a large variety of medicines. The combination of HME and 3DP techniques could be useful to overcome challenges in the formulation development of BCS class II drugs with low solubility, which represent more than 70% of new drug candidates in the pipeline [ 62 ].…”

“…This proves that 3DP can be a highly valuable technology for producing personalised pharmaceutical dosage forms to improve physical and sensory properties necessary for a large variety of medicines. The combination of HME and 3DP techniques could be useful to overcome challenges in the formulation development of BCS class II drugs with low solubility, which represent more than 70% of new drug candidates in the pipeline [62]. It is known from the drug-polymer composition-temperature previously determined by the authors (data not shown) that, at room temperature, 35 wt% PZQ in KOL corresponds to a supersaturated amorphous binary system.…”

Solid Dispersion as a Technical Solution to Boost the Dissolution Rate and Bioavailability of Poorly Water-Soluble Drugs

“…The fluid bed coating was recently introduced as an effective technique that involves loading the drug/ carrier mixture on inactive pellets evaporated by flowing air. 78,79 This method can be industrially employed since it is readily flowable for encapsulation and tableting.…”

Applicability of an Experimental Grade of Hydroxypropyl Methylcellulose Acetate Succinate as a Carrier for Formation of Solid Dispersion with Indomethacin

“…The preparation of solid dispersions has been achieved by various methods such as evaporation of a solution, ball milling, spray drying of a solution and hot-melt extrusion (HME) [ 17 , 26 ]. Since environmental concerns have increased recently, HME may be employed more frequently as a solvent-free manufacturing process [ 27 ].…”