Polymer-Assisted Polymorphic Transformation via Solvent-Free Hot-Melt Extrusion Platform

2016 ◽  
Author(s):  
Niamh Heron
Keyword(s):  
Polymorphic Transformation ◽  
Hot Melt Extrusion ◽  
Solvent Free ◽  
Melt Extrusion ◽  
Hot Melt

scholarly journals Development and Evaluation of Amorphous Oral Thin Films Using Solvent-Free Processes: Comparison between 3D Printing and Hot-Melt Extrusion Technologies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1613
Author(s):  
Jiaxiang Zhang ◽  
Anqi Lu ◽  
Rishi Thakkar ◽  
Yu Zhang ◽  
Mohammed Maniruzzaman
Keyword(s):  
Thin Films ◽  
3D Printing ◽  
Drug Release ◽  
Hot Melt Extrusion ◽  
Dosage Forms ◽  
Solvent Free ◽  
Melt Extrusion ◽  
Physico Chemical ◽  
3D Printed ◽  
Hot Melt

Conventional oral dosage forms may not always be optimal especially for those patients suffering from dysphasia or difficulty swallowing. Development of suitable oral thin films (OTFs), therefore, can be an excellent alternative to conventional dosage forms for these patient groups. Hence, the main objective of the current investigation is to develop oral thin film (OTF) formulations using novel solvent-free approaches, including additive manufacturing (AM), hot-melt extrusion, and melt casting. AM, popularly recognized as 3D printing, has been widely utilized for on-demand and personalized formulation development in the pharmaceutical industry. Additionally, in general active pharmaceutical ingredients (APIs) are dissolved or dispersed in polymeric matrices to form amorphous solid dispersions (ASDs). In this study, acetaminophen (APAP) was selected as the model drug, and Klucel™ hydroxypropyl cellulose (HPC) E5 and Soluplus® were used as carrier matrices to form the OTFs. Amorphous OTFs were successfully manufactured by hot-melt extrusion and 3D printing technologies followed by comprehensive studies on the physico-chemical properties of the drug and developed OTFs. Advanced physico-chemical characterizations revealed the presence of amorphous drug in both HME and 3D printed films whereas some crystalline traces were visible in solvent and melt cast films. Moreover, advanced surface analysis conducted by Raman mapping confirmed a more homogenous distribution of amorphous drugs in 3D printed films compared to those prepared by other methods. A series of mathematical models were also used to describe drug release mechanisms from the developed OTFs. Moreover, the in vitro dissolution studies of the 3D printed films demonstrated an improved drug release performance compared to the melt cast or extruded films. This study suggested that HME combined with 3D printing can potentially improve the physical properties of formulations and produce OTFs with preferred qualities such as faster dissolution rate of drugs.

scholarly journals Hot-melt extrusion and prilling as contemporary and promising techniques in the solvent free production of solid oral dosage forms, based on solid dispersions

2016 ◽  
Vol 62 (1) ◽  
pp. 3-24 ◽  
Author(s):  
Aleksandar Aleksovski ◽  
Chris Vervaet ◽  
Rok Dreu
Keyword(s):  
Drug Delivery ◽  
Hot Melt Extrusion ◽  
Dosage Forms ◽  
Solvent Free ◽  
Oral Dosage ◽  
Drug Dissolution ◽  
Melt Extrusion ◽  
Solid Oral Dosage Forms ◽  
Oral Dosage Forms ◽  
Hot Melt

Hot melt extrusion and prilling are gaining importance as solvent free and continuous techniques in the production of solid oral dosage forms with added value, by incorporating active compound in a molten carrier which is further solidified to form solid dispersion. This article reviews these two techniques in terms of understanding process basics, equipment characteristics, required properties of processed materials and application of the processes for development of solid oral dosage forms. Studies revealed that both hot-melt extrusion and prilling are regarded as simple, robust and continuous methods for processing different types of materials and production of solid dosage forms based on solid matrices. However, understanding of their concepts and requirements together with careful material selection is crucial for stable material processing and obtaining stable products of high-quality. Hot-melt extrusion proved to be a suitable method for production of modified release dosage forms, taste masked dosage forms and dosage forms offering improved drug dissolution rate and solubility. Prilling till now has been successfully applied just in the production of multiple unit drug delivery systems for immediate and sustained drug delivery. Further studies on product development and process understanding are required for full implementation of prilling in the pharmaceutical field.

scholarly journals HOT MELT EXTRUSION IN ENGINEERING OF DRUG COCRYSTALS: A REVIEW

2021 ◽  
pp. 10-19
Author(s):  
ARCHANA RAJADHYAX ◽  
UJWALA SHINDE ◽  
HARITA DESAI ◽  
SHRUSHTI MANE
Keyword(s):  
Crystal Engineering ◽  
Process Analytical Technology ◽  
Hot Melt Extrusion ◽  
Dosage Forms ◽  
Solvent Free ◽  
Water Soluble ◽  
Melt Extrusion ◽  
Pharmaceutical Dosage Forms ◽  
Free Process ◽  
Hot Melt

Crystal engineering technique has been widely explored in recent times to bring about changes in crystallinity which aids to achieve various goals such as solubility enhancement, stability and in vivo bioavailability without altering the chemical properties of the drug. Cocrystallisation is one of the crystal engineering approaches where the drug and an inert coformer are linked together by hydrogen bonding forming supramolecular homosynthon or heterosynthon using solvent-based or solvent-free techniques. Processing of active pharmaceutical ingredients with inert water-soluble coformers yields multicomponent crystalline cocrystals with high-performance characteristics and enhanced flow properties. Due to the emerging need of the industry for greener techniques, hot melt extrusion (HME), a continuous and solvent-free process is emerging as a field of interest in the mechanochemical synthesis of various pharmaceutical dosage forms such as solid dispersions, implants, ointments, and cocrystals. The current review emphasizes the role of HME as a cocrystallization technique for drugs to tailor-make their properties and ease of formulation. The distinct feature of HME is phase control during the process of cocrystallization. Furthermore, the selection of appropriate coformers with desirable water-solubility and stability features makes HME amenable to cocrystallization of versatile actives yielding suitable dosage forms. The application of process analytical technology further adds ease of monitoring during HME in cocrystallization approaches. Due to these salient features of HME, it can act as a prospective technique for cocrystallization of versatile drugs thus yielding dosage forms with desirable solubility and stability features.

scholarly journals Solid state thermomechanical engineering of high-quality pharmaceutical salts via solvent free continuous processing

2020 ◽  
Vol 22 (2) ◽  
pp. 540-549 ◽  
Author(s):  
Md Sadeque Hossain Mithu ◽  
Steven A. Ross ◽  
Bruce D. Alexander ◽  
Dennis Douroumis
Keyword(s):  
Solid State ◽  
Hot Melt Extrusion ◽  
Solvent Free ◽  
Continuous Processing ◽  
Melt Extrusion ◽  
High Quality ◽  
Pharmaceutical Salts ◽  
Hot Melt

Solvent-free, continuous processing of high-quality pharmaceutical salts through via hot-melt extrusion as an alternative to solvent based approaches.

Polymorphic Transformation of Indomethacin during Hot Melt Extrusion Granulation: Process and Dissolution Control

2018 ◽  
Vol 35 (7) ◽  
Author(s):  
Ting Xu ◽  
Kajalajit Nahar ◽  
Rutesh Dave ◽  
Simon Bates ◽  
Kenneth Morris
Keyword(s):  
Polymorphic Transformation ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Granulation Process ◽  
Hot Melt
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