scholarly journals DEVELOPMENT OF TAMOXIFEN CITRATE PELLETS BY HOT-MELT EXTRUSION FOR IMMEDIATE RELEASE: STUDY OF EFFECT OF VARIABLES

2019 ◽  
pp. 111-124
Author(s):  
VISHAL YADAV ◽  
S. SATHESH KUMAR
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Peg 6000 ◽  
Tamoxifen Citrate ◽  
Croscarmellose Sodium ◽  
Hot Melt ◽  
Mcf 7

Objective: Objective of the study was to develop tamoxifen citrate immediate release pellets by hot-melt extrusion (HME) and to study the effect of various formulation and process variables. Methods: Pellets were prepared by HME technique. Effect of various parameters such as the concentration of ethylcellulose, PEG 6000, croscarmellose sodium, and spheronization speed were studied by using Central Composite Design. Pellets were evaluated for theoretical yield (%), mean pellet size (mm), sphericity (pellips), friability (%), porosity (%), mechanical crushing force (n), and dissolution efficiency. Optimized formulation was studied for compatibility study using IR, DSC, and XRD, SEM, In vitro drug release. In vitro Cell Cytotoxicity and Viability Assay were carried out using MCF-7 (human breast cancer cells) by MTT assay. Results: Results showed that a variable such as the amount of Methyl Cellulose, PEG 6000 and Spheronization speed showed positive correlation and amount of Croscarmellose sodium showed a negative correlation with dependent variables. Optimized formulation showed Korsmeyer Peppas model as a mechanism of drug release. Value of n was found to be in between 0.77+0.04, which reveals that, release mechanism of the drug as non-Fickian transport (0.45<n<0.89). MTT results of MCF-7 cells showed that optimized immediate release pellets have maximum cytotoxicity at 80 µg/ml. Conclusion: Study concluded that HME method and materials i.e. PEG 6000 and methylcellulose can effectively use to get immediate release of tamoxifen citrate so as to increase dissolution rate and cytotoxic effect.

Application of hot-melt extrusion technology in immediate-release abuse-deterrent formulations

2017 ◽  
Vol 13 (6) ◽  
pp. 473 ◽  
Author(s):  
Klaus Wening, PhD ◽  
Sebastian Schwier, PhD ◽  
Hans-J. Stahlberg, MD ◽  
Eric Galia, PhD
Keyword(s):  
Phase 1 ◽  
White Male ◽  
Immediate Release ◽  
Hot Melt Extrusion ◽  
Pharmacokinetic Parameters ◽  
Mechanical Resistance ◽  
In Vitro Test ◽  
Melt Extrusion ◽  
Hot Melt

Objective: Hot-melt extrusion (HME) technology has been used for manufacturing extended-release abuse-deterrent formulations (ADFs) of opioid-type analgesics with improved tamper-resistant properties. Our objective was to describe application of this technology to immediate-release (IR) ADFs.Design: For development of a sample IR ADF (hydrocodone 10 mg/acetaminophen 325 mg) based on HME, feasibility studies were performed using different excipients. The formulation selected for further development was evaluated via in vitro test battery. Moreover, in vivo performance of IR ADF technologies was investigated in an open-label, randomized, cross-over, phase 1, relative oral bioavailability study with another opioid (model compound).Setting: Single-center bioavailability trial.Participants: Twenty-four healthy white male subjects.Interventions: ADF IR formulation of an opioid and marketed IR formulation.Main Outcome Measure(s): For feasibility and in vitro studies, dissolution profiles, syringeability, particle size distribution after physical manipulation, and extractability were evaluated. For the phase 1 study, pharmacokinetic parameters were evaluated and compared for ADF IR and a marketed IR formulation.Results: After manipulation, the majority of particles from the ADF IR formulation were >500 μm and, thus, not considered suitable for intranasal abuse, while the majority of particles for the reference marketed IR formulation were <500 μm. The ADF IR formulation was resistant to syringing and preparation for potential intravenous injection. In healthy subjects, pharmacokinetics of an ADF and marketed IR formulation of an opioid were nearly identical.Conclusions: Application of HME to IR formulations led to development of products with improved mechanical resistance to manipulation for intranasal or intravenous preparation, but similar bioavailability.

Mechanism of drug release from polymethacrylate-based extrudates and milled strands prepared by hot-melt extrusion

2009 ◽  
Vol 71 (2) ◽  
pp. 387-394 ◽  
Author(s):  
Jessica Albers ◽  
Rainer Alles ◽  
Karin Matthée ◽  
Klaus Knop ◽  
Julia Schulze Nahrup ◽  
...  
Keyword(s):  
Drug Release ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Hot Melt

scholarly journals Development of taste masked caffeine citrate formulations utilizing hot melt extrusion technology and in vitro–in vivo evaluations

2015 ◽  
Vol 487 (1-2) ◽  
pp. 167-176 ◽  
Author(s):  
Manjeet B. Pimparade ◽  
Joseph T. Morott ◽  
Jun-Bom Park ◽  
Vijay I. Kulkarni ◽  
Soumyajit Majumdar ◽  
...  
Keyword(s):  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Caffeine Citrate ◽  
Extrusion Technology ◽  
Hot Melt

scholarly journals Impact of Drug Loading Method on Drug Release from 3D-Printed Tablets Made from Filaments Fabricated by Hot-Melt Extrusion and Impregnation Processes

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1607
Author(s):  
Kasitpong Thanawuth ◽  
Lalinthip Sutthapitaksakul ◽  
Srisuda Konthong ◽  
Supakij Suttiruengwong ◽  
Kampanart Huanbutta ◽  
...  
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Hot Melt Extrusion ◽  
Water Soluble ◽  
Melt Extrusion ◽  
Drug Content ◽  
Loading Method ◽  
Lower Drug ◽  
3D Printed ◽  
Hot Melt

The purpose of this study was to investigate the impact of the drug loading method on drug release from 3D-printed tablets. Filaments comprising a poorly water-soluble model drug, indomethacin (IND), and a polymer, polyvinyl alcohol (PVA), were prepared by hot-melt extrusion (HME) and compared with IND-loaded filaments prepared with an impregnation (IMP) process. The 3D-printed tablets were fabricated using a fused deposition modeling 3D printer. The filaments and 3D printed tablets were evaluated for their physicochemical properties, swelling and matrix erosion behaviors, drug content, and drug release. Physicochemical investigations revealed no drug–excipient interaction or degradation. IND-loaded PVA filaments produced by IMP had a low drug content and a rapid drug release. Filaments produced by HME with a lower drug content released the drug faster than those with a higher drug content. The drug content and drug release of 3D-printed tablets containing IND were similar to those of the filament results. Particularly, drug release was faster in 3D-printed tablets produced with filaments with lower drug content (both by IMP and HME). The drug release of 3D-printed tablets produced from HME filaments with higher drug content was extended to 24 h due to a swelling-erosion process. This study confirmed that the drug loading method has a substantial influence on drug content, which in turn has a significant effect on drug release. The results suggest that increasing the drug content in filaments might delay drug release from 3D-printed tablets, which may be used for developing dosage forms suited for personalized medicine.

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 Extended release pellets prepared by hot melt extrusion technique for abuse deterrent potential: Category-1 in-vitro evaluation

2020 ◽  
Vol 587 ◽  
pp. 119624 ◽  
Author(s):  
Arun Butreddy ◽  
Sandeep Sarabu ◽  
Nagireddy Dumpa ◽  
Suresh Bandari ◽  
Michael A. Repka
Keyword(s):  
Extended Release ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
In Vitro Evaluation ◽  
Hot Melt
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