Performance and paroxetine stability in tablets manufactured by fused deposition modelling-based 3D printing

2021 ◽  
Author(s):  
Sara Figueiredo ◽  
Ana I Fernandes ◽  
Fátima G Carvalho ◽  
João F Pinto
Keyword(s):  
Process Parameters ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Fused Deposition Modelling ◽  
Dissolution Profile ◽  
Fused Deposition ◽  
The Impact ◽  
Hot Melt

Abstract Objectives The objective of this study was to develop a method for the preparation and characterization of paroxetine (PRX) tablets, obtained by coupling hot-melt extrusion and fused deposition modelling (FDM)-based three-dimensional printing (3DP) technology. The impact of the printing process parameters on the drug stability and on the tablets performance was assessed. Methods Tablets were obtained by FDM of hot-melt extruded PRX-loaded filaments. Physicochemical, thermal, spectroscopic, diffractometric analysis and in-vitro dissolution tests of the intermediate products and the finished dosage forms were performed. Key findings The characterization of printed tablets evidenced mass and dimensions uniformity, and consistency of drug content and dissolution profile. The formation of amorphous solid dispersions and interaction of formulation components throughout the manufacturing process were demonstrated. Layer thickness, printing temperature, printing and travelling speeds, and infill were the most impacting process parameters on both the physicochemical properties and the in-vitro performance of the 3D-printed tablets. Conclusions PRX tablets, meeting compendial limits, were manufactured by 3DP, envisaging their clinical use as individually designed dosage forms. The assessment of the impact of processing parameters on the printed tablets provided insights, which will ultimately allow streamlining of the 3D process set-up for quicker and easier production of patient-centric medicines.

scholarly journals Non-compendial vs compendial analytical tests - a powerful tool for predicting in vitro similarity of highly viscous oral suspension

2019 ◽  
Vol 64 (02) ◽  
pp. 61-72
Author(s):  
Elena Kazandjievska ◽  
Iva Antova ◽  
Slavica Mitrevska ◽  
Aleksandar Dimkovski ◽  
Elena Dimov ◽  
...  
Keyword(s):  
Drug Release ◽  
Negative Impact ◽  
In Vitro Release ◽  
Active Pharmaceutical Ingredient ◽  
Pharmaceutical Products ◽  
Dosage Forms ◽  
Oral Suspension ◽  
In Vitro Dissolution ◽  
Dissolution Profile

In vitro dissolution profiles are increasingly used to evaluate drug release characteristics of pharmaceutical products. The dissolution methods is expected to be an appropriate tool for checking consistency of the pharmaceutical attributes by discriminating similarities and dissimilarities between different drug formulations. Expansion in development of novel “special” dosage forms, due to the manner in which these dosage forms release the active pharmaceutical ingredient, usually requires applying non-compendial dissolution strategy that differs from the traditional compendial recommendations. For demonstrating sameness in the dissolution profile, in vitro drug release comparison between test and reference product of highly viscous oral suspension by applying non-compendial peak vessel against conventional hemispheric vessel was demonstrated in this study. All reference batches exhibited high variability in dissolution data when using hemispheric vessel due to forming mound compact mass at the bottom of the vessel. Different strategies for samples manipulation, before and during dissolution period, were performed in order to eliminate additional variabilities. Modifications of conventional USP 2 apparatus such as using peak vessel provided with more reproducible and reliable result for distinguishing in vitro similarities between different formulations of oral suspensions. Misinterpretation of dissolution data can lead to negative impact on product development. Taking time to observe and evaluate what is happening to the product in the vessel during dissolution is of curtail consideration for proper selection of the dissolution strategy. Keywords: oral suspensions; in-vitro release; hydrodynamic variability; USP apparatus 2/ Paddle apparatus; peak vessel

scholarly journals Preliminary Characterization and Comparison of Mucilage from Leaves of Hibiscus Sabdariffa L. as A Tablet Binder

2021 ◽  
Vol 12 (1) ◽  
pp. 487-496
Author(s):  
Gayathri R ◽  
Benedict Jose C ◽  
Ramkanth S ◽  
Pradheesh Mohan S ◽  
Swetha V ◽  
...  
Keyword(s):  
Flow Characteristics ◽  
In Vitro Dissolution ◽  
Binding Property ◽  
Dissolution Profile ◽  
Hibiscus Sabdariffa ◽  
Comparative Binding ◽  
Tablet Formulations ◽  
Granule Properties

The present research dealt with the extraction and characterization of mucilage from the Hibiscus sabdariffa leaves. Compared with normal binding agents such as starch and Poly Vinyl Pyrrolidine (PVP), the mucilage of Hibiscus sabdariffa (HSM) was assessed for its binding properties in tablet formulations. Tablets were formulated using HSM, starch and PVP as binders at a various concentration to evaluate its comparative binding efficiency. The compressed tablets were analyze for their quality control tests as per IP. The extracted HSM showed the characteristics of mucilage and good physicochemical properties. The FTIR and thermal analysis compatibility tests showed that there were no significant reactions between the drug and mucilage. Granule properties of various formulations were found to be comparable and have excellent flow characteristics. Post compression parameters suggested that tablets formulated with mucilage had better hardness and friability as that of the tablets prepared with starch and PVP. The formulations exhibited a better and more consistent release as compared to standard formulations using starch and PVP as a binder. The statistical analysis of in vitro dissolution profile by using DD solver software for difference factor (f1), similarity factor (f2), and Rescigno index (ξ) values also indicated promising results. The results notably indicate that binding property of HSM was at par with starch and PVP.

scholarly journals Hot Melt Extrusion Processing Parameters Optimization

Processes ◽  
2020 ◽  
Vol 8 (11) ◽  
pp. 1516
Author(s):  
Abdullah Alshetaili ◽  
Saad M. Alshahrani ◽  
Bjad K. Almutairy ◽  
Michael A. Repka
Keyword(s):  
Factorial Design ◽  
Processing Parameters ◽  
Hot Melt Extrusion ◽  
Parameters Optimization ◽  
Extrusion Temperature ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Melt Extrusion ◽  
The Impact ◽  
Hot Melt

The aim of this study was to demonstrate the impact of processing parameters of the hot-melt extrusion (HME) on the pharmaceutical formulation properties. Carbamazepine (CBZ) was selected as a model water-insoluble drug. It was incorporated into Soluplus®, which was used as the polymeric carrier, to produce a solid dispersion model system. The following HME-independent parameters were investigated at different levels: extrusion temperature, screw speed and screw configuration. Design of experiment (DOE) concept was applied to find the most significant factor with minimum numbers of experimental runs. A full two-level factorial design was applied to assess the main effects, parameter interactions and total error. The extrudates’ CBZ content and the in vitro dissolution rate were selected as response variables. Material properties, including melting point, glass transition, and thermal stability, and polymorphs changes were used to set the processing range. In addition, the extruder torque and pressure were used to find the simplest DOE model. Each change of the parameter showed a unique pattern of dissolution profile, indicating that processing parameters have an influence on formulation properties. A simple, novel and two-level factorial design was able to evaluate each parameter effect and find the optimized formulation. Screw configuration and extrusion temperature were the most affecting parameters in this study.

scholarly journals Polymer Selection for Hot-Melt Extrusion Coupled to Fused Deposition Modelling in Pharmaceutics

Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 795 ◽  
Author(s):  
Gabriela G. Pereira ◽  
Sara Figueiredo ◽  
Ana Isabel Fernandes ◽  
João F. Pinto
Keyword(s):  
Raw Materials ◽  
Three Dimensional ◽  
Hot Melt Extrusion ◽  
Dosage Forms ◽  
Fused Deposition Modelling ◽  
Melt Extrusion ◽  
Fused Deposition ◽  
The Many ◽  
House Production ◽  
Hot Melt

Three-dimensional (3D) printing offers the greatest potential to revolutionize the future of pharmaceutical manufacturing by overcoming challenges of conventional pharmaceutical operations and focusing design and production of dosage forms on the patient’s needs. Of the many technologies available, fusion deposition modelling (FDM) is considered of the lowest cost and higher reproducibility and accessibility, offering clear advantages in drug delivery. FDM requires in-house production of filaments of drug-containing thermoplastic polymers by hot-melt extrusion (HME), and the prospect of connecting the two technologies has been under investigation. The ability to integrate HME and FDM and predict and tailor the filaments’ properties will extend the range of printable polymers/formulations. Hence, this work revises the properties of the most common pharmaceutical-grade polymers used and their effect on extrudability, printability, and printing outcome, providing suitable processing windows for different raw materials. As a result, formulation selection will be more straightforward (considering the characteristics of drug and desired dosage form or release profile) and the processes setup will be more expedite (avoiding or mitigating typical processing issues), thus guaranteeing the success of both HME and FDM. Relevant techniques used to characterize filaments and 3D-printed dosage forms as an essential component for the evaluation of the quality output are also presented.

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

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1114
Author(s):  
Janine Boniatti ◽  
Patricija Januskaite ◽  
Laís B. da Fonseca ◽  
Alessandra L. Viçosa ◽  
Fábio C. Amendoeira ◽  
...  
Keyword(s):  
3D Printing ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Fold Increase ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Fused Deposition Modelling ◽  
Amorphous Solid Dispersions ◽  
Fused Deposition

For the last 40 years, praziquantel has been the standard treatment for schistosomiasis, a neglected parasitic disease affecting more than 250 million people worldwide. However, there is no suitable paediatric formulation on the market, leading to off-label use and the splitting of commercial tablets for adults. In this study, we use a recently available technology, direct powder extrusion (DPE) three-dimensional printing (3DP), to prepare paediatric Printlets™ (3D printed tablets) of amorphous solid dispersions of praziquantel with Kollidon® VA 64 and surfactants (Span™ 20 or Kolliphor® SLS). Printlets were successfully printed from both pellets and powders obtained from extrudates by hot melt extrusion (HME). In vitro dissolution studies showed a greater than four-fold increase in praziquantel release, due to the formation of amorphous solid dispersions. In vitro palatability data indicated that the printlets were in the range of praziquantel tolerability, highlighting the taste masking capabilities of this technology without the need for additional taste masking excipients. This work has demonstrated the possibility of 3D printing tablets using pellets or powder forms obtained by HME, avoiding the use of filaments in fused deposition modelling 3DP. Moreover, the main formulation hurdles of praziquantel, such as low drug solubility, inadequate taste, and high and variable dose requirements, can be overcome using this technology.

scholarly journals FORMULATION, OPTIMIZATION, AND CHARACTERIZATION OF TRANSDERMAL DRUG DELIVERY SYSTEMS CONTAINING EPLERENONE

2022 ◽  
pp. 198-207
Author(s):  
RAMESH SHINDE ◽  
MALARKODI VELRAJ
Keyword(s):  
Skin Irritation ◽  
In Vitro Dissolution ◽  
Log P ◽  
P Value ◽  
Dissolution Profile ◽  
After Effects ◽  
Transdermal Drug Delivery Systems

Objective: The proposed work was aimed at optimization, formulation, and characterization of transdermal patches of eplerenone for efficient transdermal delivery of the drug. Methods: The log p estimation of eplerenone is 1.34, it was closer to standard worth. Log P value in a range of 1 to 4 indicates higher permeation through the skin. FTIIR study was carried out individually for drug, each polymer, and finished product (Patches) compared eplerenone and FTIR spectra of pure drug and polymer. The calibration curve of eplerenone in Phosphate buffer pH 6.8 was analyzed. Results: The selected range of eplerenone was found to be linear. A regression coefficient (R2) at 245 nm was found to be 0.994. Drug content outcomes additionally discovered uniform in all clusters in a range of 97 % to 98 %, that batches arranged with ERS 100 show great mechanical properties contrast with different polymers however helpless glue properties. The flatness of 4 cm2 patches ranges from 348±0.087 mg to 387±0.527 mg. skin irritation it was produced irritation with negligible erythema following 10 d and unequivocal erythema, promptly obvious edema was produced following 12 d. Conclusion: These after-effects of the in vivo skin irritation study recommended that advanced batch S9 doesn't show any kind of significant disturbance on rodent skin for as long as 14 d and it was securely utilized around 24 h. the optimized batch S9 drug was constantly discharged through the Wistar rodent skin up to 16 hr and the delivery design was like an in vitro dissolution profile of the market product.

PERILAKU DISOLUSI KETOPROFEN DAN INDOMETASIN FARNESIL TERSALUT GEL KITOSAN-GOM GUAR

2012 ◽  
Vol 12 (1) ◽  
Author(s):  
Purwantiningsih Sugita ◽  
Bambang Srijanto ◽  
Budi Arifin ◽  
Fithri Amelia ◽  
Mahdi Mubarok
Keyword(s):  
Room Temperature ◽  
Guar Gum ◽  
Tween 80 ◽  
Chitosan Solution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Magnetic Stirrer ◽  
Dissolution Behaviour ◽  
Shrimp Shell Waste

Chitosan, a modification of shrimp-shell waste, has been utilized as microcapsule. However, it’s fragile gel property needs to be strengthened by adding glutaraldehyde (glu) and natural hydrocolloid guar gum (gg). This research’s purposes were to study dissolution behaviour of ketoprofen and infar through optimum chitosan-guar gum microcapsule. Into 228.6 mL of 1.75% (w/v) chitosan solution in 1% (v/v) acetic acid,38.1 mL of gg solution was added with concentration variation of 0.35, 0.55, and 0.75% (w/v) for ketoprofen microcapsules and 0.05, 0.19, and 0.33% (w/v) for infar microcapsules, and stirred with magnetic stirrer until homogenous. Afterwards, 7.62mL of glu was added slowly under stirring, with concentrations varied: 3, 3.5, and 4% (v/v) for ketoprofen microcapsules, and 4, 4.5, and 5% (v/v) for infar microcapsules. All mixtures were shaked for 20 minutes for homogenization. All mixtures wereshaked for 20 minutes for homogenization. Into each  microcapsule mixture for ketoprofen, a solution of 2 g of ketoprofen in 250 mL of 96% ethanol was added, whereas solution of 100 mg of in 250 mL of 96% ethanol was added into each microcapsule mixture for infar. Every mixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Everymixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Conversion of suspension into fine powders/granules (microcapsules) was done by using spray dryer. The data of [gg], [glu], and medicine’s content from each microcapsule were treated with Minitab 14 software to obtain optimum [gg] and [glu] for microencapsulation. The dissolution behaviour of optimum ketoprofen and infar microcapsules were investigated. The result of optimization by using Minitab Release 14 software showed that among the microcapsule compositions of [gg] and [glu] were 0.35% (w/v) and 3.75% (v/v), respectively, optimum to coat ketoprofen, whereas [gg] and [glu] of 0.05% (w/v) and4.00% (v/v), respectively, optimum to coat infar, at constant chitosan concentration (1.75% [w/v]). In vitro dissolution profile showed that chitosan-guar gum gel microcapsule was more resistant in intestinal pH condition (rather basic) compared with that in gastric pH (very acidic).

Formulation and Evaluation of Bilayer Sustained Release Tablets of Salbutamol and Theophylline

2009 ◽  
Vol 2 (3) ◽  
pp. 638-646
Author(s):  
R. Nagaraju ◽  
Rajesh Kaza
Keyword(s):  
Ethyl Cellulose ◽  
Xanthan Gum ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Dissolution Studies ◽  
Sustained Release Tablets ◽  
Dissolution Apparatus ◽  
Single Dosage

Salbutamol and theophylline are available in conventional dosage forms, administered four times a day, leading to saw tooth kinetics and resulting in ineffective therapy. The combination of these two drugs in a single dosage form will enhance the patient compliance and prolong bronchodilation. Various polymers, such as hydroxy propyl methylcellulose K4M (HPMC- K4M), hydroxy propyl methylcellulose K100M (HPMC- K100M), xanthan gum, ethyl cellulose and hydroxy propyl methylcellulose phthalate (HPMC-P) were studied. HPMC-P and HPMC- K4M were found to be best in controlling the release. In-vitro dissolution studies were carried out for all the bi-layered tablets developed using USP dissolution apparatus type 2 (paddle). It was found that the tablet FB15-FW3 showed 50% release of salbutamol in first hour and the remaining was released for eight hours. However, theophylline was found to be released as per the USP specifications. The IR spectrum was taken for FB15-FW3 formulation and it revealed that there is no disturbance in the principal peaks of pure drugs salbutamol and theophylline. This further confirms the integrity of pure drugs and no incompatibility of them with excipients. Also, formulation of FB15-FW3 has shown required release pattern and complies with all the evaluated parameters and comparable to the marketed formulation.

Sign in / Sign up

Export Citation Format

Share Document