Dual Release Model to Evaluate Dissolution Profiles from Swellable Drug Polyelectrolyte Matrices

2020 ◽  
Vol 17 (6) ◽  
pp. 511-522 ◽  
Author(s):  
Alicia Graciela Cid ◽  
María Verónica Ramírez-Rigo ◽  
María Celeste Palena ◽  
Elio Emilio Gonzo ◽  
Alvaro Federico Jimenez-Kairuz ◽  
...  

Background: Mathematical modeling in modified drug release is an important tool that allows predicting the release rate of drugs in their surrounding environment and elucidates the transport mechanisms involved in the process. Objective: The aim of this work was to develop a mathematical model that allows evaluating the release profile of drugs from polymeric carriers in which the swelling phenomenon is present. Methods: Swellable matrices based on ionic complexes of alginic acid or carboxymethylcellulose with ciprofloxacin were prepared and the effect of adding the polymer sodium salt on the swelling process and the drug release was evaluated. Experimental data from the ciprofloxacin release profiles were mathematically adjusted, considering the mechanisms involved in each stage of the release process. Results: A proposed model, named “Dual Release” model, was able to properly fit the experimental data of matrices presenting the swelling phenomenon, characterized by an inflection point in their release profile. This entails applying the extended model of Korsmeyer-Peppas to estimate the percentage of drug released from the first experimental point up to the inflection point and then a model called Lumped until the final time, allowing to adequately represent the complete range of the drug release profile. Different parameters of pharmaceutical relevance were calculated using the proposed model to compare the profiles of the studied matrices. Conclusion: The “Dual Release” model proposed in this article can be used to predict the behavior of complex systems in which different mechanisms are involved in the release process.

2021 ◽  
Vol 321 ◽  
pp. 03012
Author(s):  
Jianfei Song ◽  
Navideh Abbasnezhad ◽  
Mathieu Specklin ◽  
Mohammadali Shirinbayan ◽  
Smaine Kouidri ◽  
...  

With the aim of optimizing Drug Eluting Stents (DES), particular attention has been laid on computational methods of controlling the drug release profile among researchers. Consequently, various models and simulations are available in the literature. Nevertheless, validations based on biorelevant in-vitro trials are lacking. In the present study, a comparison of drug release from polyurethane samples between calculated results and experimental-data has been carried out. The calculation results are from a numerical simulation and a newly established mathematical model for reproducing the liberation kinetic. Different fluid flow rates and initial drug concentrations in polymer have been taken into account.


2019 ◽  
Vol 9 (01) ◽  
pp. 58-64
Author(s):  
Senthilnathan B ◽  
Billy Graham R ◽  
Chaarmila Sherin C ◽  
Vivekanandan K ◽  
Bhavya E

Objective: Drug targeting is the capacity of the dosage form. In which the therapeutic agent acts specifically to desired site of action in the non-targeted tissue with the help of Nano particles is called as the drug targeting. IMATINIB is a used to treat cancer by chemo therapy. Cancers like chronic myeloid leukemia cancer (CML) and acute lymphoblastic leukemia cancer (ALL) and other specific types of gastrointestinal stromal cell tumor (GIST) systemic mast cell disease and Bone marrow failure disorder. It is administered by oral root. For ATP, Tyrosine kinase is act as a binding site. Methodology: The drug IMATINIB is loaded in the polymer chitosan, poly-(D) glucosamine is a bio compactible, bio degradable, nontoxic, antimicrobial and soluble in solvents. This preparation is done by emulsion-droplet coalescence method. Content of the Drug, Size of the particle and Zeta potential, Encapsulation efficiency and Drug release testing are described for this formulation in this study. Results: The Imatinib Nano particles were formulated and evaluated for its invitro drug release profile. Based on the invitro drug release profile of Imatinib nano particles formulation (INP1 – INP5) formulation INP3 was selected as the best formulation in which the particle size was 285.9nm. The invitro % drug release of INP3 formulation was 99.76 ± 0.82 and it was found to be the suitable formulation to manage the cancer. Conclusion: Hence it is concluded that the newly formulated controlled release nanoparticle drug delivery system of Imatinib may be idol and effective by allowing the drug to release continuously for 24 hrs.


Author(s):  
Rajesh Dubey ◽  
Udaya K. Chowdary ◽  
Venkateswarlu V.

A controlled release formulation of metoclopramide was developed using a combination of hypromellose (HPMC) and hydrogenated castor oil (HCO). Developed formulations released the drug over 20 hr with release kinetics following Higuchi model. Compared to HCO, HPMC showed significantly higher influence in controlling the drug release at initial as well as later phase. The difference in the influence can be explained by the different swelling and erosion behaviour of the polymers. Effect of the polymers on release was optimized using a face-centered central composite design to generate a predictable design space. Statistical analysis of the drug release at various levels indicated a linear effect of the polymers’ levels on the drug release. The release profile of formulations containing the polymer levels at extremes of their ranges in design space was found to be similar to the predicted release profile


2010 ◽  
Vol 5 (4) ◽  
pp. 155892501000500 ◽  
Author(s):  
Hang Liu ◽  
Karen K. Leonas ◽  
Yiping Zhao

Poly(εepsilon;-caprolactone) (PCL) electrospun fibers containing ampicillin sodium salt have been produced and twisted into nanofiber yarns. The fiber diameters and crystallinity, the in vitro antimicrobial properties of the yarns, and the in vitro release of ampicillin from yarns containing various ampicillin concentrations are studied. Decreased fiber diameters and reduced diameter variation are observed with the addition of ampicillin salt into the polymer solution. The results from the zone of inhibition test of the yarns against both gram-positive Staphylococcus aureus and gram-negative Klebsiella pneumoniae indicate that the released ampicillin retains its effectiveness after the production processes, therefore the as-spun yarns are antimicrobial active. A burst release of ampicillin from the yarns has been observed in the first hour, and the release is almost completed in 96 hours. The burst release is believed to be due to the low compatibility of ampicillin with PCL, the accumulation of ampicillin on fiber surface and the small fiber diameters. An empirical release model is developed to describe the release profile. The results indicate that the electrospun nanofibers yarns will have a great potential to be used for biomaterials, such as surgical sutures, to decrease the surgical site infection rate.


2014 ◽  
Vol 659 ◽  
pp. 503-508
Author(s):  
Sorin Gabriel Vernica ◽  
Aneta Hazi ◽  
Gheorghe Hazi

Increasing the energy efficiency of a gas turbine plant can be achieved by exhaust gas heat recovery in a recovery boiler. Establishing some correlations between the parameters of the boiler and of the turbine is done usually based on mathematical models. In this paper it is determined from experimental point of view, the effectiveness of a heat recovery boiler, which operates together with a gas turbine power plant. Starting from the scheme for framing the measurement devices, we have developed a measurement procedure of the experimental data. For experimental data processing is applied the effectiveness - number of transfer unit method. Based on these experimental data we establish correlations between the recovery boiler effectiveness and the gas turbine plant characteristics. The method can be adapted depending on the type of flow in the recovery boiler.


Author(s):  
Adam Barylski ◽  
Mariusz Deja

Silicon wafers are the most widely used substrates for fabricating integrated circuits. A sequence of processes is needed to turn a silicon ingot into silicon wafers. One of the processes is flattening by lapping or by grinding to achieve a high degree of flatness and parallelism of the wafer [1, 2, 3]. Lapping can effectively remove or reduce the waviness induced by preceding operations [2, 4]. The main aim of this paper is to compare the simulation results with lapping experimental data obtained from the Polish producer of silicon wafers, the company Cemat Silicon from Warsaw (www.cematsil.com). Proposed model is going to be implemented by this company for the tool wear prediction. Proposed model can be applied for lapping or grinding with single or double-disc lapping kinematics [5, 6, 7]. Geometrical and kinematical relations with the simulations are presented in the work. Generated results for given workpiece diameter and for different kinematical parameters are studied using models programmed in the Matlab environment.


Author(s):  
Fakhreddine Landolsi ◽  
Fathi H. Ghorbel ◽  
James B. Dabney

AFM-based nanomanipulation is very challenging because of the complex mechanics in tip-sample interactions and the limitations in AFM visual sensing capabilities. In the present paper, we investigate the modeling of AFM-based nanomanipulation emphasizing the effects of the relevant interactions at the nanoscale. The major contribution of the present work is the use of a combined DMT-JKR interaction model in order to describe the complete collision process between the AFM tip and the sample. The coupling between the interactions and the friction at the nanoscale is emphasized. The efficacy of the proposed model to reproduce experimental data is demonstrated via numerical simulations.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 933
Author(s):  
Runqiao Dong ◽  
James C. DiNunzio ◽  
Brian P. Regler ◽  
Walter Wasylaschuk ◽  
Adam Socia ◽  
...  

The kinetics of water transport into tablets, and how it can be controlled by the formulation as well as the tablet microstructure, are of central importance in order to design and control the dissolution and drug release process, especially for immediate release tablets. This research employed terahertz pulsed imaging to measure the process of water penetrating through tablets using a flow cell. Tablets were prepared over a range of porosity between 10% to 20%. The formulations consist of two drugs (MK-8408: ruzasvir as a spray dried intermediate, and MK-3682: uprifosbuvir as a crystalline drug substance) and NaCl (0% to 20%) at varying levels of concentrations as well as other excipients. A power-law model is found to fit the liquid penetration exceptionally well (average R2>0.995). For each formulation, the rate of water penetration, extent of swelling and the USP dissolution rate were compared. A factorial analysis then revealed that the tablet porosity was the dominating factor for both liquid penetration and dissolution. NaCl more significantly influenced liquid penetration due to osmotic driving force as well as gelling suppression, but there appears to be little difference when NaCl loading in the formulation increases from 5% to 10%. The level of spray dried intermediate was observed to further limit the release of API in dissolution.


Author(s):  
RubÉn Ramos Islas ◽  
Leopoldo Villafuerte Robles

<p><strong>Objective: </strong>The aim of this work is the assessment of an eventual improvement in flowability of free flowing excipients on formulations containing Noveon AA1 and their influence on compactibility and release profile.</p><p><strong>Methods: </strong>Mixtures containing 20% Noveon AA1 and variable proportions of metronidazole and the free flowing excipients Prosolv EasyTab and GalenIQ 720 and 721were tested in their powder flow rate and the tablets compactibility and released profiles.</p><p><strong>Results: </strong>The powder flowability obtained with GalenIQ is about 20% better than that obtained with EasyTab. However, it is lesser than that considered as acceptable for a high-speed tableting machine. EasyTab reduces the drug release up to a half along with a continuing flattening of the release profile. This is attributed to an increasing tortuosity of the drug release path as the proportion EasyTab increases. GalenIQ restricts drug release in about a third with a lesser change in the release mechanism. This is attributed to competition for the available water inside the tablet, between the hydrating Noveon AA1 and the dissolving GalenIQ. The compactibility of the metronidazole/Noveon AA1 mixtures increases after addition of EasyTab in about 3.5 N per unit percentage of the added excipient while GalenIQ does it in about 2.6 N.</p><p><strong>Conclusion: </strong>The powder flowability of mixtures of metronidazole with Noveon AA1 was not suited for direct compression after addition of 40% of the free-flow excipient. The free-flow excipients reduce the metronidazole release rate and increase its compactibility. It was not observed a different clear functioning between both types of GalenIQ.</p>


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