scholarly journals A Review on Computer - Aided Formulation Development

Author(s):  
Chaudhari R. G. ◽  
Raut D. B. ◽  
Barhewar P. A. ◽  
Mali A. S. ◽  
Burade K. B.

This chapter introduces the concept of formulation development assisted by computer applications. Development and optimization of various types of pharmaceutical emulsions microemulsions, self- microemulsifying systems, and double emulsions are presented. Illustrative examples are presented to demonstrate the ability of computer-aided tools to facilitate formulation development. Various techniques, such as design of experiments and arti?cial neural networks, are implemented for optimization of the formulation and/or processing parameters. Furthermore, some of the critical quality attributes and processing parameters are optimized simultaneously. The examples presented should serve as the foundation for the future quality- by-design development of pharmaceutical emulsion and (self) microemulsion formulations.

2020 ◽  
Vol 152 ◽  
pp. 282-295
Author(s):  
Marta F. Simões ◽  
Gabriel Silva ◽  
Ana C. Pinto ◽  
Marlene Fonseca ◽  
Nuno E. Silva ◽  
...  

Author(s):  
KAVITHA A. N. ◽  
JANAKIRAMAN K. ◽  
RAMAN DANG

Objective: The main objective of the present research work was to develop systematically the Self Micro Emulsifying Drug Delivery system of BCS Class IV drug in a Quality by Design framework. Methods: The quality by design-based formulation development proceeds with defining the Quality Target Product Profile and Critical Quality Attributes of dosage form with appropriate justification for the same. The statistical Mixture design was used for the development of the formulation. The independent variables selected for the design were Oleic acid, Labrasol and PEG 6000, whereas droplet size (nm), emulsification time (sec), % drug loading and % drug release at 15 min were considered as the potential quality attributes of the Self Micro Emulsifying System. The eight different batches of Etravirine-Self Micro Emulsifying systems (ETV-SMEDDS) were prepared and checked for the Critical Quality Attributes. The simultaneous optimization of the formulation was done by the global desirability approach. Results: The characterization report obtained for all the different batches of formulation was analyzed statistically by fitting into regression models. The statistically significant models determined for droplet size (nm) (R2= 0.96 and p-0.1022), emulsification time (sec) (R2= 0.99 and p-0.0267), % drug loading (R2= 0.93 and p-0.1667) and % drug release at 15 min (R2= 0.96 and p-0.0911) and were statistically significant. The maximal global desirability value obtained was 0.9415 and the value indicates, the selected factors and responses have a good correlation and are significant enough for optimization and prediction of best formulation. Conclusion: The QbD approach utilized during the development of ETV-SMEEDS facilitated the identification of Critical Material Attributes and their significant impact on the Critical Quality Attributes of SMEDDS. The concept of building quality into product through the QbD application was utilized successfully in the formulation development.


2019 ◽  
Vol 9 (3) ◽  
pp. 240-247
Author(s):  
Prabhakar Panzade ◽  
Priyanka Somani ◽  
Pavan Rathi

Background and Objective: The top approach to deliver poorly soluble drugs is the use of a highly soluble form. The present study was conducted to enhance the solubility and dissolution of a poorly aqueous soluble drug nevirapine via a pharmaceutical cocrystal. Another objective of the study was to check the potential of the nevirapine cocrystal in the dosage form. Methods: A neat and liquid assisted grinding method was employed to prepare nevirapine cocrystals in a 1:1 and 1:2 stoichiometric ratio of drug:coformer by screening various coformers. The prepared cocrystals were preliminary investigated for melting point and saturation solubility. The selected cocrystal was further confirmed by Infrared Spectroscopy (IR), Differential Scanning Calorimetry (DSC), and Xray Powder Diffraction (XRPD). Further, the cocrystal was subjected to in vitro dissolution study and formulation development. Results: The cocrystal of Nevirapine (NVP) with Para-Amino Benzoic Acid (PABA) coformer prepared by neat grinding in 1:2 ratio exhibited greater solubility. The shifts in IR absorption bands, alterations in DSC thermogram, and distinct XRPD pattern showed the formation of the NVP-PABA cocrystal. Dissolution of NVP-PABA cocrystal enhanced by 38% in 0.1N HCl. Immediate release tablets of NVP-PABA cocrystal exhibited better drug release and less disintegration time. Conclusion: A remarkable increase in the solubility and dissolution of NVP was obtained through the cocrystal with PABA. The cocrystal also showed great potential in the dosage form which may provide future direction for other drugs.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
A. Wong ◽  
Z. Q. Lin ◽  
L. Wang ◽  
A. G. Chung ◽  
B. Shen ◽  
...  

AbstractA critical step in effective care and treatment planning for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the cause for the coronavirus disease 2019 (COVID-19) pandemic, is the assessment of the severity of disease progression. Chest x-rays (CXRs) are often used to assess SARS-CoV-2 severity, with two important assessment metrics being extent of lung involvement and degree of opacity. In this proof-of-concept study, we assess the feasibility of computer-aided scoring of CXRs of SARS-CoV-2 lung disease severity using a deep learning system. Data consisted of 396 CXRs from SARS-CoV-2 positive patient cases. Geographic extent and opacity extent were scored by two board-certified expert chest radiologists (with 20+ years of experience) and a 2nd-year radiology resident. The deep neural networks used in this study, which we name COVID-Net S, are based on a COVID-Net network architecture. 100 versions of the network were independently learned (50 to perform geographic extent scoring and 50 to perform opacity extent scoring) using random subsets of CXRs from the study, and we evaluated the networks using stratified Monte Carlo cross-validation experiments. The COVID-Net S deep neural networks yielded R$$^2$$ 2 of $$0.664 \pm 0.032$$ 0.664 ± 0.032 and $$0.635 \pm 0.044$$ 0.635 ± 0.044 between predicted scores and radiologist scores for geographic extent and opacity extent, respectively, in stratified Monte Carlo cross-validation experiments. The best performing COVID-Net S networks achieved R$$^2$$ 2 of 0.739 and 0.741 between predicted scores and radiologist scores for geographic extent and opacity extent, respectively. The results are promising and suggest that the use of deep neural networks on CXRs could be an effective tool for computer-aided assessment of SARS-CoV-2 lung disease severity, although additional studies are needed before adoption for routine clinical use.


2021 ◽  
Vol 2 (4) ◽  
Author(s):  
Daniel M. Lima ◽  
Jose F. Rodrigues-Jr ◽  
Bruno Brandoli ◽  
Lorraine Goeuriot ◽  
Sihem Amer-Yahia

1988 ◽  
Vol 31 (6) ◽  
pp. 1087-1093 ◽  
Author(s):  
Marcel F. Hibert ◽  
Maurice W. Gittos ◽  
Derek N. Middlemiss ◽  
Anis K. Mir ◽  
John R. Fozard

Author(s):  
Kamyab Keshtkar

As a relatively high percentage of adenoma polyps are missed, a computer-aided diagnosis (CAD) tool based on deep learning can aid the endoscopist in diagnosing colorectal polyps or colorectal cancer in order to decrease polyps missing rate and prevent colorectal cancer mortality. Convolutional Neural Network (CNN) is a deep learning method and has achieved better results in detecting and segmenting specific objects in images in the last decade than conventional models such as regression, support vector machines or artificial neural networks. In recent years, based on the studies in medical imaging criteria, CNN models have acquired promising results in detecting masses and lesions in various body organs, including colorectal polyps. In this review, the structure and architecture of CNN models and how colonoscopy images are processed as input and converted to the output are explained in detail. In most primary studies conducted in the colorectal polyp detection and classification field, the CNN model has been regarded as a black box since the calculations performed at different layers in the model training process have not been clarified precisely. Furthermore, I discuss the differences between the CNN and conventional models, inspect how to train the CNN model for diagnosing colorectal polyps or cancer, and evaluate model performance after the training process.


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