Formulation Development Studies for Sterile Dosages: A Comprehensive Review

Sterile generic dosage development requires that specific critical quality attributes be considered and evaluated, regardless of the route of delivery or the type of registration application. The review briefed with an overview of Pharmaceutical Development study requirements. Each of the various stages of studies like Compatibility with the packaging materials, manufacturing vessels, processing aids, MOCs, Filters, Tubing’s and Gaskets also with special studies to be conducted as part of Regulatory Submission, process considerations. Thus, the chapter offers the formulator an overview of the foundational principles associated with formulation development /Pre-formulation studies of sterile products. Keywords: Pharmaceutical Development, Compatibility, Studies, Hold time.

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A Review on Computer - Aided Formulation Development

International Journal of Scientific Research in Science and Technology ◽

10.32628/ijsrst196658 ◽

2019 ◽

pp. 328-337

Author(s):

Chaudhari R. G. ◽

Raut D. B. ◽

Barhewar P. A. ◽

Mali A. S. ◽

Burade K. B.

Keyword(s):

Neural Networks ◽

Design Of Experiments ◽

Quality By Design ◽

Processing Parameters ◽

Computer Applications ◽

Design Development ◽

Formulation Development ◽

Critical Quality Attributes ◽

Double Emulsions ◽

Computer Aided

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.

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Stereolithography Apparatus Evolution: Enhancing Throughput and Efficiency of Pharmaceutical Formulation Development

Pharmaceutics ◽

10.3390/pharmaceutics13050616 ◽

2021 ◽

Vol 13 (5) ◽

pp. 616

Author(s):

Carlo Curti ◽

Daniel J. Kirby ◽

Craig A. Russell

Keyword(s):

3D Printing ◽

High Throughput Screening ◽

The Novel ◽

Formulation Development ◽

Pharmaceutical Development ◽

3D Print ◽

Development Processes ◽

Pharmaceutical Production ◽

Efficient Screening ◽

Limited Choice

Pharmaceutical applications of 3D printing technologies are growing rapidly. Among these, vat photopolymerisation (VP) techniques, including Stereolithography (SLA) hold much promise for their potential to deliver personalised medicines on-demand. SLA 3D printing offers advantageous features for pharmaceutical production, such as operating at room temperature and offering an unrivaled printing resolution. However, since conventional SLA apparatus are designed to operate with large volumes of a single photopolymer resin, significant throughput limitations remain. This, coupled with the limited choice of biocompatible polymers and photoinitiators available, hold back the pharmaceutical development using such technologies. Hence, the aim of this work was to develop a novel SLA apparatus specifically designed to allow rapid and efficient screening of pharmaceutical photopolymer formulations. A commercially available SLA apparatus was modified by designing and fabricating a novel resin tank and build platform able to 3D print up to 12 different formulations at a single time, reducing the amount of sample resin required by 20-fold. The novel SLA apparatus was subsequently used to conduct a high throughput screening of 156 placebo photopolymer formulations. The efficiency of the equipment and formulation printability outcomes were evaluated. Improved time and cost efficiency by 91.66% and 94.99%, respectively, has been confirmed using the modified SLA apparatus to deliver high quality, highly printable outputs, thus evidencing that such modifications offer a robust and reliable tool to optimize the throughput and efficiency of vat photopolymerisation techniques in formulation development processes, which can, in turn, support future clinical applications.

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Molecular Dynamics Simulations in Drug Discovery and Pharmaceutical Development

Processes ◽

10.3390/pr9010071 ◽

2020 ◽

Vol 9 (1) ◽

pp. 71

Author(s):

Outi M. H. Salo-Ahen ◽

Ida Alanko ◽

Rajendra Bhadane ◽

Alexandre M. J. J. Bonvin ◽

Rodrigo Vargas Honorato ◽

...

Keyword(s):

Molecular Dynamics ◽

Drug Discovery ◽

Drug Development ◽

Development Process ◽

Md Simulations ◽

Disordered Proteins ◽

Drug Development Process ◽

Formulation Development ◽

Pharmaceutical Development

Molecular dynamics (MD) simulations have become increasingly useful in the modern drug development process. In this review, we give a broad overview of the current application possibilities of MD in drug discovery and pharmaceutical development. Starting from the target validation step of the drug development process, we give several examples of how MD studies can give important insights into the dynamics and function of identified drug targets such as sirtuins, RAS proteins, or intrinsically disordered proteins. The role of MD in antibody design is also reviewed. In the lead discovery and lead optimization phases, MD facilitates the evaluation of the binding energetics and kinetics of the ligand-receptor interactions, therefore guiding the choice of the best candidate molecules for further development. The importance of considering the biological lipid bilayer environment in the MD simulations of membrane proteins is also discussed, using G-protein coupled receptors and ion channels as well as the drug-metabolizing cytochrome P450 enzymes as relevant examples. Lastly, we discuss the emerging role of MD simulations in facilitating the pharmaceutical formulation development of drugs and candidate drugs. Specifically, we look at how MD can be used in studying the crystalline and amorphous solids, the stability of amorphous drug or drug-polymer formulations, and drug solubility. Moreover, since nanoparticle drug formulations are of great interest in the field of drug delivery research, different applications of nano-particle simulations are also briefly summarized using multiple recent studies as examples. In the future, the role of MD simulations in facilitating the drug development process is likely to grow substantially with the increasing computer power and advancements in the development of force fields and enhanced MD methodologies.

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COMPATIBILITY STUDIES OF ACETAZOLAMIDE WITH EXCIPIENTS BY USING HIGHPERFORMANCE LIQUID CHROMATOGRAPHY (HPLC) TECHNIQUE

INDIAN DRUGS ◽

10.53879/id.49.05.p0039 ◽

2012 ◽

Vol 49 (05) ◽

pp. 39-46

Author(s):

T. E. G. K Murthy ◽

◽

Priya M Bala Vishnu ◽

Babu V. V. Suresh

Keyword(s):

Methyl Cellulose ◽

Gelatin Capsule ◽

Compatibility Studies ◽

Formulation Development ◽

Related Substances ◽

Hard Gelatin Capsule ◽

Highperformance Liquid Chromatography ◽

Hplc Technique ◽

Preformulation Studies ◽

Physical And Chemical

Compatibility studies are essential for preformulation studies of formulation development. Acetazolamideis a carbonic anhydrase inhibitor used in the treatment and management of cardiac oedema, glaucomaand other conditions. The objective of this study was to evaluate the physical and chemical stability ofacetazolamide, when mixed with excipients as binary mixture. These samples were stored and evaluatedfor related substances at 400/75 % RH for 28 days and 550 for 14 days and the samples were analyzedusing HPLC. The results demonstrated the suitability of acetazolamide with Avicel PH 101, MethocelK4M premium CR hydroxy propyl methyl cellulose, Methocel E10M premium CR hydroxy propyl methylcellulose, talc, sodium lauryl sulphate and size 00 white/white hard gelatin capsule.

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QUALITY BY DESIGN BASED DEVELOPMENT OF ETRAVIRINE SELF MICRO EMULSIFYING DRUG DELIVERY SYSTEM

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i3.40488 ◽

2021 ◽

pp. 103-111

Author(s):

KAVITHA A. N. ◽

JANAKIRAMAN K. ◽

RAMAN DANG

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Droplet Size ◽

Quality By Design ◽

Drug Loading ◽

Quality Attributes ◽

The Self ◽

Formulation Development ◽

Critical Quality Attributes

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.

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