Neural Expert System for Pharmaceutical Formulation Development — Focus on Solid Dispersions

2003 ◽  
pp. 480-485
Author(s):  
Aleksander Mendyk ◽  
Renata Jachowicz ◽  
Anna Błasiak
Keyword(s):  
Expert System ◽  
Solid Dispersions ◽  
Pharmaceutical Formulation ◽  
Formulation Development

scholarly journals Relative Contributions of Solubility and Mobility to the Stability of Amorphous Solid Dispersions of Poorly Soluble Drugs: A Molecular Dynamics Simulation Study

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 101 ◽  
Author(s):  
Michael Brunsteiner ◽  
Johannes Khinast ◽  
Amrit Paudel
Keyword(s):  
Molecular Dynamics ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Dynamics Simulation ◽  
Limiting Factor ◽  
Poorly Soluble Drugs ◽  
Formulation Development ◽  
Amorphous Solid Dispersions ◽  
Poorly Soluble

Amorphous solid dispersions are considered a promising formulation strategy for the oral delivery of poorly soluble drugs. The limiting factor for the applicability of this approach is the physical (in)stability of the amorphous phase in solid samples. Minimizing the risk of reduced shelf life for a new drug by establishing a suitable excipient/polymer-type from first principles would be desirable to accelerate formulation development. Here, we perform Molecular Dynamics simulations to determine properties of blends of eight different polymer–small molecule drug combinations for which stability data are available from a consistent set of literature data. We calculate thermodynamic factors (mixing energies) as well as mobilities (diffusion rates and roto-vibrational fluctuations). We find that either of the two factors, mobility and energetics, can determine the relative stability of the amorphous form for a given drug. Which factor is rate limiting depends on physico-chemical properties of the drug and the excipients/polymers. The methods outlined here can be readily employed for an in silico pre-screening of different excipients for a given drug to establish a qualitative ranking of the expected relative stabilities, thereby accelerating and streamlining formulation development.

Formulation development and invitro evaluation of elvitegravir sustained release using solid dispersions

2020 ◽  
Vol 13 (12) ◽  
pp. 5909-5913
Author(s):  
Mohammad Akthar Sulthana ◽  
Mangulal Kethavath ◽  
Fazil Ahmad ◽  
Abeer Mohammed Al-Subaie
Keyword(s):  
Sustained Release ◽  
Solid Dispersions ◽  
Formulation Development

scholarly journals Contribution to the Improvement of an Oral Formulation of Niclosamide, an Antihelmintic Drug Candidate for Repurposing in SARS-CoV-2 and Other Viruses

2020 ◽  
Author(s):  
Eduardo José Barbosa ◽  
Mariana Ribeiro Gubitoso ◽  
Nádia Araci Bou-Chacra ◽  
Stephen R. Byrn ◽  
Flavio M. S. Carvalho ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Oral Dosage ◽  
Drug Candidate ◽  
Formulation Development ◽  
Polymer Dispersions ◽  
Kinetic Solubility ◽  
Oral Dosage Forms

<p>Niclosamide (NCL) is an effective anthelmintic agent that has been shown to possess broad-spectrum antiviral activity, including against<b> </b>SARS-CoV-2. Due to its poor solubility in aqueous medium, however, the commercially available NCL formulations can act only locally in gastrointestinal worms and are not suitable to achieve plasmatic levels to treat systemic diseases. Consequently, the repurposing of this drug represents a challenge for formulation development with serious risks to the biological availability and can compromise preclinical and clinical outcomes. Herein, we report possible formulation, through the research and development, of stable amorphous solid dispersions to improve its solubility. The results of exploratory screening of NCL-polymer dispersions (performed through X-ray powder diffraction and kinetic solubility studies) indicate that soluplus-niclosamide dispersions can increase its aqueous solubility and, consequently, have the potential to enhance NCL bioavailability. <a>This outcome can be used for the development of oral dosage forms for clinical trials in SARS-CoV-2 and other viruses. </a></p>

scholarly journals Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1679
Author(s):  
Thao T.D. Tran ◽  
Phuong H.L. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Insoluble Polymers

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

scholarly journals Contribution to the Improvement of an Oral Formulation of Niclosamide, an Antihelmintic Drug Candidate for Repurposing in SARS-CoV-2 and Other Viruses

2020 ◽  
Author(s):  
Eduardo José Barbosa ◽  
Mariana Ribeiro Gubitoso ◽  
Nádia Araci Bou-Chacra ◽  
Stephen R. Byrn ◽  
Flavio M. S. Carvalho ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Oral Dosage ◽  
Drug Candidate ◽  
Formulation Development ◽  
Polymer Dispersions ◽  
Kinetic Solubility ◽  
Oral Dosage Forms

<p>Niclosamide (NCL) is an effective anthelmintic agent that has been shown to possess broad-spectrum antiviral activity, including against<b> </b>SARS-CoV-2. Due to its poor solubility in aqueous medium, however, the commercially available NCL formulations can act only locally in gastrointestinal worms and are not suitable to achieve plasmatic levels to treat systemic diseases. Consequently, the repurposing of this drug represents a challenge for formulation development with serious risks to the biological availability and can compromise preclinical and clinical outcomes. Herein, we report possible formulation, through the research and development, of stable amorphous solid dispersions to improve its solubility. The results of exploratory screening of NCL-polymer dispersions (performed through X-ray powder diffraction and kinetic solubility studies) indicate that soluplus-niclosamide dispersions can increase its aqueous solubility and, consequently, have the potential to enhance NCL bioavailability. <a>This outcome can be used for the development of oral dosage forms for clinical trials in SARS-CoV-2 and other viruses. </a></p>

scholarly journals Solubility Enhancement of Diclofenac Using Solid Dispersions

2021 ◽  
Vol 5 (1) ◽  
pp. 1-6
Author(s):  
Mohd. Aamir Mirza ◽  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Diclofenac Sodium ◽  
Active Pharmaceutical Ingredient ◽  
Solubility Enhancement ◽  
Solvent Evaporation ◽  
Limiting Factor ◽  
Formulation Development ◽  
Enhanced Solubility ◽  
Evaporation Technique

Background: The phenomenon which gives rise to a homogenous system, formed by the dissolution of solute in a solvent is known as solubility. Low solubility is the limiting factor in formulation development. Diclofenac being BCS class II drug have low aqueous solubility of 0.00401mg/ml. Amongst various solubility enhancement techniques, solid dispersion is the easiest one. Objective: Present work is primarily focused on the development of solid dispersions of diclofenac through solvent evaporation technique utilizing Eudragit E100 as a carrier. Methods: Solid dispersion consists of at least one active pharmaceutical ingredient as a carrier in solid state. Various methods for preparing solid dispersions includes melt extrusion, fusion lyophilization, spray drying, solvent evaporation, and super critical fluid (SCF) technology. Solvent evaporation technique is used among various solid dispersion methods. Conclusion: The enhanced solubility found to be 0.485mg/ml. The dissolution was performed using USP Type II apparatus was %CDR of pure drug and its solid dispersion in 8 hr were found out to be 45.14926% and 98.04758% respectively. Henceforth, solid dispersion technique results marked solubility enhancement of diclofenac sodium.

scholarly journals An Overview on Recent Patents and Technologies on Solid Dispersion

2020 ◽  
Vol 14 (1) ◽  
pp. 63-74 ◽  
Author(s):  
Ritu Kaushik ◽  
Vikas Budhwar ◽  
Deepak Kaushik
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Bioavailability Enhancement ◽  
Molecular Arrangement ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Cryogenic Processing

The oral bioavailability enhancement of poorly water-soluble medicaments is still one of the most complicated aspects of the formulation development. Various approaches are currently available for solubility and rate of dissolution enhancement such as salt formation, solubilization and reduction of particle size, each with its own limitations and advantages. Solid dispersion is one of the most suitable approaches for the formulation development of poorly water-soluble drugs. The popularity of solid dispersion is evident from the increasing number of patent applications and patents granted in this field during recent years. This article reviews the various approaches for the preparation of solid dispersion such as a solvent melting, hot-melt extrusion method, solvent evaporation method, cryogenic processing approaches etc. from the perspective of patents filed or granted for these techniques. Some of the aspects taken into account before the preparation of solid dispersions are carrier selection and physicchemical testing along with an insight into the molecular arrangement of medicaments in solid dispersion. The manuscript further highlights various commercial patented technology platforms such as Solumertm, Hovione and Kinetisol which are based on the concept of solid dispersions.

Recent update of 3D printing technology in pharmaceutical formulation development

2021 ◽  
pp. 1-26
Author(s):  
Gaurav ◽  
Nazeer Hasan ◽  
Ankit Kumar Malik ◽  
Vanshikha Singh ◽  
Kaisar Raza ◽  
...  
Keyword(s):  
3D Printing ◽  
Pharmaceutical Formulation ◽  
Formulation Development ◽  
Printing Technology ◽  
3D Printing Technology
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