Solid Phospholipid Dispersions for Oral Delivery of Poorly Soluble Drugs: Investigation Into Celecoxib Incorporation and Solubility-In Vitro Permeability Enhancement

2016 ◽  
Vol 105 (3) ◽  
pp. 1113-1123 ◽  
Author(s):  
Sophia Yui Kau Fong ◽  
Susana M. Martins ◽  
Martin Brandl ◽  
Annette Bauer-Brandl
Keyword(s):  
Oral Delivery ◽  
Poorly Soluble Drugs ◽  
Permeability Enhancement ◽  
Poorly Soluble

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.

In vitro -in vivo correlation in the effect of cyclodextrin on oral absorption of poorly soluble drugs

2021 ◽  
pp. 120494
Author(s):  
Risa Aihara ◽  
Roman Messerschmid ◽  
Masashi Mizoguchi ◽  
Koichi Wada ◽  
Keiko Minami ◽  
...  
Keyword(s):  
Oral Absorption ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs

2012 ◽  
Vol 423 (2) ◽  
pp. 452-460 ◽  
Author(s):  
Nicolas Duhem ◽  
Julien Rolland ◽  
Raphaël Riva ◽  
Pierre Guillet ◽  
Jean-Marc Schumers ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Poorly Soluble Drugs ◽  
Glycol Chitosan ◽  
Poorly Soluble

An in vitro kinetic method for detection of precipitation of poorly soluble drugs

2005 ◽  
Vol 304 (1-2) ◽  
pp. 1-3 ◽  
Author(s):  
Zimei Wu ◽  
Ian G. Tucker ◽  
Majid Razzak ◽  
Natalie J. Medlicott
Keyword(s):  
Kinetic Method ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

Oxidized Mesoporous Silicon Microparticles for Improved Oral Delivery of Poorly Soluble Drugs

2009 ◽  
Vol 7 (1) ◽  
pp. 227-236 ◽  
Author(s):  
Feng Wang ◽  
He Hui ◽  
Timothy J. Barnes ◽  
Christian Barnett ◽  
Clive A. Prestidge
Keyword(s):  
Oral Delivery ◽  
Poorly Soluble Drugs ◽  
Mesoporous Silicon ◽  
Poorly Soluble

Improved Oral Delivery of Drugs Using Nanoemulsion

2022 ◽  
pp. 93-117
Author(s):  
Subramanian Natesan ◽  
Victor Hmingthansanga ◽  
Nidhi Singh ◽  
Pallab Datta ◽  
Sivakumar Manickam ◽  
...  
Keyword(s):  
Oral Administration ◽  
Oral Delivery ◽  
Oral Route ◽  
Poorly Soluble Drugs ◽  
Site Specific ◽  
Anatomy And Physiology ◽  
Oral Application ◽  
Biological Fate ◽  
Poorly Soluble ◽  
Low Solubility

Administration of drugs through the oral route is considered the simplest and most convenient way to offer greater patient compliance than other routes. Most active drugs discovered in the past and those being discovered in recent times are inadequate because of their inherent limitations in physicochemical properties such as low solubility and permeability, resulting in poor bioavailability, especially after oral administration in the form of tablet or capsule. Pharmaceutical nanoemulsion is the most promising, safer, and multimodal technique for delivering poorly soluble drugs and gaining more attention due to its characteristics such as higher solubilisation capacity, smaller size, surface charge, and site-specific drug targeting. This chapter focuses on the biological fate of nanoemulsion after oral administration and a few case studies related to the oral application of nanoemulsion in delivering poorly soluble drugs. In addition, the anatomy and physiology of the GI tract, components of nanoemulsion, and methods of preparation are addressed.

Chapter 5 Oral Delivery of Poorly Soluble Drugs

2017 ◽  
pp. 125-186
Author(s):  
Dev Prasad ◽  
Akash Jain ◽  
Sudhakar Garad
Keyword(s):  
Oral Delivery ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

scholarly journals OPTIMISATION OF STARCH OXALATE AS A NOVEL SUPERDISINTEGRANT IN FAST DISSOLVING SYSTEMS OF POORLY SOLUBLE DRUGS

2019 ◽  
Vol 9 (1-s) ◽  
pp. 185-195
Author(s):  
SANTOSH KUMAR RADA ◽  
T. Naga Satya Yagnesh
Keyword(s):  
Factorial Design ◽  
Amorphous Powder ◽  
Immediate Release ◽  
Poorly Soluble Drugs ◽  
Disintegration Time ◽  
23 Factorial Design ◽  
Drug Content ◽  
Poorly Soluble ◽  
Dissolution Efficiency

Objective: To enhance the solubility of poorly soluble drugs by using 23 factorial design in the formulation of fast dissolving tablets by employing starch oxalate as a superdisintegrant. Methods: Starch oxalate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch oxalate. By using 23 factorial design, atenolol fast dissolving tablet was prepared by employing starch oxalate as a superdisintegrant in different proportions in each case by direct compression method. In the evaluation of fast dissolving tablets the drug content, hardness, friability, disintegration time and other dissolution characteristics were utilized. Results: The starch oxalate prepared was found to be fine, free-flowing completely amorphous powder. The compatibility between atenolol and starch oxalate were studied and showed no interaction. The drug content, hardness, and friability have been effective with regard to all the formulated fast dissolving tablets employing starch oxalate. The optimised formulation F8 has the least disintegration time i.e., 24±0.06s. The In–vitro wetting time was less (i.e., 28s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be more in F8 formulation 94.42±0.18%. The cumulative drug dissolved in the optimized formulation F8 was found to be 98.70±0.24% in 5 min. Conclusion: The dissolution efficiency of atenolol was enhanced when starch oxalate was found to be a superdisintegrant when combined with sodium starch glycolate, crospovidone and, hence to provide immediate release of the formulated fast dissolving tablets contained drug it could be used.

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