scholarly journals Molecular complexation of curcumin with Eudragit� EPO to enhance the aqueous solubility, stability and bioavailability of curcumin

2016 ◽  
Vol 4 ◽  
Author(s):  
Kesharwani Siddharth ◽  
Kumar Sunny ◽  
Mathur Himanshi ◽  
Tyagi Mohit ◽  
Bhat G Jayarama ◽  
...  
Keyword(s):  
Aqueous Solubility ◽  
Molecular Complexation ◽  
Eudragit Epo

Molecular complexation of curcumin with pH sensitive cationic copolymer enhances the aqueous solubility, stability and bioavailability of curcumin

2016 ◽  
Vol 82 ◽  
pp. 86-96 ◽  
Author(s):  
Sunny Kumar ◽  
Siddharth S. Kesharwani ◽  
Himanshi Mathur ◽  
Mohit Tyagi ◽  
G. Jayarama Bhat ◽  
...  
Keyword(s):  
Aqueous Solubility ◽  
Ph Sensitive ◽  
Molecular Complexation

Solubility Enhancement of Poorly Soluble Drug Simvastatin by Solid Dispersion Technique

2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N
Keyword(s):  
Dissolution Rate ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Onset Of Action ◽  
Kneading Method ◽  
Wetting Property ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Low Solubility

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.

Revised aqueous solubility product constants and a simple laboratory synthesis of the Pb(II) hydroxycarbonates: Plumbonacrite and hydrocerussite

2017 ◽  
Vol 51 (4) ◽  
pp. 315-328
Author(s):  
Arturo Mendoza-Flores ◽  
Mario Villalobos ◽  
Teresa Pi-Puig ◽  
Nadia Valentina Martínez-Villegas
Keyword(s):  
Solubility Product ◽  
Aqueous Solubility ◽  
Laboratory Synthesis

Ruthenium Complexes for 1- and 2-Photon Photodynamic Therapy: From In Silico Prediction to In Vivo Applications

2020 ◽  
Author(s):  
Johannes Karges ◽  
Shi Kuang ◽  
Federica Maschietto ◽  
Olivier Blacque ◽  
Ilaria Ciofini ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
In Silico ◽  
Aqueous Solubility ◽  
The Body ◽  
Photon Absorption ◽  
Multicellular Tumor Spheroids ◽  
Spectral Window ◽  
Photon Excitation ◽  
Polypyridine Complexes

<div>The use of photodynamic therapy (PDT) against cancer has received increasing attention overthe recent years. However, the application of the currently approved photosensitizers (PSs) is somehow limited by their poor aqueous solubility, aggregation, photobleaching and slow clearance from the body. To overcome these limitations, there is a need for the development of new classes of PSs with ruthenium(II) polypyridine complexes currently gaining momentum. However, these compounds generally lack significant absorption in the biological spectral window, limiting their application to treat deep-seated or large tumors. To overcome this drawback, ruthenium(II) polypyridine complexes designed in silico with (E,E’)-4,4´-bisstyryl 2,2´-bipyridine ligands showed impressive 1- and 2-Photon absorption up to a magnitude higher than the ones published so far. While non-toxic in the dark, these compounds were found phototoxic in various 2D monolayer cells, 3D multicellular tumor spheroids and be able to eradicate a multiresistant tumor inside a mouse model upon clinically relevant 1-Photon and 2 Photon excitation.</div>

A Free Energy Perturbation Approach to Estimate the Intrinsic Solubilities of Drug-like Small Molecules

2019 ◽  
Author(s):  
Sayan Mondal ◽  
Gary Tresadern ◽  
Jeremy Greenwood ◽  
Byungchan Kim ◽  
Joe Kaus ◽  
...  
Keyword(s):  
Solid State ◽  
Small Molecules ◽  
Three Dimensional ◽  
Aqueous Solubility ◽  
Computational Approach ◽  
Free Energy Perturbation ◽  
Perturbation Approach ◽  
Energy Perturbation ◽  
State Form ◽  
Good Agreement

<p>Optimizing the solubility of small molecules is important in a wide variety of contexts, including in drug discovery where the optimization of aqueous solubility is often crucial to achieve oral bioavailability. In such a context, solubility optimization cannot be successfully pursued by indiscriminate increases in polarity, which would likely reduce permeability and potency. Moreover, increasing polarity may not even improve solubility itself in many cases, if it stabilizes the solid-state form. Here we present a novel physics-based approach to predict the solubility of small molecules, that takes into account three-dimensional solid-state characteristics in addition to polarity. The calculated solubilities are in good agreement with experimental solubilities taken both from the literature as well as from several active pharmaceutical discovery projects. This computational approach enables strategies to optimize solubility by disrupting the three-dimensional solid-state packing of novel chemical matter, illustrated here for an active medicinal chemistry campaign.</p>

Formulation and Evaluation of Baclofen Orally Disintegrating Tablets

1970 ◽  
Vol 2 (4) ◽  
pp. 733-738
Author(s):  
Dumpeti Janardhan ◽  
Joginapally Sreekanth ◽  
P.Theja Pavan Kumar ◽  
M.Vamshi Krishna
Keyword(s):  
Pilot Scale ◽  
Taste Masking ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Disintegration Time ◽  
Granulation Process ◽  
Good Taste ◽  
Orally Disintegrating Tablets ◽  
Human Volunteers ◽  
Eudragit Epo

The purpose of this study was to evaluate the potential of polymers for masking the taste of bitter drugs when incorporated into orally disintegrating tablets. The tablets were produced by simple wet granulation technique with a model compound (baclofen) which is moderately bitter. The formulating procedure had two variables to obtain good taste masking with desirable characteristics. The optimal granulation process parameters were polymer selection and its concentration (w/w), suitable for pilot scale level. Dextrates, β- cyclodextrin, eudragit EPO and PVP K-30 were used in preparation of granules by using water and iso-propyl alcohol. Crospovidone was used intra and extra granularly as superdisintegrant.  Sodium bicarbonate and citric acid were used as effervescent for fast disintegration of tablets, which also optionally act as desensitizer of taste buds. Results from evaluation of tablets indicated a disintegration time (avg) of 30-35 sec and 100% drug release was achieved within 5 min. But taste masking was achieved by only with eudragit EPO. Results from an evaluation by a panel of six human volunteers demonstrated that the orally disintegrating tablets which are prepared by using polymer Eudragit EPO (5% and 7.5% w/w of tablet) and PVP (7.5% w/w of tablet) improved taste, significantly. On studying physical parameters, F9 formulation demonstrated acceptable level of hardness and friability with good taste masking and it was thus considered as an optimized formulation

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