scholarly journals Enhancement of solubility and therapeutic potential of poorly soluble lovastatin by SMEDDS formulation adsorbed on directly compressed spray dried magnesium aluminometasilicate liquid loadable tablets: A study in diet induced hyperlipidemic rabbits

2015 ◽  
Vol 10 (1) ◽  
pp. 40-56 ◽  
Author(s):  
Mohd Javed Qureshi ◽  
Chitneni Mallikarjun ◽  
Wong Gan Kian
Keyword(s):  
Therapeutic Potential ◽  
Poorly Soluble ◽  
Spray Dried

scholarly journals Spray-Dried Amorphous Solid Dispersions of Griseofulvin in HPC/Soluplus/SDS: Elucidating the Multifaceted Impact of SDS as a Minor Component

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 197 ◽  
Author(s):  
Mahbubur Rahman ◽  
Stephanie Ahmad ◽  
James Tarabokija ◽  
Nathaniel Parker ◽  
Ecevit Bilgili
Keyword(s):  
Solid Dispersions ◽  
Sodium Dodecyl ◽  
Minor Component ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersions ◽  
Acetone Water ◽  
Poorly Soluble ◽  
A Minor ◽  
The Impact ◽  
Spray Dried

This study aimed to elucidate the impact of a common anionic surfactant, sodium dodecyl sulfate (SDS), along with hydroxypropyl cellulose (HPC) and Soluplus (Sol) on the release of griseofulvin (GF), a poorly soluble drug, from amorphous solid dispersions (ASDs). Solutions of 2.5% GF and 2.5%–12.5% HPC/Sol with 0.125% SDS/without SDS were prepared in acetone–water and spray-dried. The solid-state characterization of the ASDs suggests that GF–Sol had better miscibility and stronger interactions than GF–HPC and formed XRPD-amorphous GF, whereas HPC-based ASDs, especially the ones with a lower HPC loading, had crystalline GF. The dissolution tests show that without SDS, ASDs provided limited GF supersaturation (max. 250%) due to poor wettability of Sol-based ASDs and extensive GF recrystallization in HPC-based ASDs (max. 50%). Sol-based ASDs with SDS exhibited a dramatic increase in supersaturation (max. 570%), especially at a higher Sol loading, whereas HPC-based ASDs with SDS did not. SDS did not interfere with Sol’s ability to inhibit GF recrystallization, as confirmed by the precipitation from the supersaturated state and PLM imaging. The favorable use of SDS in a ternary ASD was attributed to both the wettability enhancement and its inability to promote GF recrystallization when used as a minor component along with Sol.

Development of an Oral Curcumin Nanocrystal Formulation

2012 ◽  
Vol 3 (4) ◽  
Author(s):  
R. Ravichandran
Keyword(s):  
The Body ◽  
Dissolution Behavior ◽  
Poorly Soluble Drugs ◽  
Solid Dosage Forms ◽  
Bioavailability Enhancement ◽  
Solid Dosage ◽  
Rapid Dissolution ◽  
Poorly Soluble ◽  
Drug Nanocrystal ◽  
Spray Dried

During the last ten years, the formulation of drugs as nanocrystals has rapidly evolved into a mature drug delivery strategy, with currently five products on the market. The major characteristic of these systems is the rapid dissolution velocity, enabling bioavailability enhancement after oral administration. This study describes the preparation of a solid dosage capsule form of spray-dried curcumin nanocrystal and compares its dissolution behavior with market capsule in different media. The aim was to obtain a stable nanocrystal loaded drug capsule with an increased drug saturation solubility and dissolution velocity. The solubility and dissolution experiments were performed to verify the obvious improvement of the dissolution behavior compared with commercial product. Improved dissolution behavior in drug nanocrystal-loaded solid dosage forms should lead to better bioavailability of poorly soluble drugs in the body.

Cardiovascular safety pharmacology studies in dogs enabled for a poorly soluble molecule using spray-dried dispersion: Impact on lead selection

2016 ◽  
Vol 512 (1) ◽  
pp. 137-146 ◽  
Author(s):  
Yin-Chao Tseng ◽  
Brian Linehan ◽  
Khing Jow Ng ◽  
Dustin M. Smith ◽  
Michael Markert ◽  
...  
Keyword(s):  
Cardiovascular Safety ◽  
Safety Pharmacology ◽  
Lead Selection ◽  
Poorly Soluble ◽  
Soluble Molecule ◽  
Spray Dried

scholarly journals Amelioration of Diabetes and Painful Diabetic Neuropathy byPunica granatumL. Extract and Its Spray Dried Biopolymeric Dispersions

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
K. Raafat ◽  
W. Samy
Keyword(s):  
Diabetic Neuropathy ◽  
Therapeutic Potential ◽  
Antinociceptive Effect ◽  
Punica Granatum ◽  
Glucose Levels ◽  
Peripheral Nerve Function ◽  
And Control ◽  
Dose Levels ◽  
Spray Dried

Aims.To evaluate the effect ofPunica granatum(Pg) rind extract and its spray dried biopolymeric dispersions with casein (F1) or chitosan (F2) againstDiabetes mellitus(DM) and diabetic neuropathy (DN).Methods.We measured the acute (6 h) and subacute (8 days) effect of various doses ofPg, F1, and F2 and the active compounds on alloxan-induced DM mouse model. We evaluated DN utilizing latency tests for longer period of time (8 weeks). In addition, thein vivoantioxidant activity was assessed utilizing serum catalase level.Results.The results proved that the highest dose levels ofPgextract, F1, F2 exerted remarkable hypoglycemic activity with 48, 52, and 40% drop in the mice glucose levels after 6 hours, respectively. The tested compounds also improved peripheral nerve function as observed from the latency tests. Bioguided fractionation suggested that gallic acid (GA) wasPgmain active ingredient responsible for its actions.Conclusion. Pgextract, F1, F2, and GA could be considered as a new therapeutic potential for the amelioration of diabetic neuropathic pain and the observedin vivoantioxidant potential may be involved in its antinociceptive effect. It is highly significant to pay attention toPgand GA for amelioration and control of DM and its complications.

scholarly journals PARTIAL AMORPHIZATION OF POORLY-SOLUBLE SIMVASTATIN USP USING MEDIA MILLING IN SYNERGISM WITH SPRAY-DRYING

2020 ◽  
pp. 114-121
Author(s):  
HARITA R. DESAI ◽  
ARCHANA B. RAJADHYAX ◽  
PURNIMA D. AMIN
Keyword(s):  
Differential Scanning Calorimetry ◽  
Spray Drying ◽  
Scanning Calorimetry ◽  
Intrinsic Dissolution ◽  
X Ray ◽  
Media Milling ◽  
Rate Testing ◽  
Poorly Soluble ◽  
Spray Dried

Objective: The objective of the current study was to explore top down methods of size reduction like high speed homogenisation and media milling in synergism with spray drying in amorphization and solubility enhancement of BCS Class II antilipidemic drug Simvastatin USP. Methods: Spray-dried micronized simvastatin USP was formulated by homogenisation and media milling of drug suspension in optimized stabilizer solution. Stabilizer combination, duration of homogenisation and ball milling and drug: stabilizer ratio was optimized. The obtained dispersion was transformed into solid powder using spray drying. The obtained Spray-dried micronized Simvastatin USP was evaluated for visual morphology, Infrared spectroscopy, Differential scanning calorimetry, in vitro drug release studies, X-Ray diffractometry, Scanning electron microscopy, contact angle measurement, solubility studies, dispersibility studies and intrinsic dissolution rate testing. Results: Spray-dried micronized simvastatin USP was found to show amorphization of crystalline Simvastatin USP as confirmed by the absence of drug peak in Differential scanning calorimetry and lowered signal intensity in X-Ray diffraction studies. Spray-dried micronized Simvastatin USP was found to show enhanced drug hydrophilicity and solubility as confirmed by lowering in contact angle and increase in solubility and ease of dispersibility observations. In vitro dissolution testing and intrinsic dissolution rate testing were found to show an increase in drug release from 11% to 79% and 4 mg min-1 cm-2 to 17 mg min-1 cm-2 for drug and Spray-dried micronized Simvastatin USP respectively. Conclusion: Media milling in synergism with spray-drying was found to be a prospective solubility enhancement technique for poorly-soluble Simvastatin USP.

Spray-dried redispersible oil-in-water emulsion to improve oral bioavailability of poorly soluble drugs

2003 ◽  
Vol 19 (4) ◽  
pp. 273-280 ◽  
Author(s):  
Gilles Dollo ◽  
Pascal Le Corre ◽  
Alexis Guérin ◽  
François Chevanne ◽  
Jean Louis Burgot ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Poorly Soluble Drugs ◽  
Water Emulsion ◽  
Oil In Water ◽  
Poorly Soluble ◽  
Oil In Water Emulsion ◽  
Spray Dried

scholarly journals Computer-Aided Discovery of New Solubility-Enhancing Drug Delivery System

Biomolecules ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 913
Author(s):  
Mikołaj Mizera ◽  
Eugene N. Muratov ◽  
Vinicius M. Alves ◽  
Alexander Tropsha ◽  
Judyta Cielecka-Piontek
Keyword(s):  
Therapeutic Potential ◽  
Aqueous Solubility ◽  
Cefuroxime Axetil ◽  
Structure Property ◽  
Pharmaceutical Ingredients ◽  
Structure Property Relationship ◽  
Poorly Soluble ◽  
The Stability ◽  
First Time ◽  
Poor Stability

The poor aqueous solubility of active pharmaceutical ingredients (APIs) places a limit on their therapeutic potential. Cyclodextrins (CDs) have been shown to improve the solubility of APIs, but the magnitude of the improvement depends on the structure of both the CDs and APIs. We have developed quantitative structure–property relationship (QSPR) models that predict the stability of the complexes formed by a popular poorly soluble antibiotic, cefuroxime axetil (CA) and different CDs. We applied this model to five CA–CD systems not included in the modeling set. Two out of three systems predicted to have poor stability and poor CA solubility, and both CA–CD systems predicted to have high stability and high CA solubility were confirmed experimentally. One of the CDs that significantly improved CA solubility, methyl-βCD, is described here for the first time, and we propose this CD as a novel promising excipient. Computational approaches and models developed and validated in this study could help accelerate the development of multifunctional CDs-based formulations.

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