Molecular salts of quinine. A crystal engineering route to enhance the aqueous solubility

CrystEngComm ◽  
2021 ◽  
Author(s):  
Indira S Divya ◽  
Amrutha Surendran ◽  
Sunil SeethaLekshmi ◽  
Sunil Varughese
Keyword(s):  
Crystal Engineering ◽  
Classification System ◽  
Dicarboxylic Acids ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Bcs Class Ii ◽  
Molecular Salts ◽  
Aliphatic Dicarboxylic Acids ◽  
Biopharmaceutical Classification System

The anti-malarial drug quinine (QUN) has poor aqueous solubility and belongs to Biopharmaceutical Classification System (BCS) Class-II. We report 12 novel molecular salts of QUN with α,ω-aliphatic dicarboxylic acids, and...

scholarly journals PREPARATION, CHARACTERIZATION AND DISSOLUTION STUDY OF SPRAY DRIED SOLID DISPERSIONS OF SIMVASTATIN WITH PVP K25 AND AEROSIL 200

2021 ◽  
Vol 10 (6) ◽  
pp. 3806-3812
Author(s):  
Pritam Singh
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Drying Method ◽  
Bcs Class Ii ◽  
Enhanced Dissolution ◽  
Amorphous Nature ◽  
Characterization Studies

BCS class II is well-known for the drugs, having poor aqueous solubility and high permeability. Simvastatin is also categorized as BCS class II, suffering from poor aqueous solubility, affecting its bioavailability. In an attempt to resolve this problem, solid dispersions of simvastatin were prepared by spray-drying method. Solid dispersions of simvastatin with PVP K25 and aerosol in ratio (1:1:1 to 1:5:1) and without aerosil 200 (1:1 to 1:5) were prepared by spray drying method. The dissolution test showed the enhancement of dissolution as compared to the pure drug and nearly equal to marketed formulation “SIMVOTIN 20mg” in both types of formulation, but formulations with aerosil 200 showed faster drug release as compared to the simple formulations without aerosil. The formulation containing the 1:3:1 (simvastatin: PVP K25: Aerosil 200) showed the faster drug release as compared to other formulation that do not contain the Aerosil 200. Other characterization studies were also performed such as FTIR, differential scanning colorimetry and powdered X-ray crystallographic studies. These studies showed the increased amorphous nature of the drug in the formulation, which explain the enhanced dissolution rate of the drug for these formulations.

scholarly journals Formulation Development and Evaluation of Liposphere of Poor Water Soluble Drug for Hyperlipidemia

2021 ◽  
Vol 11 (2) ◽  
pp. 23-30
Author(s):  
Anil Kumar ◽  
Umesh K. Jain ◽  
Ajay Patel
Keyword(s):  
Drug Release ◽  
Stearic Acid ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Water Soluble ◽  
Fibric Acid Derivative ◽  
Formulation Development ◽  
Bcs Class Ii ◽  
Paraffin Oil

Lipospheres offer a new approach to improve an aqueous solubility of BCS class-II drugs. Simvastatin is a third generation fibric acid derivative belonging to this class, employed clinically as a hypolipidemic agent to lessen the risk caused by atherosclerosis. An attempt was made to improve aqueous solubility of Simvastatin by aid of stearic acid and Paraffin oil. The factorial batches of the Simvastatin lipospheres were formulated by melt dispersion technique using 32 factorial design with variables X1- concentration of stearic acid and X2- concentration of paraffin oil and responses Y1 - % Drug Entrapment (% DE) and Y2 - % Drug Release (% DR). From the surface response graphs the optimized batch was formulated and evaluated for saturation solubility, in-vitro drug release studies. Significant improvement in the aqueous solubility of the drug in the Simvastatin lipospheres supports the applicability of lipospheres as a tool for improving aqueous solubility of the BCS class-II drugs. Keywords: Linospheres; Simvastatin; Drug release; Hyperlipidemic; Drug entrapment.

scholarly journals Cellulosic Polymers for Enhancing Drug Bioavailability in Ocular Drug Delivery Systems

2021 ◽  
Vol 14 (11) ◽  
pp. 1201
Author(s):  
Bharti Gupta ◽  
Varsha Mishra ◽  
Sankalp Gharat ◽  
Munira Momin ◽  
Abdelwahab Omri
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Delivery Systems ◽  
Solubility Enhancement ◽  
Ocular Drug Delivery ◽  
Drug Bioavailability ◽  
Bcs Class Ii ◽  
Cellulosic Polymers

One of the major impediments to drug development is low aqueous solubility and thus poor bioavailability, which leads to insufficient clinical utility. Around 70–80% of drugs in the discovery pipeline are suffering from poor aqueous solubility and poor bioavailability, which is a major challenge when one has to develop an ocular drug delivery system. The outer lipid layer, pre-corneal, dynamic, and static ocular barriers limit drug availability to the targeted ocular tissues. Biopharmaceutical Classification System (BCS) class II drugs with adequate permeability and limited or no aqueous solubility have been extensively studied for various polymer-based solubility enhancement approaches. The hydrophilic nature of cellulosic polymers and their tunable properties make them the polymers of choice in various solubility-enhancement techniques. This review focuses on various cellulose derivatives, specifically, their role, current status and novel modified cellulosic polymers for enhancing the bioavailability of BCS class II drugs in ocular drug delivery systems.

Novel Solid Forms of Insomnia Drug Suvorexant with Improved Solubility and Dissolution: Accessing Salts from Salt-Solvates Route

CrystEngComm ◽  
2021 ◽  
Author(s):  
Suman Gundlapalli ◽  
Ramesh Devarapalli ◽  
Ramesh Reddy Mudda ◽  
Ramanaiah Chennuru ◽  
Ravi Chandra Babu Rupakula
Keyword(s):  
Receptor Antagonist ◽  
Classification System ◽  
Class Ii ◽  
Biopharmaceutics Classification System ◽  
High Permeability ◽  
Poor Solubility ◽  
Bcs Class Ii ◽  
Biopharmaceutics Classification

Suvorexant (SRX) is a dual orexin receptor antagonist used for the treatment of insomnia. It belongs to the Biopharmaceutics Classification System (BCS) class-II with high permeability and poor solubility in...

scholarly journals Improved Solubility of Vortioxetine Using C2-C4 Straight-Chain Dicarboxylic Acid Salt Hydrates

Crystals ◽  
2018 ◽  
Vol 8 (9) ◽  
pp. 352 ◽  
Author(s):  
Lei Gao ◽  
Xian-Rui Zhang ◽  
Shao-Ping Yang ◽  
Juan-Juan Liu ◽  
Chao-Jie Chen
Keyword(s):  
Dicarboxylic Acid ◽  
Crystal Engineering ◽  
Dicarboxylic Acids ◽  
Acid Salt ◽  
X Ray Diffraction ◽  
Straight Chain ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Salt Hydrates ◽  
Aliphatic Dicarboxylic Acids

The purpose of this study was to improve the solubility of vortioxetine by crystal engineering principles. In this paper, three C2-C4 straight-chain dicarboxylic acid salt hydrates of vortioxetine (VOT-OA, VOT-MA-H2O, and VOT-SUA-H2O, VOT = vortioxetine, OA = Oxalic acid, MA = malonic acid, SUA = succinic acid) were synthesized and characterized by single X-ray diffraction, powder X-ray diffraction, and differential scanning calorimetry. The single crystal structure of three salts reveals that vortioxetine has torsional flexibility, which can encourage VOT to allow combination with aliphatic dicarboxylic acids through N+-H···O hydrogen bonds. The solubility of all salts exhibits a dramatic increase in distilled water, especially for VOT-MA-H2O salt, where it shows the highest solubility, by 96-fold higher compared with pure vortioxetine.

FORMULATION AND OPTIMIZATION OF TELMISARTAN MULTIPARTICULATE SYSTEM USING A 22 FACTORIAL DESIGN

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (03) ◽  
pp. 47-51
Author(s):  
G Sailesh ◽  
◽  
T. E. G. K. Murthy
Keyword(s):  
Factorial Design ◽  
Classification System ◽  
Water Solubility ◽  
Class Ii ◽  
Treatment Of Hypertension ◽  
Poor Water Solubility ◽  
Biopharmaceutical Classification System

Telmisartan is used in the treatment of hypertension. It exhibits poor water solubility. It belongs to class II of Biopharmaceutical Classification system (BCS). It needs enhancement in dissolution and hence bioavailability. The dissolution of drug was improved by coating the drug and carrier over sugar spheres.Size of sugar spheres and concentration of the carrier were two critical variables that were found to affect the dissolution of drug. A 22 factorial design was used to study the effect of concentration of carrier and size of the non-pareil seeds on dissolution. Dissolution of telmisartan was found to increase with increasing concentration of carrier and decreased with respect to size of non-pareil seeds.

Enhanced Aqueous Solubility of the Solid Forms of a BCS Class-II Anti-Tuberculosis Drug, Prothionamide

2020 ◽  
Vol 20 (8) ◽  
pp. 5086-5096 ◽  
Author(s):  
S. Amrutha ◽  
Lopamudra Giri ◽  
Sunil SeethaLekshmi ◽  
Sunil Varughese
Keyword(s):  
Aqueous Solubility ◽  
Class Ii ◽  
Bcs Class Ii
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