Dissolution Rate and Apparent Solubility of Poorly Soluble Drugs in Biorelevant Dissolution Media

2010 ◽  
Vol 7 (5) ◽  
pp. 1419-1430 ◽  
Author(s):  
Jonas H. Fagerberg ◽  
Oksana Tsinman ◽  
Na Sun ◽  
Konstantin Tsinman ◽  
Alex Avdeef ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Poorly Soluble Drugs ◽  
Biorelevant Dissolution ◽  
Apparent Solubility ◽  
Poorly Soluble ◽  
Biorelevant Dissolution Media

scholarly journals A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound

2021 ◽  
Vol 22 (22) ◽  
pp. 12406
Author(s):  
Emilia Jakubowska ◽  
Bartłomiej Milanowski ◽  
Janina Lulek
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Particle Morphology ◽  
Feed Concentration ◽  
Bottom Up ◽  
Antisolvent Precipitation ◽  
Process Characterization ◽  
Apparent Solubility ◽  
Poorly Soluble ◽  
Successful Approach

Nanosizing is an approach to improve the dissolution rate of poorly soluble drugs. The first aim of this work was to develop nanosuspension of cilostazol with liquid antisolvent precipitation (LASP) and its combination with ultrasound. Second, to systematically study the effect of bottom-up processing factors on precipitated particles’ size and identify the optimal settings for the best reduction. After solvent and stabilizer screening, in-depth process characterization and optimization was performed using Design of Experiments. The work discusses the influence of critical factors found with statistical analysis: feed concentration, stabilizer amount, stirring speed and ultrasound energy governed by time and amplitude. LASP alone only generated particle size of a few microns, but combination with ultrasound was successful in nanosizing (d10 = 0.06, d50 = 0.33, d90 = 1.45 µm). Micro- and nanosuspension’s stability, particle morphology and solid state were studied. Nanosuspension displayed higher apparent solubility than equilibrium and superior dissolution rate over coarse cilostazol and microsuspension. A bottom-up method of precipitation-sonication was demonstrated to be a successful approach to improve the dissolution characteristics of poorly soluble, BCS class II drug cilostazol by reducing its particle size below micron scale, while retaining nanosuspension stability and unchanged crystalline form.

scholarly journals Solubility Enhancement of Poorly soluble Drugs by using Novel Techniques : A Comprehensive Review

2020 ◽  
Vol 13 (2) ◽  
pp. 80-93 ◽  
Author(s):  
Abikesh P.K. Mahapatra ◽  
Vinod Patil ◽  
Ravindra Patil
Keyword(s):  
Dissolution Rate ◽  
Class Ii ◽  
Systemic Circulation ◽  
Poorly Soluble Drugs ◽  
Formulation Development ◽  
Solid Dosage ◽  
Bcs Class Ii ◽  
Pharmacological Response ◽  
Poorly Soluble ◽  
Low Solubility

The primary aim of this review was to improve the solubility and Bioavailability of BCS Class-II drugs because of their low solubility and dissolution rate. Solubility is one of the imp parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Hence the class- II drugs require enhancement in solubility and dissolution rate in there formulation development particularly in solid dosage form such as in tablet and capsule. So because of this there are several methods and newer emerging technologies have been developed for increasing the solubility as well as Bioavailability of class –II drugs. In this article review on literature on newer techniques or methods as well as recent research on formulation development of class- II drugs was done.

Drug Nanocrystals: A Comprehensive Review with Current Regulatory Guidelines

2020 ◽  
Vol 17 (6) ◽  
pp. 470-482
Author(s):  
Mori Dhaval ◽  
Jalpa Makwana ◽  
Ekta Sakariya ◽  
Kiran Dudhat
Keyword(s):  
Dissolution Rate ◽  
Dosage Form ◽  
Poorly Soluble Drugs ◽  
Comprehensive Review ◽  
Drug Molecules ◽  
Regulatory Guidelines ◽  
Poorly Soluble ◽  
Form Design ◽  
Capsule Suspension ◽  
Final Dosage Form

Drug nanocrystals offer an attractive approach for improving the solubility and dissolution rate of poorly soluble drugs which accounts for nearly 40 % newly discovered drug molecules. Both methods for manufacturing drug nanocrystals have high industrial acceptability for being simple and easy to scale which is evident from the number of approved products available in the market. Ability to modify multiple aspects of dosage form like bioavailability, release pattern and dosage form requirement along with flexibility in choosing final dosage form starting from the tablet, capsule, suspension to parenteral one, have made nanocrystal technology one of the very promising and adaptable technology for dosage form design.

ChemInform Abstract: Enhancement the Dissolution Rate and Solubility of Poorly Soluble Drugs: Review

ChemInform ◽  
2014 ◽  
Vol 45 (34) ◽  
pp. no-no
Author(s):  
Mubarak Abdullah Saleh ◽  
Salam A. Mohammed ◽  
Ezzat C. Abdullah ◽  
Laith A. Hashim
Keyword(s):  
Dissolution Rate ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

scholarly journals Evaluation of Poorly Soluble Drugs’ Dissolution Rate by Laser Scattering in Different Water Isotopologues

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 601
Author(s):  
Elena V. Uspenskaya ◽  
Tatiana V. Pleteneva ◽  
Ilaha V. Kazimova ◽  
Anton V. Syroeshkin
Keyword(s):  
Dissolution Rate ◽  
Isotope Effect ◽  
Targeted Delivery ◽  
Kinetic Isotope Effect ◽  
The Body ◽  
Poorly Soluble Drugs ◽  
Laser Scattering ◽  
Kinetic Isotope ◽  
Medicinal Substances ◽  
Poorly Soluble

The most important task in the design of dosage forms is to modify the pharmaceutical substances structure in order to increase solubilization, targeted delivery, controlled rate of drug administration, and its bioavailability. Screening—laboratory (in vitro) or computer (in silico)—as a procedure for selecting a prototype for the design of a drug molecule, involves several years of research and significant costs. Among a large number of solvents and diluents (alcohol, ether, oils, glycerol, Vaseline) used in the pharmaceutical industry for the manufacture of drugs water finds the greatest application. This is because all biological reactions (reactions in living systems) take place in water and distribution of the fluid in the body and the substances found within is critical for the maintenance of intracellular and extracellular functions. Modern studies in the field of the stable isotopic compositions of natural water and its structure and properties make it possible to use isotopic transformations of the water to improve the pharmacokinetic properties of medicinal substances without previous structural modification. It is known that by replacing any of the atoms in the reacting substance molecule with its isotope, it is possible to record changes in the reactivity, which are expressed as a change in the reaction rate constant, i.e., in the manifestation of the kinetic isotope effect (KIE). The article presents the results of studies on the effect of the kinetic isotope effect of a solvent—water—on increasing the solubility and dissolution rate constants of poorly soluble drugs using laser diffraction spectroscopy. The results of the studies can be successfully implemented in pharmaceutical practice to overcome the poor solubility of medicinal substances of classes II and IV, according to the biopharmaceutical classification system (BCS), in water for pharmaceutical purposes by performing its preliminary and safe isotopic modification.

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