Effect of hydrotalcite-like compounds on the aqueous solubility of some poorly water-soluble drugs

2003 ◽  
Vol 92 (7) ◽  
pp. 1407-1418 ◽  
Author(s):  
Valeria Ambrogi ◽  
Giuseppe Fardella ◽  
Giuliano Grandolini ◽  
Morena Nocchetti ◽  
Luana Perioli
Keyword(s):  
Aqueous Solubility ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

scholarly journals Solubility enhancement of carvedilol using drug–drug cocrystallization with hydrochlorothiazide

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shivarani Eesam ◽  
Jaswanth S. Bhandaru ◽  
Chandana Naliganti ◽  
Ravi Kumar Bobbala ◽  
Raghuram Rao Akkinepally
Keyword(s):  
Aqueous Solubility ◽  
Sem Analysis ◽  
Water Soluble ◽  
High Permeability ◽  
Poorly Water Soluble Drugs ◽  
Drug Discovery And Development ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dissolution In Vitro

Abstract Background Increasing hydrophilicity of poorly water-soluble drugs is a major challenge in drug discovery and development. Cocrystallization is one of the techniques to enhance the hydrophilicity of such drugs. Carvedilol (CAR), a nonselective beta/alpha1 blocker, used in the treatment of mild to moderate congestive heart failure and hypertension, is classified under BCS class II with poor aqueous solubility and high permeability. Present work is an attempt to improve the solubility of CAR by preparing cocrystals using hydrochlorothiazide (HCT), a diuretic drug, as coformer. CAR-HCT (2:0.5) cocrystals were prepared by slurry conversion method and were characterized by DSC, PXRD, FTIR, Raman, and SEM analysis. The solubility, stability, and dissolution (in vitro) studies were conducted for the cocrystals. Results The formation of CAR-HCT cocrystals was confirmed based on melting point, DSC thermograms, PXRD data, FTIR and Raman spectra, and finally by SEM micrographs. The solubility of the prepared cocrystals was significantly enhanced (7.3 times), and the dissolution (in vitro) was improved by 2.7 times as compared to pure drug CAR. Further, these cocrystals were also found to be stable for 3 months (90 days). Conclusion It may be inferred that the drug–drug (CAR-HCT) cocrystallization enhances the solubility and dissolution rate of carvedilol significantly. Further, by combining HCT as coformer could well be beneficial pharmacologically too.

scholarly journals REVIEW ARTICLE: SOLUBILITY ENHANCEMENT BY SOLID DISPERSION

2017 ◽  
Vol 9 (3) ◽  
pp. 15
Author(s):  
A. N. Patil ◽  
D. M. Shinkar ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Full Potential ◽  
Drug Selection ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Enhancement of solubility, dissolution rate and bioavailability of the drug is a very challenging task in drug development, nearly 40% of the new chemical entities currently being discovered are poorly water soluble drugs. The solubility behaviour of the drugs remains one of the most challenging aspects in formulation development. This results in important products not reaching the market or not achieving their full potential. Solid dispersion is one of the techniques adopted for the formulation of such drugs and various methods are used for the preparation of solid dispersion. Solid dispersion is generally prepared with a drug which is having poor aqueous solubility and hydrophilic carrier. This article review various methods and concept of solid dispersion, criteria for drug selection, advantage and disadvantage, characterization, and application.

Environment safe Method development and Validation of Dolutegravir in Bulk and Tablet dosage form by UV-Visible spectroscopy

2021 ◽  
pp. 139-144
Author(s):  
Poonam A. Borse Salunke ◽  
S.D. Barhate ◽  
Rupali S. Wagh
Keyword(s):  
Method Development ◽  
Aqueous Solubility ◽  
Solubility Enhancement ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Label Claim ◽  
Enhancement Method ◽  
Poorly Water Soluble ◽  
Tablet Dosage

To develop an environment-safe aqueous solubility enhancement method of poorly water-soluble drugs is the need of the pharmaceutical field. Because when organic solvents were used for solubility enhancement, there are many disadvantages like carcinogenicity, environment pollutant, flammable, toxicity, and cost. The hydrotropic method has been used to enhance the aqueous solubility of poorly water-soluble drugs. Dolutegravir is slightly soluble in water. To enhance aqueous solubility various hydrotropes were used and optimized the concentration of each hydrotrope. From these hydrotropes, a mixture of 10% sodium tricitrate and 10% sodium benzoate was selected because Dolutegravir was completely soluble in a mixed hydrotropic solution. Method development and analytical validation were performed. The maximum wavelength of Dolutegravir in the hydrotropic mixture was found a 268nm, and the linearity curve in the range of 5-25µg/ml. A regression coefficient was found to be 0.999. Percent label claim, accuracy (% RSD) were found 99.58%, 0.13(80%), 0.11(100%), 0.13(120%), respectively. The LOD for Dolutegravir was determined to be 0.037μg/ mL, and LOQ was found to be 0.11μg/mL.

Solubility Enhancement Techniques for Poorly Water-Soluble Drugs

2017 ◽  
Vol 10 (3) ◽  
pp. 3701-3708
Author(s):  
Amol S Deshmukh ◽  
Kundan J Tiwari ◽  
Vijay R Mahajan
Keyword(s):  
Plasma Concentrations ◽  
Aqueous Solubility ◽  
Systemic Circulation ◽  
Water Soluble ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Poor Solubility ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for optimum pharmacological response. Poorly water-soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Poor aqueous solubility is a major problem encountered with formulation development of new chemical entities. There are over 40% of new chemical entities that exhibit poor solubility and low bioavailability. As per BCS classification system, these drugs comes under BCS class II that show poor solubility and high permeability. The bioavailability of these drugs can be dramatically improved by increasing the solubility of these drugs. This review article highlights a number of techniques for enhanc

scholarly journals Engineering Cocrystals of Poorly Water-Soluble Drugs to Enhance Dissolution in Aqueous Medium

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 108 ◽  
Author(s):  
Indumathi Sathisaran ◽  
Sameer Dalvi
Keyword(s):  
Crystal Engineering ◽  
Halogen Bonding ◽  
Aqueous Solubility ◽  
Pharmaceutical Formulation ◽  
Water Soluble ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Enhanced Solubility ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Biopharmaceutics Classification System (BCS) Class II and IV drugs suffer from poor aqueous solubility and hence low bioavailability. Most of these drugs are hydrophobic and cannot be developed into a pharmaceutical formulation due to their poor aqueous solubility. One of the ways to enhance the aqueous solubility of poorlywater-soluble drugs is to use the principles of crystal engineering to formulate cocrystals of these molecules with water-soluble molecules (which are generally called coformers). Many researchers have shown that the cocrystals significantly enhance the aqueous solubility of poorly water-soluble drugs. In this review, we present a consolidated account of reports available in the literature related to the cocrystallization of poorly water-soluble drugs. The current practice to formulate new drug cocrystals with enhanced solubility involves a lot of empiricism. Therefore, in this work, attempts have been made to understand a general framework involved in successful (and unsuccessful) cocrystallization events which can yield different solid forms such as cocrystals, cocrystal polymorphs, cocrystal hydrates/solvates, salts, coamorphous solids, eutectics and solid solutions. The rationale behind screening suitable coformers for cocrystallization has been explained based on the rules of five i.e., hydrogen bonding, halogen bonding (and in general non-covalent bonding), length of carbon chain, molecular recognition points and coformer aqueous solubility. Different techniques to screen coformers for effective cocrystallization and methods to synthesize cocrystals have been discussed. Recent advances in technologies for continuous and solvent-free production of cocrystals have also been discussed. Furthermore, mechanisms involved in solubilization of these solid forms and the parameters influencing dissolution and stability of specific solid forms have been discussed. Overall, this review provides a consolidated account of the rationale for design of cocrystals, past efforts, recent developments and future perspectives for cocrystallization research which will be extremely useful for researchers working in pharmaceutical formulation development.

HYDROTROPIC SOLUBILISATION OF IRBESARTAN: MECHANISTIC STUDY AND DISSOLUTION PROFILING

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 74-76
Author(s):  
C Jose ◽  
K Amra ◽  
M. Momin ◽  
Keyword(s):  
Sodium Benzoate ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Mechanistic Study ◽  
Dissolution Profile ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Water Insoluble Drug ◽  
Hydrotropic Agent

Irbesartan (IB) is a water insoluble drug belonging to BCS II that exerts its anti-hypertensive effect through the blockage of angiotensin II receptors. The aqueous insolubility of IB limits its bioavailability and overall efficacy. Hydrotrophy, a solubilization technique to achieve an augmentation in aqueous solubility of poorly water-soluble drugs, has recently gained a lot of interest due to its safety, economics, and use of non-toxic and non-flammable adjuvants. The present study deals with application of hydrotrophy techniques to increase the solubility of IB using sodium benzoate and urea as the hydrotropic agent. The results showed a significant enhancement in dissolution profile of IB as compared to non-hydrotropic drug. The dissolution rate and solubility comparison of both hydrotropic agents revealed that sodium benzoate has a better solubilizing efficiency than urea. Hence, it can be concluded that hydrotropic concept can be adopted as a solubility enhancement technique for poorly water-soluble drugs.

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