Improvement of Dissolution and Oral Absorption of ER-34122, A Poorly Water-Soluble Dual 5-Lipoxygenase/Cyclooxygenase Inhibitor With Anti-Inflammatory Activity by Preparing Solid Dispersion

2002 ◽  
Vol 91 (1) ◽  
pp. 258-266 ◽  
Author(s):  
Ikuo Kushida ◽  
Masaki Ichikawa ◽  
Naoki Asakawa
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Water Soluble ◽  
Inflammatory Activity ◽  
Cyclooxygenase Inhibitor ◽  
Poorly Water Soluble ◽  
Anti Inflammatory

scholarly journals Enhancement of solubility of poorly soluble drugs by solid dispersion: An Overview

2017 ◽  
Vol 5 (04) ◽  
pp. 17-23
Author(s):  
Katta Manogna ◽  
P. Nagaveni ◽  
K. Thyagaraju
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Drug Solubility ◽  
Solid Dosage Forms ◽  
Preparation Methods ◽  
Solid Dosage ◽  
Poorly Soluble ◽  
Poorly Water Soluble

Most of the newly invented chemical drug moieties are poorly water soluble. According to BCS classification, class II and IV drugs are considered as poorly water soluble. So enhancement of oral absorption and bioavailability of solid dosage forms remains a challenge to formulation scientists due to their solubility criteria. Therefore many techniques are being explored to enhance the solubility of poor soluble drugs. Solid dispersion is one of the most important method for enhance the solubility (dissolution rate) and hence oral bioavailability of poorly soluble drugs. In solid dispersion the particle size of drug is reduced or a crystalline pure drug is converted into amorphous form and hence the solubility is increased. Polymer incorporating in solid dispersion technology is usually hydrophilic in nature and also showing compatibility with the drug to enhance the drug solubility. This review mainly discus about solid dispersion, preparation methods, and finally characterization.

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

Design and Synthesis of Novel Anti-inflammatory/Anti-ulcer Hybrid Molecules with Antioxidant Activity

2020 ◽  
Vol 16 ◽  
Author(s):  
Bhim Bahadur Chaudhari ◽  
Alka Bali ◽  
Ajitesh Balaini
Keyword(s):  
Antioxidant Activity ◽  
Oral Absorption ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Antioxidant Potential ◽  
Inflammatory Activity ◽  
In Vivo Models ◽  
Standard Drug ◽  
Hybrid Molecules ◽  
Anti Inflammatory

Background: NSAIDs are the most widely prescribed medications worldwide for their anti-inflammatory, antipyretic, and analgesic effects However, their chronic use can lead to several adverse drug events including GI toxicity. The selective COX-2 inhibitors developed as gastro-sparing NSAIDs also suffer from serious adverse effects which limit their efficacy. Objective: Local generation of reactive oxygen species is implicated in NSAID-mediated gastric ulceration and their combination with H2 antagonists like famotidine reduces the risk of ulcers. The objective of this work was to design and synthesize novel methanesulphonamido isoxazole derivatives by hybridizing the structural features of NSAIDs with those of antiulcer drugs (ranitidine, famotidine, etc.) to utilize a dual combination of anti-inflammatory activity and reducing (antioxidant) potential. Method: The designing process utilized three dimensional similarity studies and utilized an isoxazole core having a potential for anti-inflammatory as well as radical scavenging antioxidant activity. The compounds were assayed for their antiinflammatory activity in established in vivo models. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. Results: Compounds (5, 6, 9 and 10) showed anti-inflammatory activity comparable to the standard drugs and were also found to be non-ulcerogenic at the test doses. Compounds 6-10 exhibited good antioxidant effect in the concentration range of 1.0-50.0 µmol/ml. The test compounds were also found to comply with the Lipinski rule suggesting good oral absorption. Conclusion: A new series of isoxazole based compounds is being reported with good anti-inflammatory activity coupled with antioxidant potential as gastro-sparing anti-inflammatory agents.

Formulation and Food Effects on the Oral Absorption of a Poorly Water Soluble, Highly Permeable Antiretroviral Agent

2002 ◽  
Vol 91 (6) ◽  
pp. 1390-1395 ◽  
Author(s):  
Bruce J. Aungst ◽  
Nhung H. Nguyen ◽  
Nancy J. Taylor ◽  
Dilbir S. Bindra
Keyword(s):  
Oral Absorption ◽  
Water Soluble ◽  
Food Effects ◽  
Poorly Water Soluble

BEHAVIOURAL STUDY OF CYCLODEXTRIN INCLUSION COMPLEX ON ENHANCEMENT OF SOLUBILITY OF ACECLOFENAC

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (11) ◽  
pp. 19-23
Author(s):  
J Shaikh ◽  
◽  
S. V. Deshmane ◽  
R. N Purohit ◽  
K. R. Biyani
Keyword(s):  
Inclusion Complex ◽  
Solid Dispersion ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Solubility Study ◽  
Cyclodextrin Inclusion ◽  
Poorly Water Soluble ◽  
Cyclodextrin Inclusion Complex

The main objective of the present study was to enhance the solubility and dissolution rate of poorly water soluble aceclofenac using its solid dispersion with β-cyclodextrin. FTIR and DSC study was carried out to find out any incompatibility. The phase solubility of drug was carried out in 1, 2, 5, and 10% of β-cyclodextrin in distilled water. Kneading method and solvent evaporation method was use to prepared solid dispersion of aceclofenac and β-cyclodextrin. Different evaluation tests like solubility study in different solvents, PXRD and in vitro dissolution study of aceclofenac- β-cyclodextrin inclusion complex were carried out. The overall finding indicated that β-cyclodextrin is a desirable water soluble carrier, that helps in increasing solubility of drug. Due to its structural feature, β-cyclodextrin forms a good inclusion complex that decreases contact angle of drug with water molecules by increasing wetting properties. Hence, it can be concluded that, β-cyclodextrin is better water soluble carrier molecule in terms of its compatibility and increasing solubility behavior of poorly water soluble drug aceclofenac.

ENHANCED DISSOLUTION OF A POORLY WATER-SOLUBLE DRUG BY SOLID DISPERSIONS (SOLVENT EVAPORATION) TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 13-19
Author(s):  
R. O Sonawane ◽  
◽  
S. Nayak ◽  
M. D. Chaudhari ◽  
V. V. Pande
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Differential Scanning Calorimetric ◽  
Maximum Enhancement ◽  
Enhanced Dissolution ◽  
Water Soluble Drugs ◽  
Fusion Methods ◽  
Poorly Water Soluble

The poorly water soluble drugs tend to have low bioavailability and this can be improved by several methods. Solid dispersion is a promising formulation approach to improve solubility and dissolution and ultimately oral bioavailability of these drugs. The aim of this study was to prepare and characterize solid dispersion of anti-diabetic glimepiride, a BCS class II drug, with the hydrophilic carrier PVP K30 by solvent evaporation and microwave induced fusion methods. Scanning electron microscopy (SEM), X–ray powder diffractometry (XRD) and differential scanning calorimetric (DSC) were used to evaluate the physical state of the drug. The solid dispersions were also evaluated for drug content, solubility and dissolution studies. Solid dispersions prepared by solvent evaporation method were showed maximum enhancement of solubility and dissolution in comparison to that prepared by other method.

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.

scholarly journals Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1679
Author(s):  
Thao T.D. Tran ◽  
Phuong H.L. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Insoluble Polymers

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

Sign in / Sign up

Export Citation Format

Share Document