Physicochemical Characterization of a New Crystal Form and Improvements in the Pharmaceutical Properties of the Poorly Water-Soluble Antiosteoporosis Drug 3,9-bis(N,N-Dimethylcarbamoy-loxy)- 5H-benzofuro[3,2-c]quinoline-6-one (KCA-098) by Solid Dispersion with Hydroxypropylcellulose

2000 ◽  
Vol 5 (4) ◽  
pp. 443-454 ◽  
Author(s):  
Tatsuhiko Yamada ◽  
Noriyasu Saito ◽  
Makoto Anraku ◽  
Teruko Imai ◽  
Masaki Otagiri
Keyword(s):  
Solid Dispersion ◽  
Physicochemical Characterization ◽  
Crystal Form ◽  
Water Soluble ◽  
Poorly Water Soluble ◽  
Pharmaceutical Properties

scholarly journals Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

2009 ◽  
Vol 59 (4) ◽  
pp. 453-461 ◽  
Author(s):  
Vikrant Vyas ◽  
Pankajkumar Sancheti ◽  
Poonam Karekar ◽  
Manali Shah ◽  
Yogesh Pore
Keyword(s):  
Solid Dispersion ◽  
Binary Systems ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Water Soluble Drug ◽  
Dispersion Systems ◽  
Rapid Dissolution

Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407 Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (DE30 70.9 ± 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug, indicating altered rheological characteristics of the polymer at its higher concentration, which might have retarded the release rate of tadalafil.

scholarly journals Solid Dispersion: Solubility Enhancement Technique of Poorly Water Soluble Drug

2020 ◽  
Vol 10 (1) ◽  
pp. 173-177 ◽  
Author(s):  
, Ikram ◽  
Kapil Kumar
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Inert Carrier ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion is a technique which is widely and successfully applied to improve the solubility, dissolution rates and consequently the bioavailability of poorly soluble drugs. Dispersion of one or more active ingredients (hydrophobic) is done with an inert carrier (hydrophilic) at solid-state prepared by fusion method, solvent, and melting solvent method. In this review article, we have focused on the methods of preparation, advantages, disadvantages and characterization of the solid dispersions. Keywords: Solid dispersion; dissolution; solubility.

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.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

scholarly journals Synthesis, Characterization and Bactericidal Activity of a 4-Ammoniumbuthylstyrene-Based Random Copolymer

Polymers ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1140
Author(s):  
Silvana Alfei ◽  
Gabriella Piatti ◽  
Debora Caviglia ◽  
Anna Maria Schito
Keyword(s):  
Antibacterial Activity ◽  
Bactericidal Activity ◽  
Antimicrobial Agents ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
Random Copolymer ◽  
Water Soluble ◽  
Cationic Polymers ◽  
Severe Infections

The growing resistance of bacteria to current chemotherapy is a global concern that urgently requires new and effective antimicrobial agents, aimed at curing untreatable infection, reducing unacceptable healthcare costs and human mortality. Cationic polymers, that mimic antimicrobial cationic peptides, represent promising broad-spectrum agents, being less susceptible to develop resistance than low molecular weight antibiotics. We, thus, designed, and herein report, the synthesis and physicochemical characterization of a water-soluble cationic copolymer (P5), obtained by copolymerizing the laboratory-made monomer 4-ammoniumbuthylstyrene hydrochloride with di-methyl-acrylamide as uncharged diluent. The antibacterial activity of P5 was assessed against several multi-drug-resistant clinical isolates of both Gram-positive and Gram-negative species. Except for strains characterized by modifications of the membrane charge, most of the tested isolates were sensible to the new molecule. P5 showed remarkable antibacterial activity against several isolates of genera Enterococcus, Staphylococcus, Pseudomonas, Klebsiella, and against Escherichia coli, Acinetobacter baumannii and Stenotrophomonas maltophilia, displaying a minimum MIC value of 3.15 µM. In time-killing and turbidimetric studies, P5 displayed a rapid non-lytic bactericidal activity. Due to its water-solubility and wide bactericidal spectrum, P5 could represent a promising novel agent capable of overcoming severe infections sustained by bacteria resistant the presently available antibiotics.

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.

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