scholarly journals Improvement of the water solubility of tolfenamic acid by new multiple-component crystals produced by mechanochemical methods

CrystEngComm ◽  
2014 ◽  
Vol 16 (35) ◽  
pp. 8252-8262 ◽  
Author(s):  
K. Gaglioti ◽  
M. R. Chierotti ◽  
F. Grifasi ◽  
R. Gobetto ◽  
U. J. Griesser ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Solid State ◽  
Dissolution Rate ◽  
Water Solubility ◽  
Tolfenamic Acid ◽  
Solubility In Water ◽  
Poor Solubility ◽  
Multiple Component

Tolfenamic acid (HTA) is a drug characterized by very poor solubility in water. By mechanochemical methods, new solid-state forms of HTA were obtained, showing better thermal stability than pure HTA and an improved dissolution rate.

scholarly journals Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Qingyun Zeng ◽  
Liquan Ou ◽  
Guowei Zhao ◽  
Ping Cai ◽  
Zhenggen Liao ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Molecular Weight ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Water Soluble ◽  
Carrier Material ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion (SD) is the effective approach to improve the dissolution rate and bioavailability of class II drugs with low water solubility and high tissue permeability in the Biopharmaceutics Classification System. This study investigated the effects of polyethylene glycol (PEG) molecular weight in carrier material PEG palmitate on the properties of andrographolide (AG)-SD. We prepared SDs containing the poorly water-soluble drug AG by the freeze-drying method. The SDs were manufactured from two different polymers, PEG4000 palmitate and PEG8000 palmitate. The physicochemical properties of the AG-SDs were characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, dissolution testing, and so on. We found that AG-PEG4000 palmitate-SD and AG-PEG8000 palmitate-SD were similar in the surface morphology, specific surface area, and pore volume. Compared with the AG-PEG4000 palmitate-SD, the intermolecular interaction between PEG8000 palmitate and AG was stronger, and the thermal stability of AG-PEG8000 palmitate-SD was better. In the meanwhile, the AG relative crystallinity was lower and the AG dissolution rate was faster in AG-PEG8000 palmitate-SD. The results demonstrate that the increasing PEG molecular weight in the PEG palmitate can improve the compatibility between the poorly water-soluble drug and carrier material, which is beneficial to improve the SD thermal stability and increases the dissolution rate of poorly water-soluble drug in the SD.

scholarly journals Preparation and Characterization of Hemicellulose Films from Sugarcane Bagasse

Materials ◽  
2020 ◽  
Vol 13 (4) ◽  
pp. 941 ◽  
Author(s):  
Roberta da Silva Braga ◽  
Matheus Poletto
Keyword(s):  
Thermal Stability ◽  
Sugarcane Bagasse ◽  
Tensile Strain ◽  
Water Solubility ◽  
Raw Material ◽  
Dense Structure ◽  
Solubility In Water ◽  
Hemicellulose Content ◽  
The Fourier Transform

Hemicellulose is one of the most common polysaccharides found in nature. Its use as a green and sustainable raw material for industries is desirable. In this work, an alkaline-alcoholic method was used to extract hemicelluloses from sugarcane bagasse. After extraction, films with 2%, 3% and 4% (w/v) hemicellulose were produced. The films’ morphology, thickness, water solubility, tensile properties and thermal stability were evaluated. The Fourier Transform Infrared Spectroscopy (FTIR) results reveal that the method used removes the hemicellulose from bagasse with a low concentration of lignin. The films presented a compact and dense structure with uniformity in thickness associated with higher solubility in water. The increase in hemicellulose content increased tensile strength, but reduced the tensile strain of the films. Thermogravimetric analysis indicated that the increase in hemicellulose content reduced the films’ thermal stability. Thus, these films may act as useful, biodegradable and environmentally friendly materials for engineering applications.

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

2018 ◽  
Vol 6 (02) ◽  
pp. 43-52 ◽  
Author(s):  
R. Bhaskar ◽  
Monika OLA ◽  
Ravindra M. Ghongade
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Solubility In Water ◽  
Characterization Methods ◽  
Poor Solubility ◽  
Novel Drugs ◽  
Poorly Soluble ◽  
Pharmaceutical Industries ◽  
Poorly Soluble Drug ◽  
Dispersion Technique

Nearly 40% of novel drugs comes in pharmaceutical industries are showing poor capability of solubilization in water. Therefore enhancing the solubilization of such drugs in water to enhance their bioavailability be the major challenge to formulation scientists. So the preparation of solid dispersion from the drug which shows poor solubility in water with carriers having good water solubility has decrease the occurrence of such problems and increase dissolution. Hence solid dispersion found to be attention-grabbing method for solubility enhancing of drugs which showing poor solubility in water. This review, shows an overview on the different solid dispersion types, rationale, their advantages, limitations, manufacturing processes as well as its characterization methods.

scholarly journals Enhancement of Solubility of Rilpivirine by Inclusion Complexation with Cyclodextrins

2018 ◽  
Vol 10 (01) ◽  
Author(s):  
Srivani Srivani ◽  
Y. Anand Kumar ◽  
N. G. Raghavendra Rao
Keyword(s):  
Solid State ◽  
Dissolution Rate ◽  
Binary Systems ◽  
Water Solubility ◽  
Inclusion Complexation ◽  
Solvent Evaporation ◽  
Physical Mixture ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Pure Drug

Rilpivirine having lowest water solubility indicates class II drugs of BCS. These classes of drugs could potentially exhibit dissolution rate limited absorption. The objective of the present study is to improve the solubility and dissolution of Rilpivirine through inclusion complexation with βCD and HPβCD. Solid binary systems of Rilpivirine with βCD and HPβCD were prepared by solvent evaporation and kneading methods at 1:1 and 1:2 M ratios. The prepared solid binary systems were studied in solution state by phase solubility, in vitro dissolution rate and solid state by FTIR and XRD. The dissolution parameters were studied by using dissolution software PCP Disso V3. The drug content was uniform in all the solid binary systems with low SD and CV values. The apparent stability constant indicates there is a 1:1 stochiometric complex with βCD and HPβCD. The formation of inclusion complexes with βCD and HPβCD in the solid state were confirmed by FTIR, XRD. The dissolution data clearly suggest drug release was method dependent and type of cyclodextrin. The dissolution of solid binary systems obeyed first-order kinetics and model fitted with Hixon crowel. A true inclusion complex of Rilpivirine was observed with βCD and HPβCD. Dissolution properties of solid binary systems were superior then rilpivirine alone and its corresponding physical mixtures. Overall dissolution rate was solvent evaporation > kneaded binary systems > physical mixture > pure drug. One-way ANOVA results suggest the DE30 and DE60 values were significantly higher (P less than 0.05) in solid binary systems when compared to physical mixture and pure drug.

scholarly journals Supercritical Assisted Atomization: Polyvinylpyrrolidone as Carrier for Drugs with Poor Solubility in Water

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Sara Liparoti ◽  
Renata Adami ◽  
Giuseppe Caputo ◽  
Ernesto Reverchon
Keyword(s):  
Dissolution Rate ◽  
Weight Ratio ◽  
Spherical Shape ◽  
Pharmaceutical Compounds ◽  
Water Medium ◽  
Solubility In Water ◽  
Poor Solubility ◽  
Composite Microspheres ◽  
Uniform Dispersion ◽  
Lower Drug

Supercritical assisted atomization (SAA) is an efficient technique to produce microparticles and composite microspheres formed by polymers and pharmaceutical compounds. In this work polyvinylpyrrolidone (PVP) was proposed as carrier for pharmaceutical compounds that show a poor solubility in water medium. Indeed, this polymer is hydrosoluble and can be generally used to enhance the dissolution rate of hydrophobic compounds when finely dispersed in it. However, it is difficult to obtain coprecipitates with a uniform dispersion of the active molecule using other micronization techniques. The experiments were performed using ethanol as solvent; SAA plant was operated at 40°C and 76 bar in the saturator and 70°C and 1.6 bar in the precipitator. Three different dexamethasone/polymer weight ratios were selected: 1/2, 1/4, and 1/8. Produced composite particles showed a regular, spherical shape and a mean diameter ranging from about 0.8 to 1 μm, depending on the polymer/drug weight ratio. Dissolution analysis demonstrated that microparticles containing a lower drug amount show a higher dissolution rate.

Improved Water-Solubility of Phytosterol by Hydroxypropyl-β-Cyclodextrin

2012 ◽  
Vol 554-556 ◽  
pp. 922-925
Author(s):  
Xiao Yan Zhang ◽  
Yong Peng ◽  
Guo Qing He
Keyword(s):  
Complex Formation ◽  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Phase Solubility ◽  
Solubility In Water ◽  
Solubility Study ◽  
Phase Solubility Study ◽  
Low Solubility ◽  
Initial Dissolution Rate

Phytosterol has been shown to lower the serum cholesterol concentrations, but its low solubility in water restricts its application. In this study, hydroxypropyl-β-cyclodextrin was used to improve the water-solubility of phytosterol. Phase solubility study pointed out the formation of 1:1 inclusion complexes between phytosterol and hydroxypropyl-β-cyclodextrin. The initial dissolution rate was remarkedly improved in the first two minutes. The suitable solvent and temperature for complex formation was n-butanol and 40°C.

New Technological Approach for Glycyrrethic Acid Oral and Topical Administration

2020 ◽  
Vol 26 (6) ◽  
pp. 664-674 ◽  
Author(s):  
Cinzia Pagano ◽  
Luana Perioli ◽  
Paola Calarco ◽  
Alessandro Di Michele ◽  
Maria C. Tiralti ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Water Solubility ◽  
Local Therapy ◽  
Topical Administration ◽  
Application Site ◽  
Vaginal Mucosa ◽  
Anionic Clays ◽  
Dissolution Rate Enhancement ◽  
Technological Approach ◽  
Bioactive Component

Background: 18β- glycyrrhetinic acid (Gly) is the major bioactive component of licorice roots and rhizomes of the Glycyrrhiza glabra species. It shows many activities such as antiviral, anti-inflammatory, antioxidant, antimicrobial, and antifungal, however, its use in the health field is very limited due to the low water solubility. Methods: This paper deals with the development of a new technological approach for Gly dissolution rate enhancement. It consists of Gly intercalation (guest) in the interlamellar spaces between the inorganic spaces (host) of the anionic clays “hydrotalcites” (HTlc) to obtain hybrids MgAl-HTlc-Gly and ZnAl-HTlc-Gly. Gly can find applications in both systemic and local therapies, thus advantages of the use of the hybrids in these two fields were investigated. Results: Gly dissolution rate from hybrids in the intestinal environment, site in which it is preferentially absorbed, resulted enhanced (ZnAl-HTlc-Gly > MgAl-HTlc-Gly) compared to the crystalline form, thereby, making them suitable for oral administration as dry powder in hard capsules. : For a local therapy, bioadhesive, vaginal emulgels loaded with the hybrids were developed. These showed suitable mucoadhesive property to the vaginal mucosa, necessary to prolong the residence time in the application site. The emulgel containing ZnAl-HTlc-Gly showed a faster and higher release profile than that containing MgAl- HTlc-Gly. Conclusions: The obtained results suggest that Gly intercalation into HTlc, especially in ZnAl-HTlc, allows to enhance Gly dissolution when the hybrids are formulated both as oral or topical products.

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