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 Study on Mixed Solvency Concept in Formulation Development of Aqueous Injection of Poorly Water Soluble Drug

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Shailendra Singh Solanki ◽  
Love Kumar Soni ◽  
Rajesh Kumar Maheshwari
Keyword(s):  
Propylene Glycol ◽  
Sodium Benzoate ◽  
Sodium Citrate ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Pharmaceutical Industries ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

In the present investigation, mixed-solvency approach has been applied for the enhancement of aqueous solubility of a poorly water- soluble drug, zaltoprofen (selected as a model drug), by making blends (keeping total concentrations 40% w/v, constant) of selected water-soluble substances from among the hydrotropes (urea, sodium benzoate, sodium citrate, nicotinamide); water-soluble solids (PEG-4000, PEG-6000); and co-solvents (propylene glycol, glycerine, PEG-200, PEG-400, PEG-600). Aqueous solubility of drug in case of selected blends (12 blends) ranged from 9.091 ± 0.011 mg/ml–43.055 ± 0.14 mg/ml (as compared to the solubility in distilled water 0.072 ± 0.012 mg/ml). The enhancement in the solubility of drug in a mixed solvent containing 10% sodium citrate, 5% sodium benzoate and 25 % S cosolvent (25% S cosolvent contains PEG200, PEG 400, PEG600, Glycerine and Propylene glycol) was more than 600 fold. This proved a synergistic enhancement in solubility of a poorly water-soluble drug due to mixed cosolvent effect. Each solubilized product was characterized by ultraviolet and infrared techniques. Various properties of solution such as pH, viscosity, specific gravity and surface tension were studied. The developed formulation was studied for physical and chemical stability. This mixed solvency shall prove definitely a boon for pharmaceutical industries for the development of dosage form of poorly water soluble drugs.

scholarly journals COMPARISON AND CHARACTERIZATION OF INCLUSION COMPLEXES AND SOLID DISPERSIONS IN ENHANCEMENT OF DISSOLUTION RATE OF POORLY WATER SOLUBLE DRUG

2018 ◽  
Vol 10 (5) ◽  
pp. 173
Author(s):  
Radha Rani Earle ◽  
Rambabu Jammu ◽  
Lakshmi Usha ◽  
Ratna Kanth Lingam
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Peg 6000 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Objective: The purpose of the present study was to enhance solubility and dissolution characteristics of indomethacin by preparing inclusion complexes with hydroxypropyl β-cyclodextrin (HP β-CD) and solid dispersions with PEG 6000 to enhance its in vitro drug release and to further formulate it as a tabletMethods: Solid dispersions (SDs) and inclusion complexes (ICs) of Indomethacin with PEG 6000 and HP β-CD respectively were prepared to enhance the dissolution rate of this poorly water-soluble drug belonging to BCS class II. A comparison was made between two systems: solid dispersions with PEG 6000 obtained using melting and solvent evaporation technique, inclusion complexes with HP β-CD prepared by kneading technique. SDs were prepared in 1:1, 1:2, 1:3 and ICs in 1:0.25, 1:0.5, 1:1 w/w ratios of drug: polymer. Both the systems were characterized by FTIR, SEM, DSC, X-RD.Results: The dissolution of indomethacin increased with the increase in the concentration of the polymers. F4 and F9 formulations showed complete drug release in less than 30 min. Dissolution studies indicated that cyclodextrin complexes showed a better enhancement of dissolution rate when compared to solid dispersions. CDs were found to be more effective than PEGs at lower concentrations. These formulations were further compressed as tablets.Conclusion: The FTIR and DSC studies showed that no interactions existed between the drug and the polymer.

scholarly journals Solid Dispersion (Kneading) Technique: A Platform for Enhancement Dissolution Rate of Valsartan Poorly Water Soluble Drug

2020 ◽  
Vol 11 (01) ◽  
pp. 20-24
Author(s):  
Vinod T. Wagh ◽  
Ritu M. Gilhotra ◽  
Rajendra D. Wagh
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
X Ray Diffraction ◽  
Water Soluble Drug ◽  
Kneading Method ◽  
Differential Scanning Colorimetry ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The objective of this study was to the enhancement of dissolution rate of Valsartan. Using a solid dispersion (kneading) method with Kollidon and Povidone K30 as a carrier. Eight different drugs: Carrier ratios were prepared. Using factorial design taking 3 factors i.e., the concentration of Valsartan (x1), Kollidon (x2), and Povidone K30(x3). The enhancement of dissolution depends on the amount of carrier and an increase in the concentration of carrier. Enhancement of dissolution rate depends on reduce particle size of drug place on the surface of carrier and increased wettability of drug particle by carrier. Solid Dispersions prepared with Kollidon as a carrier in ratio 1:4 shows the enhancing dissolution in 30 mins to drug and Physical Mixture. Formulation evaluated by fourier-transform infrared spectroscopy, differential scanning colorimetry, X-ray diffraction, Scanning Electron Microscopy.

scholarly journals Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics

2021 ◽  
Vol 71 (5) ◽  
pp. 393-409
Author(s):  
Earle Radha-Rani ◽  
Gadela Venkata-Radha
Keyword(s):  
Benzoic Acid ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
X Ray Diffraction ◽  
X Ray ◽  
Water Soluble Drug ◽  
Novel Approach ◽  
Enhanced Solubility ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

In the present study, co-crystals (CCs) of Paliperidone (PPD) with coformers like benzoic acid (BA) and P-amino benzoic acid (PABA) were synthesized and characterized to improve the physicochemical properties and dissolution rate. CCs were prepared by the solvent evaporation (SE) technique and were compared with the products formed by neat grinding (NG) and liquid assisted grinding (LAG) in their enhancement of solubility. The formation of CCs was confirmed by the IR spectroscopy, powder X-ray diffraction and thermal analysis methods. The saturation solubility studies indicate that the aqueous solubility of PPD-BA and PPD-PABA CCs was significantly improved to 1.343±0.162mg/ml and 1.964±0.452mg/ml, respectively, in comparison with the PPD solubility of 0.473mg/ml. This increase in solubility is 2.83-and 3.09-fold, respectively. PPD exhibited a poor dissolution of 37.8% in 60min, while the dissolution of the CCs improved tremendously to 96.07% and 89.65% in 60min. CCs of PPD with BA and PABA present a novel approach to overcome the solubility challenges of poorly water-soluble drug PPD.

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.

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