DISSOLUTION ENHANECEMENT OF AN ANTIHYPERTENSIVE AGENT BY SOLID DISPERSION

2013 ◽  
pp. 21-24
Author(s):  
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
X Ray Diffraction ◽  
Peg 6000 ◽  
X Ray ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: To evaluate dissolution enhancement of IS, a poorly water-soluble drug, by PEG 6000-based solid dispersion and investigate mechanism of dissolution enhancement from the solid dispersion. Methods: Solid dispersion was prepared by melting method. Dissolution test was performed at pH 6.8. Powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR) were used to investigate the drug crystallinity as well as the interaction between drug and polymer. Results: Dissolution rate of IS from the solid dispersion was significantly increased at pH 6.8 as compared to the pure drug. Drug crystallinity was reduced. FTIR showed the interaction between polymer and IS in the solid dispersion. Conclusions: PEG 6000 was successfully used to increase the dissolution of IS. Moreover, mechanism of the dissolution enhancement was fully explained in the study. Key words: poorly water-soluble drug, dissolution, solid dispersion.

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.

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.

Physical Stabilizing Effect of Biopolymers on Solid Dispersions Containing Indomethacin and Polyethylene Glycol

2012 ◽  
Vol 506 ◽  
pp. 307-310 ◽  
Author(s):  
Benchawan Chamsai ◽  
Pornsak Sriamornsak
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drug ◽  
Stabilizing Effect ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersions of poorly water-soluble drug, indomethacin (IMC), and carriers at a ratio of 1:9 were prepared by melting method. The carriers used in this study were polyethylene glycol 4000 (PEG4000), hydroxypropyl methylcellulose (HPMC) and pectin. The solid dispersions obtained were characterized by powder x-ray diffractometry (PXRD) and dissolution studies. PXRD patterns showed that all solid dispersions led to amorphous products while their physical mixture still showed the crystalline state of drug. Crystalline drug was clearly detectable in solid dispersion products containing only IMC and PEG4000 after storage for 2 months. The formulations with biopolymer (i.e., HPMC, pectin or their combination) showed no drug crystal after storage. More than 80% of IMC dissolved within 5 minutes for all formulations after preparation while less than 40% of IMC dissolved, within 5 minutes, from the formulations containing IMC, PEG4000 and HPMC after storage for 2 months. The slower drug dissolution may be due to the gel-forming properties of HPMC as well as the agglomeration of the products after storage. The results suggested that either HPMC or pectin in solid dispersions can help to prevent the crystallization of amorphous IMC in solid dispersion, probably by a polymer anti-plasticizing effect. Pectin showed superior stabilizing effect with no retardation effect on drug dissolution.

scholarly journals SOLUBILITY AND DISSOLUTION ENHANCEMENT OF PIOGLITAZONE USING SOLID DISPERSION TECHNIQUE

2017 ◽  
pp. 186-193
Author(s):  
Bhushan A. Bhairav ◽  
Lalit R. Jagtap ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Chemical Interaction ◽  
Physicochemical Characteristics ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Hydrophobic Drug ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Dispersion Technique ◽  
Poorly Water Soluble Drug

Objective: To design the study to improve the solubility and hence enhance the dissolution of hydrophobic drug Pioglitazone in order to increase its bioavailability.Methods: Solid dispersion of Pioglitazone using carriers Poloxomer 188 and HPβCD was formulated in different ratios by microwave induced fusion method. In particular, the Microwave technology has been considered in order to prepare an enhanced release dosage form for poorly water soluble drug Pioglitazone. Statistical Analysis: Their physicochemical characteristics and solubility were compared to the corresponding dispersions and marketed drug. Drug and polymer were further characterized by FTIR.Results: The results of FTIR revealed that no chemical interaction between the drug and the polymer exist.Conclusion: All the formulations showed a marked increase in drug release with the increase in the concentration of Poloxomer 188 and HPβCD. 

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 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.

In Vitro-In Vivo Correlation for Solid Dispersion of a Poorly Water-Soluble Drug Efonidipine Hydrochloride

2020 ◽  
Vol 21 (5) ◽  
Author(s):  
Xu Cheng ◽  
Jianlong Gao ◽  
Jiaqi Li ◽  
Gang Cheng ◽  
Meijuan Zou ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Bioavailability of a Poorly Water-Soluble Drug from Tablet and Solid Dispersion in Humans

1991 ◽  
Vol 80 (7) ◽  
pp. 712-714 ◽  
Author(s):  
Pai-Chang Sheen ◽  
Soo-Il Kim ◽  
John J. Petillo ◽  
Abu T.M. Serajuddin
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug
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