Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers

2007 ◽  
Vol 65 (1) ◽  
pp. 26-38 ◽  
Author(s):  
Naveen Ahuja ◽  
Om Prakash Katare ◽  
Bhupinder Singh
Keyword(s):  
Mathematical Modeling ◽  
Drug Release ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

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.

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.

Melt extrusion process for adjusting drug release of poorly water soluble drug felodipine using different polymer matrices

2018 ◽  
Vol 114 ◽  
pp. 332-345 ◽  
Author(s):  
Eirini Palazi ◽  
Evangelos Karavas ◽  
Panagiotis Barmpalexis ◽  
Margaritis Kostoglou ◽  
Stavroula Nanaki ◽  
...  
Keyword(s):  
Drug Release ◽  
Extrusion Process ◽  
Water Soluble ◽  
Polymer Matrices ◽  
Melt Extrusion ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

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 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. 

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