Improvement of the diuretic effect of triamterene via solid dispersion technique with PEG 4000

1994 ◽  
Vol 19 (4) ◽  
pp. 295-302 ◽  
Author(s):  
M. J. Arias ◽  
J. M. Gines ◽  
J. R. Moyano ◽  
M. J. Perez-Barrales ◽  
M. T. Vela ◽  
...  
Author(s):  
Mustapha M. AlKhalidi ◽  
Fatima J. Jawad

Etoricoxib (EXB) is a highly selective cox-2 inhibitor which belongs to the non-steroidal anti-inflammatory drug (NSAID). EXB is a class II drug according to the biopharmaceutical classification system (BCS), which possess a very low aqueous solubility in water.  In the present study, many trials were made to improve the aqueous solubility and dissolution rate of EXB by solid dispersion technique. Eighteenth EXB formulas were formulated as a solid dispersion using a variety of hydrophilic polymers (as carriers)   including poloxamer 407 (PXM 407), poloxamer 188 (PXM 188) and polyethylene glycol 4000 (PEG 4000) at different drug: polymer ratios (1:1, 1:3 and 1:5). These formulas were prepared by two methods; solvent evaporation and fusion method. The prepared formulas were evaluated for practical yield percent (PY %), drug content, saturated solubility and release rate, Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD). It was found that the solubility was affected by the polymer type and the method of preparation. The polymers (as carriers) used to prepare EXB- solid dispersion showed improvement in the solubility in the following descending order; PXM 407>PXM 188> PEG 4000. The optimum formula (SD15) composed of the drug: PXM 407 at a ratio of 1:5 was prepared by solvent evaporation showed 7.76 folds (676.40%) solubility improvement as compared to pure EXB. The optimum formula showed a release rate of 99.8% through the first 15 min. The advance characterization of the selected formula indicated the possible transformation of the drug to the amorphous state. Keywords: EXB, Solid dispersion, PXM 407, PXM 188, PEG 4000.


2013 ◽  
Vol 43 (1) ◽  
pp. 45-53 ◽  
Author(s):  
Pranav V. Patel ◽  
Shital S. Panchal ◽  
Tejal A. Mehta

2015 ◽  
Vol 5 (2) ◽  
pp. 1463-1472 ◽  
Author(s):  
Shete A.S . ◽  
Yadav V.B . ◽  
Sakhare S.S . ◽  
Patil S.B . ◽  
Sajane S.J . ◽  
...  

2018 ◽  
Vol 8 (5) ◽  
pp. 19-22
Author(s):  
Pralhad K. Kanke ◽  
Pankaj Sawant ◽  
Ajit Jadhav ◽  
Md. Rageeb Md. Usman

A number of sustained release formulations are available in the market which successfully sustained the drug release over a prolonged period of time by different mechanisms. The new approach for sustaining the drug release is disintegration control matrix tablet which sustained the drug release up to 24hrs by controlling the disintegration rate of tablet. Disintegration control matrix tablet (DCMT) mainly forms the granules containing drug and disintegrating agent such as low substituted hydroxyl propyl cellulose by various methods such as solid dispersion technique. The sustained release of drug is maintained by increasing the wax coating or decreasing the amount of disintegrants. The release of drug from tablet is uniform throughout till all the drug releases from tablet as it involves drug release by diffusion, dissolution and surface erosion mechanism. DCMT increases the solubility of drug and improves the bioavailability without disturbing gastrointestinal transit. BCS Class II, III, IV drugs are the best candidate for DCMT formulations. Keywords: Disintegration control matrix tablet (DCMT), Wax, Disintegrating agent, Solid dispersion.


2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1772-1778
Author(s):  
Jyoti Maithani ◽  
Ranjit Singh ◽  
Sanjay Singh ◽  
Kapil Kalra

Improvement in the solubility of a hydrophobic drug has a significant role in formulation development. The target of this study was the use of solid dispersion and inclusion complex method to enhance and to compare the watery solubility and dissolution qualities of Rifabutin. Various strategies in various proportions have been used in the preparation of the consideration complex with ß-cyclodextrin (ß-CD) and Hydroxypropyl-ß-cyclodextrin (HPß-CD) and found that the better-improved solubility has been seen in kneading technique (AK1) in comparison to the physical mixture method and solvent evaporation method. Various techniques were applied in the preparation of the solid dispersion of Mannitol and polyethene glycol (PEG) 4000. They observed that solvent evaporation (CS4) had shown the better improvement of solubility when compared with the physical mixture method and kneading method. As the two methodologies were analysed, it was observed that the inclusion complex technique was far better as it caused a noteworthy enhancement in dissolution profile (99.23±0.25). The drug content was calculated (99.15±0.14) and % inclusion yield was calculated (99.5 %), which was found to be maximum with the kneading technique (AK1). The characterization FTIR and SEM of the complexes shows that the drug had an amorphous structure. The amorphous structure of a drug has higher dissolution potential than the crystalline structure of the drug. The IR Spectroscopy and Scanning electron microscopy (SEM) were done to check their impact on dissolution behaviour and any if there was any physicochemical interaction between the carrier and the drug.


Author(s):  
Sanjoy Kumar Das

Improving oral bioavailability of drugs those given as solid dosage forms remains a challenge for the formulation scientists due to solubility problems. The dissolution rate could be the rate-limiting process in the absorption of a drug from a solid dosage form of relatively insoluble drugs. Therefore increase in dissolution of poorly soluble drugs by solid dispersion technique presents a challenge to the formulation scientists. Solid dispersion techniques have attracted considerable interest of improving the dissolution rate of highly lipophilic drugs thereby improving their bioavailability by reducing drug particle size, improving wettability and forming amorphous particles. The term solid dispersion refers to a group of solid products consisting of at least two different components, generally a hydrophilic inert carrier or matrix and a hydrophobic drug. This article reviews historical background of solid dispersion technology, limitations, classification, and various preparation techniques with its advantages and disadvantages. This review also discusses the recent advances in the field of solid dispersion technology. Based on the existing results and authors’ reflection, this review give rise to reasoning and suggested choices of carrier or matrix and solid dispersion procedure.


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