Solid Carriers for Improved Solubility of Glipizide in Osmotically Controlled Oral Drug Delivery System

Mehramizi, Ali; Alijani, Behnaz; Pourfarzib, Mojgan; Dorkoosh, Farid Abedin; Tehrani, Morteza Rafiee

doi:10.1080/03639040601128753

Cited by 14 publications

(12 citation statements)

References 23 publications

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“…[9] As per BP, It GZ is practically insoluble in water; because of its poor aqueous solubility (classified as BCS class II drug), conventional GZ dosage form show absorption problem, and its dissolutions is are considered to be a rate determining step in its absorption from gastrointestinal tract. [10,11] During high blood glucose level conditions, an antidiabetic drug should show quick and high oral bioavailability, which can be achieved by high aqueous solubility. Many hydrophilic excipients like PEG4000, PEG 6000, urea, Mannitol, PVP and poloxamers can be used to enhance the dissolution of drugs.…”

Section: Introductionmentioning

confidence: 99%

Enhancement of solubility and dissolution of glipizide by solid dispersion (kneading) technique

Choudhary¹,

Kumar²,

Gupta³

2009

Asian J Pharm

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G lipizide is a poorly water-soluble (BCS class II) antidiabetic drug. Due to the poor water solubility of this drug, its bioavailability is dissolution rate-limited. The purpose of this study was is to increase the solubility of Glipizide (GZ) in aqueous media by solid dispersion (SDs) technique with Poloxamer (PXM) 188 and Poloxamer (PXM) 407 by using the kneading method. The GZ-PXM solid dispersion system was characterized by dDifferential scanning calorimetry (DSC), X-ray powder diffraction (XRD) analysis, Fourier transform-infrared spectroscopy (FT-IR) and Scanning electron microscopy (SEM), and in vitro dissolution studies. No chemical interaction was found between GZ and PXM 188 or PXM 407. The results from DSC, XRD and SEM studies show that PXM 188 or PXM 407 inhibits the crystallization of GZ. The SDs prepared in this study were found to have better dissolution rates in comparisoncompared to intact GZ and physical mixture of PXM 188 or PXM 407 and GZ. It was found that the optimum weight ratio for drug: Carrier is 1:5 for PXM 188 and 1:6 for PXM 407.

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Section: Introductionmentioning

confidence: 99%

Enhancement of solubility and dissolution of glipizide by solid dispersion (kneading) technique

Choudhary¹,

Kumar²,

Gupta³

2009

Asian J Pharm

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“…2, insert). The results are typical for a weak base titrated by a weak acid, although xymedon is a weak base and meglumine is medium-strength base [24,25].…”

Section: Acid-base Interactions Of Betulin-3 28-diphosphate With Aqumentioning

confidence: 78%

“…Meglumine ((2R,3R,4R,5S)-6-(methylamino)hexan-1,2,3,4,5-pentol, Megl) traditionally used both for acidosis correction, pH-regulation and making plasma isoosmotic and to improve permeability of poorly soluble lipophilic pharmaceutical substances [24,25] was chosen as one of these amino alcohols ( fig. 1b).…”

Section: Fig 1: Formulas Of Salt Complexes Componentsmentioning

confidence: 99%

The Improvement of Betulin-3, 28-Diphosphate Water-Solubility by Complexation With Amines–meglumine and Xymedon

Мельникова

Malygina

Panteleev

et al. 2019

Int J Pharm Pharm Sci

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Objective: To study betulin-3,28-diphosphate (BDP) water solubility improved by forming salt complexes with hydrophilic amino alcohols: meglumine as acidosis corrector and xymedon as the water-soluble antioxidant. Methods: We used 13C-, 31P-NMR, UV-spectroscopy and potentiometric titration to study the BDP-amine salt complexes formation and their solubility using HPLC-analysis. Results: The participation of xymedon in the proton transfer reaction with BDP in aqueous solutions was confirmed by the bathochromic shift of the carbonyl band from 299.1 nm to 304.2 nm, and by a hyperchromic effect (molar extinction ε from 8508 to 10 441 l·mol-1·cm-1) in UV-spectra. BDP complexation with meglumine was estimated by UV-spectral molar ratio method at 256 nm. Molar ratio of BDP-amine complexes (1:4) was proved by 31P-NMR. The chemical shift of phosphorus at C-3 atom of BDP (δ =-0.58 ppm) changed to+3.39 ppm, and at C-28 atom (δ =+0.28 ppm)–to+4.60 ppm. BDP solubility increased 100-600 fold according to HPLC-analysis. Conclusion: BDP interaction with amine in an aqueous solution was shown to proceed via a proton transfer due to relatively weak forces such as London forces, hydrogen bonding, electrostatic and hydrophobic interactions. In general, the formation of BDP salt complexes with amines in solution determines BDP water solubility. Water-soluble BDP enables to develop hydrophilic dosage forms.

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“…Several approaches were investigated to enhance the rate of dissolution of lovastatin and/or improve bioavailability. These include: preparation of amorphous lovastatin using freeze drying; inclusion complexes with β‐cyclodextrin (β‐CD) in the absence and the presence of a dissolved polymer or its monomeric compound; solid dispersions using different polymers and superdisintegrants; a sustained release gastroretentive drug delivery system based on floating microspheres using various polymers and their blends; a bilayer regioselective floating tablets of atenolol and lovastatin to give immediate release of lovastatin and sustained release of atenolol; A microemulsion formulation; Nanocrystals prepared using simple precipitation method without using stabilizers or surfactants; Nanostructured lipid carriers (NLCs); and solid lipid nanoparticles (SLNs) prepared by hot homogenization followed by ultrasonication …”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of lovastatin polymeric microparticles by coacervation‐phase separation method for dissolution enhancement

Al-Nimry

Khanfar

2015

J of Applied Polymer Sci

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Dissolution rate of lovastatin is slow, only 30% of the oral dose is absorbed, and it undergoes extensive first-pass extraction resulting in low and variable bioavailability. The objective of this research was to enhance the dissolution rate through preparing polymeric microparticles. Coacervation-phase separation method through the addition of a non-solvent was used to prepare polymeric microparticles. The method was optimized through studying effects of the type of solvent, the type of polymer, drug : polymer ratio and concentration of surfactant on particle size, particle size distribution, and in-vitro drug release. Optimized polymeric microparticles and unprocessed drug were characterized using different techniques (SEM, FTIR, DSC, and PXRD) and their flow properties were evaluated. The optimum microparticles were prepared using ethanol as a solvent, Eudragit V R L 100 as a polymer in a drug:polymer ratio of 1:2 and SDS in a concentration of 0.25%. Characterization techniques indicated a change from the crystalline form to an amorphous form that was molecularly dispersed into the polymer. Flow properties of these microparticles were improved as compared to unprocessed drug. Drug release was enhanced 4-to 5-folds probably due to precipitation of the drug in an amorphous form; wetting enhancement; size reduction and stabilization by polymers and surfactants. In conclusion the selection of proper process parameters enhanced drug release 5 folds. The use of DMSO as a solvent and the preparation of physical mixtures in this research provided a means for controlled or prolonged release.

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Solid Carriers for Improved Solubility of Glipizide in Osmotically Controlled Oral Drug Delivery System

Cited by 14 publications

References 23 publications

Enhancement of solubility and dissolution of glipizide by solid dispersion (kneading) technique

Enhancement of solubility and dissolution of glipizide by solid dispersion (kneading) technique

The Improvement of Betulin-3, 28-Diphosphate Water-Solubility by Complexation With Amines–meglumine and Xymedon

Preparation and characterization of lovastatin polymeric microparticles by coacervation‐phase separation method for dissolution enhancement

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