Investigation of Solid Dispersion of Atorvastatin Calcium in Polyethylene Glycol 6000 and Polyvinylpyrrolidone

Hu, Liandong; Gu, Deliang; Hu, Qiaofeng; Shi, Yanjing; Gao, Na

doi:10.4314/tjpr.v13i6.2

Cited by 16 publications

(6 citation statements)

References 20 publications

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“…However, it has poor oral bioavailability (12%), which is a result of low aqueous solubility and high hepatic degradation by first-pass metabolism. 8 In addition, its bioavailability is highly variable due to instability in acidic media. 9 Many approaches have been developed to improve the solubility of ATC, including: salt formation, solid dispersion technique using mannitol, PEG-4000, PEG-6000, and PVP-K30, 10 nanosuspension, 11 complexation with cyclodextrins, 12 self-emulsifying drug delivery system, 13,14 conjugation with chitosan, 15 and nanosuspension incorporated transdermal patch.…”

Section: Introductionmentioning

confidence: 99%

Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization

2019

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Purpose: To enhance the dissolution rate of the poorly soluble drug atorvastatin calcium (ATC) by cocrystallization with selected coformers. Enhancement of the dissolution rate and solubility of the drug, which is classified as Class II of the Biopharmaceutical Classification System (BCS), is expected to enhance the bioavailability.Methods: Two methods were used for preparing the cocrystals, solvent drop grinding (SDG) and solvent evaporation (SE) method using 1:1, 1:3, and 1:10 drug-coformer molar ratios. Glucosamine hydrochloride (GluN) and nicotinamide (NIC) were investigated as coformers. The cocrystals, their physical mixtures, and the raw ATC were characterized by fourier transform infrared (FTIR spectroscopy), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), mass spectroscopy (MS), scanning electron microscopy (SEM), solubility, and dissolution rate studies. Results: SDG and SE were effective in improving the dissolution rate of ATC with both coformers. Drug: coformer ratio 1:3 was optimum. The solubility values for ATC, GluN-, and NIC-cocrystals were 26, to 35 and 50 µg/mL, respectively. The dissolution rate of ATC from cocrystals was > 90% after 5 minutes, compared to 41% untreated ATC. Conclusion: Cocrystallization significantly improved the solubility and dissolution, in comparison to the untreated ATC.

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Section: Introductionmentioning

confidence: 99%

Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization

2019

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“…Various techniques have been used for enhancing drug's dissolution rate. One of these methods was solid dispersion (SD) method [4][5][6][7][8]. It is an effective method used in improving the dissolution of drugs.…”

Section: Fig 1: Chemical Structure Of Meloxicam [3]mentioning

confidence: 99%

“…SD may improve the dissolution of various drugs by improving drug wettability, reducing drug particle size and converting the drug into an amorphous state. Many methods were used in preparing SD such as; Fusion method, Solvent method, Hot melt extrusion, Lyophilization, Spray drying, Kneading and supercritical fluid technique [5,6,9].…”

Section: Fig 1: Chemical Structure Of Meloxicam [3]mentioning

confidence: 99%

Effect of Selected Polymers on Dissolution and Stabilization of Amorphous Form of Meloxicam

Obaidat

Al-Taani

Al-quraan

2017

Int J Pharm Pharm Sci

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Objective: Meloxicam is classified as class II corresponding to its high permeability and low solubility (12μg/ml). This study aims to compare the effect of selected polymers on stabilization of amorphous form, and dissolution of meloxicam by preparation of different solid dispersions using selected polymers (chitosan oligomers, polyvinylpyrrolidone K30, and polyethylene glycols).Methods: These solid dispersions were prepared using two different methods; solvent evaporation method for the two molecular weights chitosan carriers (16 and 11KDa) and polyvinylpyrrolidone-K30 and melting method for the two different molecular weights polyethylene glycol (4000 and 6000). The physicochemical properties of solid dispersions were analyzed using differential scanning calorimetry, Fourier transform infra-red analysis, Powder X-ray diffraction, and scanning electron microscopy. Selected dispersions were then compared to two selected marketed drugs (Mobic® and Moven®).Results: Best dissolution rates were obtained for both polyvinylpyrrolidone-K30 and polyethylene glycol 6000, followed by chitosan 16 kDa, chitosan 11 kDa, and polyethylene glycol 4000. Increasing polymeric ratio increased dissolution rate except for chitosan. Precipitation of the drug as amorphous form occurred in chitosan and polyvinylpyrrolidone-K30 dispersions, while no change in crystallinity obtained for polyethylene glycol dispersions. Failure of polyvinylpyrrolidone-K30 in the maintenance of stability during storage time was observed while re-crystallization occurred in chitosan-based dispersions, which ends with preferences to polyethylene glycol dispersions. After comparing the release of selected dispersions with the two selected polymers; all dispersions got a higher release than that of the two marketed drugs release. Conclusion:The dissolution profile of meloxicam has been increased successfully in a reproducible manner.

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“…Different techniques have been implemented to increase the aqueous solubility of atorvastatin such as nano-suspension, co-crystals, Microwave induced solubility enhancement, spray-drying and supercritical antisolvent (SAS) process, self-emulsifying drug delivery systems, cyclodextrin complexation and solid dispersion approaches (Arunkumar et al, 2009;Kim et al, 2008;Maurya et al, 2010;Naqvi et al, 2020;Palem et al, 2009;Rodde et al, 2014). The solubility and dissolution rate of atorvastatin have been improved by solid dispersion approach through different hydrophilic polymers such as PEG 6000, polyvinylpyrrolidone-K30, Soluplus ® , PVP VA64, HPMC, Poloxamer 188 (Bobe et al, 2011;Dong et al, 2018;Ha et al, 2014;Hu et al, 2014;Jahan et al, 2013;Shamsuddin et al, 2016). The dissolution profile of atorvastatin was studied and reported to our previous publications (Sarkar et al, 2012;Sarkar et al, 2014) using physical mixing and fusion techniques.…”

Section: Introductionmentioning

confidence: 99%

Enhancement of dissolution profile of poorly aqueous soluble atorvastatin calcium by binary and ternary solid dispersion techniques

Sarkar¹,

Hossin²,

Hossain³

et al. 2021

Bangladesh J. Sci. Ind. Res.

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Atorvastatin calcium (ATV) is an HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase inhibitor commonly known as a cholesterol-lowering agent. As a poorly water-soluble drug its absolute bioavailability is very low. To increase the water solubility as well as oral bioavailability, different hydrophilic carriers were used in different ratios (1:0.5, 1:1 and 1:2) to prepare reproducible binary and ternary solid dispersion formulations of ATV by simple physical mixing (PM) and fusion or melting technique. In vitro dissolution studies results revealed that in all cases, the cumulative percent drug release from ATV ternary SD formulations were greater than binary formulations, some marketed products and pure ATV powder. The order of the carriers in enhancing the drug release was found as kollidon 90F > pregelatinized starch > lutrol> kollidon 12F (99.1%, 98.8%, 96% and 95% respectively) for ternary SD formulations whereas pure ATV powder and marketed products showed cumulative percentage release 70.8%, 68.9% (B1) and 73.1% (B2), respectively. The best-out performed ternary SD formulation ATV:Kollidon 90 F (1:2) were further characterized using FT-IR and SEM. SEM analyses indicated conversion of crystal drug to amorphous form and FT-IR data suggested that little or no interaction between the drug and polymer. Bangladesh J. Sci. Ind. Res.56(3), 165-176, 2021

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Investigation of Solid Dispersion of Atorvastatin Calcium in Polyethylene Glycol 6000 and Polyvinylpyrrolidone

Cited by 16 publications

References 20 publications

Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization

Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization

Effect of Selected Polymers on Dissolution and Stabilization of Amorphous Form of Meloxicam

Enhancement of dissolution profile of poorly aqueous soluble atorvastatin calcium by binary and ternary solid dispersion techniques

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