Preparation, Characterization, and Dissolution Behavior of a Solid Dispersion of Simvastatin with Polyethylene Glycol 4000 and Polyvinylpyrrolidone K30

Patel, Rakesh P.; Patel, M. P.

doi:10.1080/01932690701706946

Cited by 37 publications

(38 citation statements)

References 37 publications

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“…When formulated as tablets, the solid dispersions prepared with PEG4000 and PVP K30 showed significant improvement in the release profile of SIM as compared to tablets containing SIM without PEG 4000 or PVP K30. [26] …”

Section: Solid Dispersionmentioning

confidence: 99%

“…These crystalline structures may have retarded the dissolution rate of the coatings, resulting in a delayed release of SIM. [49] [26] Lipid nanoparticles Improvements in bioavailability Lipid nanoparticles may be a promising sustained-release and drug-targeting system for statin drug therapy [27][28][29][30] Periodontal gels Effects of simvastatin gels on murine calvarial bone For the treatment of chronic periodontitis [31][32][33] Biodegradable polymeric nanoparticle technology…”

Section: Cyclodextrin Inclusion Systemmentioning

confidence: 99%

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Statins therapy: a review on conventional and novel formulation approaches

Tiwari

Pathak

2011

Journal of Pharmacy and Pharmacology

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Background and objective High levels of cholesterol lead to atherosclerosis, a factor predisposing to the development of coronary artery disease. Statin drugs, i.e. HMG-CoA reductase inhibitors, have been known since the end of the last century for their benefits against cardio-and cerebrovascular diseases and are widely used clinically. This review aims at compiling the research inputs being made for developing therapeutically efficacious dosage forms that have the potential to surmount the limitations of conventional dosage forms of statins. Key findings Statin drugs can reduce the endogenous synthesis of cholesterol and prevent the onset and development of atherosclerosis, and are therefore used as an effective treatment against primary hypercholesterolemia. At present, statin drugs are most often administered orally, on a daily basis. After administration, the bioavailability and the general circulation of statin drugs is fairly low due to the first-pass metabolism in the liver and clearance by the digestive system. Extensive pharmaceutical research in understanding the causes of low oral bioavailability has led to the development of novel technologies to address these challenges. Summary These technologies vary from conventional dosage forms to nanoparticulate drug-delivery systems, and have the potential to cause improvements in bioavailability and consequently therapeutic efficacy.

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Section: Solid Dispersionmentioning

confidence: 99%

Section: Cyclodextrin Inclusion Systemmentioning

confidence: 99%

Statins therapy: a review on conventional and novel formulation approaches

Tiwari

Pathak

2011

Journal of Pharmacy and Pharmacology

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“…The dissolution studies were performed in 500 mL of 0.5 % (w/v) SLS aqueous solution at 37 ± 0.5°C and 50 rpm. Samples were collected at 5,10,15,20,25,30,35,40,50, and 60 min using an automatic sampler, and filtered (0.20-lm pore size) and analyzed immediately after sampling. The quantitative determination for SIM and ASA was performed with HPLC system with a VWD (Agilent 1100).…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

“…Several approaches have been employed to improve the solubility of SIM such as the preparation of spherically agglomerated crystals of the drug [17], solid dispersions with PEG 6000 [18,19], PEG 4000 [19,20], PVP K30 [20,21], poloxamer 188 [21], or preparation of inclusion complexes with ß-cyclodextrin [22] and hydroxypropyl-bcyclodextrin [19,23].…”

Section: Introductionmentioning

confidence: 99%

Thermal, spectroscopic, and dissolution studies of the simvastatin–acetylsalicylic acid mixtures

Gòrniak

Karolewicz

Żurawska-Płaksej

et al. 2012

J Therm Anal Calorim

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The objective of the present investigation was to study the effect of eutectic formation on in vitro dissolution of simvastatin (SIM) released from mixtures with acetylsalicylic acid (ASA) prepared by a grinding method. SIM-ASA mixtures were characterized by means of differential scanning calorimetry (DSC), infrared spectroscopy (IR), X-ray powder diffractometry (XRPD), and in vitro dissolution tests. IR spectroscopy and XRPD studies indicated no interaction between SIM and ASA in the solid state. The DSC investigation has revealed that SIM and ASA form a simple eutectic system containing 66.6 % w/w of SIM at the eutectic point. In vitro dissolution studies of SIM and its mixtures with ASA were carried out. The eutectic mixture shows an appreciable increase in the dissolution rate in comparison with other ratios and SIM in 0.5 % w/v sodium lauryl sulfate. The dissolution enhancement of SIM was related to the effective wetting of the drug particles with a significantly reduced size released from eutectic composition. In conclusion, dissolution of SIM can be enhanced through eutectic formation with ASA by means of simple mechanical activation (a grinding method).

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“…After oral ingestion, SIM, an inactive lactone, is hydrolyzed to the corresponding β-hydroxy acid form. This is a principal metabolite and an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme-A (HMG Co-A) reductase, the enzyme that catalyses an early and rate-limiting step in the biosynthesis of cholesterol (12). SIM is a white, crystalline, nonhygroscopic powder, insoluble in water and 0.1 N HCl (30 µg/mL and 60 µg/mL, respectively).…”

Section: Introductionmentioning

confidence: 99%

Formulation and Optimization of Nanosuspensions for Enhancing Simvastatin Dissolution Using Central Composite Design

Pandya¹,

Patel²,

Patel³

2011

Dissolution Technol.

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Simvastatin is a poorly water-soluble drug, and bioavailability from its crystalline form is very low. The purpose of this investigation was to increase the solubility and dissolution rate of simvastatin by the preparation of nanosuspensions with Pluronic F127 and zirconium oxide (ZrO 2 ) beads using a wet-milling technique at the laboratory scale. Prepared nanosuspensions were evaluated for particle size and in vitro dissolution. A 3 2 central composite design was employed to study the effect of the independent variables (i.e., amount of Pluronic F127, X 1 , and amount of ZrO 2 , X 2 ) on the dependent variables (i.e., particle size [nm] and percentage of drug released after 10 min, Q 10 ). The relationship between the dependent and independent variables was further elucidated using multiple liner regression analysis (MLRA) and contour plots. The results show that nanosuspensions prepared with the higher concentrations of Pluronic F127 and the higher quantities of ZrO 2 (up to 8 g) reduced the particle size and enhanced the dissolution rate of the formulation. The dissolution rate of the optimized nanosuspension was enhanced (64% in 10 min) relative to that of a micronized suspension of simvastatin (3.5% in 10 min), mainly because of the formation of nanosized particles. These results show that the preparation of simvastatin-loaded nanosuspensions significantly improved the in vitro dissolution rate, thus possibly enhancing the fast onset of therapeutic drug effect.

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Preparation, Characterization, and Dissolution Behavior of a Solid Dispersion of Simvastatin with Polyethylene Glycol 4000 and Polyvinylpyrrolidone K30

Cited by 37 publications

References 37 publications

Statins therapy: a review on conventional and novel formulation approaches

Statins therapy: a review on conventional and novel formulation approaches

Thermal, spectroscopic, and dissolution studies of the simvastatin–acetylsalicylic acid mixtures

Formulation and Optimization of Nanosuspensions for Enhancing Simvastatin Dissolution Using Central Composite Design

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