Development and characterization of an atorvastatin solid dispersion formulation using skimmed milk for improved oral bioavailability

Ankush, Choudhary; Rana, Avtar Chand; Aggarwal, Geeta; Kumar, Virender; Zakir, Foziyah

doi:10.1016/j.apsb.2012.05.002

Cited by 89 publications

(65 citation statements)

References 25 publications

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“…However, it has low oral bioavailability (12%) as a result of low aqueous solubility, crystalline nature, rapid presystemic clearance in the gut wall and hepatic first-pass metabolism (Lau et al, 2006). Poor performance of AT leads to administration in high doses possibly leading to liver abnormalities, rhabdomyolysis, arthralgia and kidney failure (Choudhary et al, 2012). So, improvement of solubility and hence oral bioavailability of crystalline AT can be achieved through developing a method that reduces the particle size and maintains the drug in an amorphous state (Anwar et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Atorvastatin-loaded nanostructured lipid carriers (NLCs): strategy to overcome oral delivery drawbacks

et al. 2017

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Atorvastatin (AT) is a widely used lipid-regulating drug to reduce cholesterol and triglycerides. Its poor aqueous solubility and hepatic metabolism require development of drug delivery systems able to improve its solubility and bypass hepatic effect. For this purpose, atorvastatin nanostructured lipid carriers (AT-NLCs) were prepared and characterized. AT-NLCs were prepared by emulsification using high-speed homogenization followed by ultrasonication. The prepared NLCs showed particle size between 162.5 ± 12 and 865.55 ± 28 nm while zeta potential values varied between À34 ± 0.29 and À23 ± 0.36 mV. They also showed high encapsulation efficiency (>87%) and amorphous state of the drug in lipid matrix. Pharmacokinetic parameters of optimized formulation (NLC-1; composed of 2% Gelucire V R 43/01, 8% Capryol V R PGMC, 2% Pluronic V R F68 and 0.5% lecithin) revealed 3.6-and 2.1-fold increase in bioavailability as compared to atorvastatin suspension and commercial product (Lipitor V R ), respectively. Administration of NLC-1 led to significant reduction (p < .05) in the rats' serum levels of total cholesterol (TC), triglyceride (TG), low-density lipoprotein (LDL) and significant increase in highdensity lipoprotein (HDL). This improvement was confirmed histologically by minimizing the associated hepatic steatosis. These investigations demonstrated the superiority of NLCs for improvement of oral bioavailability and in vivo performance of AT. ARTICLE HISTORY

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Section: Introductionmentioning

confidence: 99%

Atorvastatin-loaded nanostructured lipid carriers (NLCs): strategy to overcome oral delivery drawbacks

et al. 2017

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“…21 Use of skimmed milk is also preferred over polymers in case of poorly soluble or lipophilic drugs because of their own high viscosity. 16 It also represses gastric irritation and hence no abdominal pain is noticed with the use of milk as a dispersion medium with NSAIDs. 22 NSAIDs are advised to be administered with milk to reduce the side effects that appear with their use like gastric irritation which is due to COX inhibition.…”

Section: Composition Based Mechanism Of Milkmentioning

confidence: 99%

“…For this reason, this approach can be considered universal for ionized as well as unionized lipophilic drugs. 16 Milk has not been officially registered as an excipient from a regulatory aspect; but casein which is considered as a major protein present in the milk is included in the list of Generally Recognized as Safe (GRAS) substance.…”

Section: Regulatory Aspectsmentioning

confidence: 99%

An Investigative and Explanatory Review on Use of Milk as a Broad-Spectrum Drug Carrier for Improvement of Bioavailability and Patient Compliance

Kamal¹,

Kaur²,

Singh³

et al. 2016

JYP

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Objective: The main objective of this review is to investigate the potential role of milk in improvement of bioavailability and patient compliance. Method: The study reviews the types of milk based on its composition, mechanism of how milk improves the solubility of poorly soluble drugs, masks the taste of bitter drugs and improves the patient compliance to dosage regimen. It also reviews various research studies done so far that recommend the use of milk in formulations. Along with this, the regulatory aspect of using milk is also considered in the present study. Conclusion: Investigation concludes that medicated milk formulations open a new hope of utilizing milk as multi-functional drug carrier for a variety of drugs.

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“…Third method was physical mixture in which the mixture of drug and excipient was taken in mortar and triturated by pestle. [7] Phase solubility study [8] Phase solubility studies were performed as directed by the methods described in Higuchi and Connors.…”

Section: Preparation Of Solid Dispersionmentioning

confidence: 99%

“…Aliquots of regularly taken samples analyzed spectrophotometrically, and equal volume of dissolution medium was replaced. [7,9] Preparation of tablets [10,11] Tablets were prepared by the direct compression method from an optimized batch of kneaded Tablets were compressed into the tablets using 8 mm diameter punches on rotary tablet machine. The tablets were prepared separately in the proportions given in Table 1.…”

Section: In-vitro Dissolution Studiesmentioning

confidence: 99%

Assessment of Ludiflash as a Superdisintegrant in Formulation and Evaluation of Fast Disintegrating Tablet of Febuxostat

Rajpure¹

2017

WJPR

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Development and characterization of an atorvastatin solid dispersion formulation using skimmed milk for improved oral bioavailability

Cited by 89 publications

References 25 publications

Atorvastatin-loaded nanostructured lipid carriers (NLCs): strategy to overcome oral delivery drawbacks

Atorvastatin-loaded nanostructured lipid carriers (NLCs): strategy to overcome oral delivery drawbacks

An Investigative and Explanatory Review on Use of Milk as a Broad-Spectrum Drug Carrier for Improvement of Bioavailability and Patient Compliance

Assessment of Ludiflash as a Superdisintegrant in Formulation and Evaluation of Fast Disintegrating Tablet of Febuxostat

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