Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique

Dong, Wenxiang; Su, Xitong; Xu, Meng; Hu, Mingming; Sun, Yinghua; Zhang, Peng

doi:10.1016/j.ajps.2018.08.010

Cited by 47 publications

(33 citation statements)

References 39 publications

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“…Hence, the preparation of ATO-loaded SD essentially showed the initial burst release taking advantage of the increased surface area, amorphous state, and effective wettability of carriers (HPMC and SLS). Similar drug kinetic results have been reported for atorvastatin [30], atorvastatin calcium/ezetimibe [24], itraconazole [43], etc. By 60 min, both the ATO and F2 had dissolved to their maximum state, showing plateaus thereafter.…”

Section: Resultssupporting

confidence: 84%

“…We hypothesized that the in vitro and in vivo characteristics of atorvastatin calcium (ATO) would be improved by incorporating the drug into a cellulose matrix. Several studies have been carried out with ATO, such as preparation of ATO SDs [30,31,32], size reduction (i.e., ATO nanopreparations) [33]. However, the influence of the cellulose matrix system on the preparation and characterization ATO-loaded ternary solid dispersion system is an area of interest that needs investigating.…”

Section: Introductionmentioning

confidence: 99%

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Spray-Dried Amorphous Solid Dispersions of Atorvastatin Calcium for Improved Supersaturation and Oral Bioavailability

et al. 2019

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Over the past few decades, the amorphous solid dispersions (ASDs) technique has emerged as a promising strategy to enhance the in vitro/in vivo characteristic of hydrophobic drugs. The low aqueous solubility and poor bioavailability of atorvastatin calcium (ATO), a lipid-lowering drug, present challenges for effective drug delivery. The objective of this work was to improve the aqueous solubility, in vitro dissolution, and oral absorption of ATO with amorphous solid dispersion technique prepared by spray-drying method. The optimized ternary formulation comprising of ATO; hydroxypropyl methylcellulose (HPMC), as a hydrophilic polymer; and sodium lauryl sulfate (SLS), as a surfactant, at a weight ratio of 1/1/0.1, showed significant improvement in aqueous solubility by ~18-fold compared to that of the free drug, and a cumulative release of 94.09% compared to a release of 59.32% of the free drug. Further, physicochemical studies via scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction revealed a change from the crystalline state of the free drug to its amorphous state in the ASD. Pharmacokinetic analysis in rats demonstrated 1.68- and 2.39-fold increments in AUC and Cmax, respectively, in the ASD over the free drug. Altogether, hydrophilic carrier-based ASDs prepared by the spray-drying technique represent a promising strategy to improve the biopharmaceutical performance of poorly soluble drugs.

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Section: Resultssupporting

confidence: 84%

Section: Introductionmentioning

confidence: 99%

Spray-Dried Amorphous Solid Dispersions of Atorvastatin Calcium for Improved Supersaturation and Oral Bioavailability

et al. 2019

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“…Due to its low melting point, high drug loading, good hydrophilicity, and good safety, PLX is not only widely used in some traditional formulations, such as suppositories, tablets, and emulsions, but also can form micelles to increase the solubility of insoluble drugs, increase the stability of drugs, and promote the absorption of drugs by the body. Additionally, it is a surfactant approved by the FDA [19]. Moreover, PLX is also a commonly used carrier material for poorly water-soluble PLX is also a commonly used carrier material for poorly water-soluble drugs, which can ensure the high dispersibility of drugs in water and prevent drug aggregation [20,21].…”

Section: Introductionmentioning

confidence: 99%

Highly Water-Soluble Solid Dispersions of Honokiol: Preparation, Solubility, and Bioavailability Studies and Anti-Tumor Activity Evaluation

et al. 2019

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Honokiol (HK), a well-tolerated natural product, has many multiple pharmacological activities. However, its poor water solubility and low bioavailability limit its clinical application and development. The aim of this research was to prepare the solid dispersion (SD) formulation of honokiol (HK) with poloxamer-188 (PLX) as the carrier, thereby improving its solubility and oral bioavailability. Firstly, by investigating the relationship between the addition amount of the PLX and the solubility of HK, and the effects of solid dispersions with different ratios of HK–PLX on the solubility of HK, we determined that the optimum ratio of PLX to HK was (1:4). Then, the HK–PLX (1:4) SD of HK was prepared using the solvent evaporation method. The morphology of the obtained HK–PLX (1:4) SD was different from that of free HK. The HK in the HK–PLX (1:4) SD existed in amorphous form and formed intermolecular hydrogen bonds with PLX. Additionally, the solubility values of the HK–PLX (1:4) SD were about 32.43 ± 0.36 mg/mL and 34.41 ± 0.38 mg/mL in artificial gastric juice (AGJ) and in artificial intestinal juice (AIJ), respectively. Compared with free HK, the release rate and the bioavailability was also substantially improved for HK in its SD form. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay indicated that the HK–PLX (1:4) SD showed higher inhibition of HepG2 cells than free HK. Taken together, the present study suggests that the HK–PLX (1:4) SD could become a new oral drug formulation with high bioavailability and could produce a better response for clinical applications of HK.

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“…There is no statistically noteworthy differences found in any of the lipid values estimated between the morning and night administration of atorvastatin 12 . Therefore, the development of formulation with ATR is challenging to the formulator requiring solubility enhancement through solid dispersion technique 13 . The aim of the work was to develop and evaluate an oral pharmaceutical equivalent, a stable, robust, and controlled bilayer tablet of Atorvastatin and Captopril, which is very well tolerated, having less side effects with improved bioavailability and high patient acceptance.…”

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confidence: 99%

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2020

IJPSR

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The aim of the present research work was to develop a bilayer floating dosage form of immediate-release Atorvastatin (ATR) and sustained release Captopril (CPT) in matrix form for the treatment of hyperlipidaemia and hypertension to reduce multiple dosing frequencies and enhance patient compliance. ATR belongs to the BCS Class II category having poor aqueous solubility, which was enhanced by using hydrophilic polymer PEG 8000 by kneading technique. A sustained layer of CPT was prepared by melt granulation technique using various concentrations of carnauba wax with HPMC K 100 M and Carbopol 934 P. All the parameters before and after compression were evaluated. ATR-PEG ratio of 1:0.25 showed a higher drug release of about 97.42% within 60 min. The optimized CPT sustained layer SR2 shown the highest drug release 98.2% in 12 h. In-vitro drug release studies carried out as per USP in pH 1.2 buffer using type II apparatus. The CPT layer exhibited release kinetics in the first order and followed the diffusion and erosion mechanism. The FTIR, XRD studies, and SEM analysis indicated the absence of strong interaction between drug and polymer and compatibility among them. The novel concept of Bi-layer gastric floating can be utilized for the formulation of ATR and sustained release of CPT with a floating period of >12 h and 45 s lag time.

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Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique

Cited by 47 publications

References 39 publications

Spray-Dried Amorphous Solid Dispersions of Atorvastatin Calcium for Improved Supersaturation and Oral Bioavailability

Spray-Dried Amorphous Solid Dispersions of Atorvastatin Calcium for Improved Supersaturation and Oral Bioavailability

Highly Water-Soluble Solid Dispersions of Honokiol: Preparation, Solubility, and Bioavailability Studies and Anti-Tumor Activity Evaluation

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