Evaluation of In Vitro Equivalence for Tablets Containing the Poorly WaterSoluble Compound Atorvastatin

Popy, Farzana Akter; Dewan, Irin; Parvin, Most. Nazma; Islam, Saiful

doi:10.14227/dt190412p30

Cited by 10 publications

(11 citation statements)

References 11 publications

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“…Calculation of DE employs area under dissolution curve over a time period. The test products are considered to be similar when their DE values are close to that of reference product (within ± 10% is often acceptable) (26). DE values of all generic products selected in this study ranged from 74.2% to 88.0%, which were within ± 10% range of the innovator product (81.4%), as shown in Table 2.…”

Section: Dissolution Profilementioning

confidence: 78%

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Assessment of Physicochemical Properties and Comparison of Dissolution Profiles of Metformin Hydrochloride Tablets in Saudi Arabia

Bratty¹,

Alhazmi²,

Alam³

et al. 2020

Dissolution Technol.

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Although prevalence of substandard or counterfeit drugs is a world-wide problem, poor and developing countries are affected the most. To be a quality product, drug formulation must comply with certain standards. Consequently, in this study, metformin hydrochloride (MH) tablets (500 mg) available in the Saudi Arabian market were assessed through various pharmacopeial quality control tests. Parameters including weight variation, hardness, friability, drug content, and disintegration time were evaluated. Results were within acceptable limits for all selected products (nine generic and an innovator). Fourier-transform infrared spectroscopy (FT-IR) spectra of MH for all tested products were completely superimposed with that of the pure drug, confirming the use of correct active ingredient in all tablet formulations. The products were also evaluated by comparing the dissolution profile of the generic products with the innovator brand in pH 6.8 phosphate buffer. The range of percent drug release in 30 min was 82.71-98.43%, in comparison to 91.86% for reference product, which complies with the USP-NF specification of at least 80% drug release in 30 min. The difference factor (f 1 ), similarity factor (f 2 , except product H), and dissolution efficiency revealed that the dissolution profiles of the tested products were comparable to that of the reference product. These results show that the tested generic products were biopharmaceutically similar (except product H) to the innovator formulation. Therefore, the consumer can select any one of these equivalent products as a substitute for innovator product in case of cost concern or unavailability.

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Section: Dissolution Profilementioning

confidence: 78%

“…The values of f 1 and f 2 were used to analyze the dissolution profiles of the test products. A generic product with a value of f 1 between 0-15 and f 2 in the range of 50-100 is considered to have a similar drug release profile as the innovator product (25,26).…”

Section: Dissolution Testmentioning

confidence: 99%

Assessment of Physicochemical Properties and Comparison of Dissolution Profiles of Metformin Hydrochloride Tablets in Saudi Arabia

Bratty¹,

Alhazmi²,

Alam³

et al. 2020

Dissolution Technol.

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“…respectively. If f 1 is found in between 0-15 and f 2 in between 50-100, the dissolution profile of test generic brand is considered as bioequivalent with the innovator brand [9,10].…”

Section: Dissolution Studymentioning

confidence: 99%

Quality Control Measurement and in vitro Bioequivalence of Candesartan Cilexetil Tablets Marketed in Saudi Arabia

Bratty

Alhazmi

Makeen

et al. 2020

JPRI

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Aim: Some generics were reported to be counterfeit and inferior quality than the innovators. This study was aimed to make sure about the compliance with standard specifications and evaluation of the quality of different selected brands (generic and innovator), after performing different pharmacopeial quality control tests, of Candesartan cilexetil tablets (16 mg) commercially available in Saudi Arabia for hypertensive patients. Study Design: In vitro study of tablets. Place and Duration of Study: College of Pharmacy, Jazan University, Jazan, KSA, between September 2018 and May 2019. Methodology: The different generic brands of Candesartan cilexetil (CC) and innovator brand (16 mg) were subjected to weight variation, hardness, friability, assay, and disintegration tests following the established protocols. The purity of active ingredient was authenticated by comparative analysis of FT-IR spectra with pure drug. In vitro bioequivalence was studied after analyzing the results of dissolution summaries in phosphate buffer (pH 6.5) mixed with polysorbate 20 (0.35% v/v). Results: The results of the tests conducted for evaluation of the tablets were found to be in acceptable limits for all the selected brands. After comparative analysis of FT-IR spectra with pure drug, it was inferred that correct active ingredient was used for the preparation of tablets. The drug release profile exhibited 96.89 – 101.97% of release of CC from all generic brands, in comparison to 99.4% for innovator brand after 60 min of study. The assessment of difference factor (f1<15) and similarity factor (f2>50) revealed the resemblance of generic brands with that of innovator brand. Furthermore, the dissolution efficiency (DE = ±10% of the innovator value) of all generic brands (73.12 – 73.25%) exhibited equivalency with that of innovator brand (70.45%). Conclusion: The selected generics were considered to be biopharmaceutically equivalent to the innovator and maintained their efficacy. As a consequence, these brands can be used interchangeably by the hypertensive patients in Saudi Arabia.

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“…The solubility is pH-dependent i.e at pH 1.2 is 0.02mg/mL while increases to 1.23mg/mL at pH 6.8 (Kearney et al, 1993). The dose/solubility ratio for atorvastatin calcium is more than 250mL for the 10mg dose at pH 1.2 and dissolves in 250mL at pH 6.8 (Popy et al, 2012). The low oral bioavailability of atorvastatin calcium (12-14%) is caused by low aqueous solubility in the gastric and high first-pass metabolism in the liver (Sonje et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

“…The low oral bioavailability of atorvastatin calcium (12-14%) is caused by low aqueous solubility in the gastric and high first-pass metabolism in the liver (Sonje et al, 2010). The dissolution profiles of atorvastatin calcium tablets which are currently marketed with generic and branded generic names vary per product and affect their bioavailability profiles (Oishi et al, 2011;Popy et al, 2012). Several techniques have been developed to increase the dissolution of atorvastatin calcium, including crystal modification (Gozali et al, 2014; ), co-grinding (Prabhu and Patravale, 2015), solid dispersion (Gozali et al, 2015;Rodde et al, 2014;Panghal et al, 2014;Khan and Dehghan, 2011), lipid-based formulations such as micro and nanoemulsions (Chouksey et al, 2011;Snela et al, 2019;Kadu et al, 2011), and liquisolid technique (Gubbi and Jarag, 2010;Baskaran et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

Liquisolid Tablets Formulation of Atorvastatin Calcium Using Polyethylene Glycol 400 as Solvent and Some Carrier Materials

et al. 2020

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The dissolution of atorvastatin calcium need to be improved since included BCS Class II drugs with low solubility and high permeability, meaning that the dissolution affects the bioavailability of drugs. This research aimed to develop a formulation of a liquisolid tablet using PEG 400 as a solvent and some carrier materials in various compositions to increase the dissolution of atorvastatin calcium. Different formulations of liquisolid tablets were conducted using different quantities of carrier and coating material for adsorbing liquid solvent to produce a free-flowing and compressible powder. Avicel PH 101, Avicel PH 102, Neusilin US2 were employed as the carrier and Aerosil 200 as the coating material. A disintegrant and lubricant were then added to the formed liquisolid system and compressed into tablets by the direct compressing method. The liquisolid tablets were characterized for their tableting properties and possible drug-excipient interaction by XRD and FTIR analysis. The tableting characteristics of atorvastatin calcium liquisolid tablets were within the acceptable limits criteria. The dissolution of AA4 and NA1 liquisolid tablets was higher compared to marketed tablets. Based on the XRD and FTIR analysis, no interactions between drug and excipient.

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Evaluation of In Vitro Equivalence for Tablets Containing the Poorly WaterSoluble Compound Atorvastatin

Cited by 10 publications

References 11 publications

Assessment of Physicochemical Properties and Comparison of Dissolution Profiles of Metformin Hydrochloride Tablets in Saudi Arabia

Assessment of Physicochemical Properties and Comparison of Dissolution Profiles of Metformin Hydrochloride Tablets in Saudi Arabia

Quality Control Measurement and in vitro Bioequivalence of Candesartan Cilexetil Tablets Marketed in Saudi Arabia

Liquisolid Tablets Formulation of Atorvastatin Calcium Using Polyethylene Glycol 400 as Solvent and Some Carrier Materials

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