A comparative pH-dissolution profile study of selected commercial levothyroxine products using inductively coupled plasma mass spectrometry

Pabla, Dimple; Akhlaghi, Fatemeh; Zia, Hossein

doi:10.1016/j.ejpb.2008.10.008

Cited by 113 publications

(103 citation statements)

References 19 publications

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“…Furthermore, Table III indicates that the experimental results obtained for C max and AUC were close to the simulated values. This finding is in accordance with the results described in other studies that applied the GastroPlus™ (10,12,15,35,36). This provides evidence that the ASF Opt logD Model SA/V 6.1 was a good prediction model of the absorption properties of batch A based on in vivo studies.…”

Section: In Silico Studiessupporting

confidence: 92%

“…This phenomenon was shown to be clearly differentiated for the powder dissolution method (P<0.05). Some previous dissolution studies using SLS have shown that the use of lower percentages of surfactant in the media provides greater discriminatory power to the dissolution method (34)(35)(36). Based on the Farmanguinhos method, the percentage of efavirenz dissolved during a 60-min period was 87.51% for biobatch A versus 66.93% for biobatch B (Fig.…”

Section: Powder and Tablet Dissolution Studiesmentioning

confidence: 92%

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In Vitro–In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

et al. 2013

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Abstract. The aim of the present work was to use GastroPlus™ software for the prediction of pharmacokinetic profiles and in vitro-in vivo correlation (IVIVC) as tools to optimize the development of new generic medications. GastroPlus™ was used to simulate the gastrointestinal compartment and was based on the advanced compartmental absorption and transit model. Powder dissolution and efavirenz tablet dissolution studies were carried out to generate data from which correlation was established. The simulated plasma profile, based on the physicochemical properties of efavirenz, was almost identical to that observed in vivo for biobatches A and B. A level A IVIVC was established for the dissolution method obtained for the generic candidate using the Wagner-Nelson (r 2 =0.85) and for Loo-Riegelman models (r 2 =0.92). The percentage of fraction absorbed indicated that 0.5% sodium lauryl sulfate may be considered a biorelevant dissolution medium for efavirenz tablets. The simulation of gastrointestinal bioavailability and IVIVC obtained from immediate-release tablet formulations suggests that GastroPlus™ is a valuable in silico method for IVIVC and for studies directed at developing formulations of class II drugs.KEY WORDS: bioavailability; computational simulation; efavirenz; GastroPlus™; in vivo-in vitro correlation.

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Section: In Silico Studiessupporting

confidence: 92%

Section: Powder and Tablet Dissolution Studiesmentioning

confidence: 92%

In Vitro–In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

et al. 2013

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“…Batches A and B were considered statistically different only in media containing 0.5% (p < 0.001) and 1.0% SLS (p < 0.001) according to ANOVA analysis. Evaluation of both intrinsic dissolution profiles in comparison to the IDR values (Table 4) shows differences between batches A and B at these surfactant concentrations, especially 0.5% SLS, indicating that the higher surfactant concentrations resulted in nondiscriminatory media, as shown in other studies (46)(47)(48).…”

Section: Intrinsic Dissolution Rate Of Different Efavirenz Raw Materialssupporting

confidence: 64%

Development of a Discriminative Intrinsic Dissolution Method for Efavirenz

Pinto¹,

Cabral²,

Sousa³

2014

Dissolution Technol.

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Efavirenz is a poorly water-soluble drug categorized as a Class 2 drug under the Biopharmaceutics Classification System (BCS). Intrinsic dissolution is an effective tool for evaluating the physical-chemical properties of an active pharmaceutical ingredient (API). The aim of this study was to develop an intrinsic dissolution method for use in quality control of efavirenz to be used in the selection of an API for the production of dosage forms. The influence of compression force, rotation speed, dissolution medium, and surfactant concentration on the intrinsic dissolution rate (IDR) of efavirenz were evaluated using a rotating-disk holder. The developed method was applied to the evaluation of batches using different raw materials (batches A-G). Dissolution media containing 0.5% sodium lauryl sulfate (SLS) and a rotation speed of 100 rpm proved the most discriminative. Batches A, D, and F provided intrinsic dissolution rate (IDR) values greater than 36 µg/min/cm 2 in this medium, while batches B and E provided IDR values of approximately 31 µg/min/cm 2 . The IDRs obtained showed a high correlation with the surface areas of the batches. The method may be used in the development of efavirenz formulations to select API with physical-chemical properties that enable appropriate dosage form dissolution.

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“…There is also evidence indicating that hypothyroid patients treated with levothyroxine gel caps may experience less thyroid hormone fluctuation than with treatment using levothyroxine tablets [23][24][25][26][27][28].…”

Section: Introductionmentioning

confidence: 99%

The Economic Impact of Changing Levothyroxine Formulations in Difficult-to-Treat Hypothyroid Patients: An Evidence-Based Model

Elmor¹,

Sandulli²,

Carter³

2017

Pharmacoeconomics

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Objective: To determine the budget impact of incorporating levothyroxine gel caps in the treatment plan of patients diagnosed with hypothyroidism who experience multiple levothyroxine dose or formulation changes annually due to inadequate efficacy or tolerability.Methods: Cost estimates of levothyroxine formulations were obtained. Estimated utilization patterns and costs of physician services, laboratory tests, ancillary healthcare services, and lost productivity were quantified based on published literature and government/public sources. The patient population was based on epidemiology reports and estimates from the American Association of Clinical Endocrinology and the American Thyroid Association. All calculations of economic outcomes were determined using a budget impact model constructed in a MS Excel platform.Results: The economic model demonstrated for a population of 500,000 persons, there are 23,000 (4.6%) people with hypothyroidism, of which 18,400 (80.0%) receive pharmacologic treatment, including 17,480 (95.0%) that receive levothyroxine. The proportion of patients requiring ≥ 1 dosage changes annually is 31.4%, producing 5,489 "hard-to-treat" patients. Similarly, the proportion of patients requiring ≥ 2 dosage changes annually is 8.0% or 1,398 "harder-to-treat" patients. Using evidence-based data of the tolerability and absorption characteristics of levothyroxine gel caps, changing 20.0% of the target cohort to the gel cap formulation produced annual net cost savings of $542,901 in direct medical costs and $564,650 in lost productivity for "hard-to-treat" patients and savings of $409,107 in direct medical costs and $441,926 in lost productivity for "harder-to-treat" patients. Conclusions:Consideration of switching levothyroxine product from a tablet to a gel cap formulation is justified on an economic and therapeutic basis for hypothyroid patients at risk of subadequate drug efficacy or tolerability as measured by the need for one or more annual levothyroxine dosage or formulation adjustments.

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A comparative pH-dissolution profile study of selected commercial levothyroxine products using inductively coupled plasma mass spectrometry

Cited by 113 publications

References 19 publications

In Vitro–In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

In Vitro–In Vivo Correlation of Efavirenz Tablets Using GastroPlus®

Development of a Discriminative Intrinsic Dissolution Method for Efavirenz

The Economic Impact of Changing Levothyroxine Formulations in Difficult-to-Treat Hypothyroid Patients: An Evidence-Based Model

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