Modulation of gastric pH by a buffered soluble effervescent formulation: A possible means of improving gastric tolerability of alendronate

Hodges, Lee Ann; Connolly, S.M.; Winter, John; Schmidt, Thomas; Stevens, H. N. E.; Hayward, Marshall A.; Wilson, Clive G.

doi:10.1016/j.ijpharm.2012.04.073

Cited by 16 publications

(10 citation statements)

References 15 publications

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“…In light of these considerations an effervescent formulation of alendronate rather than tablets has been proposed, showing a more rapid gastric transit and the ability to rapidly increase gastric pH after the ingestion of the drug [51]. This last finding could have extremely important implications in reducing the intrinsic pro-inflammatory action of these compounds at the esophageal level.…”

Section: Discussionmentioning

confidence: 99%

“…The observation was conducted by Hodges et al [51] in a single-center, open-label, randomized, two-way crossover study in 12 healthy female volunteers. This clinical study evaluated gastric emptying and gastric pH after administration of alendronate tablets and a novel effervescent alendronate formulation with a high buffering capacity.…”

Section: New Alendronate Formulationmentioning

confidence: 99%

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The potential impact of new effervescent alendronate formulation on compliance and persistence in osteoporosis treatment

2014

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Osteoporotic fractures are a public health problem and their incidence and subsequent economic and social costs are expected to rise in the next future. Different drugs have been developed to reduce osteoporosis and the risk of osteoporotic fractures, and among them, antiresorptive agents, and in particular oral alendronate, are the most widely utilized. However, one of the most common problems with antiresorptive drugs is poor adherence to treatment, which is associated with a high fracture incidence and with an increase in hospitalization costs. One of the main reasons of poor adherence to these treatments is the occurrence of adverse events, mainly at gastrointestinal (GI) level, including dyspepsia, dysphagia, and esophageal ulcers. In light of these considerations the aim of this paper is to perform a literature review to show the pathophysiologic bases of GI alendronate-induced adverse events and how new bisphosphonate formulations like effervescent alendronate can improve compliance and persistence to treatment and decrease the fracture rate incidence in osteoporotic patients.

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Section: Discussionmentioning

confidence: 99%

Section: New Alendronate Formulationmentioning

confidence: 99%

The potential impact of new effervescent alendronate formulation on compliance and persistence in osteoporosis treatment

2014

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“…Probably a combination of all these recommendations would be the best strategy to promote compliance and adherence. On the other hand, as most osteoporosis patients are elderly and may have difficulty swallowing, a soluble dosage form would improve the gastric tolerability of bisphosphonates, which would favor patients' treatment compliance, as noted by 88.9% of those physicians surveyed 40 .…”

Section: Discussionmentioning

confidence: 99%

Percepción de los profesionales médicos respecto la adherencia terapéutica de los pacientes con osteoporosis

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Casado

González

et al. 2016

Rev Osteoporos Metab Miner

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Introduction: Adherence to oral treatment of patients with osteoporosis is low, with a high dropout rate in the first year. The most noteworthy result is the lack of therapeutic response. Objective: To ascertain the perception of physicians working with osteoporotic patients regarding adherence of these patients. Methods: Cross-sectional study conducted by opinion survey aimed at primary care physicians and specialists involved in osteoporosis treatment. Participants were selected by purposive sampling. Results: The questionnaire was answered by 235 specialists encompassing rheumatology (54.5%), orthopedics (10.6%) and primary care (18.7%). In 43.8% of participants, more than 25% of patients sometimes forget to take their treatment. According to 34.9%, more than 75% of patients are aware of treatment. Side effects and management complexity are the majority reasons that lead to a change in medication, mean value of 7.94±2.06 6±2.01 points respectively on a 0-10 scale. Conclusions: Overall, medical specialists attributed low adherence to side effects, polypharmacy and lack of communication between professionals. Dosage and space use of soluble dosage forms may be options to facilitate patient adherence to treatment with oral bisphosphonates. Improved education concerning the importance of the disease or increased patient monitoring could foster adherence.

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“…In the present work, effervescent floating tablets of Ca-Na 2 EDTA using 13 different formulation combinations were prepared and the combination showing the best results (formula F8) with respect to floating lag time, total floating duration, swelling ability, and sustained drug release was chosen and compared with conventionally made non-floating tablet of Ca-Na 2 EDTA for drug-release data. Effervescent oral drug delivery systems are known to be beneficial in the sense that they also reduce several of the local GIT side effects associated with administration of oral formulations, such as gastric irritation, nausea, and gastritis (25). Combination of sodium bicarbonate and citric acid was chosen as effervescing agent to provide the desired floating ability to the formulation.…”

Section: Discussionmentioning

confidence: 99%

Development and Optimization of Gastro-Retentive Controlled-Release Tablet of Calcium-Disodium Edentate and its In Vivo Gamma Scintigraphic Evaluation

et al. 2015

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ABSTRACT. Medical management of heavy metal toxicity, including radioactive ones, is a cause for concern because of their increased use in energy production, healthcare, and mining. Though chelating agents like EDTA and DTPA in parenteral form are available, no suitable oral formulation is there that can trap ingested heavy metal toxicants in the stomach itself, preventing their systemic absorption. The objective of the present study was to develop and optimize gastro-retentive controlled-release tablets of calcium-disodium edentate (Ca-Na 2 EDTA). Gastro-retentive tablet of Ca-Na 2 EDTA was prepared by direct compression method. Thirteen tablet formulations were designed using HPMC-K4M, sodium chloride, and carbopol-934 along with effervescing agents sodium bicarbonate and citric acid. Tablet swelling ability, in vitro buoyancy, and drug dissolution studies were conducted in 0.1 N HCl at 37±0.5°C. Ca-Na 2 EDTA was radiolabeled with technetium-99m for scintigraphy-based in vivo evaluation. Formula F8 (Ca-Na 2 EDTA 200 mg, carbopol 100 mg, avicel 55 mg, citric acid 30 mg, NaHCO 3 70 mg, NaCl 100 mg, and HPMC 95 mg) was found to be optimum in terms of excellent floating properties and sustained drug release. F8 fitted best for KorsmeyerPeppas equation with an R 2 value of 0.993. Gamma scintigraphy in humans showed mean gastric retention period of 6 h. Stability studies carried out in accordance with ICH guidelines and analyzed at time intervals of 0, 1, 2, 4, and 6 months have indicated insignificant difference in tablet hardness, drug content, total floating duration, or matrix integrity of the optimized formulation. Gastro-retentive, controlled-release tablet of CaNa 2 EDTA was successfully developed using effervescent technique as a potential oral antidote for neutralizing ingested heavy metal toxicity.

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Modulation of gastric pH by a buffered soluble effervescent formulation: A possible means of improving gastric tolerability of alendronate

Cited by 16 publications

References 15 publications

The potential impact of new effervescent alendronate formulation on compliance and persistence in osteoporosis treatment

The potential impact of new effervescent alendronate formulation on compliance and persistence in osteoporosis treatment

Percepción de los profesionales médicos respecto la adherencia terapéutica de los pacientes con osteoporosis

Development and Optimization of Gastro-Retentive Controlled-Release Tablet of Calcium-Disodium Edentate and its In Vivo Gamma Scintigraphic Evaluation

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