Influence of Mineral Water on Absorption of Oral Alendronate in Rats

Akagi, Yuuki; Sakaue, Tomoyuki; Yoneyama, Eiji; Aoyama, Takao

doi:10.1248/yakushi.131.801

Cited by 6 publications

(7 citation statements)

References 12 publications

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“…These results were similar to those reported for alendronate. 4) In examinations of calcium and magnesium chloride aqueous solutions of the same hardness, the cumulative recovery rates of risedronate were 54% (0.27±0.04%) and 12% (0.51±0.08%) lower, respectively, than that for ultrapure water (Table 3, Fig. 4).…”

Section: Discussionmentioning

confidence: 89%

“…We previously reported the influence of mineral water on the absorption of orally administered alendronate in rats. 4) Risedronate is a BP that is often prescribed for patients with osteoporosis, similar to alendronate. In this study, we investigated the effect of three kinds of mineral water ("Amami no mizu" (DeepSeawater), evian ® , and Contrex ® ) on the absorption of orally administered risedronate, based on analysis of urinary excretion in rats.…”

Section: Discussionmentioning

confidence: 99%

“…We previously reported that the absorption of alendronate decreases with increasing calcium concentration of mineral water consumed when taking that drug. 4) However, standards regarding metal cations in mineral waters taken with alendronate have not been defined. The bioavailability of BPs after oral administration is very low (1-2%), and gastrointestinal absorption can be inhibited even further due to chelation of metal cations.…”

Section: )mentioning

confidence: 99%

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Interaction between Bisphosphonates and Mineral Water: Study of Oral Risedronate Absorption in Rats

Itoh

Akagi

Shimomura

et al. 2016

Biological & Pharmaceutical Bulletin

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Bisphosphonates are antiosteoporotic agents prescribed for patients with osteoporosis. Drug package inserts for bisphosphonate supplements indicate that their bioavailability is reduced by high levels of metal cations (Ca 2 , Mg 2 , etc.). However, standards for these cations in water used for taking risedronate have not been defined. Here, we examined the effect of calcium and magnesium in mineral waters on the bioavailability of the third-generation bisphosphonate, risedronate, following oral administration in rats. As risedronate is unchanged and eliminated renally, risedronate absorption was estimated from the amount excreted in the urine. Risedronate was dissolved in mineral water samples and administered orally at 0.35 mg/ kg. Urine samples were collected for 24 h after dosing. Risedronate was extracted from urine using ion-pair solid-phase cartridges and quantified by HPLC with UV detection (262 nm). Cumulative recovery of risedronate was calculated from the amount excreted in the urine. Key words risedronate; mineral water; drug interaction; urine excretion; rat Osteoporosis is a systemic disease characterized by reduced bone mass and structural deterioration of bone tissue, leading to an increased risk of fracture. According to the 2011 Guidelines for the Treatment of Osteoporosis, the number of patients with osteoporosis in the rapidly aging population of Japan is increasing and is now estimated at about 13 million. 1)The occurrence of a fracture significantly impacts a person's daily activities, so pharmacotherapy for the prevention of osteoporosis is recommended for patients who are at high risk of bone fracture. A variety of drugs are available for treating osteoporosis, including calcium agents, active vitamin D 3 , raloxifene, and bisphosphonates (BPs). BPs exhibit particularly potent bone resorption inhibitory activity and are therefore the first-choice drug for treating osteoporosis. 1)Because they inhibit resorption and thus increase bone mineral density, BPs play an important role in treating postmenopausal osteoporosis. The resorption-inhibiting activity of risedronate, a third-generation BP, is reported to be approximately 3000 times that of etidronate, a first-generation BP.2) Recently, risedronate began to be marketed for once per month (75 mg), in addition to daily (2.5 mg) and weekly (17.5 mg) dosing.The variety of mineral waters sold and consumed in Japan has increased in recent years. Annual consumption of mineral water per person in Japan was 25.7 L in 2014 (approximately 3 times that of 15 years ago).3) The consumption of mineral waters in Japan is predicted to increase further in coming years. For orally administered BPs, the package inserts advise patients and health care workers that the bioavailability of the drug may be reduced when taken with mineral waters containing high levels of metal cations (Ca 2+ , Mg 2+, etc.), as a result of chelation (Ajinomoto Co., Inc., Actonel ® package insert [2013/2]). As the hardness of a mineral water depends on its calcium and magnesium conten...

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Section: Discussionmentioning

confidence: 89%

Section: Discussionmentioning

confidence: 99%

Section: )mentioning

confidence: 99%

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Interaction between Bisphosphonates and Mineral Water: Study of Oral Risedronate Absorption in Rats

Itoh

Akagi

Shimomura

et al. 2016

Biological & Pharmaceutical Bulletin

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“…However, all of these regimens, like other oral bisphosphonate dosing schedules, require dosing at least 30 min before food or drink. Even taking oral bisphosphonates with tap water or bottled water can decrease bioavailability [20]. None of the current oral bisphosphonate dosing schemes solves the possible detrimental effect of poor compliance with dosing instructions on bisphosphonate absorption and clinical effectiveness.…”

Section: Discussionmentioning

confidence: 99%

Treatment of postmenopausal osteoporosis with delayed-release risedronate 35 mg weekly for 2 years

et al. 2012

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SummaryBone mineral density response to once weekly delayed-release formulation of risedronate, given before or following breakfast, was non-inferior to that seen with traditional immediate-release risedronate given daily before breakfast. Delayed-release risedronate is a convenient dosing regimen for oral bisphosphonate therapy that might avoid poor compliance.IntroductionThis 2-year, randomized, controlled, non-inferiority study assessed the efficacy and safety of a delayed-release (DR) 35-mg weekly oral formulation of risedronate that allows subjects to take their weekly risedronate dose before or immediately after breakfast. Results from the first year of the study were published previously (McClung et al. Osteoporos Int 23(1):267-276, 2012); we now report the final results after 2 years.MethodsWomen with postmenopausal osteoporosis were randomly assigned to receive risedronate 5 mg immediate-release (IR) daily (n = 307) at least 30 min before breakfast, or risedronate 35 mg DR weekly, either immediately following breakfast (FB, n = 307) or at least 30 min before breakfast (BB, n = 308). Bone mineral density (BMD), bone turnover markers (BTMs), fractures, adverse events, and bone histomorphometry were evaluated.ResultsA total of 248 subjects (80.8 %) in the IR daily group, 234 subjects (76.2 %) in the DR FB weekly group, and 240 subjects (77.9 %) in the DR BB weekly group completed the 2-year study. After 2 years of treatment, BMD increases at the lumbar spine and total hip with the weekly DR doses similar to or greater than that with the IR daily dose. Decreases in BTMs were similar or significantly lower in the DR groups. Bone histomorphometry results did not differ among the DR weekly and the IR daily formulations. The three regimens were similarly well tolerated.ConclusionsRisedronate 35 mg DR weekly is as effective and as well tolerated as risedronate 5 mg IR daily, and will allow subjects to take their weekly risedronate dose immediately after breakfast.

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“…Additionally, the study concluded that taking oral bisphosphonates with mineral water that contains high calcium and magnesium levels reduced the effect of the drug; therefore it is advisable to take it as soon as the patient wakes up and in a vertical position [97]. These authors previously described the effect of water in combination with taking alendronate [98].…”

Section: Metabolismmentioning

confidence: 99%

Osteonecrosis of the Jaws. Prevalence, Risk Factors and Role of Microbiota and Inflammation in a Population of Spain

Pérez‐Sayáns¹,

Vidal-Real²,

Suárez‐Peñaranda³

et al. 2017

Osteonecrosis

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Introduction: The purpose of this article is to determine the prevalence of ONJ in patients who have undergone intravenous bisphosphonate therapy, and relate the risk factors described (including Actinomices); indeed, to establish a protocol to reduce the risk of developing ONJ and to evaluate the evolution of the patient according to the sample's antibiogram. Results: The prevalence of ONJ was 12.9%. Most of the non-diabetic patients did not develop ONJ (92.3%) (p = 0.048). In regards to the periodontal state, 94.3% of patients without periodontal problems did not develop ONJ (p = 0.001). Almost 50% of the necrosis were unifocal and located on the mandible (p < 0.001). The number of affected patients and the aggressiveness of the disease increased significantly three years after starting treatment (p < 0.001). 87.5% of biopsies showed the presence of Actinomyces. The inflammatory response was very variable, ranging from absent to intense but it increased with age (p = 0.005). The combination of amoxicillin with clavulanic acid showed good sensitivity in the majority of patients (82.6%). Conclusions: As the etiology of ONJ remains unknown, it is essential to prioritize prevention while assessing the risk factors.

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Influence of Mineral Water on Absorption of Oral Alendronate in Rats

Cited by 6 publications

References 12 publications

Interaction between Bisphosphonates and Mineral Water: Study of Oral Risedronate Absorption in Rats

Interaction between Bisphosphonates and Mineral Water: Study of Oral Risedronate Absorption in Rats

Treatment of postmenopausal osteoporosis with delayed-release risedronate 35 mg weekly for 2 years

Osteonecrosis of the Jaws. Prevalence, Risk Factors and Role of Microbiota and Inflammation in a Population of Spain

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