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Allopathic Medicines
Published in Varma H. Rambaran, Nalini K. Singh, Alternative Medicines for Diabetes Management, 2023
Varma H. Rambaran, Nalini K. Singh
It was found that the duration of binding showed good correlation with relatively similar efficacy. In 2012, Kawamori et al. conducted a 16-week clinical trial aimed at investigating the relative efficacy and safety of repaglinide and nateglinide on 130 Japanese patients with T2DM and glycated haemoglobin (HbA1c). During the 16-week study period, the patients were treated with repaglinide (0.5 mg) and nateglinide (90 mg) three times a day together with diet and exercise. At the end of the study, the group reported that repaglinide monotherapy had given greater glycaemic improvement than nateglinide monotherapy, by more efficiently reducing both HbA1c and fasting plasma glucose (PG) values (Kawamori, Kaku et al. 2012).
Diabetes mellitus and cardiovascular disease in the elderly
Published in Wilbert S. Aronow, Jerome L. Fleg, Michael W. Rich, Tresch and Aronow’s Cardiovascular Disease in the Elderly, 2019
Using surrogate markers, meglitinides have shown promise as a class of agents that may have beneficial effects on cardiovascular risk factors. A study comparing the effects of repaglinide (a meglitinide) versus glimepiride on cardiovascular risk factors after a test meal showed repaglinide to be more efficient than the sulfonylurea in lowering plasma free fatty acids, fibrinogen, thrombin–antithrombin complex, and plasminogen activator 1 levels (135). However, when studied in a large cardiovascular outcomes trial, meglitinides did not show benefit in an at risk population with impaired glucose tolerance. The Nateglinide and Valsartan in Impaired Glucose Tolerance Outcomes Research (NAVIGATOR) trial included 9306 patients with impaired glucose tolerance and cardiovascular disease or risk factors. Participants received nateglinide versus placebo and valsartan versus placebo in a 2 × 2 factorial design. They were followed for a median of 5 years with primary endpoints of incident diabetes, core cardiovascular outcome (death from cardiovascular cause, nonfatal MI, nonfatal stroke, or hospitalization for HF) and an extended cardiovascular outcome (composite of core outcome components plus hospitalization for unstable angina or arterial revascularization). Compared to placebo, nateglinide did not reduce the incidence of diabetes or the composite cardiovascular outcomes (136).
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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Antidiabetics: may improve glucose tolerance and have an additive effect with insulin or sulphonylureas; possibly enhanced effect with nateglinide; increased risk of severe hypoglycaemia with repaglinide – avoid.
Careful use to minimize adverse events of oral antidiabetic medications in the elderly
Published in Expert Opinion on Pharmacotherapy, 2021
Two RCTs, one as initial monotherapy versus placebo and the other as add-on to metformin versus glibenclamide reported that nateglinide is well tolerated and produces clinically meaningful improvements in glycemic control in elderly patients with T2DM aged ≥65 years, with a lower risk of hypoglycemic episodes compared with glibenclamide (glyburide) [55]. Retrospective subgroup analyses performed on pooled data from all nateglinide studies showed that nateglinide was effective while being well tolerated in subgroups of patients over age 64 years and old patients with renal impairment (estimated creatinine clearance <60 ml/min per 1.73 m2). The conclusion was that in subgroups in which metformin and long-acting SUs must be used with caution, nateglinide may be considered as an alternative as it has a low risk of adverse events and hypoglycemia [56]. An open-labeled 12-week, parallel study confirmed that nateglinide was effective and well tolerated in elderly patients up to 84 years with T2D [57].
Co-processing of nateglinide with meglumine for enhanced dissolution rate: in vitro and in vivo evaluation
Published in Drug Development and Industrial Pharmacy, 2020
Alaa Y. Bazeed, Ebtessam A. Essa, Ahmed Nouh, Gamal M. El Maghraby
Nateglinide is orally active drug for management of type II diabetes mellitus. It does not belong to the sulfonylurea group. Nateglinide is weakly acidic lipophilic compound (pKa of 3.1 and log P value is 4.2) [1,2]. The acidic nature of the drug resulted in a pH dependent dissolution with degree of ionization increasing as we move toward the distal parts of the gastrointestinal tract (GIT). This provides narrow absorption for nateglinide and better absorption is expected from the upper part of the GIT. In addition to the passive absorption process, nateglinide can be transported through a H + driven carriers which is site specific [3,4]. These restrictions are responsible for low and variable oral bioavailability. Fast dissolution can provide greater chance for passive absorption from the upper part of the GIT. Many techniques have been tried to improve the dissolution of poorly soluble drugs such as solid dispersion, formation of inclusion complex, nanosizing, among others [5–9]. Modification of crystalline structure is another promising alternative. This strategy has been adopted for enhancing the dissolution rate of nateglinide with promising data being recorded. For example, co-amorphization was used to prepare a mixture of nateglinide with metformin which liberate nateglinide at faster rate compared to the unprocessed drug [10]. In a more recent study, nateglinide was co-crystallized with sucralose and the developed co-crystals exhibiting faster dissolution of nateglinide [11].
Effect of semicrystalline polymers on self-emulsifying solid dispersions of nateglinide: in vitro and in vivo evaluation
Published in Drug Development and Industrial Pharmacy, 2018
Ranjit Prasad Swain, Bharat Bhusan Subudhi
Low aqueous solubility is often a limiting factor for the bioavailability of poorly soluble and high permeable drugs (class II of the Biopharmaceutical Classification System, BCS). So, there is great interest among the formulation scientists to improve their in vitro dissolution rate in order to enhance in vivo bioavailability [1,2]. Nateglinide is an oral antidiabetic agent, classified as BCS class II drug [3,4]. Its poor aqueous solubility is a major hurdle in its bioavailability and therapeutic application [5]. Accordingly, efforts have been made to improve its solubility in recent years. Techniques including nanotechnology [5,6], co-mixing [5], co-milling [7], complexation with β-cyclodextrin, hydroxypropyl-β-cyclodextrin [8,9], co-crystallization [10], and liquisolid compacts [11] have been studied with varying degree of success. Amongst these approaches, nanotechnology has shown promise. However, it has failed to provide the ideal solution. While it needed high energy for long times for size reduction in nanotechnology, it could not provide significant improvement in the solvation rate of nateglinide [5]. Besides, issues related to wettability, aggregation after preparation and recrystallization remain to be addressed by these approaches. In this scenario, it is necessary to evaluate other approaches to improve solubility and bioavailability of nateglinide.