Nicorandil, a new vasodilator drug, in patients with essential hypertension

Leonetti, Gastone; Fruscio, M.; Gradnik, R.; Chianca, Roberto; Bolla, G.; P, Prandi; Zanchetti, Alberto

doi:10.1097/00004872-198900076-00142

Cited by 11 publications

(3 citation statements)

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“…1 Although nicorandil is one of the emerging molecules in the case of hypertension and angina, successful treatment means maintenance of blood pressure at a normal physiological level, for which a constant and uniform supply of drug is desired. 2,3 Nicorandil has a short half-life, and the usual oral dosage regimen is 5 to 40 mg taken 2 to 4 times a day. To reduce the frequency of administration and to improve patient compliance, a once-daily sustained-release formulation of nicorandil is desirable.…”

Section: Introductionmentioning

confidence: 99%

Once-daily sustained-release matrix tablets of nicorandil: Formulation and in vitro evaluation

2003

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The objective of the present study was to develop once-daily sustained-release matrix tablets of nicorandil, a novel potassium channel opener used in cardiovascular diseases. The tablets were prepared by the wet granulation method. Ethanolic solutions of ethylcellulose (EC), Eudragit RL-100, Eudragit RS-100, and polyvinylpyrrolidone were used as granulating agents along with hydrophilic matrix materials like hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose, and sodium alginate. The granules were evaluated for angle of repose, bulk density, compressibility index, total porosity, and drug content. The tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, and in vitro release studies. The granules showed satisfactory flow properties, compressibility, and drug content. All the tablet formulations showed acceptable pharmacotechnical properties and complied with in-house specifications for tested parameters. According to the theoretical release profile calculation, a once-daily sustained-release formulation should release 5.92 mg of nicorandil in 1 hour, like conventional tablets, and 3.21 mg per hour up to 24 hours. The results of dissolution studies indicated that formulation F-I (drug-to-HPMC, 1:4; ethanol as granulating agent) could extend the drug release up to 24 hours. In the further formulation development process, F-IX (drug-to-HPMC, 1:4; EC 4% wt/vol as granulating agent), the most successful formulation of the study, exhibited satisfactory drug release in the initial hours, and the total release pattern was very close to the theoretical release profile. All the formulations (except F-IX) exhibited diffusion-dominated drug release. The mechanism of drug release from F-IX was diffusion coupled with erosion.

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Section: Introductionmentioning

confidence: 99%

Once-daily sustained-release matrix tablets of nicorandil: Formulation and in vitro evaluation

2003

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“…65141-46-0, molecular weight 211.17 g·mol –1 , chemical name: N -(2-hydroxyethyl)nicotinamide nitrate ester, structural formula shown in Figure S1 of the Supporting Information) is a well-known antianginal agent belonging to the class of aromatic heteromonocyclic compounds. It is a nicotinamide containing a pyridine ring substituted at the 3-position by a carboxamide group originally developed by Chugi company in Japan. − Faced with the increasing incidence rate of cardiovascular disease (CVD) year by year, nicorandil is a widely used vasodilatory drug used to treat angina and myocardial infarction symptoms, that is, chest pain resulting from episodes of transient myocardial ischemia, and shows great equivalent to that of classic antianginal agents. Nicorandil has also been applied clinically in various CVDs such as variant or unstable angina and reperfusion-induced damage following coronary angioplasty or thrombolysis. , Subsequently, in humans, the nitrate action of nicorandil dilates the large coronary arteries at low plasma concentrations, which also has satisfactory, safe, and cardioprotective effect in reducing the attack of coronary disease and protecting the heart.…”

Section: Introductionmentioning

confidence: 99%

Solubility Determination and Mathematical Modeling of Nicorandil in Several Aqueous Cosolvent Systems at Temperature Ranges of 278.15–323.15 K

Zhang

Huang

2020

J. Chem. Eng. Data

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In the liquid dispersion structure, pure methanol, ethanol, isopropanol, and N,N-dimethyl formamide (DMF) play a major role in dissolution and then water was added in sequence for dilution to obtain a dispersion system with different composition structures, and the concentration gradient between each mixed liquid was 0.1 (mass fraction). The drug nicorandil whose solubility was to be tested is added to it, using the isothermal method, with a high temperature of 323.15 K as the starting point and an interval of 5 K to a low temperature of 278.15 K. The pressure conditions did not require special requirements in an ordinary atmospheric pressure environment (101.1 kPa). Results show that when the temperature approaches the high level, more drugs can be dissolved in the same amount of solvent. Conversely, when the temperature was close to the low level, the drug is more difficult to dissolve. If the temperature was constant and the proportion of the organic solvent was large, the dissolving capacity of the dispersion system will develop in a positive direction. Conversely, if the proportion of water was large, the dissolving power will decrease. Nicorandil crystals accepted the determination of various dissolution data including undissolved raw materials have undergone X-ray power diffraction detection. The results obtained were gratifying, and no change in the crystal structure of the substance was found. Three modelsJouyban−Acree model, Van't Hoff−Jouyban−Acree model, and modified Apelblat−Jouyban−Acree modelwere employed to calculate the experimental nicorandil solubility, and relative average deviation and root-mean-square deviation were no higher than 0.88 and 1.69 × 10 −4 , respectively. The research on nicorandil is not only a simple measurement of the dissolution data but also more important is that with the support of these data, more thermodynamic data can be calculated to study nicorandil, which is for the improvement of the production process of nicorandil and the synthesis of pharmaceutical preparations is an indispensable link.

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“…The first therapeutic drug shown to possess an ability to hyperpolarize smooth muscle cell membranes is nicorandil, a potent coronary vasodilator [1]. Although nicorandil is one of the emerging molecule in the case of hypertension and angina [2,3], successful treatment means maintenance of blood pressure at a normal physiological level, for which a constant and uniform supply of drug is necessary [4]. Nicorandil has low oral bioavailability (70 %) and a short half-life just 1 hr, so the usual oral dosage regimen is 5 to 40 mg used 2 to 4 times a day.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Microsponge Based Nicorandil Sustained Released Tablet

Patel

2017

J. Sci. Res.

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The aim of the present work was to develop once-daily sustained release microsponges formulations of Nicorandil, a potent potassium channel opener used in cardiovascular diseases and it has low oral bioavailability (70%) and half-life 1 h. So, it is good candidate for sustained release formulations based on microsponge technology. The microsponges were prepared by using quasi-emulsion solvent diffusion method. Scanning Electron Microscopy (SEM) revealed that the microsponges of nicorandil with Eudragit -RSPO and HPMC K100M were smooth, porous, glossy and discrete spherical. The actual drug content and encapsulation efficiency of batch M1 to M9 were obtained in range of 62.05 ± 0.31 to 80.69 ± 0.43 and 64.41 ± 1.71 to 70.58 ± 1.12, respectively. The microsponges formulations were subjected to in-vitro release studies and the results were evaluated kinetically and statically. The best fitted model was found to be Korsmeyer -Peppas model (R 2 = 0.9992) for M6 batch. The 'n' value for Korsmeyer -Peppas model was between 0.5 and 1.0 which is indicative of non-Fickian diffusion. Statistical analysis using ANOVA yielded a p value of 0.572 for all the formulations, indicating that there was no significant difference among them.

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Nicorandil, a new vasodilator drug, in patients with essential hypertension

Cited by 11 publications

References 0 publications

Once-daily sustained-release matrix tablets of nicorandil: Formulation and in vitro evaluation

Once-daily sustained-release matrix tablets of nicorandil: Formulation and in vitro evaluation

Solubility Determination and Mathematical Modeling of Nicorandil in Several Aqueous Cosolvent Systems at Temperature Ranges of 278.15–323.15 K

Formulation and Evaluation of Microsponge Based Nicorandil Sustained Released Tablet

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