- Preparation and Optimization of Fast-Disintegrating Tablet Containing Naratriptan Hydrochloride Using D-Optimal Mixture Design. [Journal Article]
- APAAPS PharmSciTech 2018 Jun 04
- Optimization of a lyophilized fast-disintegrating tablet (LFDT) formulation containing naratriptan hydrochloride, an antimigraine drug, was the foremost objective of the study, aiming in achieving fa...
Optimization of a lyophilized fast-disintegrating tablet (LFDT) formulation containing naratriptan hydrochloride, an antimigraine drug, was the foremost objective of the study, aiming in achieving fast headache pain relief. The Design-Expert® v10 software was used to generate formulations using D-optimal mixture design with four components: gelatin (X1), hydrolyzed gelatin (X2), glycine (X3), and mannitol (X4) of total solid material (TSM) w/w. The effect of the relative proportion of each component was determined on friability (Y1), hardness (Y2), and in vitro disintegration time (Y3), which was then applied for formulation optimization. In addition, their effect on tablet porosity was determined via scanning electron microscopy (SEM). Drug-excipient interaction was evaluated using differential scanning calorimetry (DSC). A comparative dissolution study against the conventional tablets was studied. Accelerated stability study was carried out in (Al/Al) and (Al/PVC) blister packs. An in vivo pharmacokinetic study was carried out to compare the optimized formulation and the conventional tablets. The optimized formulation's responses were 0.30%, 3.4 kg, and 6.12 s for Y1, Y2, and Y3, respectively. No drug-excipient interaction was specified via DSC. The optimized formulation exhibited porous structure as determined via SEM. Dissolution study demonstrated complete dissolution within 1.5 min. Study indicated stability for 78 months in (Al/Al) blister packs. In vivo pharmacokinetic study demonstrated that Cmax, AUClast, and AUCinf were significantly higher for the developed formulation. As well, the Tmax was 1 h earlier than that of convenient tablet. An LFDT would achieve a faster onset of action for naratriptan compared to other formulations.
- Efficacy and Safety of 5HT1B/D Reseptoragonists, Triptans, for the Treatment of Migraine Disorders [BOOK]
- BOOKKnowledge Centre for the Health Services at The Norwegian Institute of Public Health (NIPH): Oslo, Norway
- BackgroundThe Norwegian Knowledge Centre for the Health Service (NOKC) was requested by the Norwegian Medicines Agency to do a health technology assessment (HTA) on the efficacy and safety of 5HT1B/D...
BackgroundThe Norwegian Knowledge Centre for the Health Service (NOKC) was requested by the Norwegian Medicines Agency to do a health technology assessment (HTA) on the efficacy and safety of 5HT1B/D receptor agonists, triptans, for the treatment of migraine disorders. Migraine has a one-year prevalence of 16–18% in women and 6–9% in men in Europe. A migraine attack usually lasts between 4 and 72 hours and recurrent attacks can affect daily functioning and quality of life. Triptans, selective 5HT1B/D receptor agonists, are today the main treatment option for migraine sufferers. There are seven different triptans available in Norway and these are used in the treatment of single migraine attacks in patients aged between 18 and 65 years. Objective This report is a systematic review of randomised, controlled head-to-head trials of various triptans to document comparative effectiveness and safety in adult patients with migraine. Methods Systematic searches were performed after published systematic reviews and randomised controlled trials in international databases. The literature was evaluated in a stepwise manner according to general principles of HTA. Studies that fulfilled our predetermined inclusion criteria were assessed and summarized. The work was reviewed by two independent external professionals. Results Sixteen randomised, controlled head-to-head trials were identified and met the inclusion criteria. The majority of the head-to-head trials involved and oral sumatriptan comparator. Our main findings are summarized below:Rizatriptan 10 mg is superior to sumatriptan 100 mg, naratriptan 2.5 mg and zolmitriptan 2.5 mg for the outcome 2-hour painfree. There is no significant difference between rizatriptan 10 mg, naratriptan 2.5 mg and zolmitriptan 2.5 mg for the outcome 24 hours sustained relief. The available head-to-head trials do not examine rizatriptan 10 mg and sumatriptan 100 mg for the outcome 24 hour sustained relief. Therefore, evidence is insufficient to judge the overall balance of advantages and disadvantages of this comparison. Head-to-head trials of various triptans with short follow-up period (24 hours) did not show significant differences in the reported adverse events frequencies. Comments We conclude that only small differences in efficacy can be documented between the various triptans in this systematic review. Rizatriptan 10 mg is superior to the other triptans for the outcome 2-hour painfree and have comparable effect for the outcome 24 hour sustained relief. Triptans are generally equally safe and well tolerated in the treatment of migraine patients. Future head-to-head trials should include more comparisons among triptans other than sumatriptan and should use currently recommended doses.
- Evaluation of electrochemical, UV/VIS and Raman spectroelectrochemical detection of Naratriptan with screen-printed electrodes. [Journal Article]
- TTalanta 2018 Feb 01; 178:85-88
- Naratriptan, active pharmaceutical ingredient with antimigraine activity was electrochemically detected in untreated screen-printed carbon electrodes (SPCEs). Cyclic voltammetry and differential puls...
Naratriptan, active pharmaceutical ingredient with antimigraine activity was electrochemically detected in untreated screen-printed carbon electrodes (SPCEs). Cyclic voltammetry and differential pulse voltammetry were used to carry out quantitative analysis of this molecule (in a Britton-Robinson buffer solution at pH 3.0) through its irreversible oxidation (diffusion controlled) at a potential of +0.75V (vs. Ag pseudoreference electrode). Naratriptan oxidation product is an indole based dimer with a yellowish colour (maximum absorption at 320nm) so UV-VIS spectroelectrochemistry technique was used for the very first time as an in situ characterization and quantification technique for this molecule. A reflection configuration approach allowed its measurement over the untreated carbon based electrode. Finally, time resolved Raman Spectroelectrochemistry is used as a powerful technique to carry out qualitative and quantitative analysis of Naratriptan. Electrochemically treated silver screen-printed electrodes are shown as easy to use and cost-effective SERS substrates for the analysis of Naratriptan.
- Naratriptan May Become an Alternative Prophylactic Option for Patients with Cluster Headache. [Editorial]
- IMIntern Med 2017 10 01; 56(19):2547-2548
- Naratriptan in the Prophylactic Treatment of Cluster Headache. [Case Reports]
- IMIntern Med 2017 Oct 01; 56(19):2579-2582
- Objective Naratriptan has been reported to reduce the frequency of cluster headache. The purpose of this study was to determine whether naratriptan is effective as a prophylactic treatment for cluste...
Objective Naratriptan has been reported to reduce the frequency of cluster headache. The purpose of this study was to determine whether naratriptan is effective as a prophylactic treatment for cluster headache in Japan. Methods We retrospectively reviewed all 43 patients with cluster headache who received preventive treatment with naratriptan from April 2009 to April 2015. The International Classification of Headache Disorders, 3rd Edition (beta version) (ICHD-3 beta) was used to diagnose cluster headache. This study was conducted at 3 centers (Department of Neurology, Saitama Medical University; Saitama Neuropsychiatric Institute; Saitama Medical University International Medical Center). Patients were recruited from these specialized headache outpatient centers. Naratriptan was taken before the patient went to bed. Results The study population included 30 men (69.8%) and 13 women (30.2%). Twenty-two cases received other preventive treatments (51.2%), while 21 cases only received naratriptan (48.8%). Among the 43 cases, 37 patients (86.0%) achieved an improvement of cluster headache on naratriptan. Conclusion Naratriptan has been suggested as a preventive medicine for cluster headache because of the longer the biological half-life in comparison to other triptans. The internal use of naratriptan 2 hours before attacks appears to achieve a good response in patients with cluster headache.
- Variation in Prescription Drug Coverage for Triptans: Analysis of Insurance Formularies. [Journal Article]
- HHeadache 2017; 57(8):1243-1251
- CONCLUSIONS: There are substantial variations in coverage and quantity limits and a high degree of complexity in triptan coverage for both government and commercial plans.
- Preparation and Optimization of Fast Dissolving Film of Naratr iptan Hydrochloride. [Journal Article]
- RPRecent Pat Drug Deliv Formul 2017; 11(2):124-131
- Naratriptan is second-generation triptan class of antimigraine drug which selectively bind with 5-HT(1B/1D) receptor. It is widely used to treat the migraine attack due to its better tolerability and...
Naratriptan is second-generation triptan class of antimigraine drug which selectively bind with 5-HT(1B/1D) receptor. It is widely used to treat the migraine attack due to its better tolerability and lower recurrence rate as compared to other triptans. Despite of the applicability, Naratriptan also have several drawback like slow onset of action and fist pass metabolism which reduce its efficacy. In order to increase the efficacy of naratriptan fast dissolving film is prepared.
- Triptans and migraine: advances in use, administration, formulation, and development. [Review]
- EOExpert Opin Pharmacother 2017; 18(4):387-397
- Recent triptan development has focused on new administration methods and formulations, triptan combination therapies, treatment in menstrually related migraines, and novel serotonin receptor subtype ...
Recent triptan development has focused on new administration methods and formulations, triptan combination therapies, treatment in menstrually related migraines, and novel serotonin receptor subtype agonists (5HTf). Areas covered: Clinical triptan research related to migraine was reviewed, analyzing EMBASE and PUBMED data bases from 01/01/2011 to 06/29/2016, with a focus on clinical trials of class 1 or 2 level of evidence. There have been advances in drug combination therapies, as well as administration devices that aid in ease of use, increase efficacy, and decrease adverse reactions. Some new agents and devices have similar or less efficacy compared to previous generic triptan formulations. New agents have action at the 5HTf receptor subtype, and avoid vascular side effects of classic 5Ht1b/d agonists, however adverse reactions may limit their clinic use. Long half-life triptans, frovatriptan and naratriptan, do appear to have good benefit in menstral related migraine. Expert opinion: Recent advances in triptan development can offer some advantages to migraine therapy and patient preferences, but have a much higher cost compared to individual generic triptan agents. In the coming years, triptan advances with high efficacy, limiting ADRs and cost are welcomed, in this regard the 5HT1b/d triptans are already well established.
- Quantitative structure-retention relationship model for the determination of naratriptan hydrochloride and its impurities based on artificial neural networks coupled with genetic algorithm. [Journal Article]
- TTalanta 2017 Mar 01; 164:164-174
- Mathematical modeling of Quantitative Structure - Property Relationships met great interest in fields of in silico drug design and more recently, pharmaceutical analysis. In our approach we proposed ...
Mathematical modeling of Quantitative Structure - Property Relationships met great interest in fields of in silico drug design and more recently, pharmaceutical analysis. In our approach we proposed automated method of creation Quantitative Structure-Retention Relationship (QSRR) for analysis of triptans, selective serotonin 5-HT1 receptor agonists used for the treatment of acute headache. The method was created using hybrid machine learning approach, namely Genetic algorithm (GA) coupled with artificial neutral networks (ANN). Performance of proposed hybrid GA-ANN model was evaluated with predicting relative retention times of naratriptan hydrochloride impurities. Several ANN types were coupled with GA and tested: single-layer ANN (SL-ANN), double-layer ANN (D-ANN) and higher order architectures: pi-sigma ANN (PS-ANN) and sigma-pi-sigma ANN (SPS-ANN). Partial Least Squares (PLS) method was used as a reference. The separation of naratriptan hydrochloride and its related products (impurities and degradation products) was obtained by developing a gradient high-performance liquid chromatography method with diode-array detector (HPLC-DAD). Degradation products during acid-basic hydrolysis were identified with an electrospray ionization tandem mass spectrometry (Q-TOF-MS/MS) detector. Independent data for outer validation of QSRR model was obtained from the determination of related products of sumatriptan succinate via an HPLC-DAD method. Accuracy of QSRR was measured by inner-validation on naratriptan data and outer validation on sumatriptan succinate samples. The best performing model were PS-ANN and SPS-ANN with mean errors of 8% (Q2=0.87) and 15% (Q2=0.77) on an inner-validation data set, respectively. Validation on similar samples from an outer validation data set of sumatriptan succinate impurities gave mean errors of 18% (R2pred=0.64) and 17% (R2pred=0.63) for the PS-ANN and SPS-ANN models, respectively.
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- Triptan use in Australia 1997-2015: A pharmacoepidemiological study. [Journal Article]
- ANActa Neurol Scand 2017; 136(2):155-159
- CONCLUSIONS: The use of triptan derivatives in Australia per head of population for treating migraine attacks continued to increase over the 18-year period studied, with use of recently introduced derivatives more than substituting for decreased use of older triptans. This suggests that the available treatments of migraine attacks had achieved what were considered less than adequate therapeutic outcomes.