Background: Frequent administration caused by short half-life and low bioavailability due to poor solubility and low dissolution rate limit the further application of poorly water-soluble nimodipine, although several new indications have been developed. To overcome these shortcomings, sophisticated technologies had to be used since the dose of nimodipine was not too low and the addition of solubilizers could not resolve the problem of poor release.
Objective: The purpose of this study was to obtain sustained and complete release of nimodipine with a simple and easily industrialized technology.
Methods: The expandable monolithic osmotic pump tablets containing nimodipine combined with poloxamer 188 and carboxymethylcellulose sodium were prepared. The factors affecting drug release including the amount of solubilizing agent, expanding agent, retarding agent in core tablet and porogenic agent in semipermeable film were optimized. The release behavior was investigated both in vitro and in beagle dogs.
Results: It was proved that the anticipant release of nimodipine could be realized in vitro. The sustained and complete release of nimodipine was also realized in beagles because the mean residence time of nimodipine from the osmotic pump system was longer and Cmax was lower than those from the sustained-release tablets in market while there was no difference in AUC(0-t) of the monolithic osmotic pump tablets and the sustained release tablets in market.
Conclusion: It was reasonable to believe that the sustained and complete release of poorly watersoluble nimodipine could be realized by using simple expandable monolithic osmotic pump technology combined with surfactant.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2174/1567201814666161109122840 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Introduction: Neurotrophic factors are widely known for their protective effect on spiral ganglion neurons (SGN) and the protection of these neurons is of great importance to optimize Cochlear Implants, which directly stimulate SGN in deaf patients. Previous studies have identified Cometin - also known as Meteroin-like - to be neuroprotective and beneficial for metabolic disorders. The aim of our study was to investigate the effects of different concentrations of recombinant human Cometin (hCometin) on SGN in regard to neuroprotection and neurite outgrowth and to evaluate its neurite guidance potential using a neurite outgrowth chamber.
View Article and Find Full Text PDFThe class-IIa HDAC inhibitor TMP269 promotes BMP-Smad signalling and is neuroprotective in in vitro and in vivo 6-hydroxydopamine models of Parkinson's disease.
Neuropharmacology
January 2025
Department of Anatomy & Neuroscience, School of Medicine, University College Cork (UCC), Cork, Ireland; APC Microbiome Ireland, UCC, Cork, Ireland. Electronic address:
Degeneration of midbrain nigrostriatal dopaminergic neurons is a pathological hallmark of Parkinson's disease (PD). Peripheral delivery of a compound(s) to arrest or slow this dopaminergic degeneration is a key therapeutic goal. Pan-inhibitors of histone deacetylase (HDAC) enzymes, key epigenetic regulators, have shown therapeutic promise in PD models.
View Article and Find Full Text PDFPerinatal exposure to methadone or buprenorphine impairs hippocampal-dependent cognition and brain development in juvenile rats.
Prog Neuropsychopharmacol Biol Psychiatry
January 2025
School of Psychology, University of New South Wales, Sydney, Australia. Electronic address:
The opioid crisis continues to escalate, disproportionately affecting women of reproductive age. Traditionally the first line of treatment for pregnant women with opioid use disorder is the mu-opioid receptor agonist methadone. However, in recent years, the use of buprenorphine as a replacement therapy has increased as it has fewer side-effects and longer duration of action.
View Article and Find Full Text PDFProline enhances the hepatic induction of lipogenic gene expression in male hepatic fasn reporter mice.
Biochem Biophys Res Commun
February 2025
Department of Physiology and Metabolism, Graduate School of Medical Sciences, Kanazawa University, 13-1 Takaramachi, 920-8640, Kanazawa, Ishikawa, Japan; Metabolism and Nutrition Research Unit, Institute for Frontier Science Initiative, Kanazawa University, 13-1 Takaramachi, 920-8640, Kanazawa, Ishikawa, Japan. Electronic address:
Hepatic de novo lipogenesis (DNL) is increased by both carbohydrate intake and protein consumption. In hepatic fat synthesis, a key role is played by the induction of the hepatic expression of lipogenic genes, including Fasn, Scd1, and Srebf1. Regarding carbohydrate intake, increased blood glucose and insulin levels promote the expression of hepatic lipogenic genes.
View Article and Find Full Text PDFThe Melatonin Type 2 Receptor Agonist IIK7 Attenuates and Reverses Morphine Tolerance in Neuropathic Pain Rats Through the Suppression of Neuroinflammation in the Spinal Cord.
Pharmaceuticals (Basel)
December 2024
Department of Anesthesiology, Cathay General Hospital, Taipei 106, Taiwan.
Background: Morphine analgesic tolerance (MAT) limits the clinical application of morphine in the management of chronic pain. IIK7 is a melatonin type 2 (MT2) receptor agonist known to have antioxidant properties. Oxidative stress is recognized as a critical factor in MAT.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!