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Antiemetic Drug (antiemetic + drug)
Selected AbstractsMucoadhesive microspheres for nasal administration of an antiemetic drug, metoclopramide: in-vitro/ex-vivo studiesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 3 2005Elisabetta Gavini Microparticulate delivery systems designed for the nasal administration of an antiemetic drug, metoclopramide hydrochloride, were prepared. Microspheres composed of sodium alginate, chitosan hydrochloride, or both, were obtained using a spray-drying method; some batches of drug-free microparticles were prepared as a comparison. The morphology, in-vitro swelling behaviour, mucoadhesive properties and drug release from microparticles were evaluated. Ex-vivo drug permeation tests were carried out using sheep nasal mucosa; permeation test of the drug solution was peformed as comparison. During ex-vivo permeation tests, transmission electron microscopy (TEM) analyses were carried out on the nasal mucosa to study the morphological changes of epithelial cells and tight junctions, while the change in microsphere morphology was examined using photostereo microscopy (PM). Spray-dried microparticles had a mean diameter (dvs) in the range of about 3,10 ,m. They showed good in-vitro mucoadhesive properties. In-vitro release profiles and swelling behaviour depended on their composition: the drug release occurred in 1,3 h. Ex-vivo studies showed that drug permeation through the mucosa from microparticles based on chitosan was higher than from those consisting of alginate alone. This can be related to the penetration enhancing properties of chitosan. Complexation of chitosan with alginate led to a control of the drug release. Microscopy observation of microspheres during the permeation tests revealed that microparticles swelled and gelled, maintaining their shape. TEM analyses of the mucosa after exposure to the microparticles consisting of alginate/chitosan showed opened tight junctions. This preliminary study shows that alginate/chitosan spray-dried microspheres have promising properties for use as mucoadhesive nasal carriers of an antiemetic drug. [source] The neurokinin-1 antagonist activity of maropitant, an antiemetic drug for dogs, in a gerbil modelJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 4 2007V. DE LA PUENTE-REDONDO Maropitant is a novel synthetic nonpeptide neurokinin type 1 (NK1) selective receptor antagonist, recently developed for use in the dog as an antiemetic. The in vivo functional activity of maropitant was investigated in the gerbil foot-tapping model, to determine the ability of maropitant to penetrate the central nervous system and inhibit foot-tapping induced by the selective NK1 agonist GR73632. In comparison with CP-122,721, a previously characterized NK1 receptor antagonist, maropitant (1 mg/kg by s.c. injection) was found to inhibit foot-tapping for significantly longer (P < 0.01). Inhibition of foot-tapping by maropitant was 100% at 2 h and approximately 50% at 8 h postdosing. The mean brain:plasma concentration ratio at 8 h post-treatment was 3.59. These data demonstrate the central functional action of maropitant as a selective and potent NK1 receptor antagonist and help to support and explain its clinical potential as a broad-spectrum antiemetic agent. [source] Granisetron, an antiemetic drug, and its cobalt complexACTA CRYSTALLOGRAPHICA SECTION C, Issue 2 2010Krishnan Ravikumar The crystal structures of granisetron [systematic name: 1-methyl- N -(9-methyl-9-azabicyclo[3.3.1]nonan-7-yl)indazole-3-carboxamide], C18H24N4O, (I), an antinauseant and antiemetic agent, and its CoII complex, diaqua[1-methyl- N -(9-methyl-9-azoniabicyclo[3.3.1]nonan-7-yl)indazole-3-carboxamide]cobalt(II) tetrachloride dodecahydrate, [Co(C18H25N4O)2(H2O)2]Cl4·12H2O, (II), have been determined by X-ray diffraction. The granisetron molecule is in an extended conformation in both structures. Twisting of the central carboxamide group facilitates the CoII coordination in (II). The CoII atom is located on an inversion centre. The azabicyclononane ring adopts a chair,boat conformation in both structures. The molecules in (I) are linked into centrosymmetric dimers and form tetracyclic rings through C,H...O hydrogen-bonding interactions. The simultaneous presence of free chloride ions in conjunction with a number of hydration water molecules in (II) provides interesting hydrogen-bond patterns. This study can aid in the investigation of the properties of metal complexes with active pharmaceuticals in which the drug molecules play the role of a ligand. [source] Electrical stimulation of the vestibular system prevents postoperative nausea and vomitingACTA ANAESTHESIOLOGICA SCANDINAVICA, Issue 9 2000F. Pusch Background: Electrical stimulation of the vestibular system may prevent nausea and vomiting. We studied the influence of transcutaneous impulse stimulation in prevention of postoperative nausea and vomiting (PONV) following gynaecological surgery. Methods: In this randomised study 70 women undergoing elective gynaecological surgery under general anaesthesia were assigned to receive either the activated (stimulation group) or the inactivated (non-stimulation group) impulse stimulator. The stimulator comprises the stimulator itself, two negative electrodes on a headset applied over both mastoid processes and a nuchal positive electrode. The device yielded a pulse frequency of 5 Hz direct current, individually adjustable between 0.5 and 4 mA. A trapezoid stimulation of 50 ms was applied. Nausea, vomiting, dizziness and the amount of antiemetic drugs used were assessed during the first 4 h postoperatively. Results: Lower postoperative nausea scores with a lower incidence of vomiting and postoperative dizziness were found in the stimulation group. A lower amount of antiemetic drugs was needed in the stimulation group when compared to the non-stimulation group (P<0.01 between groups). Conclusion: This study suggests that electrical stimulation of the vestibular system may be useful in prevention of PONV. [source] | ||||||||||