21 research outputs found

    Formulation and evaluation of diclofenac potassium fast-disintegrating tablets and their clinical application in migraine patients

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    The aim of this study was to prepare fast-disintegrating tablets (FDTs) of diclofenac potassium with sufficient integrity as well as a pleasant taste, using two different fillers and binders: Tablettose 70 (R) and Di-Pac (R). Tablets were made with direct compression method. Tablet properties such as porosity, hardness, and disintegration time were determined. Diclofenac potassium determinations were carried out using a validated spectrophotometric method for the analysis of drug. Furthermore, in vivo experiments were carried out to compare the analgesic effect and the time to relieve migraine headache between the commercial tablets and FDTs of diclofenac potassium against placebo. Results showed that FDTs of diclofenac potassium with durable structure and desirable taste can be prepared using both fillers and binders but tablets prepared with Di-Pac had a better taste so the tablet formulation containing Di-Pac was chosen for in vivo experiments. Placebo controlled in vivo trial demonstrated that 50 mg diclofenac potassium, administered as a single dose of FDTs or commercial tablets, was effective in relieving the pain and both of them were superior to placebo

    Process and formulation variables of pregabalin microspheres prepared by w/o/o double emulsion solvent diffusion method and their clinical application by animal modeling studies

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    Pregabalin is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults. In conventional therapy recommended dose for pregabalin is 75mg twice daily or 50mg three times a day, with maximum dosage of 600 mg/d. To achieve maximum therapeutic effect with a low risk of adverse effects and to reduce often drug dosing, modified release preparations; such as microspheres might be helpful. However, most of the microencapsulation techniques have been used for lipophilic drugs, since hydrophilic drugs like pregabalin, showed low-loading efficiency and rapid dissolution of compounds into the aqueous continous phase. The purpose of this study was to improve loading efficiency of a water-soluble drug and modulate release profiles, and to test the efficiency of the prepared microspheres with the help of animal modeling studies. Pregabalin is a water soluble drug, and it was encapsulated within anionic acrylic resin (Eudragit S 100) microspheres by water in oil in oil (w/o/o) double emulsion solvent diffusion method. Dichloromethane and corn oil were chosen primary and secondary oil phases, respectively. The presence of internal water phase was necessary to form stable emulsion droplets and it accelerated the hardening of microspheres. Tween 80 and Span 80 were used as surfactants to stabilize the water and corn oil phases, respectively. The optimum concentration of Tween 80 was 0.25% (v/v) and Span 80 was 0.02% (v/v). The volume of the continous phase was affected the size of the microspheres. As the volume of the continous phase increased, the size of microspheres decreased. All microsphere formulations were evaluated with the help of in vitro characterization parameters. Microsphere formulations (P1-P5) exhibited entrapment efficiency ranged between 57.00 +/- 0.72 and 69.70 +/- 0.49%; yield ranged between 80.95 +/- 1.21 and 93.05 +/- 1.42%; and mean particle size were between 136.09 +/- 2.57 and 279.09 +/- 1.97 mm. Pregabalin microspheres having better results among all formulations (Table 3) were chosen for further studies such as differential scanning calorimetry, Fourier transform infrared analysis and dissolution studies. In the last step, the best pregabalin microsphere formulation (P3) was chosen for in vivo animal studies. The pregabalin-loaded microspheres (P3) and conventional pregabalin capsules were applied orally in rats for three days, resulted in clinical improvement of cold allodynia, an indicator of peripheral neuropathy. This result when evaluated together with the serum pregabalin levels and in vitro release studies suggests that the pregabalin microspheres prepared with w/o/o double emulsion solvent diffusion method can be an alternative form for neuropathic pain therapy. Conclusively, a drug delivery system successfully developed that showed modified release up to 10 h and could be potentially useful to overcome the frequent dosing problems associated with pregabalin conventional dosage form

    Investigation of changes in the sympathetic skin response to levodopa therapy in patients with Parkinson’s disease = A levodopaterápiára adott szimpatikus bőrreakció változásának vizsgálata Parkinson-kóros betegeknél

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    Background and purpose – We sought to evaluate the acute and dynamic alterations in the sympathetic skin response (SSR) in patients with Parkinson’s disease (PD) in response to levodopa therapy.Methods – We studied patients who were diagnosed with PD in our movement disorders clinic between January 2023 and May 2023. In addition to demographic and clinical features, the levodopa equivalent dose, nonmotor symptoms scale score, and Movement Disorders Society-Unified Parkinson’s Disease Rating Scale score were evaluated. SSRs were studied during the medication-ON and medication-OFF periods by a trained neurophysiologist.Results – Overall, 22 patients with PD were enrolled in the study. The mean age of the patients was 59 ± 8.1 y. The correlation analyses between the clinical features and SSR parameters revealed only a moderate positive correlation between age and the latency of the SSR (left side). Repeated analysis of covariance revealed that the latencies of the SSR were shortened bilaterally in the medication-ON group (right, p=0.012; left, p=0.012).Conclusion – We found electrophysiological evidence regarding the corrective effect of levodopa on autonomic dysfunction (AD) in PD patients. An investigation of the possible levodopa response of the clinical features related to AD might contribute to the unknown pathomechanisms of AD in PD patients. | Bevezetés – Célunk az volt, hogy értékeljük Parkinson-kórban (Parkinson’s disease, PD) szenvedő betegek szimpatikus bőrreakciójának (SSR) levodopaterápia hatására bekövetkező akut és dinamikus változásait. Módszerek – Olyan betegeket vizsgáltunk, akiket mozgászavar-klinikánkon 2023 januárja és 2023 májusa között PD-vel diagnosztizáltak. A demográfiai és klinikai jellemzők mellett a levodopaekvivalens dózist, a nem motoros tünetskálája pontszámait és a Mozgászavarok Társaságának Egységes Parkinson-kór Értékelő Skálájának pontszámait is értékeltük. Az SSR-t képzett neurofiziológus vizsgálta a gyógyszeres kezelés on és off periódusaiban. Eredmények – Összesen 22 PD-s beteg vett részt a vizsgálatban. A betegek átlagéletkora 59 ± 8,1 év volt. A klinikai jellemzők és az SSR-paraméterek közötti korrelációelemzés csak mérsékelt pozitív korrelációt mutatott az életkor és az SSR latenciája (bal oldal) között. Az ismételt kovarianciaelemzés kimutatta, hogy az SSR latenciája mindkét oldalon rövidült a gyógyszeres kezelés alatt álló csoportban (jobb oldal p = 0,012; bal oldal p = 0,012). Következtetés – Elektrofiziológiai bizonyítékot találtunk a levodopakezelés autonóm diszfunkcióra (AD) gyakorolt korrekciós hatására PD-betegeknél. Az AD-vel kapcsolatos klinikai tünetek levodopakezelésre adott lehetséges válaszának vizsgálata hozzájárulhat a PD-betegeknél előforduló AD ismeretlen patomechanizmusainak feltárásához

    Vestibular-evoked myogenic potentials, clinical evaluation, and imaging findings in multiple sclerosis

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    Vestibular-evoked myogenic potentials (VEMP), short-latency electromyographic responses elicited by acoustic stimuli, evaluate the function of vestibulocollic reflex and may give information about brainstem function. The aim of the present study is to evaluate the potential contribution of VEMP to the diagnosis of multiple sclerosis (MS). Fifty patients with MS and 30 healthy control subjects were included in this study. The frequency of VEMP p1-n1 and n2-p2 waves; mean p1, n1, n2, and p2 latency; and mean p1-n1 and n2-p2 amplitude were determined. The relation between clinical and imaging findings and VEMP parameters was evaluated. The p1-n1 and n2-p2 waves were more frequently absent in MS than in control subjects [p1-n1 wave absent: MS, 25 (25 %) ears; control, 6 (10 %) ears; P a parts per thousand currency sign 0.02] [n2-p2 wave absent: MS, 44 (44 %) ears; control, 7 (12 %) ears; P a parts per thousand currency sign 0.001]. The mean p1-n1 amplitude was lower in MS than in control subjects (MS, 19.1 +/- A 7.2 mu V; control, 23.3 +/- A 7.4 mu V; P a parts per thousand currency sign 0.002). A total of 24/50 (48 %) MS patients had VEMP abnormalities (absent responses and/or prolonged latencies). VEMP abnormalities were more frequent in patients with than without vestibular symptoms (P a parts per thousand currency sign 0.02) and with brainstem functional system score (FSS) a parts per thousand yen1 than FSS = 0 (P a parts per thousand currency sign 0.02). In patients with MS, absence of p1-n1 wave was more frequent in patients with than without vestibular symptoms [absence of p1-n1 wave: vestibular symptoms, 9 (45 %) ears; no vestibular symptoms, 16 (20 %) ears; P a parts per thousand currency sign 0.03] and patients with Expanded Disability Status Scale (EDSS) score a parts per thousand yen5.5 [absence of p1-n1 wave: EDSS a parts per thousand yen5.5, 7 (70 %) ears; EDSS < 5.5, 18 (20 %) ears; P a parts per thousand currency sign 0.001]. Abnormal VEMP may be noted in MS patients, especially those with vestibular symptoms and greater disability. The VEMP test may complement other studies for diagnosis and follow-up of patients with MS
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