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1.
North Clin Istanb ; 10(1): 122-126, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36910437

RESUMO

The work aimed to explore the clinical hypothesis on the possible alternative to Opiorphin and its stable analogues for treating fibromyalgia pain. Fibromyalgia is a condition characterized by chronic pain triggered by an interplay of biological and psychosocial variables, although the exact pathogenesis is still controversial. Standard therapy for low threshold tender point pain includes NSAIDs and opioid analgesics, both of which have serious adverse profiles after long-term exposure, highlighting the need for an intermediate compound capable of bridging the gap between NSAIDs and opioid analgesics. Opiorphin is an anti-nociceptive modulator which inhibits the enzyme responsible for the degradation of natural endogenous opioid neuropeptides. This paper hypothesizes and concludes that Opiorphin and its stable analogues (Sialorphine, STR-324) can be an alternative for the treatment of chronic long-standing low-threshold tender point pain associated with fibromyalgia.

2.
Pak J Pharm Sci ; 34(2): 607-613, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34275836

RESUMO

The main intention of the current investigation was to fabricate ocular films of Dexamethasone sodium phosphate (DSP) impregnated in rate controlling membrane and to characterize in vitro and in vivo (iv-iv). DSP release was regulated by HPMC K4M and ethyl cellulose (EC) and dimethyl sulfoxide (DMSO) as a permeability enhancer. DSP suitability with polymers was observed by DSC and FT Infrared spectroscopic readings. The fabricated DSP ocular films were examined for physicochemical tests, in vitro discharge and in vivo infusion in rabbits. The improved formulation (F-8) was proved its stability under stressed storage conditions. The fabricated ocular films process acceptable physical characters with DSP release in a controlled manner. The optimized DSP films were intact even in stressed storage situations. It was concluded that the fabricated films effectively hold the DSP at the programmed site for the desired period of time and exhibit expected pharmacodynamics actions.


Assuntos
Conjuntivite/tratamento farmacológico , Dexametasona/análogos & derivados , Glucocorticoides/administração & dosagem , Administração Oftálmica , Animais , Celulose/análogos & derivados , Preparações de Ação Retardada , Dexametasona/administração & dosagem , Dimetil Sulfóxido , Portadores de Fármacos , Derivados da Hipromelose , Técnicas In Vitro , Permeabilidade , Coelhos
3.
Turk J Pharm Sci ; 17(4): 372-380, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32939132

RESUMO

OBJECTIVES: The aim of this study of this study was to discover the best poloxamer as a solid dispersion carrier for thiocolchicoside (TCS). MATERIALS AND METHODS: The compatibility of TCS with excipients was studied by differential scanning colorimetry and fourier transform infrared spectroscopy. Different formulations of solid dispersions (SDs) were made with poloxamer carriers, i.e. poloxamer-108, poloxamer-188, poloxamer-237, poloxamer-338, and poloxamer-407 were made by taking TCS:poloxamer in ratios of 1:1, 1:2, 1:4, and 1:6. The SDs were made by a novel microwave fusion method and compressed using an 8-station tablet compression machine. The fabricated SD tablets were characterized by physicochemical constraints and drug release rates. The release of TCS from the prepared SDs was later analyzed by kinetic models. RESULTS: TCS was observed to be compatible with the poloxamer carriers. The SD formulations showed satisfactory physicochemical constraints and TCS release following first-order release. CONCLUSION: Among the poloxamer carriers used, poloxamer-188 was the best for increasing the solubility and release rate of TCS from the SDs.

4.
Pak J Pharm Sci ; 29(3): 945-51, 2016 May.
Artigo em Inglês | MEDLINE | ID: mdl-27166538

RESUMO

The purpose of this investigation was to prepare matrix type transdermal patches of Tramadol HCl using various ratios of Ficus carica fruit mucilage and Povidone. The matrix type transdermal patches were prepared using Tramadol HCl with Ficus carica fruit mucilage and Povidone. The interactions between Tramadol HCl with F. carica fruit mucilage and Povidone were performed by Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared spectroscopy (FTIR). The prepared patches were examined for physicochemical characterization and in vitro drug permeation studies (using a Keshary-Chien diffusion cell across hairless Albino rat skin), skin irritation studies and accelerated stability studies. The drug was found to be free from negligible interactions with the polymers used. The formulated patches possessed satisfactory physicochemical properties, in vitro drug permeation and devoid of serious skin irritation. The selected formulation (F-5) was retains the characteristics even after the accelerated environmental conditions. The study concludes that F. carica fruit mucilage with Povidone is a good combination for preparing transdermal patches.


Assuntos
Adesivos/química , Analgésicos Opioides/administração & dosagem , Portadores de Fármacos , Ficus/química , Povidona/química , Tramadol/administração & dosagem , Adesivo Transdérmico , Adesivos/isolamento & purificação , Administração Cutânea , Analgésicos Opioides/química , Analgésicos Opioides/metabolismo , Animais , Varredura Diferencial de Calorimetria , Química Farmacêutica , Difusão , Estabilidade de Medicamentos , Frutas , Cinética , Microscopia Eletrônica de Varredura , Modelos Biológicos , Permeabilidade , Coelhos , Ratos , Ratos Pelados , Pele/metabolismo , Absorção Cutânea , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Tecnologia Farmacêutica/métodos , Tramadol/química , Tramadol/metabolismo
5.
Nat Prod Res ; 26(17): 1649-53, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22008064

RESUMO

Alangium salviifolium root was screened for phytochemical and anti-inflammatory properties. The percentage inhibition of carrageenan induced paw oedema was studied in rats. Alangium salvifolium gave maximum extractive values with Ethanol and the Loss on Drying value, total ash value and acid-insoluble ash and water soluble ash values were within limits. The extract gave positive tests for phytosterols, triterpenes, flavonoids, carbohydrates and alkaloids. The extract was free from glycosides, saponins, tannins, proteins and amino acids. In acute toxicity studies, Alangium salviifolium root extract was found to be safe up to 3000 mg kg⁻¹, p.o. in the albino rats. The Alangium salviifolium root gave significant per cent inhibition of the maximal paw oedema and very highly significant per cent inhibition of total paw oedema during 6 h. This study revealed that Alangium salviifolium root has good anti-inflammatory actions when compared with Diclofenac sodium.


Assuntos
Alangiaceae/química , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Raízes de Plantas/química , Animais , Diclofenaco/uso terapêutico , Edema/tratamento farmacológico , Ratos
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