ABSTRACT
Abstract Background and objectives: Tramadol hydrochloride is a centrally-acting synthetic opioid analgesic binding to specific opioid receptors. It is used in the management of chronic pain and is recommended as first line drug in the treatment of postoperative or orthopedic injury induced acute pain. The present work is designed to prepare and evaluate mucoadhesive buccal film of tramadol hydrochloride as a novel form of prolonged analgesia for patients with orthopedic injuries. Methods: Buccal films of tramadol hydrochloride were prepared by solvent casting method. The prepared films were evaluated for the various evaluation parameters like thickness, surface pH, weight uniformity, content uniformity, folding endurance, swelling index, in vitro drug release study, in vitro test for mucoadhesion and in vivo studies (primary mucosal irritancy test and analgesic activity). Results: All the formulations exhibited good results for physicochemical characterizations. In in vitro drug release study the films exhibited controlled release more than 12 hours. The formulation BFT2 (containing chitosan and PVP K-90) showed no irritant effect on buccal mucosa and elicit the significant in vivo analgesic activity with 57.14% analgesia against that of standard (61.04%). It was concluded that the mucoadhesive films of tramadol hydrochloride can be effectively used to alleviate the severe pain of orthopedic injuries with prompt onset and prolonged action.
Resumo Justificativa e objetivos: O cloridrato de tramadol é um analgésico opioide de ação central que se liga a receptores opioides específicos. É usado no tratamento de dor crônica e recomendado como fármaco de primeira linha para o tratamento no pós-operatório ou em dor aguda induzida por lesão ortopédica. O presente estudo visa a preparar e avaliar o filme bucal mucoadesivo de cloridrato de tramadol como uma nova forma de analgesia prolongada para pacientes com lesões ortopédicas. Método: Filmes bucais de cloridrato de tramadol foram preparados pelo método de evaporação de solvente. Os filmes preparados foram avaliados para os vários parâmetros de avaliação, como espessura, pH da superfície, uniformidade do peso, uniformidade do conteúdo, resistência a dobras, índice de intumescimento, estudo de liberação da droga in vitro, teste in vitro para mucoadesão e estudos in vivo (teste de irritação da mucosa primária e atividade analgésica). Resultados: Todas as formulações apresentaram bons resultados para caracterizações físico-químicas. Em estudo de libertação de droga in vitro, os filmes exibiram liberação controlada por mais de 12 horas. A formulação de BFT2 (com quitosana e PVP K-90) não mostrou efeito irritante sobre a mucosa bucal e provocou uma atividade analgésica significativa in vivo com 57,14% de analgesia versus a do padrão (61,04%). Concluiu-se que os filmes mucoadesivos de cloridrato de tramadol podem ser usados eficazmente para aliviar a dor intensa de lesões ortopédicas com início rápido e ação prolongada.
Subject(s)
Animals , Male , Rats , Tramadol/administration & dosage , Adhesives , Drug Delivery Systems , Pain Management/methods , Analgesics, Opioid/administration & dosage , Treatment Outcome , Rats, Wistar , Dosage Forms , Mouth MucosaABSTRACT
BACKGROUND AND OBJECTIVES: Tramadol hydrochloride is a centrally-acting synthetic opioid analgesic binding to specific opioid receptors. It is used in the management of chronic pain and is recommended as first line drug in the treatment of postoperative or orthopedic injury induced acute pain. The present work is designed to prepare and evaluate mucoadhesive buccal film of tramadol hydrochloride as a novel form of prolonged analgesia for patients with orthopedic injuries. METHODS: Buccal films of tramadol hydrochloride were prepared by solvent casting method. The prepared films were evaluated for the various evaluation parameters like thickness, surface pH, weight uniformity, content uniformity, folding endurance, swelling index, in vitro drug release study, in vitro test for mucoadhesion and in vivo studies (primary mucosal irritancy test and analgesic activity). RESULTS: All the formulations exhibited good results for physicochemical characterizations. In in vitro drug release study the films exhibited controlled release more than 12hours. The formulation BFT2 (containing chitosan and PVP K-90) showed no irritant effect on buccal mucosa and elicit the significant in vivo analgesic activity with 57.14% analgesia against that of standard (61.04%). It was concluded that the mucoadhesive films of tramadol hydrochloride can be effectively used to alleviate the severe pain of orthopedic injuries with prompt onset and prolonged action.
Subject(s)
Adhesives , Analgesics, Opioid/administration & dosage , Drug Delivery Systems , Pain Management/methods , Tramadol/administration & dosage , Animals , Dosage Forms , Male , Mouth Mucosa , Rats , Rats, Wistar , Treatment OutcomeABSTRACT
In order to explore the differences of chemical constituents of Paeoniae Radix Alba and Paeoniae Radix Rubra, a qualitative analytical method of liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (HPLC-Q-TOF-MS/MS) was developed for identification of multi-constituents and an HPLC-DAD analytical method was developed for simultaneously determining 14 major compounds (gallic acid, protocatechuic acid, paeoniflorin sulfonate, protocatechuic aldehyde, methyl gallate, oxypaeoniflorin, catechin, albiflorin, and paeoniflorin, ethyl gallate, benzoic acid, pentagaloylglucose, benzoyl-paeoniflorin, and paeonol) in Paeoniae Radix Alba and Paeoniae Radix Rubra. Q-TOF/MS qualitative analysis was performed under negative ion mode and inferred 38 components of Paeoniae Radix Alba and 30 components of Paeoniae Radix Rubra. HPLC-DAD quantitative method result showed the contents of 8 ingredients were different between Paeoniae Radix Alba and Paeoniae Radix Rubra. The results indicated that the new approach was applicable in qualitative and quantitative quality control of Paeoniae Radix Alba and Paeoniae Radix Rubra.
Subject(s)
Chromatography, High Pressure Liquid/methods , Drugs, Chinese Herbal/chemistry , Paeonia/chemistry , Tandem Mass Spectrometry/methods , Bridged-Ring Compounds/chemistry , Glucosides/chemistry , Molecular Structure , Monoterpenes/chemistry , Paeonia/classificationABSTRACT
Tunable all-optical plasmonic diode is proposed based on the Fano resonance in an asymmetric and nonlinear system, comprising metal-insulator-metal waveguides coupled with nanocavities. The spatial asymmetry of the system gives rise to the nonreciprocity of the field localizations at the nonlinear gap between the coupled cavities and to the nonreciprocal nonlinear response. Nonlinear Fano resonance, originating from the interference between the discrete cavity mode and the continuum traveling mode, is observed and effectively tuned by changing the input power. By combining the unidirectional nonlinear response with the steep dispersion of the Fano asymmetric line shape, a transmission contrast ratio up to 41.46 dB can be achieved between forward and backward transmission. Our all-optical plasmonic diode with compact structure can find important applications in integrated optical nanocircuits.
