Pharmacological and toxicological investigations of etodolac loaded gum katira microspheres prepared by W1/O/W2 emulsion solvent evaporation technique in rats

ABSTRACT Etodolac is a non-steroidal anti-inflammatory drug (NSAID) and approved by USFDA as a COX2 inhibitor. Although etodolac therapy provides clinical benefits, it is associated with upper gastrointestinal (GI) tract complications also. Etodolac loaded gum Katira microsphere (ELGKM) was prepared by W1/O/W2 emulsion solvent evaporation technique. The gastric irritation properties of orally administered pure etodolac, ELGKM and blank microspheres (without etodolac) were evaluated in experimental rats treated for 6 days. The stomach examination and biochemical investigation of stomach tissue of treated rats indicated that ELGKM formulation remarkably reduced ulcerogenecity as compared to pure etodolac. The anti-inflammatory activities of pure etodolac and ELGKMs were ascertained by the implantation of cotton pellets in rats for 6 days. Based on the results, ELGKMs showed significant anti-inflammatory activities (P<0.01) as compared to control group. The cotton pellets test suggested that ELGKM formulation retained more anti-inflammatory properties among the groups. The hematological changes, biochemical analysis and histopathological studies of subacute toxicity in rats revealed that ELGKM were the effective sustained release formulation in the treatment of chronic pain and inflammation. In conclusion, the physicochemical characterization, pharmacological and toxicological studies suggest that ELGKMs may represent as a potential candidate for sustained drug delivery (10-12 hours) in chronic joint pain related diseases with remarkably diminished gastrointestinal side effects.

Knowledge and attitudes of low back pain in physicians based in clinical practice guidelines / Conhecimento e conduta em casos de lombalgia com base nas diretivas de prática clínica / Conocimientos y actitudes sobre lumbalgia de médicos basados en la guía práctica clínica

Objective: To determine the level of knowledge and attitudes of physicians in Tijuana based on Clinical Practice Guidelines (CPG) for the prevention, diagnosis and treatment of Nonspecific Low Back Pain (NLBP). Methods: Prospective, cross-sectional, descriptive study. Data were obtained from doctors who practice in clinics, private surgeries, and/or government institutions. Results: Of a total of 56 doctors surveyed, 37 were men and 19 women. None of the doctors said they had not seen a patient with Back Pain. 49% knew the GPC, and 51% did not know of its existence. Conclusions: Although some physicians reported knowledge of the GPC, according to the results, there was a lack of full knowledge of, and adherence to these guidelines. Not knowing the GPC did not make it impossible to complete the questionnaire. The doctors felt more connected to the health system, but with less confidence in the management of cases of NLBP.

Objetivo: Determinar o nível de conhecimentos e a conduta dos médicos de Tijuana, com base nas Diretivas de Prática Clínica (DPC) para prevenção, diagnóstico e tratamento da dor lombar não específica (DLNE). Métodos: Estudo prospectivo, transversal e descritivo. Os dados foram obtidos junto a médicos que prestam serviços em clínicas, consultórios particulares e/ou instituições governamentais. Resultados: Atingiu-se um total de 56 médicos entrevistados, dos quais 37 eram homens e 19 mulheres. Nenhum médico disse que não atende um paciente com dor lombar. Do total, 49% conhecem as DPC e 51% não sabiam da sua existência. Conclusões: Apesar de alguns médicos relatarem conhecer as DPC, de acordo com os resultados obtidos, falta-lhes maior domínio e conformidade com relação a essas diretivas. Não conhecer as DPC não impossibilita responder ao questionário. Os médicos sentem-se mais conectados ao sistema de saúde, mas com menos confiança na conduta em casos DLI.

Objetivo: Determinar el nivel de conocimientos y las actitudes de los médicos en Tijuana, con base en la Guía de Práctica Clínica (GPC) para la prevención, diagnóstico y tratamiento del Dolor Lumbar Inespecífico (DLI). Métodos: Estudio prospectivo, transversal y descriptivo. Los datos fueron obtenidos de los médicos que prestan sus servicios en clínicas, consultorios privados y/o instituciones de gobierno. Resultados: Se obtuvo un total de 56 médicos encuestados, 37 hombres y 19 mujeres. Ningún médico contestó que no atiende un paciente con dolor lumbar. El 49% conocen la GPC y el 51% no saben de su existencia. Conclusiones: A pesar de que algunos médicos refieren conocer la GPC, según los resultados obtenidos falta mayor dominio y apego de la misma. El no conocer la GPC no hace imposible contestar el cuestionario. Los médicos se sienten más conectados con el sistema de salud, pero con menor autoconfianza en el manejo del DLI.

Preparation of brain active-targeting endomorphin loaded nanoparticles and study on its effects of passing across blood brain barrier / 国际生物医学工程杂志

Objective To prepare a novel brain active-targeting endomorphin (EM) loaded hyperbranched polyglycerols-poly (lactic-co-glycolic acid) (HBPG-PLGA) nanoparticles (NPs) and study its mechanism of passing across blood brain barrier (BBB) in brain microvascular endothelial cells (BMEC).Methods The OX26 (transferring receptor monoclonal antibody) conjugated EM loaded HBPG-PLGA NPs was constructed according to water-in-oil-in-water emulation solvent evaporation technique as a novel biodegradable brain active-targeting drug delivery system.The properties of the NPs were evaluated by transmission electron microscope (TEM) in vitro.Through flow cytometry and laser scanning confocal microscope,the mechanism of passing across BBB was evaluated.Results The preparation methodology of NPs was optimized and established.The mean diameter was (170±20) nm and Zeta potential was about-27 mV.Core-shell construction was showed on TEM.Cellular uptake study showed that the uptake of NPs was via a caveolae-mediated endocytic pathway,then endomorphin and carrier were divided into two parts in BMEC.Conclusions The OX26 conjugated EM loaded NPs were stable,and demonstrate remarkable effects on crossing BBB.Cellular uptake by BMEC is a very important mechanism of the NPs' brain activating-targeting effect.

Rol de la dexmedetomidina en el tratamiento del dolor / Role of dexmedetomidine in the treatment of pain

La dexmedetomidina es un fármaco agonista de los receptores alfa-2 adrenérgicos, altamente selectivo, utilizado para sedación en unidades de cuidados críticos. Posee también, efectos analgésicos importantes que pueden atribuirle un rol en el manejo clínico del dolor. Diversas comunicaciones científicas han estudiado su utilidad en el manejo del dolor agudo, crónico y en cuidados paliativos, tanto en adultos como en niños. En este artículo de revisión se analiza la evidencia científica disponible hasta la fecha con el objeto de dilucidar cuál es el real aporte de este fármaco en el tratamiento de las diversas formas de dolor...

Dexmedetomidine is a highly selective alpha-2 adrenergic agonist commonly used in the critical care units for sedation therapy. It has analgesic effects that may be used in pain treatment. Many scientific reports have studied its utility in the management of acute and chronic pain and palliative care. In this review we analyze the scientific evidence in relation to the real role of dexmedetomidine in pain therapy...

Benefícios e limitações da utilização da glicose no tratamento da dor em neonatos: revisão da literatura / Benefits and limitations of the use of glucose for the treatment of pain in neonates: a literature review

Esta revisão se propõe analisar os estudos que utilizaram a glicose como recurso terapêutico em neonatologia durante procedimentos que resultam em dor de intensidade leve a moderada apontando os benefícios e limitações de sua utilização. Os recém-nascidos internados em unidades neonatais são submetidos a inúmeros procedimentos dolorosos sem abordagem terapêutica adequada, apesar de a literatura recomendar de maneira enfática a necessidade de tratamento e ressaltar as repercussões neurológicas deletérias para esses pacientes. A maior parte destas intervenções constitui procedimentos frequentemente realizados nas unidades e necessários à manutenção da estabilidade clínica, nos quais a analgesia sistêmica não está indicada. A administração de solução oral de glicose parece ser eficaz e segura no controle da dor durante procedimentos que geram dor de intensidade leve a moderada nas unidades de terapia intensiva neonatais, os efeitos adversos são raros e o mecanismo de ação ainda não está descrito de maneira consistente na literatura. A indicação da solução oral de glicose durante punções venosas é bem descrita e durante punções de calcanhar parece ser o método mais eficaz de controle da dor especialmente quando associado à sucção não nutritiva, com resultados favoráveis na maior parte dos estudos.

This article aims to review the main studies evaluating glucose as a therapeutic alternative during mildly to moderately painful procedures in neonatology, highlighting its benefits and limitations. During their stay in neonatal intensive care units, neonates are constantly subjected to a number of painful procedures without proper therapeutic management, although the medical literature emphatically recommends this type of management, highlighting the deleterious neurological consequences of pain. Most of these interventions are frequently necessary in neonatal intensive care units to maintain clinical stability in these children; the use of systemic analgesia, however, is not considered to be a good option. The administration of oral glucose solution is apparently effective and safe for pain control during procedures causing mild-to-moderate pain in neonate intensive care units, with rare adverse effects; however, its mode of action has not yet been described clearly in the literature. The administration of oral glucose solution is well described for use in venous punctures; it is apparently effective also for heel punctures, especially when associated with nonnutritive sucking, with most studies showing favorable results.

Retrospective Review of Outcomes of a Multimodal Chronic Pain Service in a Major Teaching Hospital: A Preliminary Experience in Universiti Sains Malaysia

Background: Chronic pain is a common medical issue. Beside chronic devastating pain, patients also suffer dysfunction more generally, including in the physical, emotional, social, recreational, vocational, financial, and legal spheres. Integrated multidisciplinary and multimodal chronic pain management programmes offer clear evidence for relief of suffering and return to functional lifestyles. Materials and Methods: This retrospective review was performed in order to evaluate one-year outcomes among all newly referred patients of the multimodal chronic pain service at Hospital Universiti Sains Malaysia (HUSM). All patients received multimodal pain therapy, including pharmacological, physical, and psychological therapy, exercise, and pain intervention. The variables evaluated were based on a patient’s global pain assessments, which were made using the Visual Analogue Scale (VAS) and Oswestry Disability Index (ODI), modified by patient self-report, and were taken within days to months of commencing our multimodal pain regime. Results: A total of 169 patients were enrolled in this study. Out of this number, 102 (60.4%) were seen at the pain clinic, and 67 (39.6%) were referred while they were inpatients. About one-third of the patients had chronic pain due to cancer. Our data showed that 128 (75.7%) of our chronic pain patients were successfully managed when ≥50% of pain relief (as measured by their VAS score) was achieved at any point during the course of the study period. In addition, 104 patients (61.5%) showed improvement in their modified ODI by 50% or more. Conclusion: A multimodal chronic pain service plays a significant role in managing chronic pain patients in a major hospital, as it is capable of delivering comprehensive and attainable care to manage refractory and intractable chronic pain.

Efeito dos anticonvulsivantes gabapentina e carbamazepina associados ou não ao antidepressivo amitriptilina no controle da dor neuropática em pacientes portadores de Hanseníase / The effects of the antiepiletic drugs gabapentin, carbamazepine, either used in association with amitriptyline or not, in the control of neuropathic pain in Hansen disease patients

Este é um estudo clínico, prospectivo, aleatório, e duplamente encoberto realizado em 80 doentes hansênicos de ambos os sexos e com idade variando entre 18 e 65 anos, portadores de dor neuropática. Os pacientes foram divididos em 4 grupos: Grupo G: pacientes tratados com gabapentina na dose de 400mg diários, Grupo C: pacientes tratados com carbamazepina na dose de 200 mg diários, Grupo GA: pacientes tratados com a associação de gabapentina 400 mg e amitriptilina 25 mg diários e Grupo CA: pacientes tratados com a associação de carbamazepina 200 mg e amitriptilina 25 mg diários e avaliados durante 4 meses quanto a intensidade da dor, consumo de prednisona, necessidade do uso de talidomida, queixa de queimação, parestesia, sensação de choque e alteração da sensibilidade, bem como da necessidade de realização de neurólise e eventos adversos relacionados ao tratamento. Os resultados permitiram verificar que o valor médio de intensidade de dor foi semelhante em todos os grupos no momento da inclusão e no momento de encerramento do estudo, e a diminuição da dor foi semelhante em todos os grupos, não havendo superioridade de nenhum dos esquemas terapêuticos sobre o outro, portanto a carbamazepina isolada ou associada a amitriptilina e a gabapentina isolada ou associada a amitriptilina foram igualmente eficientes na redução da dor que os pacientes apresentavam no momento de inclusão no estudo, porém a duração da dor, em dias, foi maior no grupo medicado com a gabapentina isolada, foi menor e igual nos grupos medicados com a carbamazepina e com a gabapentina associada a amitriptilina e teve uma duração intermediária no grupo medicado com a carbamazepina associada a amitriptilina, embora a diferença não tenha sido significativa pela análise estatística. Todos os fármacos foram igualmente eficazes na redução do consumo da prednisona e na necessidade do uso de talidomida. A queixa de queimação, de parestesia, de sensação de choque e de alteração da sensibilidade...

This study is a clinical trial. During the present study a prospective controlled four-way crossover double-blind randomized protocol was followed. Eighty hansen's patients, male and female, aged 18 to 65, with neuropathic pain took part. The patients were divided into 4 groups as follows: Group G -patients treated with a gabapentin 400 mg dose daily; Group C - patients treated with a carbamazepine 200 mg dose daily; Group GA - patients treated with a gabapentin 400 mg dose in association with an amitriptyline 25 mg daily, Group CA - patients treated with a carbamazepine 200 mg dose in association with an amitriptyline 25 mg daily. All four groups were assessed for four months taking into account pain intensity, prednisone consumption, the amount of thalidomide needed, burn sensation complaints, paresthesia, numbness, shock sensitivity and alterations to sensitivity, as well as neurolysis and side effects related to the treatment. The results of the study demonstrated that intensity of pain was similar in patients belonging to all four groups, both at the moment of inclusion and at the end of the study, and the reduction in the intensity of pain was also similar in all groups, without any report of superior effectiveness in any of the four groups studied. Therefore, the gabapentin and the carbamazepine, alone or in association with amitriptyline, proved to be equally effective in the reduction of the pain the patients felt at the moment of their inclusion to the present study. On the other hand, during the assessment of the duration of pain in days we noticed that it lasted longer in the group treated only with gabapentin, it was shorter or the same in the groups treated with carbamazepine and with gabapentin in association with an amitriptyline, and was considered intermediary in the group treated with carbamazepine in association with an amitriptyline, even though the difference was not considered significant in terms of statistical analysis...

Effect of Relaxing Operation with Small Needle Knife and Compound Osteotide Injection for Suprascapular Nerve Compression Syndrome: An Observation of 120 Cases / 广州中医药大学学报

[ Objective ] To observe the effect of relaxing operation with small needle knife and acupoint injection of Compound Osteotide Injection (COI) for suprascapular nerve compression syndrome (SNCS) . [Methods] Two hundred and twenty cases of SNCS were randomized to three groups: group A ( re = 120) was treated with small needle knife for relaxation and acupoint injection of COI, group B ( n = 50) with small needle knife for relaxation and group C ( re = 50) with acupoint injection of COI. The short-term and long-term effects were compared in the three groups. [Results] Total effective rate was 98.3% in group A, 88.0% in group B and 74.0% in group C ( P