Groin hernia is common, and each year 200 repairs per 100 000 adult inhabitants are performed in Sweden. Groin hernias are either inguinal or femoral (2-4%). Elective repair is not associated with an excess mortality, but adverse outcomes include recurrence and long-term pain. Emergency procedures have a 4% mortality rate with an increased risk for bowel resection and postoperative complications. The aim of this thesis was to identify risk factors for adverse outcomes and to propose measures to improve groin hernia treatment. Twenty-three per cent of female hernias were femoral. Thirty-six per cent of femoral hernias, and 5% of inguinal hernias, have emergency procedures. Females (OR 1.47) and patients above 65 years-of-age (OR 2.24) were at higher risk for emergency repair. Bowel resection was performed in 23% of emergency femoral repairs, and the 30-day mortality was 10 times that of an age- and gender-matched population. The majority of emergency patients were unaware of their hernia, and one third had previously had no groin symptoms. Femoral repairs were at larger risk for recurrence than inguinal repairs. The surgical techniques with least risk for recurrence were preperitoneal mesh repairs (open HR 0.28, and laparoscopic HR 0.31). Long-term pain was present in 24% of femoral hernia patients, of whom 5.5% described pain interfering with daily activities. The only factor predicting the risk for long-term pain was pain preoperatively. Pain decreased with time. In a randomized study on inguinal hernia, TEP resulted in less pain six weeks after surgery than Lichtenstein repair performed under local anesthesia (LLA). TEP patients were to a larger extent able to perform sporting activities. No difference was seen in intra-operative complications. Femoral hernias should be given high priority for repair and preperitoneal techniques should be used. Earlier diagnosis, in the elective setting, is probably difficult to attain. Heightened awareness in the emergency department is required. TEP is safe, and results in less pain than LLA six weeks after surgery. A widening of indications for TEP in primary inguinal hernia repair is justifiable.

The painless odontological treatment is one of the main goals of the dental surgeonand the local anesthesia is the most common used to reach it. Abilities and skills in odontological anesthesia can be acquired through different teaching methods. Thus, the objective of this work was to evaluate if there is a more effective teaching method for the teaching of the blockade of the inferior alveolar nerve technique and for the control of anxiety related to performing this technique. Odontology under graduate students at pre-clinical level were divided into three groups according to the type of teaching methodology used. At the Problem Based Learning (PBL) group, activities were performed in the tutorial model using a problem designed to achieve learning goals related to the technique. In the EXP group, the transmission of knowledge happened through classic expositive class. Whereas in the LAB group, activities in anatomical models were used as a way to present the anesthetic technique. Then, students were assessed in practice, through an objective structured clinical examination (OSCE) centered in the administration of the anesthetic technique and measuring the levels of anxiety before and after the execution of the procedure. There was also a theoretical evaluation related to execution aspects of the technique studied. Forty-one students concluded the practical test and the results did not show significant difference between the means of the groups ABP (12.62), EXP (13) and LAB (12.13). In the assessment of anxiety arising from the implementation of the procedure, the students of the LAB group seemed to be less anxious. On the other hand, the EXP group showed a positive correlation between anxiety and performance. In the theoretical evaluation, the average of the scores was equal for all groups (13.20). Considering the limitations of the study, it was found that the methodologies studied proved equally efficient when it comes to teaching the blockade of the inferior alveolar nerve technique. Pre-clinical practices seem to reduce the anxiety related to the execution of the technique, although this reduction has not produced a better clinical performance. / O tratamento odontológico sem dor é um dos principais objetivos do cirurgiãodentista e a anestesia local é o método mais utilizado para alcançá-lo. O ensino da anestesia odontológica pode ser conduzido observando os seguintes aspectos: metodologia teórica de ensino a ser utilizada, forma da primeira prática clínica anestésica e uso de atividades pré-clínicas. O objetivo deste trabalho foi de avaliar qual método de ensino é mais eficaz no aprendizado do bloqueio do nervo alveolar inferior por estudantes de graduação em odontologia. Graduandos do terceiro ano do curso de odontologia foram divididos em três grupos. A respeito da técnica de anestesia do nervo alveolar inferior, no grupo ABP foram ministradas aulas na modalidade de aprendizado baseado em problemas, no grupo EXP, aulas expositivas e no grupo LAB atividades laboratoriais em modelos anatômicos. Em seguida, foram aplicadas avaliações contendo 20 itens da seguinte forma: prática, através de anestesia nos próprios estudantes e mensuração dos níveis de ansiedade, e teórica, por julgamento de itens em correto ou incorreto. Quarenta e um estudantes concluíram a prova prática, os resultados não mostraram diferença significativa das médias entre os grupos quando julgados os 20 itens: grupo ABP (12,62), EXP (13) e LAB (12,13). Na avaliação da ansiedade da prática clínica, os estudantes dos grupos ABP e EXP estavam mais ansiosos do que aqueles do grupo LAB. Por outro lado, o grupo EXP apresentou correlação positiva entre ansiedade e desempenho. E na prova teórica, a média das notas foram iguais para todos os grupos (13,20). Constatou-se a partir destes dados que, para o ensino do bloqueio do nervo alveolar inferior, os métodos de ensino estudados mostraram-se igualmente eficazes, e a prática pré-clínica foi capaz de reduzir a ansiedade na avaliação prática embora esta redução não tenha produzido melhor desempenho. / Lagarto, SE

Orientadores: Eneida de Paula, Leonardo Fernandes Fraceto / Dissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Biologia / Made available in DSpace on 2018-08-16T01:05:29Z (GMT). No. of bitstreams: 1 Lima_RobertaAlineFrancode_M.pdf: 1479897 bytes, checksum: 3c9af4bda36adc886426ab930c957a40 (MD5) Previous issue date: 2010 / Resumo: A dor desempenha um papel biológico muito importante como indicador da presença de um estímulo nocivo, que pode representar dano real ou potencial ao organismo; entretanto, não é interessante que essa sinalização persista além das necessidades fisiológicas a ponto de tornar-se um incomodo, podendo dificultar o desempenho das atividades normais, comprometer a qualidade de vida do indivíduo e impedir a realização de práticas cirúrgicas curativas. Os anestésicos locais são fármacos empregados para alívio da dor aguda ou crônica, pois bloqueiam a condução do estímulo nervoso em membranas neuronais. Dentre eles, está a Tetracaína (TTC) um amino-éster de grande utilidade na prática clínica, empregado em procedimentos que requerem anestesia tópica, como aqueles oftalmológicos que necessitam de intervenções na córnea. As limitações do uso clínico da TTC está relacionadas à sua baixa estabilidade química (hidrólise da ligação éster por esterases plasmáticas) e sua toxicidade sistêmica. Sistemas de liberação modificada de fármacos, que empregam carreadores como ciclodextrinas, constituem uma alternativa para aumentar o tempo de ação anestésica e diminuir a toxicidade. As ciclodextrinas são capazes de formar complexos de inclusão com diversos fármacos, alterando propriedades como a solubilidade aquosa, o que torna esses oligosacarídeos cíclicos promissores para este tipo de aplicação. Neste trabalho, estudamos a complexação da TTC com beta-ciclodextrina (?-CD) e hidroxipropil-beta-ciclodextrina (HP-?-CD) em pH fisiológico e sua influência na toxicidade celular e efeito antinociceptivo, induzidos por aquele anestésico, objetivando a preparação de novas formas farmacêuticas. Para caracterização dos complexos de inclusão TTC:?-CD e TTC:HP-?-CD foram empregados métodos espectroscópicos (Ressonância Magnética Nuclear, fluorescência, absorção UV/VIS), difração de raios-X e calorimetria diferencial de varredura. A partir das análises realizadas, encontrou-se que a estequiometria de complexação da TTC com ambas as ciclodextrinas é de 1:1. A constante de associação aparente da TTC, determinada por DOSY-NMR, é de 777 M-1 e 2243 M-1, para ?-CD e HP-?-CD respectivamente, indicando uma forte interação entre as moléculas de anestésico e das ciclodextrinas, em pH fisiológico. Os dados de proximidade espacial, determinados por RMN (1DROESY) revelaram interações entre os hidrogênios Hh e Hi, (que fazem parte do anel aromático da TTC) e hidrogênios da cavidade interna das ciclodextrinas, permitindo assim propor a geometria dos complexos de inclusão da TTC com ambas ciclodextrinas. Ensaios in vitro, em cultura de fibroblastos da linhagem 3T3, mostraram aumento na viabilidade celular após complexação da TTC com ?-CD e HP-?-CD, em relação à TTC em solução. Testes de atividade biológica, de bloqueio do nervo infraorbital em ratos, demonstraram aumento significativo do tempo de duração da anestesia nos animais tratados com os complexos TTC:?-CD e TTC:HP-?-CD (40 min e 40 min), em relação ao grupo tratado com 0,5% de TTC livre (30 min). Os resultados obtidos neste estudo demonstram a formação de complexos de inclusão com forte interação entre TTC e ?-CD e HP-?-CD; indicam ainda que a utilização destes complexos de inclusão é promissora como forma farmacêutica alternativa para este anestésico, devido ao aumento da duração da anestesia (pois os complexos apresentaram maior eficácia quando comparados à TTC livre nas mesmas doses), ou ainda a diminuição da toxicidade (atingindo a mesma eficácia da TTC livre, com menores concentrações de TTC complexada). / Abstract: Pain plays an important biological role as a sign of the presence of a noxious stimulus, that denotes actual or potential damage to the body. However, it is not interesting this signal to persist beyond the physiological point, to become a nuisance that impairs the performance of normal activities, the quality of life or prevents the procedure of healing surgical practices. Local anesthetics are used for the relief of acute or chronic pain since they block the conduction of the painful stimulation in neuronal membranes. Among them is Tetracaine (TTC) an amino ester useful in clinical procedures requiring local anesthesia such as those ophthalmic ones with intervention in the cornea. The clinical use of TTC is limited by its low chemical stability (hydrolysis of the ester bond by plasma esterases) and systemic toxicity. The use of drug-delivery systems, in carriers such as cyclodextrins is a good approach to improve the duration of action and to diminish the toxicity of local anesthetics. Cyclodextrins are suitable for this type of application since these cyclic oligosaccharides are able to form inclusion complexes with several drugs improving their water solubility. Here we have studied the complexation of TTC with beta (?-CD) and hydroxypropyl-beta-cyclodextrin (HP-?-CD) and its influence in cell toxicity and antinociceptive effects induced by that anesthetic, aiming the development of new pharmaceutical forms. TTC and ?-CD or HP-?-CD inclusion complexes were characterized using spectrophotometric methods (Nuclear Magnetic Resonance, fluorescence, UV-VIS absorption), X-ray Diffraction and Differential Scanning Calorimetry. A 1:1 stoichiometry of complexation was found for both complexes. The association constant determined by DOSY was 777 M-1 and 2.243 M-1 for TTC complexation with ?-CD and HP-?-CD, respectively, indicating a strong association between the anesthetic and both cyclodextrins, at physiological pH. The nuclear overhauser NMR data (ROESY) had disclosed trough the space proximities between hydrogens Hh and Hi - at the aromatic ring of TTC - and hydrogens from the inner cavity of the cyclodextrins, allowing us to suggest the geometry of TTC:?-CD and TTC:HP-?-CD complex formation. In vitro culture tests on 3T3 fibroblasts cells revealed an increase in cell viability after TTC complexation with ?-CD and HP-?-CD, in comparison to the effect of free TTC. Biological activity was assessed in rats, through the infraorbital nerve blockade test. The results revealed a significant increase in the duration of anesthesia in animals treated with TTC:?-CD and TTC:HP-?-CD (40 min and 40 min), in comparison to a solution of 0.5% tetracaine (30 min). The results presented here demonstrate the formation of strong associated inclusion complexes between TTC and ?-CD and HP-?-CD. The in vivo results allow us to consider those complexes as promising pharmaceutical forms to increase the duration of anesthesia induced by tetracaine (since both complexes showed higher anesthetic potency when compared to free TTC at equivalent doses) or to diminish its toxicity (since the same activity can be achieved with lower concentrations of the complexed TTC formulations). / Mestrado / Bioquimica / Mestre em Biologia Funcional e Molecular

No parto normal, o trauma provocado por episiotomia ou roturas, é freqüente e a anestesia local é bastante utilizada no reparo das lesões da região vulvoperineal. Na literatura especializada, os estudos sobre as soluções anestésicas mais adequadas são escassos para essa anestesia. No entanto existem recomendações para a adoção de anestésicos com vasoconstritor pela permanência mais prolongada da solução anestésica no local, garantindo maior ação e redução da concentração plasmática da droga, mas na prática seu uso é restrito. O objetivo do estudo foi comparar a quantidade de anestésico necessária para inibir a dor durante a sutura do trauma perineal, em mulheres com episiotomia ou laceração espontânea de primeiro ou segundo graus, conforme o uso ou não de vasoconstritor na solução anestésica. Trata-se de uma pesquisa aleatorizada e controlada com mascaramento duplo, realizada no Centro de Parto Normal do Amparo Maternal na cidade de São Paulo. Foram incluídas 96 parturientes, alocadas em três blocos - laceração de primeiro grau, laceração de segundo grau e episiotomia. Em cada bloco, constituído por 32 mulheres, 16 receberam solução anestésica com vasoconstritor e 16 sem vasoconstritor. Os resultados mostraram que, na laceração de primeiro grau, a média de anestésico com vasoconstritor apresentou diferença estatisticamente significante (p=0,002), com 1,0 ml (I.C. -1,6; -0,4) menos que a média do anestésico sem vasoconstritor; em 95% dos casos, foram usados de 1 a 2 ml de solução com vasoconstritor, e em 87,5% dos casos para o anestésico sem vasoconstritor, o volume usado variou de 2 a 4 ml. Para a laceração de segundo grau, a média do anestésico com vasoconstritor foi 3,7 ml (I.C. -5,8; -1,6) menos que a média do anestésico sem vasoconstritor, sendo estatisticamente significante (p=0,001); em 87,5% dos casos, a quantidade máxima de anestésico com vasoconstritor administrada foi 6 ml, e 81,3% das mulheres que receberam anestésico sem vasoconstritor, a dose administrada foi de 7 ml ou mais. Considerando a extensão da laceração, adotou-se o tamanho da episiotomia praticada nas mulheres do estudo, como parâmetro para classificar a extensão da laceração. Foram agrupadas como pequenas as lacerações de menor extensão, como médias aquelas com tamanho semelhante à episiotomia e como grandes aquelas cuja extensão superou o tamanho da episiotomia. Para a episiotomia, a média de anestésico com vasoconstritor foi 0,3 ml (I.C. -2,1; 1,5) a menos que a média do anestésico sem vasoconstritor, considerada sem significância estatística (p=0,724). Os resultados permitiram confirmar a hipótese de que uso de anestésico com vasoconstritor na anestesia local para a sutura de lacerações perineais no parto normal aumenta a eficácia da anestesia local. Embora o volume de anestésico utilizado na sutura de laceração de primeiro e segundo graus seja significativamente reduzido pela associação com vasoconstritor, a relevância clínica desse resultado deve ser considerada. / The perineal trauma, caused by episiotomy or ruptures, is quite frequent during the spontaneous delivery, being the local anesthesia widely utilized when repairing lesions in the vulvo-perineal region. Throughout the specialized literature, scarce are the studies on the most suitable anesthetic solutions for this kind of anesthesia. Even though there are recommendations for the adoption of the anesthetic with vasoconstrictor, because of the prolonged permanence of the anesthetic solution in the region, thus ensuring a bigger time of action, and because of the reduction in the plasmatic concentration of the drug, its utilization in practice is restricted. The goal of the study was to compare the necessary quantity of anesthetic to inhibit pain during the suture of the perineal trauma in women with an episiotomy or with first or second degree spontaneous lacerations, according to the use or not of vasoconstrictor in the anesthetic solution. This is a randomized and controlled research, with double blind trial, performed in the Birth Centre at Amparo Maternal, in the city of Sao Paulo. There were 96 parturients included in the study and then divided into three blocks: first degree laceration, second degree laceration and episiotomy. In each block, constituted of 32 women, 16 women were administered the anesthetic solution with vasoconstrictor and 16 with no vasoconstrictor. Results show that in the first degree laceration block the average of anesthetic with vasoconstrictor presented a statistically significant difference (p=0,002), with 1,0 ml (C.I. -1,6; -0,4) less than the average of the anesthetic without vasoconstrictor; in 95% of the cases, 1 to 2 ml of the solution with vasoconstrictor was utilized, while in 87,5% of the cases, the anesthetic without vasoconstrictor varied from 2 to 4 ml. In the second degree laceration block, the average of anesthetic solution with vasoconstrictor was 3,7 ml (C.I. -5,8; -1,6) less than the average of the anesthetic without vasoconstrictor, being statistically significant (p=0,001); in 87,5% of the cases, the maximum quantity of anesthetic with vasoconstrictor administered was 6 ml, while in 81,3% of the cases, women who were given the anesthetic without vasoconstrictor, received 7 ml or more. Considering the extent of the laceration, the size of the episiotomy practiced on the women of the study was adopted as a parameter to classify the extent of the laceration. The lacerations of a smaller extent were grouped as small-sized, the ones in which the size was similar to the size of the episiotomy were grouped as medium-sized, and as large-sized the ones that oversized the episiotomy. For the episiotomy, the average of anesthetic with vasoconstrictor was 0,3 ml (C.I. -2,1; 1,5) less than the average of the anesthetic without vasoconstrictor, with no statistic significance (p=0,724). Results allow us to confirm the hypothesis that the utilization of the anesthetic with vasoconstrictor in the local anesthesia during the suture of the perineal lacerations in the spontaneous delivery increases the effectiveness of the local anesthesia. Although the volume of anesthetic utilized in the suture of the first and second degree lacerations is significantly reduced by the association with vasoconstrictor, the clinical relevance of this result must be taken into further consideration.

Bakgrund: Enligt barnkonventionen har barn som vistas inom hälso- och sjukvården rätt till delaktighet i sin vård genom anpassad information samt att få att uttrycka sina åsikter i alla frågor som rör dem. Insättning av perifer venkateter och blodprovstagning är smärtsamma procedurer som barn utsätts för inom barnsjukvården. Inför dessa procedurer är det viktigt att barn får goda förberedelser. Syfte: Studiens syfte var att undersöka och beskriva barns erfarenheter av delaktighet inför och under insättning av perifer venkateter och blodprovstagning. Metod: Studien genomfördes som en kvantitativ enkätstudie. Enkäterna besvarades av 47 barn i åldrarna åtta till arton år, som hade genomgått insättning av perifer venkateter alternativt lämnat venösa eller kapillära blodprov på Falu lasarett eller Akademiska barnsjukhuset i Uppsala. Resultat: Tjugoen procent av barnen fick inte lokalbedövning och 20% blev aldrig tillfrågade om önskemål i samband med smärtsamma procedurer. De barn som uppgav att personalen inte hade berättat hur de smärtsamma procedurerna skulle gå till hade lägre ålder i median jämfört med de barn som personalen berättade för (9 år versus 14 år, p=0,006). Ju högre barnen skattade att de förstått informationen de fått på en tiogradig skala desto högre skattade de att de kunde säga stopp om något var för påfrestande eller gjorde för ont i samband med smärtsamma procedurer (r=,430, p=0,004). Slutsats: Alla barn ska tillfrågas om önskemål och erbjudas lokalbedövning inför smärtsamma procedurer. Sjukvårdspersonal ska ge barn anpassad information oavsett ålder vilket främjar barns möjlighet att säga stopp om de upplever proceduren som för påfrestande. Sjukvårdspersonal måste visa extra lyhördhet gentemot barn med lägre ålder. / Background: According to the Convention on the Rights of the Child, children receiving healthcare have the right to personalized information and to have their opinions expressed on all issues that concern them. Peripheral intravenous cannulation and blood sampling are painful procedures that children are subjected to in pediatric care, and prior to these procedures it is important that children receive good preparation. Objective: The aim of the study was to investigate and describe children’s experiences of participation before and during peripheral intravenous cannulation and blood sampling. Method: The study was a quantitative survey. The questionnaires were answered by 47 children aged eight to eighteen years, who had experienced peripheral intravenous cannulation or venous/capillary blood test at the hospital in Falun or at the Children’s Hospital in Uppsala. Results: Twenty-one percent of the children did not receive local anesthesia and 20% were never asked for their preferences in connection with painful procedures. The children who stated that they were not informed by the healthcare professionals regarding the painful procedures were of younger age compared to the children that were informed (9 years versus 14 years, p=0,006). The higher the children rated on a 10-degree scale that they understood the information, the higher they also rated that they could tell the healthcare professionals to stop if the painful procedures was too demanding or too painful (r=,430, p=0,004). Conclusion: All children should be asked for their preferences and be offered local anesthesia for painful procedures. Healthcare professionals should provide the children with appropriate information regardless of the age of the child, which promotes the child’s ability to tell the healthcare professionals to stop if they experience the procedures as too demanding. Healthcare professionals should be more aware when caring for younger children.

No description available.

The ability to perform local anesthesia on dental patients is an important clinical skill for a dental hygienist. When learning this procedure in an academic situation, students often practice on their peers to build their skills. There are multiple reasons why the peer practice is not ideal; consequently, educators have sought the means to simulate the practice of local anesthetic procedures without endangering others. Mixed-reality technologies offer a potential solution to the simulated procedure problem. The purpose of this research was to determine if students could learn the techniques for providing local anesthesia using a mixed-reality system that allows them to manipulate 3D objects in virtual space. Guiding research questions were: In what ways do using 3D objects allow for a greater understanding of anatomical, spatial, and dimensional acuity? Will students develop conceptual understandings regarding the application of anatomical and technical concepts through iteration? Will students demonstrate the proper technique and verbalize a level of confidence for administering local anesthesia after using the mixed-reality system? Design-based research methods allowed for multiple iterations of design, enactment, analysis, and redesign. The first iteration focused on building a knowledge base for designing and developing virtual reality technologies for use in dental hygiene education. The second phase of research increased in technical sophistication and involved a virtual system that allowed for student interaction and manipulation of 3D objects. The interactions supported students' learning through the association of anatomical, spatial, and dimensional acuity. Built-in learner prompts promoted the understanding and identification of anatomical landmarks for performing an injection for the lower jaw. Further, the system promoted self-controlled practice and iterative learning processes. Redesign and development in the final iteration focused on design improvements of the system that included an output metric for assessing student performance, a data glove, and a marker to assist in following student interactions. Results support that students learned "while doing" in a specific immersive environment designed for dental hygiene education and they increased their level of confidence for performing a specific procedure.

Os anestésicos locais têm sido utilizados na clínica médica e odontológica com o objetivo de atenuar a dor nos procedimentos cirúrgicos. Tais fármacos são administrados usualmente por meio do uso de agulhas, o que pode diminuir o número de pacientes nos consultórios dentários, afugentados pelo medo desses dispositivos invasivos. Comprimidos mucoadesivos de dissolução rápida podem ser promissores em incorporar esses anestésicos e assim liberá-los topicamente com a finalidade de promover a anestesia de forma não invasiva. Neste intuito, comprimidos de dissolução rápida contendo os anestésicos locais cloridratos de prilocaína (PCL) e lidocaína (LDC) foram desenvolvidos por três métodos: i) compressão direta; ii) compressão após pré-processamento dos adjuvantes em secagem por atomização e iii) liofilização. Estes foram comparados em relação ao tempo de hidratação e desintegração para a escolha de uma plataforma para estudos de liberação, permeação e mucoadesão in vitro. Filme polimérico oclusivo com Eudragit S100 foi moldável e flexível para a finalidade de revestimento parcial. A massa total de desintegrantes nos comprimidos modularam sua hidratação e desintegração. Os comprimidos obtidos por liofilização apresentaram menores valores de tempo de hidratação e desintegração. Os efeitos de diluente (manitol), desintegrante (glicolato sódico de amido), promotores químicos de permeação (ácido oleico, Tween® 80 e propilenoglicol) e polímeros mucoadesivos (HPMC e pullulan) sobre liberação em éster de celulose e permeação em esôfago suíno foram avaliados. Os comprimidos apresentaram rápida liberação em uma hora. A liberação obedeceu a cinética de primeira ordem e o mecanismo de liberação foi governado pelo transporte não fickiano. A proporção de manitol e tipo de polímero mucoadesivo não teve influência significativa nos estudos de liberação. A quantidade de fármacos liberada diminuiu em comprimidos com desintegrantes e promotores químicos de permeação. Um significante efeito sinérgico entre polímero mucoadesivo e promotores químicos no coeficiente de permeabilidade, fluxo e retenção de fármacos na mucosa foi observado. Quando comparado com comprimidos de HPMC com promotores químicos, o pullulam melhorou a permeação de fármacos através da mucosa. Mucoadesão dos comprimidos com diferentes polímeros foi avaliado. HPMC e pullulan melhoraram as propriedades mucoadesivas. Todos os comprimidos se mantiveram aderidos na região do epitélio durante uma hora. A nova plataforma de liberação de fármacos obtida pela combinação de tecnologias farmacêuticas de comprimidos por liofilização, com adição de promotores de permeação e pullulan como polímero mucoadesivo mostrou uma estratégia efetiva para o desenvolvimento de um sistema transbucal para LDC e PRC que pode ser usada para melhorar anestésica sem uso de agulhas / Local anesthetics have been used in medical and dental practice aiming at to become less painful some surgical procedures. Such drugs are typically administered through needles along surgical procedures, which decrease the number of patients in the dental offices, once many people are afraid of these invasive devices. Fast dissolving and mucoadhesive tablets could be promising for incorporating these anesthetics and thus releasing them topically in order to improve noninvasive anesthesia. Herein, it were developed fast dissolving tablets containing the local anesthetic drugs prilocaine (PRC) and lidocaine (LDC) hydrochloride. Three methods were used: a) direct compression of the mixture of components; b) pre-processing by spray drying adjuvants and c) freeze drying and these tablets. The tablets were compared in terms of wetting and disintegration time for the choice of a platform for further in vitro release, permeation and mucoadhesion studies. An occlusive polymeric film of Eudragit S100 showed suitable flexibility and plasticity according to purpose of coating the tablets. The total mass of disintegrants in formulations affected the wetting and disintegration of the tablets. Freeze dryed tablets had lower wetting and disintegration time values as compared to the others. The effects of diluent (mannitol), disintegrant (sodium starch glycolate), chemical enhancers (oleic acid, Tween® 80 and propylene glycol) and mucoadhesive polymers (hydroxypropyl methylcellulose and pullulan) on the drug release from cellulose ester membrane and drug permeation through porcine esophageal mucosa were evaluated. Dissolution test showed fast release on one hour. The drug release data fit well to the First order expression and the release mechanism was non-Fickian transport. No significant influence of proportion of mannitol and type of mucoadhesive polymer on release studies was observed. Release of drugs decreased in tablets with disintegrant and chemical enhancers. A significant synergic effect between the mucoadhesive polymer and chemical enhancers on the permeability coefficient, flux and retention of drugs on mucosa was observed. As compared to HPMC for tablets containing chemical enhancers, pullulan improved the drug permeation through the mucosa. Mucoadhesion to tablets with different polymers was evaluated. HPMC and pullulan improve mucoadhesive properties. All tablets maintained in the attachment site of the epithelium for at least one hour. It conclusion, the novel drug delivery platform achieved by combining the pharmaceutical technologies of freeze-dryed tablets comprising chemical enhancers and pullulan as mucoadhesive polymer displayed an effective strategy for the development of a transbuccal system for LDC and PRC that can be used to improve needle-free buccal anesthesia.

No description available.