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Doctoral Thesis
DOI
10.11606/T.10.2011.tde-10102012-140442
Document
Author
Full name
Patrícia Helena Paiva Miguez
E-mail
Institute/School/College
Knowledge Area
Date of Defense
Published
São Paulo, 2011
Supervisor
Committee
Madureira, Ed Hoffmann (President)
Arruda, Rubens Paes de
Meirelles, Flavio Vieira
Oliveira, Claudio Alvarenga de
Perecin, Felipe
Title in Portuguese
Cinética de liberação de progesterona em dispositivos confeccionados a partir de blendas com PCL (Poli-ɛ-caprolactona) + PHB (Poli-hidroxibutirato)
Keywords in Portuguese
Biodegradáveis
Bovino
Dispositivo
Farmacocinética
Polímeros
Progesterona
Abstract in Portuguese
No Brasil, o uso da Inseminação Artificial em tempo fixo (IATF) vem crescendo rapidamente, uma vez que elimina a necessidade de observação do cio e induz a ciclicidade de vacas em anestro (MADUREIRA et al., 2004). Na maioria dos protocolos de IATF, empregam-se dispositivos de liberação sustentada de progesterona (P4) introduzidos na cavidade vaginal. Estes dispositivos são, na sua grande maioria, importados e confeccionados com uma armação de nylon, recoberta com silicone e progesterona. Visando a diminuição dos custos de produção e impacto ambiental, Pimentel (2006) confeccionaram dispositivos vaginais de liberação sustentada de progesterona, empregando uma mistura biopolimérica de PHB (Poli-hidroxibutirato) e PCL (poli-ɛ-caprolactona), para utilização no controle farmacológico do ciclo estral de vacas. No presente trabalho, foi estudado o mecanismo pelo qual, a progesterona é liberada da mistura biopolimérica (PHB46%+PCL46%+P48%). Para o estudo da cinética de liberação de P4 foram utilizados dispositivos (n=21) para experimento in vivo, onde foram introduzidos na cavidade vaginal das vacas e coletados a cada 24 horas durante 7 dias. Para experimentos in vitro foram utilizados 12 dispositivos que foram colocados em dissolutor de comprimidos e foram retirados em triplicata a cada 24 horas por 4 dias. Foi realizado experimento para avaliação da distribuição e quantidade de P4 em dispositivos de duas partidas diferentes em diversos pontos. A cinética de liberação de 4 tipos de dispositivos compostos de PHB+PCL+P4+ IrganoxB215® adicionados ou não de um protetor anti raios ultra violeta ( Tinuvin®) foi avaliada. Foi observado que a cinética de liberação de P4 se comportou de forma diferente entre sistemas in vivo e in vitro; em sistema in vivo foi de forma linear (R2=0,929), sugerindo que a progesterona possa ser liberada de acordo com o mecanismo de ordem zero e in vitro a liberação pode ser explicada pelo modelo matemático de Higuchi (R2=0,99) com o coeficiente de difusão calculado conforme a segunda lei de Fick foi de 2,09 x10-8 (cm2/s). Observou-se que a P4 no dispositivo está distribuída uniformemente (P= 0,519) e que aditivos e diferentes proporções de PHB+PCL não influenciaram a liberação de P4 por um período de 96 horas de testes in vitro.
Title in English
Release kinetics of progesterone in devices made from blends with PCL (Poly-ɛ-caprolactone) + PHB (poly-hydroxybutyrate)
Keywords in English
Biodegradable
Cattle
Device
Pharmacokinetics
Polymers
Progesterone
Abstract in English
In Brazil, the use of fixed-time artificial insemination (TAI) has been growing rapidly since it eliminates the need for estrus detection and induce cyclicity in anestrous cows (MADUREIRA et al., 2004). In most TAI protocols, devices are employed for the sustained release of progesterone (P4) introduced into the vaginal cavity. These devices are mostly imported and made with a nylon frame, covered with silicone and progesterone. Seeking to reduce production costs and environmental impact, Pimentel (2006) crafted devices for the sustained release vaginal progesterone, using a mixture biopolymer PHB (poly-hydroxybutyrate) and PCL (poly-ɛ-caprolactone), for use in pharmacological control estrous cycle of cows. In the present work was to study the mechanism by which the progesterone is released from the mixture biopolymers (PHB46 PCL46% +% +% P48). To study the kinetics of release of P4 device was used (n = 21) for in vivo experiment, where they were introduced into the vaginal cavity of cows and collected every 24 hours for 7 days. For in vitro experiments were used 12 devices were placed in dissolutor tablets and were taken in triplicate every 24 hours for 4 days. Experiment was conducted to assess the distribution and amount of P4 in two matches and different devices on several points. The release kinetics of four types of devices composed of PHB + PCL + P4 + IrganoxB215 ®, added to a protective anti ultraviolet rays (Tinuvin ®) was evaluated. It was observed that the kinetics of release of P4 behaved differently between systems in vivo and in vitro, the in vivo system was linear (R2 = 0.929), suggesting that progesterone may be released according to the mechanism of order zero and in vitro release can be explained by the mathematical model of Higuchi (R2 = 0.99) with the diffusion coefficient calculated according to Fick's second law was 2.09 x10-8 (cm2 / s). It was noted that a P4 is evenly distributed on the device (P = 0.519) and additives that different proportions of PHB and PCL + did not influence the release of P4for a period of 96 hours of in vitro tests.
 
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Publishing Date
2013-04-17
 
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