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2.
Int J Pharm ; 382(1-2): 98-103, 2009 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-19699285

RESUMO

Latex, a polyisoprene (PI) hydrophobic elastomer, was evaluated in vitro and in vivo as a matrix for intravaginal steroid hormone delivery. Matrices containing hormone were prepared by swelling latex in chloroform that contained soluble progesterone (P4). In vitro studies demonstrate that P4 release from PI follows a zero order model during at least 100 h and depends on initial load up to 10 mg cm(-2). The release of P4 from a PI matrix was found to be two times faster than from a polydimethylsiloxane (PDMS) matrix. FT-IR and X-ray powder diffraction analysis of P4 polymorphs show that when nucleated in PDMS, the hormone crystallizes only in alpha-form while in latex, crystallizes as a mixture of alpha- and beta-form. In vivo studies show that devices with a PI matrix containing 0.5 g of P4 are effective to reach plasma levels above 1 ng ml(-1) that are needed to synchronize estrous in cattle. Altogether, the results show that PI, a vulcanized polymer with a carbon-carbon backbone, can be used as a new matrix for the intravaginal administration of progesterone with improved release profile than silicone and that the matrix can influence the crystalline state of the hormone.


Assuntos
Portadores de Fármacos , Fármacos para a Fertilidade Feminina/administração & dosagem , Látex/química , Progesterona/administração & dosagem , Administração Intravaginal , Animais , Bovinos , Química Farmacêutica , Cristalização , Cristalografia por Raios X , Dimetilpolisiloxanos/química , Composição de Medicamentos , Sincronização do Estro/efeitos dos fármacos , Feminino , Fármacos para a Fertilidade Feminina/sangue , Fármacos para a Fertilidade Feminina/química , Fármacos para a Fertilidade Feminina/farmacocinética , Ovariectomia , Difração de Pó , Progesterona/sangue , Progesterona/química , Progesterona/farmacocinética , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Tecnologia Farmacêutica/métodos
3.
Anim Reprod Sci ; 108(3-4): 356-63, 2008 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-17996407

RESUMO

High temperature vulcanizing silicone elastomers have been widely used in controlled delivery systems of steroid hormones with the aim of controlling estrous cycle in livestock. This paper reports experiments conducted to evaluate the possibility of using room temperature vulcanizing (RTV) silicone elastomers for the intravaginal administration of progesterone to cattle. In vitro studies showed that RTV silicones and high-temperature vulcanizing silicone release progesterone at a similar rate. Y-shaped inserts made of different polymers were designed as supports of RTV silicone sheaths to test the in vivo release of progesterone. Field evaluation showed that RTV silicone sheaths containing 0.75 g of progesterone were at least as effective at estrous synchronization as commercially available intravaginal inserts.


Assuntos
Bovinos/fisiologia , Dimetilpolisiloxanos , Sistemas de Liberação de Medicamentos/veterinária , Sincronização do Estro/métodos , Progesterona/administração & dosagem , Administração Intravaginal , Animais , Preparações de Ação Retardada , Sistemas de Liberação de Medicamentos/métodos , Feminino , Masculino , Gravidez , Progesterona/sangue , Distribuição Aleatória
4.
Theriogenology ; 57(1): 53-72, 2002 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-11775981

RESUMO

Our expanding knowledge of the control of follicular wave dynamics during the bovine estrous cycle has resulted in renewed enthusiasm for the prospects of precisely controlling the follicular and luteal dynamics and finely controlling the time of ovulation. Follicular wave development can be controlled mechanically by ultrasound-guided follicle ablation or hormonally by treatments with GnRH or estradiol and progestogen/progesterone in combination. Treatment of cattle with GnRH in combination with prostaglandin F2 alpha (PGF) 7 d later and a second GnRH 48 h after PGF (known as Ovsynch) has resulted in acceptable pregnancy rates after fixed-time AI in lactating dairy cows and in recipients in which embryos were transferred without estrus detection. Alternatively, treatments with estradiol and progestogen/progesterone-releasing devices resulted in synchronous emergence of a new follicular wave and, when a second estradiol treatment was given 24 h after device removal, synchronous ovulation and high pregnancy rates to fixed-time AI. Self-appointed embryo transfer (without estrus detection) using estradiol and progesterone treatments have resulted in pregnancy rates comparable with those obtained with recipients transferred 7 d after estrus. Furthermore, estradiol and progesterone treatments combined with PGF and eCG (given 1 d after the expected time of wave emergence) have resulted in high rates of recipients selected for transfer (84.6%) and an overall pregnancy rate of 48.7% (recipients pregnant/recipients treated). Estradiol and progestogen/progesterone treatments have also been widely used for self-appointed superstimulation protocols with equivalent embryo production to that of donor cows superstimulated using the traditional approach beginning 8 to 12 d after estrus. In summary, exogenous control of luteal and follicular development facilitates the application of assisted reproductive technologies in cattle by offering the possibility of planning the superstimulation of donors and synchronization of recipients at a self-appointed time, without the necessity of estrus detection and without sacrificing results.


Assuntos
Cruzamento/métodos , Bovinos/fisiologia , Transferência Embrionária/veterinária , Folículo Ovariano/fisiologia , Reprodução/efeitos dos fármacos , Animais , Corpo Lúteo/fisiologia , Dinoprosta/farmacologia , Estradiol/farmacologia , Estro , Sincronização do Estro , Feminino , Hormônio Liberador de Gonadotropina/farmacologia , Inseminação Artificial/veterinária , Hormônio Luteinizante/sangue , Ovulação/efeitos dos fármacos , Gravidez , Taxa de Gravidez , Progesterona/farmacologia , Fatores de Tempo
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