We prepared, characterized and studied the biodistribution of tamoxifen citrate (TMX) loaded cross-linked guar gum (GG) nanoparticles (NPs). NPs were prepared via a single step emulsion process and particle size evalu...We prepared, characterized and studied the biodistribution of tamoxifen citrate (TMX) loaded cross-linked guar gum (GG) nanoparticles (NPs). NPs were prepared via a single step emulsion process and particle size evaluated. The extent of tissue distribution and retention following oral administration of TMX loaded GG NPs and TMX tablet in female albino mice was analyzed over a period of 48 hours. Till 48 hours, the particles remained detectable in both mammary and ovary tissue (estrogen receptors). Uptake and retention of TMX from NPs and tablet in mammary gland and ovary tissue changed with time. Results showed that the uptake and retention of NPs was more in the mammary gland between 24 - 48 hours (11.2% at 24 h;4.65% at 48 h). As mammary gland is the target organ in breast cancer therapy, it may be concluded that the cross-linked GG NPs are capable of releasing the drug at the target and minimize the uptake and retention in non target tissue, the ovary (7.98% at 24 h;1.9% at 48 h). Serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) with time were measured. No abnormal changes in the liver enzymes were observed. GG NPs under study can be used as a drug carrier system for treating cancer.展开更多
Objective To assess the effect of treatment with a combination of the tamoxifen citrate and testosterone undecanoate on sperm variables in men with idiopathic azoospermia or oIigozoospermia. Methods Four men with idio...Objective To assess the effect of treatment with a combination of the tamoxifen citrate and testosterone undecanoate on sperm variables in men with idiopathic azoospermia or oIigozoospermia. Methods Four men with idiopathic azoospermia and 8 men with idiopathic oligozoospermia were collected in this retrospective and self control trial. All patients were treated with testosterone undecanoate of 80 mg/d and tamoxifen citrate of 20 mg/d. Sperm characteristics and pregnancy incidence were measured every month during 4 months medication. Results Tamoxifen citrate plus testosterone undecanoate treatment produced a satisfactory improvement of total sperm number, motility after 2 and 3 months whereas serum FSH, LH levels increased after 2 or 3 months. Conclusion The combination of tamoxifen citrate with testosterone undecanoate could improve significantly sperm count. The combination could be used in men with idiopathic azoospermia or serious oligozoospermia.展开更多
The syntheses and HPLC analysis of N-desmethyltamoxifen and carbon11 labelled tamoxifen are described.In order to obtain the N-desmethyltamoxifen,tamoxifen citrate was first converted to tamoxifen free base.N-desmethy...The syntheses and HPLC analysis of N-desmethyltamoxifen and carbon11 labelled tamoxifen are described.In order to obtain the N-desmethyltamoxifen,tamoxifen citrate was first converted to tamoxifen free base.N-desmethyltamoxifen was prepared by reacting tamoxifen free base with 1-chloroethyl-chloroformate(ACE.C1). For ^11C labeling,N-desmethyltamoxifen was heated with ^11C methyl iodide for 10min at 130℃,and the 11C labelled compund was purified by HPLC on a μBonapak TM C18 column,Injectable ^11C-tamoxifen was obtained within 50-60 min from EOB (end-of -bombardment)with a labeling yield of 60%-70%.展开更多
文摘We prepared, characterized and studied the biodistribution of tamoxifen citrate (TMX) loaded cross-linked guar gum (GG) nanoparticles (NPs). NPs were prepared via a single step emulsion process and particle size evaluated. The extent of tissue distribution and retention following oral administration of TMX loaded GG NPs and TMX tablet in female albino mice was analyzed over a period of 48 hours. Till 48 hours, the particles remained detectable in both mammary and ovary tissue (estrogen receptors). Uptake and retention of TMX from NPs and tablet in mammary gland and ovary tissue changed with time. Results showed that the uptake and retention of NPs was more in the mammary gland between 24 - 48 hours (11.2% at 24 h;4.65% at 48 h). As mammary gland is the target organ in breast cancer therapy, it may be concluded that the cross-linked GG NPs are capable of releasing the drug at the target and minimize the uptake and retention in non target tissue, the ovary (7.98% at 24 h;1.9% at 48 h). Serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) with time were measured. No abnormal changes in the liver enzymes were observed. GG NPs under study can be used as a drug carrier system for treating cancer.
文摘Objective To assess the effect of treatment with a combination of the tamoxifen citrate and testosterone undecanoate on sperm variables in men with idiopathic azoospermia or oIigozoospermia. Methods Four men with idiopathic azoospermia and 8 men with idiopathic oligozoospermia were collected in this retrospective and self control trial. All patients were treated with testosterone undecanoate of 80 mg/d and tamoxifen citrate of 20 mg/d. Sperm characteristics and pregnancy incidence were measured every month during 4 months medication. Results Tamoxifen citrate plus testosterone undecanoate treatment produced a satisfactory improvement of total sperm number, motility after 2 and 3 months whereas serum FSH, LH levels increased after 2 or 3 months. Conclusion The combination of tamoxifen citrate with testosterone undecanoate could improve significantly sperm count. The combination could be used in men with idiopathic azoospermia or serious oligozoospermia.
文摘The syntheses and HPLC analysis of N-desmethyltamoxifen and carbon11 labelled tamoxifen are described.In order to obtain the N-desmethyltamoxifen,tamoxifen citrate was first converted to tamoxifen free base.N-desmethyltamoxifen was prepared by reacting tamoxifen free base with 1-chloroethyl-chloroformate(ACE.C1). For ^11C labeling,N-desmethyltamoxifen was heated with ^11C methyl iodide for 10min at 130℃,and the 11C labelled compund was purified by HPLC on a μBonapak TM C18 column,Injectable ^11C-tamoxifen was obtained within 50-60 min from EOB (end-of -bombardment)with a labeling yield of 60%-70%.
