Treatment and prevention of benign breast disease with 4-hydroxy tamoxifen
A technology for hydroxy tamoxifen and breast diseases, applied in diseases, endocrine system diseases, organic active ingredients, etc., can solve problems such as increased risk of breast cancer
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Embodiment 1
[0057] Example 1: Verification of transdermal release of 4-hydroxy tamoxifen
[0058] [ 3 An alcohol solution of H]-4-hydroxy tamoxifen was applied directly to the breasts of four breast cancer patients. After surgery, both the resected tissue and the breast tissue surrounding the tumor are radiosuppressed (Kuttenn et al., 1985).
[0059] In a follow-up study, 9 of 12 patients scheduled for surgical resection of hormone-dependent breast cancer received Z-[ 3 H]4-hydroxy tamoxifen (80μCi) treatment, 3 received Z-[ 3 Treatment with H]-tamoxifen (80 μCi) was used for comparison. [ 3 H]-labeled drug is applied directly to the patient's diseased breast. Three areas of breast tissue—the tumor, the tissue immediately surrounding the tumor, and normal tissue—were excised and immediately frozen in liquid nitrogen. In addition, plasma and urine samples were obtained at predetermined intervals and frozen for analysis.
[0060] Table 2 shows the analysis results. 4-Hydroxy tamoxif...
Embodiment 2
[0068] Example 2: Pharmacokinetic and pharmacodynamic verification of transdermally administered 4-hydroxy tamoxifen compared to oral administration of 20 mg tamoxifen
[0069] This study compared tissue and plasma concentrations of 4-hydroxy tamoxifen after transdermal administration of a hydroalcoholic gel to those after oral tamoxifen (Pujol, 1995).
[0070] Thirty-one patients scheduled for breast cancer surgery were randomly assigned to 1 of 5 groups. As listed in Table 3, they were treated with either oral tamoxifen or transdermal 4-hydroxy tamoxifen. Treatment was performed daily for 3-4 weeks before surgery. The study evaluated three different doses of 4-hydroxy tamoxifen (0.5, 1, or 2 mg / day) and two-area application (applied to both breasts or to a large skin surface including arms, forearms, and shoulders). ). A group of patients received oral tamoxifen (Nolvaldex ) 20mg / day (10mg each time, twice a day) treatment.
[0071] Group
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Embodiment 3
[0087] Example 3: Tolerance and pharmacokinetic verification of transdermal administration of 4-hydroxy tamoxifen to healthy women
[0088] This study demonstrates the tolerability and pharmacokinetics of topically applied 4-hydroxytamoxifen gel in healthy premenopausal women aged 18-45 years. Each participant applied the gel on each day of two menstrual cycles.
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