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充液硅橡胶胶囊:一种实现更稳定甾体药物递送系统的新方法。

Fluid-filled silastic capsules : a new approach to a more constant steroidal drug delivery system.

作者信息

Kumar D, Farooq A, Laumas K R

出版信息

Contraception. 1981 Mar;23(3):261-8. doi: 10.1016/0010-7824(81)90048-2.

DOI:10.1016/0010-7824(81)90048-2
PMID:7238045
Abstract

A new approach to a more constant steroid delivery system was made in which 7,9 mg of norethisterone acetate was shaped into a cylindrical pellet (diameter 1.47 mm, length 4 mm) and placed inside a silastic capsule (i.d. 1.57 mm, o.d. 3.18 mm) of 5 mm effective length. The extra space available around the pellet was filled with physiological saline. For the sake of comparison, the same amount of crystalline norethisterone acetate was packed up to 5 mm length inside a silastic capsule of the same dimensions. The incorporation of fluid (saline) in the system not only caused a marked decrease in the initial high release but also a more constant release. Varying the pellet diameter showed that release of the steroid increases with the increase in surface area of the pellet.

摘要

人们研发出一种新方法来构建更稳定的类固醇给药系统,即将7.9毫克醋酸炔诺酮制成圆柱形药芯(直径1.47毫米,长度4毫米),并置于有效长度为5毫米的硅橡胶胶囊(内径1.57毫米,外径3.18毫米)内。药芯周围的多余空间填充有生理盐水。为作比较,将相同量的结晶醋酸炔诺酮装入相同尺寸的硅橡胶胶囊内,长度达5毫米。系统中加入液体(生理盐水)不仅使最初的高释放量显著降低,而且释放更加稳定。改变药芯直径表明,类固醇的释放量随药芯表面积的增加而增加。

相似文献

1
Fluid-filled silastic capsules : a new approach to a more constant steroidal drug delivery system.充液硅橡胶胶囊:一种实现更稳定甾体药物递送系统的新方法。
Contraception. 1981 Mar;23(3):261-8. doi: 10.1016/0010-7824(81)90048-2.
2
Bioavailability of norethindrone in rabbits after administration of norethindrone acetate in single, double and quadruple doses released through subcutaneous silastic implants.通过皮下硅橡胶植入物以单剂量、双剂量和四倍剂量释放醋酸炔诺酮后,家兔体内炔诺酮的生物利用度。
Endocrinol Jpn. 1980 Oct;27(5):653-8. doi: 10.1507/endocrj1954.27.653.
3
Steroid release from silastic capsules and rods.类固醇从硅橡胶胶囊和棒中的释放。
Contraception. 1978 Oct;18(4):367-94. doi: 10.1016/0010-7824(78)90024-0.
4
Local tissue response to silastic implant containing norethindrone acetate in women.女性对含醋酸炔诺酮的硅橡胶植入物的局部组织反应。
Contraception. 1977 Jan;15(1):39-51. doi: 10.1016/0010-7824(77)90036-1.
5
Long-term contraception by steroid-releasing implants. II. A preliminary report on long-term contraception by a single silastic implant containing norethindrone acetate (ENTA) in women.含甾体缓释植入剂的长效避孕法。II. 关于含醋酸炔诺酮(ENTA)的单根硅橡胶植入剂用于女性长效避孕的初步报告。
Contraception. 1975 May;11(5):505-21. doi: 10.1016/0010-7824(75)90105-5.
6
Effect of norethisterone enanthate subdermal silastic implants on luteal function in rabbits.庚炔诺酮皮下硅橡胶植入物对兔黄体功能的影响。
Endokrinologie. 1982 Jul;80(1):52-5.
7
Plasma levels of norethisterone in women with subcutaneous implants of norethisterone acetate.接受醋酸炔诺酮皮下植入的女性的血浆炔诺酮水平。
Indian J Med Res. 1979 Oct;70:625-31.
8
Radioimmunoassay of norethindrone : serum levels of norethindrone in lactating women after insertion of a single Silastic implant releasing norethindrone acetate.炔诺酮的放射免疫分析:插入单个释放醋酸炔诺酮的硅橡胶植入物后哺乳期妇女血清中炔诺酮的水平。
Contraception. 1978 Dec;18(6):593-605. doi: 10.1016/0010-7824(78)90044-6.
9
Effect of norethisterone enanthate subdermal silastic implants on the ovary & uterus of adult rabbits.庚酸炔诺酮皮下硅橡胶植入物对成年兔卵巢和子宫的影响。
Indian J Exp Biol. 1980 Nov;18(11):1221-4.
10
Correlation between the serum norethindrone (NET) levels attained after insertion of a silastic implant releasing norethindrone acetate and the endogenous hormones particularly progesterone.插入释放醋酸炔诺酮的硅橡胶植入物后所达到的血清炔诺酮(NET)水平与内源性激素尤其是孕酮之间的相关性。
Contraception. 1981 Feb;23(2):211-25. doi: 10.1016/0010-7824(81)90106-2.

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Single neonatal estrogen implant sterilizes female animals by decreasing hypothalamic KISS1 expression.单个新生雌性激素植入物通过减少下丘脑 KISS1 表达来使雌性动物绝育。
Sci Rep. 2023 Jun 14;13(1):9627. doi: 10.1038/s41598-023-36727-8.
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Pharmacokinetic comparison of three delivery systems for subcutaneous testosterone administration in female mice.
三种皮下睾酮给药系统在雌性小鼠中的药代动力学比较。
Gen Comp Endocrinol. 2022 Oct 1;327:114090. doi: 10.1016/j.ygcen.2022.114090. Epub 2022 Jun 24.
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Local delivery of hormonal therapy with silastic tubing for prevention and treatment of breast cancer.硅橡胶管局部递药用于预防和治疗乳腺癌的激素治疗。
Sci Rep. 2018 Jan 8;8(1):92. doi: 10.1038/s41598-017-18436-1.
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Skin Diseases in Laboratory Mice: Approaches to Drug Target Identification and Efficacy Screening.实验小鼠的皮肤病:药物靶点识别与疗效筛选方法
Methods Mol Biol. 2016;1438:199-224. doi: 10.1007/978-1-4939-3661-8_12.