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HORMONE RELEASING DRUG DELIVERY SYSTEMS Presented by:- manchireddy praveen reddy M.Pharm. – 1st Year Dept. of Pharmaceutics Jsscp mysore. . SUBMITTED TO: Dr. Hemanth kumar yadav, Lecturer ,Dept of pharmaceutics, JSSCP ,Mysore .

Hormone releasing IUDs ::

Tuesday, March 06, 2012 2 Hormone releasing IUDs : Doyle and Clewe first initiated the use of hormone releasing iuds. Scommegna et al in 1970 carried human testing using conventional iud having contraceptive steroids. A T-shaped progesterone releasing iud having vertical limb embedded with drug-containing silicone capsule was evolved. Coated with polymer for achieving slower release.

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Tuesday, March 06, 2012 3 Progestasert : a novel progesterone releasing iud. The device has a solid poly EVA side arms and a hollow core. The microcrystalline Pg is suspended in the core in the silicone oil with BaS. Dimensions-0.25mm thick, release by diffusion through rate limiting membrane. Loaded with 38mg of Pg, release rate 65 mcg/day Approved by USFDA in 1975 for 12 month contraceptive use. Preg. rate 1.8/100 for parous and 2.5/100 for nulliparous.

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Tuesday, March 06, 2012 4 Does not inhibit ovulation but interfere with implantation in endometrium, thickening of cervical mucus. Advantages : Increased effectiveness, lower menstrual blood flow, decreased dysmenorrhea. Disadvantages: Need to be replaced yearly, intermenstrual bleeding, ectopic pregnancies.

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Tuesday, March 06, 2012 5 Antifertility action of progesterone releasing IUDs: They diminish sperm transport through the cervix to the oviduct by increasing the thickness of the cervical mucous. Steroid releasing devices induce progestational changes that result in endometrial gland atrophy and inhibit further development of the ova.

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Tuesday, March 06, 2012 6 Endometrial hypermaturation is unfavorable for implantation of a blastocyst. This is associated with decidual formation induced by progesterone. Effect of estrogen-progesterone system is related to the presence of a membrane electrical potential that inhibits the ovum-endometrium contact before the occurrence of implantations.

Biopharmaceutics of intrauterine progesterone administration: :

Tuesday, March 06, 2012 7 Biopharmaceutics of intrauterine progesterone administration: Intrauterine administration was compared with oral delivery and subcutanous injection. Progesterone administered I U shows 45 times greater bioavailability than the other 2 routes. Apparently the endometrium tissue is extremely effective for progesterone absorption.

Clinical effectiveness ::

Clinical effectiveness : Contraceptive efficacy was related with daily dose of progesterone release from device. dose mcg/day % pregnancy 10 5.2 25 2.7 65 1.1 120 0.6 8 Tuesday, March 06, 2012

Levonorgesterol releasing IUD ::

Tuesday, March 06, 2012 9 Levonorgesterol releasing IUD : These carry levonorgestrel releasing device [MIRENA]. It is an intrauterine system (LNG_IUS) that has sleeves of levenorgestrel 52 mg around its stem. It is composed of a polyethylene stem covered by matrix Silastin:LNg (2:1) and side arms. Releasing 20 mcg/day and lasting for at least 5 years. Initial fast release then at 60 % drug release rate reduces to 16mcg/day. Suppresses endometrium and ovulation. Also, unlike other IUDs, it may reduce the risk of (PID) .

Mode of action ::

Tuesday, March 06, 2012 10 Prevents fertilization by damaging or killing sperm and making the mucus thick and sticky, so sperm can't get through to the uterus. It also keeps endometrium from growing very thick, making lining a poor place for a fertilized egg to implant and grow. It may relieve irregular menstrual bleeding and cramping. Mode of action :

Disadvantages of LNg iud ::

Tuesday, March 06, 2012 11 Disadvantages of LNg iud : It may cause noncancerous (benign) growths called ovarian cysts, which usually go away on their own. It can cause hormonal side effects, such as breast tenderness, mood swings, headaches, and acne. When side effects do happen, they usually go away after the first few months. And general side effects associated with iuds.


References Y.W.Chein; Novel Drug Delivery Systems, 2 nd ed., vol.50, pg.no.585-629. Mathiowitz, Encyclopedia of Controlled Drug Delivery, Vol-I, pg.no.365-370. N.K. Jain, Advances in Controlled and Novel Drug Delivery, 1 st ed, pg.no.585-625. www.wikipedia.com 6 March 2012 12

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