Vaginal Drug Delivery Systems PDF

1 used for Vaginal Drug Delivery systems → contraception , ↳ suitable for not systemic...

1 used for Vaginal Drug Delivery systems → contraception , ↳ suitable for not systemic menopause - thick C little % reaches the circulation] - menstruation , the membrane will shed t so its a local route  Intravaginal Delivery Systems 2 contraception 1- menopause ¨ Vaginal rings reservoirs for a period of time - good long ¨ Intrauterine device (IUD) ¨ Vaginal Insert matrix > ¨ Vaginal gels → for short time couple hours ) ↳ can be used for controlledreleasebut  Intravaginal delivery systems 3 ¨ Advantages inserts to some extent ¤ Self insertion and removal (e.g. rings) gets + + ¤ Continuous administration at an effective dose level (zero order release especially with rings) can be first order depends on → → the system ¤ Minimum systemic toxicity (local effect in the vagina) is oral ¤ Good patient compliance drugs circulate through whole ↳ sustained release to reach the body vagina and cause an ellett - side effects  Types of Intravaginal delivery 4 systems I. Reservoir: drug surrounded by the polymeric membrane - through the membrane ¤ Membrane-controlled (diffusion design) C everything constant is → zero ¤ Constant rate of drug release polymer controls the rate - of release ¤ The required daily dose > → suspension → contrast suspension but in a liquid  Hormonal Intrauterine DDS 15 ¨ Mirena ¤ Levonorgestrel (synthetic progestogen)-releasing intrauterine device ¤ Contains 52 mg (Mirena), 19.5 mg (Kyleena), or 13.5 mg (Skyla) ¤ Use: É¥¥* n Provides contraception for 5 years n Treats heavy periods - more ✓ flexible twisted foaraministration  Intrauterine Progesterone DDS 16 ¨ Release in the uterine cavity provide a local rather than a systemic action. ¨ Readily absorbed into uterine epithelium Local → ¨ Systemic progesterone absorption is low ¨ Mechanism of action ¤ Increase the cervical mucus thickness (reduce sperm motility and survival). ¤ Changes the lining of the uterus (prevent implantation and egg fertilization).  Intrauterine Progesterone DDS 17 determines the location d ¨ A small string hangs down from the IUD into the upper part of the vagina and is used to periodically check the device. ¤ A shorter-than-normal string can be a warning sign of an embedded (pushed in) IUD.  Intrauterine Progesterone DDS 18 ¨ Contents → suspension ¤ Progesterone suspended in silicone oil formulation ¤ Barium sulfate to make radiopaque. ¤ Ethyl vinyl acetate (EVA) membrane surrounding the drug core controls the drug release. ¤ Titanium dioxide is added to EVA for white color ¨ At the end of the year, the device will contain excess progesterone à to maintain the thermodynamic activity of the drug reservoir b to maintain the zero order release Cto prevent the release from )  IUD Insertion 19 "" t " →wiupass wings device is pushed out cervix - adjust q the distance https://www.acog.org/programs/long-acting-reversible-contraception-larc/video-series/insertion/mirena  IUD Insertion & Removal 20 Loom the cervix  Intrauterine Progesterone DDS 21 ¨ Advantages , already foundin our body ¤ Using a natural hormone have side elleets ¤ Contains no estrogen - ¤ Using a T-shaped delivery that ensures ↳ n comfort sits in the uterus ( same shape nicely of it] n safety retained in place n retention < Locally to the site of action n êê irritation g ellects ( less side ¤ Confine hormonal action to the uterus compared to oral ]  Failure rate range Failure rate range Method used (over 12 months) Method used (over 12 months) in clinical studies (%) in clinical studies (%) None 78–94 Oral contraceptive Spermicides 0.3–37 Estrogen and progestin 0–6 Periodic abstinence 13–35 Progestin only 1–10 Withdrawal 7–22 Injection 0–0.3 Medroxyprogesterone Cervical cap with spermicide 6–27 injection (90-day) Diaphragm with spermicide 2–23 Implants Levonorgestrel implant Condom without spermicide 2–14 Six capsules 0–0.09 IUD Progesterone-releasing 1.9–2.0 Two rods 0–0.2 Sterilization Copper-T 200 3.0–3.6 Female 0–8 Copper-T 200Ag 0–1.2 Male 0–0.5 Copper-T 220C 0.9–1.8 Copper-T 380A 0.5–0.8 Copper-T 380S 0.9 22  short-term Vaginal Inserts - administration 23 Cervidil® (Forest Lab) ¨ Composed of ¤ Slab: thick, flat, rectangular, buff- colored semitransparent polymeric hydrogel containing dinoprostone - ✓ (prostaglandin E2). dissolves reeeasingtredhlg d below the ¤ Retrieval system cervix CIM n A pouch of knitted polyester enclosing the slab vagina) n Attached to a long knitted strap used to retrieve the insert 0 once they d get hydrated - medication is here theyformedwyarogd  Vaginal Insert 24 ¨ Uses ¤ For labor induction by initiation and/or continuation of cervical ripening “softening” (ê need for oxytocin) ¤ For second trimester abortion has limitations → ¨ The drug is dispersed in a polyethylene oxide matrix and released at a rate of about 0.3 mg/hr ¨ Mechanism: In moist environment à the unit absorbs water à swells and release dinoprostone in a controlled manner (swelling dissolving matrix design) ↳ if drug soluble then its by diffusion too is if drug is insoluble → dissolution only  Vaginal Insert 25 ¨ Instructions ¤ 1 unit is inserted and removed upon induction of active labor ¤ The patient must be supine for 2 hr after administration ¨ Storage ¤ -20oC → forstability ¤ It is hygroscopic and properties of the drug may be altered if stored improperly  Vaginal Gel → has to be biodegradable insoluble , polymer. 26 stones Crinone® Gel (Wyeth-Ayerst) ¨ A bioadhesive vaginal gel with extended action. ¨ Composition: ¤ Micronized progesterone ¤ Polycarbophil: water insoluble applicator < %swellable and adhesive polymer (fiber) soinsoluble → getis ¤ O/W emulsion of the drug (carrier polymer there vehicle). ¨ Mechanism: ¤ The polymer is insoluble in water à swells in the vagina à forms adhesi@ bioadhesive gel coating the walls of to the vagina. Mikasa ¤ The gel stays attached to the vaginal vagina walls for a few days as the progesterone is absorbed.  Vaginal Gel 27 ¨ Uses ¤ Assist in reproduction in infertile women with progesterone deficiency (supplemental) – used twice daily ¤ Amenorrhea (absence of menstruation) – used every other day ¨ The female hormone progesterone is one of the hormones essential for preparation of the uterus for implantation and maintenance of a pregnancy. ¨ Applied using the supplied applicator.