This document provides information about intrauterine drug delivery systems (IUDs). It discusses the anatomy and physiology of the female reproductive system. It describes the types of IUDs including non-hormonal copper IUDs and hormonal IUDs like Progestasert that release progesterone. The advantages of IUDs include avoiding first-pass metabolism and providing localized drug delivery. Applications of IUDs include emergency contraception, treatment for heavy menstrual bleeding and menopausal hormone therapy.
Himalayan Institute Research on Intrauterine Drug Delivery Systems
1. HIMALAYAN INSTITUTE OF PHARMACY & RESEARCH
PRESENTATION
ON
INTRAUTERINE DRUG DELIVERY SYSTEMS
Rajawala Road, Selakui, Uttarakhand 248007
SUBMITTED TO:
SALONI JAISWAL
SUBMITTED BY:
ANISHU RAHMAN SHEK
Bachelor of Pharmacy(4th year)
Uttarakhand Technical University
2. CONTENTS
1. Introduction
2. Anatomy & Physiology of female reproductive system
3. Intrauterine DDS
4. Advantages & Disadvantages
5. Development of intra uterine devices(IUDs)
6. Application of intra uterine devices
3. Introduction
. Vagina and Uterus are the route for administration of
contraceptives, antifungals and antimicrobials.
.These are used for local or systemic absorption .Because of vast
network of blood vessels, vaginal wall is suitable for dug
absorption.
.The rate and extent of drug absorption may vary depends upon
1) Formulation factors
2) Physiology
3) Age of patient
4) Menstrual cycle
4.
5. Vulva
Basic 5 parts involved:
• Mons pubis
• Labia majora
• Labia minora
• Clitoris
• vestibules
Vagina
• Muscular canal about 3 inches long.
• Normal pH of vagina in premenopausal female ranges
from 4.5 & rises upto 7 in postmenopausal female.
• Vaginal wall surface is covered with epithelium cells.
• Size: in premenopausal female 7.8 cm in length & 2 cm
wide, in postmenopausal female 45 cm in length &
1-1.5cm in width.
6. Uterus
• Non pregnant uterus is around 7.5cm long,
wide and 2.5cm thick.
• Endometrium is highly vascular made up of simple
columnar epithelium and highly sensitive to
hormonal secretions of ovary.
• During complete cycle endometrium goes
on thickening with hormonal impact.
Fallopian tubes
• Also called 'Oviducts' or ‘Uterine tubes’ around
10 cm long.
• The end portion is opened and funnel shaped
containing finger like projection called "Fimbriae".
• Internal surface is of ciliated columnar epithelium
cells.
7. Ovary
•Two ovaries, one on either side of the
uterus.
•These are having shape and size of
unshelled almonds.
•There are ovarian follicles containing
oocytes in various stages of development.
•OvaryMatured follicle which releases secondary oocyte is called
Graafian follicle.
•Ovaries produces hormones including progesterone and
estrogen, inhibin and relaxin.
Intrauterine DDS (IUDs)
An IntraUterine System (IUS) or IntraUterine Drug Delivery System
(IUDDS) is a small object that is placed inside the uterus above the
endometrium and is active or medicated when it contains a
therapeutic agent. This system is a combination of drug/device that
slowly releases the active ingredient
8. Types of IUDs for controlled drug delivery:
1) Non-hormonal IUDs. (Ex. copper-T, copper-7)
2) Hormonal IUDs. (Ex. Progestasert)
1) Non-hormonal IUDs/ copper medicated IUDs.
• It is consists of polyethylene or polypropylene plastic
support of number-7 or letter-T with certain amount
of pure electrolytic copper wire wound around them.
• Copper is cytotoxic and enhance spermicidal &
spermatodepressive action of IUD.
• The exposed surface area of copper is 380 mm²
• T-shaped IUD is popular since shape conforms to the
uterine cavity which resists displacement & rotation
within cavity and expulsion from cavity
• Types- Cu T-200-200 mm².
Cu T-30-30 mm².
Mechnasim of Action:- They work by changing the
lining of the uterus and fallopian tubes affecting the
movements of eggs and sperm and so that fertilization does not
occur
9. 2) Hormonal IUDs.
• T-shaped device made of polyethylene frame
that measures 32 mm in both vertical and
horizontal direction.
• There is silicone reservoir containing dispersed
levonogestrel or progesterone on vertical stem
and further enclosed in a sleeve of rate.
controlling membrane of ethylene-vinyl copolymer.
• It prevents pregnancy up to 5 yrs by steadily
releasing small amount of progesterone directly
in to uterus.
• It works by thickening the cervical mucous so
that sperm have more difficulty to swim through uterus.
For some women it may also prevent ovulation from occurring.
10. Advantages
• Minimal systemic side effects.
• Irritation to the stomach and small intestine associated with
some drugs can be avoided.
• An increase in bioavailability.
• First pass metabolism can be avoided.
• Contact with digestive fluid is avoided, thereby preventing
enzymatic degradation of some drugs.
• Self medication is possible.
• Drug delivery can be stopped by removing the dosage form. E.g.
vaginal rings
• Rapid drug absorption and quick onset of action can be achieved.
• The vaginal bioavailability of smaller drug molecule is good.
• The bioavailability of larger drug molecules can be improved by
means of absorption enhancer.
11. Disadvantages
• Patient incompliance.
• Only few drugs are administered by this route.
• Some of the drugs are sensitive at the vaginal pH.
• Local irritation because some drugs variability in drug absorption
related with menstrual cycle, menopause and pregnancy.
• Gender specificity.
• Influence with sexual intercourse.
• Some time leakage of drugs from vagina and wetting of
undergarments.
12. Development of IUDS
• Development of IUDs began in the 1920s, with the first generation
of IUDs constructed from silkworm gut and flexible metal wire.
Eg- Grafenberg star and Ota ring.
• Fell into disrepute because of the difficulty of insertion. the need
for frequent removal as a result of pain and bleeding
• Subsequently, plastic IUDs of varying shapes and sizes were
made available.
• Various inert, biocompatible, polymeric materials such as
polyethylene, EVAC, and silicone elastomer were widely used to
construct IUDs
13. • Zipper 1968 added contraceptive metals (Cu) and Doyle and
Clewe developed progestin - releasing IUD.
• This development initiated a new era of R & D for long term I. U.
contraception, leading to generation of recent IUDs - the medicated
IUDs.
• Copper bearing IUDs, such as Cu - 7, and progesterone releasing IUDs,
such as
Progestasert (approve by US FDA in 1976), thus evolved.
14. Types of IUDS
A. Non-medicated IUDs:
i) These IUDs exert their contraceptive action by producing
a sterile inflammatory response in the endometrium by its
mechanical interaction.
ii) These do not contain any therapeutic agent
e.g. ring shaped IUDs of s.s., plastic IUDs, lippes loop, Dalkon
shield, Saf-T-Coil.
B Medicated IUDs:
i) These IUDS are of delivering capable pharmacologically
active antifertility agents.
ii) e.g. copper bearing IUD, progesterone releasing IUD.
15. There are two types of medicated IUDs:-
1)Copper bearing IUDs:-
i) This devices uses copper wire wound to the stem.
ii) The device is made of T shaped polyethylene plastic.
iii) There are various grades as per the surface area of the cu-wire
such as Cu-T-30, Cu-T-200, Cu-T-380
2. Hormone releasing IUDs
i) Progestasert:
a novel progesterone releasing IUD.
ii) Dimensions-0.25mm thick, release by diffusion through rate
limiting membrane.
iii) Loaded with 38mg of Progesterone, release rate 65 mcg/day
iv) Approved by USFDA in 1975 for 12 month contraceptive use.
v) Pregnancy rate 1.8/100 for parous women and 2.5/100 for
nulliparous women.
16. Applications of IUDs
1) Emergency Contraception: The copper IUD (marketed as
Paraguard) can be inserted within 5 days after unprotected
intercourse.
2) Treatment for Heavy Menstrual Bleeding: The
progesterone IUD (marketed as Mirena) is used to reduce heavy
menstrual bleeding. It is proved to be better than oral
progesterone pills.
3) Menopausal Hormone Therapy: Mirena is an alternative
method for ancy rate of delivering progesterone of combined
menopausal hormone replacement therapy.
4) Treatment for Pelvic Pain: Some studies reveal that
Mirena IUD reduces DA approved pelvic pain associated to
endometriosis.