Formulations for reproductive health Flashcards
what are the therapetic areas
men:
Erectile dysfunction
Prostate enlargement
Prostatitis
Prostate cancer
women
hypoactive sexual desire disorder
Abortion
Labour induction
Cervicovaginal cancer
both
Contraception
Infertility
Sexually transmitted diseases
Hormone replacement therapy
Routes of drug administration for reproductive health medicines
men:
Intracavernosal injections (penile injections)
Intraurethral applications
women:
Transdermal patches
Intramuscular injections
Vaginal administration
both:
Oral administration
Sub-dermal implantation
what is viagra and what is it used for
A prescription-only medicine used to treat Erectile Dysfunction
Sildenafil citrate is a white crystalline powder with a solubility of 3.5 mg/mL in water
Viagra is formulated as blue, film-coated rounded-diamond-shaped tablets equivalent to 25 mg, 50 mg and 100 mg of sildenafil for oral administration
Excipients:
- microcrystalline cellulose
lactose
anhydrous dibasic calcium phosphate
croscarmellose sodium
magnesium stearate
Hypromellose
titanium dioxide
triacetin,
FD & C Blue #2 aluminum lake
what is Alprostadil (Prostaglandin E1)
for management of erectile dysfunction
Caverject®
Powder for injection with 10 or 20 g of API
The other ingredients:
- lactose
-cyclodextrin
sodium citrate
hydrochloric acid
sodium hydroxide.
The diluent contains water for injections and benzyl alcohol
what is Addyi
medication approved by FDA for the treatment of pre-menopausal women with hypoactive sexual desire disorder (HSDD).
100 mg of flibanserin
Excipients:
lactose monohydrate
microcrystalline cellulose
hypromellose,
croscarmellose sodium, magnesium stearate,
talc,
macrogol,
coloring agents,
titanium dioxide and iron oxide
The contraceptive injection(Depo Provera)
how long does it last for
The injection lasts for 12 weeks (depending on the type)
Sterile aqueous suspension for intramuscular injection
Medroxyprogesterone acetate 400 mg/mLPolyethylene glycol 20.3 mg/mLSodium sulphate anhydrous 11 mg/mL
Myristyl-gamma-picolinium chloride 1.69 mg/mL added as preservative
The contraceptive patch(ORTHO EVRA)
how long does it last
examples
Each patch lasts for one week. The patch should be changed every week for three weeks, then with a week off without a patch
A combination transdermal contraceptive system with a contact surface area of 20 cm²
0.75 mg Ethinylestradiol – a standard ingredient
in most contraceptive pills
6 mg norelgestromin – a progestogen. Its main role is to stop ovulation
name an Combined oral contraceptive pill
(e.g. Rigevidon® )
30µg Ethinylestradiol
150µg Levonorgestrel
The vaginal fluids
The vagina does not possess glands and goblet cells and does not produce mucin. The large amount of fluids secreted by the vagina is composed of cervical secretions (cervical mucus, endometrial and tubal fluids);
The vaginal fluid is hydrophilic and contains mucus, enzymes, enzyme inhibitors, carbohydrates, amino acids, alcohols, etc;
Enzymatic activity is present due to bacterial flora and enzymes in secretions and in the epithelium;
The bioavailability of drugs is dependent on both the effective dissolution of solid drug particles in the vaginal fluids prior to absorption and the degree of deactivation by enzymes present in the fluids.
Vaginal pH
pH in the vagina is controlled primarily by lactic acid produced by L. acidophilus from glycogen;
Vaginal pH in an adult female varies between 4.0 and 5.0, depending on the particular stage of the menstrual cycle;
The lowest pHs are found at mid-cycle and the highest during menstruation;
During pregnancy, the pH decreases to 3.9-4.4;
In the postmenopausal state the pH increases to 7.0-7.4;
The acidity of vaginal environment plays an important role in preventing the proliferation of pathogenic bacteria.
Desirable attributes of all vaginal preparations
No tissue irritation;
Ease of application;
Even distribution of the drug throughout the vagina;
Retention of the drug in the vagina;
Absence of an offensive odour;
Absence of staining of clothes or skin;
Compatibility with other forms of medication and contraception;
Minimal interference in sexual activity.
Conventional drug delivery systems for vaginal administration
Solutions and Foams
Creams and Gels
Tablets
Pessaries
Films
Solutions and foams
The foams differ from the solutions by the presence of a suitable propellant in the formulation
Plasma concentration profiles obtained after solution administration are characterised by a burst effect followed by a rapid decrease below therapeutic level, due to the low residence time of the formulation in the vagina
what are creams and gels
Creams are viscous semi-solids and are usually oil-in-water emulsions (aqueous creams) or water-in-oil emulsions (oily creams);
Gels are transparent or translucent semi-solids, consisting of solutions or dispersions of one or more active ingredients in suitable hydrophobic or hydrophilic bases (often polymers)
tablet use
advantages
Similar excipients as in tablets for oral administration;
Advantages: ease of manufacturing, ease of insertion, and low cost;
what is Pessaries
Pessaries are solid, bullet-shaped preparations designed for easy insertion into the vagina.
They are normally made of a solid vegetable oil that contains the drug. The drug is gradually released into the vagina as the pessary dissolves at body temperature.
Can ensure a sustained drug release by dissolving or melting, depending on the choice of excipients.
what is Vaginal films
Vaginal films comprise solid and flexible thin sheets in which one or more drugs are dispersed or dissolved in the matrix;
In the vaginal environment these films are hydrated by local moisture, and disperse/dissolve and adhere to the mucosa;
Vaginal films have been traditionally used for delivering spermicide compounds (Example: 28% nonoxynol-9-containing VCF® Vaginal Contraceptive Film, Apothecus)
what is advantages and disadvantages of vaginal drug delivery
Relatively large surface area (approximately 60 cm2) for drug absorption;
Rich blood supply;
Low metabolic activity;
Relatively high permeability to many drugs;
Ease of administration;
Prolonged retention is possible;
Can be used as an alternative when the oral route is not feasible;
Offers the potential to achieve zero-order controlled release
Disadvantages
Limited to potent molecules;
Adverse effects (for example, local irritation caused by vaginal devices);
Hormone-dependent changes;
Leakage;
Life-cycle constraints;
Applicability constraints
Current trends in vaginal drug delivery
Vaginal delivery of estrogens and progesterones for contraception, hormone replacement therapy (tablets, suppositories, gels, rings);
Vaginal delivery of prostaglandins for induction of labour or second trimester abortion (hydrogel pessaries, inserts, gels);
Therapeutic peptide delivery (insulin, calcitonin, gonadotropin releasing hormone)
Antiviral agents delivery (dextrin sulphate vaginal gel)
