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Endang diyah ikasari
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Sel-sel yang cepat mengadakan proliferasi terdiri 5 lapisan yang berbeda, dari dalam ke
luar:1. stratum germinativum (basal)
2. stratum spinosum (prickle)3. stratum granulosum (granular)4. stratum lucidum (lucid)5. stratum korneum
Selain stratum korneum, lapisan-lapisanmempunyai sel-sel yang hidup
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Transdermal drug delivery is an approachused to deliver drugs through the skin for
therapeutic use as an alternative to oral,intravascular, subcutaneous, andtransmucosal routes.
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1. Local application formulations, e.g.,transdermal gels
2. Penetration enhancers
3. Drug carriers, e.g., liposomes and nanoparticles
4. Transdermal patches
5. Transdermal electrotransport
6. Use of physical modalities to facilitatetransdermal drug transport
7. Minimally invasive methods of transdermal drugdelivery, e.g., needle-free
8. Injections
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a. Transdermal delivery system (patch) is easyto use
b. Used for lipid soluble drugs with low doseand low MW
Kerugian :
a. Some irritation by patch or drug
b. Permeability of skin variable withcondition, anatomic site, age, and gender
c. Expensive
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Type Examples Mechanism of actionSynthetic surfactants Laureth-9 membrane interaction
sodium lauryl sulphate extraction of membrane proteinspolysorbate 20 and 80 and lipidsPEG-8 laurate solubilization of peptidessorbitan laurateglyceryl monolauratesaponins (e.g., Quillaja saponins)
Bile salts sodium deoxycholate denaturation of proteinssodium glycocholate decrease of mucus viscositysodium fusidate decrease of peptidase activitysodium taurodihydrofusidate solubilization of peptides
formation of reversed micellesFatty acids and derivatives oleic acid fosfolipid acylchain disruption
caprylic acidlauric acidPalmitoylcarnitine
Chelators Na2EDTA Ca2complexation (influencing tight junctions)citric acidSalicylates
Inclusion complexes cyclodextrins and derivatives increasing peptide stabilityincreasing solubilityenzyme inhibition
Other agents Azone lipid structure disruption
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Transdermal scopolamin (prevent travel-
related motion sickness)
Transdermal nitroglycerin (prophylactictreatment of angina)
Transdermal clonidin (for hypertensi)
Transdermal estradiol
Transdermal testosterone
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Drugs have been administered nasally forseveral years both for topical and systemiceffect.
Topical administration includes agents for thetreatment of nasal congestion,rhinitis,sinusitis, and related allergic and otherchronic conditions.
Various medications include corticosteroids,antihistaminics, anticholinergics, andvasoconstrictors.
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1.High permeability of the nasal mucosa, compared with
the epidermis or the gastrointestinal mucosa2. Highly vascularized subepithelial tissue
3. Rapid absorption, usually within half an hour
4. Avoidance of first pass effect that occurs after absorption
of drugs from the gastrointestinal tract5. Avoidance of the effects of gastric stasis and vomiting,
for example, in migraine patients
6. Ease of administration by the patients, who are usually
familiar with nasal drops and sprays7. Higher bioavailability of the drugs than in the case of
gastrointestinal route or pulmonary route
8. Most feasible route for the delivery of peptides
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1. Diseases conditions of the nose may result in impaired
absorption.
2. Dose is limited because of relatively small area available
for absorption.
3. Time available for absorption is limited.
4. Little is known of the effect of common cold on transnasal
drug delivery, and it is likely that instilling a drug into a
blocked nose or a nose with surplus of watery rhinorrhea
may expel the medication from the nose.
5. The nasal route of delivery is not applicable to all drugs.
Polar drugs and some macromolecules are not absorbed in
sufficient concentration because of poor membrane
permeability, rapid clearance, and enzymatic degradation
into the nasal cavity.
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Factors that inf luence drug del ivery to colorectal area:
1. The rate of absorption of drugs from the colon isinfluenced by the rate of blood flow to and from theabsorptive epithelium.
2. Dietary components such as complex carbohydrates trap
molecules within polysaccharide chains.3. Lipid-soluble molecules are readily absorbed by passive
diffusion.
4. The rate of gastric emptying and small bowel transit
time.5. Motility patterns of the colon determine the rate of
transit through the colon and hence the residence time ofa drug and its absorption.
6. Drug absorption varies according to whether the drug is
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1. A relatively large amount of the drug can be administered.
2. Oral delivery of drugs that are destroyed by the stomach acidand/or metabolized by pancreatic enzymes.
3. This route is safe and convenient particularly for the infants
and the elderly.
4. This route is useful in the treatment of emergencies such asseizures in infants when the intravenous route is not available.
5. The rate of drug absorption from the rectum is not influenced
by ingestion of food or rate of gastric emptying.
6. The effect of various adjuvants is generally more effective inthe rectum than in the upper part of the gastrointestinal tract.
7. Drugs absorbed from the lower part of the rectum bypass the
liver.
8. Degradation of the drugs is much less in the rectal lumen thanin the upper gastrointestinal tract.
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1. Some hydrophilic drugs such as antibioticsand peptide drugs are not easily absorbedfrom the rectum and absorption enhancersare required.
2. Drugs may cause rectal irritation andsometimes proctitis with ulceration andbleeding.
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Hormon, peptida, dan protein tidak cocokuntuk pemberian obat melalui mulut, sehingga
kebanyakan diberikan secara parenteral.
Keunggulan formulasi peptida dan protein antaralain : Memperbaiki stabilitas secara fisika dan kimia
Memperpanjang waktu paro Meningkatkan laju absorpsi
Mengurangi terjadinya metabolisme
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Gastric retensive system Colonic delivery system
Penambahanbahan/senyawa untukmemperlama bertahan dilambung
Sistem bioadhesive
Sistem sediaan floating
Polimer yang spesifik
pada pH usus
Transit time di usus
diperlama
Polimer sensitif denganbakteri pada kolon
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Pharmacology, particularly pharmacokinetics andpharmacodynamics, have traditionally influenced drug
delivery formulations. Some of the newer
developments in pharmacology and therapeutics that
influence the development of DDSs are as follows:
1. Pharmacogenetics
2. Pharmacogenomics
3. Pharmacoproteomics4. Pharmacometabolomics
5. Chronopharmacology
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Use of recombinant DNA technology Expansion of use of protein and peptide drugs in current
therapeutics
Introduction of antisense, RNA interference, and gene therapy
Advances in cell therapy: introduction of stem cells
Miniaturization of drug delivery: microparticles andnanoparticles
Increasing use of bioinformatics and computer drug design
A trend toward development of target-organ-oriented dosageforms
Increasing emphasis on controlled-release drug delivery Use of routes of administration other than injections
Increasing alliances between pharmaceutical companies andDDS companies
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Mencari jurnal ilmiah internasional tahunjurnal > 2009
Diketik dengan huruf arial ukuran 12 dikertas A4
Masing-masing kelas dijilid jadi 1 dandikumpulkan paling lambat tanggal 11Nopember 2011
Setiap pertemuan untuk diskusi 2 atau 3
kelompok Setiap kelas dibagi menjadi 12 kelompok
(2 kelompok membuat dengan materi sama)
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Oral S terdiri dari:1. Sistem floating non effervescent
2. Sistem floating effervescent3. Sistem osmotic pump with osmogen
4. Sistem osmotic pump
5. Sistem matriks larut (soluble matrix)
6. Sistem matriks tidak larut (insoluble matrix)
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1. Oral DDS Sistem membran reservoir2. Oral DDS Sistem mucoadhesive
3. Oral DDS Sistem enterik
4. Nasal DDS (Gel dosage form)5. Nasal DDS (Spray dosage form)
6. Inhalasi DDS
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1. Transdermal DDS2. Transdermal DDS with patch
3. Colon targetted DDS
4. Liposom DDS
5. Nanopartikel DDS
6. Buccal adhesive DDS
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