Download - topikal 2013
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Bentuk sediaan obat topikal,transdermal,implant
Susana Elya Sudradjat, MFarm., Apt
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Tujuan Pembelajaran
• Menjelaskan konsep dasar fisiologi kulit dan mekanisme penyerapan obat perkutan.
•Mengklasifikasi berbagai jenis sistem penghantaran dan pelepasan obat topikal dan transdermal.
•Membandingkan keuntungan dan kerugian dari berbagai bentuk sediaan topikal dan transdermal.
•Memilih sistem penghantaran obat yang paling tepat untuk terapi yang efektif.
•Penanganan yang tepat dan penyimpanan produk topikal dan transdermal.
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Drugs enter different layers of skin via intramuscular, subcutaneous, or transdermal delivery methods.
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Topikal
Lokal
Transdermal
Sistemik
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Sediaan topikal /dermatologi: dirancang u/ membawa obat ke kulit untuk terapi kelainan dermal/kulit.
Transdermal DDS: dirancang untuk membawa obat melalui kulit (absorpsi perkutan) menuju sirkulasi umum untuk efek sistemik (kulit bukanlah organ target/tujuan)
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• Uptake into the systemic circulation ?• Healthy or diseased skin ?
Dermal VS Transdermal Delivery
Physicochemical properties of drugs are not ideally suited to uptake into and through the skin
The Challenge
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Topical
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Factors Affecting Absorption:
The absorption of a topical drug is affected by:• The strength of a drug• How long the drug is in contact with the skin• The size of the area of application• Skin thickness• Amount of water in the tissues• Amount of skin breakdown or irritation
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Why Apply Topical Drugs:
• Clean and debride (remove) a wound
• Hydrate (add water) to the skin• Reduce inflammation• Relieve itching or a rash• Provide a protection barrier to the
skin• Reduce thickening of skin
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Faktor2 yg mempengaruhi absorpsi perkutan
1. Harga koefisien partisi obat yg tgtg dr kelarutannya dlm air & minyak. Harga ini dpt berubah dgn melakukan modifikasi kimia gugus dlm struktur obat dan variasi pembawa
2. Kondisi pH akan mempengaruhi tingkat disosiasi serta kelarutan obat yg bersifat lipofil.
3. Konsentrasi obat4. Profil pelepasan obat dr pembawanya, tgtg dr
afinitas obat thd pembawa, kelarutan obat dlm pembawa dan pH pembawa
5. Komposisi sistem tempat pemberian obat, yang ditentukan dr permeabilitas stratum korneum yg disebabkan hidratasi dan perubahan struktur lipida 11
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Faktor2 yg mempengaruhi absorpsi perkutan6. Adanya efek depot pada lapisan tanduk, shg
dpt terjadi ikatan yg bersifat irreversibel dan dpt memodifikasi permeasi kulit
7. Peningkatan suhu kulit dpt menyebabkan perubahan difusi yg disebabkan oleh peningkatan kelarutan obat
8. Adanya vasodilatasi pembuluh darah juga dpt meningkatkan kelarutan obat
9. Pembawa yg dpt meningkatkan kelembaban kulit akan mendorong terjadinya absorpsi perkutan dr obat
10. Waktu kontak obat dgn kulit11. Penggunaan pembalut atau plester
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Prinsip Formulasi Sediaan Semi-Solida
Formulasi umum sediaan semi-solida
terdiri dari:1. Zat Aktif2. Pembawa3. Zat Tambahan
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Zat Aktif
1. Germisida dan zat anti-bakteri (termasuk antibiotik & antifungi)
2. Anti-inflamasi3. Anti-histamin4. Anti-puritik dan anestetik lokal5. Antiseptik6. Antiperspirant7. Astringent ringan8. Keratolitik9. Rubefacient10.Sunscreen11.Bermacam bahan aktif u/ tujuan
transdermal
Zat aktif pada sediaan semi-solid:
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Pembawa
Berdasarkan zat aktif yg akan digunakan & keadaan kulit tempat pemberian sediaan topikal tsb, dipilih pembawa yg sesuai.
Pembawa pada sediaan dermatologi dilihat dari bentuk fisiknya dapat dibagi 4 bentuk:- Padat (solid)- Cair (liquid)- Setengah padat (semisolid)- Aerosol 15
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Zat Tambahan
Zat tambahan pada sediaan topikal pada umumnya dapat dikelompokkan dalam:
1. Memperbaiki konsistensi2. Pengawet3. Pendapar4. Pelembab5. Anti-oksidan6. Pengompleks7. Peningkat penetrasi
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Disain sediaan topikal menurut Katz M dapat digambarkan sbb:
AQUEOUS
EMULSIFIER
POWDER
OIL
O/W Lotion
O/W Cream
W/O CreamW/O
Ointment
Absorption Base
Pasta
Soak Ointment
Lotion shake
Powder
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Klasifikasi Sediaan Topikal
1. Pembawa monofasik serbuk, cairan u/ topikal, lemak
2. Pembawa bifasik krem, gel, pasta berlemak, pasta kering, larutan kocok,
3. Pembawa trifasik pasta pendingin, pasta krem
Klasifikasi sediaan farmasi u/ topikal berdasarkan jenis pembawa yg digunakan:
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Salep (Ointments)Sediaan setengah padat yg berlemak, anhidrous dan mengandung bahan aktif dlm btk terlarut atau terdispersi dlm pembawa.Basis salep:
Basis hidrokarbon Lemak dan basis berminyak Senyawa silikon Basis absorpsi Basis teremulsi Basis larut air
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Krim (Cream)Sediaan emulsi setengah padat u/ pemakaian luar
Emulsi: sistem heterogen yg tddr 2 cairan yg tdk saling bercampur, yi fasa polar (air) dan fasa minyak.
Krim yg banyak dibuat di farmasi adlh:- Emulsi m/a sbg basis yg tercuci dgn air- Emulsi a/m sbg pelunak dan pembersih (emollient & cleansing)
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Pasta
Salep dgn kandungan zat padat tinggi (smp 50%) yg terdispersi dlm basis berlemak.
Tujuan pembuatan pasta awalnya dgn konsep bahwa konsentrasi zat padat yg tinggi dpt meng-absorpsi eksudat kulit,ttp konsep ini kurang benar krn partikel yg disalut lemak membatasi penyerapan air.
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GelSediaan setengah padat dgn sistem 2 komponen yg banyak mengandung air.
Pada gel yg bersifat polar (berasal dari polimer alam atau sintetik) pada konsentrasi rendah (<10%) membentuk matriks 3 dimensi pada keseluruhan massa hidrofilik.
Sistem ini dpt bersifat jernih atau keruh, krn zat pembentuk gel tdk larut sempurna atau krn membentuk agregat yg dpt membiaskan cahaya.
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Contoh resep
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Acidum boricum(antiseptik/ fungistatik)
• Solutio 3%• Bedak 3-5%• Salep 3-10%
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Kompres
R/Acid boric sol.3% 500ml Suc
R/Acid boric 3% Aqua ad 500 ml
m f sol Suc
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Pulv. adspersorius
R/ Salicyl talc pulv.adsp 2% 200
Sue
R/ Acid salicyl 2% Talc. Venet ad 200 mf. pulv. Adsp Sue
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Bedak Purol
R/Acid salicylicBals.peruv. aa 1Adeps lanae 2Oxyd. magnesicOxyd. Zincici aa 5
Talcum ad 50
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Unguenta
R/ Ichtyol ung. 10% 10
Sue
R/ Ichtyol 10% Vaselin flavum ad 10
mf ungSue 28
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Larutan Iodium
R/Iodium 2Natrii Iodium 2,4Aqua ad 100mlmf sol.Sue
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Boraks gliserin sol.
R/Natrii tetraboras 1Glycerin ad 10 ml
mf.sol Sue
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Bedak kocok
R/Lotio Faberi 100ml Sue
R/ Acidum salicylicum 500mg 0,5%Talc.Venet 5 5%Oxyd Zinci 5 5%Amylum manihot 5 5%Alkohol 90% ad 100mlmf. LotioSue
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Lotio Pekelhering/ anti ketombe
R/Acidum salicylicum 1 Glycerin 3 Alkohol 70%ad 100 ml Sue
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Lotio Kummerfeldi
R/Lotio Kummerfeldi 100ml Sue
R/ Camphora 1Sulfur praecip 6,6Etanol 90% 3 mlSol. Calc. hidr 40mlSusp.agent 1,5Ol.Rosae gtt 1Aquadest ad 100 mlmf. LotioSue
Sol. Calc. Hidr = 333 mg Ca(OH)2 /100ml
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Lotio Calamin
R/ Calamin 8Zinc oxyd 8Glycerin 2 mlBentonitum magma25mlCalcii hidroxydi sol.ad 100mlmf.lotioSue
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Pasta Lassari
R/Acidum salicylicum 200mg Zinc.Oxydum 2,5 g Amylum Tritici 2,5 g Vaselin flavum ad 10g mf pasta Sue
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Salep 2-4
R/ Acid. Salicylic. 2 Sulfur praecip. 4 Vaselin flavum ad 50 mf ung
Sue
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Ung.Leniens (salep sejuk)
R/Cetaceum 12,5 Cera alba 12 Paraffin liq 56 Natrii tetraboras 500 mg Aquadest 19 mlmf ungSue
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Liniment Calcis (Luka bakar)
R/ Ol.LiniAqua calcis aa 50mf. LinimentSue
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Liniment amonia
R/Acid.Oleinic. Crud 1 Ol. Sesami 79 Ammonii.liq 20 mf. Liniment Sue
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Daktarin
Miconazole creamCream 2% x 5g ,10g, 20gPowd 2% x 20 g
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Penulisan resep obat paten
Ketoconazole Cream 2% x 5g, 15g
R/ Ketoconazole cream 2% 5g tb No ISue 2
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Transdermal
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Transdermal• To provide controlled continuous
delivery of drugs via the skin to the systemic circulation
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Advantages
• Steady and sustained drug concentration • Variability are not exist : pH intestinal• Hepatic pass metabolism• Constant rate absorption• Ease and convenience• Terminable• Avoid gastro intestinal upset• Half time < < reduces dosing frequency
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Disadvantages
• small plasma concentration• Local irritation, enzymes in
epidermis• Less permeable• Must contains >> drugs
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Example
• Nicotine patch• Fentanyl ( Duragesic patch)• Hormonal patches : estrogen, testosterone, contraceptive• Nitroglicerin patch (angina)• Scopolamine (motion sickness)• Clonidine (anti-hypertensive)
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Implant
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Implant
An implant is a single-unit drug delivery system that has been designed to deliver a drug moiety at a therapeutically desired rate, over a prolonged period of time.
Implant are available in many forms, including:
polymers, which can be biodegradable or non-biodegradable and are available in various shapes (rod, cylinder, ring, film, etc.), sizes and mechanisms of drug release;
mini-pumps, which can be powered by osmotic or mechanical mechanisms.
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Contoh
Norplant• Terdiri dari 6 batang silastik lembut
berongga dengan panjang 3,4 cm, dengan diameter 2,4 mm yang diisi dengan 36mg Levonogestrel dan lama kerjanya 5 tahun.
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Advantages and Disadvantages of Iplantation Therapy
Convenience
Compliance
Potential for controlled release
Potential for bio-responsive release
Flexibility
Commercial
Advantages
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Advantages and Disadvantages of Implantation Therapy
Invasive
Termination
Danger of device failure
Limited to potent drugs
Possibility of adverse reactions
Biocompatibility issues
Commercial disadvantages
Disadvantages
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Selesai
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