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Area of Concentration
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Solvents : Increase penetration by swelling the polar path or by fluidizing lipids. Ex. Dimethyl sulfoxide, oleic acid, propylene glycol, and etc. Surfactants : Lipid fluidization or penetration of it into intracellular matrix and result in disruption of order of comeocytes. Ex. Anionic surfactants dicotylsulphosuccinate, sodium lauryl sulphate, and etc Non-ionic surfactants Pluronic F 127 and Pluronic F68 Natural surfactants(bile salts) Sodium taurocholate and Sodium Tauroglycholate and etc.
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IN VIVO EVALUATION
Animal Model 1. The most common animal species used for evaluating transdermal drug delivery system are mouse, hairless rats, dogs, and rhesus monkey, rabbits, guinea pig, and etc. 2. Rhesus monkey most reliable models for Vivo evaluation of transdermal drug delivery in man. 3. Alternative animals models include weanling pig and human skin grafted nude mouse.
Human Model 1. The most relevant studies are performed in humans however animal models may be used insofar as they may be effective as predictors of human response.
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IN VITRO EVALUATION
Typical Franz diffusion cell - A method transdermal system is placed in between receptor and donor compartment of the diffusion cell.
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IN VITRO EVALUATION
Typical side-by-side diffusion cell setup used for permeability/diffusion studies.
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Other Facts: If the drug is delivered to the stratum corneum at a rate less than the absorption capacity, the device is the controlling factor. BUT if the drug is delivered to the skin area to saturation, the skin is the controlling factor. TDDSs may be constructed of a number of layers: Occlusive backing membrane To protect the system from environmental-entry and from loss of drug from the system or moisture from the skin. Drug reservoir/Matrix system To store and release the drug at the skin site. Release liner which is removed before application and enables drug release. Adhesive layer To maintain contact with the skin after application. Two types of adhesive 1. Peripheral adhesive 2. Face adhesive most common.
Transdermal patches
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Transdermal patches
Design objectives are the following: 1. Deliver the drug to the skin for percutaneous absorption at therapeutic levels at an optimal rate. 2. Contain medicinal agents having the necessary physicochemical characteristics to release from the system and partition into the stratum corneum. 3. Occlude the skin to ensure one-way flux of the drug into the stratum corneum. 4. Have a therapeutic advantage over other dosage forms and drug delivery systems 5. Not irritate or sensitize the skin. 6. Adhere well to the patients skin and have size, appearance, and site placement that encourage acceptance.
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Transdermal patches
Advantages Avoid gastrointestinal drug absorption difficulties Can substitute for oral administration of medication when that route is unsuitable as vomiting and diarrhea. Avoid first-pass effect Are non invasive, avoiding the inconvenience of parenteral therapy. Provide extended therapy with a single application, improving compliance over other dosage forms requiring more frequent dose adminstration. The activity of drugs having a short half- life is extended through the reservoir of drug in the therapeutic delivery system and its controlled release. Drug therapy may be terminated rapidly by removal of the application from the surface of the skin. Are easily and rapidly identified in emergencies. Disadvantages Only relatively potent drugs are suitable candidates for transdermal delivery because of the natural limits of drug entry imposed by the skins impermeability. Some patients develop contact dermatitis at the site of application from one or more of the system components, necessitating discontinuation. The barrier function of skin changes from one site to another on the same person, from person to person and with age. Limited only to potent molecules, those requiring a daily dose of 10 mg or less. It is rather slow and sustained. Does not adhere well to all types of skin. Uncomfortable to wear May not be economical
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Examples of TDDSs
Transdermal Scopolamine Transdermal Nitroglycerin Transdermal Clonidine
Transdermal Nicotine
Transdermal Estradiol
Transdermal Testosterone
Transdermal Methylphenidate
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