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Drug Absorption Through Oral Mucosa : Drug Absorption Through Oral Mucosa A. Effect Of The Site On Absorption: Conventional Dosage Form: Absorption from stomach Superior mesenteric vein Portal vein Liver [ First pass metabolism] Inferior vena cava Arterial circulation Slide 4: Sublingual tablets: Highly vascular mucosal lining Sublingual capillaries & veins Jugular vein Superior vena cava Arterial circulation Slide 5: Ex: Naltrexone and naloxone Dosage form Bioavailability Oral 1% each Sublingual 63% and 71% B. Effect Of The Drug On Absorption : B. Effect Of The Drug On Absorption Partition coefficient: There is direct relationship between the o/w partition and drug absorption Partition coefficient Absorption 40-2000 Good 20-30 Borderline <20 Very high dose >2000 Not soluble in saliva Slide 8: pKa: The effect of pKa is similar to as in GIT absorption. Buffer tablets or buffer solutions are used to increase the absorption. Ex: Amphetamine has poor sublingual absorption @ pH < 6.6 but absorption is more at pH 9.0 Slide 9: When the 2 components have the same pKa, the compound with the greater oil/water solubility ratio will be better absorbed. Ex: n-alkanoic acids (4 to 12 carbons): All with pKa from 4.82 to 4.85 Absorption increases as the chain length and oil/water solubility increases. Choice Of Drug : Choice Of Drug The drug should have following characteristics: Undergo passive diffusion Optimum partition coefficient Aqueous solubility Optimum pKa value Dose of the drug should be low (10mg – 15mg) The drug should not be highly ionic or at least capable of being buffered in tablet form Advantages : Advantages Rapid absorption Rapid onset of action Increased bioavailability Effective dose is less No first pass metabolism Disadvantages : Disadvantages High dose can not be administered Surface area for absorption is limited Highly ionic drugs can not be formulated Drugs which are irritating and undesirable taste cannot be used Noncompliance to patient Patient should avoid eating, drinking, chewing, smoking and possible talking in order to keep the tablet in place Manufacturing of sublingual tablets : Manufacturing of sublingual tablets Molded tablets : Molded tablets Contain rapidly soluble material ( lactose, dextrose, sucrose, mannitol) or mixture of these. Sometimes insoluble excipient like finely divided kaolin, ca.carbonate, ca.phosphate. To ensure rapid solubility, the excipients are pass through a fine screen or 120-mesh bolting cloth. Molding can be prepared by Hand molding of tablets Machine molding Hand molding of tablets : Hand molding of tablets Powder mix Blending Addition of solvent Workable mass Load into mold plate Machine molding : Machine molding Powder mix Blending Addition of solvent Workable mass Hopper Rotating circular feed plate Mold plate Slide 18: Mold plate – contains 4 sets of die holes 4 different positions Packing spinner – uniformly packs the mass Smoothing spinner – smoothens top surface of tablet Rake off – excess powder is removed Ejection – ejected onto conveyer belt Removal of solvent by air drying @ 100-1200F for 1 hour. Defects in molded tablets : Defects in molded tablets Related to solvent Too little solvent – soft tablet Too much solvent – tablet shrinkage Aqueous alcohol mixture Poor water content - tent to powder & wear on edges High water content – harder & less soluble Related to drying Solvent mediated migration of drug Evaluation of molded tablets : Evaluation of molded tablets Content uniformity Disintegration test Solubility test Stability studiesd Slide 21: Solubility test: To determine rate and completeness of solubility in a specified amount of water. Method: A tablet on a multipore filter in the upper chamber of plastic millipore swinnex 25 filter holder 1 ml of water flushed through the chamber for 30 sec interval upto 2 min. Samples at interval are collected and assayed. Slide 22: Ex: Codeine phosphate tablets (30mg) Ingredient Qty. per tablet Codeine phospate 30.0 mg Lactose (bolted) 17.5 mg Sucrose (powder) 1.5 mg Alcohol-water (60:40) q.s. Slide 23: Scopolamine hydrobromide tablets: Ingredient Qty. per tablet Scopolamine hydrobromide 0.4 mg Lactose (bolted) 35.0 mg Sucrose (powder) 0.3 mg Alcohol-water (60:40) q.s. Compressed tablets : Compressed tablets Ex: Nitroglycerine tablets (0.3mg)- direct compression Ingredient Qty. per tablet Nitroglycerine (10% of 3.0mg microcrystalline cellulose) Mannitol 2.0 mg MCC 29.0 mg Flovor q.s. Sweetener q.s. Coloring agent q.s. Slide 25: 2. Nitroglycerine tablets (0.3mg)- granulation Ingredient Qty. per tablet Microcrystalline cellulose 21.0 mg Anydrous lactose 5.25 mg Starch, USP 3.0 mg Coloring agent q.s. Povidone 0.3 mg Nitroglycerine (as spirit) 0.3 mg Calcium stearate 0.15 mg Available in market : Available in market Lorazepam - ATIVAN® 1 mg SUBLINGUAL TABLETS ATIVAN® 2 mg SUBLINGUAL TABLETS Isosorbide Dinitrate - ISORDIL 2.5 mg SUBLINGUAL TABLET ISORDIL 5.0 mg SUBLINGUAL TABLET ISORDIL 7.5 mg SUBLINGUAL TABLET ISORDIL 10.0 mg SUBLINGUAL TABLET Fentanyl (as citrate) 100 mg SUBLINGUAL TABLET 200 mg SUBLINGUAL TABLET 300 mg SUBLINGUAL TABLET 400 mg SUBLINGUAL TABLET 600 mg SUBLINGUAL TABLET Slide 27: Bupronorphine Isoproterenol GTN ( glyceryl tri nitrate) Ergotamine Nicotine VITAMIN B12 zolpidem tartrate Slide 28: THANK YOU You do not have the permission to view this presentation. In order to view it, please contact the author of the presentation.