Pharmaceutical Dosage Forms I - Lecture Six - PPC PDF

Pharmaceutical Dosage Forms I PPC 201  TYPES of PHARMACEUTICAL SOLUTIONS  1. Oral solutions Syrup Draught Oral drops Elixir Dry powder for solution Linctus  Oral solutions 1.Syrup...

Pharmaceutical Dosage Forms I PPC 201  TYPES of PHARMACEUTICAL SOLUTIONS  1. Oral solutions Syrup Draught Oral drops Elixir Dry powder for solution Linctus  Oral solutions 1.Syrup Aqueous preparations characterized by sweet taste, viscous, they contain at least 45 %w/w of sucrose. Or polyhydric alcohol, sorbitol Viscosity arises from the multiple hydrogen bonds between the dissolved sugar, which has many hydroxyl (OH) groups, and the water  Types of Syrup Simple Syrup: Medicated syrup: Flavored (non- Contains only when the aqueous medicated) syrup: sucrose and preparation Syrups containing purified water, contains some flavoring agents without flavor or added medicinal but not medicinal medicine. substance e.g. substances. Syrup, B.P Phenergan syrup® Vehicles for 66.67% w/w of extemporaneous sucrose in water compounding Syrup, USP Ora-Sweet® 85% w/v of sucrose in water Ora-Sweet SF®  Sucrose & Non-sucrose-based Syrups Non-sucrose-based Syrups may contain sorbitol, glycerin, and propylene glycol. For diabetic patients and others whose diet must be controlled and restricted, these glycogenic substances (converted to glucose), are replaced by non-glycogenic. The viscosity + artificial sweeteners produces an excellent copy of a true syrup. Antitussive syrups, thick, sweet syrup has a soothing effect on the irritated tissues of the throat as it passes over them.  It is important that the concentration of sucrose approaches but not reach the saturation point WHY? Oral solutions Syrup Dilute solutions sucrose is an excellent nutrient for microorganisms. In concentration of 65 % by weight or more the solution will retard the growth of such microorganisms (WHY?) by virtue of their osmotic effect. A saturated solution may lead to crystallization of sucrose under conditions of changing temperature, so that small amounts of glycerol or propylene glycol may be added to syrup (WHY?) to prevent sugar crystallization  Antimicrobial Preservative Benzoic acid 0.1% to 0.2%, sodium benzoate 0.1% to 0.2%, and various combinations of parabens esters 0.1%. Storage conditions of Syrups Preserved in well dried bottles and stored in a cool dark place.  Oral solutions 2.Elixir Clear, sweetened hydroalcoholic solutions intended for oral use and usually flavored Elixirs containing > 10-12% of alcohol are self-preserving The proportion of alcohol in elixirs varies widely because the individual components of the elixirs have different water and alcohol solubility characteristics.  Oral solutions Elixir If an aqueous solution is added to an elixir, a partial precipitation of ingredients may occur (WHY?) due to the reduced alcoholic content in the final preparation.  Oral solutions 3.Linctus  A viscous preparation , consists of a simple solution of the active agent in a high concentration of sucrose solution  Administered orally for the relief of cough  Glycerin is added to provide sweet taste & demulcent action on the mucous membranes of the throat  Oral solutions Linctus Should be sipped and swallowed slowly without the addition of water” For diabetic use , the sucrose is replaced by synthetic sweeteners Should be sipped slowly so as to prolong action of drug Oral solutions Draught is an old term used 4. Draught to describe a single dose liquid oral preparation in a volume larger than usual. Each dose is usually supplied in a separate bottle usually about 50 ml. Example: Ipeca cuannha draught to induce vomiting after suspected poisoning.  Oral solutions 5.Oral Drops Liquid preparation for pediatrics, generally vitamins, given in the form of drops. Supplied in bottle with calibrated dropper to determine number of drops equivalent to the prescribed dose Supplied in small volume container e.g. 5-10 mL Oral solutions 6.Dry powder for solution Dry powder to be reconstituted with a vehicle (water) before use The reconstitution solution may be a clear solution or suspension WHY? For unstable drugs such as certain antibiotics have insufficient stability in aqueous solution to meet extended shelf life periods Once reconstituted, the solution remain stable for 7-14 days depending on the condition of storage Examples: Penicillin V potassium for oral solution, USP  Labeling Requirements The reconstitution procedure and the vehicle volume should be stated on the label The storage condition and the shelf period should be stated (7 days at room temperature OR 14 days in refrigerator) 7. Oral rehydration solution Effective in treatment of diarrhea and mild volume depletion (5-10% of body weight). Available as OTC Oral solution: certain amounts Na+, K+, Cl-, citrate, dextrose/L Available in liquid or powder packets form for reconstitution Should not be mixed with milk or fruit juice (electrolyte) 2. Liquid For Cutaneous Application 1. Lotions 2. Liniments 3. Paints 4. Collodion  1. Lotion Aqueous, alcoholic or oily liquid preparation (monophasic systems) or as suspension & emulsion (biphasic systems) Applied on unbroken skin without rubbing to the affected area Usually applied with the help of cotton wool or gauze 2. Liniment Alcoholic or oleaginous solutions or emulsions Applied with rubbing to the unbroken skin Alcoholic liniments are used generally for their rubefaciant & counter irritant effects Oleaginous liniments are employed primarily when massage is desired 2. Liniment It contain substances like methyl salicylate or camphor Used for sore muscles & arthritis  3. Paint Solution or dispersion of one or more active ingredient intended for application to skin or mucous membrane Skin paints contain volatile solvent that evaporates quickly to leave a dry resinous film of medicament They are used in small amounts and normally with brush 4. Collodion  Liquid preparations containing pyroxylin (nitrocellulose) in a mixture of ethyl ether & ethanol Ether and ethanol have evaporated, leave a film of pyroxylin on the surface used to seal minor injuries or retain a dissolved drug in contact with the skin for an extended period. Collodion is made flexible by the addition of castor oil = Plasticizer 4. Collodion Pyroxylin, is exceedingly flammable and must be stored away from flame in well-closed containers, protected from light The official medicated collodion, Salicylic Acid Collodion USP, contains 10 % w/v of Salicylic Acid in Flexible Collodion USP and is used as a keratolytic agent in the treatment of corns and warts TEST YOUR SELF  Give Scientific Term for each of the following 1. Clear sweetened flavored hydroalcoholic solutions intended for oral use 2. Liquid for cutaneous application that are intended to be applied on unbroken skin without rubbing 3. Solutions of pyroxylin in alcohol/ether 4. Aqueous preparations characterized by sweet taste and viscous consistency and contain at least 45 %w/w of sucrose 5. Viscous preparations sipped and swallowed slowly without addition of water for the relief of cough 3.Oromucosal Liquids Mouth wash & gargle Gingival & sub-lingual Topical Oral Dental Solutions 3. Oromucosal Liquids  Aqueous solutions for the prevention & treatment of the mouth and throat infections  Mouth cavity » mouth washes  Gargling » gargles  They are either ready to use i.e. used without dilution or in a concentration form, to be diluted with warm water before use  1.Gargles Aqueous solutions containing antiseptics, antibiotics and/or anesthetics used for treating the throat & nasopharynx by forcing air from the lungs through the gargle, which is held in the throat; subsequently, the gargle is expectorated 2. Mouth Wash Therapeutic & cosmetic purposing 3. Gingival & sublingual preparations Spray or drops for application to specific areas of the oral mucosa such as: Gums in the treatment and prevention of periodontal diseases e.g. gingivitis (inflammation of gum during teething) Under the tongue for systemic absorption of drug 4.Topical Oral Dental Solutions Benzocaine topical anesthetic: indicated for pain relief, irritation in the mouth associated with teething Eugenol Dental analgesic: applied to dental cavities. Eugenol is a pale yellow liquid having aromatic odor of clove. 4. Solutions administered into body cavities 1. Douches 2. Nasal Solutions 3. Rectal Solutions 4. Otic - Aural Solutions 5. Ocular Solutions  1. Douches/ Irrigations Sterile isotonic aqueous large volume solutions Used for the cleansing of body cavities and wounds 1. Douches/ Irrigations Examples: Eye douches are used to remove foreign particles and discharges from the eyes. Pharyngeal douches are used to prepare the interior of the throat for an operation and to cleanse it in supportive conditions. Similarly, there are nasal and vaginal douches. Ear Wash aqueous solution to clean the external auditory. They usually of a pH within the physiological limits 2. Rectal Solutions  Barium Sulfate Oral and Rectal suspensions Barium Sulfate for Suspension: administered either orally or rectally for diagnostic visualization of the GIT 3. Nasal Solutions  Aqueous solutions administered to the nasal passages in drops or sprays  Naphazoline GCl Nasal Solution USP administered for the local effect to reduce nasal congestion  Miacalcin® for its systemic effect for the treatment of osteoporosis  Intranasal drug administration offers rapid absorption to the systemic circulation  This route is safe and acceptable alternative to the parental administration Prof. Ragwa M. Farid 180 3. Nasal Solutions Nasal solutions are prepared so that they are similar in many respects to nasal secretions aqueous nasal solutions usually are isotonic & slightly buffered to maintain a pH of 5.5 to 6.5 Use of oily nasal drops should be avoided because of possible damage to the cilia of the nasal mucosa Prof. Ragwa M. Farid 181 4. Otic/ Aural Solutions  Topical administration to the ear include local anesthetics, antibiotics & anti-inflammatory agents.  Include the mainly glycerin or glycerin/ water WHY?  Viscous glycerin vehicle permits the drug to remain in the ear for a long time  Anhydrous glycerin, being hygroscopic, tends to remove moisture from surrounding tissues, thus reducing swelling Prof. Ragwa M. Farid 182 5. Ocular / Ophthalmic Solution Small volume, isotonic sterile liquid solution designed to be instilled into the eyeball Ophthalmic solutions should be free of foreign particles. The optimal volume to administer, based on eye capacity, is 5 to 10 μL. Prof. Ragwa M. Farid 183 Ocular / Ophthalmic Solution The main disadvantage of ophthalmic solutions is the relative short contact time limiting the ocular bioavailability (Viscosity enhancer) The optimum viscosity which allows drug retention and visual comfort is from 15 to 25 cps 5. Miscellaneous Liquids Extract and tincture Spirits Infusions & Decoctions Aromatic water 1.Extracts & Tincture These terms are commonly used for concentrated solution of active principles from animal or vegetables sources  Difference between Extract & Tincture Extract Tincture Very concentrated Less concentrated One part of herb : one One part of herb: 3-8 part of alcohol parts of alcohol Administered as drops Administered as mls 2.Spirit Alcoholic solution of volatile material e.g. spirit mentha, spirit anise Mostly used as flavouring agents Spirits should be stored in tight, light- resistant containers and in a cool place 8. Viscid Solutions Glycerins Oleo vitamins 1. Glycerins / Glycerites Glycerites are solutions or mixtures of medicinal substances in not less than 50% by weight of glycerin Most of glycerins are extremely viscous Glycerin is used as the only solvent for the preparation of Antipyrine & Benzocaine Otic Solution ; USP Glycerins are hygroscopic and should be stored in tightly closed containers  2.Oleo vitamins A preparation of fat-soluble vitamins (usually A&D) in fish liver or edible vegetable oil. The indicated vitamins are unstable in the presence of rancid oils and, therefore, those preparations, should be stored in small, tight containers, preferably under vacuum or under an inert gas, protected from light  Questions Formulation Cases From the following formulation records identify the type of solution with justification If you are this pharmacist which type of solution you will formulate for him from the mentioned formulations (a-d)  Case study 1 A patient got muscle sores (‫ )شد عضﻼت‬while playing a football match and went to a pharmacist to prescribe him a medication to relief his pain.) and as patient counseling what will you tell him for proper usage? …………………………………………………………………… ……………………………………………………………………  Case study 2 A patient suffering from buccal ulcers ( (‫قرح الفم‬and went to a pharmacist to prescribe him a medication to relief his pain and heal the ulcers. and as patient counseling what will you tell him for proper usage? …………………………………………………………………… …………………………………………………………………… What is the difference between: 1. Syrup & Elixir 2. Paint & Collodion 3. Lotion & Liniment 4. Aromatic water & Spirit 5. Decoction & Infusion 6. Tincture & Extract Thank You