Official Solutions PDF

Official solutions Dr.balkis ahmed Usul aldeen college of pharmacy SOLUTIONS  Solutions are liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents.  Most common pharm...

Official solutions Dr.balkis ahmed Usul aldeen college of pharmacy SOLUTIONS  Solutions are liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents.  Most common pharmaceutical solutions are aqueous solutions ( also the biological systems are mostly aqueous.)  Medicated solutions contain drugs that are usually soluble in water, and their absorption is higher than from suspension or solid dosage forms because any drug must be molecular dispersed (in-solution) before they can be absorbed across the biological membrane and be effective Official Solutions: Are liquid preparations that contain one or more soluble chemical substance dissolve in liquid solvent, these solutions are described, constituent, preparation in one of the pharmacopoeia* or national formulary. *(British pharmacopoeia and USP is a book containing directions for the identification of medicines and also contains standards of identity, strength, quality, purity, packaging and labelling for drug dosage form) This solution has specific method of preparation, uses, and method of administration. 1. They are used for their medical activity 2. As solvent for other liquid preparation 3. Or as a coloring or flavoring agent Methods for preparation of official solution: 1. Solution prepared by Simple solution, 2. Solutions prepared by chemical reaction, 3. Solutions prepared by extraction, 4. Solutions prepared by Simple solution with sterilisation include: A. ophthalmic solution B. ophthalmic solution prepared from sterile powder C. anticoagulant irrigating D. parenteral 1. Simple solution method the procedure for preparing simple solution 1. weight the solid ingredient and then dissolve it in three quarter of the solvent in beaker after subtract the volume of any liquid 2. add any liquid ingredient if present 3. complete the volume of the prescription by addition of the solvent. 4. Transfer it into wide mouth bottle and label it 2. Chemical reaction method chemical reaction take place to prepare the solution sometime the same solution can be prepared by two methods, simple solution and chemical reaction, example limewater solution *by simple solution dissolving the powder of Ca(OH)2 with water or by chemical reaction CaO + H2O Ca(OH)2  Simple solution is preferred because it is easy, does not need special condition, and does not involve all product of reaction. The chemical reaction method is only chosen when: the active constituent are not readily obtain by other method example formaldehyde the pure solute may not dissolve from Solid State so it obtain by chemical reaction Several products of chemical reaction had used for therapeutic action example magnesium citrate solution as a cathartic 3. Extraction either by maceration or percolation, they are used to isolate an active principles from crude drug it's obtained those products in pure Form e.g. solution prepared by this method is adrenaline chloride solution it is vasoconstrictor use to increase blood pressure to prevent haemorrhage (its extraction from animal tissue), another example is ipecac. 4. Solution prepared by Simple solution with a sterilisation this solution need sterilization because it is used for sensitive organs  Anticoagulant solution example citrate phosphate dextrose this solution consist of 3% citric acid 26.3% sodium citrate and 2.22% sodium biphosphate and 25.5% dexterous the solvent is water for injection it is used anticoagulant for the whole blood for storage 70 millilitres of this solution used for 500ml of whole blood - Other examples used as physiological and irrigating solution is ringer solution it is isotonic solution of 8.6% NaCl 0.3% KCL 0.33% CaCl2 called solution of the three chloride. This is dissolved in a purified water so should not use for parenteral purpose parenteral preparation need water for injection, this solution used for living tissue. Official solutions prepared by simple solution 1. Amaranth solution u.s.p. used as coloring agent 2. Strong ammonia solution N.F used as solvent reagent 3. Gentian violet solution u.s.p. topical local anti-infective Official solutions prepared by chemical reaction 1. Formaldehyde solution u.s.p. used as disinfectant 2. Magnesium citrate solution N.F used as cathartic 3. Hydrogen peroxide solution u.s.p. used as topical anti-infective. Official solution prepared by simple solution with sterilization 1. Anticoagulant , citrate dextrose solution u.s.p. as anticoagulant for storage of whole blood 2. Ringer's solution N.F irrigations solution 3. Atropine sulfate ophthalmic solution isotonic and antimicrobial solution 4. Dexamethasone sodium phosphate ophthalmic solution N.F 5. Pilocarpine hydrochloride ophthalmic sol. Official solution prepared by extraction Epinephrine solution u.s.p. vasoconstrictor, elevate B.P. and prolong action of local anesthetic. Parenteral  It means para(outside) enteral(intestine), are those sterile drugs, sol, or suspension that are packaged in a manner suitable for administration by hypodermic injection, as it or after diluted with solvent or suspending agents. The general requirements for parenteral : 1. Safety 2. Sterility 3. Freedom from pyrogen 4. Clarity 5. Stability 6. Isotonocity. Only 1 and 5 general requirement for all preparation , other specific. 1.safety: it should be safe to prevent irritation , the vehicle is generally water, but for poorly soluble compounds, alcohol or propylene glycol or polyethylene glycol may be added. *all additives, containers, under go safety test. It was found benzyl alcohol used as local anesthetic it was found to be toxic in infants. 2.sterilty: parenteral products should be free from microorganisms, and administered in away to maintain its sterility. The method of sterilization: a. moist heat (autoclave) 2. Dry heat (oven) 3.filter aids 4. Gas sterilization. 3.freedom from pyrogen: pyrogen are toxic secretions of bacteria, it causes increase in body temperature, a new test coagulation antigen and antibody also found. 4.clarity: this is done by exposing product to strong beam of light and the product should be clear, from any diameter (less than of blood vessel to prevent blockage of vessels/ 5.stability: its standard requirement for all pharmaceutical preparations not only parenteral, the dosage form must be physically and chemically stable in the selected container. To ensure effectiveness and safety(know expire date, color, precipitate, taste, order) 6.isotonicity: should adjusted be NaCl by one method of calculations or by instruments. Parenteral route of administration: 1. I.V. directly into the blood via a major peripheral vein. 2. I.M. intramuscular into skeletal muscle. 3. S.C. subcutaneous, very easy person can inject himself, in the alveolar region. 4. I.D. intradermal between skin layers 5. I.S. intraspinal in the spinal canal 6. I.A. intraarterial this is needed in certain cases for administration of antineoplastic agents to target drug to specific organs  Advantages of parenteral route: 1. if the drug is unstable orally (hydrolyzed) so it is used as injection 2. it gives fast action 3. it is used for unconscious patients 4. in case of high fever 5. for emergency 6. in renal colic 7. sever vomiting 8. psychotic patient 9. in infants  I.V route 1. it is instantaneous response it have rapid response. Its directly to blood circulation 2. the dose is controlled predictable 3. it has great intensity of response 4. less irritant with certain drug and great stability 5. we can give large volume of fluids (i.v infusion)  I.V. disadvantages 1. the dosage form is restricted to solution because of danger of insoluble particle blocking fine capillaries 2. hemolysis may take place some drugs and precipitate with others like phenytoin (antiepileptic agent) ppt. if given i.v. can be prevented by slow injection. I.M. : very common route easier than i.v. less damage to tissue we can give solutions , suspension and emulsions by this route. The drug is transferred by osmosis or osmolarity - It has slow onset and more prolonged action, it is influenced by drug release and blood flow, the absorption in i.m. is in the following order *in suspension should consider the particle size and salt from drug, e.g. K Salt of penicillin is soluble and high blood level, less prolonged action Benzathine pencillin insoluble salt low level, prolonged action Subcutaneous route: s.c This is the common route for given insulin injection, it has slow onset to avoid too intense response, this is a diffusion controlled process , this route obey fick's law of diffusion *the absorption depends on the concentration, solubility and blood flow, this route is patient self- administered. Ophthalmic solutions: or (collyria) Are soluble solutions that used ophthalmically in the eyes for different purposes: inflammation, allergy, congestion, cleaning purposes, for surgery, (for examination of the eye and for care of contact lenses). Requirements: 1.Sterility 2.Isotonicity 3.Buffering 4.Viscosity 5.Proper packaging  It should be sterile, the sterility should be maintained through the storage, if packaging in multiple dose containers Sterility usually done by autoclaving in the final container. autoclave at 121 C0 for 15 min. If the products are sensitive (affected by autoclave temp.) then sterilize by filter aids, by using special filter membrane which contain small pore size to prevent passage of the bacteria and foreign bodies (not highly affected like autoclave) Preservatives: Should be present to prevent chance of microorganism growth if accidently entered to product during multi use. *the preservative should have the following properties: 1. Should be effective in low concentrations 2. Should not interact with the active constituent or any constituent of preparation 3. Should not interact with container material itself some preservatives may be absorbed on the walls of the container so preparation is left without preservative, or the preservation will be unavailable. 4. Should be stable and not decompose in the product. Several preservatives have been used in ophthalmic Phenyl ethyl alcohol con. 0.5% Chlorobutanol con. 0.5% Benzalkonium chloride 0.01% Phenylmercurie nitrate 0.001% *ophthalmic sol. That are intended for surgical use must be sterile and must not contain any preservative. Such solution should be packed in single use disposable containers. *ophthalmic sol. For surgical use contain no preservative because: It is used once (any left amount should be discarded) The preservative is very irritant to open tissue of the eye Isotonicity The same osomotic pressure of the body fluid as 0.9% NaCl Same osmotic pressure of the lacrimal fluid, although the eye can tolerate tonicity values above and below that corresponding to 0.9% NaCl solution (0.6-2%). The methods which are used for adjusting the tonicity of ophthalmic sol. depend on colligative properties of solution (like B.p. o.p.) *the agents used to adjust the tonicity of the solution must be compatible with the active medicament. Buffering: Lacrimal fluid has good buffer capacity i.e (change in pH) can adjust pH of ophthalmic solution. It can get red of excess H or OH when apply eye drop get a retention for short time, then relief takes place. Most ophthalmic drugs are of alkaloidal salts, for these drugs the buffer capacity can adjust to the pH of the eye. But some drugs are quite acidic or basic so can overcome the buffer capacity of the eye. For example: pilocarpine HCl (for glaucoma). Other example epinephrine bitartate, in this case for maximum comfort, a suitable buffer is added to ophthalmic sol. Also for stability of the preparation. Buffer stated in u.s.p.: 1. Boric acid buffer: produce pH slightly below 5,, and these buffer suitable for many water soluble salts drug such as pilocarpine HCl. 2. Phosphate buffer: called isotonic phosphate buffer provide pH between (5.9-8) suitable for many drugs except: scopolamine, eucatropine, and homotropine. The lacrimal fluid has pH 7.4 ophthalmic sol. Should have the same pH, this is not usually possible because at this pH many drugs are not soluble in water (unionized form). And most alkaloid salts precipitate at this level, so pH must be found which have the optimum stability and maximum therapeutic effect and this level must be held by buffers. Benefits of adjustment of pH solution 1. Relieve the discomfort 2. Ensure stability of product 3. Control therapeutic activity So we have to compromise between pH for stability and therapeutic activity (solublity). Viscosity and thickening agents: Viscosity control is important in ophthalmic solution because it prolong the contact of active constituent with eye tissue, and it decrease drainage of ophthalmic solution Which contain thickening agents is better than that not contain thickening agent. Because the solution with no thickening agents will be exposed to drainage and have a short time and low bioavailability. Example of thickening agents methyl cellulose has been use in conc. of 1% as tear replacement. Proper packaging Ophthalmic sol. Should be properly packaged so they must ensure stability activity and maintain sterility, if it is in form of drops it is better to be packed in fitted typed dropper than screw type dropper. This is because it provides very low chance to introduce microorganism. The materials of the container are either glass or plastic each container has certain limitations. For plastic container may cause adsorption of the preservative or one of the ingredients make them unavailable for action or it may cause adsorption of active medical substance For glass container on the other hand, may cause some leaching of an alkaline subs from glass into solution, which change the pH of preparation for this reason for each ophthalmic sol, a study should be done to choose proper container. Ophthalmic preparation are available in dosage form other than solutions such as eye ointment which should also be sterile Eye ointment should be sterile while skin ointment may not be sterile Other dosage form suspensions like cortisone drop also sterile , but it should have a certain particle size and should test for sterility and particle size. Solutions for taking care of contact lenses also other formula for ophthalmic purposes. The lenses of 2 types 1. Soft lenses : hydrophilic and hydrophobic 2. Hard lenses These solutions are of different purposes 1. Cleaning solution 2. Wetting solution (wet the lens by making later between lens and cornea) 3. Sterilizing solution 4. All purpose solution used for wetting, sterilization and cleaning. THANK YOU