SMALL VOLUME PARENTERALS by Ashok

SMALL VOUME PARENTERALS: 

SMALL VOUME PARENTERAL S Presented By Ashok.K , M.Pharm 1 st yr 11MPCT0012

BRIEF ABOUT PARENTERALS: 

BRIEF ABOUT PARENTERALS Para: outside Enteron : intestine (i.e. beside the intestine) It denotes that route of administration other than oral route. Definition:- According to the USP 24/ NF 19 “As those preparations intended for injection through the skin or other external boundary tissue, rather than through the alimentary canal” so that the active substance they contain are administered using gravity or force directly into a blood vessel,organ,tissue or lesion.

CONTENTS : : 

CONTENTS : Definition Introduction Advantages Disadvantages Formulation of product (SVP) Evaluation of product (SVP) Containers and closures References

DEFINITION : : 

DEFINITION : According to USP : “ an injection that is packaged in containers labelled as containing 100 ml or less”

INTRODUCTION :: 

INTRODUCTION : All the sterile products packaged in vials, ampoules, cartridges, syringes, bottles or any other container that is 100ml or less fall under the class of SVP. Ophthalmic products packaged in squeezable plastic containers, although topically applied to the eye rather than administered by injection, also fall under the classification of Small Volume Injections (SVI) as long as the container size is 100ml or less. SVP aqueous solutions can be administered by intravenous route because of local irritation. Small volume parenteral products can be formulated and packaged in several ways and include a wide variety of products like :

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Pharmaceutical products. Biological products. Diagnostic agents. Allergenic extracts. Radiopharmaceutical products. Dental products. Genetically engineered or biotechnology products. Liposome and lipid products. An injection is a preparation intended for parenteral administration and/or for constituting or diluting a parenteral article prior to administration Types of preparations :- Drug injection Drug for injection Drug injectable emulsion Drug injectable suspension Drug for injectable suspension

ADVANTAGES : 

ADVANTAGES It provides rapid onset of action It provides immediate therapeutic action It can be administered accurate dose. It can be given to patients who cannot take oral medication. It minimize the first pass effect. It provides more bioavailability

disadvantage: 

disadvantage It should be administered aseptically It produces pain at the site of injection The administered of drug through wrong route may prove fatal effect Self administration is not possible If pyrogenic preparations lead to very harmful effect.

Formulation of SVP : : 

Formulation of SVP : Aqueous vehicle : Types :- purified water, WFI, sterile WFI, bacteriostatic WFI, sterile WF Irrigation. Preparation :- Distillation , ion exchange or reverse osmosis. Except purified water all are pyrogen free Non aqueous vehicle : Because of safety purity biocompatibility Several SVPs are marketed as oily solutions

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The oil must be vegetable in origin (sesame, olive, or cottonseed oil). Product USP Oil Ampicillin (suspension) Vegetable Diethyl stilbestrol Sesame,cotton Epinephrine(suspension) Sesame Penicillin G procaine Vegetable (suspension) Co solvents :- Are used to increase the stability of poorly soluble drug in water and prevent drug chemical degradation by hydrolysis Ex propylene glycol or in combination with ethanol and polyethylene glycol.

Ingredients or added substances: 

Ingredients or added substances Antimicrobial preservatives : Maintain the stability of the product during storage. Phenyl mercuric nitrate and Thiomersol 0.01% Benzethonium chloride and benzalkonium chloride, Phenol or cresol 0.5%, chlorobutanol 0.5%. Buffers : Added to maintain pH Results in stability of drug against hydrolytic degradation or enhance the solubility of drug in solution.

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Common buffers used in SVPs pH Buffer system Conc % 3.5-5.7 Aceticacid -acetate 1-2 2.5-6.0 Citricacid -citrate 1-5 6.0-8.2 Phosphoricacid - 0.8-2 phosphate 8.2-10.2 Glutamicacid - 1-2 glutamate Antioxidants : Antioxidants function by preferentially with molecular oxygen and minimizing or terminating the free radical auto-oxidation reaction. ex:- water soluble: sulfurous acid salts, ascorbic acid isomers, thiol derivatives. oil soluble: propyl gallate , butylated hydroxy anisole,ascorbyl palmitate alpha tocopherol 9.

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Tonicity adjusters : Electrolytes:Nacl Non elecrolytes : Glucose,Mannitol,Glycerine Ex. Of isotonic:Dextrose injection 5%& Nacl injection 0.9% Some solutions are iso -osmotic but not isotonic this is because the physiology of the cell membranes must be considered. For ex the cell membrane of the RBC is not semi permeable to all drugs it allows ammonium chloride, alcohol, boric acid, glycerin, propylene glycol, and urea to diffuse freely. In the eye the cell membrane is semi permeable to boric acid and a 2% soln is an isotonic ophthalmic solution.

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But even though a 2% soln of boric acid is an isotonic with the eye and is iso -osmotic, it is not isotonic with blood since boric acid can freely diffuse through the RBC– and it may cause HEMOLYSIS. Tonicity can be measurement by: osmometer Other ingredients : Bulking agents – for freeze dried preparations(solids) ex mannitol , lactose sucrose, dextran . Suspending agents – CMC, methyl cellulose gelatin, sorbitol . Emulsifying agents – lecithin, polysorbate 80 Ophthalmic ointments bases – petrolatum.

Evaluation of SVPs: 

Evaluation of SVPs SVPs must be sterile and free from pyrogens and foreign particulate matter . These three major characteristics distinguish sterile dosage forms from any other pharmaceutical product Sterility :- A state of absolute freedom from microbial contamination. Achievement of sterility involves the combination and coordination of a wide range of activities and processing such as :- Cleaning and sanitization of all facilities and equipment

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Cleaning and sterilization of equipment, packaging and all other items to be in contact with sterile product. Installation and certification of laminar air flow areas where sterile air is provide via High-Efficiency Particulate Air (HEPA) filters. Environment monitoring of the facility, equipment, water and personnel for strict microbiological and particulate control. Validation of sterilization and filter systems. Freedom from pyrogens :- Pyrogens are metabolic byproducts of microbial growth, very small water soluble, heat resistant lipo polysaccharides that cannot be destroyed by typical steam sterilization cycles.

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Pyrogenic contamination is detected by 1) Rabbit method (old method) 2) Limulus Amebocyte Lysate test (new) Rabbit method Horseshoe Crabs Being Bled

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Limulus - genera of crab Amebocyte - crab blood cell from which active component is derived Lysate - component is obtained by separating amebocytes from the plasma and then lysing them Based on clotting reaction of horseshoe crab blood to endotoxin Faster, more economical, more sensitive than rabbit pyrogen test Freedom from particulate matter :- Stability :- Isotonicity :-

Containers & closures: 

Containers & closures 1.Glass 2.Plastic Ampoules( single dose ) Vials( multiple dose) Cartridges Automatic injector 3.Rubber closure with aluminium caps Small volume parenterals : less than 100ml Large volume parenterals : more than 100ml

References :-: 

References :- Encyclopedia of pharmaceutical technology; dosage forms; parenterals page 1001-1011, drug delivery; parenteral route page 1266-1277, 2007 edition. Ansel’s pharmaceutical dosage forms and drug delivery systems; 9 th edition; parenterals ; page no 443. The theory and practice of industrial pharmacy; Leon Lackmen,Herbert Liberman ; page no 664-675. http://www.authorstream.com/Presentation/pharmacistsahu-1372909-parenterals .

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Thank You