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CONTRACT MANUFACTURING


Parenteral Preparations, Challenges in Formulations


Dr. Elham Blouet


Global Market Manager Injectable and Dialysis Global Business Unit Pharma & Health ROQUETTE


Introduction


Parenteral preparations are defined as solu- tions, suspensions, emulsions for injection or infusion, powders for injection or infusion, gels for injection and implants.1


They are ster-


ile preparations intended to be administrated directly into the systemic circulation in humans or animals.


They are required, like any pharmaceutical dosage forms, to meet the pharmaceutical quality standards as described in pharma- copeias and to be safe for the intended purpose of use.1,2,3


In addition to being sterile, parenteral preparations must be pyrogen-free. Sterility can be achieved by different processes of sterilization that should be appropriate to the formulations,4


while the pyrogen-free


aspect will require, if no depyrogenation process is used during the preparation of the sterile drug products, the use of pyrogen-free pharmaceutical ingredients; drug substances or API (Active Pharmaceutical Ingredient) and excipients.


They are usually supplied in single dose glass or plastic containers (PVC nowadays less recommended, or polyolefin) or more and more in pre-filled syringes or pens to facilitate the ease of use.1


This article will describe the main challenges encountered during the formulation of parenteral preparations, as well as Roquette’s solutions meeting the formulator’s needs.


Properties of Parenteral Preparations


Parenteral preparations are intended to be administrated through the human or animal body, either by direct injections (for example, bolus intravenous (IV), intramuscular (IM) or subcutaneous (SC)) or by infusion with


Figure 1. Decision tree for sterilization choices for aqueous products (CPMP/QWP/054/98)


a controlled infusion rate or by direct implantation through IM or SC.


They must meet the following minimum com- pendia criteria:1,2,3


• To be sterile and pyrogen-free


• To be clear or practically exempt of visible particle and to be free from sub-visible particles as required by pharmacopeias EP, USP and JP


Pharmaceutical Outsourcing | 12 | November/December 2016


• No evidence of phase separation for the emulsions, or aggregates formation for aqueous dispersions such as injectables Mab (monoclonal antibody) preparations


• In case of suspensions, the use of appropriate particle size and any sediment should be readily dispersed upon shaking to give stable formulations and ensure the correct dose to be withdrawn and injected.


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