The pharmaceutical industry thrives because it offers medications that are effective in treating the respective diseases they are for. The efficacy of medicine and its safety are the pillars upon which pharmaceutical businesses stand. There is also steep competition among pharmaceutical companies. Several of them offer medicines for the same diseases. The medical community prescribes what they prove to be most effective.
Any medicine prescribed for you first undergoes a long and complex process of pharmaceutical formulation development. This determines the final form of the medicine, the prescribed dosage, schedule of intake, and contraindicated substances. These are substances that you must avoid because they either block the action of the medicine or produce negative side effects upon interacting with the medicine.
It is, therefore, dangerous to self-medicate unless you are a physician. Two things can result from this. One is that the medicine will have no effect, meaning whatever illness you are trying to treat will worsen. The other result can be toxic either because of an overdose or a contraindication with other medicines you are taking.
Active Pharmaceutical Ingredients and Additives
The development of a medical formulation involves various steps. The first focus is on the active pharmaceutical ingredients (APIs). These are the substances that act in the body to target a disease. After establishing that these are effective and safe, scientists determine the effective dosage.
The scientist must then create a target product profile (TPP) ; to choose the right excipients based on the intended target patient population, available competing medicines, medicine appearance, and route of administration. Excipients are substances added to the APIs. They protect and support the therapeutic ingredients, enhance their bioavailability, ensure physical and chemical stability in the manufacturing process and shelf life, and improve patient acceptability. There is a list of pharmaceutical excipients in the National Formulary for scientists to choose from.
Scientists consider factors such as particle size, pH, solubility, and polymorphism. Polymorphism refers to the ability of a solid to occur in two or more crystalline forms. This affects solubility, flowability, physical and chemical stability, hygroscopicity, or the ability of the solid to absorb moisture. This also affects the resulting formulation’s bioavailability, efficacy, or toxicity.
Excipients must be inactive and non-toxic. They must not have negative interactions with the APIs or other excipients. They must not trigger any adverse reactions in patients. Tablets, for instance, usually contain excipients such as diluents from sugar compounds or silicates to add bulk and binders or compression aids. They have disintegrants that enable the tablet to disintegrate and release the APIs in the gastrointestinal tract. They have glidants or anti-caking agents and lubricants necessary in the manufacturing process. Tablet coatings and colorants protect it from the environment and may include flavoring to aid in patient acceptability.
Forms of Administration
The choice of excipients also depends on the various forms of delivery of the formulation. The choices include tablets, capsules, suspensions, solutions, topical ointments, topical gels, and subcutaneous (SC), intramuscular (IM), or intravenous (IV) injections. Some medicines have intranasal, transdermal, or pulmonary deliveries. Often, one medicine comes in several forms, and sometimes the speed of efficacy depends on the form of delivery. For instance, an injected form of the same pain medication can act faster than a tablet or capsule.
It is important to pharmaceutical companies that their medications come in forms that are acceptable to patients because this affects compliance. If the competitor offers a medicine with similar efficacy but more patient acceptability, doctors will choose to prescribe what patients are most likely to take regularly. For instance, for pediatric patients, medicines must be palatable and easy to ingest. These usually come as sweet, chewable tablets or syrups.
Design of Experiments
Every step of the process formulation development process passes through a design of experiments (DOE) and statistical analysis. This ensures the optimization and validation of each process. The DOE approach ensures that the formulation and manufacturing process is robust and scalable.
Among the steps that the formulation goes through are several excipient compatibility studies to test the interaction between various excipients and the API over a certain period. After choosing the best excipients from excipient compatibility study results, scientists do a formulation preliminary study and a formulation optimization study. These experiments test various measurement combinations of the excipients with the APIs. This could require as many as 24 experiments to test all variations. Afterward, they do more studies for manufacturing process development and optimization. This determines the best manufacturing technology and process.
This does not mean the medication is ready for full production, though. It must first undergo preclinical trials in animals and then human trials to ensure efficacy and safety. It must also obtain approval from the U.S. Food and Drug Administration (FDA).
Proper Use of Medication
The rigorous studies and testing that medication goes through before arriving at specific dosage requirements show how important it is to comply with such instructions. Deviating from the prescription negates all the work that has been done to ensure the patient’s safety and healing.