Division of Medicinal Chemistry--general oral papers

Oral drug delivery is the most common route of administration due to its convenience, cost-effectiveness, and high patient compliance. It enables precise formulation to ensure proper drug dosage and bioavailability. The development of oral dosage forms considers drug properties such as solubility, stability, and absorption to optimize therapeutic efficacy.Tablets, capsules, liquids, and chewable formulations enhance drug stability, mask undesirable tastes, and improve patient experience.

Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...

The development of extended-release formulations has facilitated the transition from intravenous to oral medication, offering a more convenient and patient-friendly approach to drug administration. This transition, however, requires careful management to ensure that therapeutic drug levels are maintained, preserving efficacy and avoiding adverse effects. Understanding pharmacokinetic principles and dosage calculations is critical during this process.Pharmacokinetics of the...

The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
Drugs in...

Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...

Conventional oral drug products, termed immediate-release (IR) formulations, are engineered to promptly release their active pharmaceutical ingredient (API) upon ingestion, typically in tablets or capsules. This rapid release often results in swift drug absorption and consequent pharmacodynamic effects, although the timing and intensity can vary depending on the drug's properties. Prodrugs within these formulations require metabolic conversion to activate their pharmacodynamic effects,...