Chemicals & raw materials
APIs to the rescue?
Oral bioavailability remains one of the biggest challenges in drug development, particularly for small-molecule APIs with poor solubility or permeability. Liam Critchley explores how
pharmaceutical companies are using integrated formulation strategies – including amorphous solid dispersions, nanosizing and lipid carriers – alongside advanced data analytics and AI-driven approaches to accelerate discovery, enhance solubility and reduce development timelines for traditionally hard-to-formulate drugs.
ral ingestion is the most common and convenient route to administer drugs to patients, and most small-molecule drugs created today are oral formulations. The properties of the drug molecules are critical to the success and effectiveness of the formulation. There are two properties of active pharmaceutical ingredients (APIs) that have typically been challenging for drug formulations: solubility and permeability. Poor solubility has been a key issue that has caused a low bioavailability for a lot of oral small-molecule drugs. However, the solubility problem has now been solved thanks to new advanced formulation methods. Pharmaceutical manufacturers are using a combination of advanced drug formulations in their products – such as amorphous solid dispersions (ASDs), nanosizing and lipid-based carriers – to improve the solubility of poorly bioavailable drugs, while simultaneously using technology advances to speed up their discovery and production processes. These integrated models
O 78
are now reducing drug development timelines for traditionally poorly bioavailable drugs, but some challenges remain.
Bioavailability challenges for oral drugs in early development phases The oral bioavailability of a drug is the amount of drug dosage that reaches the therapeutic site and depends on many properties of the APIs – including their solubility, permeability, dissolution rate, intestinal stability and metabolism. The main causes of low oral bioavailability are poor solubility and low permeability. It’s estimated that more than 40% of new chemical entities (NCEs) developed in the pharmaceutical industry are insoluble in water, leading to slow drug absorption, variable bioavailability and gastrointestinal toxicity in conventional formulations. This means a lot of drugs can take longer to develop at higher costs due to their poor bioavailability. The bioavailability challenges of many drug formulations are now solved long before they reach
www.worldpharmaceuticals.net
metamorworks/
www.shutterstock.com
Page 1 |
Page 2 |
Page 3 |
Page 4 |
Page 5 |
Page 6 |
Page 7 |
Page 8 |
Page 9 |
Page 10 |
Page 11 |
Page 12 |
Page 13 |
Page 14 |
Page 15 |
Page 16 |
Page 17 |
Page 18 |
Page 19 |
Page 20 |
Page 21 |
Page 22 |
Page 23 |
Page 24 |
Page 25 |
Page 26 |
Page 27 |
Page 28 |
Page 29 |
Page 30 |
Page 31 |
Page 32 |
Page 33 |
Page 34 |
Page 35 |
Page 36 |
Page 37 |
Page 38 |
Page 39 |
Page 40 |
Page 41 |
Page 42 |
Page 43 |
Page 44 |
Page 45 |
Page 46 |
Page 47 |
Page 48 |
Page 49 |
Page 50 |
Page 51 |
Page 52 |
Page 53 |
Page 54 |
Page 55 |
Page 56 |
Page 57 |
Page 58 |
Page 59 |
Page 60 |
Page 61 |
Page 62 |
Page 63 |
Page 64 |
Page 65 |
Page 66 |
Page 67 |
Page 68 |
Page 69 |
Page 70 |
Page 71 |
Page 72 |
Page 73 |
Page 74 |
Page 75 |
Page 76 |
Page 77 |
Page 78 |
Page 79 |
Page 80 |
Page 81 |
Page 82 |
Page 83 |
Page 84 |
Page 85
