Multi-particulate formulations: the power of many
After assessing the various routes of drug administration, oral delivery stands out as the safest and, as a result, the most universally accepted among patients. Single-unit dosage forms, including tablets followed by capsules, have been identified as the preferred designs for immediate or modified release formulations
Traditionally, multi-particulates are filled into empty hard capsules using automated capsule filling machines. However, more recent technologies have enabled pellets to be compressed into multiple-unit pellet system (MUPS) tablets or pellet-containing tablets. Once these special tablets are exposed to the aqueous environment of the stomach, they disintegrate rapidly into individual pellets, releasing the drug like uncompressed pellets filled in capsules.
MUPS technology has gained considerable acceptance, particularly in the European market, with a number of products coming to the fore, including: Beloc ZOK (metoprolol succinate sr plus hydrochlorothiazide), Antra MUPS (omeprazole) and Prevacid SoluTab (lansoprazole), Nexium (esomeprazole), Galanil PR (galantamine HBr), Lipidown (orilistat), Esomezol (esomperazole sr), Toprol XL (metoprolol succinate) and Cartia (diltiazam).
“From a patient perspective, capsules also cater to paediatric and
geriatric patients with swallowing difficulties ”
Since the total drug is divided equally into many units in a multiple-unit system, it demonstrates several advantages over single-unit systems. When administered orally, these particles (less than 2mm in size) distribute evenly across the extensive surface area of the stomach. They behave like fluids and have a shorter retention time. Their small size also facilitates uniform gastric distribution, potentially reducing food-induced variations in inter- and intra-individual bioavailability, minimising chances of side effects and local toxicity. MUPS tablets can also greatly reduce the risk of premature dose dumping leading to drug degradation or gastric irritation due to any failure in functional coating. This is because a failure of a few units may not be as detrimental as the failure of a single-unit system. Moreover, MUPS tablets also offer the possibility of adjusting dosage strengths, administering incompatible drugs together and combining multi-particulates with different drug-release rates to customise the release profiles. However, despite the various advantages that this unique dosage form provides, the appropriate presentation of these multiple units in the final formulation must be carefully considered. Should these pellets be filled in capsules or compressed into tablets? The best way to determine this depends on a comprehensive understanding of the overall formulation and manufacturing process of the MUPS technology.
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Source: Subhashis Chakraborty and Ananya Sen at ACG Capsules, IPT website Multi-particulate formulations: the power of many (iptonline.com), Innovations in Pharmaceutical Technology
Subhashis Chakraborty holds a PhD in Pharmaceutical Sciences. Presently, Dr Chakraborty holds the position of general manager, Global Product Management, for ACG Capsules. In this role, he is responsible for spearheading the new capsule technologies for pharmaceutical and nutraceutical applications, right from development to commercialisation. He has more than 15 years of experience with different MNCs in senior management roles, working across R&D, business development and product management.
Ananya Sen is a marketing communications specialist at ACG with a degree in Pharmacy and has over a decade of experience in the pharmaceutical industry. Her roles have spanned from pharmaceutical journalism and drug regulatory affairs to marketing. In her current position, she is responsible for overseeing brand communications across all ACG’s group companies.