Development of caffeine tablets exhibiting similar dissolution profile to reference tablets

Abstract

Caffeine is a naturally occurring stimulant drug that has an antagonistic effect on adenosine receptors in the central nervous system. The aim of this research project was to develop caffeine tablets with a dissolution profile that mimics the dissolution profile of good manufacturing practice conforming caffeine reference tablets (Koffein Apofri). A total of nine immediate-release formulations were manufactured using direct compression throughout the project. The ninth formulation (F9) matched the reference tablets by having six measurements that represent the entire dissolution profile within the designated ± 5% limits for dissolved caffeine. The main factors that had to be optimized to control the dissolution was the amount of disintegrant used, and the hardness of the tablets.To ensure the quality of the pharmaceutical formulation, F9 was subjected to mandatory tests from the European Pharmacopoeia, along with a few optional tests that were prescribed by the manufacturers. The formulation met all requirements, however the results from the uniformity of content test were inconclusive.

Koffín er náttúruefni sem hefur örvandi áhrif í gegnum antagonista áhrif á adenósín viðtaka í miðtaugakerfinu. Markmið þessa rannsóknarverkefnis var að þróa koffín töflur með losunarprófíl sem hermir eftir losunarferli viðmiðunartaflna sem fylgja góðum framleiðsluháttum (Koffein Apofri).Í heildina voru níu formúleringar hraðlosandi taflna framleiddar með beinum slætti. Níunda formúleringin (F9) samsvaraði viðmiðunartöflunum með því að hafa sex mælingar sem lýstu öllum losunarferlinum sem voru innan ± 5% marka með tilliti til uppleysts koffíns. Lykilatriði sem þurfti að fínstilla til að stýra upplausninni voru magn sundrunarefnis og harka taflanna.Til að tryggja gæði formúleringarinnar, gekkst F9 undir skyldubundin próf frá Evrópsku Lyfjaskránni, auk nokkurra valfrjálsra prófa sem fyrirskipuð voru af framleiðendum. Formúleringin stóðst allar gæðaprófanir, en innihaldsjöfnuðs prófið gaf ófullnægjandi niðurstöður.