Abstract
Starting from the premise that a reduced number of active pharmaceutical ingredients (APIs) are used to treat hypotension, the aim of this study consisted of developing new formulations of caffeine-orodispersible tablets (CAFODTs). The formulation variables were the type of disintegrant and its concentration. The CAF-ODTs were prepared by direct compression, (CAF1, CAF2 and, CAF3) each of them containing 100 mg of CAF / tablet. The proposed formulations were analyzed from a pharmacotechnical point of view. For the formulations developed the tablets’ physical appearance, resistance to crushing, friability, disintegration behaviour, and the in vitro caffeine release were evaluated. White tablets, with a resistance to crushing decreasing in the following order CAF1 > CAF2 > CAF3 were obtained. The friability test showed that all the formulations are respecting the in-force European Pharmacopoeia (Ph. Eur. 10) requirements with values less than 1 %. The disintegration time for all three formulations was less than 180 seconds, the smallest time being registered in the case of CAF2 formulation, where Sodium Starch Glycolate (SSG) was used as a disintegrant (24-30 s, as a result of the different methods used. Through the in vitro releasing study, it was observed that over 99.9 % caffeine was released from all three analyzed formulations. By investigating the amount of caffeine released after 1 minute, it can be noticed that the largest amount released was recorded in CAF2 formulations, where SSG was used as a disintegrant. Compared to CAF2, the amount of CAF released was reduced to half, after the first five minutes for CAF1 formulation, where sodium croscarmellose was used, and ten times lower in the case of CAF3 where no disintegrant was used. Based on the results obtained we can conclude that all three formulations are respecting the pharmacotechnical in-force officinal requirements. The presence of SSG in the CAF2 formulation led to obtaining tablets with a reduced disintegration time in comparison to the other two formulations proposed in this study.
Highlights
Caffeine (1,3,7-trimethylpurine-2,6-dione) (CAF) represents a drug that might be used for multiple therapeutic effects
The therapeutic effects that can be attributed to caffeine: analgesic effect based on the vasoconstrictor effect and on its capacity of prohibiting the prostaglandins synthesis, favours the dopaminergic neuronal protection with good effects on Parkinson disease, conducts to a decrease of β-amyloid production decreasing the risk of Alzheimer disease, has the property of increasing the arterial tension and produces bronchodilatation [2,3,4,5,6]
Taking into account this aspect, our objective is to develop and evaluate CAF orodispersible tablets (CAF-ODTs) for patients with diseases associated with hypotension
Summary
Caffeine (1,3,7-trimethylpurine-2,6-dione) (CAF) represents a drug that might be used for multiple therapeutic effects. Caffeine is a well-known used drug to treat hypotension associated with various pathologies, but on the pharmaceutical market, no caffeinecontaining (over-the-counter) OTCs are found Taking into account this aspect, our objective is to develop and evaluate CAF orodispersible tablets (CAF-ODTs) for patients with diseases associated with hypotension. The superdisintegrants that presented the best properties regarding the disintegration times are sodium croscarmellose usually used in concentrations between 2-8 %, sodium starch glycolate used in orodispersible tablets in concentrations between 4-8 % and, Crospovidone (2-5 %) [20,21]. This study aimed to obtain CAF-ODTs containing 100 mg of caffeine and to evaluate the superdisintegrant effect and compression force role
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