Introduction

The major challenge in pharmaceutical pre-formulation studies are APIs, which exhibit poor water solubility and low bioavailability. Several techniques are known to enhance the solubility and bioavailability of drugs i.e. supercritical fluid technology, grinding method, solid liquid systems.

Materials & Methods

Ibuprofen (Shasun Chemicals and Drugs, India) and furosemide (IPCA, India) were chosen as model drugs insoluble in water. Ibuprofen represents the API from BCS class II, whereas furosemide belongs to BCS class IV. To improve their solubility Neusilin US2 (Fuji Chemical Industry), PEG 400, PEG 4000 (Merck) or Labrasol (Gattefosse, France) were used. In case of furosemide supercritical fluid technique was applied to prepare solid dispersion of the API in PEG 4000 (1:11). The substances were treated by carbon dioxide in supercritical conditions using a high pressure reactor Roth. Furosemide liquisolid formulations were prepared using PEG 400 as liquid vehicle with two different drug concentations 10% and 20%. Microcrystalline cellulose, anhydrous dibasic calcium phosphate - Fujicalin®, and Neusilin US2 were used as s solid excipients. After adsorption of furosemide liquid formulation on solid carriers, liquisolid formulation were compacted directly on Korch EK0 tabletting machine. In case of ibuprofen, the API was dissolved in Labrasol and then the solution was adsorbed on Neusilin US2 by simple blending. Dissolution test was performed to examine the influence of both the process parameters and carriers on the API solubility.

Results

All the results showed that the carrier as well as process parameters had influence on the API dissolution. In case of formulations obtained after carbon dioxide treatment of furosemide in supercritical conditions, a higher solubility and dissolution rate was obtained, when the drug was present in the form of solid dispersion. Afert 1 h the amount of furosemide dissolved was approximately 30 times grater than drug alone. With regard to liquisolid formulations the best results were found for formulations containing 10% furosemide solution and Fujicalin® as a carrier material. After 2 h the amount of released drug was over 2-fold higher as compared to commercial tablets. The results showed that the release rate of furosemide increased markedly when present in liquisolid tablets. Similar results were found in case of ibuprofen liquid formulation adsorbed on Neusilins US2. After 1 h the amount of the drug dissolved increased from 36% to 76%.

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