Cardiovascular diseases (CVDs) have increased the mortality rate both in developing as well as developed countries, however a lower trend in death rates have been seen in developed and high income countries like USA, UK, Australia, Japan and other European countries due to improved life style, better strategic implementation, control of disease both in young and adults and especially reduced smoking habits. In developing countries CVD become an alarming situation due to prevalence of disease in early age that later on become chronic and difficult to control. Various risk factors that can contribute toward CVD in developing countries include smoking, high alcohol and salt intake, dietary factors, diabetes, high blood pressure and psychosocial aspects such as stress, anxiety and depression. Various other factors such as family history and the gender difference also contributing towards the high risk of developing CVD.Rehan et al., International Current Pharmaceutical Journal, July 2016, 5(8): 69-72http://www.icpjonline.com/documents/Vol5Issue8/02.pdf
Background. Poorly water-soluble drugs do not dissolve well in aqueous-based gastrointestinal fluid; therefore, they are not well absorbed. Thus, employing a suitable solubility enhancing technique is necessary for such a drug. Drug/HP-β-CD complexation is a promising way to improve solubility and dissolution of a poorly water-soluble drug. Levodropropizine was used as a model drug in this study. Objectives. The purpose of this research was to enhance the aqueous solubility and dissolution rate of levodropropizine by employing the inclusion complexation technique. Material and methods. A microparticle formulation was prepared from levodropropizine and hydroxypropyl-β-cyclodextrin (HP-β-CD) in a 1:1 molar ratio through the spray-drying technique. The host-guest relationship between levodropropizine and HP-β-CD was also investigated using the molecular docking computational methodology. The aqueous solubility and dissolution rate of levodropropizine in formulations were assessed and compared with those of the drug alone. X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FTIR) were applied for the solid-state characterization of the prepared samples. Results. According to the research outcomes, the levodropropizine/HP-β-CD formulation had enhanced the aqueous solubility (351.12 ±13.26 vs 92.76 ±5.00 mg/mL) and dissolution rate (97.83 ±3.36 vs 3.12 ±1.76% in 10 min) of levodropropizine, compared to the plain drug powder. The levodropropizine/ HP-β-CD formulation had converted the crystalline drug into its amorphous counterpart. Furthermore, no covalent interaction was found to exist between levodropropizine and HP-β-CD. The spray-dried particles were discrete. Each particle had a shriveled appearance. Conclusions. The levodropropizine/HP-β-CD formulation is, therefore, recommended for the more effective administration of levodropropizine through the oral route.
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