• PHARMSCI-3-31_F6

    Optimization of Bifonazole-Loaded Nisomal Formulation Using Plackett-Burman Design and 23 Factorial Design

    Bifonazole is an imidazole antifungal drug. It is highly lipophilic drug with a very short half-life and is minimally absorbed following dermal application. Niosomes are excellent candidate as potential drug delivery system because of their improved drug solubilization, enhanced penetration power, long shelf life and ease of preparation and administration.

  • PHARMSCI-4-23_F1

    Improvement in Dissolution of Bosentan Monohydrate by Solid Dispersions Using Spray Drying Technique

    Bosentan monohydrate (BM), a dual endothelin receptor antagonist, is indicated for the treatment of patients with pulmonary arterial hypertension (PAH). It is poorly soluble in water, and having absolute bioavailability of 50%.

  • PHARMSCI-3-79_GA1

    Structural Features of Quercetin Derivatives by Using Pharmaco-phore Modeling Approach

    Quercetin which is a natural occurring flavonoid, exert a direct pro-apoptotic effect on tumor cells by blocking the growth of several cancer cell lines at different phases of the cell cycle. Quercetin derivatives have attracted considerable attention for their cytotoxity against human cancer cell lines. In this study the derivatives of Quercetin were used for docking followed by pharmacophore modeling for studying the 3D features and configurations responsible for biological activity of structurally diverse compounds.

  • PHARMSCI-3-164_F4b

    Structural Insights into the Molecular Design of HER2 Inhibitors

    The present study was aimed at designing some potential candidates as HER2 inhibitors used in breast cancer.

  • PHARMSCI-2-66_F1

    Signal Detection and their Assessment in Pharmacovigilance

    Signal detection and its assessment is the most important aspect in pharmacovigilance which plays a key role in ensuring that patients receive safe drugs. For detection of adverse drug reactions, clinical trials usually provide limited information as they are conducted under strictly controlled conditions. Some of the adverse drug reactions can be detected only after long term use in larger population and in specific patient groups due to specific concomitant medications or disease.

Editor's Choice

Improvement in Dissolution of Bosentan Monohydrate by Solid Dispersions Using Spray Drying Technique

Pankaj V. Dangre, Vikesh B. Sormare, Mangesh D. Godbole

Background:

Bosentan monohydrate (BM), a dual endothelin receptor antagonist, is indicated for the treatment of patients with pulmonary arterial hypertension (PAH). It is poorly soluble in water, and having absolute bioavailability of 50%.

Objective:

The aim of the present work is to develop and evaluate the solid dispersions (SD) of a poorly water soluble drug bosentan monohydrate (BM).

Method:

Solid dispersions (SDs) systems of BM were prepared with Hydroxy propyle β-cyclodextrin (HPβ-CD) and Polyethylene glycol (PEG-4000) polymers using a spray drying technique.

Result:

The significant rise in a saturation solubility 174.23±1.36 mg/mL; and drug dissolution 95.11±1.22%; was observed with optimized formulation (SD 6). The solid state characterization of optimized formulation (SD 6) by SEM, DSC, and XRPD revealed the absence of crystalline nature of BM in solid dispersion. High dissolution rate of solid dispersion (SD 6) compared with pure drug indicated the increase in dissolution characteristics.

Conclusion:

In conclusion, our studies illustrated that spray drying technique could be useful large scale producing method to prepare the solid dispersion of bosentan with HP β-CD, which can improve the solubility as well as stability of the formulation.


April 28, 2017
READ MORE

Most Accessed Articles

Quick Links

Indexing Agencies

READ MORE