Screening of Sacrificial Excipients for Arresting Devitrification of Itraconazole from Solid Dispersion
Journal Title: Turkish Journal of Pharmaceutical Sciences - Year 2019, Vol 16, Issue 2
Abstract
Objectives: The aim of the present investigation was to develop a solid dispersion of itraconazole (ITR) using sacrificial excipients like pregelatinized starch and spray-dried lactose alongside hydroxypropyl methylcellulose and Poloxamer 188, thereby arresting the conversion of the amorphous form of ITR to crystalline form, and to assess the dissolution stability of an amorphous form of the drug during short-term storage. Materials and Methods: ITR-loaded solid dispersions were prepared by kneading. Formulation optimization was achieved by using a 24 full factorial design on the basis of cumulative percent drug released at t30, t60, and t120 min. An artificial neural network (ANN) was also applied as a statistical tool for obtaining better predictive ability and the outcomes of the ANN were compared with that of Design-Expert software. Results: The spectral data revealed no drug–carrier interactions. The P-X-ray diffraction study of the optimized batch showed a decrease in the crystallinity of drug as compared to the untreated drug. The in vitro dissolution studies of the optimized batch showed higher dissolution (92% at 120 min) in comparison to the other formulations. The dissolution stability study was performed at 40°C and 75% relative humidity for 90 days for the optimized formulation. The results of the optimized batch showed insignificant changes in cumulative percentage drug release during storage. Conclusion: Dissolution stability could be attributed to the presence of sacrificial excipients as they tend to absorb moisture during storage and possibly get converted into crystalline form, thereby minimizing the recrystallization of ITR.
Authors and Affiliations
Bhargavi M. PATEL, Mukesh C. GOHEL, Vaishali T. THAKKAR, Lalji H. BALDANIYA, Ruby R. CHRISTIAN, Tejal R. GANDHI
Keywords
Related Articles
- EP ID EP684684
- DOI 10.4274/tjps.galenos.2018.54871
- Views 190
- Downloads 0
The Anticancer and Anti-inflammatory Effects of Centaurea solstitialis Extract on Human Cancer Cell Lines
Objectives: Natural products originating from plants have been used for many years in the treatment of various diseases, including cancer. Centaurea solstitialis subsp. solstitialis is used in Turkish folk medicine. This...
Quantitative Structure–Activity Relationship Analysis of Selective Rho Kinase Inhibitors as Neuro-regenerator Agents
Objectives: To understand the role of Rho (serine/threonine) kinases in the treatment of neurological segments, attempts have been made to find potent inhibitors of Rho enzyme by a 2D quantitative structure–activity rela...
Considering the Effect of Rosa damascena Mill. Essential Oil on Oxidative Stress and COX-2 Gene Expression in the Liver of Septic Rats
Objectives: Sepsis is a clinical illness with a high rate of mortality all over the world. Oxidative stress is considered the main phenomenon that occurs in sepsis. Rosa damascena Mill. is an ancient herbal plant with hi...
The In Vivo Antinociceptive and Antiinflammatory Effects of Verbascum exuberans Hub.-Mor.
Objectives: Safe and effective drugs are still lacking for many pain therapies. In recent years, growing interest has been devoted thus on herbal drugs as an option to identify new pain killers. Based on this, extensive...
In Vivo Antioxidant Activity of Different Fractions of Indigofera Barberi Against Paracetamol-induced Toxicity in Rats
Objectives: To evaluate the in vivo antioxidant activity of chloroform extract fractions of Indigofera barberi (whole plant) against paracetamol-induced toxicity in rats. Materials and Methods: For 7 days, rats were tre...