Development of Controlled- Release Solid Dispersion Granules Containing a Poorly Water-Soluble Drug, Porous Calcium Silicate, and the Water-Soluble Polymer Polyvinylpyrrolidone
Journal Title: Journal of Pharmaceutics & Pharmacology - Year 2018, Vol 6, Issue 1
Abstract
Objectives: This study sought to develop controlled-release solid dispersion granules containing a poorly water-soluble drug, porous calcium silicate (PCS), and a water-soluble polymer. Methods: Nifedipine (NIF) and indomethacin (IND), and several water-soluble polymers were selected to prepare solid dispersion granules. Differential scanning calorimetry, Powder X-ray diffraction, and Fourier transform infrared (FT-IR) were used to estimate the crystallinity of drugs in the PCS granules and to determine interactions between drug and PCS. Results: Among the water-soluble polymers used in this study, only polyvinylpyrrolidone (PVP) permitted sustained release from the NIF granules. The release rates of NIF from the granules decreased as the molecular weight or amount of PVP in the granules was increased. A significant loss of crystallinity of NIF in the granules and the existence of a hydrogen bond between NIF and PCS or PVP, as well as between PCS and PVP were observed. To examine the applicability of this system to other drugs, indomethacin (IND) was selected. However, IND was rapidly released from the PVP-containing granules. FT-IR spectroscopy results revealed the existence of a hydrogen bond between IND and PVP, but IND and PCS appeared to interact via salt formation. Conclusion: Hydrogen bonding among the drugs, PCS, and PVP may have contributed to the slow drug release in the developed system.
Authors and Affiliations
Koichi Takahashi
Keywords
Related Articles
- EP ID EP486690
- DOI 10.13188/2327-204X.1000025
- Views 89
- Downloads 0
Molecular Inclusion Complexes of β-Cyclodextrin Derivatives Enhance Aqueous Solubility and Cellular Internalization of Paclitaxel: Preformulation and In vitro Assessments
Drugs with low aqueous solubility and permeability possess substantial challenges in designing effective and safe formulations. Synergistic solubility and permeability enhancement in a simple formulation can increase bio...
The Role of Glycogen Synthase Kinase 3 Beta in Neuroinflammation and Pain
Neuroinflammation is a crucial mechanism related to many neurological diseases. Extensive studies in recent years have indicated that dysregulation of Glycogen Synthase Kinase 3 Beta (GSK3β) contributes to the developmen...
NMDA Receptor Antagonism by Phencyclidine Reduces NWASP and WAVE1 Protein Expression and Reduces Levels of Myelination Markers in the Prefrontal Cortex of Rats
N-methyl-D-aspartate (NMDA) receptor antagonism by perinatal phencyclidine (PCP) treatment leads to neuronal damage and causes long-term behavioural alterations in rodents. It is routinely used to model pathological proc...
Prevention of Crystal Formation during Formulation of Acyclovir Powder for Solution for Infusion
Aims and objectives: The main objective of the present work is to develop acyclovir powder for solution for infusion with clear solution upon half sealing and formation of stable cake after freezing drying programme. Dur...
Instability of Cefpodoxime Proxetil Oral Suspension at Different Temperature Storage Conditions
The advantages of oral dosage form over other dosage forms are responsible for its popularity which includes its ease of administration, patient compliance and stability of the formulation. This study compared the stabil...