Abstract: The main perspective of the present study aims at overcoming solubility problems by using the technique of solid dispersion. Repaglinide is a BCS Class II drug, having low aqueous solubility and therefore, low bioavailability. Solid dispersions of repaglinide with different carriers Polyvinyl Pyrrolidone (PVP) and Ethyl Cellulose (EC) in different ratios were prepared by suspending method and Dissolving methods. In vitro release studies revealed that the F7 formulation showed extended drug release. So, the dissolution profile of solid dispersion containing EC and PVP K30 (1: 3) was selected as the best formulation because of its extended drug release among all formulations. In conclusion, solid dispersions of Repaglinide in PVP have shown to be a promising approach to improve the bioavailability of Repaglinide.
Abstract: Diabetes is a chronic metabolic disorder that affects the quality of life in terms of physical health, social and psychological well-being. In spite of the enormous progress in the treatment of diabetes using existing commercial drugs, such as, insulin and oral hypoglycemic agents, the quest and search for new drugs is imperative due to several limitations of the commercial drugs. In addition, the existing diabetic drugs are expensive and unaffordable by the rural populace in the developing countries. The present study demonstrates the anti-diabetic property of aqueous extract of Bryophyllum pinnatum (BP) leaves using diabetic rats (albino rats) as models. At the same time, the anti-diabetic effect of the aqueous extract was compared to that of a sample containing a mixture of the extract and a commercial diabetic medicine, glibenclamide. A specified dosage of aqueous extract of Bryophyllum pinnatum (BP) leaves was administered on the experimental diabetic rats, and their BGL was measured and recorded. The results showed a significant drop in the BGL of the diabetic rats to a value close to normal blood glucose level within 120 minutes when only aqueous extract from BP leaves was used. When a sample containing a mixture of the aqueous extract and glibenclamide was administered, a further drop in BGL was observed. Therefore, the results reveal that aqueous extract of Bryophyllum pinnatum leaves have significant anti-diabetic properties, and that the performance of the existing drugs (glibenclamide) could be enhanced with the use of the aqueous extract.
Abstract: The aim of present work was to optimize the effect of Ethyl Cellulose (EC) and Polyvinyl Pyrrolidone (PVP) concentration in extended release solid dispersion of Glibenclamide using combination of hydrophilic and hydrophobic polymers such as Polyvinyl Pyrrolidone and Ethyl cellulose. The advantage of solid dispersion technique provides a unique approach to particle size reduction and increased rates of dissolution. The compatibility studies of the drug and polymers were studied by TLC and results suggested no interaction between drug and polymers. Solid dispersions of Glibenclamide were prepared by common solvent evaporation method using Polyvinyl Pyrrolidone and Ethyl cellulose. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. F2 formulation prepared by solid dispersion method, displayed extended drug release followed by Higuchi matrix model indicating diffusion release of GLB from polymer matrices.
Abstract: This study has investigated the antidiabetic and
antioxidant potential of Pseudovaria macrophylla bark extract on
streptozotocin–nicotinamide induced type 2 diabetic rats. LCMSQTOF
and NMR experiments were done to determine the chemical
composition in the methanolic bark extract. For in vivo experiments,
the STZ (60 mg/kg/b.w, 15 min after 120 mg/kg/1 nicotinamide, i.p.)
induced diabetic rats were treated with methanolic extract of
Pseuduvaria macrophylla (200 and 400 mg/kg·bw) and
glibenclamide (2.5 mg/kg) as positive control respectively.
Biochemical parameters were assayed in the blood samples of all
groups of rats. The pro-inflammatory cytokines, antioxidant status
and plasma transforming growth factor βeta-1 (TGF-β1) were
evaluated. The histological study of the pancreas was examined and
its expression level of insulin was observed by
immunohistochemistry. In addition, the expression of glucose
transporters (GLUT 1, 2 and 4) were assessed in pancreas tissue by
western blot analysis. The outcomes of the study displayed that the
bark methanol extract of Pseuduvaria macrophylla has potentially
normalized the elevated blood glucose levels and improved serum
insulin and C-peptide levels with significant increase in the
antioxidant enzyme, reduced glutathione (GSH) and decrease in the
level of lipid peroxidation (LPO). Additionally, the extract has
markedly decreased the levels of serum pro-inflammatory cytokines
and transforming growth factor beta-1 (TGF-β1). Histopathology
analysis demonstrated that Pseuduvaria macrophylla has the
potential to protect the pancreas of diabetic rats against peroxidation
damage by downregulating oxidative stress and elevated
hyperglycaemia. Furthermore, the expression of insulin protein,
GLUT-1, GLUT-2 and GLUT-4 in pancreatic cells was enhanced.
The findings of this study support the anti-diabetic claims of
Pseudovaria macrophylla bark.