International Journal of Pharmaceutical Sciences and Drug Research

149-159

Authors: SK Nagar1*, MM Soniwala2

The purpose of this investigation was to increase the solubility and dissolution rate of Cilnidipine by the preparation of nanosuspensions with solvent antisolvent method at the laboratory scale. Drug solution of Cilnidipine in acetone this mixture was added to stabilizer solution under continuous homogenization. Central composite design was employed to study the effect of the independent variables on the dependent The relationship between the dependent and independent variables was further Elucidated using multiple liner regression analysis (MLRA) and contour plots. Various process and formulation parameters were screened like homogenization speed, solvent to antisolvent ratio, homogenization time, type of stabilizer, concentration of drug and concentration of stabilizer. Physical stability can be enhancing physical stability of this colloidal system; nanosuspensions were freeze dried using D-mannitol. Seven different stabilizers were tried. Among them Poloxamer 407, Poloxamer 188, PVA and Tween 80 yielded nanosuspension in range of 90 to 350 nm. Freeze dried nanosuspensions were filled in capsules to make a deliverable dosage form and almost 100% drug dissolved in 5 minutes. The outcome of this study reveals the immense potential of nanosuspensions for delivery of Cilnidipine by improving its solubility and dissolution rate. These results show that the preparation of Cilnidipine-loaded nanosuspensions significantly improved the in vitro dissolution rate, thus possibly enhancing the fast onset of therapeutic drug effect.

169-177

Authors: Umang Motka1, Mahesh Dabhi1, Navin Sheth2, Ashvin Dudhrejiya3*

Isradipine is a poorly water soluble antihypertensive drug has low bioavailability. The aim of this study was to formulate and characterize isradipine nanosuspension to enhance the solubility of isradipine and thus its bioavailability. Media milling technique was used for the formulation of nanosuspension. The effects of different important process parameters, i.e. the selection of stirring time, selection of concentration of zirconium beads, stirring speed were investigated by preliminary studies while concentration of stabilizers were optimized by simplex lattice design. Concentration of HPMC E3 LV(X1), Carbopol 934P(X2) and PVP K25(X3) were selected as the independent variables whereas mean particle size (Y1), saturation solubility (Y2) and cumulative percentage drug release (cpr) (Y3) were selected as dependent variables. The optimized batch had 100% w/v of zirconium beads, 0.5%w/v of PVP K25 as stabilizer, 0.1%w/v of isradipine, 15 ml of distilled water and 20 hours of stirring time. The particle size and zeta potential of optimized nanosuspension were 248.6 ± 20 nm and 13.96 ± 5 mV respectively. The size of particles of nanosuspension was measured by particle size analyser and transmission electron microscopy (TEM). Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR) analysis indicated that there was no interaction between drug and stabilizers. The saturation solubility and in vitro dissolution rate of isradipine was significantly increased by particle size reduction and which may leads to increase the bio-availability of the Isaradipine. The stability study of the formulation was carried out for a period of 12 months.

182-186

Authors: Harleen Kaur*, Sunil Kumar Bose, Anitha Vadekeetil, Geeta, Kusum Harjai, Richa

Achillea filipendulina is an aromatic plant of family Asteraceae with bright yellow colour flowers. The objective of the study was to extract the essential oil from the flowers of the selected plant using Clevenger apparatus, to analyse the chemical composition of the oil using GC-MS and to screen the essential oil for its antibacterial property against both gram-positive and gram-negative bacteria. GC-MS results revealed that the main chemical constituents present in the oil were trans 2,7 Dimethyl 4,6 octadien-2-ol (27.93%), borneol (21.44%) and santolina triene (7.13%). The results of agar well diffusion assay revealed that the oil showed antibacterial activity against all the tested bacteria except Pseudomonas aeruginosa. Minimum inhibitory concentration (MIC) of oil was determined against the sensitive bacteria. MIC values against Staphylococcus aureus and Escherichia coli were similar (0.312% v/v) and for Bacillus cereus, MIC value was found to be (0.156%). Results indicated the great antibacterial potential of oil of this plant against gram positive and gram negative bacteria.

195-200

Authors: Animeshchandra G. M. Haldar1*, Santosh S. Chhajed2, Debarshi Kar Mahapatra3, Kanhiya M. Dadure4

In the present investigation, the synthesis of few novel leads bearing 2-(p-hydroxyphenyl)-4–(substitutedphenyl)-1H-1,5–benzodiazepine pharmacophore is described. The substituted chalcone and their derivatives 3(a-j) were synthesized by base catalyzed Claisen-Schmidt condensation between p-hydroxy-acetophenone and appropriate aldehydes. The dibromostyryl ketones 4(a-j) were obtained by the reaction the chalcone with bromine in acetic acid. The dibromostyryl ketone were reacted with methanol in presence of sodium methoxide followed by acidic hydrolysis give 1-(4-hydroxyphenyl)-3-(substitutedphenyl)-1,3-propanediones. The targeted compounds; the substituted 1,5-benzodiazepines were synthesized with o-phenylenediamine and synthesized 1,3-propanediones. The structures of synthesized compounds were confirmed by spectroscopic and analytical techniques (IR, 1H-NMR, and MS). The free radical scavenging activity of the synthesized analogs was monitored by in vitro antioxidant activity protocol. The derivatives 6f, 6g, 6i, and 6j were found to exhibit good antioxidant activity with 59.07%, 41.33%, 68.3% and 60.4% scavenging activity respectively as compared to standard ascorbic acid which demonstrated 79.73% activity. The current research revealed the potential of 2-(p-hydroxyphenyl)-4–(substituted-phenyl)-1H-1,5–benzodiazepine as emerging free radical scavengers. The study helped to establish a structure-activity relationship (SAR) where the substitution on the phenyl moiety of the 1,5-benzodiazepine was found to play profound role and influence over biological activity. The research will open new avenues for the development of antioxidant moieties having perspectives in cancer, inflammation, and several other ailments.