Current Issue : July - September Volume : 2016 Issue Number : 3 Articles : 8 Articles
This work aimed to improve carvedilol dissolution through preparation of nanoparticles to be formulated as buccoadhesive gel. Drug excipients compatibility was studied using fourier transform infra-red spectroscopy and differential scanning calorimetry. Carvedilol nanoparticles were prepared by nanoprecipitation method using Eudragit® RS100 as a polymer and poloxamer 407 as a stabilizer. Eight nanoparticles formulations were prepared adopting a 41×21 factorial design. The nanoparticles appearance was spherical and uniform. The particle size of the prepared formulations ranged from 149 to 177 nm and it wasn’t significantly affected by any of the tested formulation variables. On the other hand, changing the drug to polymer ratio significantly affected both drug loading and dissolution parameters (P value < 0.05). Drug loading ranged from 76.2-95.97%. The release data showed fickian diffusion mechanism. The formula of choice was suspended in 4% w/v HPMC gel. The gel had pH of 6.36, pseudoplastic flow and acceptable bioadhesion which are required for buccal application. It enhanced drug permeation through chicken pouch membrane in comparison to control drug gel of the same concentration and it was physically and chemically stable on storage for six months at 40±2°C /75±5%RH and one year at 5±3°C....
In the present study porous scaffold films of clarithromycin were prepared by the process of solvent casting method. The porous films were prepared using chitosan dissolved in acetic acid in different concentrations and PEG-4000 which works as plasticizer and porosity enhancer. The preliminary drug identification studies showed that drug confers to all standard values for solubility, melting point, UV and IR. Porous films prepared by solvent casting method with different polymer concentrations were subjected to various investigations namely moisture content, water absorption ratio, swelling index, porosity, folding endurance, tensile strength, drug content and in-vitro drug release. Formulation FB4 was found to be an optimized formulation with moisture content 4.36±0.316, water absorption ratio 245±1.57, swelling index 219.47±3.66, porosity 54.71±0.737, folding endurance 213±4.16, tensile strength 43.7 mJ/cm2, drug content 99.6±0.88 and in-vitro drug release 99.64±0.88 for 12 hrs. From the present study it was concluded that porous scaffold film of clarithromycin was successfully prepared by solvent casting method using chitosan polymer in different ratio with PEG-4000 to achieve a controlled and efficient release of the drug. Overall the porous scaffold films offered potential advantage of high drug content (99.6±0.88) and homogenous drug dispersion....
Migraine is a common chronic disorder with episodic attacks. Zolmitriptan is an effective drug used for the treatment of migraine. This study aimed to formulate fast dissolving oral films (FDOFs) of zolmitriptan (FDOFs) using different polymers such as hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose (NaCMC), sodium alginate (Na alginate), hydroxyethyl cellulose (HEC), gelatin, polyvinyl alcohol (PVA) in addition to glycerin as a plasticizer. The films were prepared by solvent casting method. The prepared films were evaluated for peeling from Petri dish, color, transparency, homogeneity, average weight, thickness, disintegration, folding endurance, drug content and in-vitro drug release. Results showed that the film containing 1% PVA, 5 % mannitol and 10 % glycerin (F3) appeared to have superior properties as FDOF. The optimized film disintegrated within 9 seconds and released 100 % of zolmitriptan in 3 min. The folding endurance was satisfactory (˃300). Moreover, drug content was found to be 99.5 % and thickness was 0.08 mm....
Granisetron hydrochloride (GH) is a potent, selective antagonist of 5-HT3 receptors that is mainly absorbed after oral administration; oral bioavailability is about 60% as a result of first pass hepatic metabolism. The objective of this study was to develop GH-loaded intranasal spanlastic dispersions to produce a more targeted delivery to brain bypassing the liver metabolism and control release of the drug in the brain. GH-loaded spanlastic dispersions were prepared by ethanol injection method using span 60 and tween 60 or tween 80 were explored as edge activators. The prepared eleven dispersions were evaluated for vesicle size, zeta potential, polydispersity index (PI), entrapment efficiency (EE %) and in-vitro drug release studies. The selected dispersions were evaluated for morphology. The best achieved spanlastic dispersions (S4, S9) displayed nanosized spherical vesicles (338.5, 426.6 nm) respectively having a negative zeta potential S4 (-23.1Mv), S9 (-27.5 mV), EE% S4 (22.2%) S9 (24.7%) and optimum specification with drug release about S4 (99.3%), S9 (86.3%) after 6 hrs....
Repaglinide (RPG) is poorly water soluble drug in BCS (Low solubility, High permeability). The objective of this study was to enhance the dissolution of RPG for oral drug delivery. RPG solid dispersions (F1-F12) were prepared by solvent evaporation method using PVP K30, PEG 4000, HPMC E5, HPMC E50 with a different drug: polymer ratios. The prepared SD were evaluated for drug content, practical yield, saturated solubility, in-vitro dissolution, X-ray diffraction, DSC, IR and SEM. The differential scanning calorimetry (DSC) thermograms and infra-red (IR) spectra revealed that there was no interaction of RPG with additives. RPG-SD gave higher solubility and faster dissolution rate when they compared to pure drug due to decrease of crystallinity of RPG which confirmed by XRD results. Repaglinide solid dispersions using PEG 4000 (1:2) as a polymer in solid dispersions showed promising results in enhancement of repaglinide properties....
The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug by a solid dispersion technique, in order to investigate the effect of these polymers on release mechanism from solid dispersions. Telmisartan was used as a model drug to evaluate its release characteristics from different matrices. Solid dispersions were prepared by using polyethylene glycol 6000 (PEG-6000), in different drug-to-carrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solid dispersions were prepared by solvent method. The pure drug and solid dispersions were characterized by in-vitro dissolution study. Distilled water was used as dissolution media, 1000 ml of distilled water was used as dissolution medium in each dissolution basket at a temperature of 37°C and a paddle speed of 100 rpm. The very slow dissolution rate was observed for pure telmisartan and the dispersion of the drug in the polymers considerably enhanced the dissolution rate. This can be attributed to improved wettability and dispersibility, as well as decrease of the crystalline and increase of the amorphous fraction of the drug. In this study solvent evaporation technique was used for the preparation of solid dispersion with high drug content, dissolution rate, solubility in PEG 6000 (1:6). From this study it was concluded that solubility and dissolution rate was increased with the ratio of drug:PEG 6000 at 1:6 as compare with pure drug. Solid dispersion containing polymer prepared with solvent method showed significant improvement in the release profile as compared to pure drug, telmisartan....
Solid lipid nanoparticles (SLNs) are drug carriers offering clear advantages over other existing methods for nanoparticle preparation such as ease of handling and faster production process without any sophisticated equipment. The lipids used are generally biocompatible, biodegradable with less toxicity compared to polymeric nanoparticles. The objective of this work was to prepare SLNs with optimized physical properties, thereby further drug loading and optimizing SLNs targeting could be obtained. For that purpose, different lipids with various concentrations were tried: Precirol®5ATO, Compritol®888 ATO, glyceryl monostearate and palmitic acid. The chosen surfactants were Tween 80 and Brij®78. The obtained plain SLNs varied in size from 156 nm to >1 µm with Tween 80 and from 107 nm to >1 µm with Brij®78. The PDI values with both surfactants varied from 0.28 to 1. The recorded zeta potential values (ζ) ranged from -3.6 to -30.8 with both surfactants. The largest particles were obtained with palmitic acid; hence it was excluded from further studies. The average particle sizes ranged from 44 to 914 nm and the PDI varied from 0.17 to 0.67. However, the ζ values didn’t change considerably. So it can be concluded that SLNs with a reasonable particle size can be loaded with a drug for targeting....
Avanafil is a phosphodiesterase type 5 (PDE5) inhibitor characterized by a faster onset and lower side effects than other PDE5 inhibitors. This study aimed at improving avanafil solubility in water by its complexation with β-cyclodextrin. Two methods of preparation of complex were investigated namely, rotavap or kneading techniques. Phase solubility analysis showed that drug and β-cyclodextrin formed complex in ratio of 1:1. The complex prepared by rotavap exhibited significantly higher solubility in water than that prepared by kneading (p<0.05). The prepared complexes were investigated using infrared spectroscopy, differential scanning calorimetry and x-ray powder diffraction. Solid state characterization showed that the use of heat during preparation resulted in formation of a new solid phase with lower crystalline properties. The complex prepared by rotavap had higher extent of dissolution in-vitro than pure avanafil, without any significant change in rate....
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