25 research outputs found
EFFECT OF A PARTICLE ENGINEERING PROCESS ON POLYMORPHIC TRANSITION OF PYRAZINAMIDE
No full textObjective: The objective of this work was to investigate the effect of processing on physicochemical properties of spray dried Pyrazinamide. Methods: Pyrazinamide was spray dried using several spray drying conditions, FTIR, XRD and thermal analysis were undertaken for all samples. A comparison of crystalline/amorphous nature of the starting material as well as processed materials was carried out.Results: The unprocessed material was a typical crystalline material composed of a mixture of alpha and gamma polymorphic forms of pyrazinamide.In contrast spray dried materials showed other mixtures of different polymorphs of  pyrazinamide based on spray drying conditions. In other words, the solid state of spray dried material was dependent on processing parameters (solvent systems, inlet temperature), which may indicate the effect of processing conditions on the solid state of Pyrazinamide.Conclusion: Processing of Pyrazinamide without excipients gave different polymorphs, according to the solvent mixture used in the spray drying processÂ
EFFECT OF VISCOSITY, SURFACTANT TYPE AND CONCENTRATION ON PHYSICOCHEMICAL PROPERTIES OF SOLID LIPID NANOPARTICLES
No full textObjective: The aim of the current work was to look into the feasibility of planning of solid lipid nanoparticles of Glyceryl mono stearate containing Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs.Methods: Solid lipid nanoparticles loaded with three model lipophilic drugs were developed by high shear hot homogenization method. The model drugs used are Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide. Glyceryl monostearate was used as the lipid core; Tween 20 and Tween 80 were employed as surfactants and lecithin asco-surfactant. Many formulation parameters were manipulated to receive high quality nanoparticles. The prepared solid lipid nanoparticles were evaluated by different standardphysical and imaging methods. The efficiency of drug release form prepared formulaewas studied using In vitro technique to utilize of dialysis bag technique. The stability of prepared formulae was studied by thermal procedures and infrared spectrum analysis.The physicochemical properties of the prepared formulae like particle size, drug entrapment efficiency, drug loading capacity, yield content and In vitro drug release behavior were too assessed.Results: The average particle diameter measured by a laser diffraction technique was (194.6±5.03 to 406.6±15.2 NM) for Dibenzoyl peroxide loaded solid lipid nanoparticles, (220±6.2 to 328.34±2.5) NM for Erythromycin loaded solid lipid nanoparticles and (227.3±2.5 to 480.6±24) NM for Triamcinolone acetonide loaded solid lipid nanoparticles. The entrapment efficiency and drug loading capacity, determined with ultravioletspectroscopy, were 80.5±9.45% and 0.805±0.093%, for Dibenzoyl peroxide, 96±11.5 and0.96±0.012 for Triamcinolone acetonide and 94.6±14.9 and 0.946±0.012 for Erythromycinbase respectively. It was found that model drugs showed significant faster release patterns when compared with commercially available formulations and pure drugs(pË‚0. 05). Thermal analysis of prepared solid lipid nanoparticles gave indication ofsolubilization of drugs within a lipid matrix. Fourier Transform Infrared Spectroscopy(FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating nointeraction between drugs and lipid matrix and being only dissolved in it. Electronmicroscope of scanning and transmission techniques indicated sphere form of preparedsolid lipid nanoparticles with smooth surface with size below 100 nm.Conclusion: In conclusion, it may be concluded that solid lipid nanoparticles with small particle size have high encapsulation efficiency, and relatively high loading capacity for Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs can be obtained by this method.Â
Design and evaluation of combined atorvastatin and ezetimibe optimized self- nano emulsifying drug delivery system
No full textEFFECT OF ADDITIVES ON INTRANASAL PREPARATION OF CYANOCOBALAMIN
No full textThe following study involves formulation and evaluation of intranasal preparation of cyanocobalamin. The design of the formula was achieved by preformulation studies of each of solubility, partition, permeation and stability of cyanocobalamin. HPLC (stability indicating assay) wasused only in the stability studies of cyanocobalamin, other parameters were analyzed using a prevalidated spectrophotometric analytical method. In the meantime,such selected adjuncts should have no significant effects on the physical characteristics of the intranasal drops. All components included in the formula were tested regarding their effects on the tested parameter. Also, they were investigated regarding their effect on each parameter tested including the permeation pattern. The latter parameter could be a substitute for in vivo bioavailability, since the data proved that such parameter is highly indicative. Based on the above studies a formula of intranasal drops of cyanocobalamin was designed to contain ingredients suitable for nasal administration. Such formula achieve another important goal which is improving the patient compliance. The formula contains: Cyanocobalamin 0.5%, Sodium metabisulphite 0.5%, β-cyclodextrin 0.5%, Glycerol 10% and Benzalkonium chloride 0.1%. All ingredients were dissolved in a solution prepared at pH value 5.6 using citrate/phosphate buffer.Â
EZETIMIBE NANOSTRUCTURED LIPID CARRIERS (NLCs): A NEW TECHNIQUE TO OVERCOME THE LIMITATIONS OF ORAL ADMINISTRATION
No full textObjective: Ezetimibe (EMB) is a commonly used lipid-lowering medication that lowers cholesterol and triglycerides. Because of its lower water solubility and hepatic metabolism, it necessitates the formulation of drug delivery systems that are capable of improving solubility and avoiding hepatic effect.
Methods: Ezetimibe nanostructured lipid carriers (EMB-NLCs) were formulated and examined. They were formulated through emulsification with a high homogenization speed and ultrasonication (The method and evaluation parameters have been mentioned under method section in Formulation of EMB-NLCs paragraph).
Results: The formulated NLCs have exhibited particle size (P. S.) between 163.6±7.20 and 866.66±18.65 nm and the zeta potential (Z. P.) values have ranged between-24±1.25 and-35±0.25 mV. Besides, they exhibited higher EE% than 77 percent and the drug encapsulated in lipid matrix was in amorphous state. Pharmacokinetics of optimized formula (F1; composed of 2% w/w Gelucire® 43/01, 8% w/w Miglyol® 812 N, 0.5% w/w lecithin and 2% w/w Poloxmer® 188) have exhibited 2.63-and 2.33-fold increase in oral bioavailability in comparison with EMB suspension and marketing product (Ezetrol® 10 mg tablet), respectively.
Conclusion: These studies have demonstrated that, NLCs are superior for enhancing in vivo behavior and oral bioavailability of EMB
Design, Formulation, and Characterization of Valsartan Nanoethosomes for Improving Their Bioavailability
No full textThe objective of this study was to formulate and evaluate valsartan (VLT) ethosomes to prepare an optimized formula of VLT-entrapped ethosomes that could be incorporated into a sustained release transdermal gel dosage form. The formulation of the prepared ethosomal gel was investigated and subjected to in vitro drug release studies, ex vivo test, and in vivo studies to assess the effectiveness of ethosomal formulation in enhancing the bioavailability of VLT as a poorly soluble drug and in controlling its release from the transdermal gel dosage form. The acquired results are as follows: Dependent responses were particle size, polydispersity index, zeta potential, and entrapment efficiency. The optimized VLT-ETHs had a nanometric diameter (45.8 ± 0.5 nm), a negative surface charge (−51.4 ± 6.3 mV), and a high drug encapsulation (94.24 ± 0.2). The prepared VLT ethosomal gel (VLT-ethogel) showed a high peak plasma concentration and enhanced bioavailability in rats compared with the oral solution of valsartan presented in the higher AUC (0–∞). The AUC (0–∞) with oral treatment was 7.0 ± 2.94 (μg.h/mL), but the AUC (0–∞) with topical application of the VAL nanoethosomal gel was 137.2 ± 49.88 (μg.h/mL), providing the sustained release pattern of VLT from the tested ethosomal gel
Effect of Antiadherents on the Physical and Drug Release Properties of Acrylic Polymeric Films
No full textAntiadherents are used to decrease tackiness of a polymer coating during both processing and subsequent storage. Despite being a common excipient in coating formulae, antiadherents may affect mechanical properties of the coating film as well as drug release from film-coated tablets, but how could addition of antiadherents affect these properties and to what extent and is there a relation between the physical characteristics of the tablet coat and the drug release mechanisms? The aim of this study was to evaluate physical characteristics of films containing different amounts of the antiadherents talc, glyceryl monostearate, and PlasACRYL(TM) T20. Eudragit RL30D and Eudragit RS30D as sustained release polymers and Eudragit FS30D as a delayed release material were used. Polymer films were characterized by tensile testing, differential scanning calorimetry (DSC), microscopic examination, and water content as calculated from loss on drying. The effect of antiadherents on in vitro drug release for the model acetylsalicylic acid tablets coated with Eudragit FS30D was also determined. Increasing talc concentration was found to decrease the ability of the polymer films to resist mechanical stress. In contrast, glyceryl monostearate (GMS) and PlasACRYL produced more elastic films. Talc at concentrations higher than 25% caused negative effects, which make 25% concentration recommended to be used with acrylic polymers. All antiadherents delayed the drug release at all coating levels; hence, different tailoring of drug release may be achieved by adjusting antiadherent concentration with coating level
Enhancing Pharmacokinetics and Pharmacodynamics of Rosuvastatin Calcium through the Development and Optimization of Fast-Dissolving Films
No full textRosuvastatin (RSV) is a widely used cholesterol-lowering medication, but its limited bioavailability due to its susceptibility to stomach pH and extensive first-pass metabolism poses a significant challenge. A fast-dissolving film (FDF) formulation of RSV was developed, characterized, and compared to the conventional marketed tablet to address this issue. The formulation process involved optimizing the thickness, disintegration time, and folding durability. All formulations were assessed for in vitro disintegration, thickness, folding endurance, in vitro dissolution, weight, and content uniformity. The study’s results revealed that the optimized RSV-FDF displayed a significantly faster time to maximum plasma concentration (tmax) of 2 h, compared to 4 h for the marketed tablet. The maximum plasma concentration (Cmax) for the RSV-FDF (1.540 µg/mL ± 0.044) was notably higher than that of the marketed tablet (0.940 µg/mL ± 0.017). Additionally, the pharmacodynamic assessment in male Wistar rats demonstrated that the optimized RSV-FDF exhibited an improved lipid profile, including reduced levels of low-density lipoproteins (LDLs), elevated high-density lipoproteins (HDLs), decreased triglycerides (TGs), and lower very-low-density lipoproteins (VLDLs) compared to the conventional tablet. These findings underscore the potential of RSV-FDFs as a promising alternative to enhance the bioavailability and therapeutic efficacy of rosuvastatin in treating dyslipidemia. The faster onset of action and improved lipid-lowering effects make RSV-FDFs an attractive option for patients requiring efficient cholesterol management
EFFECT OF ADDITIVES ON IN-VITRO RELEASE OF ORODISPERSIBLE DOSAGE FORM
No full textObjective: The aim of this investigation was to prepare orodispersible tablets of meloxicam using various concentrations of superdisintegrants like Ac-DI-Sol, crospovidone, sodium starch glycolate by the direct compression method. Methods: Nine formulae of Meloxicam orodispersible tablets were prepared. These tablets were evaluated for their drug content, weight variation, friability, hardness, wetting time, In-vitro disintegration time and drug release.Results: All the formulation exhibited hardness between 4.21–4.55 kg/cm2. The tablets were disintegrating within 8.3 to 21.9 sec. Dissolution studies revealed that formula containing 7.5 % sodium starch glycolate showed 100% of drug release, at the end of six minutes. Among the formulated tablets, formula F9 containing 7.5 % sodium starch glycolate showed superior organoleptic properties along with excellent In-vitro disintegration time and drug release as compared to other formulae. The concentration of superdisintegrants had an effect on disintegration time and In-vitro drug dissolution whereas hardness and friability of resulting tablets were found to be independent of disintegrant concentration. It was concluded that the superdisintegrants addition technique is a useful method for preparing orodispersible tablets by the direct compression method.Â
Well as its Microcapsules in Rats
No full textABSTRACT Ketorolac is a potent non-steroidal analgesic drug. It is 36 times more potent than phenyl butazone, and twice as that of indomethacin. The oral administration of ketorolac is associated with high risk of adverse effects such as irritation, ulceration, bleeding of gastrointestinal tract, edema as well as peptic ulceration. These attributes make ketorolac a good candidate for controlled release dosage forms, so as to ensure slow release of the drug in the stomach. The present study reports on the formulation of ketorolac loaded Eudragit RS100, Eudragit RL100 as well as Ethyl cellulose as a controlled release drug delivery system. Solid dispersion and microencapsulation by air suspension method were the techniques of choice in order to coat the drug so as to improve bioavailability and stability and also target a drug at specific sites. The ratio of (1:3) drug to polymer from all polymers used was selected from solid dispersions systems as well as microcapsules to conduct further in vivo evaluation, since it was the best ratio which achieved significant reduction in the release of ketorolac at acidic pH of the stomach and maximal release at alkaline pH of the intestine. The effects of various formulations on ulcer index as well as ulcer incidence were studied. The obtained results indicate that microencapsulation technique was able to protect the stomach from ulcerogenic effect ketorolac compared to solid dispersion technique
