Current Issue : October - December Volume : 2013 Issue Number : 4 Articles : 7 Articles
Purpose of the research was to present Budesonide (BUD), a glucocorticoid, as a novel formulation showing improved aqueous solubility, which may decrease patient to patient absorption variability, and target the drug to colon for the treatment of inflammatory bowel disease. To improve aqueous solubility, solid dispersion (SD) of the BUD with poloxamer 188 was prepared by melting method. Physical characterization of solid dispersion was performed. The tablets containing SD equivalent to 9mg of BUD were prepared by wet granulation. The tablets were coated with pH dependent polymers Eudragit (EUD) S100 & Eudragit (EUD) L100 to achieve colon targeting. The ratio of EUD S100 and EUD L100 and the % weight gain was optimized using factorial design. Factors studied in design were ratio of EUD S100 in combination with EUD L100 and the effect of coating level on in-vitro drug release at 7 & 10 hours. Dissolution studies of coated tablets in with different pH media (1.2, 4.6, 6.8 and 7.4) showed that drug release in colon could be modulated by optimizing the ratio of EUD S100 & EUD L100 (12.15:2.57) and (3.52:11.47) with % weight gain of 6.05% & 9.5% respectively. The study showed that, lag time prior to drug release was highly affected by the coating level. The dissolution data showed that the level of coating and the ratio of polymers are very important to get optimum formulation. Stability study of the optimized formulation indicates no significant change in release after a period of one month....
The aim of the present investigation is to formulate mouth dissolving tablets of Ketotifen Fumarate. Mouth dissolving tablets of Ketotifen Fumarate were prepared by two different techniques, Super disintegrant addition method and Effervescent formulation approach. Twelve formulations were prepared by Super disintegrant addition method using Sodium starch glycolate, Crospovidone, and Croscarmellose sodium as super disintegrants in combinations and at different concentrations. Another three batches were prepared by Effervescent formulation approach using Sodium bicarbonate and Citric acid (anhydrous) as effervescent agents. The prepared batches were evaluated for organoleptic properties, hardness, friability, weight variation, in vitro disintegration time, wetting time, in vitro drug release studies, and stability studies. Formulation prepared by Super disintegrant addition method using Sodium starch glycolate and Crospovidone in 3% and 5% w/w respectively, showed minimum time to disintegrate (18 sec.) and almost complete release of drug within 5 minutes. Finally it was concluded that MDT of Ketotifen Fumarate can be successfully formulated by both methods with improved patient compliance....
The present work was to design and evaluation of mouth dissolving tablets of Loratadine by using with different concentration of different super disintegrants. The Drug and excipient were characterized using differential scanning calorimetry (DSC) and automated total reflectance spectrometer (ATR). The drug excipient blend was evaluated for examined physiochemical properties. The prepared tablets were evaluated for thickness, hardness, friability, wetting time, water absorption ratio, content uniformility, in-vitro disintegration time and in-vitro dissolution studies. Formulation (F-1) show quick disintegration time of 15.26 s, which is very charterstics of mouth dissolving tablet and formulation (F-1) were subjected to accelerated stability studies for 3 months at temperature 40±5°C/75±5% RH. The tested did not show any change with respect to taste, disintegration and dissolution profile. Additionally inclusion of stevia (stevia rebidiana) leaves powder still makes the formulation 400 times sweeter then sucrose and diabetic friendly....
The aim of the current study was the development of Nicorandil mucoadhesive matrix tablets using direct compression. Mucoadhesive formulations were developed using various blends of mucoadhesive polymers. A 32 randomized factorial design was adopted to control both the adhesion properties and the release rate of the drug from the delivery system. In this study 2 factors were evaluated, each at 3 levels. The amount of HPMC K100M: Sod Alginate (X1) and Carbopol 974P (X2) were selected as independent variables and the mucoadhesive strength (f), times required for 50% of drug release (t50%), amount of drug release at 12 h (Rel 12 h) and release exponent (n) were selected as dependent variables. Prepared tablets were evaluated for their Physico-chemical parameter, swelling index, ex-vivo bioadhesion, in-vitro drug release and in-vivo γ- scintigraphy experiments in humans. Data obtained in these studies demonstrated that optimized formulation MF3, containing (3:1 ratio of HPMC K100M: Sodium Alginate, 100mg and Carbopol 974P, 45mg,) showed Mucoadhesion force (f) as 146.61 dynes/cm2, time to release 50% of drug (t50%) as 4.8 h, release of drug at 12h (Rel 12 h) as 99.93% and release exponent (n) as 0.709 confirming non-Fickian diffusion. In-vivo γ- scintigraphy studies revealed that mucoadhesive matrix tablet was retained in the human stomach for more than 6h....
The aim of present investigation is to formulate the mouth dispersible film of Desloratadine by solvent casting technique. The Desloratadine is class of antihistaminic drug which does not cross blood brain barriers like other first generation antihistaminic. Drug shows hepatic first pass metabolism hence there is need to develop fast dispersible film. The film prepared by solvent casting technique and evaluated for their mechanical properties. The thickness of film lies between 0.05 to 0.07mm. The weight of all factorial batches observed between 31.15 to 35.60 mg with standard deviation less than 0.2%. The folding endurance of all batches observed between 90.33to135 .For the batches F4, F7, F9 the folding endurance observed 124,131.33,135 respectively. The in vitro disintegration time for all batches measured between 9.6 to 15.3 seconds. The percent drug content observed between 97.85 to 99.16 %. In case of F4 and F6 formulations about 99.25% and 97.38% of drug was released at 2min which shows faster drug release....
Gels and microemulsions are classes of dosage forms that have emerged as promising drug delivery system for the delivery of various drugs. The objective of this study is to prepare tenoxicam, a non-steroidal anti-inflammatory drug (NSAID), topical gel formulae using cellulose derivatives (Sodium carboxymethyl cellulose (NaCMC), Methyl cellulose (MC), Hydroxypropyl methyl cellulose (HPMC), Hydroxy ethyl cellulose (HEC), and Hydroxy propyl cellulose (HPC)) as gelling agents and to prepare topical microemulsions, microemulsion-gel formulae using (labrasol, tween 80 and tween 20) mainly as surfactants, (Oleic acid and isopropylmyristate (IPM)) as oils. Fifteen gel formulae were prepared (F1-F15) and evaluated for physical properties (color, clarity, homogeneity), rheological properties, pH measurements, in vitro drug permeation through cellulose dialysis membranes and in vitro drug permeation studies through natural rat skin. The gel formulae which showed best physical properties and highest drug permeation were chosen in the preparation of microemulsion-gel formulae. Ten microemulsion formulae were prepared (M1-M10) and those with the broadest microemulsion region as shown by the phase diagrams and those with the maximum loading capacity of tenoxicam were chosen to be formulated into microemulsion-gel formulae. Nine microemulsion-gel formulae were prepared (S1-S9) and evaluated for physical properties (color, clarity, homogeneity), rheological properties, pH measurements, in vitro drug permeation through cellulose dialysis membranes and in vitro permeation studies through natural rat skin. In vivo rat-paw edema tests were carried out to evaluate the activity of gel formulae and microemulsion-gel formulae which showed maximum tenoxicam permeation through rat-skin, and compared them with market product Feldene® gel (Piroxicam 0.5%) The obtained results showed that S3 microemulsion-gel formula possesses the maximum drug permeation as well as anti-inflammatory activity which proved to be even greater than Feldene® gel. Therefore, S3 is effectively promising as topical anti-inflammatory dosage forms, due to the permeation enhancement caused by using microemulsions together with the gel base....
Lower bioavailability is one of the main culprit for new drug entity when formulation is to be decided. Self-emulsifying drug delivery systems (SEDDS) are the type of formulations where drug itself is given in presolubilized form which improves the bioavailability by virtue of improvement in dissolution. As it is lipid based system it also improves the permeability. Certain disadvantages associated with conventional SEDDSs are now overcome by some of the recent advancement are described in this manuscript with recent patents in such fields....
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