Formulation of pyridoxine hydrochloride sustained release capsules: Effect of propylene glycol co-solvent on the in vitro release (original) (raw)
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In vivo evaluation of rapid release and sustained release Gelucire capsule formulations
1990
was dispersed in a water miscible, highly ethoxylated wax and filled into hard gelatin capsules. This produced drug absorption equivalent in rate and extent to conventional rapid release formulations. Where gastric spreading/dispersion was slow, gastric emptying was delayed and the rate of drug absorption reduced. The use of a slowly hydrating, erodible wax formulation was shown to produce sustained release in vivo, prolonging drug levels relative to conventional formulations. Good in vitro-in vivo correlation was not observed and a relative bioavailability lower than expected was determined. However, comparing the semi-solid ketoprofen capsule (100 mg) plasma data with the comparable product (Oruvail 200 mg) by normalizing for a 200 mg dose, it is apparent that the two formulations are likely to yield similar terminal plasma concentrations. Controlled drug release was not achieved and drug absorption was dependent upon physiological variables such as gastric emptying and intestinal transit as assessed by gamma scintigraphy.
Ankara Universitesi Eczacilik Fakultesi Dergisi, 2009
The purpose of this study was to evaluate the flow properties and compressibilities of different direct tableting agents (DTA) by using pyridoxine hydrochloride as a model drug. Avicel PH 102 ® , Tablettose 100 ® , StarLac ® and Ludipress ® were used as DTAs. Flow rate, angle of repose, bulk and tapped densities of DTAs, binary mixture of drug and DTA and mixtures of drug-DTA-magnesium stearate were examined. Carr's index and Hausner index were calculated to determine the consolidation character of powder mixtures. Tablets were compressed at different pressure by a manual hydraulic press. Heckel and Kawakita equations were fitted to the data obtained from compressibility studies. StarLac ® and Ludipress ® showed good flow properties as indicated by the lowest angle of repose and the highest flow rate. The Hausner and Carr's index values of these agents were in the range of good flow characteristic values according to the pharmacopoeial limits. The lowest Py values of powder mixture prepared with StarLac ® or Ludipress ® were also pointed out of acceptable compressibility. When Tablettose ® was used in the formulation, capping and lamination problems were occurred at the higher compression pressure. The effect of the increased percent amount of drug (12% to 36%) on the consolidation properties and compressibility was also determined at the Müge KILIÇARSLAN, Rüya ÇAMCA, Selin ĐMAMOĞLU, Mustafa Naim ANTEP, Başak OCAK, Nilüfer YÜKSEL 332 formulations prepared with Ludipress ®. Optimum consolidation and compressibility characters were obtained by 18% drug while more than 24% drug amount was caused to decreased volume reduction.
International Journal of Pharmaceutics, 2000
The aim of the present study was to investigate the effect of hydroxypropylmethylcellulose (HPMC-2208), used as an excipient for controlled release of drug, on the release profiles and bioavailability of the poorly water-soluble nifedipine (NP) from a tablet prepared using macrogol 6000 (PEG) and HPMC. The crushing tolerance of the NP tablet prepared using PEG and HPMC (NP-PEG-HPMC tablet) was markedly increased with increasing compression force used during the preparation from 20 to 200 MPa. The values reached their maximal levels (approximately 13 kg for the NP-PEG-HPMC tablet and 8 kg for the PEG tablet) at the compression force of 100 MPa. Although NP is a poorly water-soluble drug, it was rapidly dissolved from the NP-PEG tablet (without HPMC) due to the improvement of its dissolution rate in the presence of PEG. NP dissolution was complete at the latest within 1 h. On the other hand, dissolution of NP from the NP-PEG-HPMC tablet was significantly delayed with an increase in the concentration of HPMC in the tablet. The dissolution of NP from the NP-PEG-HPMC tablet containing 50% HPMC-2208 was markedly delayed as the viscosity of HPMC also increased. Interestingly, the same peak plasma NP concentration (C max) and the area under the plasma NP concentration-time curve (AUC 0-10) were observed for both the NP-PEG tablet and NP-PEG-HPMC tablets, however, the time to C max (t max) for the NP-PEG-HPMC tablet was significantly higher when the NP-PEG-HPMC tablet was orally administered to rabbits. We describe here a preparation method of a new sustained-release NP-PEG-HPMC tablet using a mixture of NP-PEG granules (prepared with PEG) and HPMC.
A Review on Formulation Approaches in Immediate Release Tablet
Journal of Drug Delivery and Therapeutics
Sometimes immediate onset of action is required than conventional treatment in many patients. Among all dosage forms tablet is the most popular dosage form existing today because of its convenience of self-administration, compactness and easy manufacturing. to overcome these drawbacks, immediate release dosage form has emerged as alternative oral dosage forms. Immediate drug release dosage forms disintegrate quickly after administration with enhanced rate of dissolution. The basic approach used in development tablets is the use of superdisintegrants like Cross linked Polyvinylpyrrolidone or crospovidone (Polyplasdone), Sodium starch glycolate (Primogel, Explotab), carboxymethylcellulose (Croscarmellose) etc. In this field immediate release liquid dosage forms and parenteral dosage form have also been introduced for treating patients. The development of immediate release therapy also provides an opportunity for a line extension in the marketplace, a wide range of drugs e.g., anticoagulant and other drugs can be considered candidates for this dosage form. The development of immediate release therapy also provides an opportunity for a line extension in the marketplace, a wide range of drugs e.g., anticoagulant and other drugs can be considered candidates for this dosage form.
To Evaluate and Study the Swelling and Drug Release Behavior of Poly (N-Vinyl-2-Pyrrolidone) Gel
The drug loading and drug release efficiency of the P (N-vinyl-2-pyrrolidone) hydrogel was evaluated using the ketotifen as model drugs. The hydrogel was cut into small discs (3 mm thickness and diameter) and immersed in the solutions of the ketotifen for three days to achieve the maximum (equilibrium) swelling. The hydrogel immersed in 0.1 N HCl and phosphate buffers (pH 6.8) showed the 31.828 % and 29.783 % loading of the ketotifen by weight of the dried hydrogel, respectively that was not significantly difference (p was greater than 0.05). However, the slow swelling behavior of the hydrogel in the acidic medium was observed in the absence of the drug. The method of analysis of ketotifen using U.V-visible spectrophotometer and HPLC was developed for the analysis of these components in the dissolution medium. The methods were linear (r = 0.9967) over the range of 0.1 to 10 µg.ml for ketotifen using U.V Visible spectrophotometer and 2 1 HPLC respectively. The precision, accuracy and reproducibility of the methods were in an agreeable range to analyze the samples obtained from the dissolution medium. The various parameters for the methods of analysis of the ketotifen using spectrophotometer and HPLC methods were validated. The linearity of the method using UV Visible spectrophotometer and HPLC were (r = 0.9967). The release of ketotifen from the P (N-vinyl-2-2 pyrrolidone) hydrogel under acidic condition was only 10 % of the drug released in about 72 hours and followed Higuchi model and drugs were released through Fickian diffusion. The data was best fitted in the Higuchi model (R = 0.9566) indicating the drug release followed Fickian diffusion. The application of the 2 Korsmeyer's equation showed that the release of ketotifen release from the hydrogel disc followed the Fickian diffusion. Under basic conditions (pH 6.8), it was observed that the in-vitro release of ketotifen from hydrogel disc GS2 best fitted to the Hixon-Crowell (0.9917) indicating the erosion and dissolution of hydrogel. As the value of (n) for the GS2 was 1.2634, it indicating that the release of ketotifen from hydrogel disc followed non-Fickian super case II release. Under mixed conditions (for the first two hours in acidic condition (pH 0.1N HCl) and then for the rest of time at (pH 6.8), it was found that the in-vitro release of ketotifen from hydrogel loaded disc GS3 best fitted to the Higuchi model (0.9821) indicating the drug release followed Fickian diffusion. The value (0.9216) of release exponent "n" obtained with Korsmeyer's-Pappas equation suggested that drug release from GS3 formulation followed anomalous transport.
Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel
Brazilian Journal of Pharmaceutical Sciences, 2013
A hydrogel was developed from 70 kDa dextran (DEX-70) and praziquantel (PZQ) incorporated as a model drug. Biopharmaceutical properties, such as solubility and dissolution rate, were analysed in the design of the hydrogel. Furthermore, the hydrogel was also characterized by IR spectroscopy and DSC. Tests of the swelling rate showed that the hydrogel swelled slowly, albeit faster than the rate for the free polymer. In dissolution tests, the hydrogel released the drug slowly and continuously. This slow release was similar to that observed in the swelling tests and resulted in controlled release of the drug. Thus, this dextran is a suitable polymer for the development of hydrogels as vehicles for the controlled release of drugs.
The objective of the present investigation was to develop a sustained release (SR) tablet formulation of glipizide by employing two hydrophobic polymers (ethyl cellulose and ethylene vinyl acetate copolymer) and two natural hydrophilic gum resins olibanum resin and colophony). Different batches of glipizide sustained release tablets were prepared by using lactose and dicalcium phosphate as diluents by wet granulation technique. The prepared tablets were evaluated for various parameters. In vitro drug release study was carried out and compared with the commercial Glynase XL tablets. The independent model method, Lin Ju and Liaw's difference factor (ƒ1) and similarity factor (ƒ2) were used to compare various dissolution profiles. The dissolution profiles of an ideal formulation (SR F3) containing olibanum resin and lactose as diluent was found to be comparable with the reference product. The kinetics of drug release was best explained by Korsmeyer and peppas model and the mechanism of drug release from these tablets was by non-fickian diffusion mechanism. The ideal formulation (SR F3) was stable when it was stored at 4±2°C, 27±2°C and 45±2°C for 6 months. In conclusion, SR formulation of Glipizide could be developed employing olibanum resin as rate-controlling matrix former and lactose as diluent.
AAPS PharmSciTech, 2012
Different hydroxypropyl methylcellulose (HPMC)/anhydrous dibasic calcium phosphate (ADCP) matrix tablets have been developed aiming to evaluate the influence of both components ratio in the control release of a water-soluble drug (theophylline). In order to characterise the matrix tablets, swelling, buoyancy and dissolution studies have been carried out in different aqueous media (demineralised water, progressive pH medium, simulated gastric fluid, simulated intestinal fluid and simulated colonic fluid). The HPMC/ADCP ratio has turned out to be the determinant in the matrix behaviour: the HPMC characteristic swelling behaviour was modulated, in some cases, by the ADCP characteristic acidic dissolution. When the HPMC/ADCP ratio was ≥0.69, buoyancy, continuous swelling and low theophylline dissolution rate from the matrices (H1, H2 and H3) were observed in all dissolution media. Consequently, these formulations could be adequate as gastro-retentive drug delivery systems. Additionally, HPMC/ADCP ratio ≤0.11 (H5 and H6) induces a pH-dependent drug release which could be applied to design control drug release enteric formulations (with a suitable enteric coating). Finally, a HPMC/ ADCP ratio between 0.11 and 0.69 (H4) yield a gastrointestinal controlled drug release, due to its timedependent buoyancy (7 h) and a total drug delivery in 17 h in simulated colonic fluid.
Preparation and in vitro & in vivo evaluation of cephalexin matrix tablets
BJPS, 2018
The purpose of the study is to develop cephalexin controlled-release matrix tablets by using lower proportions of release retardant polymer and to establish their in vitro & in vivo correlation. Tablets were compressed by incorporating polymers in a matrix form along with drug which prolong the drug release. Twelve formulations were prepared by mixing ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC) (three different viscosity grades) in various proportions. F-1 to F-4 formulations were prepared by incorporating drug, HPMC K4M and ethyl cellulose in 100 : 5 : 5, 100 : 10 : 5, 100 : 15 : 5 and 100 : 20 : 5; similarly, F-5 to F-8 were prepared with HPMC K15M; and F-9 to F-12 were prepared with HPMC K100M using a wet granulation process maintained same proportions, along with drug and EC. Tablets were evaluated for their pre-compression and post-compression characteristics and they were found to be in limits. From the dissolution testing, F-4 showed 100.34% medicament release in 12 h. In vivo studies were conducted on rabbit and pharmacokinetic parameters of the optimized formulation were evaluated using HPLC method. It was found that matrix tablets showed increased t 1/2 and decreased K el. The design signified that the drug release rate from tablets was influenced by the small proportion (around 7% of a tablet weight) of polymer mixture and it controlled 100% medicament release upto 12 h effectively with the low grade viscosity of HPMC combination, with good in vitro & in vivo correlation.