Matrix tablets

The present study focuses on the development and evaluation of sustained release matrix tablets of Repaglinide, a short-acting antidiabetic drug, using processed Aloe vera mucilage as a natural release-modifying agent. The primary objective was to extend the drug release profile, reduce dosing frequency, and improve patient compliance. Aloe vera mucilage was extracted, processed, and characterized for its physicochemical properties, including swelling index, viscosity, and compatibility with the drug through FTIR and DSC studies. Matrix tablets were formulated using the wet granulation method with varying concentrations of Aloe vera mucilage and evaluated for pre-compression and post-compression parameters such as hardness, friability, weight variation, drug content, and in vitro drug release. The release data were analyzed using various kinetic models to determine the mechanism of drug release. Among the formulations, the batch containing a higher concentration of Aloe vera mucilage demonstrated a sustained release of Repaglinide over 12 hours, following a non-Fickian diffusion mechanism. Comparative analysis with synthetic polymers revealed that Aloe vera mucilage exhibited comparable or superior release-controlling potential, supporting its use as an effective natural excipient. The study concludes that processed Aloe vera mucilage can be successfully employed as a cost-effective, biocompatible, and efficient release modifier in the formulation of sustained release matrix tablets of Repaglinide.

The objective of this research work was to carry out design and evaluation of sustained release matrix tablets of Itopride by use of natural and synthetic polymers.  Matrix tablets were prepared by wet granulation technique by using natural polymers like Carbopol 934, Tamarind poly saccharide, Locust bean gum, Ethyl cellulose, HPMC K 100 as matrix forming agent and excipients such as Lactose, Starch 1500, Magnesium stearate, MCC and talc were used. The dissolution medium consisted of 900 ml of 0.1 N HCl for first 2 hours and then 7.4 phosphate buffer for remaining 10 hours. The release of Itopride from matrix containing lactose, micro crystalline cellulose and starch 1500 as diluents. The drug release rate was found in order of lactose> micro crystalline cellulose>starch 1500. The formulation was optimized on the basis of acceptable tablet properties and in-vitro drug release. The release data were fit into different kinetic models (zero-order, first-order, Higuchi’s equation and Korsmeyer-Peppas equation). Optimized formulation was tested for their compatibility with Itopride by FT-IR studies, which revealed that there is no chemical interaction occurred with polymer and other excipients. The drug release profile of the best formulation was well controlled and uniform throughout the dissolution studies.

The aim of present work was to design and evaluate sustained release matrix tablets of antihyperlipidemic drug. In the present investigation, polymers used in different combinations such as Eudragit RL100 and HPMC E5 in the ratio of 1:1, 1:2, 1:3 and vice versa with PVP K25 using direct compression technique were prepared. The tablets were evaluated for physical parameters like thickness, hardness, friability, weight variation, and in vitro release studies. The FTIR study indicated that the drug is stable in formulation. The maximum drug release was found to be 94.41% over a period for 12 hours for F4 batch, thus concluded that as the concentration of Eudragit RL100 is increased the drug release decreased. The drug release mechanism followed non-fickian transport from both polymer matrices. All the formulations were stored at 250C/60% RH and 450C/75% RH for 3 months. It showed that all the formulations were physically and chemically stable.

The idea of formulation of controlled release drug delivery has become beneficial in the treatment of diseases. At this time, the increased understanding in the community and the significance of safe use of drugs encouraged to develop novel drug delivery system. In the present study, an attempt was made to expand the release of Cefpodoxime proxetil from matrix tablets by sintering technique. This has been an evolving one in the study of effect of heating on mechanical properties of pharmaceutical powders that is used in the formulation of sustained release matrix tablet. The tablets were formulated by direct compression method. The punched tablets were subjected to sintering process and exposed to three different durations of sintering (1.5, 3.0 and 4.5 hours). This type of system provides a important and suitable method for achieving controlled release in oral dosage forms. The release of the drug form un-sintered matrix tablets containing 100 mg polymer was 100% within 90 minutes. For a particular sintering time, the release rate decreased with increasing polymer concentration. For 1.5, 3.0, and 4.5 hours sintering durations the least retardation is offered by least polymer concentration. The highest retardation was offered by matrices with highest polymer concentration.

Tablets of Oxaliplatin combined with Curcumin was prepared for colon specific delivery using guar gum as matrix carriers in varying concentrations from 40% to 65%. The drug concentration in the tablet was estimated by the newly developed and validated UV derivative spectroscopy method. In vitro drug release profile was studied in changing media method (0.1N HCl, phosphate buffer media, pH 7.4 and simulated colon fluid containing phosphate buffer pH 6.8 added with rat ceacal content). The drug release profiles from PB7.4 and simulated colon fluid were found to be dependent on the gaur gum concentration. Matrix tablets of Oxaliplatin and Curcumin combination showed ~65% of Oxaliplatin and 37% of curcumin release. The colon tissue homogenate studies conducted after oral administration of the optimized tablets showed the recovery of 167.5µg Oxaliplatin and 80µg. curcumin. X-ray Images of matrix tablets containing barium sulphate in Rabbit showed tablets to be intact in small intestine (3 hours after administration) but were diffused and spread out in large intestine and colon later confirming enzyme mediated erosion of the tablet in these regions. Keywords- Oxaliplatin, Curcumin, Matrix tablets, Guar gum, Colon specific delivery, Controlled release.

Colon specific tablets of Oxaliplatin combined with anti-inflammatory agents, Diclofenac sodium were prepared using guar gum as matrix carriers in varying concentrations from 40% to 65%. The drug combination in the tablet was estimate simultaneously using newly developed and validated UV derivative spectroscopy method. In vitro drug release profile was studied in changing media method, first in 0.1N HCl for two hours followed by 3 hours in phosphate buffer media, pH 7.4 (PB7.4) and in simulated colon fluid (phosphate buffer pH 6.8 added with rat ceacal content) (SCF) for 19 hours. The drug release profiles from PB7.4 and simulated colon fluid were found to be dependent on the gaur gum concentration. Matrix tablets of oxaliplatin and diclofenac sodium combination with 60% w/w Gaur gum showed a total release of ~66% of Oxaliplatin and ~53% of Diclofenac sodium after 24 hrs. The colon tissue homogenate studies conducted after oral administration of the optimized matrix tablet in New Zealand Rabbits showed 156 µg oxaliplatin and 96 µg Diclofenac sodium recovery in 24 hours.  X-ray Images of matrix tablets containing barium sulphate in Rabbit showed tablets to be intact in small intestine (6 hours after administration) but were diffused and spread out in large intestine and colon confirming enzyme mediated erosion of the tablet in these regions. 

Mosapride citrate a potent anti-histaminic drug, drug which has short half life, makes the development of sustained release (SR) forms extremely advantageous. Therefore, the present investigation of this study was to develop Mosapride citrate SR matrix tablets that provide complete drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain therapeutic effect. Mosapride citrate  showed maximum absorption at wavelength 274 nm in Acetate buffer pH 4.0, Drug-polymer compatibility studies by FTIR gave confirmation about their purity and showed no interaction between drug and selected polymers. Various formulations were developed by using release rate controlling and gel forming polymers like HPMC (K4M, K100M) by direct compression method. From among all the developed formulations, F6 formulation sustained the drug release for longer period of time as compared to other formulations. So, F6 was selected as the best formulation. It was concluded that the release followed zero order kinetics, as the correlation coefficient (R2 value) was higher for zero order release, so the drug release mechanism is controlled release. The best formulation was found to be stable during stability studies for two months. Thus, best formulation satisfied physicochemical parameters and in vitro drug release profile requirements for a sustained drug delivery.

The concept of controlled release tablet can be utilized to provide a long lasting and more reliable release of drug in GIT to ultimately develop a once daily formulation. Thus, they prolong the dosing intervals, but also increase patient compliance beyond the level of existing conventional dosage forms. Erythromycin, macrolide antibiotics is used in the treatment of Mycoplasma pneumoniae infections, Chlamydial infections, etc. It is a drug with short biological half-life 1.5 hrs and dosing frequency more than one per day which makes it an ideal candidate for controlled release. The present investigation was planned to formulate the Erythromycin stearate once daily controlled release tablets. The tablets were prepared by direct compression method and were subjected for in vitro drug release studies. The mechanism of drug release was determined using various kinetic models. The results revealed that all the formulated tablets had acceptable physical properties and showed release up to 24 hrs. The kinetic studies revealed that all the formulations followed Zero order release kinetics. The tablets were prepared by Direct Compression technique and evaluated for various parameters. The optimized formulation contains Erythromycin Stearate as active ingredient, HPMC K15M, Chitosan and Xanthan gum as rate retarding polymers.

  Matrix tablets of Indomethacin were prepared by wet granulation method. Guar gum as a carrier, 10% starch paste, HPMC, citric acid and the mixture of talc and magnesium stearate at 2:1 ratio were used. Coating was carried out by using 10% Eudragit L 100. All the prepared formulations were evaluated for hardness, drug content uniformity, stability study and were subjected to in vitro drug release studies in rat caecal contents. The highest in vitro dissolution profile at the end of 24 h was shown by IF6 followed by IF7, IF8. The other formulation IF4, IF3, IF2 and IF1 were failed to target in colon and these formulation releases the majority of drug within 10 h of study. It may be due to the less proportion of guar gum to retard the drug release.  The colon targeted matrix tablet of Indomethacin showed no change either in physical appearance, drug content or in dissolution pattern after storage at 30˚ C/ 65±5 % RH for 2 months.   Key words: Colon targeted, Eudragit L-100, Guar gum, Indomethacin, Matrix tablets, Rat caecal content.

  The aim of the present study was to prepare and characterize twice-daily sustained-release matrix tablets of Timolol maleate (TM) using different concentrations of hydrophilic Hydroxypropylmethylcellulose (HPMC K100M CR) alone and its combination with hydrophobic ethyl cellulose (EC). Formulations prepared by the wet granulation technique and were evaluated for the release of TM over a period of 12 hours using United States Pharmacopoeia (USP) type-II dissolution apparatus. Along with physical properties, the dynamics of water uptake and erosion degree of tablets were also studied. The in-vitro drug release study revealed that formulation F3 (40% wt/wt HPMC K100M) could extend the drug release up to 8 hours. The most successful formulation of the study, F5 (HPMC to EC, 1:1), extended the drug release up to 12 hours, exhibited satisfactory drug release in the initial hours, and the total release pattern was close to the theoretical release profile. The drug release from optimized formulation (F5) followed first-order kinetics via Non-Fickian (anomalous) diffusion. FTIR studies revealed that there was no interaction between the drug and excipients. In conclusion, the results indicated that the prepared sustained-release tablets of TM could perform therapeutically better than conventional tablets with improved efficacy and better patient compliance.   Key words: Timolol maleate; Matrix tablets; Sustained-release; Ethyl cellulose; Hydroxypropylmethylcellulose; In-vitro drug release.