M.U. Mishra33 et al., undertaken to assess the potential of Tamarind seed polysaccharide to act as a biodegradable carrier for colon specific drug delivery. The matrix tablets were prepared by wet granulation technique containing different concentrations (30% w/w to 70% w/w) of TSP using Ibuprofen as a model drug. The results of in vitro drug release study indicate that the matrix tablets prepared by using TSP are able to carry most of the drug to the colon and restrict the release in upper GIT.
Rishabha Malviya34 et al (2010) was made to formulate sustained release matrix tablets of Diclofenac sodium using gum acacia and tamarind gum as release modifier. Six batches of sustained release matrix tablets of Diclofenac sodium were prepared by using different drug: polymer ratios viz. 1:1, 1:1.5, 1:2, 1:2.5,1:3, and 1:3.5 for both gum acacia and tamarind gum. Results showed that the drug release from matrix tablets prepared by using natural polymers can be sustained for more than 12 hrs and the drug release vary with concentration of polymer in matrix tablets.
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Srivastava Pranati35 et al (2010) made to increase therapeutic effectiveness, reduce dose frequency and so improvement in patient compliance, by developing sustained release matrix tablets using tamarind gum and pectin as release modifier. Six batches of sustained release matrix tablets of Diclofenac sodium were prepared by using different drug: polymer ratios viz. 1:1, 1:1.5, 1:2, 1:2.5, 1:3, 1:3.5 for tamarind gum and pectin. A better sustained release was obtained with the matrix tablet of tamarind gum. It is cleared that the drug release from matrix tablets prepared by using tamarind gum can be sustained for more than 12 hrs and release of drug vary with concentration of polymers in matrix tablets.
Pratik Shah36 et al (2010) research was developed and evaluate a matrix system for Chronotherapeutic delivery of NSAID (Non-steroidal anti-inflammatory drug) containing Natural polysaccharide in Rheumatoid Arthritis. The natural polysaccharides, Guar gum, were used as a carrier for drug delivery along with three different polymeric binders to optimize the proper formulation for Chronotherapeutic drug delivery. Different bathes of matrix tablet Of Diclofenac Sodium- Guar gum were prepared using wet granulation method . The release profile of Diclofenac Sodium from the matrix tablets is dependent upon the gelling property of Guar gum and degradation of Guar gum by colonic bacteria. It is concluded from the present investigation that Guar gum containing matrix tablets are promising controlled release systems for colon-targeted delivery of Diclofenac sodium.
V.V. Kale37 et al (2010) investigated the significance of factors such as drug solubility, proportion of polymers and other additive on drug release from guar gum based matrix system. Pseudoephedrine HCl, Metformin, Tetracycline and Diclofenac sodium with solubilities > 50%<_%<_10%,0.1% respectively were used as drug models. As the guar gum content was increased, drug release rate was decreased. When the guar gum and drug proportion was constant, change in the rate of drug release was observed with the change in the drug solubility.
Rishabha Malviya38 et al (2010) attempt was made to increase therapeutic effectiveness, reduction in dosing frequency and thus improving patient compliance, by developing sustained release matrix tablets of Diclofenac sodium using guar gum as release modifier. Six batches of sustained release matrix tablets of Diclofenac sodium was prepared by using different drug : polymer ratios viz. 1:1, 1:1.5, 1:2, 1:2.5, 1:3, 1:3.5 for guar gum. Result show that as the concentration of gum increases, swelling index also increased proportionally. It is clear through the dissolution studies that the release profile of Diclofenac sodium from matrix tablets prepared using guar gum was retarded approximately 24h.
Gurpreet Kaur39 et al (2010) The present study was designed to formulate colon release tablets of fluticasone by employing cross linked chitosan (CH) and carboxymethyl guar gum (CMG) inter polymer complexes (IPC). Matrix tablets were prepared by wet granulation method using IPC as binder and coating agent.The uncoated and coated tablets were tested for their suitability as colon specific drug delivery system by in vitro dissolution studies. The coated tablets were evaluated for their pharmacodynamic performance after oral administration to TNBS induced ulcerative colitis rats. Histopathology of the rat colon after oral administration of these IPC film coated tablets revealed significantly greater (p<0.05) reduction in TNBS-induced ulcerative colitis The study confirmed that selective delivery of fluticasone to the colon can be achieved using cross-linked CH and CMG polysaccharides.
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Hindustan Abdul Ahad40 et al (2010) investigation was to develop matrix tablets of Aceclofenac with Prosophis juliflora gum and to study its functionality as a matrix forming agent for once daily sustained release tablet formulations. Physicochemical properties of dried powdered Prosophis juliflora gum were studied. Various formulations of Aceclofenac Prosophis juliflora gum were prepared.The dissolution study proved that the dried Prosophis juliflora gum can be used as a matrix forming material for making once daily Sustained release matrix tablets.
Santanu Ghosh41 et al (2010) was to develop matrix tablets for oral controlled release of aceclofenac. Matrix tablets of aceclofenac, using various viscosity of hydrophilic polymer HPMC in two different proportions, hydrophobic polymer ethyl cellulose and Guar gum were prepared by wet granulation method and subjected to in vitro drug release studies. The drug release from all HPMC matrix tablets followed various release kinetics, formulation no -F7 followed higuchi kinetics. Furthermore, the results of the in vitro studies in pH 7.5 phosphate buffer medium showed that F7 tablets provided controlled release comparable with market sustained release formulation (Aeroff-SR tablets). F7 tablets showed no change in physical appearance, drug content, or in dissolution pattern after storage at 40Â°C with 75%RH for 6 months. Based on the results of the in vitro studies, it was concluded that the HPMC matrix tablets provided oral controlled release of aceclofenac.
Santanu Ghosh and Barik42 et al (2010) was to develop matrix tablets for oral controlled release of aceclofenac using ethyl cellulose, guar gum, and various grades of cellulose polymers. The release profile of one of the formulated aceclofenac tablets, which contained hydroxypropyl methyl cellulose, was statistically similar to that of the commercial aceclofenac brand in all the dissolution media. The result indicate that it is feasible to achieve a stable once daily sustained release aceclofenac tablet formulation by using HPMC k4M of 4000cps viscosity grade as matrix material.
Suresh V Kulkarni43 et al (2010) investigation an attempt was made to reduce the frequency of dose administration and to improve the patient compliance by developing controlled release (CR) matrix tablet of Stavudine using naturally occurring (Guar gum and Xanthun gums) and Synthetic Polymers( HPMC and Ethyl cellulose). Six batches of CR matrix tablets of Stavudine were developed by using wet granulation technique. Tablets were evaluated for weight variation, hardness, friability and In vitro dissolution studies. All formulation showed compliance with pharmacopoeial standards. Among the six formulations, F3 showed controlled release of drug for 12 hours with 91.65% drug release. The release data was fitted to various mathematical models such as, Higuchi, Korsmeyer-Peppas, First-order, and Zero-order to evaluate the kinetics and mechanism of the drug release was found to be diffusion coupled witherosion.
Amit K Nagariya44 et al (2010) made in the research and development of rate-controlled oral drug delivery systems by overcoming physiological adversities, such as short gastric residence times (GRT) and unpredictable gastric emptying times (GET). Several approaches a recurrently utilized in the prolongation of the GRT, including floating drug delivery systems (FDDS), Gastro retentive floating drug delivery systems (GFDDS) are the systems which are retained in the stomach for a longer period of time and thereby improve the bioavailability of drugs. Natural polymer shave a number of advantages like Biocompatibility, Natural in origin, biodegradable to normal body constituents, safe and non-toxic. Natural gums are among the most popular hydrophilic polymers because of their cost-effectiveness and regulatory acceptance. In this paper we have tried to give a brief over view to the potential of natural polymer in the development of gastro retentive floating drug delivery system.
Dr.Umesh.D .Shivhare45 et al (2009) was to develop "once daily" sustained release tablets of aceclofenac by wet granulation using carboxypolymethylene polymer. The drug excipient mixtures were subjected to preformulation studies while the tablets were subjected to physicochemical studies, in vitro drug release, stability studies andvalidation studies. The physicochemical properties of tablets were found within the limits. Formulation F2 & F9containing Carbopol 971P and Carbopol 974P were found to release the drug in sustained manner up to 24 hour were stable under accelerated conditions of temperature for 6 months since there were no significant changes in drug content and physical parameters.
Raghavendra Rao N. G46 et al (2009) was to develop sustained release matrix tablets of water soluble Tramadol hydrochloride using different polymers viz. Hydroxy propyl methyl cellulose (HPMC) and natural gums like Karaya gum (KG) and Carrageenan (CG). Varying ratios of drug and polymer like 1:1 and 1:2 were selected for the study. After fixing the ratio of drug and polymer for control the release of drug up to desired time, the release rates were modulated by combination of two different rates controlling material and triple mixture of three different rate controlling material. After evaluation of physical properties of tablet, the in vitro release study was performed in 0.1N HCl pH 1.2 for 2 hrs and in phosphate buffer pH 6.8 up to 12 hrs. The effect of polymer concentration and polymer blend concentration were studied. Different ratios like 80:20, 60:40, 50:50, 40:60 and 20:80 were taken. Dissolution data was analyzed by Korsmeyer- Peppas power law expression and modified power law expression. It was observed that matrix tablets contained polymer blend of HPMC/CG were successfully sustained the release of drug upto 12 hrs. Among all the formulations, formulation F16 which contains 20% HPMC K15M and 80% of CG release the drug which follow Zero order kinetics via, swelling, diffusion and erosion and the release profile of formulation F16 was comparable with the marketed product. Stability studies (40Â±2°C/75Â±5%RH) for 3 months indicated that Tramadol hydrochloride was stable in the matrix tablets. The DSC and FTIR study revealed that there was no chemical interaction between drug and excipients.
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Bhavin Patel47 et al (2009) were fabricated the buccal mucoadhesive tablets of nifedipine with objective of avoiding first pass metabolism and prolonging duration of action. The mucoadhesive polymers used in formulations were carbopol (cp934),hydroxyl propyl methyl cellulose (HPMC K4M), carboxy methyl cellulose (CMC), and tamarind seed polysaccharide (TSP).These formulations were characterized for physiochemical parameters, in vitro retention time, in vitro bioadhesive strength ,percent hydration and drug release. The modified in vitro assembly was used to measure the bioadhesive strength of tablets with fresh goat buccal mucosa as a model tissue. The best mucoadhesive performance and in vitro drug release profile were exhibited by the tablet containg carbopol and TSP in the ratio of 1:1. This formulation was more comfortable to the user due to less erosion, faster hydration rate, and optimum pH of surrounding medium.
UK Patil48 et al (2008) were fabricated using pectin, guar gum and xanthan gum. The tablets were evaluated for physical characteristic like hardness, weight variation, fraibilty, and drug content. In-vitro release of drug was performed in PBS pH 7.2 for fifteen hours. All the physical characters of the fabricated tablet were within acceptable
limits. The tablet with guar gum exhibited greater swelling index than those with pectin and xanthan gum. A better controlled drug release (80.74%) was obtained with the matrix tablet (G4) made-up of the guar gum than with the pectin and xanthan gum. It is cleared through the dissolution profile of furosemide from matrix tablets prepared using different natural polymers were retarded approximately 15 hrs.
Jolly M. Sankalia49 et al (2008) was to examine a level A in vitro-in vivo correlation (IVIVC) for glipizide hydrophilic sustained-release matrices, with an acceptable internal predictability, in the presence of a range of formulation/manufacturing changes. The effect of polymeric blends of ethyl cellulose, microcrystalline cellulose, hydroxy propyl methylcellulose, xanthan gum, guar gum, Starch 1500, and lactose on in vitro release profiles was studied and fitted to various release kinetics models. Water uptake kinetics with scanning electronmicroscopy (SEM)was carried out to support the drug release mechanism. An IVIVC was established by comparing the pharmacokinetic parameters of optimized (M-24) and marketed (Glytop-2.5 SR) formulations after single oral dose studies on white albino rabbits. The matrix M-19 (xanthan: MCC PH301 at 70:40) and M-24 (xanthan :HPMC K4M:Starch1500 at 70:25:15) showed the glipizide release within the predetermined constraints at all time points with Korsmeyer-Peppas' and zero-order release mechanism, respectively. Kopcha model revealed that the xanthan gum is the major excipient responsible for the diffusional release profile and was further supported by SEM and swelling studies. A significant level A IVIVC with acceptable limits of prediction errors (below 15%) enables the prediction of in vivo performance from their in vitro release profile. It was concluded that proper selection of rate controlling polymers with release rate modifier excipients will determine overall release profile, duration and mechanism from directly compressed matrices.
Jaleh Varshosaz50 et al (2006) was to develop matrix sustained release tablets of highly water-soluble tramadol HCl using natural gums (xanthan [X gum] and guar [G gum]) as costeffective,nontoxic, easily available, and suitable hydrophilic matrix systems compared with the extensively investigated hydrophilic matrices (ie, hydroxypropyl methylcellulose[HPMC]/ carboxymethyl cellulose [CMC] with respect to in vitro drug release rate) and hydration rate of the polymers. Matrix tablets of tramadol (dose 100 mg) were produced by direct compression method. Different ratios of 100:0, 80:20,60:40, 20:80, 0:100 of G gum (or X):HPMC, X gum: G gum, and triple mixture of these polymers (G gum, X gum ,HPMC) were applied. After evaluation of physical characteristics of tablets, the dissolution test was performed in the phosphate buffer media (pH 7.4) up to 8 hours. Tablets with only X had the highest mean dissolution time (MDT), the least dissolution efficiency (DE8%), and released the drug following a zero-order model via swelling, diffusion, and erosion mechanisms. Guar gum alone could not efficiently control the drug release, while X and all combinations of natural gums with HPMC could retard tramadol HCl release. However, according to the similarity factor ( f2), pure HPMC and H8G2 were the most similar formulations to Topalgic-LP as the reference standard.
Saleh M51.et al (2005) was to develop guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride. Matrix tablets of diltiazem hydrochloride, using various viscosity grades of guar gum in 2 proportions, were prepared by wet granulation method and subjected to in vitro drug release studies Based on the results of in vitro and in vivo studies it was concluded that that guar gum matrix tablets provided oral controlled release of water-soluble diltiazem hydrochloride.
Tejraj M. Aminabhavi52 et al (2004) was prepared by taking three different ratios of guar gum to acrylamide(1:2, 1:3.5 and 1:5). Amide groups of these grafted copolymers were converted into carboxylic functional groups. Tablets were prepared by incorporating an antihypertensive drug viz., diltiazem hydrochloride. In-vitro drug release was carried out in simulated gastric and intestinal conditions. Effect of drug loading on release kinetics was evaluated. Release continued up to8 and 12 h, respectively, for pAAm-g-GG and hydrolyzed pAAm-g-GG copolymers. Nature of drug transport through the polymer matrices was studied by comparing with Higuchi, Hixson-Crowell and Kopcha equations. Drug release was found to be dissolution-controlled in case of unhydrolyzed copolymer. With hydrolyzed copolymers, drug release was swelling controlled initially (i.e., in 0.1 N HCl), but at later stage, it became dissolution-controlled in pH 7.4. Hydrolyzed pAAm-g-GG matrices are pH sensitive and can be used for intestinal drug delivery.
Y.S.R. Krishnaiah53 et al (2004) was to carry out pharmacokinetic evaluation of oral controlled release formulation (guar gum-based three layer matrix tablets) containing highly soluble metoprolol tartrate as a model drug. The results of the study indicated that guar gum three-layer matrix tablets were able to provide oral controlled delivery of highly water-soluble drug such as metoprolol tartrate in humans.
Alor R. Ray54 et al (2003) studied the role of modulating factors such as drug to polymer ratio, drug loading, particle size, and compaction pressure ant amount of lubricant on release Caffeine from tamarind seed polysaccharide, which is for hydrophilic matrix for drug delivery system. The following observation on release rate were made using Korsmeyer-Peppas's and Higuchi's equations i) the compaction pressure had no significant effect on release. ii) the effect of particle size polysaccharide on release was insignificant except in the range of 250-150 microns. iii) the increase in polymer content showed decreases in both rate of release and dissolution. Iv) the increase in drug loading showed the rate of release and dissolution decreased. v) the presence of lubricant up to 2% had no effect on the rate of release. The mechanism of release was found to be anomalous (n>0.5) in all the cases.
Y.S.R. Krishnaiah55 et al (2002) designed oral controlled drug delivery systems for highly water-soluble drugs using guar gum as a carrier in the form of a three-layer matrix tablet. The results indicated that guar gum, in the form of three-layer matrix tablets, is a potential carrier in the design of oral controlled drug delivery systems for highly water-soluble drugs such as metoprolol tartrate.