File Name: formulation and evaluation of extended release tablets .zip
Pharmacy College, Paloncha - , Telangana, India. ABSTRACT: The objective of the present study is to develop a pharmaceutically stable sustained release matrix tablets of Baclofen and perform the pre-compression, post compression and in-vitro evaluation studies of developed formulation.
- FORMULATION, DEVELOPMENT AND IN VITRO EVALUATION OF TRAMADOL EXTENDED RELEASE TABLETS
- Formulation and Evaluation of Sustained Release Matrix Tablets of Nifedipine
- Formulation and evaluation of extended release tablets of salbutamol sulphate
Shailesh T. Prajapati, Amit N.
FORMULATION, DEVELOPMENT AND IN VITRO EVALUATION OF TRAMADOL EXTENDED RELEASE TABLETS
Rabeprazole, a member of substituted benzimidazoles, inhibits the final step in gastric acid secretions. This drug claims to cause fastest acid separation due to higher pKa , and more rapidly converts to the active species to aid gastric mucin synthesis. The most significant pharmacological action of Rabeprazole is dose dependent suppression of gastric acid secretion; without anticholinergic or H2-blocking action.
It completely abolishes the hydrochloric acid secretion as it is powerful inhibitor of gastric acid. Rabeprazole is acid labile and hence commonly formulated as an enteric coated tablet. The absorption of rabeprazole occurs rapidly as soon as tablet leaves the stomach. In the present study an attempt was made to formulate and evaluate Rabeprazole sustained release matrix tablet using wet granulation technique incorporating various polymers like HPMC-E15, Carbopol, and sodium carboxymethyl cellulose CMC.
Studies revealed that all the physicochemical parameters comply with the official standards. The sustained release matrix tablets of rabiprazole shown better bioavailability, efficacy and potency, when compared with official standards.
Retention of drug delivery systems in the stomach prolongs overall gastrointestinal transit time improving oral bioavailability of the drugs that are having site specific absorption from the stomach or upper part of the small intestine. Therefore different approaches have been proposed to retain the dosage form in the stomach including bioadhesive systems, swelling, and expanding systems and delayed gastric emptying devices to achieve gastric residence time for sustained drug release.
The most employed method to modulate the sustained drug release is to include it in a matrix system. Because of their flexibility, hydrophilic polymer matrix systems are widely used in oral controlled drug delivery to obtain a desirable drug release profile, cost-effectiveness, and broad regulatory acceptance. In this type of drug delivery system, the drug is homogeneously dispersed throughout the matrix of crosslink of linear polymer chain.
Most of the highly water-soluble drugs, if not formulated properly, may readily release the drug at a faster rate, and are likely to produce toxic concentration.
Sustained release matrix tablets prepared by wet granulation technique using microcrystalline ethyl cellulose polymer and Bees wax showed good sustaining drug release concluding that sustained release tablet could be successfully combined with accurate control and prolongation of the drug release patterns. Chemically Rabeprazole is designated as RS [4- 3-methoxypropoxy methylpyridinyl] methylsulfinyl -1H-benzo[d] imidazole with molecular formula C 18 H 21 N 3 O 3 S.
It is the member of substituted benzimidazoles which inhibits the final step in gastric secretion. This probably reflects rabeprazole's faster activation in the parietal cell canaliculus. It inhibits the final transport of hydrogen ions via exchange with potassium ions into the gastric lumen. It does not have anticholinergic or histamine H 2 -receptor antagonist properties,[ 12 ] and is acid-labile. Once Rabeprazole has left the stomach, absorption occurs within 1 hour of administration.
The differences in the metabolism of these drugs may favorably or unfavorably affect their pharmacodynamics e. It has short biological half-life h that requires frequent daily dosing and therapeutic use in acid-related diseases that necessitates its formulation into sustained release dosage form. Talc, Magnesium stearate was from S. Fine Chem. All the chemicals were of analytical grade. Identification of Rabeprazole was examined by FT-IR and compared with the reference spectrum of drug.
The drug Rabeprazole Sodium was dissolved in phosphate buffer 7. Accurately 25 mg of Rabeprazole was taken in a ml volumetric flask. Sufficient amount of water was added to make up the mark stock solution. The absorbance of these solution were measured spectrophotometrically at a suitable wavelength. The observed absorbance was plotted against concentration [ Table 1 and Figure 1 ]. All the polymers and active ingredients were passed through sieve no. Accurately weighed amount of polymers and excipients were thoroughly mixed in glass mortar pestle.
The granules were prepared by wet granulation technique and passed them to sieve no. The granules were then mixed properly with magnesium stearate, talc and punched with the help of automatic punching machine to a desired hardness, shape, and size [ Table 2 ].
Randomly sampled 5 tablets in each batch of formulation were used for the determination of hardness with the help of Monsanto type hardness [ Table 3 ]. Roche friabilator is used in which approx. Then the deviation of individual weight from the drug weight was calculated [ Table 3 ]. The individual crown to crown thickness of ten tablets was determined using slide calipers for each batch [ Table 3 ].
The approach densities of the tablet were calculated from the volumes and masses in triplicate. The volumes v of the cylindrical tablets were calculated from their heights h and radius r are both determined with micrometer gauze using the mathematical equation for a cylinder [ Table 3 ]. Kept it for 48 hours then took 1ml from each of volumetric flask was transferred to the test tubes samples were then filtered, suitable diluted and analyzed spectrophotometrically at a suitable wavelength [ Table 3 ].
It was determined by using funnel method. The accurately weighed spheres were taken in funnel, and were adjusted in such a way that the tip of funnel just touches the apex of the heap of blends. The blends were allowed to flow through the funnel, freely on the surface.
The diameter of the powder concentration was measured; angle of repose was calculated by using following equation [ Table 3 ].
Apparent bulk density was measured by pouring the pre-weighed blend into a graduated cylinder. The bulk volume of the blend was determined, and then the bulk density was calculated by using the formula [ Table 3 ]. The measuring cylinder containing a known mass of blend was tapped for a fixed time and the min.
Volume Wt occupied in the cylinder was measured; the tapped density pt was calculated by using the following formula [ Table 3 ]. It is one method for determining flow properties and also called as carr's index of compressibility. It is indirectly related to the relative flow rate, cohesiveness, and particle size.
It is simple, fast, and popular method of predicting powder flow characteristic [ Table 3 ]. The possible interactions between Rabeprazole sodium and distinct polymers were investigated via FT-IR studies. Results proved that the drug was found to be compatible with excipients as wave numbers are almost similar for pure drug as well as drug excipients mixture.
The matrix tablet mainly fabricated using wet granulation method. As such all the formulated matrix tablets were of good quality respect to size, hardness, and drug content. The hardness measured by Monsanto type hardness tester was found within the range of 3 to 4.
The weight variation study was performed on 20 individuals on randomly selected samples from each batch; the weight uniformity results of prepared matrix tablets indicate no significant difference in the weight of individual tablet from average value and the variation was found within the limit [ Table 3 ]. The thickness of the formulated tablets was within the range of 0.
The drug content study was performed on 3 randomly selected samples from each batch. The formulated granules of different formulations were evaluated for their rheological properties like angle of repose, bulk density, tapped density, and Carr's index [ Table 3 ].
The result of angle of repose indicates the good flow properties of all the formulated granules. The bulk density, tapped density, and Carr's index values also suggested that the prepared granules have good property regarding flow ability.
In vitro releases of rabeprazole from different batches were studied using USP-II paddle type dissolution apparatus in acidic pH for 2 hrs and in phosphate buffer for 10 hrs. The different concentrations of different polymers showed different release patterns. By observing the release data it may be concluded that the release rate of drug from matrix formulations largely depends upon type of polymer and its amount.
In our study, our observation shows that the Rabeprazole matrix tablet extends the release rate of drug for a prolong period of time at least 10 hrs and shows to increase the bioavailability and simultaneously decrease the dosing interval as well as dosing amount. The formulation minimizes the blood level oscillations, dose related adverse effects and cost and ultimately improve the patient compliance and drug efficiency.
The authors are humbly thankful to Mr. Durga Verma Chairman and Mr. Chauhan Vice-chancellor, Uttarakhand Technical University, Dehradun for providing lab and library facilities. Source of Support: Nil. Conflict of Interest: None declared.
National Center for Biotechnology Information , U. J Pharm Bioallied Sci. Author information Article notes Copyright and License information Disclaimer. Hardoi, UP, India. Address for correspondence: Dr. Muhammad Afzal, E-mail: moc. This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3. Abstract Introduction: Rabeprazole, a member of substituted benzimidazoles, inhibits the final step in gastric acid secretions.
Aim: In the present study an attempt was made to formulate and evaluate Rabeprazole sustained release matrix tablet using wet granulation technique incorporating various polymers like HPMC-E15, Carbopol, and sodium carboxymethyl cellulose CMC.
Results: Studies revealed that all the physicochemical parameters comply with the official standards. Conclusion: The sustained release matrix tablets of rabiprazole shown better bioavailability, efficacy and potency, when compared with official standards. Methods Identification of pure drugs Identification of Rabeprazole was examined by FT-IR and compared with the reference spectrum of drug. Method used to estimate rabeprazole sodium The drug Rabeprazole Sodium was dissolved in phosphate buffer 7.
Prepration of calibration curve Rabeprazole in water Accurately 25 mg of Rabeprazole was taken in a ml volumetric flask. Table 1 Data for standard curve of rabeprazole in distilled water. Open in a separate window. Figure 1. Fabrication of tablets Wet granulations All the polymers and active ingredients were passed through sieve no. Table 2 Formulation chart. Determination of hardness of tablet Randomly sampled 5 tablets in each batch of formulation were used for the determination of hardness with the help of Monsanto type hardness [ Table 3 ].
Determination of friability Roche friabilator is used in which approx. Determination of weight variation 20 tablets were selected at random and weighed accurately; the average weight of the tablet was calculated. Determination of thickness of tablets The individual crown to crown thickness of ten tablets was determined using slide calipers for each batch [ Table 3 ].
Formulation and Evaluation of Sustained Release Matrix Tablets of Nifedipine
Department of Pharmaceutical Technology, Smt. Nagpur University Nagpur , India. Metformin hydrochloride has relatively short plasma half-life, low absolute bioavailability. The need for the administration two to three times a day when larger doses are required can decrease patient compliance. Sustained release formulation that would maintain plasma level for h might be sufficient for daily dosing of metformin.
Conventional drug delivery system for treating the angina and hypertension are not much effective as the drug do not reach the site of action in appropriate amounts. Thus potent and guarded therapy of this angina and hypertension disorder using specific drug delivery system is a challenging task to the pharmaceutical professionals. Most oftenly used method of regulating the drug release is to include it in a matrix system because of their pliability, hydrophilic polymer matrices are widely used in oral controlled drug delivery to obtain a desirable drug release pattern, methodical, and broad regulatory compliance. Formulation of Nifedipine sustained release matrix tablet was prepared by the polymers blend with to get desirable drug release profile. Evaluation parameters of formulated tablets were hardness, friability, thickness, drug content uniformity weight variation, and the in vitro drug release rate pattern. Sustained release dosage form is a modified dosage form that prolongs the therapeutic activity of the drug. Sustained release products provide an immediate release of drug that promptly produces the desired therapeutic effect which is followed by gradual release of additional amounts of drug to maintain this effect over a predetermined period of time.
If your institution subscribes to this resource, and you don't have a MyAccess Profile, please contact your library's reference desk for information on how to gain access to this resource from off-campus. Please consult the latest official manual style if you have any questions regarding the format accuracy. Most conventional immediate release oral drug products, such as tablets and capsules, are formulated to release the active drug immediately after oral administration. In the formulation of conventional drug products, no deliberate effort is made to modify the drug release rate. Immediate-release products generally result in relatively rapid drug absorption and onset of accompanying pharmacodynamic effects. In the case of conventional oral products containing prodrugs, the pharmacodynamic activity may be slow due to conversion to the active drug by hepatic or intestinal metabolism or by chemical hydrolysis. Alternatively, conventional oral products containing poorly soluble lipophilic drugs , drug absorption may be gradual due to slow dissolution in or selective absorption across the GI tract, also resulting in a delayed onset time.
PDF | The controlled or sustained release dosage forms are designed to complement the pharmaceutical activity of the medicament in order to.
Formulation and evaluation of extended release tablets of salbutamol sulphate
Rabeprazole, a member of substituted benzimidazoles, inhibits the final step in gastric acid secretions. This drug claims to cause fastest acid separation due to higher pKa , and more rapidly converts to the active species to aid gastric mucin synthesis. The most significant pharmacological action of Rabeprazole is dose dependent suppression of gastric acid secretion; without anticholinergic or H2-blocking action. It completely abolishes the hydrochloric acid secretion as it is powerful inhibitor of gastric acid.
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