Concentration Of Sodium Starch Glycolate Research Articles

Formulation, Evaluation and Study of Super Disintegrants effect on Olmesartan Medoxomil Fast Dissolving Tablets

The current research was to enhance solubility and dissolution rate of the slightly soluble drug, Olmesartan medoxomil, solid dispersions by physical mixing, solvent evaporation and kneading techniques, with soluplus. The solid dispersions prepared are tested for flow properties, drug content, and particle size. In vitro dissolution studies were carried out to analyse the drug release from solid dispersions. Crystal morphology, drug and polymer interaction for selected solid dispersions was studied by FT-IR and DSC analysis. Fast-dissolving tablets were formulated by using optimized solid dispersions using different concentrations of sodiumstarch glycolate, crosscarmellosesodium, and crospovidone as superdisintegrants using direct compression technique. The tablets prepared are tested for Weight variation, friability, disintegration, content uniformity and harness. The mechanism and kinetics of drug release from the fast-dissolving tablets were tested by in-vitro dissolution studies. The current research proves that combining solid dispersions along with the use of superdisintegrants is novel approach to formulate of Olmesartan medoxomil fast-dissolving tablets.

Application of Biomaterials in the Development of Hydrogel-Forming Microneedles Integrated with a Cyclodextrin Drug Reservoir for Improved Pharmacokinetic Profiles of Telmisartan.

Telmisartan (TEL) is a promising antihypertensive agent among other angiotensin receptor blockers. However, its oral application is limited by its poor water solubility. This study presents the successful utilization of biomaterial-based hydrogel-forming microneedles integrated with a direct compressed tablet reservoir (HFMN-DCT) for the transdermal delivery of telmisartan in the treatment of hypertension. The combination of PVP, PVA, and tartaric acid was used in the HFMN formulation. A range of cross-linking temperatures and times were employed to optimize the characteristics of the HFMN. The HFMN exhibited excellent swelling capacity, mechanical strength, and insertion properties. Additionally, the poorly soluble characteristic of TEL was improved by the inclusion complex formulation with β-cyclodextrin (βCD). Phase solubility analysis showed an Ap-type diagram, indicating a higher-order complex between TEL and βCD, with respect to βCD. A ratio of TEL:βCD of 1:4 mM demonstrates the highest solubility enhancement of TEL. The inclusion complex formation was confirmed by FTIR, XRD, DSC, and molecular docking studies. A significantly higher release of TEL (up to 20-fold) from the inclusion complex was observed in the in vitro release study. Subsequently, a DCT reservoir was developed using various concentrations of sodium starch glycolate. Essentially, both the HFMN and DCT reservoir exhibit hemocompatibility and did not induce any skin irritation. The optimized combination of the HFMN-DCT reservoir showed an ex vivo permeation profile of 83.275 ± 2.405%. Notably, the proposed system showed superior pharmacokinetic profiles in the in vivo investigation using male Wistar rats. Overall, this study highlights the potential of HFMN-DCT reservoir systems as a versatile platform for transdermal drug delivery applications.

Drug Formulation of Securigera securidaca Seed Extracts

S. securidaca seeds are reported to treat a variety of diseases; they contain multiple antidiabetic constituents and are widely used as anti-hyperglycemic, antibacterial, as well as anti-hyperlipidemic agents. The present work aimed to propose tablet formulations containing extracts of S. securidaca seeds in an attempt to obtain antibacterial and anti-hyperglycemic formulations with a more efficient oral hypoglycemic impact, limited side effects, and higher patient compliance for the first time, resulting in multiple benefits. Tablet formulations were created by encapsulating granules from S. securidaca seed extracts with varying concentrations of sodium starch glycolate as a super-disintegrant (0–3%). The final formulations were examined for weight variation, solubility, hardness, water content, disintegration time, friability, drug content (trigonelline and diosgenin), and in vitro drug release. The S. securidaca tablet formulations completed the weight test because the percentage deviation in the personal tablet weight and mechanical resistance from the mean were identified to be within the average range. In accordance with the results, formulations containing diosgenin as well as trigonelline as a super-disintegrant were identified as the ideal formulations. The amount of the active substance released from the tablet (S. securidaca seed extract formulation) was consistent throughout the results with the standard methods recommended by the FDA (94.05%) for diosgenin and 87.25% for trigonelline after 45 min. The acceptable limit, according to the FDA, is not more than (N.L.T.) 80% after 45 min for phase #1. The present study aimed to obtain an optimized formula for S. securidaca extract tablets that met the requirements of a good pharmaceutical preparation according to the United States Pharmacopeia (USP) and National Formulary (NF). This has important implications for the development of novel, effective treatments and significantly advances the development of natural medicine. Our findings are expected to be of interest to researchers, clinicians, and other experts in this field of study. Based on these findings, it can be inferred that the formulation of S. securidaca seed extracts with appropriate and compatible herbal dosage forms has fewer side effects and is more effective than traditional treatments.

Formulation and characterization of metformin hydrochloride orodispersible tablets with super disintegrants

Metformin hydrochloride's fast onset of action is very desirable, making it a prime candidate for the preparation of orodispersible tablets in the present study. This medication is prescribed for the management of type 2 diabetes, which does not respond to insulin. The tablets were made using direct compression and a mixture of the super disintegrants sodium starch glycolate (SSG) and croscarmellose sodium (CCS). Mannitol is a sugar-based excipient that serves as a binding agent, dissolves well in water, and provides a pleasant mouth feel. The blend's pre-compression results show that the medication excipients work well together and have desirable compression characteristics. Eight distinct formulations with varying amounts of SSG, CCS, and Mannitol were made. The properties of the tablets' drug release were measured, including their in vitro disintegration time, water absorption ratio, mechanical stability, wetting time, and so on. When using a greater concentration of SSG, CCS, and Mannitol, formulations F4 and F8 showed shorter in vitro disintegration times of 10.2 and 7.8 ​s, respectively, and formulation F8 showed 99.65% in vitro drug release at the end of 30 ​min. The orodispersible tablet performance can be enhanced through direct compression using the super disintegrants inclusion methodology.

Optimization of Tablet Formulations Containing Green Robusta Coffee Beans (Coffea canephora) Extract with Various Concentrations of Sodium Starch Glycolate As a Disintegrant

Chlorogenic acid, found in robusta green coffee beans, is an antidiabetic agent. It is made into robusta green coffee bean extract tablets which are varied with 3 concentrations of sodium starch glycolate (SSG) as a disintegrant. This paper aimed to determine the effect of variations in the concentration of sodium starch glycolate (4%, 6%, 8%) on the physical characteristics of the granules (particle size distribution, flow properties, angle of repose and compressibility) and tablet dosage characteristics, which include, hardness, friability, and disintegration time of robusta green coffee extract tablets. Robusta green coffee bean extract tablets were made with varying concentrations of sodium starch glycolate (4%, 6%, 8%) using the dry granulation method. The granule test parameters: flow properties test, compressibility test and particle size distribution test, were carried along with the tablet test parameters: hardness test, friability test and disintegration time test. Data were analyzed using the one Way-Anova. From the results of the study, it was found that the concentration of SSG did affect granule properties and tablet hardness. There was a significant difference in the friability test and disintegration time test.
 Keywords: sodium starch glycolate, disintegrant, robusta green coffee bean extract, tablet

Polymeric hydrogel forming microneedle-mediated transdermal delivery of sildenafil citrate from direct-compressed tablet reservoir for potential improvement of pulmonary hypertension therapy

Pulmonary hypertension (PH) is a cardiovascular disease affecting patient’s life. Sildenafil citrate (SC), the first-line treatment, is present in oral and injectable forms with some drawbacks, primarily poor patient’s comfort and low oral bioavailability. To counter these limitations, stratum corneum-penetrating hydrogel-forming microneedles (HFM) was created, making it easier to distribute SC transdermally. HFM was fabricated using polyvinyl alcohol (PVA) and two variations of polyvinyl pyrrolidone’s (PVP) concentration as polymers and citric acid (CA) as crosslinking agent. The crosslinking time was also variated. The assessment of swelling, insertion characteristics, and mechanical resistance revealed that it possessed swelling capacities up to 470 % and strong insertion capabilities. This HFM was integrated with a tablet reservoir prepared using several concentrations of sodium starch glycolate (SSG) as super disintegrant. The tablet reservoir's hardness, dissolution rate, XRD, and FTIR profiles were evaluated and the results showed that 4 % of SSG was the option for enhancing SC’s solubility. According to ex vivo study, this system released 24.12 ± 0.92 % of SC. For the first time, SC was successfully incorporated into a system of HFM and tablet reservoir and was non-toxic, showing promise in terms of improving PAH therapy's efficacy following comprehensive in vivo studies in the future.

OPTIMIZATION OF CROSCARMELLOSE AND SODIUM STARCH GLYCOLATE ON ORALLY DISINTEGRATING METOCLOPRAMIDE HCL TABLETS

Dosage form of metoclopramide HCl which has high solubility but low permeability is Orally Disintegrating Tablet (ODT), because can decrease first-pass-effect metabolism so that its bioavailability and effectiveness increase. Superdisintegrant is an excipient that has a major role in the formulation of ODT. The combination of croscarmellose and Sodium Starch Glycolate (SSG) can accelerate tablet disintegration time so that the resulting ODT is suitable for its intended use. The purpose of this study was to determine the effect of each and the interaction of the use of croscarmellose and SSG on the physical characteristics of ODT metoclopramide HCl, and to get the optimum formula of ODT metoclopramide HCl. Tablets were prepared by direct compression method. Optimization process by using simplex lattice design (design expert 10.0.1.R program) with eight formulas, including FI (5.25%A:1.75%B), FII (0%A:7%B), FIII (7%A:0%B), FIV (1,75%A:5,25%B), FV (7%A:0%B), FVI (3.5%A:3.5%B), FVII (3.5%A:3.5%B) and FVIII (0%A:7%B). Component A is the concentration of croscarmellose and component B is the concentration of SSG. Based on SLD equation could be seen the single-use croscarmellose and SSG components be increased flowability, hardness, moisture content, friability, water ratio absorption, weight uniformity, uniformity of content, accelerate disintegration time, wetting time, and dissolution. Interaction of the two components was increased flowability, moisture content, water ratio absorption and dissolution, decreased hardness, friability, uniformity of content, weight uniformity, accelerate disintegration time, and wetting time. The optimum formula of ODT metoclopramide HCl with proportion 5.145% croscarmellose and 1.855% SSG. Based on the one sample t-test between theoretical results and the experimental results could be seen that there were no significant differences between them

Design, Formulation and Evaluation of Fexofenadine HCl Immediate Release Tablets by Solid Dispersion Method using Solvent Evaporation Technique

Currently, this study focuses on developing immediate-release Fexofenadine hydrochloride tablets. The Fexofenadine HCl tablets have super disintegrants that help to accelerate dissolution and bioavailability. Sodium lauryl sulphate, microcrystalline cellulose as filler, crospovidone, and sodium starch glycolate were used to make the tablets using a direct compression method (2-8 percent). Pre and post compressional parameters were used in the preparation of the tablets. The In-vitro disintegration study shows that as concentration of sodium starch glycolate is increased, there is an increase in the amount of time it takes for the solution to disintegrate, but at the same time, there is a decrease in the amount of time it takes for the solution to disintegrate when the crospovidone level is increased. When combined with the crospovidone tablet formulation, the test found that the resulting tablets broke down in approximately 3 to 6 minutes, with enough force to release the fragments but not to harm the friability of the product. It was found that Fexofenadine hydrochloride tablet, a fast-acting form of treatment for allergic rhinitis, could be formulated in an immediate-release form.

Formulation, optimization and evaluation of fast dissolving tablets of Lamotrigine using natural disintegrant agent

Objective: The present investigative work is aimed for formulating, optimizing and evaluating the Fast Dissolving Tablets (FDT) of Lamotrigine in improving the disintegration time and dissolution rate with Locust bean gum as natural disintegrant agent in combination with Sodium Starch Glycolate (SSG). Methods: Employed 32 full factorial design for optimization of Lamotrigine blend formulations. Concentrations of Locust bean gum (X1) and concentration of SSG (X2) are two factor independent variables. Experiments are conducted to identify their effect on three dependent variables are disintegration time (Y1), drug release in 5 min (Y2), and drug release in 30 min (Y3). Drug interactions between Lamotrigine and Locust bean gum were investigated with FTIR, DSC, XRD compatibility studies. Direct compression method is used for tablet manufacturing. Results: Pre and post compression parameters of Lamotrigine FDT’s are evaluated and found within acceptable limits. Among multiple formulations, LF8 formulation has demonstrated lower disintegration time in 40 ± 3.81sec and wetting time in 38 ± 0.31sec, maximum drug release is 97.88% in 30min. In short time stability studies, no major transformations are identified in physical and chemical properties of Lamotrigine FDT’s. In-vivo studies of Lamotrigine fast dissolving tablets showed faster absorption rate.

A recent solidification approach for nanosuspension: formulation, optimisation and evaluation of canagliflozin immediate release pellets.

Abstract.

Maraviroc Oral Disintegration Tablet: Analytical Design of Experiments (DoE) for Assessment and Comparison of In vitro Dissolution Profiles

Background: The bioavailability of a drug in a solid oral dose depends on its release from the drug product and its balance in dissolution. Compared with a reference drug, the newly developed formulation needs to establish bioequivalence by comparing the dissolution profile. Objective: To compare dissolution profiles of a newly developed maraviroc oral disintegration tablet and the reference Axentri® tablet. The current research was designed to establish and validate an integral analytical consistency by Quality by Design (QbD) approach to quantify maraviroc from dissolution samples using the RP-HPLC method. Methods: Maraviroc was formulated into an orally disintegrating tablet using a direct compression technique at different concentrations of sodium starch glycolate as super disintegrants and talc and magnesium stearate as glidants. The dissolution test in 0.1N HCl was performed according to standard procedures to predict bioequivalence. The results of dissolution tests were analyzed using the QbD Box Behnken Design multivariate RP-HPLC method. Results: The optimized formulation (F2) was selected as it showed 90% drug release in 5 min and a disintegration time of 22 sec with dissolution profiles to the marketed reference to meet the FDA requirements of f2 similarity factor statistics. The integrated analytical QbD method was statistically analyzed by ANOVA, counter-plot, and 3D response surface plots, which demonstrated that the model is statistically significant. The developed method was validated as per ICH guidelines Q2 (R1). Conclusion : In conclusion, maraviroc oral disintegrating tablets have been well prepared, and superior statement consistency is established by the implementation of the QbD analytical method for orally disintegrating tablet excellence and adoption.

Design and development of fast dissolving liquisolid formulation

Various techniques have been employed for the solubility modification of BCS class II drugs. Out of the recent solubility enhancement techniques, Liquisolid technique based on the work of Spireas et al has explored as method that can supplement drug release. Formulations containing Etodolac were developed by dissolving the drug in a non-volatile solvent and then employing the adsorption absorption principle with a carrier and coated material admixture. The post formulation saturation solubility study has highlighted significant modification in solubility of the drug in comparison to pre solubility modification. The Liquisolid formulation then subjected to direct compression for the development of Fast dissolving tablet formulation using two varying concentrations of Sodium Starch Glycolate. The in vitro - in vivo evaluation of research study concludes adaptability and applicability of fast dissolving liquisolid tablet formulation allowing it to overcome barriers associated with the solubility. The optimized formulation found to unveil dissolution along with diffusion from the dosage form by Fickian mechanism. Keywords: Etodolac, Liquisolid, Carrier material, Coating material Fast dissolving tablet, Superdisintegrant.

Time-controlled release by the incorporation of superdisintegrants within the coat of zein dry coated tablets

The aim of this work was to develop zein-based press coated tablets for delayed, time-controlled drug release. Press coated tablets containing dextrates and chlorpheniramine maleate (BCS class 1 drug) in the core, and zein and either NaCl, sodium starch glycolate (SSG) or crospovidone (XPVP) in the coat were produced. Results show that tablets containing zein and NaCl in the coating could not release nearly any drug over 8 h. On the contrary, when SSG and XPVP were incorporated at a level of 8 % in the coating, a delayed drug release pattern was obtained, characterised by a lag-time of 3 h, followed by a burst of >80 % drug release over 6–7 h. Drug release was dependent on the concentration of SSG and XPVP in the formulations. Images of the tablets showed that during the lag-time the dosage forms did not change shape, although they started to swell. After this time, tablets gradually deformed and eventually ruptured. The lag-time is due to the time needed for the water to diffuse in, for the drug to dissolve and for the coating to become sufficiently permeable. The addition of the hydrophilic and swellable superdisintegrants SSG and XPVP to zein shifted the hydrophilic/hydrophobic balance of the coatings to higher hydrophilicity, thus enabling rapid hydration and drug release after the lag-time. This study demonstrates that zein-based macroscopic drug delivery systems can be tuned to tailor drug release to specific needs, i.e. delayed release in this case.

A Comparative Evaluation of Fast Dissolving Tablets of Acetaminophen Using Super-disintegrant Blends and Sublimation Method

Fast disintegrating tablets (FDTs) are gaining prominence as drug delivery systems and emerging as one of the popular and widely accepted dosage forms, especially for the peadiatric and geriatric patients. This study aims to evaluate and compare the tablet properties of fast disintegrating tablets of acetaminophen prepared by super-disintegrant blends and sublimation methods. Two groups of tablets comprising various batches were prepared by wet granulation. Granules batches of one group of tablets (A-G) were prepared with different concentrations of sodium starch glycolate and croscarmellose sodium while the other group of tablets (H-N) were incorporated with varying concentrations of menthol into the batches. The granules were subjected to analysis and compressed into tablets. The post-compression parameters of the tablets such as weight uniformity, crushing strength, friability, wetting and disintegration times, as well as dissolution studies were evaluated. Drug-excipient compatibility studies using Fourier transform infrared (FTIR) analysis was also carried out. Granules were fair to good in flow with Carr’s indices ≤ 20.14 and angles of repose ranging from 21.34 to 35.00°. Tablets crushing strength values were between 3.44 to 8.26 kp while their friability values were < 1.52%. They showed wetting and disintegration times that were ≥ 0.18 and ≥ 0.25 min. Dissolution studies showed that four batches of tablets (two from each method used in formulation) achieved 100% drug release within 30 min. FTIR analysis shows no interactions between acetaminophen and excipients used in formulation. Tablets from both methods were comparable in their tablet properties but the disintegrant blend tablets exhibited superior crushing strengths, hence formed harder tablets, while the sublimation method tablets were superior in their wetting and disintegration times.
 Keywords: acetaminophen, super-disintegrants, sublimation, tablet parameters

Optimization formula of fast disintegrating tablets Ketoprofen β-cyclodextrin inclusion complex with sodium starch glycolate and crospovidone as the superdisintegrants

Ketoprofen has low solubility in water with unpleasant taste. Efforts to improve solubility and taste are by forming inclusion complexes using β-cyclodextrin. In its development to release Ketoprofen quickly, fast disintegrating tablets (FDT) were prepared. The speed of drug release is influenced by the speed of disintegration tablets. The combination of sodium starch glycolate (SSG) and crospovidone (CP) combines swelling and wicking action which speeds up the disintegration of tablets. This study aims to obtain the optimum value of the combination of both in order to obtain FDT with optimum evaluation parameters according to the requirements. The study made 8 run FDT directly with variations in the concentration of SSG 2–8% and CP 2-5%. Evaluations carried out at each run included flow velocity tests, uniformity of preparation, hardness, friability, disintegration time, wetting time and dissolution. Data were analyzed using simplex lattice design method. The optimum formula predicted results are verified by analysis of one sample t-test. The results showed increasing the proportion of SSG increases hardness, disintegration time and wetting time and decreases fragility of FDT. The optimum formula found at combination of 2% SSG and 5% CP with optimum physical properties and percent release and sweet taste.

Optimized chronomodulated dual release bilayer tablets of fexofenadine and montelukast: quality by design, development, and in vitro evaluation

BackgroundThe conventional oral dosage forms are not effective in dealing with chronopathological conditions, such as nocturnal asthma. Therefore, there is an unmet need to develop a delivery system that can deliver drug as per the chronopharmacology of the diseases. The purpose of the study is to use quality by design (QbD) technique and pulsatile principles for the development of Eudragit-coated dual release bilayer tablets. The dual layer consists of immediate release layer of fexofenadine HCl and sustained release layer of montelukast sodium.ResultsThe quality target product profile of the formulation was developed, and the critical quality attributes were identified. Three-level, three-factor Box-Behnken design was used for the optimization of the bilayer tablets. Based on the design, a total of 13 formulation combinations (F1–F13 and M1–M13) were made having acceptable micromeritic properties. The developed immediate and sustained release layers were evaluated for physicochemical properties. Depending upon the value of the diffusion exponent, the Fickian diffusion mechanism is dominant among immediate and sustained release tablet layers. Response curve for immediate release layer showed that concentrations of sodium starch glycolate and sodium bicarbonate had a negative effect on disintegration time and a positive effect on drug release. For sustained release tablet layer, concentrations of HPMC E 5 LV and magnesium stearate had a significant effect on drug release. The ANOVA and diagnostic plots confirmed the significance and goodness of fit of the used model. Based on desirability plot values, optimized formulation was developed and coated with Eudragit coat. The coated bilayer tablet showed met the requirement of providing an immediate release during the first hour and a sustained release action for a period of more than 8 h after passing the gastric region.ConclusionsThe formulation can be fruitful in curbing the menace of nocturnal asthma and providing a high degree of patient compliance as the patient will not have to wake up at night to take the medication.

FORMULATION AND CHARACTERIZATION OF MODIFIED RELEASE TABLET OF CAPTOPRIL FOR THE TREATMENT OF HYPERTENSION

Modified release formulation has been the first choice for formulators of Pharmaceutical formulation it is due to their versatile potential of releasing the drug in desired rate and release kinetic irrespective of their physiochemical and Biopharmaceutical properties. In this research work an attempt was made to formulate Captopril modified release tablet in order to facilitate its release in desired rate and in optimum concentration , Formulation of Tablet formulation was done by preparing bilayer tablet of the drug in which immediate release layer was optimized by using different concentration of sodium starch glycolate and controlled release tablet was formulated by optimizing the concentration of Hydroxypropyl methyl cellulose K4M then they were united and compressed together to formulate optimized formulation among the prepared formulation batches optimized batch F2 exhibited best results of all the evaluation parameters.

Formulation and Evaluation of Immediate release tablets of Topiramate using Sodium starch glycolate

The aim of the current study was to develop immediate release tablets (IRT) of topiramate using different concentrations of sodium starch glycolate (SSG) as super disintegrant. Four different formulations of IRT were prepared using wet granulation method. Different pre compression and post compression characterization of tablet was carried out. In vitro drug release studies were carried out in USP II paddle type dissolution apparatus for different formulation and the batch containing 7.5 mg of SSG per tablet gave maximum amount of drug release of 90.76% at the end of 50 mins. Drug and excipients compatibility studies were carried out through FTIR spectroscopy. FTIR spectroscopy studies revelled that there is no interaction between drug and different excipients used in formulation. Short term stability studies (at 40±2oC/75±5% RH) on the best formulation indicated that there were no significant changes in release profile and drug content after a period of one to three month. Among all the formulations, F4 formulation was finally optimized.

FORMULATION AND EVALUATION OF LIDOCAINE HYDROCHLORIDE CHEWABLE TABLET

Objective: The objective of this study was to formulate and optimize a chewable formulation of lidocaine hydrochloride using a 32 factorial design for optimized the superdisintegrant concentration.Methods: Various concentrations of sodium starch glycolate (SSG) (13.33 mg, 26.66 mg, and 40 mg) of superdisintegrant and starch (50 mg, 83 mg, and 116.66 mg) were added in the formulation; nine formulations were prepared according to 32 factorial designs and evaluated. The responses were analyzed for analysis of variance using Design-Expert version 10 software. Statistical models were generated for each response parameter. The models were tested for significance. Procedure to manufacture chewable tablets by direct compression was established.Results: The results show that the presence of a superdisintegrant is desirable for chewable formulation. The best-optimized batch F7 found the batch having starch of amount 116.66 mg and SSG 13.33 mg. All the prepared batches of tablets were within the range. Optimized batch F7 showed drug content 102.46±0.0543, wetting time 18±1.7320, friability 0.65±0.0216, and drug release rate 99.97±0.0124% at the end of 30 min.Conclusion: It can be concluded that 32 full factorial design and statistical models can be successfully used to optimize the formulations, and it was concluded that the trial batch F7 is the optimized formulation which compiles official specifications of chewable tablets. The optimized batch was evaluated for thickness, weight variation, hardness, friability, drug dissolution, and stability study for 3 months. The similarity factor was calculated for comparison of dissolution profile before and after stability studies. After 30 min the drug release rate for batch F7 was 98.97% (Table 6). Hence, the results of stability studies reveal that the developed formulation has good stability.

FORMULATION AND EVALUATION OF FAST DISINTEGRATING LOSARTAN POTASSIUM TABLETS BY FORMAL EXPERIMENTAL DESIGN

In the treatment of hypertension fast onset of action is the major concern. The problem of slow onset of action of drugs can be overcome by development of appropriate dosage forms. Fast disintegrating tablets in mouth are best suited and have gained popularity in the oral antihypertensive drug therapy. These are advantageous over other conventional systems in terms of patient compliance, rapid onset of action, accurate dosing, good chemical stability, convenience of self-administration and compactness. Losartan potassium is widely used as an antihypertensive drug, which is a potent drug candidate for developing in to Fast Dissolving Tablets (FDT’s). It has low bioavailability due to first pass metabolism. Hence the main objective of the study was to formulate fast dissolving tablets of Losartan potassium to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablet of Losartan potassium were formulated by using microcrystalline cellulose with different concentration of super disintegrants like sodium starch glycolate and Isabgol Mucilage. All the batches were prepared by direct compression.
 API characterization studies were conducted to check the purity of API .The tablets were evaluated for Pre compression parameters and post compression parameters. Before the formulation of the tablets IR spectroscopic studies were also performed to check the compatibility with the excipients.
 A 23 full factorial design was applied to investigate the combine effect of 3 formulation variables. Here the concentration of Isabgol mucilage, concentration of Sodium Starch Glycolate and concentration of Microcrystalline Cellulose were taken as independent variable X1, X2 & X3 respectively and their effect of disintegration time is studied as dependent parameter. To represent the data Design Expert software is used.