Croscarmellose Research Articles

FORMULATION AND EVALUATION OF PIROXICAM FAST DISSOLVING TABLETS

Piroxicam is an analgesic, antipyretic and anti-inflammatory effects drugs, used to reduce pain, swelling joint stiffness from osteoarthritis, rheumatoid arthritis and by inhibiting prostaglandin synthetase. In the research work, seven formulations (F1 to F7) were prepared direct compression method by using 3 superdisintegrants namely Crospovidone, Crosscarmellose sodium and Sodium starch glycolate in two ratio (1:0.5 and 1:1) and F7 (without superdisintegrant). All the formulations evaluated various post compression parameters thickness, weight variation, disintegration time, hardness, friability, wetting time, drug content water absorption ratio and in- vitro dissolution studies. The best formulation was studied anti-inflammatory activity in rats by using the paw-edema method. Among all formulations (F1) which contains 1:0.5ratio of Croscarmellose sodium, showed to be the optimized formulation as it give good wetting time (51.66 sec), fast disintegration time (29.16 sec), maximum drug release of 99% within 30 minutes and superior anti-inflammatory activity.

Formulation and Evaluation of Effects of Superdisintegrants on Immediate Release Tablet of Linagliptin, a DPP-4 Inhibitor

The study aimed to develop and evaluate an immediate-release tablet dosage form of Linagliptin. Different concentrations (ranges 5-10%) of super-disintegrants, Croscarmellose sodium (CCS), and Sodium starch glycolate (SSG) were used to prepare nine tablet dosage forms (F1 to F9) through the direct compression method. The compatibility of the formulations was evaluated by FTIR to reveal any possible drug-excipient interactions and it was proved to be compatible with all formulations. Precompression (bulk density, tapped density, Carr’s index, Hausner’s ratio, and angle of repose) and post-compression parameters (weight variation, hardness, thickness, and friability) were analyzed for all tablets and the results were found satisfactory as well as within limits as per USP guidelines. All the formulated batches (F1 to F9) exhibited disintegration of tablets within 2 minutes, where formulation F9 represented the lowest disintegration time (51±3 sec) which was also found significantly better than the marketed product (310±5 sec). In terms of drug dissolution, 90% of drug release was observed for all nine formulations within 45 minutes and formulation F9 (5% CCS and 5% SSG) illustrated the rapid and highest dissolution rate compared to the marketed one’s, 100% drug release at 20 minutes and 91.77 % drug release at 30 minutes successively. The respective data sets of drug release were mathematically fitted to several kinetic models and for all formulations, drug release pattern obeyed first-order kinetics amongst those, formulation F2 (r2= 0.98), F4 (r2= 0.99), F5 (r2= 0.98), and F9 (r2= 0.97) were found to be best fitted in this kinetic norm. Based on disintegration time and dissolution data comparison to a brand leader market product, F9 was experienced as the best formulation. Furthermore, it was observed that if SSG and CCS were combined, then these two parameters were more improved compared to their separate uses. Thus, incorporation of the optimum amount of super-disintegrants in a formulation showed rapid swelling, faster disintegration as well as ease of dissolution of tablet dosage forms. Bangladesh Pharmaceutical Journal 24(2): 168-179, 2021

Characterization of the viscoelasticity of disintegrants by dynamic rheological analysis

This study focused on defining a quantitative disintegration index for tablet disintegrants based on a dynamic viscoelastic analysis of the complex disintegration mechanism associated with swelling and wicking. We used an oscillatory rheometer with a serrated-plate measuring system to evaluate the viscoelastic properties of three disintegrants, croscarmellose sodium (CCS), crospovidone (CPV), and corn starch (CS), which were prepared with distilled water at different liquid-to-solid ratios. The swelling and wicking disintegration indices were calculated from the obtained data. The results showed that the three disintegrants could be evaluated by the shear stress and loss tangent as representative dynamic viscoelasticity parameters that changed depending on the water content in the disintegrant preparation. Additionally, the viscoelasticity of CCS and CPV was strongly affected by swelling, whereas that of CS was mainly associated with wicking and water penetration. Furthermore, CPV had the largest swelling disintegration index value, whereas CS showed the largest wicking disintegration index value among the three disintegrants. These results suggested that the disintegration indices based on viscoelasticity established in this study could reflect the disintegration properties inherent to each disintegrant type. Our findings provide valuable guidance for selecting suitable disintegrants in the formulation design.

DESIGN, OPTIMIZATION AND EVALUATION OF ACECLOFENAC FAST DISSOLVING TABLETS EMPLOYING STARCH VALERATE–A NOVEL SUPERDISINTEGRANT

Objective: To synthesize, characterize and evaluate starch valerate as a superdisintegrant in the formulation of aceclofenac fast dissolving tablets by employing 23 factorial design.
 Methods: Starch valerate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of aceclofenac was prepared by employing starch valerate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design for evaluation of tablet parameters like disintegration and dissolution efficiency in 5 min.
 Results: The starch valerate prepared was found to be fine, amorphous and free flowing. Starch valerate exhibited good swelling in water with swelling index (125.2%). The study of starch valerate was shown by fourier transform infrared spectra (FTIR). The drug content (200±5%), hardness (3.5–4 kg/sq. cm), and friability (<0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch valerate. The disintegration time of all the formulated tablets was found to be in the range of 14±0.04 to 25.7±0.02 sec. The optimized formulation F4 had the least disintegration time i.e., 12.8±0.02 sec. The wetting time of the tablets was found to be in the range of 76±0.21 to 217±0.17s. The In vitro wetting time was less (i.e., 28±0.02s) in optimized formulation F4. The water absorption ratio of the formulated tablets was found to be in the range of 46±0.12 to 100±0.27%. The percent drug dissolved in the optimized formulation F8 was found to be 99.93% in 5 min.
 Conclusion: Starch valerate, when combined with sodium starch glycolate, croscarmellose sodium, with aceclofenac, was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 5 min.

OPTIMIZATION OF STARCH CROTONATE AS A NOVEL SUPERDISINTEGRANT IN THE FORMULATION OF FAST DISSOLVING TABLETS THROUGH 23 FACTORIAL DESIGN

Objective: To synthesize, characterize and evaluate starch crotonate as a superdisintegrant in the formulation of Piroxicam fast dissolving tablets by employing 23 factorial design.
 Methods: Starch crotonate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of Piroxicam were prepared by employing starch crotonate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design.
 Results: The starch chrotonate prepared was found to be fine, free flowing and amorphous. Starch crotonate exhibited good swelling in water with swelling index (50%). The study of starch crotonate was shown by fourier transform infrared spectra (FTIR). The drug content (100±5%), hardness (3.6–4 kg/sq. cm), and friability (<0.15%) have been effective with regard to all the formulated fast dissolving tablets employing starch crotonate. The disintegration time of all the formulated tablets was found to be in the range of 18±03 to 66±03 sec. The optimized formulation F8 had the least disintegration time i.e., 18±03 sec. The wetting time of the tablets was found to be in the range of 49.92±0.11 to 140±0.18s. The In vitro wetting time was less (i.e., 74±0.37s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 27.58±0.01 to 123.07±0.33%. The percent drug dissolved in the optimized formulation F8 was found to be 99.83% in 10 min.
 Conclusion: Starch crotonate, when combined with sodium starch glycolate, croscarmellose sodium, with Piroxicam was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 10 min.

Formulation and Invitro evaluation of immediate release tablets containing febuxostat

In the present research work, Febuxostat Immediate Release Tablet was prepared by direct compression method using varying concentrations of Lycoat, Crospovidone& Croscarmellose sodium as disintegrants. The formulations prepared were evaluated for precompression& post-compression parameters. From the drug excipient compatibility studies, we observe that there are no interactions between the pure drug (Febuxostat) and optimized formulation (Febuxostat+ excipients) which indicates there are no physical changes. Post compression parameters were found to be within the limits. Among the formulation prepared the tablet containing 12mg of CCS shows 98.13% of the drug release within 45 min & follows first-order kinetics.

Formulation and Evaluation of Mouth Dissolving Tablet of Benazepril Hydrochloride

Antihypertensive drugs are expected to give quicker action with better bioavailability. In the present study, mouth dissolving tablets of Benazepril Hydrochloride were formulated by using direct compression technique employing combination of a superdisintegrants to achieve rapid disintegration of the tablets in oral cavity Croscarmellose sodium, sodium starch glycolate and crospovidone were used as superdisintegrant to prepare six batches of mouth dissolving tablets out of which tablets prepared from crospovidone showed best results. Drug and physical mixture was characterized by FTIR for compatibility study. Optimization technique was employed to predict the best formulation of all the combinations prepared. Prepared formulations were optimized and evaluated for wetting time, dispersion time and different quality parameters. Optimized formulation was compared with marketed formulation for in vitro drug release and it was found that mouth dissolving tablet shows efficient drug release.

Orally Disintegration Tablet (ODT) Formulation of Candesartan Cilexetil With Croscarmellose Sodium and Crospovidone as Superdisintegrant

Candesartan cilexetil is a group of selective AT1 hypertension drugs (angiotensin II receptor antagonist 1). The drawback of candesartan cilexetil in conventional tablets is that it cannot be used for geriatric patients who have difficulty swallowing tablets, patients with developmental disorders of the muscle and nervous system (tremors), and in schizophrenic patients that lead to poor patient compliance, so to overcome this problem alternative dosage forms are made new namely ODT candesartan cilexetil. This study aims to determine the effect of the combination of superdesintegrant croscarmellose sodium and crospovidone on the quality test of the physical properties of tablets. Candesartan cilexetil ODT tablets bolted by direct compression method with variations in levels of superdesintegrant croscarmellose sodium and crospovidone 2: 3,5%, 2,75: 2,75%, 5: 0,5%, 4,25: 1,25 %, 3,5: 2%. Tests conducted to determine the physical quality of candesartan cilexetil ODT, namely organoleptic, weight uniformity, size uniformity, hardness, brittleness, disintegration time, wetting time and water absorption ratio. Showed an increase in the use of crospovidone (5%) and a decrease in croscarmellose sodium (0.5%) had a greater effect on the disintegration time because it could make the tablet porous when in contact with water so that it would accelerate the disintegration time of 29.167 seconds and increase the speed of wetting the tablets 25.33 seconds. The combination of superdisintegrant croscarmellose sodium and crospovidone (0.5: 5%) in formula 3 can provide physical properties that meet the best quality ODT requirements for candesartan cilexetil.

Solubility and Dissolution Enhancement of Ebastine by Surface Solid Dispersion Technique

Ebastine (EBS) is a non-sedating antihistamine with a long duration of action. This drug has predominantly hydrophobic property causing a low solubility and low bioavailability. Surface solid dispersions (SSD) is an effective technique for improving the solubility and dissolution rate of poorly soluble drugs by using hydrophilic water insoluble carriers.
 The present study aims to enhance the solubility and dissolution rate of EBS by using surface solid dispersion technique. Avicel® PH101, Avicel® PH 102, croscarmellose sodium(CCS) and sodium starch glycolate(SSG) were used as water insoluble hydrophilic carriers.
 The SSD formulations of EBS were prepared by the solvent evaporation method in different drug: carrier weight ratios and evaluated for their percentage yield, drug content , water solubility, dissolution study in 0.1 N HCl, crystal lattice using powder X-ray diffraction (PXRD) and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier interaction.
 Most of the prepared SSD formulas showed improvement of drug solubility. The best result was obtained with formula SSD16 (EBS:CCS 1:15) that showed high percentage yield (98.5%), high drug content (98.39%) and 8.2 fold increase in solubility compared to solubility of pure drug with improved dissolution rate. The drug was converted to amorphous form without chemical interaction with the carrier.

Formulation and In-Vitro Evaluation of Orally Disintegrating Tablets (ODTs) of Tramadol Hydrochloride

Since orally disintegrating tablets (ODTs) of tramadol hydrochloride are not available in the market, so an attempt has been taken to formulate and evaluate ODT preparation of tramadol hydrochloride. In this present work, direct compression was the technique used for preparing ODT using superdisintegrants like croscarmellose sodium, sodium starch glycolate and crospovidone at different concentrations. Prepared formulations were evaluated for various quality parameters- angle of repose, Carr’s index, Hausner ratio, weight variation, friability, hardness, drug content, dispersion time, wetting time and in-vitro dissolution. The angle of repose data indicated that the flow property of all the formulations was good to excellent. Comparing with the specifications, the results of Carr's index (%) and Hausner’s ratio indicated that the flowability of all the formulations blend was significantly good. Prepared formulations showed average wetting time ranging from 40-45 seconds, average dispersion time with 3-6 minutes. In-vitro dissolution profile indicated the cumulative % drug release between 30-80% for most of the cases.
 Keywords: Orally disintegrating tablets, Tramadol hydrochloride, Superdisintegrants, Direct compression.

Development and Characterization of a Combination Tablet Dosage Form Containing Sofosbuvir and Ribavirin Using Design of Experiments (DoE) Approach

Worldwide more than 180 million people get infected by chronic Hepatitis C Virus (HCV) and around 700,000 people pass away every year due to HCV related problems. Sofosbuvir and Ribavirin are prescribed as combined medication for the management of HCV infection globally. Therefore, optimization of a pharmaceutical dosage form containing Sofosbuvir and Ribavirin can open a new hope in the treatment of HCV infection. This study was conducted by using the Design of Experiments (DoE) approach. It is a systematic process aiming to determine the correlation between formulation factors affecting the approach and the output of the approach. During the development of formulations, two factors were considered, which are Croscarmellose Sodium (CCS) and Povidone K30 (PK30) at different concentrations ranging from 0.19% to 2.31% of the total tablet weight in 9 different formulations. Their effect on disintegration time (DT) was evaluated through statistical method and it was found between 3±0.003 and 6.5±0.015 minutes. The use of these two different disintegrants exhibited a significant effect on DT. The contour plot showed predicted ranges of concentrations of CCS and PK30 for desired DT. Fourier Transform Infrared Spectroscopy (FTIR) data, Thermogravimetric Analysis (TGA) and X-ray Diffractometry (XRD) spectrums confirmed that there was no interaction between Sofosbuvir and Ribavirin or with any other excipients used in this experiment.
 Dhaka Univ. J. Pharm. Sci. 20(1): 121-133, 2021 (June)

Fabrication And In-Vitro Analysis Of Mouth Dissolving Tablets Of Ondansetron Using Water Insoluble Super Disintegrant

In the present time, a mouth dissolving tablets become popular over conventional oral solid dosage form as it overcome common problem associated with conventional oral tablet dosage form such as issue in swallowing tablets in paediatric as well as geriatric population as well as avoid first pass metabolism and provide quick onset of action as it starts to absorb directly from oral cavity. Ondansetron HCl is used to prevent nausea and vomiting. In case of vomiting as well as in nausea, drug must require to act quickly to treat therapeutic condition of patient in need thereof. Therefore, combining Mouth dissolving technology with Ondansetron HCl as active pharmaceutical ingredient could be potential strategy to provide quick onset of action without swallowing entire tablet. Therefore, aim of the present research work is to fabricate mouth dissolving tablets of Ondansetron HCl using different concentration, i.e. 3%, 5% and 9%w/w, of different water insoluble super-disintegrants, namely Kollidon CL-SF, croscarmellose sodium and sodium starch glycolate. Batch F2 prepared using 6% Kollidon CL-SF with 2.5% sodium saccharine by direct compression method shown better taste masking as well as satisfied all mouth dissolving tablet criteria’s. Thus, it was concluded that taste masked mouth dissolving tablets of Ondansetron HCl could be successfully formulated by direct compression methods using 6% Kollidon CL-SF as water insoluble super-disintegrant that can effectively provide quick onset of action by eliminating need of administration of entire dosage form.

Time-domain NMR analysis for the determination of water content in pharmaceutical ingredients and wet granules

The application of time-domain NMR (TD-NMR) analysis to quantify water content in pharmaceutical ingredients is demonstrated. The initial phase of the study employed a range of disintegrants with defined amounts of added water (0–30% of the total weight) as samples; the disintegrants included croscarmellose sodium, corn starch, low-substituted hydroxypropyl cellulose, and crospovidone. After acquisition of the T2 relaxation curves of the samples by TD-NMR measurements, these curves were analyzed by partial least squares (PLS) regression. According to the analysis, accurate and reliable PLS models were created that enabled accurate assessment of water content in the samples. A powder blend consisting of acetaminophen (paracetamol) and tablet excipients was also examined. Both a physical mixture of the powder blend and a wet granule prepared with a high-speed granulator were tested as samples in this study. Precise determination of water content in the powder blend was achieved by using the TD-NMR method. The accuracy of water content determination was equivalent to or better than that of the conventional loss on drying method. TD-NMR analysis samples were measured nondestructively and rapidly with low cost; thus, it could be a powerful quantitative method for determining water content in pharmaceuticals.

Investigating the Influence of Excipients on the Stability of Levothyroxine Sodium Pentahydrate.

A range of tablet excipients were evaluated for their influence on the physical form and chemical stability of levothyroxine sodium pentahydrate (LSP; C15H10I4NNaO4·5H2O). LSP-excipient binary powder blends were stored under two conditions: (a) in hermetically sealed containers at 40 °C and (b) at 40 °C/75% RH. By use of synchrotron X-ray diffractometry, the disappearance of LSP could be quantified and the appearance of crystalline levothyroxine (free acid) could be identified. Under hermetically sealed conditions (40 °C) hygroscopic excipients such as povidone induced partial dehydration of LSP to form levothyroxine sodium monohydrate. When stored at 40 °C/75% RH, acidic excipients induced measurable disproportionation of LSP resulting in the formation of levothyroxine (free acid). HPLC analyses of drug-excipient mixtures revealed that lactose monohydrate, microcrystalline cellulose, and croscarmellose sodium caused pronounced chemical decomposition of LSP. On the other hand, magnesium stearate, sodium stearyl fumarate, and alkaline pH modifiers did not affect the physical and chemical stability of the API following storage at 40 °C/75% RH. HPLC, being a solution based technique, revealed chemical decomposition of the API, but the technique was insensitive to physical transformations. Excipient properties such as hygroscopicity and microenvironmental acidity were identified to be critical determinants of both physical and chemical stability of LSP in a drug product. For drugs exhibiting both physical and chemical transformations, simultaneous solid-state and solution based analyses will enable comprehensive stability evaluation.

Formulation and Characterization of Dispersible Tablets of Cefpodoxime Proxetil: A Cephalosporin Antibiotic

The objective was to formulate rapid dispersible tablets of Cefpodoxime Proxetil using various types of superdisintegrants viz., Croscarmellose sodium (CCS), Sodium starch glycolate (SSG) and Crospovidone (CP) in varied concentrations (1-5%). The model drug for current investigation, Cefpodoxime Proxetil, a broad spectrum third generation Cephalosporin antibiotic belongs to BCS class IV. The preformulation studies were accomplished by determining the compatibility of model drug with respective excipients by FTIR studies. These studies, revealed no chemical interaction of excipients with the model drug. The formulation development was achieved in phases comprising of preliminary screening, pre-optimization and optimization studies. The bitter taste of model drug was masked by addition of flavors and sweeteners to make it pleasant for pediatric patients upon oral administration. The formulations (F1-F6) were prepared by direct compression method. The percent released from all formulations showed release of more than 90% of drug within 30 min with drug content of more than 95%. The study showed that formulation containing CCS as superdisintegrants furnished best results. Formulation F5 showed maximum (99.6%) drug release within 30 minutes which is prerequisite for dispersible tablets. It also possessed a rapid release of drug from the formulation. The F5 formulation showed comparative dissolution profile vis-a-vis a commercialized formulation. The study concluded that dispersible tablets of Cefpodoxime Proxetil can be an alternative to conventional dosage form for the treatment of urinary tract infection, skin infection, and upper respiratory tract infections.

Formulation and Evaluation of Dispersible tablets of a Model Anti-Parasitic Drug

The study was aimed to formulate and evaluate dispersible tablets of a model anti-parasitic drug (XXX) with an objective to produce fast dispersion of tablets by reducing the disintegration time using three superdisintegrants like Sodium Starch Glycolate (SSG), Crospovidone (PVP K30) and Croscarmellose sodium (CCS) and also diluents namely MCC and Lactose by changing their concentrations in each formulations. Totally six formulations (F1-F6) were prepared by direct compression method and evaluated for hardness, thickness, weight variation, friability, wetting volume, wetting time, water absorption ratio, uniformity of dispersion, in-vitro disintegration time, Drug content, in-vitro dissolution test and release kinetics study. FTIR studies was carried out to see possible drug excipients interaction. The stability studies were performed as per ICH guidelines. Among the formulations F6 formulation was found to be promising as it showed better results than other five formulations with In-vitro disintegration time, percentage drug release and dispersion time of 16 ± 0.93 seconds, 98.32±0.54% and 66±1.30 seconds respectively. Further the FTIR results revealed that there was no interactionF between drug and excipients. Stability study of formulation showed no significant changes in tablet properties and the drug follows Higuchi release kinetics with Fickian diffusion mechanism.

Novel Extraction Method Using Excipients to Enhance Yield of Genistein and Daidzein in Trifolium pratensis L.

Isoflavones can be found in different chemical forms, but the health beneficial effects mainly appear in their free forms—aglycones. Their yield in red clover (Trifolium pratensis L.) extracts differs due to different extraction and hydrolysis methodologies. The main aim of this study was to obtain the highest yields of daidzein and genistein from red clover blossoms through the various extraction and hydrolysis methods and to increase their quantities using additional excipients. Extracts were obtained by ultrasound-assisted, heat-reflux and maceration methods combining them with acidic, alkaline, and thermal hydrolysis. Using ultrasound-assisted extraction with optimal conditions and heat-reflux method highest yields of isoflavones were obtained in UTE510 (393.23 ± 19.66 µg/g daidzein and 171.57 ± 8.58 µg/g genistein); UTE530 (415.07 ± 20.75 µg/g daidzein and 150.57 ± 7.53 µg/g genistein) and HNE5 (432.30 ± 21.61 µg/g daidzein and 154.50 ± 7.72 µg/g genistein) samples. These conditions were used with excipients: magnesium aluminometasilicate, croscarmellose sodium, sodium carboxymethyl starch and vinylpyrrolidone-vinyl acetate copolymer. This is the first study reporting the ability of the vinylpyrrolidone-vinyl acetate copolymer to promote solubilization and availability of active compounds from a herbal extract, resulting in enhanced isoflavones yield. The results of the present study showing increased solubility and availability provided by the vinylpyrrolidone-vinyl acetate copolymer suggest that this preparation could in principle also reduce variability due to limited water solubility of isoflavones.

Formulation and Optimization of Zolmitriptan Orodispersible Tablets

Zolmitriptan is a selective 5-hydroxytryptamine receptor agonist reported for the acute migraine treatment, having poor water solubility leads to poor bioavailability. In the present study, attempt to improve the bioavailability of zolmitriptan with the help of PVP K-30 using the microwave irradiation method. The zolmitriptan and PVP K- 30 in 1:1 ratio was subjected to microwave irradiation for different times such as 60,80,100,120 seconds at 650 watts. Characterization of solid dispersion was done by drug content, XRD, FTIR, DSC. FTIR analysis demonstrated there are no compatibility issues. XRD studies prove that the solid dispersion was in amorphous form. DSC studies prove that solid dispersion was amorphous based on the intensity of peaks. The prepared dispersion was made into orodispersible tablets by direct compression. The optimization of these formulations was carried out by using 32 factorial designs on Design Expert 10.0 software. In order to examine the effect of independent variables Crospovidone (X1), croscarmellose sodium (X2), and combined effect of independent variables 32 factorial design was selected. In this design, two responses such as disintegration time and % drug release were evaluated, and experimental trials are performed for all 9 formulations. For all formulations, the precompression and post-compression parameters were studied. Based upon the model optimized formulation (C1 and C2) was obtained having the disintegration time (34.4±0.84 and 39.8±0.91) and %drug release (98.7±0.42 and 93.2±0.46) respectively.
 Keywords: Zolmitriptan, Solid dispersion, Microwave irradiation, Crospovidone, Croscarmellose sodium.

Development of Tropisetron Hydrochloride Orodispersible Tablet using Natural Superdisintigrants

The foremost objective of this research was to compare and evaluate natural super disintegrants with synthetic super disintegrants for the preparation of the orodispersible tablet. Tropisetron hydrochloride is widely used as an antiemetic drug, which is a potential drug candidate for developing an orodispersible tablet for quick onset of action. Various formulations were prepared using different concentrations (5%, 7.5%, and 10%) by direct compression method of natural super disintegrants (Banana power and Cassia tora powder) and synthetic super disintegrants (Croscarmellose sodium, Crospovidone, and Sodium starch glycolate). The compatibility studies between the drug and excipients were carried out using FTIR spectroscopy before tablet formulation. The pre-compression parameters were evaluated for additive properties. Standardization of banana powder was done by various parameters like extractive value, ash value, loss on drying, TLC identification test, etc. Post-compression parameters like hardness, weight variation, friability, thickness, the time required for disintegration, wetting time, the release of drug in-vitro, and in-vitro dispersion time of the tablets were evaluated. The disintegration time and in-vitro drug release of optimized formulation (F2) were found to be 4.66±1.15 secs and 99.25±0.15%. The optimized formulation (F2) was subjected to stability studies (40 C& 75 % RH) for one month. The results were shown that natural super disintegrants require less disintegration time as compared to synthetic super disintegrants. Hence present study reveals that the orodispersible tablets prepared using Banana powder and Cassia tora powder is super disintegrants that shown better appearance and rapid disintegration time.

Physico-Chemical Characterization of Rivaroxaban and Compatibility Studies with Its Pharmaceutical Excipients

Physico-chemical compatibility studies were performed to check the effect of different excipients on API and it is the prerequisite in the preformulation studies. The main aim of this research is to study the behavior of the API individually and with the selected pharmaceutical excipients which mainly contribute in the selection of suitable excipients for developing an ideal dosage form. Rivaroxaban is an oral anticoagulant that mainly acts by blocking coagulant factor Xa. Incompatibility studies were performed for rivaroxaban with selected pharmaceutical excipients like HPMC, lactose, magnesium stearate, sodium lauryl sulfate, microcrystalline cellulose, croscarmellose sodium, HPC using the Scanning electron microscopy, X-ray powder diffraction and differential scanning calorimeter. A 1:1 physical mixture of rivaroxaban and selected excipient was analysed using differential scanning calorimeter. Rivaroxaban showed the transition at 231.79 0C with 114.2J/g specific heat of fusion. The transition temperature of rivaroxaban has not changed much when compared with the combination of rivaroxaban with excipients. The 2θ values of the standard drug were compared with the spectrum obtained from the XRD study. This comparison showed that there was no evidence regarding the incompatibility of the drug with excipients. The photomicrographs obtained by SEM did not showed any interaction between rivaroxaban and the excipients, providing visual support for the results.Â