DESIGN, DEVELOPMENT AND EVALUATION OF MOUTH DISSOLVING TABLETS OF TOFACITINIB CITRATE

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.

Exploring the transverse wicking behavior of mechanically robust warp super-elastic woven fabric for tight-fitting garments

The ability of a fabric to wick moisture away from the human body directly determines the moisture management ability of any given textile, and thereby has a great influence on the comfort offered by garments made from that textile. In this paper, the effects of tensile extension and liquid drop height on the transverse wicking behavior of a warp stretch woven fabric were systematically investigated. By virtue of the unique structure of the nylon/spandex air-covered warp yarn, the woven fabric has a denser and tighter surface, which facilitates its warp elastic stretchability beyond 60%. Furthermore, an acceptable cyclic tensile behavior at an extension of 30% was obtained, indicating the superior mechanical robustness of the fabric to a certain extent. The experimental results demonstrated that the transverse wicking performances of the fabric, including the wetting time and liquid spreading area, were dependent on the tensile extensions and the heights between the water droplet and the fabric surface. Specifically, the wetting time increased with an increase of tensile extension or a decrease of liquid drop height. The spreading area of the water droplet increases as a function of the wicking time, and it fits a power relation appropriately. In addition, the water vapor transmission behavior of our fabric during stretch was clarified. Such work is essential to get an in-depth evaluation of the wicking behavior of complex stretchable fabric structures.

Formulation and Evaluation of Ibuprofen Fast Dissolving Tablets Employing Starch Malonate (Modified Starch) as a Superdisintegrant

Aim: The goal of the study was to prepare a superdisintegrant named starch malonate followed by its evaluation for physicochemical properties. Prepared starch malonate was optimized in the preparation of fast dissolving tablets of ibuprofen by using 23 factorial designs. Methods: Compatibility studies like FTIR, TLC and DSC were performed to check any interaction between starch malonate and ibuprofen. Fast dissolving tablets were compressed by direct compression method and subjected to various official tests like hardness, friability, drug content, dissolution etc. Wetting time and water absorption ratio were also performed. At last response surface plot and contour plot was plotted to check the effects of starch malonate, croscarmellose sodium and crospovidone (independent variables) on disintegration time and dissolution efficiency in 5 minutes (dependent variables). Stability studies were also performed to check the stability of prepared fast dissolving tablets of ibuprofen. Results: Results of the studies showed that all the results are within acceptable limits and complying with the criteria of fast dissolving tablets. Drug content was found to be (100±5%), hardness of all tablets were found in between 3.8 -4 kg/cm2, friability was found less than 0.15%. Optimized formulation has showed less wetting time, less disintegration time followed by enhanced drug release. Among all formulation, formulation F2 has shown least disintegration time and enhanced drug release (99.89%) as compared to other formulations. We can conclude that starch malonate can be used as a novel superdisintegrant.

Formulation development and evaluation of Orally Disintegrating Tablets Rizatriptan Benzoate

Formulation research is oriented towards safety, efficacy and quick onset of action of existing drug molecule through novel concepts of drug delivery. Orally disintegrating tablets of Rizatriptan benzoate were prepared by direct compression method to provide faster relief from pain to migraine sufferers. About eleven formulations for the present study were carried out. Croscarmellose sodium, Crospovidone and Sodium starch glycolate (SSG) were used as superdisintegrants, while microcrystalline cellulose was used as diluent. The prepared batches of tablets were evaluated for weight variation, hardness, friability, wetting time, invitro dispersion time, drug content and invitro dissolution studies. The formulation containing combination of Croscarmellose sodium and Sodium starch glycolate showed rapid invitro dispersion time as compared to other formulations. The optimized formulation dispersed in 8 seconds. It also showed a higher water absorption ratio and 99.58% of drug is released within 2 minutes.

Formulation and Evaluation of Mouth Dissolving Tablet of Almotriptan Malate

Mouth dissolving tablet disintegrates and dissolves rapidly in the saliva, within a few seconds without the need of drinking water or chewing. A mouth dissolving tablet usually dissolves in the oral cavity within 15 seconds to 3 minutes. Almotriptan malate is an anti migraine drug with bitter taste and shows hepatic metabolism. In the present work, Mouth dissolving tablets of almotriptan malate were prepared by direct compression method using sodium starch glycolate and croscarmellose sodium as superdisintegrant with a view to enhance patient compliance and to avoid gastric dysmotility which is common with migraine drugs and for fast action of drug. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water-absorption ratio and in-vitro dispersion time. Short-term stability studies on the promising formulation indicated that there are no significant changes in drug content and disintegration time. Keywords: Almotriptan malate, Superdisintegrant, Sodium starch glycolate, Crosscarmellose sodium, Taste masking.

Investigation of the Wetting Process of Glass Fiber with Oligophenylene Sulfide Sulfone

The wettability of reinforcing fillers such as glass and carbon fibers is a significant factor influencing the mechanical properties of the composite. This study focuses on the effect of finishing glass fiber surfaces with different concentrations of oligophenylene sulfide sulfone solution on fiber wettability, which is determined by contact angle and wetting time. The Adam-Schütte method was chosen as a method for determining the contact angle. According to the study results a 1.5% solution of oligophenylene sulfide sulfone in N, N'-dimethylacetamide gives a contact angle of 45°, forming over time a thin film on the fiber surface, which indicates a sufficiently high sizing ability.

QUALITY BY DESIGN (QBD) AS A TOOL FOR THE OPTIMIZATION OF INDOMETHACIN FREEZE-DRIED SUBLINGUAL TABLETS: IN VITRO AND IN VIVO EVALUATION

Objective: This study aims to prepare and optimize indomethacin freeze-dried sublingual tablets (IND-FDST) by utilizing a quality by design (QbD) approach to achieve rapid drug dissolution and simultaneously bypassing the GIT for better patient tolerability. Methods: A screening study was utilized to determine the most significant factors which the quality attributes, namely disintegration time and % friability. Then an optimization study was conducted using a full response surface design to determine the optimized formula by varying the amount of the matrix-forming polymer (gelatin) and super disintegrant (croscarmellose sodium (CCS)). The variables' effect on the % friability, disintegration time, wetting time, and amount of drug release after 10 min (%Q10) was studied. The optimized formula was tested for compatibility, morphology as well as stability studies under accelerated conditions in addition to the in vivo pharmacodynamics in rats. QbD was adopted by utilizing a screening study to identify the significant formulation factors followed by a response surface optimization study to determine the optimized IND-FDST formulation. Results: Optimized IND-FDST comprised of gelatin/CCS combination in a ratio of 1:1 possessed adequate %friability (0.73±0.03%), disintegration time (25.40±1.21 seconds), wetting time (3.49±0.68 seconds), and % Q10 (100.99±5.29%) as well as good stability under accelerated conditions. IND-FDST also showed significant inhibition of edema, tumour necrosis factor-alpha, and interleukin-6 release in vivo compared to the oral market product by 70%, 42%, and 65%, respectively. Conclusion: QbD presents a successful approach in the optimization of a successful IND-FDST formula that showed superior in vivo and in vitro characteristics.

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

Objective: To synthesize, characterize and evaluate starch glycolate as a superdisintegrant in the formulation of Glipizide fast dissolving tablets by employing 23 factorial designs. Methods: Starch glycolate was prepared and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of Glipizide was prepared by employing starch crotonate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design for the evaluation of tablet parameters like disintegration and dissolution efficiency in 5 min. Results: The starch glycolate prepared was found to be fine, free-flowing and amorphous. Starch glycolate exhibited good swelling in water with a swelling index (10%). The study of starch glycolate was shown by fourier transform infrared spectra (FTIR). The drug content (100±5%), hardness (3.5–4 kg/sq. cm), and friability (<0.15%) was been effective with regard to all the formulated fast dissolving tablets employing starch glycolate. The disintegration time of all the formulated tablets was found to be in the range of 13±0.015 to 180±0.014 sec. The optimized formulation F8 had the least disintegration time i.e., 13±0.015 sec. The wetting time of the tablets was found to be in the range of 8±0.015 to 95±0.013 sec. The In vitro wetting time was less (i.e., 8±0.015s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 75±0.012 to 150±0.014%. The percent drug dissolved in the optimized formulation F8 was found to be 99.95% in 5 min. Conclusion: Starch glycolate was an efficient superdisintegrant for fast-dissolving tablets. The disintegration and dissolution efficiency of the fast dissolving tablets of glipizide was good and depended on the concentration of superdisintegrant employed i.e., starch glycolate, sodium starch glycolate, crospovidone. The formulated fast dissolving tablets of glipizide exhibited good dissolution efficiency in 5 min which can be used for the fast therapeutic action of glipizide.

Development, Formulation and Evaluation of Sustain Release Dispersible Tablet of Ornidazole

This Present research with dispersible tablet can compromise the efficacy and safety of the treatment to children’s and geriatric patients with masking the bitter taste of drug and developing its dispersible tablet. The purpose of this research work was to develop Dispersible tablet of Ornidazole by masking the bitter taste. Tablet containing drug and excipients were prepared by direct compression method. Excipients in combinations were incorporated to achieve the aim. Effect of different combinations was studied to optimize the ideal formulation. Drug excipients interaction studies were carried out by FTIR spectral analysis. The tablets were evaluated for their hardness, wetting time, disintegrating time and dissolution parameters. It was concluded that the tablets having the combination of Dried Mucilage (obtained from dried seeds of ocimum bacilicum) and Sodium starch glycolate met all the evaluation parameters and thus selected as the optimized formulation. Optimized formulation was undergone for stability testing as a parameter to predict the shelf life as per ICH guidelines and proved for its adequate shelf life.

Application of optimization tools for preparation of nebivolol liquid solid composite compressed tablet

The purpose of this study is to make Nebivolol more efficient by converting it into a liquid solid composite compressed tablet. Blending cum sonication process was used to create the liquid solid composite. By altering the independent variables such as vehicle, carrier, and superdisintegrants, nearly 12 compositions were created in a 23 factorial design with four centre points. The influence on response, such as disintegration time in seconds and wetting time in seconds, was then determined. In addition, the liquid solid composite was compacted into a tablet and its percent invitro drug release was assessed. Based on disintegration time and wetting time, the optimal solid liquid compacts sustained release tablet formulation was identified to be LSC6 , which may be ideal candidates for boosting the solubility and dissolution rate of less soluble medications like Nebivolol.