Developing and evaluation of orodispersible tablets containing caffeine

Starting from the premise that a reduced number of active pharmaceutical ingredients (APIs) are used to treat hypotension, the aim of this study consisted of developing new formulations of caffeine-orodispersible tablets (CAFODTs). The formulation variables were the type of disintegrant and its concentration. The CAF-ODTs were prepared by direct compression, (CAF1, CAF2 and, CAF3) each of them containing 100 mg of CAF / tablet. The proposed formulations were analyzed from a pharmacotechnical point of view. For the formulations developed the tablets’ physical appearance, resistance to crushing, friability, disintegration behaviour, and the in vitro caffeine release were evaluated. White tablets, with a resistance to crushing decreasing in the following order CAF1 > CAF2 > CAF3 were obtained. The friability test showed that all the formulations are respecting the in-force European Pharmacopoeia (Ph. Eur. 10) requirements with values less than 1 %. The disintegration time for all three formulations was less than 180 seconds, the smallest time being registered in the case of CAF2 formulation, where Sodium Starch Glycolate (SSG) was used as a disintegrant (24-30 s, as a result of the different methods used. Through the in vitro releasing study, it was observed that over 99.9 % caffeine was released from all three analyzed formulations. By investigating the amount of caffeine released after 1 minute, it can be noticed that the largest amount released was recorded in CAF2 formulations, where SSG was used as a disintegrant. Compared to CAF2, the amount of CAF released was reduced to half, after the first five minutes for CAF1 formulation, where sodium croscarmellose was used, and ten times lower in the case of CAF3 where no disintegrant was used. Based on the results obtained we can conclude that all three formulations are respecting the pharmacotechnical in-force officinal requirements. The presence of SSG in the CAF2 formulation led to obtaining tablets with a reduced disintegration time in comparison to the other two formulations proposed in this study.

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FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS (ODTS) OF DICLOFENAC SODIUM BY USING SUPERDISINTEGRANT FROM NATURAL ORIGIN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i6.33480 ◽

2019 ◽

pp. 190-197

Author(s):

SATYAJITH PANDA ◽

NODAGALA HEMALATHA ◽

PANCHAGNULA UDAYA SHANKAR ◽

SRINIVASA RAO BARATAM

Keyword(s):

Cajanus Cajan ◽

Diclofenac Sodium ◽

Pigeon Pea ◽

Disintegration Time ◽

In Vitro Drug Release ◽

Sodium Starch Glycolate ◽

Orodispersible Tablets ◽

Pregelatinized Starch ◽

The Stability

Objective: In this study, a polysaccharide isolated from the seeds of Cajanus cajan (pigeon pea) was investigated as a super disintegrant in the orodispersible tablets of diclofenac sodium. Methods: Diclofenac sodium tablets were prepared separately using different concentrations (5%, 7.5%, 10%, and 15% w/w) of isolated Cajanus cajan seed polysaccharide (natural) and sodium starch glycolate (synthetic) as super disintegrant by the direct compression method. Evaluation of tablets was done for various pre-and post-compression parameters. The stability studies were performed on optimized formulation F5. The disintegration time and in vitro drug release of the formulation F5 was compared with pregelatinized starch and synthetic super disintegrant (sodium starch glycolate). Results: The drug-excipient interactions were characterized by Fourier transform infrared studies. The Optimized formulation F5 containing 15% polysaccharide showed wetting time of 118.7 seconds with 105.3 seconds of disintegration time and 95.61% dissolved in 3 min. Conclusion: The present work revealed that Cajanus cajan seed polysaccharide has a good disintegrating agent in the formulation of orodispersible tablets.

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Formulation and in vitro evaluation of orodispersible tablets of fexofenadine hydrochloride

Tropical Journal of Pharmaceutical Research ◽

10.4314/tjpr.v19i5.2 ◽

2020 ◽

Vol 19 (5) ◽

pp. 919-925

Author(s):

Durgaramani Sivadasan ◽

Muhammad Hadi Sultan ◽

Osama Madkhali ◽

Shamama Javed ◽

Aamena Jabeen

Keyword(s):

Guar Gum ◽

Polymer Concentration ◽

In Vitro Release ◽

Direct Compression ◽

Compression Technique ◽

Disintegration Time ◽

Weight Fluctuation ◽

Orodispersible Tablets ◽

Croscarmellose Sodium

Purpose: To develop orodispersible tablets (ODTs) of fexofenadine hydrochloride using three different superdisintegrants in various ratios and to compare their disintegration properties.Methods: Direct compression technique was used for the preparation of ODTs. Mannitol and Avicel CE-15 (microcrystalline cellulose and guar gum) were used as direct compression diluents. The disintegration time of tablets using each polymer (superdisintegrant) was evaluated as well as othertablet properties including weight fluctuation, hardness, friability, wetting time and water absorption ratio.Results: Satisfactory values were obtained for all the evaluated parameters. As the polymer concentration increased, there was a decrease in disintegration time. A comparison of the three different polymers used revealed that CCM3 formulated with 12 % croscarmellose sodium and 14.66 % lactose had the least disintegration time of 32.33 ± 3.23 s. In vitro release studies showed that the maximum drug release of 94.38 ± 0.12 % in 25 min was obtained for ODT tablets containing croscarmellose sodium (CCM3).Conclusion: The orodispersible tablets had quick disintegrating property which was achieved using superdisintegrants. Thus, superdisintegrants improve the disintegration efficiency of orodispersible fexofenadine tablets at low concentrations, when compared to traditional disintegrants. Keywords: Croscarmellose sodium, Direct compression, Fexofenadine, Orodispersible tablets

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Understanding the formulation variables of orodispersible tablets containing simvastatin solid dispersion using Box-Behnken design

Drugs and Therapy Studies ◽

10.4081/dts.2012.e7 ◽

2012 ◽

Vol 2 (1) ◽

pp. 7

Author(s):

Ahmed Abd Elbary ◽

Howida K. Ibrahim ◽

Balquees S. Hazaa

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Magnesium Stearate ◽

Stability Study ◽

Disintegration Time ◽

Box Behnken Design ◽

Orodispersible Tablets ◽

Formulation Variables

Simvastatin is a well established oral antihypercholesterolemic agent. This study aimed to formulate simvastatin as orodispersible tablets. The drug was incorporated as a solid dispersion using Pluronic® F68 as carrier. Croscarmellose Na was used as superdisintegrant, microcrystalline cellulose as filler, PVP K-30 as binder and 1:1 magnesium stearate/talc mixture as lubricant. Box- Behnken design was adapted to explore the main and interaction effects of three independent formulation variables on the prepared tablets, namely superdisintegrant concentration (X1), lubricant mixture concentration (X2), and binder concentration (X3). A total of 13 tablet formulations were fabricated in addition, to two replicates of the center point to assess variability and experimental error. The selected dependant variables were the<em> in vitro</em> and <em>in vivo</em> disintegration times, dissolution rate at 4 min, and dissolution efficiency after 30 min. Wetting time, drug content, hardness and friability were also evaluated. Tablet formula, composing of 12% superdisintegrant, 2% lubricant mixture and 3% binder, showed the highest dissolution rate with an acceptable disintegration time (43 sec), hardness, and friability and was chosen as the best formula. An accelerated stability study was conducted for 6 months at 40°C/75% RH. Results showed no significant changes in any of the tested parameters.

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

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i5.41940 ◽

2021 ◽

pp. 244-251

Author(s):

A. HARI OM PRAKASH RAO ◽

R. SANTOSH KUMAR ◽

SHAMBHAVI KANDUKURI ◽

M. RAMYA

Keyword(s):

Direct Compression ◽

Factorial Designs ◽

Therapeutic Action ◽

Compression Method ◽

Disintegration Time ◽

23 Factorial Design ◽

Sodium Starch Glycolate ◽

Wetting Time ◽

Dissolution Efficiency

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.

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Formulation and evaluation of oral disintegrating tablets of furosemide

World Journal of Current Medical and Pharmaceutical Research ◽

10.37022/wjcmpr.v3i6.200 ◽

2021 ◽

pp. 149-156

Author(s):

Manish Khadka ◽

Dharma Prasad Khanal ◽

Deepti Piya Baniya ◽

Prakash Karki ◽

Saurav Shrestha

Keyword(s):

In Vitro Dissolution ◽

Direct Compression ◽

Compression Method ◽

Drug Molecule ◽

Disintegration Time ◽

Sodium Starch Glycolate ◽

Ftir Studies ◽

Orally Disintegrating Tablets ◽

Dissolution Properties

Orally disintegrating tablets of Furosemide were prepared, evaluated and the comparison of the action of different concentrations of disintegrants on disintegration and dissolution of the tablets were studied. Direct compression method was used to prepare the orally disintegrating tablets containing 20 mg of Furosemide. The formulation was conducted using different concentrations of crospovidone, croscarmellose and sodium starch glycolate as superdisintegrants and their interactions with Furosemide were also evaluated using FTIR. FTIR studies using the drug and its mixtures with the excipients showed that the peaks correlate with one another which signify that there is no interaction between the drug molecule and the excipients used. The obtained results revealed that the disintegration time of ODTs were between 9 to 59 seconds. The percentage drug content of tablets in all the formulations was found between 91.51% to 106.69%, which complies with the limits established in pharmacopoeia. The in-vitro dissolution studies show maximum release of 89.47% in formulation F3 and minimum of 77.64% in formulation F12. Higher concentration of crospovidone and croscarmellose in formulations F3 and F6 showed better dissolution properties than SSG. So by varying the concentrations of superdisintegrants, oral disintegrating tablets can be formulated.

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PREPARATION & EVALUATION OF ORODISPERSIBLE TABLET CONTAINING ASPIRIN BY SUBLIMATION METHOD

INDIAN DRUGS ◽

10.53879/id.52.12.10465 ◽

2015 ◽

Vol 52 (12) ◽

pp. 60-62

Author(s):

P. Jain ◽

◽

A Mishra ◽

A. Pathak

Keyword(s):

Content Uniformity ◽

Disintegration Time ◽

Sodium Starch Glycolate ◽

Orodispersible Tablets ◽

Weight Variation ◽

Orally Disintegrating Tablets ◽

Orodispersible Tablet ◽

Sublimation Method ◽

Dispersing Ability

Orodispersible tablets are uncoated tablets which when taken into the mouth, get easily dispersed within 3 min before swallowing. they are also known as orally disintegrating tablets, mouth-dissolving tablets, rapid dissolving tablets fast-disintegrating tablets, fast-dissolving tablets. In this work, sublimation process was used to prepare orodispersible tablets of aspirin by formulating various batches using different concentration of sodium starch glycolate, camphor and cross povidone. An effort was made by using two modes, first, to increase water uptake for the fast dispersion by creating pores by sublimation methods in tablets and second, use of super disintegrantes like sodium starch glycolate to minimise disintegration time and promote fast dispersing ability. Prepared formulations were evaluated for weight variation, content uniformity, friability, hardness, wetting time, disintegration time, in vitro drug release and interaction study by differential scanning calorimetery. The best formulation was selected on the basis of evaluation results.

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Formulation, Characterization and In-vitro Evaluation of Cetrizine HCL Oral Disintegrating Tablets

Asian Journal of Pharmaceutical Research and Development ◽

10.22270/ajprd.v7i5.563 ◽

1970 ◽

Vol 7 (5) ◽

pp. 19-24

Author(s):

HARITHA PASUPULATI ◽

Y PHALGUNA ◽

SANDHYA RUDRA

Keyword(s):

Bulk Density ◽

Direct Compression ◽

Compression Method ◽

Disintegration Time ◽

Sodium Starch Glycolate ◽

Weight Variation ◽

Wetting Time ◽

Croscarmellose Sodium ◽

In Vitro Disintegration

The main objective of this work is to formulate and evaluate Cetirizine HCl MFDT’s using different concentrations of superdisintegrants like croscarmellose sodium (CCS), sodium starch glycolate (SSG) and their combinations in different ratios. The in vitro disintegration time of Cetrizine Hcl prepared by direct compression method by super disintegrates were found to be in the range of 18 to 11sec fulfilling the official requirements. The bulk density and tapped bulk density for the entire formulation blend varied from 0.508 gm/cc to 0.5438 gm/cc and 0.5941 to 0.6408 respectively. The friability was found in all designed formulations in the range 0.42 to 0.74% to be well within the approved range (<1%). The weight variation was found in all designed formulation in the range 97 to 102 mg. The wetting time were found to be in the range of 11 to 18sec. Water absorption ratio for all the formulations found in the range 11 to 16%.combination of sodium starch glycolate and cross carmellose sodium (6% of 25%-ssg&75%ccs)) promotes dissolution rate of drug release when compared to formulation of SSG & CCS alone. It may be due to capillary and wicking mechanism of SSG & CCS. Keywords:

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Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00824 ◽

2021 ◽

pp. 4736-4742

Author(s):

Sarika S. Malode ◽

Milind P. Wagh

Keyword(s):

Overactive Bladder ◽

Bitter Taste ◽

In Vitro Release ◽

In Vitro Dissolution ◽

Dissolution Time ◽

Disintegration Time ◽

Orodispersible Tablets ◽

Weight Variation

The objective of present work was to develop taste masked orodispersible tablets of mirabegron. Mirabegron is beta 3 adrenoceptor agonist used to treat overactive bladder. Overactive bladder (OAB) is defined as a symptom syndrome showing feeling of urgency to urinate, typically accompanied by frequent daytime and nocturnal urination, in the absence of proven infection or other obvious pathology. Over active bladders are generally common in geriatrics. Moreover, this drug has a very strong bitter taste. Frequent dosing requires frequent water intake, which further aggregates the condition of over active bladder and bitter taste of drug affects patient compliance. Hence a need arises to mask the bitter taste for development of an ODT which does not require consuming water with every dosage. In this work, the bitter taste of mirabegron was masked by forming a complex with an ion exchange resin tulsion 344. The drug resin complexation process was optimized for resin activation, drug: resin ratio, soaking time and stirring time. In –vitro release studies revealed complete drug elution from the complex within 10 minutes in pH 1.2 buffer. The taste-masked complex was then formulated into palatable orodispersible tablets using a direct compression approach by use of superdisintegrants to achieve a rapid disintegration. The tablets were evaluated for weight variation, hardness, friability, drug content, wetting time, In- vivo disintegration time and in-vitro dissolution time.

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FORMULATION AND EVALUATION OF ORAL FAST DISINTEGRATING TABLET OF IBUPROFEN USING TWO SUPER DISINTEGRANTS

International Journal of Current Pharmaceutical Research ◽

10.22159/20966 ◽

2017 ◽

Vol 9 (4) ◽

pp. 92

Author(s):

Hrishav Das Purkayastha ◽

Bipul Nath

Keyword(s):

Drug Release ◽

Magnesium Stearate ◽

Direct Compression ◽

Compression Method ◽

Disintegration Time ◽

Orally Disintegrating Tablet ◽

Rapid Release ◽

Weight Variation ◽

Fast Disintegrating Tablet

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant.

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Formulation and evaluation of taste masked oral disintegrating tablets of lornoxicam

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v11i5.5124 ◽

2021 ◽

Vol 11 (5) ◽

pp. 115-120

Author(s):

Kritika Rai ◽

Vivek Jain ◽

Sunil Kumar Jain ◽

Pushpendra Kumar Khangar

Keyword(s):

Cation Exchange Resin ◽

The Elderly ◽

In Vitro Dissolution ◽

Taste Masking ◽

Direct Compression ◽

Compression Technique ◽

Disintegration Time ◽

Weight Variation ◽

Croscarmellose Sodium

Orally disintegrating tablets (ODT) disintegrate quickly with saliva when administered into the oral cavity and taken without water or chewed. ODT are easy to take for children and the elderly, who may experience difficultly in taking ordinary oral preparations such as tablets, capsules, and powders. The ODT threes substantial benefits for the patient (or elder) who cannot swallow (Dysphagia), or who is not permitted water intake due to disease. The reason of the current research was to prepare taste masking oral disintegrating tablets of poorly soluble lornoxicam (LXM) by direct compression technique using Kyron T-114 (cation exchange resin) as a taste masking agent. With in various ratios the Drug-resin of 1:4 was established to present best taste masking. The superdisintegrants used in formulation are croscarmellose sodium and cross povidone. Among these croscarmellose sodium demonstrated superior drug release. The tablets were evaluated for friability, weight variation, wetting time, hardness, disintegration time and uniformity of content. Optimized formulations were evaluated for in vitro dissolution test. Amongst all the formulations F-6 was found to be most successful tablets prepared by this technique had disintegration time of 30sec and % CDR 94.78 within 30min. Hence, this advance can be utilized for taste masking of bitter pharmaceutical ingredients leading to superior patient compliance. Keywords: Oral disintegration tablets, Lornoxicam, Kyron T-114, Superdisintegrants, Direct Compression.

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