scholarly journals DEVELOPMENT AND OPTIMIZATION OF ORODISPERSIBLE TABLETS OF CARVEDILOL BY COMBINATION OF SUPER-DISINTEGRANTS ADDITION AND SUBLIMATION TECHNIQUES

2017 ◽  
Vol 9 (7) ◽  
pp. 155
Author(s):  
Vijayanand P. ◽  
Sridevi P. ◽  
Bhagavan Raju M.
Keyword(s):  
Research Work ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Drug Sample ◽  
Croscarmellose Sodium ◽  
Model Drug ◽  
Hypertensive Drug ◽  
Dysphagic Patients

Objective: Objective of the present research work was to prepare orodispersible tablets of carvedilol (CDL) for dysphagic patients.Methods: Carvedilol, an anti-hypertensive drug, was chosen as a model drug in this study. Orodispersible tablets of carvedilol were prepared using different super-disintegrating agents such as crospovidone, croscarmellose sodium and sodium starch glycolate at different concentrations. The best formulation was selected based on disintegration and dissolution profile that was further taken for sublimation studies using camphor, menthol and thymol. Drug-excipients interaction studies were carried out by fourier transform infra-red (FTIR) spectrophotometer with pure drug sample and optimized formulation.Results: The orodispersible tablet formulation having 4% croscarmellose sodium disintegrated in 92 sec. Hence this formulation was considered best formulation and taken further for sublimation studies. A formulation containing 10% w/w of menthol showed disintegration time of 16 sec with more than 96.64% drug release within 15 min. Menthol leaves the porous structure as it sublimates from the tablet. This might have contributed to the decrease in disintegration time. Hence, this formulation was considered optimized.Conclusion: From this study, it can be concluded that orodispersible tablets of carvedilol may prove to be more efficacious in the treatment of hypertension particularly in dysphagic patients.

Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative

2020 ◽  
Vol 18 (5) ◽  
pp. 342-353
Author(s):  
José Lourenço de Freitas Neto ◽  
Ilka do Nascimento Gomes Barbosa ◽  
Camila Gomes de Melo ◽  
Matheus Alves Ângelos ◽  
Larissa Morgana dos Santos Mendes ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Aqueous Solubility ◽  
Dissolution Profile ◽  
Multicomponent Systems ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Immunodeficiency Syndrome

Background: Efavirenz is the most used medication in the treatment of Acquired Immunodeficiency Syndrome (AIDS). The limited number of pediatric antiretroviral formulations approved by regulatory agencies is the most significant obstacle to adequate and efficient pharmacotherapy for this group of patients. The efavirenz has excellent therapeutic potential, but has low aqueous solubility/bioavailability. Methods: To minimize these limitations, multicomponent systems with β-cyclodextrin and polyvinylpyrrolidone K-30 were obtained. Due to the limited number of pediatric antiretroviral formulations, the development of a pediatric orodispersible tablet is an alternative that is thought easy to administer, since it disintegrates rapidly in the oral cavity. The multicomponent systems were obtained by the method of kneading and characterized by solubility test, X-ray diffraction, differential scanning calorimetry and infrared absorption spectroscopy by Fourier transform. The orodispersible tablets were prepared by direct compression. The quality control of hardness, friability, disintegration, and dissolution was performed. The influence of the components of the formulation on the characteristics of the tablets was evaluated through a 22 factorial design added with three central points, to compare the effect of the dependent variables on the responses. Results: An increase in drug solubility was observed, with a decrease in crystallinity. Besides that, an excellent dissolution profile presented with more than 83% of the drug's content dissolved in less than 15 minutes. Satisfactory disintegration time and friability were observed. Conclusion: It was observed that reduced concentrations of mannitol decreased the hardness and disintegration time of the formulations. The orodispersible tablet composed of efavirenz: β- cyclodextrin: polyvinylpyrrolidone, favors greater absorption and bioavailability. It has several advantages for pediatric patients, as the dosage form disintegrates quickly in the mouth and does not require water for administration, thereby improving patient compliance with the treatment.

scholarly journals Research Article. Kinetics and Mechanism of Drug Release from Loratadine Orodispersible Tablets Developed without Lactose

2017 ◽  
Vol 63 (1) ◽  
pp. 23-26
Author(s):  
Adriana Ciurba ◽  
Emőke Rédai ◽  
Ioana Pop ◽  
Paula Antonoaea ◽  
Nicoleta Todoran
Keyword(s):  
Zero Order ◽  
Order Kinetic ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Research Article ◽  
Orodispersible Tablets ◽  
Orally Disintegrating Tablets ◽  
Dissolution Properties ◽  
Gelatinized Starch ◽  
Croscarmellose Sodium

Abstract Objective: The aim of this study is to develop lactose-free orodispersible tablets with loratadine for patients with lactose intolerance. Materials and methods: Seven compositions (F1-F7) of 10 mg loratadine were prepared in form of orally disintegrating tablets, by direct compression, using croscarmellose sodium and pre-gelatinized starch in various concentrations as superdisintegrants, diluted with microcrystalline cellulose and combined with mannitol and maltodextrin as binder agents. The tablets had been studied in terms of their pharmacotechnical characteristics, by determining: the weight uniformity of the tablets, their friability, breaking strength and disintegration time, drug content and the dissolution profile of loratadine. The statistical analyses were performed with GraphPad Prism Software Inc. As dependent variables, both the hardness of the tablets and their disintegration ability differ between batches due to their compositional differences (as independent variables). DDSolver were used for modeling the kinetic of the dissolution processes by fitting the dissolution profiles with time-dependent equations (Zero-order, First-order, Higuchi, Korsmeyer-Peppas, Peppas-Sahlin). Results: All proposed formulas shows rapid disintegration, in less than 15 seconds, and the dissolution loratadine spans a period of about 10 minutes. Akaike index as well as R2 adjusted parameter have demonstrated that the studied dissolution profiles are the best fitted by Zero-order kinetic. Conclusion: In conclusion, association of croscarmellose sodium (7.5%) with pre-gelatinized starch (6%) as superdisintegrants and mannitol as the binder agent (35%), positively influences the dissolution properties of loratadine from orally fast dispersible tablets.

scholarly journals Formulation and Evaluation of Orodispersible Tablet of Fluvastatin Sodium

2021 ◽  
Vol 11 (1) ◽  
pp. 42-47
Author(s):  
Pooja Kanathe ◽  
Ruchi Jain ◽  
Nilesh Jain ◽  
Surendra Kumar Jain
Keyword(s):  
Diffusion Mechanism ◽  
Research Work ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
The Matrix

The purpose of this research work is to formulate and evaluate the Orodispersible tablet of Fluvastatin Sodium to enhance the bioavailability and effectiveness of the drug. The objectives of the drug work were to formulate and evaluate Orodispersible tablets of Fluvastatin Sodium, having adequate mechanical strength, rapid disintegration, and fast action. Precompression parameters like angle of repose, bulk density, tapped density, compressibility index & post-compression parameters like wetting time, water absorption ratio, in-vitro disintegration, and in-vitro dispersion time were studied. The hardness, friability, and drug content of all the formulations were found to be within the limits. The best formulation PK09 has shown good disintegration time, dissolution time, and dispersion time. The optimized formulation of batch PK9 gave the best in-vitro release of 99.60% in 3min in phosphate buffer pH 6.8. The release of the drug followed the matrix diffusion mechanism as compared to the commercial formulation. Formulation PK9 gives quick disintegration and better drug release. Hence it can be concluded that the formulation of PK9 is stable and effective for quick action and it is an alternative to the conventional tablets. Keywords:  Orodispersible Tablets, Fluvastatin Sodium, Fast dissolving/disintegrating tablets, GIT, bioavailability, first-pass metabolism, superdisintegrants

scholarly journals Formulation and evaluation of orodispersible tablet of ivabradine hydrochloride

2017 ◽  
Vol 4 (3) ◽  
pp. 162
Author(s):  
D. B. Patel ◽  
K. J. Patel ◽  
P. D. Bharadia
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Dissolution Behaviour ◽  
Wetting Time ◽  
The Difference ◽  
Selection Of

Objective: The objective of present research work was to develop formulation of orodispersible tablets of Ivabradine HCl and evaluate it for different evaluation parameters.Methods: The tablets were prepared by direct compression method. The formulation of the tablets were evaluated before compression for characterization of flow properties and after compression for different parameters of orodispersible tablet formulation.Results: Ivabradine hydrochloride orodispersible tablets were developed with considerable increase in drug release as compared to marketed formulations; nine formulations were developed and studied. The difference in drug release values was found to be 100.88 ± 0.10 respectively. The drug was characterized according to different compendial methods, on the basis of identification by HPLC, pH, organoleptic properties and other tests. Parameters evaluated were within prescribed limits and indicated good free flowing properties. The F6 batch with disintegration time 21 ± 3.0 and dissolution 99.29% was selected as optimized formulation. This was compared with conventional marketed formulation and was found superior. Batch F6 was also subjected to stability studies for two months and was tested for its hardness, wetting time, disintegration time, drug contents and dissolution behaviour monthly.Conclusions: By appropriate selection of excipients, it was possible to develop orodispersible tablets of Ivabradine HCl.

The Effect of Different Superdisintegrants and their Concentrations on the Dissolution of Topiramate Immediate Release Tablets

2009 ◽  
Vol 2 (2) ◽  
pp. 531-5366
Author(s):  
V A. Vamshi Priya ◽  
G. Chandra Sekhara Rao ◽  
D. Srinivas Reddy ◽  
V. Prabhakar Reddy
Keyword(s):  
Immediate Release ◽  
Drug Dissolution ◽  
Dissolution Profile ◽  
Dissolution Medium ◽  
Lactose Monohydrate ◽  
Sodium Starch Glycolate ◽  
Tablet Disintegration ◽  
Croscarmellose Sodium ◽  
Model Drug ◽  
Usp Apparatus

The purpose of this study was to investigate the efficiency of superdisintegrants: sodium starch glycolate, croscarmellose sodium and crospovidone in promoting tablet disintegration and drug dissolution of Topiramate immediate release tablets. The efficiency of superdisintegrants was tested, by considering four concentrations, viz., like 2%, 3%, 4% and 5% in the formulations. The dissolution was carried out in USP apparatus II at 50 rpm with distilled water as a dissolution medium. The dissolution rate of the model drug topiramate was found highly dependent on the tablet disintegration, on the particle size of the superdisintegrant, on the solubility of the drug and also on the type of superdisintegrant in the dissolution medium. There was no effect of the diluent (Lactose monohydrate) on the disintegration of different concentrations of superdisintegrants. These results suggest that, as determined by the f2 metric (similarity factor), the dissolution profile of the formulation containing 4% sodium starch glycolate and lactose monohydrate as a diluent was similar to that of a marketed product.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF FAST DISSOLVING TABLET OF VERAPAMIL HYDROCHLORIDE

2018 ◽  
Vol 10 (10) ◽  
pp. 93 ◽  
Author(s):  
Dattatraya M. Shinkar ◽  
Pooja S. Aher ◽  
Parag D. Kothawade ◽  
Avish D. Maru
Keyword(s):  
Drug Release ◽  
Phosphate Buffer ◽  
Research Work ◽  
Time Interval ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Verapamil Hydrochloride ◽  
Sodium Starch Glycolate ◽  
Croscarmellose Sodium

Objective: The main objective of this research work was to formulate and evaluate fast dissolving tablet of verapamil hydrochloride for the treatment of hypertension.Methods: In this study, fast dissolving tablet were prepared by wet granulation method by using croscarmellose sodium and sodium starch glycolate as superdisintegrants in the concentration of 2%, 4%, and 6%. Polyvinyl pyrollidone K30 is used as a binder. The designed tablets were subjected to various assessment parameters like friability test, hardness test, disintegration test, wetting time, in vitro drug release and drug content.Results: All the prepared formulations were subjected to various assessment parameters, and the findings obtain within the prescribed limit. The calibration curve of pure drug using various solvents like distilled water, phosphate buffer pH 6.8 was plotted. F1-F9 containing croscarmellose sodium and sodium starch glycolate in various concentration demonstrate the minimum disintegration time. Among all these formulations F8 shows disintegration time upto 19±0.06 seconds due to the high concentration of superdisintegrants. In vitro drug release was tested in phosphate buffer pH 6.8 at a time interval of 0, 1, 3,6,9,12,15 min. The F8 shows drug release 98.5±0.567%. Accelerated stability study of optimized formulation (F8) up to 2 mo showed there was no change in disintegration time and percentage drug release.Conclusion: The results obtained in the research work clearly showed a promising potential of fast dissolving tablets containing a specific ratio of crosscarmellose sodium and sodium starch glycolate as superdisintegrants for the effective treatment of hypertension. 

scholarly journals Formulation and Optimization of Zolmitriptan Orodispersible Tablets

2021 ◽  
Vol 11 (3) ◽  
pp. 50-57
Author(s):  
T.V. Hari Hara Nadh ◽  
P. Sivaram Kumar ◽  
M. Venkata Ramana ◽  
N. Rama Rao
Keyword(s):  
Drug Release ◽  
Microwave Irradiation ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Migraine Treatment ◽  
Disintegration Time ◽  
Independent Variables ◽  
Dsc Studies ◽  
Orodispersible Tablets ◽  
Croscarmellose Sodium

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.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF ORO-DISPERSIBLE TABLETS OF METFORMIN HYDROCHLORIDE USING CAJANUS CAJAN STARCH AS A NATURAL SUPERDISINTEGRANT

2022 ◽  
pp. 139-147
Author(s):  
SONIA DHIMAN ◽  
RITCHU BABBAR ◽  
THAKUR GURJEET SINGH ◽  
SHIVANGI ANAND ◽  
ASHI MANNAN ◽  
...  
Keyword(s):  
Cajanus Cajan ◽  
Research Work ◽  
Pigeon Pea ◽  
Granular Structure ◽  
Metformin Hydrochloride ◽  
Compression Process ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Dispersible Tablets

Objective: The aim of the research work was to explore the use of Cajanus cajan (Pigeon pea) polysaccharide as a superdisintegrant. The novel superdisintegrant has been evaluated for its action by incorporating it into orodispersible tablets of Metformin Hydrochloride. Methods: Cajanus cajan starch was extracted from its seeds and superdisintegrant was developed by microwave modification of the extract. Various characterization tests such as gelatinization temperature, water absorption index, pH, and viscosity were used to identify the microwave-modified polysaccharide. The orodispersible tablets were made using a direct compression process employing varying concentrations of modified Cajanus cajan starch. Prepared tablets were tested for several pre and post-compression parameters and compared with a well-established synthetic superdisintegrant, sodium starch glycolate. The stability studies were conducted on an optimized formulation. Results: Fourier transform infrared spectroscopy study showed that the drug had no interactions with the microwave-modified Cajanus cajan starch. SEM confirmed that Cajanus cajan starch granules exhibited intact granular structure in oval shapes and smooth surfaces. After microwave modification, the Cajanus cajan starch component lost its granular structure, which further led to the generation of surface pores and internal channels, causing overall swelling responsible for superdisintegrant activity. The optimized formulation (ODF5) containing 15 % modified Cajanus cajan starch performed better in terms of wetting time (22.21 s), disintegration time (53.3 s), and in vitro drug release (92%), as compared to formulation prepared by synthetic superdisintegrant (ODF1). Conclusion: The present investigation concluded that modified Cajanus cajan starch has good potential as a superdisintegrant for formulating oro-dispersible tablets. Furthermore, modified Cajanus cajan starch is inexpensive, non-toxic and compatible in comparison with available synthetic superdisintegrants.

scholarly journals A Comparative Study on In-vitro Quality Control Parameters of Different Brands of Loratadine Tablets Commercially Available in Bangladesh

2021 ◽  
pp. 50-58
Author(s):  
Rosy Fatema ◽  
Sumaiya Khan ◽  
A. S. M. Roknuzzaman ◽  
Ramisa Anjum ◽  
Nishat Jahan
Keyword(s):  
Research Work ◽  
Drug Market ◽  
Quality Standard ◽  
In Vitro Dissolution ◽  
Active Principle ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Weight Variation ◽  
Local Companies

Loratadine, a second generation H1-receptor antagonist, works by blocking the action of histamine and is widely prescribed for itching, runny nose, watery eyes, and sneezing from "hay fever" and other allergic conditions. To ensure quality the main requirements for a medicinal product are safety, potency, efficacy and stability. This research work aimed to compare and assess the quality levels of different local brands of loratadine tablets available in the drug market of Bangladesh. Six different brands of loratadine 10 mg tablet manufactured by the local companies were used for the analysis. The evaluation was performed through the determination of weight variation, hardness, friability, percent potency, disintegration time, and dissolution profile in accordance with USP-NF specifications. All brands showed acceptable weight variation and % friability. The percent potency for tested samples by UV method ranges from 97.02%-108%, showing none of the brands contains less than 90% of the active principle as per the specification. The result of the physical and chemical studies, such as in-vitro dissolution, disintegration, hardness, etc., has been found to differ but lie within the specified limit. After analyzing the data obtained from the tests, it can be claimed that loratadine 10 mg tablets manufactured and marketed by several local companies in Bangladesh meet the quality standard required to achieve the desired therapeutic outcomes.

scholarly journals Formulation and in vitro evaluation of orodispersible tablets of fexofenadine hydrochloride

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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