The test was performed on CL containing tablets in triplicate. Moreover, Jagdale et al. Todos os comprimidos possuC-am dureza na faixa de 4,0-5,2 kp e a friabilidade inferior a 1%. Pharm. The impact of the use of different disintegrants on the time required for disintegration of the ODTs containing 75 mg CL is displayed in Table IV.
Accessibility Fast dissolving drug delivery systems: a brief overviewInt. CENTER FOR DRUG EVALUATION AND RESEARCH (CDER) . Technol. (DHHS). 0Qo&& The assay of active ingredient (ibuprofen) of the final formulation (F22s), after conducting the related estimations, was determined to be 98.78% 0.05 (mean standard deviation; n = 3) which complied with the acceptable limit of 95.0-105.0% mentioned in the literature (26). Microcrystalline cellulose (Avicel(r) PH101) was purchased from Serva Feinbiochemica (Heidelberg, Germany). This goal can be accomplished predictably and efficiently using the Nanocrystal technology. After mixing the ingredients, formulation flowability was determined on the basis of Carrs index (21) and then formulations were compressed using a tablet press equipped with 14 mm flat punches. All tablets had hardness values in the range 4.0-5.2 kp and friability lower than 1%. ; LACHMAN, L.; SCHWARTZ, J.B. The weight and drug content uniformity of all formulations was within official limits according to BP. In series B formulations, polyethylene glycol 1000 was substituted by polyvinyl pyrrolidone in the intra-granular part of the formulation and magnesium stearate and silicon dioxide were omitted from the extra-granular part due to good flow and non-stickiness to punches and die. ; BADHAN, A.C.; MAHAJAN, H.S. The method used for preparation of series C, D, E and F formulations and physicochemical tests conducted were the same as series B formulations.
(ed.).
Then by adding xylitol to formulation F20, formulation F20a was made. The ultimate ibuprofen ODT formulation selected was formulation F22s, which contained polyvinyl pyrrolidone, ibuprofen and croscarmellose as the intra-granular components and xylitol along with saccharin as the extra-granular components.
Formulations administered via the oral route represent 50-60% of the total pharmaceutical dosage forms in the market (Bandelin, 1989BANDELIN, F.J. Compressed tablets by wet granulation. Pharm. 'rF: h7.
The ability through class-leading ZydisODT technology to deliver fast dissolve formulations of large molecule allergens, viral vaccines, and peptides. 8600 Rockville Pike The use of ODTs could help to reduce the gastrointestinal side effects of ibuprofen, since the tablet is disintegrated within the mouth (13-15). Tablets formulated without superdisintegrants exhibited a disintegration time of about 236 seconds.
Using CCS and CPV as superdisintegrants, when the concentration of the superdisintegrant was increased from 2% to 5%, enhanced tablet disintegration was observed. The flowability of series A formulations, except for F5 formulation, was worse than ibuprofen powder and there was a significant difference between the results obtained (ANOVA, p < 0.05). The granules of this series consisted of polyvinyl pyrrolidone and glucose. IR spectra (Figure 3) of clopidogrel, mannitol and their physical mixture were recorded in order to determine whether there was a chemical interaction between them.
The average values of weight B1 SD were recorded. Stage 4 Sealing Dr. Abdoallah Momajed is also thanked for his assistance in this work. Moreover, the amount of drug that is subjected to first pass metabolism is reduced compared with conventional tablets (Biradar, Bhagavati, Kuppasad, 2006BIRADAR, S.S.; BHAGAVATI, S.T. Mouth dissolving tablets : An overview of evaluation techniques. The tablet crushing strength (hardness) was investigated using a hardness tester (Pharma test GmbH, Hainburg, Germany) for samples of 10 compressed tablets for each tablet formula. The authors interpreted these results on the basis of that the fibrous nature of CCS at low concentrations is responsible for its disintegrating action, which results from the wicking of water into tablet matrices. The low mechanical strength of some formulations makes very fragile tablets; hence the companies should develop a special handling and packaging system for these cases. Clopidogrel hydrogen sulphate (named hereafter clopidogrel) was discovered by Sanofi. These results are in agreement with those found by Ferrero et al., who studied the disintegration efficiency of croscarmellose sodium and reported that at high concentrations (> 8%), the disintegration time was found to be longer (Ferrero et al., 1997FERRERO, C.; MUOZ, N.; VELASCO, M.V. O principal objetivo deste trabalho foi preparar e desenvolver ODTs de clopidogrel. Effect of superdisintegrants on dissolution of cationic drugs. Ibuprofen powder was purchased from Biocause Co. (Japan). Mean disintegration time of series F ibuprofen ODT formulations (n = 6). Pharmaceutical dosage forms: tablets. Half of the volunteers reported that the palatability was acceptable while the other half reported good palatability. The intra-granular components of series A, B, C, D, E and F ibuprofen ODT formulations, Physicochemical tests conducted on ibuprofen ODT formulations. To v.3, p.138-145, 2003. Dissol. HPLC was used for the assay of active ingredient after weighting and powdering 20 tablets randomly (26). However, the presence of superdisintegrants in the tablet formulations caused an enhanced initial dissolution rate of CL, especially at the 5% superdisintegrant level. The IR spectrum of clopidogrel is characterised by principal absorption peaks at 3107.16 cm-1 (C-H aromatic), 1752 cm-1 (C=O stretching), and 1178 cm-1 (C-O stretching) (Shailendra, Soukarya, Upender, 2011SHAILENDRA, K.S. Clopidogrel exhibited very slow dissolution rates from the formulas at the higher pH value (no more than 30% was released after 30 minutes), while complete drug dissolution from both formulas was observed after 15 minutes at the lower pH (pH 2.0). ; CHABUKSWAR, A.R. Sharma S, Gupta GD. The aim of this study was the preparation of a novel simple matrix-type ibuprofen ODT formulation, using special polymers, water-soluble excipients, super-disintegrants and quickly soluble granules. In the Flashtab technology microgranules of the taste-masked active drug are used. These granules were made as follows: first of all polyethylene glycol 1000 was melted on a heater, then glucose or sucrose was added at room temperature under the action of a four-propeller mixer set at 50 rpm. The United States Pharmacopeial Convention: Rockville MD, 2011. ; SAKR, A. (FDA).
The first series of formulations (series A) contained polyethylene glycol 1000, glucose or sucrose as the intra-granular part of formulation and ibuprofen, croscarmellose, magnesium stearate and silicone dioxide as the extra-granular part. Different formulations using various ingredients were prepared in 8 series (A-H), accounting for a total number of 45 formulations. However, since ODT formulations should have a lower hardness in order to be disintegrated quickly within the buccal cavity, they would be expected to have a higher friability than conventional tablets and hence need special packaging. The challenges of oral delivery of proteins & peptides well documented and are not limited to: ZydisBio sub-lingual delivery overcomes these challenges: Benefits of ZydisBio for peptide & protein drugs. In these series of formulations, there was a significant difference between the results of flowability, thickness, uniformity of weight, hardness and disintegration time of formulations F20 and F20a (t-test, p < 0.05) and a significant difference between the flowability results of formulations F20 and F20a with formulation F17 (ANOVA, Tukey post-hoc test, p < 0.05).
SURESH, B.; KUMAR, M.; RAMESH, G.; MADHUSUDAN, R. Orodispersible tablets: an overview. Um destes avanC'os C) a formulaC'C#o de comprimidos de desintegraC'C#o oral (ODTs), que se dissolvem instantaneamente, liberando o fC!rmaco, em alguns segundos, sem a necessidade de C!gua. Brazilian Journal of Pharmaceutical Sciences, Text Drugs v.60, n.2, p.347-377, 2000.). DSC scans were performed on the drug, the tested excipients and their corresponding physical mixtures. Selection of superdisintegrant for famotidine rapidly disintegrating tablets. (ed.). BALASUBRAMANIAM, J.; BINDU, K.; RAO, V.U. Development and optimization of dextromethorphan hydrobromide oral disintegrating tablets: effect of formulation and process variables. SHAILENDRA, K.S.
Int. Recent advances in drug delivery systems have aimed to achieve better patient compliance. This phenomenon is due to the lower solubility of CL at higher pH values because of its basic nature (Sahitya et al., 2014SAHITYA, A.; KRISHNAMOORTHY, B.; MUTHUKUMARAN, M.; KISHORE, G. Formulation and evaluation of fast dissolving tablets using solid dispersion of clopidogrel bisulphate.
Effect of superdisintegrants on dissolution of cationic drugs. Furthermore, a lower compaction force is used for manufacturing these tablets, in order to obtain soft and quickly disintegrating tablets. Wow means without water. Preparation and evaluation of mouth dissolving tablets of salbutamol sulphate.
official website and that any information you provide is encrypted (2). The measured tablet weights ranged from 0.295-0.304 g and the average tablet hardness was found to be 4.2-5.2 kp. However, many paediatric and geriatric patients are unwilling to take solid preparations due to a fear of choking or because of difficulty in swallowing (dysphagia).
Iranian Journal of Pharmaceutical Research : IJPR, http://creativecommons.org/licenses/by/3.0/. In other study conducted by Suresh et al., salbutamol sulphate tablets were prepared by wet granulation process using sublimable components (camphor and ammonium bicarbonate). The amount of ibuprofen in each formulation was 100 mg. mentioned that CCS gave a short disintegration time at low concentrations with a sudden rise when the concentration was increased from 4% to 6%.
In this series of formulations, the flowability of formulation F17b was better than formulation F17a and there was a significant difference between the results obtained (t-test, p < 0.05). Rev., v.85, p.28-35, 2001.; Mostafa, Ibrahim, Sakr, 2013MOSTAFA, H.F.; IBRAHIM, M.A. Formulation F22s was found to be acceptable in terms of physicochemical tests conducted, showing quick disintegration within the buccal cavity, appropriate hardness and rather low friability. The FTIR spectra of TNX, KL and their binary systems were recorded using a Perkin Elmer FTIR spectrophotometer (Spectrum BX). Taste of series H ibuprofen ODT formulations (scoring scale: the best = 1 and the worst = 5; n = 10).
Most formulations consisted of intra-granular (quickly soluble granules) and extra-granular parts. FOOD AND DRUG ADMINISTRATION. The results of ibuprofen ODT formulations. Formulation and characterization of fast-dissolving tablet of promethazine theoclate. Tech., May, p.18-25, 2008. Mouth dissolving tablets: A novel drug delivery system. Series G and H ibuprofen ODT formulations. ; RAY, D.; HALDAR, R.; BRZECZKO, A.W. ), where the disintegration time of clopidogrel tablets containing Polyplasdone XL showed the fastest release in compendial medium (pH 2.0), compared with SSG and croscarmellose sodium. ; KUPPASAD, I.J.
Conventional blenders and tableting equipments are used for preparation of these tablets. Among these dosage forms are the orally disintegrating tablets (ODTs). In the first stage of this study, physicochemical characteristics of ibuprofen powder including organoleptic properties, flowability, compressibility, disintegration time of the compacted powder and powder purity were investigated in the standard way (12, 21). ; SHAH, T.P. Finally, the correct amount of magnesium stearate was mixed with the powder blend for a further 2 minutes. The study was approved by the King Saud University Ethics committee, Riyadh, Saudi Arabia. Polyvinyl pyrrolidone was purchased from Sigma Co. (USA). Chemical analysis of API in support of preformulation studies (e.g., solubility determinations, compatibility testing). These techniques are based on the principles of increasing porosity and/or addition of super-disintegrants and water soluble excipients to the tablets. There are some disadvantages to these technologies.
Although, numerous technologies had been developed for the fabrication of these unique dosage forms in the last two decades, but so far, no standardized technique has been designed or mentioned in the literature for their preparation and evaluation (18). The aim of the present work was to prepare fast disintegrating clopidogrel tablets by direct compression and to study the effect of the type and concentration of the superdisintegrant used on the physical properties of the prepared tablets, as well as on drug dissolution and disintegration.
Pharm., v.2, p.2-11, 2008. BALASUBRAMANIAM, J.; BINDU, K.; RAO, V.U. Regarding thickness, uniformity of weight and disintegration time, there was no significant difference between the results of formulations F20 and F17 (t-test, p > 0.05), but there was a significant difference between formulations F20a and F17 (t-test, p < 0.05). Dissol. Mean hardness of series F ibuprofen ODT formulations (n = 10). The major problems existing in series B formulations, resulting in their rejection and preparation of series C formulations were low hardness and high friability as well as inappropriate disintegration time in most cases (7-11 min). ; LACHMAN, L.; SCHWARTZ, J.B. O teste de palatabilidade em voluntC!rios humanos mostrou sabor e sensaC'C#o na boca aceitC!veis. Series D formulations were made by the addition of xylitol and aspartame to formulation F17, extra-granularly. PORTER, S. C. Novel drug delivery: review of recent trends with oral solid dosage forms. One of these advances is the formulation of orally disintegrating tablets (ODTs) that dissolve instantaneously, releasing drugs within a few seconds without the need of water. Moreover, series E formulations could not provide a better taste than the previous formulations studied. The dissolution CL from ODT formulations F3, F6 and F9 (containing 5% each of CCS, SSG, and CPV, respectively) was studied in two different dissolution media, at pH 2.0 and pH 6.8 and the results are displayed in Figure 7. The Friedman test shows the existence or non-existence of significant difference between formulations and Wilcoxon paired test compares formulations with each other pair-wise, in order to specify samples with significant differences. A variaC'C#o de peso e o teor de fC!rmaco de todas as formulaC'C5es mostraram-se dentro do limite oficial, de acordo com a BP. ; RAY, D.; HALDAR, R.; BRZECZKO, A.W. Croscarmellose sodium (CCS), sodium starch glycolate (SSG) and crospovidone (CPV) were kindly supplied by Riyadh Pharma, Riyadh, KSA. About 60 mL of 0.1 N HCl was added and the flask was sonicated for 10 min, then shaken mechanically for 30 min and the volume made up to 100 mL with the same solvent, followed by sonication and filtration. Statistical tests showed that there was no significant difference between the flowability of series B formulations (ANOVA, p > 0.05), but there were significant differences between the flowability of series B formulations with series A formulations and ibuprofen powder (ANOVA, p < 0.05). The ODTs were prepared by direct compression. Regarding the results obtained from the disintegration time, there was a significant difference between formulations F17a and F17b (t-test, p < 0.05) and also formulations F17a and F17 (t-test, p < 0.05).
At predetermined time points (5, 10, 15, 20 and 30 minutes), a 5 mL sample was withdrawn and replaced with fresh dissolution medium. and transmitted securely. Our Swindon, U.K. facility is dedicated to Zydis unit production. An ODT formulation should disintegrate or dissolve in water quickly. Spray dried mannitol (MannogemTM EZ), used as a filler for the orally disintegrating tablets, was kindly supplied by SPI, Grand Haven, USA. ODTs are capable of turning quickly into a liquid dosage form in contact with the saliva (5, 6), resulting in pre-gastric absorption of drug so that more rapid onset of action and greater bioavailability would be expected (7). Development and evaluation of regioselective bilayer floating tablets of atenolol and lovastatin for biphasic release profile. By using this website you understand and accept that Catalent tracks your website activities to be able to offer you a more tailored response or information to meet your requirements, and that your personal data will be held in accordance with our, Copyright 2022, Catalent, Inc - All Rights Reserved, Copyright 2020, Catalent, Inc - All Rights Reserved, Case Study: Zydis Fast Dissolve Technologies , Better pregastric absorption for certain drug compounds, Anti-psychotic (Parkinsons disease, schizophrenia), Embossing with corporate logos and product codes, Unique packaging, including child-resistant options, Taste masking and flavors formulated for specific markets, including pediatrics and veterinary medicine, Functional coating for controlled / sustained release applications, Potential interaction with other constituents of GI fluids, Use of bio-adhesives / absorption enhancers, Pre-gastric delivery (e.g. government site. Effect of superdisintegrants on dissolution of cationic drugs. Asian J. PMC legacy view The amount of ibuprofen in each formulation was 100 mg (22). Also, some technologies utilize special facilities and unique methods that are not easily available and practical for all companies. The oral administration route is considered to be the most widely accepted route because of its convenience, ease of administration, avoidance of pain and patient compliance (Bandelin, 1989BANDELIN, F.J. Compressed tablets by wet granulation. However, there was no significant difference between formulations F17b and F17 (t-test, p > 0.05). In vitro drug release studies of the ODTs showed that more than 90% of the drug was released within ten minutes. JAGDALE, S.C.; FERNANDES, N.C.; KUSHEKAR, B.S. Each flask contained 500 mL 0.1N HCl, adjusted to pH 2.0 or phosphate buffer at pH 6.8 maintained at 37 B1 0.5 B0C. The mean in vivo disintegration time for the ten volunteers was about ten seconds, which is in accordance with the in vitro disintegration time for F9. Development and optimization of dextromethorphan hydrobromide oral disintegrating tablets: effect of formulation and process variables. This might be advantageous during the formulation of CL ODTs, since the manufactured ODTs formulations containing the drug exhibited rapid disintegration at the higher pH value (pH 6.8), which simulates saliva fluid, while the drug dissolves slowly, which may mask its undesirable taste. National Formulary USP 34-NF 29. Hence, for improving these characters, the use of appropriate ingredients and a suitable manufacturing method were necessary. Hence, series A formulations were rejected completely due to poor flowability, sticking to tablet press punches, undesirable appearance, unsuitable uniformity of weight, low hardness, high friability, and a long disintegration time (30 min). ; AJAZ, U.; FATIMA, S.F. Decreasing the particle size increases the surface area, which leads to an increase in dissolution rate.
These tablets are called fast dissolving tablets, orally disintegrating tablets (ODTs) or mouth-dissolving tablets. 52 Flashdose technology uses the combination of both Shearform and Ceform technologies in order to mask the bitter taste of the drug. The physicochemical characteristics of different ibuprofen ODT formulations prepared including power/granule flowability, appearance, thickness, uniformity of weight, hardness, friability and disintegration time were investigated. Orasolv technology involves taste masking of active drug.
Quickly soluble granules can dissolve in water within a few seconds, thus causing dissolution of the tablet.
This observation was in agreement with the higher disintegration times expected with such formulas. Sci. For the corresponding physical mixtures of the drug with all of the additives except mannitol, the characteristic endothermic peak of the drug was seen in its melting range (184B13 oC), but with lower intensity (Figure 2). Samples (3-5 mg) were weighed and hermetically sealed in aluminium pans and heated at a constant rate of 10 B0C/min, in a temperature range from 25 B0C to 250 B0C. Tech., May, p.18-25, 2008.). In series C formulations, ibuprofen, croscarmellose and glucose were used together in the granules. Clopidogrel is an antiplatelet agent, which selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and blocks the subsequent GPIIb/IIIa complex, thereby inhibiting platelet aggregation (Jarvis, Simpson, 2000JARVIS, B.; SIMPSON, K. Clopidogrel: a review of its use in the prevention of atherothrom-bosis. formulated a solid dispersion of clopidogrel into fast dissolving tablets. Moreover, there was a significant difference between the taste of formulation F22s with other formulations (Wilcoxon test, p < 0.05). The side effects will be reduced due to a reduction of drug dosage, resulting in metabolite rate reduction in comparison to the usual dosage forms (9). Preparation of ibuprofen ODT formulations. In the next step, the duration of time required for disintegration of tablets were recorded. ; KUPPASAD, I.J. P-values less than 0.5 were considered as significant in all the above-mentioned tests. Nanocrystal technology can also be used in the formulation of ODTs, and helps to improve compound activity and final product characteristics. Friability (%) of series F ibuprofen ODT formulations (n = 1). The aim of this study was to develop a novel and simple method for producing an ibuprofen ODT formulation, which besides having the mentioned advantages, is cost-effective and the facilities needed for their preparation are available for all pharmaceutical companies. Thereafter, the formula weight of mannitol was mixed with the MCC-superdisintegrant mixture for 10 min. THE UNITED STATES PHARMACOPEIA (USP). ; RAY, D.; HALDAR, R.; BRZECZKO, A.W.
Therefore, in series E formulations, in order to improve the taste, alcohol was substituted by water in the polyvinyl pyrrolidone solution. The target communities in using ODTs are children, the elderly, hospitalized patients, bodily and mental cripples, those with mastication and deglutition problems, patients with resistant chronic nausea, patients under chemotherapy, psychotic patients who hide their tablets beneath their tongue and those persons or travelers who have no access to water (6, 10, 11). Quickly soluble granules of series A formulations included two parts. Durasolv technology is one of the most suitable technologies to prepare products requiring low amounts of active ingredients. SAHITYA, A.; KRISHNAMOORTHY, B.; MUTHUKUMARAN, M.; KISHORE, G. Formulation and evaluation of fast dissolving tablets using solid dispersion of clopidogrel bisulphate. The manufactured ODTs containing 75 mg CL were successfully prepared using the direct compression method. Res., v.2, n.2, p.65-72, 2010. The bulk API is formulated into a liquid solution or suspension. Also, formulations F7 and F8 were too sticky to measure their flowability and compressibility. ; MUOZ-RUIZ, A.; JIMNEZ-CASTELLANOS, R. Disintegrating efficiency of croscarmellose sodium in a direct compression formulation. The data were analysed using Perkin Elmer software (Spectrum V5.3.1). Orally Disintegrating Tablets; Rockville: CDER, 2008. Pharm. The new PMC design is here! Pharm., v.147, n.1, p.11-21, 1997. (FDA). All these physicochemical tests were conducted in the standard way (5, 21, 24, 25), except for the disintegration time. (8, 9). ; RAY, D.; HALDAR, R.; BRZECZKO, A.W. Development and optimization of dextromethorphan hydrobromide oral disintegrating tablets: effect of formulation and process variables. The Dean of the Faculty of Pharmacy, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran, Iran is thanked for providing the facilities to complete this thesis.
Khawla A, Vincent L, Jee L, Graham P, Matthew S. The United States Pharmacopoeia and National Formulary. The release measurements were performed using a USP dissolution apparatus 2 (Caleva Ltd., Model 85T), using the paddle method at 50 rpm. Pharma. J. Adv. Zade PS, Kawtikwar PS, Sakarkar DM. The frozen units are then transferred to large-scale freeze dryers for the lyophilization process. Examples of these are: cross-linked carboxymethyl cellulose (croscarmellose(r)), sodium starch glycolate (primogel(r), explode(r)) and crospovidone (polyplasdone(r)). ; 2015ASHRAF, Z.; KHURRAM, S.; MAQBOOL, U.; KHAN, K.R. Pharmaceutical dosage forms: tablets. FOIA Results of physicochemical tests conducted on formulation F22a (in series F) was found to be acceptable, making it the chosen formulation for further studies. Pharmaceutics: The Science Of Dosage Form Design. A palatability test in human volunteers showed acceptable taste and mouth feel. Results of formulation F22a (in series F), was found to be acceptable, making it the chosen formulation for further studies. Recent technological advances in oral drug delivery: a review. Recentes avanC'os em sistemas de liberaC'C#o de fC!rmacos novos visam C obtenC'C#o de melhor adesC#o do paciente. Technol. Stage 2 Filling and freezing Pharmaceutical dosage forms: tablets. Today, there are different drug delivery systems in the global drug market, aiming to facilitate the process of drug delivery and greater patient compliance. Therefore, formulation F17 was chosen as the selected ODT formulation among the formulations prepared, with a disintegration time of 5 sec. HHS Vulnerability Disclosure, Help It is a unique freeze-dried tablet in which the active drug is incorporated within a water-soluble matrix, which is then transformed into blister pockets and freeze dried to remove water by sublimation. The results of taste studies (1 = best and 5 = worst) conducted on series F, G and H ibuprofen ODT formulations (n = 10; Mean SD). ; SAKR, A. In addition, there was a significant difference between the results of flowability, thickness, uniformity of weight and hardness of formulations F17a and F17b with formulation F17 (ANOVA, Tukey post-hoc test, p < 0.05). Increasing the concentration of CCS or CPV from 5% to 10% in the tablets did not show any further significant increase in the disintegration rate.
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