Suresh S, Pandit V, Joshi HP. This formulation had PVP, ibuprofen and croscarmellose as the intra-granular components and xylitol and saccharin as the extra-granular ingredients. (2010JAGDALE, S.C.; FERNANDES, N.C.; KUSHEKAR, B.S. Tech., May, p.18-25, 2008.). Pharm., v.147, n.1, p.11-21, 1997.). Orally disintegrating tablets (ODTs) are capable of turning quickly into a liquid dosage form in contact with the saliva, thus possessing the advantages of both the solid dosage forms particularly stability and liquid dosage forms specially ease of swallowing and pre-gastric absorption of drug. Pharm., v.2, p.2-11, 2008.). ; RAY, D.; HALDAR, R.; BRZECZKO, A.W. (8, 9). Fast dissolving drug delivery systems: a brief overviewInt. Ten healthy and non-smoking volunteers; 5 females and 5 males, aged between 23 to 27 years; took part in this study and expressed their opinion on the appropriateness of the taste of formulated tablets. Asian J. DSC studies revealed that there were no interactions between the drug and the excipients used. Pharm. The results of physicochemical tests conducted on series A,B,C,D,E and F ibuprofen ODT formulations (results are presented as mean standard deviation). 8th ed. Fast dissolving tablets are those which, when put onto the tongue, disintegrate instantaneously releasing the drug, which dissolves or disperses in the saliva (Venkateswara, Nyshadham, Joseph, 2003VENKATESWARA S.S.; NYSHADHAM, J.R.; JOSEPH, A.F. (2014SAHITYA, A.; KRISHNAMOORTHY, B.; MUTHUKUMARAN, M.; KISHORE, G. Formulation and evaluation of fast dissolving tablets using solid dispersion of clopidogrel bisulphate. The average values of weight B1 SD were recorded. Nanocrystal technology can also be used in the formulation of ODTs, and helps to improve compound activity and final product characteristics. Mouth dissolving tablets : An overview of evaluation techniques. (2008BALASUBRAMANIAM, J.; BINDU, K.; RAO, V.U. Stage 4 Sealing Pharm. This goal can be accomplished predictably and efficiently using the Nanocrystal technology. A 10% solution of polyvinyl pyrrolidone was prepared in alcohol for making these granules. This formulation strategy could be cost-beneficial and can be easily adopted by the pharmaceutical companies. 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). Zade PS, Kawtikwar PS, Sakarkar DM. 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. Selection of superdisintegrant for famotidine rapidly disintegrating tablets. 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. Samples were mixed with potassium bromide (spectroscopic grade) and compressed into disks using a hydraulic press before scanning from 4000 to 600 cm-1. Pharma. National Formulary USP 34-NF 29. (2). Zydis was the first commercially available ODT in the drug market. Although, all the in-vitro results of formulations F17a and F17b, except for hardness and friability, were within the acceptable but none of them had a desirable taste. Pharm. The release measurements were performed using a USP dissolution apparatus 2 (Caleva Ltd., Model 85T), using the paddle method at 50 rpm. Mean disintegration time of series F ibuprofen ODT formulations (n = 6). These superdisintegrants provide instantaneous disintegration of the tablet when it is placed on the tongue. Times, v.35, p.3-10, 2003. Durasolv technology is one of the most suitable technologies to prepare products requiring low amounts of active ingredients. Using CCS and CPV as superdisintegrants, when the concentration of the superdisintegrant was increased from 2% to 5%, enhanced tablet disintegration was observed. The thermal behaviour of CL alone and in physical mixtures with tablet excipients was studied using DSC. Guidance for Industry. Formulation F22s; which contained intra-granular ingredients of formulation F22a, including polyvinyl pyrrolidone, ibuprofen and croscarmellose and extra-granular components including xylitol and saccharin; was examined in terms of various physicochemical tests, as well as the assay of active ingredient. However, such formulations have reduced palatability due to the rapid dissolution in the mouth. A more rapid onset of action has a significant effect on different clinical manifestations such as insomnia, anxiety, pain, fever, inflammation, etc. Sci. Then by adding xylitol to formulation F20, formulation F20a was made. Upon scanning the DSC thermogram of the drug-mannitol physical mixture, the drug fusion peak appeared at about 154 oC suggesting an interaction between the drug and mannitol. These components were throughly mixed and subsequently compressed into tablets, using a single punch tablet press equipped with 9 and 14 mm flat punches. FOOD AND DRUG ADMINISTRATION. In evaluation of mouth feel, eight of the volunteers reported that it was acceptable while the other two exhibited taste responses with no complaints of numbness. The results obtained from the physicochemical tests conducted on formulation F22a (with a disintegration time of 4 sec), were desirable and acceptable in terms of all the tests conducted and as a result this formulation was chosen as the selected formulation. 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). The results of ibuprofen ODT formulations. National Library of Medicine Finally, the correct amount of magnesium stearate was mixed with the powder blend for a further 2 minutes. It can be concluded that the optimum concentration of superdisintegrant is 5%, which gave rapid disintegration of CL tablets. In order to study qualitative data (taste studies), Friedman and Wilcoxon paired statistical tests were used. Gen. Conventional blenders and tableting equipments are used for preparation of these tablets. Orasolv technology involves taste masking of active drug. BALASUBRAMANIAM, J.; BINDU, K.; RAO, V.U. (DHHS). Int. The results of palatability test were illustrated in Tables V and VI. ; LACHMAN, L.; SCHWARTZ, J.B. Co, Tabuk, Saudi Arabia. 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. ), 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. J. Adv. 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. Tech., v.18, n.2, p.454-463, 2013. All of the principal absorption beaks of clopidogrel appeared in the physical mixture at the same positions. HPLC was used for the assay of active ingredient after weighting and powdering 20 tablets randomly (26). ASHRAF, Z.; KHURRAM, S.; MAQBOOL, U.; KHAN, K.R. The .gov means its official. (DHHS). An effervescent disintegrating agent is also used in these tablets. BIRADAR, S.S.; BHAGAVATI, S.T. Twenty accurately weighed tablets (W1) were placed in the friability tester (Erweka, TA3R, Heusenstamm, Germany), and allowed to rotate for 4 min at 25 rpm. In: LIEBERMAN, H.A. Pharm. Clopidogrel hydrogen sulphate (named hereafter clopidogrel) was discovered by Sanofi. ; LACHMAN, L.; SCHWARTZ, J.B. ; AJAZ, U.; FATIMA, S.F. Pharm. Effect of superdisintegrants on dissolution of cationic drugs. Following the comparison of their taste with each other through asking 10 volunteers, the most suitable formulation regarding the taste, being formulation F22s, was chosen as the ultimate formulation. The extra-granular components of series A, B, C, D, E and F ibuprofen ODT formulations. This formulation also provided a desirable taste and hence could be considered as a promising ODT formulation. Thermal analysis data were recorded using a TA 50I PC system with Shimadzu software programs. Then, by adding various flavorants and sweeteners to this formulation, complementary series of formulations named G and H were prepared. buccal, sublingual, oesophageal), pH relatively neutral (5.5 7.2 depending on salivary flow rate), Potential for sublingual / buccal absorption, Solid, unit doses presented in protective pack, Low temperature processing minimizes manufacturing losses of labile drugs, Solution / suspension dosing achieves good content uniformity for low dose actives, Solid dosage form and low water activity aids long term stability, Liquid processing facilitates containment of potent drugs in production, Tailored to meet the known product requirements such as API unit dose, Consideration of the relevant API characteristics identified during the technical evaluation of preformulation data, A range of prototype Zydisformulations prepared under different processing conditions (bench-scale); analytical techniques applied as appropriate to determine the compatibility of a candidate API with the Zydistechnology, Short-term (4 week) accelerated physical stability studies typically undertaken before recommendations for a full development program are made, Operational excellence and efficiency via Lean Six Sigma principles, Full in-house analytical and regulatory services, Full characterization of your API and associated Zydisformulations via expert analysis and interpretation of data throughout the development process to provide a robust data package in support of regulatory filings, Smart full-lifecycle management from molecule to market with Lean efficiency standards, Expert handling and maximization of potent and controlled drugs, Bench, pilot, and full-scale cGMP manufacturing, Pilot line with controlled and potent drug capabilities, FDA and MCA audited Controlled drug capabilities. A sugar based matrix, called Floss is used, which is made up of a combination of excipients (crystalline sugars) alone or in combination with drug. 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 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. This could be due to the use of water instead of alcohol in the polyvinyl pyrrolidone solution. Moreover, Jagdale et al. Croscarmellose sodium (CCS), sodium starch glycolate (SSG) and crospovidone (CPV) were kindly supplied by Riyadh Pharma, Riyadh, KSA. Dec., p.1-6. BALASUBRAMANIAM, J.; BINDU, K.; RAO, V.U. Stay informed of issues for this journal through your RSS reader, Resumo J. Rev., v.85, p.28-35, 2001. Brazilian Journal of Pharmaceutical Sciences, Text The result of powder purity was 100.1% 0.2 (mean standard deviation; n = 3), showing compliance with the acceptable range of 98.5% to 101.0% mentioned in the literature (12). 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. ; SAKR, A. Hence, for the purpose of conducting the disintegration time test, 6 tablets from each formulation were chosen randomly and each individually dropped into a basket connected to the wall of a beaker containing 10 mL pH 7.2 phosphate buffer (same as the salivas pH). Decreasing the particle size increases the surface area, which leads to an increase in dissolution rate. Orally disintegrating tablets are defined as solid oral preparations that disintegrate rapidly in the oral cavity with an in vitro disintegration time of less than 30 seconds, according to FDA guidelines (DHHS, 2008DEPARTMENT OF HEALTH AND HUMAN SERVICES. ; SHAH, T.P. Examples of these are: cross-linked carboxymethyl cellulose (croscarmellose(r)), sodium starch glycolate (primogel(r), explode(r)) and crospovidone (polyplasdone(r)). The granules of this series consisted of polyvinyl pyrrolidone and glucose. CENTER FOR DRUG EVALUATION AND RESEARCH (CDER) . The clinical benefits of clopidogrel have been demonstrated and it is used worldwide for the long-term prevention of atherothrombotic events such as myocardial infarction, stroke, peripheral arterial disease and acute coronary syndrome (Jarvis, Simpson, 2000JARVIS, B.; SIMPSON, K. Clopidogrel: a review of its use in the prevention of atherothrom-bosis. Times, v.35, p.3-10, 2003.; Suresh et al., 2008SURESH, B.; KUMAR, M.; RAMESH, G.; MADHUSUDAN, R. Orodispersible tablets: an overview. The The authors explained their results on the basis that of the commonly used superdisintegrants, crospovidone is nonionic, while SSG and croscarmellose sodium are anionic. 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. J. 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). BANDELIN, F.J. Compressed tablets by wet granulation. P-values less than 0.5 were considered as significant in all the above-mentioned tests. In recent years, several new advanced technologies have been introduced for the formulation of ODTs with very interesting features such as extremely low disintegration time, exceptional taste masking ability, pleasant mouth feel and sugar free tablets for diabetic patients (6, 18). The use of superdisintegrants is essential in development of orally disintegrating tablets. Moreover, series E formulations could not provide a better taste than the previous formulations studied. KUCCHERKAR, B.S. There was a significant difference between the taste results of formulation F22a and series G and H formulations (Friedman test, p < 0.05). Potassium dihydrogen orthophosphate and Sodium hydroxide were purchased from Merck, Darmstadt, Germany. The manufactured ODTs containing 75 mg CL were successfully prepared using the direct compression method. 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. Res., v.2, n.1, p.15-23, 2014. The ODTs were prepared by direct compression. 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. ; LACHMAN, L.; SCHWARTZ, J.B. Quickly soluble granules were used alongside other formulation ingredients. Wow means without water. 8600 Rockville Pike The calculated bulk density was between 0.39-0.44 g/cc and the tapped density was between 0.398B10.007 and 0.43-0.50 gm/cc for all tested powder blends. Quickly soluble granules of series A formulations included two parts. New York: Marcel Dekker, 1989. v.1, p.131-94,). Twenty tablets from each batch were individually weighed (Analytical balance, Shimadzu, EB-3200D, Tyoto, Japan) and the average weight B1 SD was calculated. 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). Series G and H complementary formulations were made by the addition of various flavorants and sweeteners to formulation F22a. Tablets formulated without superdisintegrants exhibited a disintegration time of about 236 seconds. Pharmacol., v.4, n.2, 2006.). At predetermined time points (5, 10, 15, 20 and 30 minutes), a 5 mL sample was withdrawn and replaced with fresh dissolution medium. ; KUPPASAD, I.J. The fibrous nature of CCS is more pronounced at lower concentrations and smoothens gradually with time. This observation was in agreement with the higher disintegration times expected with such formulas. Res, v.4, n.10, p.377-381, 2015). All the prepared tablets were found to disintegrate fast. The main objective of this paper was to prepare and develop ODTs of clopidogrel. ; NAZ, S.; MUNEER, F.; IRFAN, U.; AYUB, M. Assay of clopidogrel hydrogen sulphate in tablet form from different manufacturing sources by using UV spectroscopy. All of our sites are subject to annual review so we can remain in highest compliance with: CATALENTS BEST-IN-CLASS FAMILY OF FAST DISSOLVE TECHNOLOGIES. For systemic delivery, the oral route has been the preferred route of administration (1-4). In series B formulations, polyethylene glycol 1000 was substituted by polyvinyl pyrrolidone in the intra-granular part and magnesium stearate and silicone dioxide were omitted from the extra-granular part of formulation. Formulation, evaluation and optimization of fast dissolving tablet containing tizanidine hydrochloride. However, there was no significant difference between formulations F17b and F17 (t-test, p > 0.05). This indicates that there is no interaction between clopidogrel and these excipients. Pharmaceutical dosage forms: tablets. Pharm. In the next stage, ibuprofen as the active ingredient, croscarmellose as the super-disintegrant, silicone dioxide as the glidant and magnesium stearate as the lubricant were screened and weighted separately. (ed.). Friability (%) of series F ibuprofen ODT formulations (n = 1). 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