Use Of Superdisintegrants Research Articles

Formulation, Evaluation and Study of Super Disintegrants effect on Olmesartan Medoxomil Fast Dissolving Tablets

The current research was to enhance solubility and dissolution rate of the slightly soluble drug, Olmesartan medoxomil, solid dispersions by physical mixing, solvent evaporation and kneading techniques, with soluplus. The solid dispersions prepared are tested for flow properties, drug content, and particle size. In vitro dissolution studies were carried out to analyse the drug release from solid dispersions. Crystal morphology, drug and polymer interaction for selected solid dispersions was studied by FT-IR and DSC analysis. Fast-dissolving tablets were formulated by using optimized solid dispersions using different concentrations of sodiumstarch glycolate, crosscarmellosesodium, and crospovidone as superdisintegrants using direct compression technique. The tablets prepared are tested for Weight variation, friability, disintegration, content uniformity and harness. The mechanism and kinetics of drug release from the fast-dissolving tablets were tested by in-vitro dissolution studies. The current research proves that combining solid dispersions along with the use of superdisintegrants is novel approach to formulate of Olmesartan medoxomil fast-dissolving tablets.

Immediate Release Drug Dosage Form

Among all drug forms tablet is the most popular dose form being moment because of its convenience of tone administration, conciseness and easy manufacturing; occasionally immediate onset of action is needed than conventional remedy in numerous cases. So that to overcome these downsides, immediate release lozenge form has surfaced as indispensable oral dose forms. Immediate medicine release lozenge forms disintegrate fleetly after administration with enhanced rate of dissolution .The introductory approach used in development of tablets is the use of superdis integrants like Cross linked Polyvinylpyrrolidone or Sodium bounce glycolate (Primogel, Explotab), carboxymethylcellulose (Croscarmellose) etc. These superdisintegrants give immediate disinteragation of tablet after administration in stomach. In this field immediate release liquid medicinal forms and parenteral medicinal form have also been introduced for treating disease . In liquid medicinal form can be dormancies with typical dissipation agents like hydroxypropyl methylcellulose, AOT (dioctylsulfosuccinate) etc.

Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

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.

Recent Strategic Developments in the Use of Superdisintegrants for Drug Delivery.

Improving drug bioavailability in the pharmaceutical field is a challenge that has attracted substantial interest worldwide. The controlled release of a drug can be achieved with a variety of strategies and novel materials in the field. In addition to the vast development of innovative materials for improving therapeutic effects and reducing side effects, the exploration of remarkable existing materials could encourage the discovery of diverse approaches for adapted drug delivery systems. Recently, superdisintegrants have been proposed for drug delivery systems as alternative approaches to maximize the efficiency of therapy. Although superdisintegrants are well known and used in solid dosage forms, studies on strategies for the development of drug delivery systems using superdisintegrants are lacking. Therefore, this study reviews the use of superdisintegrants in controlled drug release dosage formulations. This overview of superdisintegrants covers developed strategies, types (including synthetic and natural materials), dosage forms and techniques and will help to improve drug delivery systems.

EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX

Objective: This study aims to determine the effect of the inclusion complex formation of ibuprofen (IB) with β-cyclodextrin (β-CD) in improving water solubility and taste masking as well as to study the effect of the combined use of super disintegrants in IB-β-CD ODT (Orally disintegrating tablet).
 Methods: IB-β-CD inclusion complex was prepared by spray drying technique with a 1:1 molar ratio. ODTs were prepared by the direct compression method using various ratios of Ac-Di-Sol® and Kollidon® CL as super disintegrant. The inclusion complex was characterized using spectroscopy FT-IR (Fourier-transform infrared) and DSC (Differential Scanning Calorimetry). The physical properties and dissolution rate of ODTs were evaluated. Dissolved drug concentration at 60 min (Q60) and Dissolution Efficiency (DE60) was calculated using the dissolution test result.
 Results: The unpleasant taste of IB had been successfully masked by IB-β-CD. Formula 1 was observed having 14.5 sec of disintegration, fastest compared to the other formulas. Moreover DE60 value of formula I was higher than the other formulas (113.45).
 Conclusion: IB-β-CD Inclusion complex prepared by spray drying method (1: 1) increased the water solubility and masked the unpleasant taste compared to IB moreover combination of Ac-Di-Sol® and Kollidon® CL increased ODT dissolution rate.

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF ANTIEPILEPTIC DRUG

The objective of the present study was to prepare and evaluate the mouth dissolving tablet of lacosamide using super disintegrants like Guar Gum, and other excipients like microcrystalline cellulose and mannitol in different concentrations by direct compression method. Lacosamide has been shown to be an effective antiepileptic agent appropriate for epilepsy patients. The mouth dissolving tablets were prepared by a single punch machine using a powder blend of super disintegrants and lacosamide. Post-compression parameters like hardness, weight variation, friability, in-vitro dispersion, drug content uniformity, and in-vitro drug release studies were carried out for all formulations. All formulations results were within official limits. Fast disintegration time obtained between 35 sec. and 128 sec, was within the official limit. Different drug release kinetic models were applied for selecting batches for stability studies. These showed that there was no significant change in residual drug content in mouth dissolving tablets. By the in-vitro disintegration, it is concluded that formulation prepared by Guar Gum (10%) showed faster disintegration time than that of MCC. This indicates that the use of super disintegrants increases the release of drug from the formulation. Therefore, it can be concluded that such mouth dissolving tablets are suitable delivery systems for lacosamide.
 Peer Review History: 
 UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency.
 Received file 
 
 Average Peer review marks at initial stage: 3.0/10
 Average Peer review marks at publication stage: 7.0/10
 Reviewer(s) detail:
 Name: Dr. Iman Muhammad Higazy
 Affiliation: National Research Center, Egypt
 E-mail: imane.higazy@hotmail.com
 
 Name: Dr. Mohamed Salama 
 Affiliation: Modern University for Technology & Information, Egypt
 E-mail: salama47@yahoo.com
 Comments of reviewer(s): 
 
 Similar Articles:
 FAST DISSOLVING DRUG DELIVERY SYSTEMS: FORMULATION, PREPARATION TECHNIQUES AND EVALUATION
 FAST DISSOLVING TABLETS: A PROMISING APPROACH FOR DRUG DELIVERY
 DEVELOPMENT AND EVALUATION OF FAST DISSOLVING THIN FILMS OF ARIPIPRAZOLE

Formulation and evaluation of immediate release tablet of zopiclone using wet granulation method

Zopiclone, a cyclopyrolone, is a non-benzodiazepine derivative used as a hypnotic agent in the treatment of short term insomnia. The main objective of the present investigation was to formulate a pharmaceutically active stable and bioequivalent immediate release (IR) tablets of zopiclone using wet granulation method. The prepared formulations were evaluated using various physical parameters, equipment, dissolution study and drug release profile. The basic approach used in development of zopiclone IR tablets was that the use of superdisintegrants as like Corn starch (maize) and Sodium starch glycolate which provide instant disintegration after administration. In-vitro dissolution testing study was carried out for 1 hours using 0.1N HCl in a dissolution apparatus for evaluation of Drug release. On the basis of the dissolution profile, F3 gives a better result and were found 100 % release in just 20 minutes and also found that as the polymer ratio were increases the drug release rate also increased from the formulation. Keywords: Hypnotic agent, immediate release, Wet granulation Method, Non-benzodiazepine derivative, Superdisintegrants, Zopiclone

FORMULATION AND EVALUATION OF TRAZODONE HYDROCHLORIDE ORODISPERSIBLE TABLETS

Objective: The objective of the existing research was to develop an oral disintegrating dissolving system as one of the taste masking orodispersible forms together of trazodone hydrochloride tablets using direct compression technique through the use of superdisintegrants together with FlowLac, StarLac, and sodium starch glycolate. Methods: The tablets were formulated using the direct compression approach. The drugs prepared have been evaluated for diverse parameters which include hardness, friability, weight variation, drug content uniformity, water absorption ratio, in vitro drug release, and wetting time. Results: The hardness of all formulations from F1 to F7 proved that the tablet means thickness was nearly uniform in all formulations with the range of 0.520 mm–0.522 mm. Water absorption of prepared formulations was found to be 68.59%–73.21%. Bulk density, tapped density, and friability of the formulations were established within the limits, results of in vitro drug release study showed the drug released between 90.27% and 96.17% at 60 min. Conclusion: The overall study concluded that orodispersible tablets of trazodone hydrochloride have greater dissolution rate and will result in enhanced bioavailability. The taste masked systems are designed to provide better acceptability, improved bioavailability, for chronic patients. The study results revealed that the formulation F6 was contemplated as the top formulation.

A REVIEW ON FAST DISSOLVING TABLET

In the present scientific scenario, the drug delivery technology has become extremely competitive and quickly evolving with ever-increasing demand. Fast dissolving tablet (FDT) is one such style of an innovative and distinctive drug delivery system. Once FDT is placed on the tongue, it disintegrates or dissolves quickly (in seconds) without chewing or water. Fast dissolving pills became well-liked because of higher patient compliance and most popular over typical capsules and tablets. Numerous FDT products entered the market in the nineteen eighties. This novel drug delivery like FDT or mouth dissolving tablet (MDT) has overcome several disadvantages like dysphagia or non-accessibility of water whereas travel. Compared with typical dosage form FDT is an alternative as well as helpful for the patient. The basic approach employed in the development of FDT is that the use of superdisintegrants like crosspovidone, croscarmellose sodium or maximizing pore structure within the formulation. This review article contains different techniques used for preparing FDT, silent features, numerous proprietary technologies, mechanism of super disintegration, and also the limitations.

FORMULATION AND EVALUATION OF SUBLINGUAL TABLET OF LOSARTAN POTASSIUM

The objective of the current study was to develop and optimize a sublingual tablet of Losartan potassium, which is an effective drug in the treatment of hypertension. Owing to number of advantages dissociated with the quick onset of action and it by passes the liver. Sublingual tablets offer effective and easier way for management of Hypertension. The basic approach used in development of Sublingual tablet was the use of super disintegrants by direct compression method. Oral mucosal drug delivery is one of the promising method of systemic drug delivery which offers several advantages. The literal meaning sublingual is ''under the tongue''. Hence the method includes the administrating drug via mouth so that it is absorbed via blood vessels (systemic) present under the tongue. Sublingual tablet is tablet that dissolves or disintegrates in the oral cavity without need of drinking water. Sublingual tablet traditionally have been used as an effective method to improve the dissolution properties and bioavailability of water-soluble drugs. In the preformulation studies, Losartan potassium was characterized by its physiochemical properties such as melting point, solubility, partition coefficient, UV and FTIR studies. UV spectroscopic method was established for quantitative estimation of the drug and the absorbtion maxima were 234 nm. The tablets were formulated by using the direct compression technique. The post compression studies i.e. shape, size, weight variation, hardness, friability and wetting time determined the quality of the product.
 Key words:-Sublingual, oral cavity, mucous, bioavailability, Gland, Losartan potassium, Systemic, Solubility.

A REVIEW ON FORMULATION APPROACHES IN IMMEDIATE RELEASE TABLET

Sometimes immediate onset of action is required than conventional treatment in many patients. Among all dosage forms tablet is the most popular dosage form existing today because of its convenience of self-administration, compactness and easy manufacturing. to overcome these drawbacks, immediate release dosage form has emerged as alternative oral dosage forms. Immediate drug release dosage forms disintegrate quickly after administration with enhanced rate of dissolution. The basic approach used in development tablets is the use of superdisintegrants like Cross linked Polyvinylpyrrolidone or crospovidone (Polyplasdone), Sodium starch glycolate (Primogel, Explotab), carboxymethylcellulose (Croscarmellose) etc. In this field immediate release liquid dosage forms and parenteral dosage form have also been introduced for treating patients. The development of immediate release therapy also provides an opportunity for a line extension in the marketplace, a wide range of drugs e.g., anticoagulant and other drugs can be considered candidates for this dosage form. The development of immediate release therapy also provides an opportunity for a line extension in the marketplace, a wide range of drugs e.g., anticoagulant and other drugs can be considered candidates for this dosage form. Keywords: Immediate release, super disintegrates, direct compression, wet GranulationÂ

FAST DISSOLVING TABLETS: A PROMISING APPROACH FOR DRUG DELIVERY

Aim of novel drug delivery system is to enhance safety and efficacy of drug molecules by formulating a convenient dosage form for administration and to achieve better patient compliance. One such approach led to development of fast dissolving tablets. Now-a-days fast disintegrating tablets (FDTs) gaining significance with wide variety of drugs serving many purposes. These are novel types of tablets that disintegrate/dissolve/ disperse in saliva within few seconds (less than 60 seconds) without chewing and additional water. The basic approach used in development of FDTs is the use of superdisintegrants and the elimination of bitterness. FDTs reduces the disadvantages of conventional dosage form especially dysphasia (difficulty in swallowing) in pediatric and geriatric patients. These oral dosage forms have many benefits such as self medication, increased compliance, ease of manufacturing and noninvasive. This review presents description of fast dissolving tablets including need for development, challenges in formulation, suitability of drug candidates, composition, various technologies involved, advantages, disadvantages, and evaluation parameters. Peer Review History: Received 19 August 2017; Revised 28 August; Accepted 5 September, Available online 15 September 2017 UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file: Reviewer's Comments: Average Peer review marks at initial stage: 4.0/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Dr. Ogbonna B. Onyebuchi, Nnamdi Azikiwe University, Awka, Nigeria, summitpharm@yahoo.com Dr. Gulay B Anadolu, Anadolu University, Eskisehir, Turkey, gbuyukko@anadolu.edu.tr Similar Articles: FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF ANTIEPILEPTIC DRUG IN VITRO-IN VIVO BIO-EQUIVALENCE CORRELATION STUDY OF ATENOLOL, AND ITS BRANDS OF IMMEDIATE RELEASE TABLET UNDER BIO-WAIVER CONDITIONS This article has been cited by: Recent developments in orally disintegrating mini tablets Sachin Sarashetti, Vikas Jain, Gowda D V, Pooja Mallya, Satish Babu. International journal of research in pharmaceutical sciences 2020, 11(3), 3606-3612. Pubmed

EFFECT OF EFFERVESCENCE IN COMBINATION WITH SUPERDISINTEGRANTS IN THE FORMULATION OF PROPRANOLOL HCL ORAL DISINTEGRATING TABLETS

ABSTRACTObjective: The current research work is intended to formulate propranolol HCl (PLH) as orally disintegrating tablet (ODT). It is also intending to checkthe superiority in a combination of superdisintegrants and effervescent mixture than the use of superdisintegrants alone by a direct compressiontechnique. To fasten the onset of action and thereby enhancing the bioavailability of PLH in comparison to its conventional tablets.Methods: Standard calibration curve of PLH was obtained in pH 6.8 phosphate buffer by spectrophotometric method, drug-excipient compatibilitystudies were carried by Fourier transform infrared (FT-IR) studies. All the formulations were evaluated for pre and postcompression studies.Accelerated stability studies were carried out up to 6 months for the optimized formulation, EF3.Results and Discussion: Superdisintegrants used in the study are compatible with PLH. Pre- and post-compression parameters were within theacceptable limits for all formulations. In vitro dissolution kinetic studies indicate the release of PLH from ODT increases as the concentration ofsuperdisintegrants as well as the ratio of citric acid: NaHCO3 of effervescent mixture increases. Formulations with an effervescent mixture are havingrapid disintegration and dissolution rate when compared to the formulations with superdisintegrants alone. The order of superdisintegrants inenhancing the dissolution rate of PLH is crospovidone (CPV) > croscarmellose sodium (CCS) > sodium starch glycolate (SSG). Formulation, EF3 (10%CPV and 1:3, citric acid: NaHCO3 ratio, respectively) had the highest dissolution efficiency at 10 minutes (DE10=82.74%); the first order dissolutionrate constant (K1=0.141/minutes) with a regression coefficient (r2=0.974) and lesser time for 90% of drug release (t90=4 minutes), was considered asthe optimal ODT in this study. Formulation EF3, passed the test for stability.Conclusion: Hence, an effective PLH ODT was formulated by the direct compression technique with disintegration by combination of superdisintegrantsand effervescent mixture, will fasten the onset of action and enhances the bioavailability of PLH in comparison to its conventional tablets.Keywords: Propranolol HCl, Orally disintegrating tablet, Sodium starch glycolate, Croscarmellose sodium, Crospovidone, Direct compression, In vitrodissolution studies.

Mouth Dissolving Delivery System: A Novel Approach for Angina

Aim: The study aims to see the sights of potential of mouth dissolving tablets for improving the oral delivery of nicorandil by the use of superdisintegrants. Materials and Methods: Fast dissolving tablets of nicorandil successfully prepared by direct compression techniques using various concentrations of sodium starch glycolate, croscarmellose sodium, and crospovidone (CP) as superdisintegrants. The optimized batch of fast dissolving tablets of nicorandil were characterized for hardness, friability, in vitro disintegration, dissolution, stability studies. Results and Discussion: In comparison to marketed immediate-release formulation, the formulation (F9) was found to be faster in drug release profile as well as short disintegration time. The formulation F9 were found to be stable in 6 months stability studies in different packing. Conclusion: Nicorandil tablets containing CP as a superdisintegrant show faster disintegration and dissolution rate.

FORMULATION AND EVALUATION OF TASTE MASK ORALLY DISPERSIBLE PARACETAMOL TABLET

Mostly the drugs are administered by oral route. Orally dispersible tablets are achieving importance when compared to novel oral drug delivery system. Orodispersible tablets are suitable for all age patients by masking the taste of drug. The objective of the present study was to optimize, formulate and evaluate orally dispersible tablet (ODT) of Paracetamol which disintegrates within few seconds in presence of saliva fluid by the use of super disintegrants. Paracetamol is widely used over-the counter analgesic (pain reliever) and antipyretic (fever reducer). It is a very bitter drug so the patients unable to take orally; hence their bitter taste were masked. ODTs Formulations were prepared by Direct Compression and wet granulation method by the use of superdisintegrants and taste masking (F7;F8) is done by Eudragit EPO. The developed formulations were evaluated in terms of weight variation, drug content, friability, thickness, hardness, disintegration and in vitro dissolution test. Stability study of optimized formulation was also carried out as per ICH guidelines. The effects of disintegrants as well as binders in different concentration on the release profile of paracetamol ODTs were studied. The studied parameters were found to be satisfactory for all formulations. Disintegration time for the formulations was found to be less than 40 seconds. Disintegration time for all ODTs decreased with increase in disintegrant concentration. ODTs prepared using Avicel possessed least disintegration time (11s), offered better dissolution profile than that of all the ODTs formulations. Accelerated studies proved that the optimized formulation was stable even after three months. Keywords: Orodispersible tablets, Paracetamol, Prosolv ODT; Eudragit EPO, physical characterization. in-vitro dissolution,

Novel use of superdisintegrants as viscosity enhancing agents in biocompatible polymer films containing griseofulvin nanoparticles

The advantages of using superdisintegrants, sodium starch glycolate (SSG), croscarmellose sodium (CCS) and crospovidone (CP) over traditional high molecular weight (MW) viscosity enhancing agents, guar gum (GG), xanthan gum (XG), pectin and high MW HPMC are examined for improving drug content uniformity without compromising dissolution of films containing nanoparticles of griseofulvin (GF), used as a model poorly water-soluble drug. Films were fabricated by preparing low MW HPMC solutions to which a fixed amount of viscosity enhancing agents was added and mixed with GF nanosuspensions produced via wet milling, followed by casting and drying. The addition of superdisintegrants and high MW HPMC led to an increase in viscosity of precursor suspensions without GF particle aggregation, and hence excellent drug content uniformity along with retention of the high surface area of the GF nanoparticles in dried films. In contrast, the addition of XG and pectin resulted in aggregation of GF particles in suspensions, leading to poor content uniformity and incomplete recovery of GF nanoparticles upon redispersion of dried films. In spite of their high precursor viscosity, the films containing superdisintegrants did not lead to increased mechanical strength and demonstrated fast drug release, suggesting faster matrix erosion. In contrast, films with high MW polymers (GG, XG, and pectin and high MW HPMC) had increased mechanical strength and their subsequent slow erosion/disintegration along with longer hydration times resulted in significant delay of drug release, which was found to be directly proportional to their MW. These results demonstrate novel use for superdisintegrants as economical and superior alternative to traditional viscosity enhancing agents in forming drug laden biocompatible polymer films.

IMMEDIATE DRUG RELEASE DOSAGE FORM: A REVIEW

Among all dosage forms tablet is the most popular dosage form existing today because of its convenience of self administration, compactness and easy manufacturing; sometimes immediate onset of action is required than conventional therapy in many cases. So that to overcome these drawbacks, immediate release dosage form has emerged as alternative oral dosage forms. Immediate drug release dosage forms disintegrate rapidly after administration with enhanced rate of dissolution. The basic approach used in development tablets is the use of superdisintegrants like Cross linked Polyvinylpyrrolidone or crospovidone (Polyplasdone), Sodium starch glycolate (Primogel, Explotab), carboxymethylcellulose (Croscarmellose) etc. These superdisintegrants provide instantaneous disintegration of tablet after administration in stomach. In this field immediate release liquid dosage forms and parenteral dosage form have also been introduced for treating patients. In liquid dosage form can be suspensions with typical dispersion agents like hydroxypropyl methylcellulose, AOT (dioctylsulfosuccinate) etc. The development of immediate release therapy also provides an opportunity for a line extension in the marketplace, a wide range of drugs e.g., neuroleptics, cardiovascular drugs, analgesics, antihistamines and other drugs can be considered candidates for this dosage form. As a drug entity nears the end of its patent life, it is common for pharmaceutical manufacturers to develop a given drug entity in a new and improved dosage form. A new dosage form allows a manufacturer to extend market exclusivity, while offering its patient population a more convenient dosage form or dosing regimen. Keywords: - : Immediate release, polymers, superdisintegrant.