Superdisintegrant Concentration Research Articles

Comparative study between the Full Factorial, Box–Behnken, and Central Composite Designs in the optimization of metronidazole immediate release tablet

The purpose of this paper is to summarize the fundamentals, benefits and limitations of various models of Design of Experiments (DoE) such as 2-Level Full Factorial Design, Central Composite Design (CCD), and Box–Behnken Design (BBD) while establishing a comparison between these models by taking the Metronidazole immediate release (IR) tablets as a case study. Metronidazole IR tablets were prepared by wet granulation method. The Quality Target Product Profile (QTPP) and Critical Quality Attributes (CQA) were selected based on literature review and prior knowledge about the formulation. Critical Material Attributes (CMA) (concentration of binder, super disintegrant, and glidant), and Critical Process Parameters (CPP) (compression of the tablets) were identified based on their risk to the CQA. Screening and optimization of the CMA were performed using DoE. From the Full Factorial Design, it was observed that the disintegration time and dissolution at 30 min were significantly influenced by the selected CMAs. These significant factors were further optimized using CCD and BBD to achieve the constraints (minimum disintegration and maximum dissolution). The levels of povidone K30, crospovidone, and magnesium stearate were optimized to 10 mg, 32 mg, and 1.6 mg respectively using CCD and BBD.

Formulation and evaluation of oral dispersible tablet of nimesulide by direct compression method

Based on Biopharmaceutics Classification System (BCS), nimesulide is a class II drug, characterized by low solubility and high permeability. Thus, its dissolution represents a limiting step in the drug absorption process which directly affects the bioavailability of the drug. Oral Dispersible tablets (ODTs) of nimesulide overcome the problem related to dissolution by enhancing the rate of dissolution by decreasing the disintegration time and making it easy to administer to patients who refuse to swallow a tablet. In the present study, different formulations of nimesulide were prepared to vary the concentration of superdisintegrants: crospovidone, croscarmellose sodium, sodium starch glycolate along with other excipients: PVP K-30, Aerosil, Mannitol, and Magnesium stearate by direct compression method. Precompression and post-compression parameters were evaluated and also the effect of different concentrations of superdisintegrants on the release profile of Nimesulide ODT was studied. The final data revealed that a combination of 10% crospovidone and 8.33% SSG i.e. formulation B4 was found best combination with the lowest dispersion time of 40 seconds, lowest disintegration time of 19.16 seconds, and lowest wetting time of 15 seconds as compared to other formulations. All other studied parameters were found to be satisfactory for all ODT formulations for Nimesulide. It was concluded that Nimesulide can be successfully formulated as oral dispersible tablets using various superdisintegrants in different concentrations by direct compression method. The optimized batch can be subjected to real-time and accelerated stability studies to determine the shelf life for commercial use.

Formulation and in-vitro evaluation of floating pulsatile drug delivery of chronotherapeutic release of h2 receptor antagonist of famotidine

In the present study famotidine floating pulsatile drug delivery system was developed. Various type and different concentrations of superdisintegrants and polymer affect the drug release. FTIR studies concluded that there is no interaction between drug and excipients. Based on disintegration time and dissolution time the formulation (F2) which contains 8% sodium starch glycollate was optimised. The optimised formulation F2 was further coated with different concentrations of HPMC K4M,HPMC K 15M and HPMC K 100M..Based on the concentration of the coating layer and solubility of the coating layer and the dissolution data the formulation (F6) which was coated with 150mg of HPMC K 15M was optimised.

Design and Development of Oxyclozanide Chewable Tablet Formulation Employing Quality by Design Approach

Abstract: Background: The focus of this research was to identify undiscovered knowledge associated with the production of oxyclozanide tablets utilizing Quality by Design (QbD) in order to develop an ideal formulation that would guarantee constant product quality. The modern approach to formulation design and optimization essentially entails QbD which is a systemic method of pharmaceutical development and comprises of the design and development of formulations as well as manufacturing processes to meet the target product quality. Materials and Methods: Pre-formulation studies on excipient flow properties, compactibility and tabletability profiles, identification of Critical Process Parameters (CPP) and Critical Quality Attributes (CQA) were carried out. An experimental design was adopted to investigate the effect of formulation and process variables (compression force, super-disintegrant type and concentration) on the CQAs using Modde Pro 12.1. The obtained results were used to generate a Design Space (DS) based on the study data. Results: Preformulation studies carried out on the core excipients used, gave an understanding to their tabletability and compactibility. Process parameters such a compaction force and formulation variables such as super-disintegrant concentration were studied within the framework of Quality by Design (QbD) and the new optimized formulation derived was tested and confirmed to be within the design space generated. Conclusion: At the end of the study, the aim was achieved; which was to implement pre-formulation studies and QbD to design a formulation containing Oxyclozanide (API) with a combination of excipients. Keywords: Quality by Design (QbD), Oxyclozanide, Chewable tablet, Compactibility, Tabletability.

Implementation and comparison of different taste masking techniques to design and assess dispersible tablet formulations

The objective of this study was to assess the efficacy of several taste-masking techniques and to study the impact of different formulation variables on the physicochemical properties of dispersible tablets containing Ranitidine as a model drug. Ranitidine powder was taste masked using various techniques. Factorial design (24) was applied to design the set of tablet formulations. The four factors implemented were the manufacturing method, filler type, superdisintegrant type and superdisintegrant concentration. Levels selected were direct compression and wet granulation for the manufacturing method, microcrystalline cellulose and mannitol for the diluent type, sodium starch glycolate and croscarmellose sodium for superdisintegrant type, and 2% and 10% for superdisintegrant concentration. Granulation with calcium carbonate (ratio of 1:8) was the taste-masking method of choice to be implemented. The formulated tablets results revealed that the manufacturing method has a significant influence on all the tested physicochemical properties (p-values < 0.05) such as tablet’s weight variation, hardness, friability, and disintegration time. Croscarmellose sodium obtained better results than sodium starch glycolate. Both fillers obtained good properties when implementing direct compression method with croscarmellose sodium concentration of 2%, or wet granulation method with croscarmellose sodium concentration of 10%. Drug release was also increased by increasing concentration of croscarmellose sodium. These findings represent an easy manufacturing procedure with relatively low-cost materials that can be implemented to formulate dispersible tablets of bitter tasting drugs that will enhance patient compliance and lead to faster onset of action.

Formulation and Evaluation of Posaconazole Bilayer Delayed Release Tablets Using Solid Dispersion Technique

The aim of present investigation to formulate bilayer tablets of posaconazole by using solvent evaporation technique. Posaconazole belongs to BCS class 2 which has high permeability and low solubility. In order to enhance the solubility of posaconazole solvent evaporation technique was applied where HPMC AS was used as carrier. This tablet consist of two layers of which first layer serves as loading dose which produce immediate release of drug and second layer serves as maintenance dose that provide controlled release of drug. The whole bilayer tablet is coated with Eudragit L30D55 to produce delayed release and protect drug from acid environment in stomach. The drug excipient compatibility study was performed by FTIR and no interaction was found. Croscaramellose was used in immediate release layer as superdisintegrant. Methocel K100M and Methocel E5M are used for sustain drug release in control release layer. The powder blend for evaluated for flow properties like angle of repose, bulk density, tapped density, Carr’s index and Hausner’s ratio which showed good results. Invitro dissolution studies was performed with USP dissolution apparatus 2- Paddle type. Invitro dissolution was performed for 2 hours in 0.1N HCl which showed no drug release followed by 6.8 phosphate buffer for 12 hours. The bilayer tablet showed initial release to provide loading dose of drug followed by controlled release up to 12 hours. Change in concentration of polymer and superdisintegrant showed impact on drug release profile. Increase in concentration of superdisintegrant in immediate release layer showed increased % drug release. Whereas increase in sustain release polymers in controlled release layer showed decrease % drug release. F9 batch showed satisfactory release up to 100% for 12 hours and was selected as best formulation. Reproducible batch for F9 was formulated and called F10 which also showed satisfactory results.

Formulation and Evaluation of Aripiprazole Oral Disintegrating Tablets

Aim: This work aims to develop oral disintegrating tablets from solid dispersion of aripiprazole that are capable of enhancing solubility.
 Methodology: Aripiprazole an antipsychotic is a BCS class IV drug with Oral bioavailability of 87%. To enhance the solubility of this drug the solid dispersions were prepared by using a combination of β-Cyclodextrin and PVP K30 in 1:1, 1:2 by using a physical mixture and solvent evaporation method. The prepared solid dispersions were analyzed for all the physical parameters and drug excipient interactions. The solid dispersion was optimized for the preparation of oral disintegrating tablets by direct compression technique using different concentrations of various natural super disintegrants namely Tapioca starch, Amorphophallus campanulactus, and synthetic super disintegrants namely Sodium starch glycolate, crospovidone.
 Results: FTIR showed that the drug and excipients are compatible with each other. Among all the solid dispersion formulations SCD6 (Drug: β-cyclodextrin) shows a high percentage of drug release i.e., 98.58±0.28% for 45 min, and solubility was found to be 0.954±0.32mg/ml. Percentage practical yield was found to be 98.36±0.14% and drug content was found to be 97.31±0.04%. SCD6 formulation was optimized for the preparation of oral disintegrating tablets. The post-compression parameters of all the prepared tablets were within the limits. Among all, F3 formulations containing tapioca starch, 7.5% were found to possess a better disintegration time (28±1.52sec) and in-vitro dissolution (98.64±0.29% for 45min).
 Conclusion: It can be concluded that solid dispersions of Aripiprazole incorporated in oral disintegrating tablets are a very useful approach for better release of Aripiprazole in an efficient manner.

ANALYSIS OF IN VITRO DISINTEGRATION AND DISSOLUTION EFFECT OF CUCURBITA MAXIMA STARCH IN LOSARTAN FDT

Objective: In this work, Curcurbita maxima was used as a superdisintegrant in the preparation of fast dissolving tablets containing Losartan. A Losartan is readily ionized in the presence of an acidic pH, resulting in decreased absorption via the GIT. Superdisintegrant can be used to solve this problem. Methods: Losartan fast-dissolving tablets were made using the direct compression method and two distinct superdisintegrants, derived starch and Curcurbita maxima mucilage, in various quantities. Eleven formulations with varied concentrations of superdisintegrants were created to determine their efficacy and critical concentration levels. For each formulation, several pre-compression and post-compression assessment parameters were used. Results: The disintegration time of the FDT (F1-F4) prepared with derived starch ranges from 4.28±1.02 min to 8.20±1.02 min, while the disintegration time of the FDT (F5-F8) prepared with Cucurbita maxima starch ranges from 1.02±0.02 min to 5.02±1.02 min. The remaining three formulations, F9-F11, have a disintegration time of more than 10 min. In comparison to other formulations, FDT containing Curcurbita maxima mucilage demonstrated improved organoleptic qualities, as well as outstanding in vitro disintegration and dissolution drug release. Conclusion: It was determined that a lower concentration of Cucurbita maxima starch (10 mg) was the optimal concentration level for the Losartan FDT formulation.

Orodispersible films of Ledipasvir and Sofosbuvir Combination: Formulation optimization and development using Design of Experiments

Ledipasvir (LDV) and sofosbuvir (SBV) are poorly soluble drugs and hence dissolution limited bioavailability is a major concern. Further, the high total dose of this combination (LDV-90mg and SBV-400mg) may cause swallowing difficulties if formulated into tablets. Considering these challenges, it was aimed in the current research work to develop orodispersible films (ODFs) for this combination to enhance dissolution thereby bioavailability and also patient convenience. ODFs, because of their ready dispersibility in the oral cavity dissolution would be rapid and also high doses of drugs can be incorporated avoiding swallowing difficulties. HPMC E15 was taken as the film former. Thickness of the films (50µm – 150µm), concentration of superdisintegrant (sodium starch glycolate 6-12% w/w) and concentration of plasticizer (polyethylene glycol 400, 10-20% w/w) were taken as three formulation factors each at three levels. Using Design Expert software, Box-Behnken design under response surface methodology was selected as the experimental design. Disintegration time (DT), time for 90% dissolution of LDV (LDV-T90%) and time for 90% dissolution of SBV (SBV-T90%) of the ODFs were taken as response. The films were developed using solvent casting method. The obtained films were subjected for various quality characteristic studies like differential scanning calorimetry, X-ray diffraction, tensile strength, % elongation, folding endurance, disintegration time, drug content uniformity and dissolution studies. All the formulations were found to have favorable tensile strength, % elongation and folding endurance. The DT values were found to be in the range of 37 – 139 sec.; the values of LDV-T90% and SBV-T90% were found to be in the range of 7.1 – 20.7 min. and 6.8 – 15.6 min. respectively. The results of these three responses were subjected to ANOVA studies and found that all the three formulation factors were having significant effect. The results of optimization by desirability functions approach indicated the ODFs with thickness 50µm, disintegrant at 12% w/w and plasticizer at 17.46%w/w as the optimized formulation. The ODFs prepared at this combination showed DT of 45 sec, LDV-T90% of 7.51 min. and SBV-T90% of 6.23 min. these results indicated that ODFs for LDV and SBV were successfully optimized and developed.

Formulation and in-vitro characterization of fast-disintegrating herbal extract sublingual immunotherapy tablet for peanut-induced allergic asthma

BackgroundAllergen immunotherapy (AIT) involves the regimen of gradually incrementing doses of the allergen, thereby inducing desensitization and tolerance. Sublingual Immunotherapy tablets (SLIT-tablets) have been formulated for several allergies and had manifested efficacy for allergic rhinitis and allergic asthma. SLIT promises an alternative method to other routes of AIT enabling patients to self-administer AIT. ObjectiveThe study aimed to formulate fast disintegrating SLIT containing crude peanut extract for peanut-induced allergic asthma. MethodsThe crude peanut extract was prepared by a simple extraction method and was subjected to quantitative and qualitative analysis. The extract was also characterised for its physical properties. The preformulation study for the extract and excipients of the tablet was performed using FT-IR spectroscopy and Differential scanning calorimetry. The tablet powder blends were characterised for pre-compression properties. The SLIT tablets were developed by direct compression and the post-compression evaluation was performed. ResultsThe results of the quantitative and qualitative analysis of extract confirmed the presence of peanut proteins in the extract. The preformulation studies using FT-IR spectroscopy and Differential Scanning Calorimetry revealed that there is no significant interaction between the CPE and excipients. The pre-compression characterisation showed that the powder blends had good flowproperties. Three doses of SLIT tablets were formulated with each dose containing four batches and the tablet of each dose was optimized by studying the effect of varying concentrations of super disintegrants on disintegration time and dissolution rate. The post compression characterization of the tablets was performed and the optimized batch of the three doses with the concentration of 5% crospovidone and 2% croscarmellose sodium showed less wetting time and high-water absorption ratio, shorter disintegration time of 14secs and maximum drug release of >90% within 2–3 min. ConclusionThe results indicated the suitability of formulated SLIT tablets for peanut induced allergic asthma.

Formulation and evaluation of oral disintegrating tablets of furosemide

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

Formulation and Optimization of Dolutegravir Fast Dissolving Tablets Using Various Solubility Enhancement Methods

Dolutegravir is a HIV-1 antiviral agent to control HIV/AIDS. In the present study Dolutegravir solid dispersion has been subjected to improve the solubility and dissolution rate performance by formulating as fast dissolving tablets, in which PEG 6000 and Poloxamer 407 were used as polymers. Solid dispersions of Dolutegravir were prepared with different carriers in different ratios of drug and carriers such as PEG 6000 and Poloxamer 407 (1:1, 1:2 and 1:3) by solvent evaporation and fusion method. The pre-compression and post-evaluation parameters were studied and the results were shown. All the results were within acceptable IP limits Finally, by comparing all the dissolution profile of solid dispersions , formulation F3 containing Dolutegravir + PEG 6000 (1:3) showed better results by solvent evaporation method at the end of 60 min with maximum drug release, hence it is selected as the best formulation. From the obtained optimized solid dispersion formulation, the fast dissolving tablets were prepared by using different concentrations of various super disintegrants. The in-vitro drug releases of the formulated Dolutegravir tablets were performed using a 6.8 pH Phosphate buffer as dissolution medium. The optimized DF3 formulation containing Sodium starch glycolate (SSG) (6% w/w) as super disintegrant, and it showed 98.04±1.9 % percentage drug release at 25 min. Characterization in solid-state were done by analytical methods such as UV-Visible, FT-IR studies. The optimized formulation followed first order release kinetics.

Optimization and development of orodispersible films for ledipasvir and sofosbuvir through solid dispersion using Box-Behnken design

The fixed dose combination of ledipasvir (LDV) and sofosbuvir (SBV) is approved by USFDA in 2014 for the treatment of Hepatitis C virus infection and is available in the form of tablets. In the present work, the principal aim is to explore orodispersible films type dosage form to impart its characteristic advantages to these poorly soluble drugs so as to improve their bioavailability and ease of administration. Solid dispersions with low viscosity grade methyl cellulose A 15-LV (MC A 15-LV) at different ratios with LDV and SBV were prepared and evaluated to check their ability in improving the solubility of the drugs. The best drug to polymer ratio was selected to develop the films, using other excipients including plasticizer and superdisintegrant. Solvent casting method was used to develop the films. Three formulation parameters were selected as independent factors viz. thickness of the film (50-150 µm), concentration of superdisintegrant (sodium starch glycolate 6-10%) and concentration of plasticizer (polyethylene glycol 400, 10-20%). Disintegration time (DT), time for 90% dissolution (T90%) of LDV and time for 90% dissolution of SBV were taken as the response variables. The experiment was designed using Box-Behnken design. Among the polymers, MC A 15-LV produced maximum solubility at 1:2 ratio. The films obtained were found to have good tensile strength and % elongation with disintegration times in the range of 43-162 sec. The T90% values for LDV and SDV were found to be in the range of 8.4-21.2 min and 7.2-18.4 respectively. All the three formulation factors were found to have significant effect on the three responses. The optimum formulation was identified at 100 µm thickness, 10% superdisintegrant and 20% plasticizer which showed DT of 89 sec with T90% values of 8.4 min and 7.2 min for LDV and SBV respectively. The rapid disintegration and dissolution of the films signified that the set objective was achieved.

Formulation and Evaluation of Effects of Superdisintegrants on Immediate Release Tablet of Linagliptin, a DPP-4 Inhibitor

The study aimed to develop and evaluate an immediate-release tablet dosage form of Linagliptin. Different concentrations (ranges 5-10%) of super-disintegrants, Croscarmellose sodium (CCS), and Sodium starch glycolate (SSG) were used to prepare nine tablet dosage forms (F1 to F9) through the direct compression method. The compatibility of the formulations was evaluated by FTIR to reveal any possible drug-excipient interactions and it was proved to be compatible with all formulations. Precompression (bulk density, tapped density, Carr’s index, Hausner’s ratio, and angle of repose) and post-compression parameters (weight variation, hardness, thickness, and friability) were analyzed for all tablets and the results were found satisfactory as well as within limits as per USP guidelines. All the formulated batches (F1 to F9) exhibited disintegration of tablets within 2 minutes, where formulation F9 represented the lowest disintegration time (51±3 sec) which was also found significantly better than the marketed product (310±5 sec). In terms of drug dissolution, 90% of drug release was observed for all nine formulations within 45 minutes and formulation F9 (5% CCS and 5% SSG) illustrated the rapid and highest dissolution rate compared to the marketed one’s, 100% drug release at 20 minutes and 91.77 % drug release at 30 minutes successively. The respective data sets of drug release were mathematically fitted to several kinetic models and for all formulations, drug release pattern obeyed first-order kinetics amongst those, formulation F2 (r2= 0.98), F4 (r2= 0.99), F5 (r2= 0.98), and F9 (r2= 0.97) were found to be best fitted in this kinetic norm. Based on disintegration time and dissolution data comparison to a brand leader market product, F9 was experienced as the best formulation. Furthermore, it was observed that if SSG and CCS were combined, then these two parameters were more improved compared to their separate uses. Thus, incorporation of the optimum amount of super-disintegrants in a formulation showed rapid swelling, faster disintegration as well as ease of dissolution of tablet dosage forms. Bangladesh Pharmaceutical Journal 24(2): 168-179, 2021

FORMULATION DEVELOPMENT AND EVALUATION OF CHRONOMODULATED DRUG DELIVERY SYSTEM BY ZAFIRLUKAST

Objective: The main objective of the present study was to formulate and evaluate a time-controlled single-unit oral pulsatile drug delivery system containing Zafirlukast for the prevention of nocturnal asthma attacks. To provide time-scheduled drug release for Asthma disease. It is used for preventing asthmatic attacks at early morning. Pulsatile release dosage form is increasing patient compliance by reducing the dosing frequency, especially in the early morning.
 Methods: Core tablets were prepared by incorporating different concentrations of natural and synthetic super disintegrants. Drug-containing core tablets (ZC1-ZC15) with different compositions of natural super disintegrants (Plantago ovata seed powder, Locust bean gum) synthetic super disintegrants (Sodium starch glycolate (SSG), Cross carmellose sodium (CCS), Crospovidone (CP)) were prepared by direct compression technique. The core tablets were subjected to pre-formulation, physicochemical and In vitro drug release studies. The fast disintegrating core tablet formulation was selected and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic polymers Eudragit RS100, Eudragit RL 100, Ethylcellulose and hydrophilic polymers Hydroxypropyl methylcellulose K4M, K100M. The optimized formulation was selected and quantified based on in vitro drug release profile in simulated gastric and intestinal fluids.
 Results: The pre and post-compression parameters of tablets were also found to be within limits. Formulation ZC5 with 16 mg of Locust bean gum showed the least disintegrating time, i.e., 22.13 sec, and was selected as the best immediate release core tablet. The press-coated tablet formulation P8 having 62.5 mg Eudragit RS100 and 62.5 mg of HPMC K4M in ratio 1:1 over the core tablet ZC5 showed rapid and drug release nearly after 4 h lag time and 98.86 % up to 12 h. Accelerated stability studies of the optimized formulation P8 indicated no significant difference in release profile after 3 mo.
 Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating amount level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.

Design, Characterization and In-vitro Evaluation of Favipiravir Orodispersible Films

Introduction: Orodispersible films (ODF) is a thin strip that is mostly transparent, biodegradable and it has hydrophilic polymers that disintegrate and dissolves immediately when getting in contact with saliva. Different disintegrants play a crucial role in film properties such as organoleptic properties, film thickness, and in particular disintegration time of the film. The main reason for the development of oral films is for their prominent role in increased patient compliance among pediatrics and geriatrics by disintegrating faster, releasing the drug rapidly, without the need for water, and mostly decreasing the risk of choking.
 Aim: To formulate orodispersible films of favipiravir and to study the effect of different superdisintegrants on various film properties.
 Methods: The method used to prepare the film is the solvent casting method. In this method, the solution is prepared using polymer, drug, and superdisintegrants. This solution is casted on a film-forming apparatus using a spreader an instrument to obtain a thin film.
 Results: The prepared oral films weights ranging from 148mg to 237mg based on the superdisintegrant concentration. The pH of the prepared films didn’t vary significantly and percent moisture absorption doesn’t have significant variation. However, the texture varied from smooth to rough and transparent to translucent. Disintegration time is varying from 28 to 42 seconds. The optimum batch formulation gave 98% of drug release.

Mouth Dissolving Tablets of Favipiravir using Superdisintegrants: Preparation, Optimization and In-vitro Evaluation

To formulate and evaluate the mouth dissolving tablet dosage forms of favipiravir using various superdisintegrants by using wet granulation technique.
 Batches of favipiravir Mouth dissolving tablets were formulated by using the wet granulation technique. The formulated granules were evaluated for their flow properties as a pre-compression parameter and the friability, hardness, disintegration, wetting ratio, wetting time, dissolution, and drug release parameters were evaluated as post-compression parameters. The effect of the varying concentrations of superdisintegrants on the formulation for disintegration time was ascertained and the results were compared.
 The tablet had friability and hardness values ranging from 0.60 to 0.68 % and 3.9 to 4.3 (kg/cm2). Tablet weights did not vary significantly but the disintegration time varied from 44.66 to 142.66±2.51 min and the wetting time varied from 45.33 to 144 min and the optimal batch of tablets shows a drug release of 98.8% within 60 min and first-order release kinetics of the formulations are compared.

Enhancing the Low Oral Bioavailability of Sulpiride via Fast Orally Disintegrating Tablets: Formulation, Optimization and In Vivo Characterization.

Sulpiride (SUL) is a dopamine D2-receptor antagonist used for management of GIT disturbance and it has anti-psychotic activities based on the administered dose. SUL undergoes P-glycoprotein efflux, which lead to poor bioavailability and erratic absorption. Therefore, the objective of this research was an attempt to enhance the oral bioavailability of SUL via formulation of fast disintegrating tablets (SUL-FDTs) with a rapid onset of action. A 32 full-factorial design was performed for optimization of SUL-FDTs using desirability function. The concentration of superdisintegrant (X1) and Prosolv® (X2) were selected as independent formulation variables for the preparation and optimization of SUL-FDTs using direct compression technique. The prepared SUL-FDTs were investigated regarding their mechanical strength, disintegration time, drug release and in vivo pharmacokinetic analysis in rabbits. The optimized formulation has hardness of 4.58 ± 0.52 KP, friability of 0.73 ± 0.158%, disintegration time of 37.5 ± 1.87 s and drug release of 100.51 ± 1.34% after 30 min. In addition, the optimized SUL-FDTs showed a significant (p < 0.01) increase in Cmax and AUC(0–∞) and a relative bioavailability of about 9.3 fold compared to the commercial product. It could be concluded that SUL-FDTs are a promising formulation for enhancing the oral bioavailability of SUL concomitant with a fast action.

Formulation of Fast Disintegrating Tablet Paracetamol Employing Selected Super-disintegrant

The objective of this research was to investigate paracetamol FDT formula with potato starch and xanthan gum or glycine or ac di sol combination that can produce the best tablet quality. The tablets were prepared by direct compression technique. Superdisintegrant such as Glycine, Ac di sol, Xanthan Gum, and Potato Starch Extract was optimized as 1-19 % on the basis of least disintegration time. Binders such as HPMC were optimized along with optimized superdisintegrant concentration. 3,5% HPMC was selected as optimum binder concentration on the basis of least disintegration time. Granule parameters included in the analysis were flowability, angle of repose, Carr’s index, Hausner’s ratio, and loss on drying (LOD). Tablet parameters included in the analysis were hardness, friability, disintegration time, dissolution, wetting time, and absorption ratio. The result was analyzed by Design Expert 11.1.0.1 program to decide the combination of superdisintegrant that can provide the best tablet qualities. The result showed that potato starch 15.162% and xanthan gum 4,838%, potato starch 15,050% and glycine 4,950%, and potato starch 18.390% and ac di sol 1.610%. Combination of superdisintegrant that can provide the best tablet qualities. It was concluded that, by employing commonly available pharmaceutical excipients such as superdisintegrants, hydrophilic and swellable excipients and proper filler, a fast disintegrating tablet of Paracetamol in tablet dosage form, were formulated successfully with desired characteristics.

Factorial design, formulation, in vitro and in vivo evaluation of rapid orally disintegrating tablets prepared by sublimation technique using captopril as a model drug

A factorial design (23) was applied to the formulation of rapid orally disintegrating tablets, in order to investigate the feasibility of using superdisintegrant and sublimation technique on the onset of antihypertensive action of captopril. The three independent factors, superdisintegrant (Ac-di-sol) concentration (2.5% or 5%), subliming agent type (menthol or camphor) and its concentration (5% or 10%), were studied for their main effects on three dependent responses, tablet hardness, disintegration time and in vitro drug release. Statistical analysis of obtained data and optimization of formulation variables were carried out using Design-Expert® software, which selected formulation (F10), prepared with 5% Ac-di-sol and 10% camphor, that displayed suitable in range hardness (3.425 ± 0.12 Kilopond), least disintegration time (17.48 ± 1.36 Seconds) and highest in vitro drug release (99.51 ± 0.24% after 8 min), as the optimum formulation with the highest desirability (0.937). F10 was then chosen for drug-excipients interaction studies (DSC and FTIR), accelerated stability study at 40 °C and 75% RH for 3 months and in vivo evaluation against conventional captopril tablets, in hypertensive rats, using tail-cuff method. F10 showed no interaction between drug and excipients, chemical and physical stability and 15 min faster normalization of mean arterial pressure, of hypertensive rats, than conventional captopril tablets.