scholarly journals Optimasi Formula Tablet Effervescent Dispersi Padat Meloksikam Menggunakan Desain Faktorial

2018 ◽  
Vol 6 (2) ◽  
pp. 225
Author(s):  
Lusia Oktora Ruma Kumala Sari ◽  
Tiara Berlianti ◽  
Eka Deddy Irawan
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Factorial Design ◽  
Solid Dispersion ◽  
Software Design ◽  
Geriatric Patients ◽  
Two Factors ◽  
Optimum Formula ◽  
Effervescent Tablet

  An effervescent tablet of meloxicam solid dispersion has been developed for geriatric patients who have difficulty swallowing. The objective of this research was to know the optimum concentration of citric acid and sodium bicarbonate which produce the best effervescent tablet. A 2² factorial design was applied to investigate the effect of two factors: concentration of citric acid and sodium bicarbonate (effervescent materials) on hardness, dissolve time, and %drug released t30. Citric acid (6-18 mg) was used as acid source and sodium bicarbonate (18-105 mg) was used as base source. Software Design Expert trial version 10.0.5. was used to determine the optimum formula. The result showed that all formula satisfied the limit of hardness 2-4 kg/cm2 and friability <1%, but only formula (1), b, and ab that satisfied the limit of dissolve time <300 sec and %drug release t30 >70%. Formula A showed dissolve time 436 sec and %drug release t30 less than 70%. Desirability value of 0.917, which indicated the optimum formula, was obtained from the use of citric acid 6 mg and sodium bicarbonate 105 mg.   Keywords: meloxicam, effervescent tablet, solid dispersion, factorial design  

3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Batch Size ◽  
Metoprolol Succinate ◽  
Zero Order Kinetics ◽  
Two Factors ◽  
Puffed Rice ◽  
Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

Optimization and In Vitro Evaluation of Famotidine Loaded Effervescent Orally Disintegrating Tablets using a Central Composite Design

2021 ◽  
Vol 16 ◽  
Author(s):  
Ramesh Kumar ◽  
Ravinder Verma ◽  
Ritu Kaushik ◽  
Prerna Kaushik ◽  
Parijat Pandey ◽  
...  
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Central Composite Design ◽  
Pediatric Population ◽  
Direct Compression ◽  
Disintegration Time ◽  
Orally Disintegrating Tablets ◽  
Swallowing Problems ◽  
Central Composite

Background: Over the years, effervescent orally disintegrating tablets (ODTs) have proved their worth over conventional tablets in overcoming the swallowing problems associated with the geriatric and pediatric population. The addition of effervescent agents in ODT provides a rapid disintegration along with masking of the slightly bitter taste of drugs and is worth exploring. Objective: The present research investigation deals with the preparation of effervescent ODTs by direct compression with rapid disintegration and adequate hardness using the central composite design response surface methodology. Method: Central composite design was used to study the effect of concentration of crospovidone (X1) and concentration of citric acid and sodium bicarbonate (X2) as independent factors on the two responses: disintegration time (Y1) and drug release (Y2). The tablets were prepared by direct compression approach using directly compressible mannitol. Results: Central composite design was used to study the effect of concentration of crospovidone (X1) and concentration of citric acid and sodium bicarbonate (X2) as independent factors on the two responses: disintegration time (Y1) and drug release (Y2). The tablets were prepared by direct compression approach using directly compressible mannitol. Conclusion: The results obtained in the present investigation revealed a successful development of famotidine effervescent ODTs with a better release profile compared to marketed formulation.

scholarly journals Preparation and In vitro Evaluation of Theophylline Loaded Gastroretentive Floating Tablets of METHOCEL K4M

1970 ◽  
Vol 7 (1) ◽  
pp. 65-70 ◽  
Author(s):  
Ferdous Khan ◽  
Md Shaikhul Millat Ibn Razzak ◽  
Md Ziaur Rahman Khan ◽  
Kazi Rashidul Azam ◽  
Sams Mohammad Anowar Sadat ◽  
...  
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Release Rate ◽  
Lag Time ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Floating Tablets ◽  
Time Required

This investigation describes the preparation and in vitro evaluation of gastroretentive floating tablets of theophylline. Hydrophilic polymer METHOCEL K4M was used for its gel forming and release controlling properties. Sodium bicarbonate and citric acid were incorporated as gas generating agents. The effects of soluble components (sodium bicarbonate and citric acid), gel forming agent (METHOCEL K4M) and dose variation on drug release profile and floating properties were investigated. It has been observed that in all cases increase of the amount of floating agent caused a decrease of the floating lag time. Increase of theophylline load showed an increase of the floating lag time, which was independent of floating agent content. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixon-Crowell equations. The release rate, extent and mechanisms were found to be governed by the content of polymer and floating agent. The content of active ingredient was also a vital factor in controlling drug release pattern. It was found that polymer content and amount of floating agent significantly affected the time required for 50% of drug release (T50%), percentage drug release after 8 hours, release rate constant, and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed that the drug release mechanism could range from diffusion controlled to case II transport, which was mainly dependent on presence of relative amount of theophylline, polymer and floating agent. Key words: Gastroretention, Floating tablet, Theophylline  DOI = 10.3329/dujps.v7i1.1220 Dhaka Univ. J. Pharm. Sci. 7(1): 65-70, 2008 (June)

Optimization and Evaluation of Solubility-Modulated Gastroretentive Floating Matrix Tablet of Furosemide

2014 ◽  
Vol 7 (3) ◽  
pp. 2581-2589
Author(s):  
Anita Lalwani ◽  
D Bhalodiya ◽  
C Patel ◽  
L Panchal ◽  
P Shelat
Keyword(s):  
Experimental Design ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Delivery System ◽  
Solid Dispersion ◽  
Lag Time ◽  
Storage Conditions ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Scanning Calorimetry

The objective of the present study was to prepare delivery system for furosemide which has poor solubility and has specific absorption in stomach. Solid dispersion of furosemide (SD) was prepared in polyethylene glycol 6000 and characterized using differential scanning calorimetry. Floating gastroretentive tablets of the prepared solid dispersion were then prepared by wet granulation technique, using polymer Methocel K100M CR (HPMC) and sodium bicarbonate. A 32 factorial design was applied systematically to study the effect of the amount of HPMC (X1) and sodium bicarbonate (X2) on the floating lag time (YFLT) and amount of drug release at the end of 1st hr (Y60), 6th hr (Y360) and 12th hr (Y720). The solubility of SD was higher than that of drug alone and the physical mixture. The results of multiple regression analysis, when applied to responses obtained for experimental design batches, indicated that low level of HPMC and high level of sodium bicarbonate decreased the floating lag time, while the amount of drug released at all time points decreased with increase in level of HPMC. Swelling behavior of experimental design batches was studied and its relationship with mechanism of drug release was interpreted.  Batch D3 came close to satisfying the drug release and floating criteria. Drug compatibility with the excipients used was ascertained using FTIR. Stability studies were carried out at recommended storage conditions and the tablets were found to be stable. Delivery system could be developed for furosemide which addressed the solubility and site specificity issues of drug.  

scholarly journals Formulation and Evaluation of Gastro Retentive Floating Tablets of Simvastatin using Hydrophilic Rate Retardant

2012 ◽  
Vol 15 (2) ◽  
pp. 119-126 ◽  
Author(s):  
Md Nazmul Hussain ◽  
Md Abdullah Al Masum ◽  
Sharmin Akhter ◽  
Florida Sharmin ◽  
Md Selim Reza
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Release Rate ◽  
Dissolution Time ◽  
Drug Release Profile ◽  
Compression Technique ◽  
Weight Variation ◽  
Gastro Retentive

Gastro retentive floating tablet of Simvastatin was prepared by direct compression technique using Methocel K4M as the rate controlling polymer. The hydrophilic cellulose derivative, Methocel K4M was evaluated for its gel forming and release controlling properties. Sodium bicarbonate and citric acid were incorporated as gas generating agents. The effects of soluble components (sodium bicarbonate and citric acid) and gel forming agents on drug release profile and floating properties were investigated. The tablets from all formulations were evaluated for thickness, diameter, weight variation, hardness, and friability. The tablets were also tested for the buoyancy studies and in vitro drug release studies. The drug release study was evaluated for eight hours using USP XXII paddle-type dissolution apparatus using 0.1N HCl with 1% Sodium Lauryl Sulphate as dissolution medium. The release mechanisms were explored and explained with zero order, first order, Higuchi, Hixon Crowell and Korsmeyer equations. The release rate, extent and mechanisms were found to be governed by the polymer content. It was found that the mean dissolution time, percentage drug release, release rate constant and diffusion exponent were influenced significantly by the amount of polymer incorporation. DOI: http://dx.doi.org/10.3329/bpj.v15i2.12575 Bangladesh Pharmaceutical Journal 15(2): 119-126, 2012

scholarly journals Enhancement of Solubility of Lamotrigine by Solid Dispersion and Development of Orally Disintegrating Tablets Using 32 Full Factorial Design

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Jatinderpal Singh ◽  
Rajeev Garg ◽  
Ghanshyam Das Gupta
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Solid Dispersion ◽  
Disintegration Time ◽  
Drug Release Study ◽  
Orally Disintegrating Tablets ◽  
Wetting Time ◽  
Release Study ◽  
Full Factorial

Present investigation deals with the preparation and evaluation of orally disintegrating tablets (ODTs) of lamotrigine using β-cyclodextrin and PVP-K30 as polymers for the preparation of solid dispersion which help in enhancement of aqueous solubility of this BCS CLASS-II drug and sodium starch glycolate (SSG) and crospovidone as a superdisintegrating agent, to reduce disintegration time. The ODTs were prepared by direct compression method. Nine formulations were developed with different ratios of superdisintegrating agents. All the formulations were evaluated for disintegration time, weight variation, hardness, friability, drug content uniformity, wetting time, and in vitro drug release study. In vitro drug release study was performed using United States Pharmacopoeia (USP) type 2 dissolution test apparatus employing paddle stirrer at 50 rpm using 900 mL of 0.1 N HCl maintained at 37°C ± 0.5°C as the dissolution medium. On the basis of evaluation parameters formulations were prepared using β-CD 1 : 1 solid dispersion. Then 32 full factorial design was applied using SSG and crospovidone in different ratios suggested by using design expert 8.0.7.1 and optimized formulation was prepared using amount of SSG and crospovidone as suggested by the software. The optimized formulation prepared had disintegrating time of 15 s, wetting time of 24 s, and % friability of 0.55.

scholarly journals Formulation and Evaluation of Gastroretentive Floating Tablets of Quetiapine Fumarate

2021 ◽  
Vol 11 (3-S) ◽  
pp. 65-73
Author(s):  
Keyur S. Patel ◽  
Akshar N. Rao ◽  
Deepa R. Patel ◽  
Dhaval M. Patel ◽  
Advaita B. Patel
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Factorial Design ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Lag Time ◽  
Quetiapine Fumarate ◽  
Floating Tablets ◽  
Vitro Release

The objective of the present study was to develop gastroretentive floating tablets of quetiapine fumarate. The gastroretentive floating tablets of quetiapine fumarate were formulated using natrosol 250 HHX as a sustained release polymer and sodium bicarbonate as a gas forming agents.  A 32 factorial design was employed to study the influence of concentration of natrosol HHX 250 (X1) and concentration of sodium bicarbonate (X2) on the dependent variables % drug release at 1h (Y1), % drug release at 8 h (Y2) and floating lag time (Y3). The optimized formulation (O1) showed floating lag time 49 ± 3 sec and % drug release 99.54± 0.81 at 12 h. The in vitro release of F1-F9 batches were found in between 99.95 ± 1.18 %  to  86.32 ±1.71 % at 12 h. Floating lag time of F1-F9 batches were found to be 25± 2 sec to 178 ± 3 sec. FTIR studies shown that there was no  interaction between quetiapine fumarate and excipients. From the factorial design batches it was found that floating lag time was decreased with increasing the amount of sodium bicarbonate and decreasing the amount of natrosol 250 HHX. Here % release of drug was decreased with increase the extent of natrosol 250 HHX. The in-vitro release kinetics revealed Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion. Keywords: Quetiapine fumarate, Natrosol 250 HHX, Sodium bicarbonate, Gastroretentive floating tablets

scholarly journals FORMULATION AND OPTIMIZATION OF FLOATING TABLETS OF CLOPIDOGREL BISULPHATE USING DESIGN OF EXPERIMENTS

2018 ◽  
Vol 10 (6) ◽  
pp. 126
Author(s):  
Sanjeevani S. Deshkar ◽  
Arvind S. Pawara ◽  
Satish V. Shirolkar
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Factorial Design ◽  
Water Uptake ◽  
Lag Time ◽  
Matrix Tablets ◽  
Lower Percentage ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Bicarbonate Concentration

Objective: The present study aimed at designing of floating matrix tablet of clopidogrel bisulphate by design of experiments.Methods: The tablets were prepared by direct compression technique using hydroxypropyl methylcellulose K15 (HPMC) as a matrix polymer and sodium bicarbonate as a gas generating agent. In order to optimize the concentration of HPMC (X1) and sodium bicarbonate (X2), a 32 full factorial design was employed. The tablet formulations were evaluated for floating lag time (Y1), floating or buoyancy time (Y2), percent water uptake, and differential scanning calorimetry (DSC) and in vitro drug release (Y3).Results: The formulation variables, HPMC concentration, and sodium bicarbonate concentration exerted a significant effect on floating behavior and drug release characteristics of the tablet. The optimized formulation, with 15% sodium bicarbonate concentration and 30 % HPMC concentration resulted in 5±2.6 sec of floating lag time, 22.0±0.6 h of floating time and 42.0±0.99% of clopidogrel bisulphate release in 8 h of dissolution study. The drug release mechanism was identified as nonfickian. The water uptake studies revealed that with an increase in HPMC concentration, there was an increase in swelling index of tablet whereas higher sodium bicarbonate concentration supported the faster erosion of matrix tablets. DSC study revealed no interaction of drug and polymers. The lower percentage error between predicted and observed responses of the optimized formulation validated the design.Conclusion: The study demonstrated successful designing of floating clopidogrel bisulphate tablet with factorial design.

scholarly journals PREPARATION AND EVALUATION OF FAST DISSOLVING TABLETS OF PITAVASTATIN BY 32 FULL FACTORIAL DESIGN

2019 ◽  
pp. 108-114
Author(s):  
NIRMALA DASARI ◽  
VIDYAVATHI MARUVAJALA
Keyword(s):  
Drug Release ◽  
Water Absorption ◽  
Factorial Design ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Absorption Ratio ◽  
Conventional Film ◽  
Two Factors ◽  
The Stability

Objective: The objective of the present work was to prepare an optimized, fast dissolving tablet (FDT) of Pitavastatin to increase its dissolution by applying 32full factorial design. Methods: Nine formulations (PF1 to PF9) with all possible combinations according to 32full factorial design by selecting two factors i.e. concentration of super disintegrant, Indion414 (5-15%) (A) and sublimating agent, camphor (40-60%) (B) as independent variables at three levels of-1, 0 and 1. The effect of these two variables on three dependent parameters, water absorption ratio (Y1), disintegration time (Y2) and in vitro drug release (Y3) was studied. All the powder blends were evaluated for precompression parameters, and the tablets were prepared by direct compression method which were further evaluated for post-compression parameters. The effect of change in concentration of two selected factors on dependent parameters was studied through 3D surface response plots and polynomial equations using Design expert software version11. Optimized formula was obtained by desirability and overlay plots for which compatibility stability was assessed. Results: Precompression and post-compression parameters were satisfactorily within acceptable limits. Optimized formulation was prepared to prove the validity of the evolved mathematical model, which contained 6.75 mg of indion414(0.9) and 54 mg of camphor(0.9) with a disintegration time of 21 sec., water absorption ratio of 113 and 93% of drug release within 12 min. The compatibility between drugs and excipients was proved. The dissolution profiles of optimized formulation and commercially available conventional film-coated tablets of Pitavastatin were compared. Conclusion: The optimized formulation showed significantly (P>0.05) increased drug release compared to commercially available film-coated tablets. No changes in disintegration time, drug content and in in vitro drug release from optimized formulation on storage for 3months at 40 °C±2 °C/75% RH±5% RH were observed during stability studies which confirmed the stability of the optimized formulation.

scholarly journals Formulasi Sediaan Tablet Effervescent dari Ekstrak Etanol Tanaman Bundung (Actionoscirpus grossus) sebagai Antioksidan

2021 ◽  
Vol 7 (1) ◽  
pp. 128-139
Author(s):  
Noval Noval ◽  
Ilham Kuncahyo ◽  
Adam Ferdian Sigit Pratama ◽  
Syafira Nabillah ◽  
Roosma Hatmayana
Keyword(s):  
Citric Acid ◽  
Sodium Bicarbonate ◽  
Plant Extract ◽  
Metal Binding ◽  
Research Method ◽  
Negative Impact ◽  
The Body ◽  
Antioxidant Compounds ◽  
Bicarbonate Concentration ◽  
Optimum Formula

Bundung (Actinoscirpus grossus) is a plant that contains an antioxidant compound proven in previous studies, which has a moderate antioxidant or IC50 by 128 ppm. Antioxidant compounds can reduce the negative impact of oxidants, including metal binding enzymes and proteins. Antioxidant compounds act by donating one electron to the oxidant compound to inhibit oxidants activity. The purpose of this study was to formulate the Bundung plant extract into effervescent tablets, obtain effervescent samples that are physically stable, and can be used as antioxidants to inhibit free radicals in the body. The research method was experimental by using scoring parameters to determine the most optimal formulation. Physical evaluation includes organoleptic, weight uniformity, friability, hardness, and dissolving time. The results showed that the optimum formula was the formula I with a concentration of 68 mg of citric acid and sodium bicarbonate. Tablet effervescent is a brown color and characteristic odor of Bundung plant extract. Effervescent tablets have an weight uniformity (0.314 grams), friability (0.05%), hardness (7.75 ± 0.43 kg). Variations in citric acid and sodium bicarbonate concentration can affect uniformity, friability, hardness, and dissolving time. Room conditions cause this during the production process of effervescent tablets.

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