Tablet formulation of an active pharmaceutical ingredient with a sticking and filming problem: direct compression and dry granulation evaluations

2013 ◽  
Vol 41 (2) ◽  
pp. 333-341 ◽  
Author(s):  
Naveen K. Bejugam ◽  
Shravan K. Mutyam ◽  
Gita N. Shankar
Keyword(s):  
Active Pharmaceutical Ingredient ◽  
Tablet Formulation ◽  
Direct Compression ◽  
Dry Granulation

scholarly journals Effect of Extracted Microcrystalline Cellulose from Dracaenea arborea Stem on Aceclophenac Tablet Formulation

2021 ◽  
pp. 107-117
Author(s):  
J. I. Ordu ◽  
I. E. Udenze
Keyword(s):  
Drug Release ◽  
Corn Starch ◽  
Tablet Formulation ◽  
Qualitative Assessment ◽  
Crystalline Cellulose ◽  
Burst Release ◽  
Direct Compression ◽  
Drug Release Profile ◽  
Compression Technique ◽  
Hydration Capacity

Micro crystalline cellulose (MCC) is a major derivative from the bio composite of natural materials such as D. arborea plant stem. It could be useful as a secondary binder and disintegrant in tablet formulation especially following direct compression technique anticipating it to provide high level of disintegration at low use level and utilizing dual mechanisms of wicking and swelling. Tablets of aceclofenac a BCS class II and non steroidal anti inflammatory drug (NSAID) which potently inhibits the cyclo oxygenase enzyme (COX-2) involved in prostaglandin synthesis was formulated by direct compression using MCC from D. arborea stem. Qualitative assessment of the plant extract was carried out and the presence of cellulose confirmed by the appearance of violet – blue coloration while the physicochemical and physicotechnical properties were comparatively evaluated with reference to avicel and corn starch. Three batches of aceclofenac tablets involving Batch A (D. arborea MCC), Batch B (Corn starch) and Batch C (Corn starch and D. arborea MCC in a 1:1 ratio), were implcated in the formulation. Physicochemical study of the MCC reveals a pH of 7.8, mean swelling index 1.14±0.05 ml and hydration capacity of 3.60±0.15 g while the pH of corn starch is 3.90 with swelling and hydration capacity at 5.09±0.03 ml and 8.26±0.01 g respectively. Quality control evaluation of resulting tablet was investigated and the wetting time of batch A tablets was 1.50, batch B 2.30 and batch C 1.80 with percentage moisture content (%) of 60.5, 56.56 and 57.8 and disintegration time (minutes) of 0.22±0.07, 0.35±0.051 and 1.60±0.286 respectively. The drug release profile of batch A, reveals an initial burst release within 10 minutes followed by gradual release while batch C had consistent drug release which was maintained although faster than that of batch A after 10 minutes but batch B had the least drug release rate.

scholarly journals INHIBITION OF GASTRIC DEGRADATION OF OMEPRAZOLE USING A pH-SENSITIVE POLYMER AS A BINDER IN TABLET FORMULATION

2021 ◽  
pp. 331-335
Author(s):  
EMMANUEL O. OLORUNSOLA ◽  
IMO E. UDOH ◽  
STEPHEN O. MAJEKODUNMI ◽  
INIOBONG J. ODIONG ◽  
UWAKMFON O. EBONG
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Ph Sensitive ◽  
Tablet Formulation ◽  
Direct Compression ◽  
Dissolution Medium ◽  
Ultraviolet Spectrophotometry ◽  
Substantial Inhibition ◽  
Ph Sensitive Polymer

Objective: This work was aimed at formulating omeprazole tablets using afzelia gum as a binder that is capable of inhibiting the gastric degradation of the drug. Methods: Afzelia gum at different concentrations of 0, 5, 10, 15, 20 and 30% was used as a binder to formulate omeprazole tablets. The tablets were formulated by direct compression and the batches labelled F1 to F6 respectively. A batch containing 15% hydroxypropyl methylcellulose (F7) was also formulated. The tablets were characterized; and dissolution in a pH 1.2 dissolution medium over 120 min period was studied. Aliquots taken every 20 min were analyzed by ultraviolet spectrophotometry to determine the amount of drug released and not degraded. Results: Amounts of drug released and not degraded at time 120 min were 53.1%, 57.3%, 57.8%, 58.8%, 62.1%, 83.4% and 90.0% for F1 to F7 respectively. Conclusion: Afzelia gum at a concentration of 30% is suitable for use as a binder in tablet formulation of omeprazole to ensure substantial inhibition of gastric degradation of the drug.

scholarly journals Formulation of Furosemide Oral Disintegrating Tablets Using Natural and Synthetic Superdisintegrants by SeDeM Expert Design System

2019 ◽  
Vol 9 (6) ◽  
pp. 55-63 ◽  
Author(s):  
Mulchand A. Shende ◽  
Kajal D Chavan
Keyword(s):  
Active Pharmaceutical Ingredient ◽  
In Vitro Dissolution ◽  
Design System ◽  
Direct Compression ◽  
Compression Technique ◽  
Drug Content ◽  
Weight Variation ◽  
Preformulation Studies ◽  
Natural And Synthetic

SeDeM design expert technique used to evaluate the risks of poor flow of pharmaceutical powders under preformulation studies which reveals direct compression suitability and prepare robust composition of active pharmaceutical ingredient (API) and excipient in tablets formulation. The purpose of this study was to develop oral disintegrating tablets of Furosemide using different concentration of natural and synthetic superdisintegrants by means of SeDeM design technique. Oral disintegrating tablets (ODT) of Furosemide were prepared by direct compression technique using isolated banana powder and croscarmellose sodium (Ac-di-sol) together with microcrystalline cellulose as superdisintegrants. SeDeM design was performed to check suitability and deficient of excipients and drug for optimized composition derived based on IPP value. These tablets were evaluated for hardness, friability, drug content, weight variation, wetting time and in-vitro dissolution. All the formulations showed low weight variation with dispersion time less than 173.5±0.70 seconds and rapid in-vitro dissolution. The drug content of all the formulations was within the acceptable limits. Lubricated blend composition of F4 found average radius value 5.24, 0.66 and 5.509 for IGC, IP and IPP respectively, compressed tablet shown good physical properties. The optimized formulation F4 showed good release profile with 99.25 percentage drug release compared to other trial batches. It was concluded that natural superdisintegrant (banana powder) showed better disintegrating property than synthetic super disintegrant (Ac-di-sol) in the formulations of ODTs. Keywords: Furosemide, Oral disintegrating tablets, SeDeM expert system, Superdisintegrants

scholarly journals STUDY ON CAUSE-EFFECT RELATIONS AND OPTIMIZATION OF TABLETS CONTAINING AQUILARIA CRASSNA SPRAY-DRIED EXTRACT

2017 ◽  
Vol 9 (10) ◽  
pp. 312
Author(s):  
Bui Thi Thu Huong ◽  
Boonyaphat Monsatta ◽  
Nguyen Duc Hanh ◽  
Phan Hoang Doan Phuong ◽  
Do Quang Duong
Keyword(s):  
High Performance ◽  
Tablet Formulation ◽  
Simulated Gastric Fluid ◽  
Direct Compression ◽  
Disintegration Time ◽  
Independent Variables ◽  
Weight Variation ◽  
Dried Extract ◽  
Aquilaria Crassna ◽  
Spray Dried

Objective: The aim of this study was to develop and optimize the formulation of tablets containing Aquilaria crassna extract using the direct compression method.Methods: D-optimal design based on three independent variables was applied to evaluate the cause-effect relations and optimize the A. crassna tablet formulation. The weight variation (Y1), disintegration time (Y2), hardness (Y3) and friability (Y4) were investigated with respect to three independent variables including % dicalcium phosphate anhydrous (DCPA) in filler (X1), % filler (X2) and % croscarmellose sodium (CCNa) (X3). The dissolution study of the optimized A. crassna tablets were investigated in simulated gastric fluid (SGF) (pH 1.2) using a validated high-performance liquid chromatography (HPLC) method for mangiferin analysis.Results: All investigation factors were found to have significant effects on the physical properties of A. crassna tablet. The tablet hardness and the disintegration time increased in positive relations with the ratios of DCPA. The results exhibited the negative relations between disintegration time and the percentages of CCNa. The optimized A. crassna tablet formulation which included 35 % (w/w) DCPA in filler, 60 % (w/w) filler and 7% (w/w) CCNa possessed the weight variation of 1.38 % (w/w), the disintegration time of 6.29 min, the hardness of 85.63 N and the friability of 0.41 % (w/w). The optimized A. crassna tablet formulation was experimentally examined which demonstrated a good agreement between the experimental and predicted values. Mangiferin was found to release completely from the optimized A. crassna tablets within 30 min.Conclusion: The cause-effect relations and optimization of A. crassna tablet formulation were investigated and reported for the first time. The A. crassna spray-dried extract could be formulated into tablet by direct compression method with good mechanical properties and acceptable release profile.

scholarly journals Modification of natural hydrocolloid as disintegrant in aceclofenac tablet formulation

2021 ◽  
Vol 11 (2) ◽  
pp. 42-50
Author(s):  
Vandana Gupta ◽  
Ashish Manigauha
Keyword(s):  
Comparative Investigation ◽  
Gel Strength ◽  
Tablet Formulation ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Compression Method ◽  
Reaction Conditions ◽  
Disintegration Time ◽  
Evaluation Parameters ◽  
Chemical Cross Linking

The purpose of present exploration was to modify kappa (k)-Carrageenan, by crosslinking, and assessed it as a tablet disintegrant to strengthen the solubility of the drug (aceclofenac) in tablet formulation. Modified k-Carrageenan was synthesized by reacting it with epichlorhydrin at heterogenous  conditions. The swelling action of the product was investigated in order to optimize reaction circumstances for chemical cross-linking. Best modified k-Carrageenan procured by optimizing the reaction conditions and it was characterized for swelling index, particle size distribution, solubility, viscosity, gel strength and Fourier transform infrared spectroscopy (FTIR). Influence of modified k-Carrageenan on dissolution profile of therapeutic was also investigated along with other evaluation parameters. Modified k-Carrageenan exhibiting significant swelling index which is comparable to that of superdisintegrants. On comparative investigation as a tablet disintegrant by preparing anhydrous dicalcium phosphate tablet, modified k-Carrageenan showed disintegration time less than 20 seconds. Dissolution of aceclofenac (Class II) tablet formulaion utilizing modified k-Carrageenan was comparable with commercially available superdisintegrants. Faster dissolution of the accommodated drug was achieved with modified k-Carrageenan which was comparable with dissolution of the tablet formulation containing other superdisintegrants. The competent concentration of k-Carrageenan was found to be 5-15% as tablet disintegrant. Modified k-Carrageenan might be encouraging tablet disintegrant in fast dissolving formulations and can be worn in direct compression method. Keywords: k-Carageenan. Epichlorhydrin. Aceclofenac. Crosslinking. Superdisintegrant

scholarly journals A REVIEW ON CO-PROCESSED EXCIPIENTS: CURRENT AND FUTURE TREND OF EXCIPIENT TECHNOLOGY

2019 ◽  
Vol 11 (1) ◽  
pp. 1
Author(s):  
Liew Kai Bin ◽  
Anand Gaurav ◽  
Uttam Kumar Mandal
Keyword(s):  
Active Pharmaceutical Ingredient ◽  
Future Trend ◽  
Pharmaceutical Manufacturing ◽  
Direct Compression ◽  
Future Trends ◽  
Formulation Development ◽  
Compression Method ◽  
Novel Concept ◽  
Tablet Preparation ◽  
A Current

There is no single-component excipient fulfills all the requisite performance to allow an active pharmaceutical ingredient to be formulated into a specific dosage form. Co-processed excipient has received much more attention in the formulation development of various dosage forms, specially for tablet preparation by direct compression method. The objective of this review is to discuss the emergence of co-processed excipients as a current and future trend of excipient technology in pharmaceutical manufacturing. Co-processing is a novel concept of combining two or more excipients that possess specific advantages that cannot be achieved using a physical admixture of the same combination of excipients. This review article discusses the advantages of co-processing, the need of co-processed excipient, general steps in developing co-processed excipient, limitation of co-processed excipient, technologies used in developing co-processing excipients, co-processed excipients in the literature, marketed products and future trends. With advantages offered by the upcoming newer combination of excipients and newer methods of co-processing, co-processed excipients are for sure going to gain attraction both from academia and pharmaceutical industry. Furthermore, it opens the opportunity for development and use of single multifunctional excipient rather than multiple excipients in the formulation.

scholarly journals CAUSE-EFFECT RELATIONS AND OPTIMIZATION OF TABLET CONTAINING EUCOMMIA ULMOIDES AND GARDENIA JASMINOIDES SPRAY-DRIED EXTRACTS

2018 ◽  
Vol 10 (7) ◽  
pp. 33
Author(s):  
Vo Thanh Hoa ◽  
Bui Thi Thu Huong ◽  
Do Quang Duong ◽  
Nguyen Duc Hanh
Keyword(s):  
Tablet Formulation ◽  
Direct Compression ◽  
Compression Method ◽  
Active Ingredients ◽  
Disintegration Time ◽  
Independent Variables ◽  
Gardenia Jasminoides ◽  
Weight Variation ◽  
Dried Extract ◽  
Spray Dried

Objective: The E. ulmoides and G. jasminoides (EG) tablets containing 67 mg E. ulmoides spray-dried extract (ESE) and 173 mg G. jasminoides spray-dried extract (GSE) were prepared by employing the direct compression method. Due to the poor flowability and compressibility of the two spray-dried extracts, various excipients were added at different ratios so that the blends can be compressed into tablets with the required standards. This study aimed at the cause-effect relations and optimization of the EG tablet formulation.Methods: Different diluents including dibasic calcium phosphate anhydrous (DCPA), silicified microcrystalline cellulose (SMCC), spray-dried lactose (SDL) and the active ingredients (blend of ESE and GSE at the ratio of 67:173, w/w) were separately investigated their own physical properties. The binary mixtures of the active ingredients with different ratios of DCPA, SMCC, and SDL were evaluated their flowability. D-optimal design based on three independent variables (% DCPA, % croscarmellose sodium (CCS) and % SMCC) was applied to evaluate the cause-effect relations and optimize the EG tablet formulation. The weight variation, disintegration time, hardness and friability were investigated as four dependent variables.Results: The flowability of the powders was found to be affected by the particle size distribution, particle shape and density. The three diluents could significantly improve the flowability of the active ingredients. All independent variables had significant effects on the dependent variables. An increase in % SMCC reduced the weight variation, hardness and increased the friability of tablets. Disintegration time was found to be in the negative relations with % CCS. The tablet hardness was in positive relations with % DCPA. The optimized EG tablet formulation composed of 9 % DCPA (w/w), 35 % SMCC (w/w), and 14 % CCS (w/w) of the excipient blend. The weight variation, disintegration time, hardness and friability of the optimized EG tablets were found to be 1.8 %, 11.7 min, 61.4 N, and 0.5 %, respectively.Conclusion: The ESE and GSE could be formulated into tablet by using direct compression method. The cause-effect relations and optimization of EG tablet formulation were studied and reported for the first time.

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