Flexibility in tablet formulation by use of lactose based direct compression compounds

2007 ◽  
pp. 112-115
Author(s):  
Klaus Peter Aufmuth
Keyword(s):  
Tablet Formulation ◽  
Direct Compression

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 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 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.

scholarly journals Formulation Study of a Co-Processed, Rice Starch-Based, All-in-One Excipient for Direct Compression Using the SeDeM-ODT Expert System

2021 ◽  
Vol 14 (10) ◽  
pp. 1047
Author(s):  
Karnkamol Trisopon ◽  
Nisit Kittipongpatana ◽  
Phanphen Wattanaarsakit ◽  
Ornanong Suwannapakul Kittipongpatana
Keyword(s):  
Expert System ◽  
Tablet Formulation ◽  
Physical Mixture ◽  
Rice Starch ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Drug Content ◽  
Weight Variation ◽  
Pharmaceutical Properties

A co-processed, rice starch-based excipient (CS), previously developed and shown to exhibit good pharmaceutical properties, is investigated as an all-in-one excipient for direct compression (DC). An SeDeM-ODT expert system is applied to evaluate the formulation containing CS, in comparison with those containing the physical mixture and the commercial DC excipients. The results revealed that CS showed acceptable values in all six incidence factors of the SeDeM-ODT diagram. In addition, the comprehensive indices (IGC and IGCB) were higher than 5.0, which indicated that CS could be compressed with DC technique without additional blending with a disintegrant in tablet formulation. The formulation study suggested that CS can be diluted up to 60% in the formulation to compensate for unsatisfactory properties of paracetamol. At this percentage, CS-containing tablets exhibited narrow weight variation (1.5%), low friability (0.43%), acceptable drug content (98%), and rapid disintegration (10 s). The dissolution profile of CS displayed that more than 80% of the drug content was released within 2 min. The functionality of CS was comparable to that of high functionality excipient composite (HFEC), whereas other excipients were unsuccessful in formulating the tablets. These results indicated that CS was a suitable all-in-one excipient for application in DC of tablets.

scholarly journals Formulation & Evaluation of Effervescent Tablet of Verapamil Hydrochloride

2021 ◽  
pp. 81-89
Author(s):  
Rajeev Kumar ◽  
Sushant Kumar Shrivastava
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Tablet Formulation ◽  
Direct Compression ◽  
Compression Technique ◽  
Verapamil Hydrochloride ◽  
Floating Tablets ◽  
Weight Variation ◽  
Karaya Gum ◽  
Effervescent Tablet

The chief aim of the present investigation is to study the Formulation & Evaluation of Effervescent Tablet of Verapamil Hydrochloride. The floating tablets of verapamil hydrochloride were prepared by direct compression technique. For each tablet formulation,  drug, HPMC-K15M, karaya gum, sodium bicarbonate, and diluents were blended homogeneously for 10 min followed by addition of magnesium stearate. The total weight of each tablet was 300 mg. The amount of karaya gum used was in the range of 40–90 mg, whereas HPMC was used in the range of 20-40 mg. The powder mixture was further mixed for 5 min in a mortar. The resultant mixture was compressed into tablets using a Rimek rotary tablet machine. After preparation, the formulations were evaluated by various parameters. The friability of the tablet formulation varied between 0.3 ± 0.0063 to 0.59 ± 0.0076%. The weight variation of prepared tablet formulation complies with USP limits. The thickness was found to be in the range of 4.1 ± 0.48 to 4.2 ± 0.76 mm. The assay for drug content varied between 96.53 ± 0.36 to 102.03 ± 0.52%. The B1, B5, B6, B9, and B10 exhibited more than 75% drug release at 12 h. The B1 exhibited a maximum of 30 % drug release in the 1st hour and constant release for almost up to 12 h. B8 showed the least drug release among all other formulations; this may be due to the formation of a thick gel barrier on the tablet. Tablets were prepared by direct compression. Technological characteristics of floating tablets were within the Pharmacopoeial limit. Tablets floated for more than 8 h. Complete swelling was achieved by the end of 8 h, so percent swelling was determined at the end of 8 h for all the developed formulations.

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