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

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.

2021 ◽  
Vol 10 (5) ◽  
pp. 131-136
Author(s):  
Asim pasha ◽  
C N Somashekhar

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.


2019 ◽  
Vol 9 (6) ◽  
pp. 55-63 ◽  
Author(s):  
Mulchand A. Shende ◽  
Kajal D Chavan

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


Author(s):  
Bui Thi Thu Huong ◽  
Boonyaphat Monsatta ◽  
Nguyen Duc Hanh ◽  
Phan Hoang Doan Phuong ◽  
Do Quang Duong

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.


2021 ◽  
Vol 11 (2) ◽  
pp. 42-50
Author(s):  
Vandana Gupta ◽  
Ashish Manigauha

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


Author(s):  
Sabina Akhtar ◽  
Pulak Dev

Objective: The overall objective of the present study was to formulate the chewable multivitamin tablet prepared by direct compression method.Methods: The excipient used in this study are mannitol, sucrose, starch, talc, magnesium stearate, vanilla powder for the effective formulation. As it is multivitamin, ascorbic acid, riboflavin, nicotinamide, thiamine HCL are used and evaluated for precompression parameter. The chewable tablets were better presented using sweetener sucrose and vanilla powder as a flavouring agent. The formulated tablet was evaluated for post compression parameter. The chewable tablet are prepared to ensure that they are easily crushed by chewing. The tablet was evaluated for weight variation, hardness, thickness, friability, drug content. Their dissolution properties were assessed using USP (paddle apparatus).Conclusion: From the above study, we conclude that the chewable tablets were prepared by direct compression method and gave the satisfactory and acceptable result. The tablet shows immediate drug release due to direct compressed tabletResults: All the parameter were found within the specification. Drug content of ascorbic acid (103.62%-108.84%), riboflavin (99.88%-112.02%), nicotinamide (93.44%-100.31), thiamine Hcl (105.94%-108.5%) were found.


Author(s):  
Vo Thanh Hoa ◽  
Bui Thi Thu Huong ◽  
Do Quang Duong ◽  
Nguyen Duc Hanh

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.


Author(s):  
Rajeev Kumar ◽  
Sushant Kumar Shrivastava

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.


2013 ◽  
Vol 49 (4) ◽  
pp. 783-792
Author(s):  
Mangesh Machhindranath Satpute ◽  
Nagesh Shivaji Tour

The demand for fast dissolving tablets has been growing during the last decade, especially for elderly and children who have swallowing difficulties. In the present work, fast dissolving tablets of metoprolol tartrate, were prepared using sodium starch glycolate, sodium croscarmellose and crospovidone as superdisintegrants, by the direct compression method. The tablets prepared were evaluated for various parameters including weight variation, hardness, friability, in vitro dispersion time, drug-polymer interaction, drug content water absorption ratio, wetting time, in vitro drug release, FTIR and DSC studies. The tablets prepared by the direct compression method had a weight variation in the range of 145 mg to 152 mg, which is below ± 7.5%, a hardness of 3.6 kg/cm² to 4.5 kg/cm², percentage friability of 0.46% to 0.73%, in vitro dispersion time of 18 s to 125 s, drug content uniformity of between 98.12% and 100.03%, a water absorption ratio of 67% to 87%, wetting time of 32 sec. to 64 sec., and an in vitro drug release of 53.92% - 98.82% within 15 min. The IR spectral analysis and DSC study showed no drug interaction with formulation additives of the tablet, and the formulations indicated no significant changes in hardness, friability, drug content or in vitro drug release. Fast dissolving tablets of metoprolol tartrate have enhanced dissolution and will lead to improved bioavailability and more effective therapy.


2021 ◽  
Vol 11 (2) ◽  
pp. 54-64
Author(s):  
ARTI CHOURSIYA ◽  
◽  
DEEPIKA PANDIT ◽  

The present study was focused on preparation and evaluation of Lanzoprazole fast dissolving tablets. Lansoprazole (LAN) is a proton pump inhibitor drug and used for the treatment of gastric ulcer. Lansoprazole is acid labile drug and to avoid the acidic pH of the stomach LAN is formulated as oral fast dissolving tablets. Lansoprazole is the class II drug of the BCS classification and has a low aqueous solubility. Hence, to improve the solubility of the drug we have prepared Lansoprazole solid dispersion with poly ethylene glycol and complex with β cyclodextrin. Fast Dissolving tablets of LAN were formulated using different superdisintegrants like Sodium Starch Glycolate, Cross Povidone, Cross Carmellose Sodium by direct compression method. The prepared fast dissolving tablets were evaluated for various parameters like weight variation, hardness, friability, disintegration time, drug content, wetting time, in-vitro drug release and short term stability studies. Percentage weight variation, hardness, friability and drug content uniformity were found to be within the approved range for all the formulations. The in-vitro release studies showed that 99.6% of LAN within 90 sec. Overall, in the formulations prepared by the direct compression method, F3, which contains 6% CCS as super disintegrants release 99% of (LAN) in 2 min was found to be the best formulation. The results concluded that fast dissolving tablets of LAN showing enhanced dissolution might lead to improved bioavailability and effective therapy for gastric ulcer. KEYWORDS: β cyclodextrin, Cross Povidone, Fast dissolving tablets, Gastric ulcer, Lanzoprazole, Solid dispersion


2021 ◽  
Vol 11 (3-S) ◽  
pp. 1-6
Author(s):  
Nusrat Ahmed ◽  
Jesmin Akter ◽  
Sabrina Rahman Archie

Since orally disintegrating tablets (ODTs) of tramadol hydrochloride are not available in the market, so an attempt has been taken to formulate and evaluate ODT preparation of tramadol hydrochloride. In this present work, direct compression was the technique used for preparing ODT using superdisintegrants like croscarmellose sodium, sodium starch glycolate and crospovidone at different concentrations. Prepared formulations were evaluated for various quality parameters- angle of repose, Carr’s index, Hausner ratio, weight variation, friability, hardness, drug content, dispersion time, wetting time and in-vitro dissolution. The angle of repose data indicated that the flow property of all the formulations was good to excellent. Comparing with the specifications, the results of Carr's index (%) and Hausner’s ratio indicated that the flowability of all the formulations blend was significantly good. Prepared formulations showed average wetting time ranging from 40-45 seconds, average dispersion time with 3-6 minutes. In-vitro dissolution profile indicated the cumulative % drug release between 30-80% for most of the cases. Keywords: Orally disintegrating tablets, Tramadol hydrochloride, Superdisintegrants, Direct compression.


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