Development of Prolonged Action, Bioadhesive and Slowly Dissolving Minitablets

2010 ◽  
Vol 93-94 ◽  
pp. 425-428
Author(s):  
Noppawan Choudbua ◽  
Thawatchai Phaechamud ◽  
Garnpimol C. Ritthidej
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Direct Compression ◽  
Flow Properties ◽  
Compression Method ◽  
Prolonged Action ◽  
Mixed Powder ◽  
Multiple Unit ◽  
Spray Dried

Minitablets can be used either single or multiple unit sustained release dosage form. The objectives of this study were to prepare and evaluate the prolonged action, bioadhesive and slowly dissolving minitablets. The minitablets (Ø 2.5 mm, 7 mg) were prepared by direct compression method using 75%w/w of various hydrophilic polymers: hydroxypropylcellulose (HPC), hydroxypropyl methylcellulose (HPMC), carboxy methylcellulose (CMC), pectin (PT) and chitosan (CS). Spray dried lactose was used as diluent. Prior to compression, the angle of repose, bulk-tab density and %compressibility of each mixed powder were evaluated. The rate of hydration and erosion of the obtained minitablets were carried out in phosphate buffer (pH 7.4). The powder blends containing HPC, CMC or HPMC showed satisfactory flow properties and compressibility. Accordingly, the prepared matrix tablets of HPC, CMC and HPMC showed good physical properties such as hardness, while those of CS and PT showed poor properties. The degree of swelling were ranked as CS>CMC>PT>HPC>HPMC, while the erosion were ranked as CMC≈HPMC≈PT > HPC≈CS. Adhesion time of these minitablets on isolated pig intestine was >30 min for CMC, PT and CS tablets while HPC and HPMC tablets exhibited weaker bioadhesion. In conclusion, among tested polymers, CS, PT and CMC were appropriate for prolonged action, bioadhesive and slowly dissolving minitablets.

scholarly journals Comparative Study of Natural and Synthetic Superdisintegrants in Orodispersible Metformin Tablet

2019 ◽  
Vol 7 (3) ◽  
pp. 46-53
Author(s):  
Anupam Kumar Sachan
Keyword(s):  
Comparative Study ◽  
Angle Of Repose ◽  
Metformin Hydrochloride ◽  
Wet Granulation ◽  
Direct Compression ◽  
Flow Properties ◽  
Compression Method ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Natural And Synthetic

Objective: The main objective of this study is comparative study of natural and synthetic superdisintegrants in orodispersible Metformin tablet by using direct compression method and wet granulation method. Method: Orodispersible Metformin tablet were prepared by wet granulation method and direct compression method by using different synthetic and natural superdisintegrants. Orodispersible tablets (ODTs) have received more interest in the pharmaceutical industry for their easy to use and self medication. ODTs overcome the problem of dysphagia (difficulty in swallowing) in the all group age of patients and advantage particularly for the paediatric and geriatric patients. Metformin hydrochloride (Hcl) is an orally administered antihyperglycemic agent, used in the management of non-insulin dependent (type-2) diabetes mellitus. Metformin orodispersible tablet is prepared by using two methods i.e. direct compression method and wet granulation method. Both methods are applied to prepare Orodispersible Metformin tablet. Orodispersible tablet of Metformin was prepared by using superdisintegrants from both natural and synthetic origin. In natural superdisintegrants we used the mucilage of Fenugreek and Lepidium sativum. In synthetic superdisintegrants we used crospovidone and sodium starch glycolate. Conclusion: In direct compression and wet granulation method final blend and granules were evaluated the flow properties like bulk density, tapped density, compressibility index, hausner’s ratio and angle of repose. The values of precompression parameter evaluated were found to be within the prescribed limit and indicated good flow properties. The data obtained from the post compression methods was studied. Other parameters such as wetting time, water absorption ratio were also evaluated. The formulation (F5) containing 10% crospovidone prepared by wet granulation method was found the optimize formulation. Keywords: Metformin Hcl, Orodispersible tablets, Superdisintegrants, Direct Compression, and Wet granulation Objective: The main objective of this study is comparative study of natural and synthetic superdisintegrants in orodispersible Metformin tablet by using direct compression method and wet granulation method. Method: Orodispersible Metformin tablet were prepared by wet granulation method and direct compression method by using different synthetic and natural superdisintegrants. Orodispersible tablets (ODTs) have received more interest in the pharmaceutical industry for their easy to use and self medication. ODTs overcome the problem of dysphagia (difficulty in swallowing) in the all group age of patients and advantage particularly for the paediatric and geriatric patients. Metformin hydrochloride (Hcl) is an orally administered antihyperglycemic agent, used in the management of non-insulin dependent (type-2) diabetes mellitus. Metformin orodispersible tablet is prepared by using two methods i.e. direct compression method and wet granulation method. Both methods are applied to prepare Orodispersible Metformin tablet. Orodispersible tablet of Metformin was prepared by using superdisintegrants from both natural and synthetic origin. In natural superdisintegrants we used the mucilage of Fenugreek and Lepidium sativum. In synthetic superdisintegrants we used crospovidone and sodium starch glycolate. Conclusion: In direct compression and wet granulation method final blend and granules were evaluated the flow properties like bulk density, tapped density, compressibility index, hausner’s ratio and angle of repose. The values of precompression parameter evaluated were found to be within the prescribed limit and indicated good flow properties. The data obtained from the post compression methods was studied. Other parameters such as wetting time, water absorption ratio were also evaluated. The formulation (F5) containing 10% crospovidone prepared by wet granulation method was found the optimize formulation. Keywords:

scholarly journals Formulation and evaluation of floating bioadhesive Doxofylline tablets

2017 ◽  
Vol 8 (4) ◽  
Author(s):  
Bhukya Nagaraju ◽  
B Ramu ◽  
S V Saibaba ◽  
B Rajkamal
Keyword(s):  
Quality Control ◽  
Angle Of Repose ◽  
Direct Compression ◽  
Flow Properties ◽  
Compression Method ◽  
Retarding Effect ◽  
Control Evaluation ◽  
Tapped Density ◽  
Evaluation Parameters ◽  
Gastro Retentive

<p>In the present work, an attempt has been made to develop gastro retentive floating tablets of Doxofylline<strong> .</strong>HPMC K4M and carbopol were used as controlled release polymers<strong>.</strong> All the formulations were prepared by direct compression method on 12 station rotary tablet punching machine. The blend of all the formulations showed god flow properties such as angle of repose, bulk density, tapped density. The prepared tablets were shown good post compression parameters and they passed all the quality control evaluation parameters as per I.P limits. FH 5 was the best optimized floating formulation because it released drug completely in 12hrs.It was also observed that the increasing concentration of polymers had a retarding effect on the drug release from the polymer matrices.</p>

Optimization of Microcrystalline Cellulose PH 101, Lactose, and Kollidon® K 30 To Obtain Co-Processed Excipient Through Spray Drying

2017 ◽  
Vol 7 (2) ◽  
Author(s):  
Kusuma P. ◽  
Syukri Y ◽  
Sholehuddin F. ◽  
Fazzri N. ◽  
Romdhonah . ◽  
...  
Keyword(s):  
Spray Drying ◽  
Microcrystalline Cellulose ◽  
Chemical Change ◽  
Direct Compression ◽  
Flow Properties ◽  
Scanning Calorimetry ◽  
Compression Process ◽  
Infrared Spectrophotometer ◽  
Physical Mixtures ◽  
Spray Dried

The most efficient tablet processing method is direct compression. For this method, the filler-binder can be made by coprocessing via spray drying method. The purpose of this study was to investigate the effect of spray dried co-processing on microcrystalline cellulose (MCC) PH 101, lactose and Kollidon® K 30 as well as to define the optimum proportions. Spray dried MCC PH 101, lactose, and Kollidon® K 30 were varied in 13 different mixture design proportions to obtain compact, free-flowing filler-binder co-processed excipients (CPE). Compactibility and flow properties became the key parameters to determine the optimum proportions of CPE that would be compared to their physical mixtures. The result showed that the optimum proportion of CPE had better compactibility and flow properties than the physical mixtures. The optimum CPE, consisting of only MCC PH 101 and Kollidon® K 30 without lactose, that were characterized using infrared spectrophotometer, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscope (SEM) indicated no chemical change therein. Therefore, this study showed that spray dried MCC PH 101, lactose and Kollidon® K 30 could be one of the filler-binder alternatives for direct compression process.

scholarly journals The Effect of Manufacturing Methods and Different Shapes on the Release Pattern of Diclofenac Sodium Matrix Tablet

1970 ◽  
Vol 2 (2) ◽  
pp. 76-80
Author(s):  
Tajnin Ahmed ◽  
Muhammad Shahidul Islam ◽  
Tasnuva Haque ◽  
Mohammad Abusyed
Keyword(s):  
Sustained Release ◽  
Release Rate ◽  
Diclofenac Sodium ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Release Pattern ◽  
Peg 600

In the present study sustained release diclofenac sodium matrix tablets were prepared using Kollidon SR polymer. Hydroxypropyl methylcellulose (HPMC 15 cps) and poly ethylene glycol (PEG-600) polymers respectively were used in formulating tablets prepared by direct compression and wet granulation methods. The polymers were used to explore the release pattern of the drug into the dissolution media. The tablets were also prepared in various shapes (caplet oval, round oval and flat oval). A comparatively higher release rate of drug was obtained from the polymer HPMC 15 cps at 10% concentration for directly compressed matrix tablet than those containing 20% of HPMC after a definite period of time. In wet granulation process, 10% PEG-600 containing tablets showed a better release than those containing 20% PEG. The drug release was also found to be sustained in case of wet granulation method than that of the direct compression method. Again the caplet shaped tablets in case of direct compression method showed better release rate of drug than those of the round oval and flat oval shaped tablets. Thus the result of this study shows that the proper selection of the percentage of polymer and the suitable shape of tablet and proper manufacturing method can provide a greater opportunity in designing sustained release dosage forms. Key words: Matrix tablet; release pattern; direct compression; wet granulation; PEG 600; Kollidon SR.DOI: 10.3329/sjps.v2i2.5828Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 76-80

scholarly journals Effect of a co-processed excipient on the disintegration and drug release profile of ibuprofen tablets

Bio-Research ◽  
2020 ◽  
Vol 18 (1) ◽  
Author(s):  
BB Mohammed ◽  
EJ John ◽  
NK Ajuji
Keyword(s):  
Drug Release ◽  
Release Profile ◽  
Angle Of Repose ◽  
Oral Dosage ◽  
Direct Compression ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
Crushing Strength ◽  
Tablet Properties ◽  
Spray Dried

Tablets at present, remain the most preferred oral dosage form because of many advantages they offer to formulators as well as physicians and patients. The objective of this work was to determine the effect of co-processing on the disintegration and drug-release profile of ibuprofen tablets prepared from a co-processed excipient. The co-processed excipient (CE) containing lactose, gelatin and mucin in the ratio 90:9:1 was prepared using co-fusion. The excipient was evaluated for its physicochemical properties and then used to formulate tablets with the addition of a disintegrant by direct compression. The tablets were evaluated for their tablet properties and compared with tablets prepared with cellactose- 80® (CEL) and spray dried lactose® (SDL) and a physical mix (PM) of the co-processed ingredient. Results from evaluation of CE showed that flow rate, angle of repose, Carr’s index and Hausner’s ratio were 5.28 g/sec, 20.30o, 23.75 % and 1.31, respectively. Tablets prepared with CE had friability (0%), crushing strength (5.25) KgF, disintegration time (3 mins) and T50% (2 mins). For CEL, friability (0.4 %), crushing strength (7.25) KgF, disintegration time (1 min) and T50% (2 mins); SDL, friability (1.57 %), crushing strength (7.50) KgF, disintegration time (4 mins) and T50% (2 mins) and PM, friability (2.38 %), crushing strength (5.00) KgF, disintegration time (1 min) and T50% (2 mins). In conclusion, the disintegration time and drug release profile for CE was not superior but compared favorably with CEL, SDL and PM.  

scholarly journals Repurposing Butenafine as An Oral Nanomedicine for Visceral Leishmaniasis

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 353 ◽  
Author(s):  
Adriana Bezerra-Souza ◽  
Raquel Fernandez-Garcia ◽  
Gabriela F. Rodrigues ◽  
Francisco Bolas-Fernandez ◽  
Marcia Dalastra Laurenti ◽  
...  
Keyword(s):  
Drug Stability ◽  
Drug Loading ◽  
Cost Effective ◽  
Angle Of Repose ◽  
Proof Of Concept ◽  
Flow Properties ◽  
Non Invasive ◽  
Long Duration ◽  
Effective Drugs ◽  
Spray Dried

Leishmaniasis is a neglected tropical disease affecting more than 12 million people worldwide, which in its visceral clinical form (VL) is characterised by the accumulation of parasites in the liver and spleen, and can lead to death if not treated. Available treatments are not well tolerated due to severe adverse effects, need for parenteral administration and patient hospitalisation, and long duration of expensive treatments. These treatment realities justify the search for new effective drugs, repurposing existing licensed drugs towards safer and non-invasive cost-effective medicines for VL. In this work, we provide proof of concept studies of butenafine and butenafine self-nanoemulsifying drug delivery systems (B-SNEDDS) against Leishmania infantum. Liquid B-SNEDDS were optimised using design of experiments, and then were spray-dried onto porous colloidal silica carriers to produce solid-B-SNEDDS with enhanced flow properties and drug stability. Optimal liquid B-SNEDDS consisted of Butenafine:Capryol 90:Peceol:Labrasol (3:49.5:24.2:23.3 w/w), which were then sprayed-dried with Aerosil 200 with a final 1:2 (Aerosil:liquid B-SNEDDS w/w) ratio. Spray-dried particles exhibited near-maximal drug loading, while maintaining excellent powder flow properties (angle of repose <10°) and sustained release in acidic gastrointestinal media. Solid-B-SNEDDS demonstrated greater selectivity index against promastigotes and L. infantum-infected amastigotes than butenafine alone. Developed oral solid nanomedicines enable the non-invasive and safe administration of butenafine as a cost-effective and readily scalable repurposed medicine for VL.

scholarly journals FORMULATION DEVELOPMENT AND CHARACTERIZATION OF FAST DISSOLVING TABLET OF ATENOLOL BY DIRECT COMPRESSION METHOD

2021 ◽  
Vol 9 (10) ◽  
pp. 1277-1286
Author(s):  
Sarvesh Patel ◽  
◽  
Jai Narayan Mishra ◽  
Dhaneswar Kumar Vishwakarma ◽  
◽  
...  
Keyword(s):  
Uv Spectroscopy ◽  
Magnesium Stearate ◽  
Angle Of Repose ◽  
Project Work ◽  
Direct Compression ◽  
Formulation Development ◽  
Compression Method ◽  
Weight Variation ◽  
Compression Parameter ◽  
Hypertensive Drug

Finally in the project work Atenolol is an anti-hypertensive drug. It has been formulated into fast dissolving tablets by direct compression method by using the Excipients like lactose, sucrose magnesium stearate, sodium lauryl and sulphate and many type super disintegrates such as crosscarmellose and sodium starch glycolate and the prepared by the tablets were evaluated for the pre-compression parameter such as angle of repose, bulk density, tapped density, % index, Hausners ratio, partition coefficients, melting points, UV spectroscopy, % assay, TLC, loss on drying and post compression parameter such as thickness, hardness, friability, drugs contents, weight variation, water absorbance ratio, Invitro disintegrating time , Invitro dissolution studies. All the parameter shows good results. FDTs are prepared by direct compression method are results found to be that the among of nine formulation as the F9 to be best as its shows 87.10% (direct compression method) maximum drug release respectively. The stability testing of manufactured tablets have being at 400 c having 75% relativity humidity for 1month and found to be stable. Prepared fast dissolving tablets of Atenolol 10 mg was found to be under fasting federal condition.

scholarly journals Evaluation and Comparison of Three Types of Spray Dried Coprocessed Excipient Avicel® for Direct Compression

2018 ◽  
Vol 2018 ◽  
pp. 1-15 ◽  
Author(s):  
Pavlína Vodáčková ◽  
Barbora Vraníková ◽  
Petra Svačinová ◽  
Aleš Franc ◽  
Jan Elbl ◽  
...  
Keyword(s):  
Tensile Strength ◽  
Negative Charge ◽  
Electrostatic Charge ◽  
Direct Compression ◽  
Nonspherical Particles ◽  
Flow Properties ◽  
Sem Images ◽  
Pycnometric Density ◽  
Ejection Force ◽  
Spray Dried

As coprocessed excipients (CPE) gain a lot of focus recently, this article compares three commercially available CPE of Avicel brand, namely, CE 15, DG, and HFE 102. Comparison is based on measured physical properties of coprocessed mixtures, respectively, flow properties, pycnometric density, mean particle size, specific surface area, moisture content, hygroscopicity, solubility, pH leaching, electrostatic charge, SEM images, and DSC. Tablets were made employing three pressure sets. Viscoelastic properties and ejection force were assessed during compression, as well as pycnometric density, mass uniformity, height, tensile strength, friability, disintegration, and wetting times. Avicel CE 15 is of mid-range flow properties, contains mid-size and nonspherical particles, and has high hygroscopicity, growing negative charge, best lubricity, lowest tensile strength, and mid-long disintegration times. Avicel DG possesses the worst flow properties, small asymmetrical particles, lowest hygroscopicity, stable charge, intermediate lubricity, and tensile strength and exhibits fast disintegration of tablets. Finally, Avicel HFE 102 has the best flow properties, large symmetrical particles, and middle hygroscopicity and its charge fluctuates throughout blending. It also exhibits inferior lubricity, the highest tensile strength, and slow disintegration of tablets. Generally, it is impossible to select the best CPE, as their different properties fit versatile needs of countless manufacturers and final products.

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 IMPACT OF HYDROXYPROPYL METHYLCELLULOSE (HPMC) TYPE AND CONCENTRATION ON THE SWELLING AND RELEASE PROPERTIES OF PROPRANOLOL HYDROCHLORIDE MATRIX TABLETS USNING A SIMPLEX CENTROID DESIGN

2019 ◽  
pp. 143-151
Author(s):  
PAKORN KRAISIT
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Direct Compression ◽  
Propranolol Hydrochloride ◽  
Buffer Solution ◽  
Solution Ph ◽  
Vitro Release

Objective: To prepare hydroxypropyl methylcellulose (HPMC) matrix tablets of propranolol hydrochloride (PNL) using a simplex centroid design. Methods: HPMC matrix tablets with different amounts and types of HPMC were prepared by direct compression. A simplex centroid design was used to evaluate tablet weight (Y1), thickness (Y2), hardness (Y3), axial swelling time at 0.5–12 h (Y4-Y9), radial swelling time at 0.5–12 h (Y10-Y15), and % released at 1–12 h (Y16-Y19). Results: The tablet weight, thickness, and hardness were 397.6–400.4 mg, 3.967–4.029 mm, and 106.9–139.0 N, respectively. The % swelling (axial) and % swelling (radial) at 0.5–12 h were-8.715 to 59.889 and-1.887 to 49.287, respectively. The negative % swelling could be attributed to erosion of the tablets. The in vitro release of PNL from the tablets in buffer solution pH 1.2 (1 h) and pH 7.5 (3–12 h) was 21.12–76.22%. Tables with a high proportion of K100M HPMC had high PNL release, and the mechanism of PNL release was diffusion-and erosion-controlled. Conclusion: The simplex centroid design is potentially advantageous for formulating PNL-HPMC matrix tablets.

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