scholarly journals Formulation and evaluation of third-generation Cefpodoxime proxetil as an Oro-dispersible tablets for treating infections

2020 ◽  
Vol 11 (1) ◽  
pp. 921-932
Author(s):  
Akshay Kumar S ◽  
Gowda D V ◽  
Sharadha M ◽  
Famna Roohi N K

The main problems to humans include the infection caused in the respiratory tract and urinary tract, namely respiratory tract infection (RTI) and urinary tract infection (UTI). Cefpodoxime Proxetil drug is available in the market that has a problem with drug release profile and flows property. To overcome this problem, the compacted powder form made into a micro-ionized form for its better flow property and drug release by using a direct compression technique. The study was based on the aim to evaluate and formulate oro-dispersible tablets as an effective approach via orally for the treatment of RTI & UTI prepared by direct compression technique. FTIR and DSC showed no incompatibility between drugs and excipients. The pure drug Cefpodoxime Proxetil and the excipients were blended using an octagonal blender. The Pre-formulation study was performed for this blend and pure drug. Further, the blend was made compressed into a tablet by direct compression technique. Two factorial design was implemented. Prepared tablets were evaluated for drug content, hardness, thickness, uniformity in the weight, friability, disintegration test, dispersion time, in-vitro studies, release kinetics, and also stability studies. The optimized formulation A6 found to have good flow property. The evaluation results of optimized formula A6 showed 99.60% drug content, 390mg average weight, 0.91% weight uniformity, 3.80 kg/cm2 hardness, 0.67%, friability, 23.70sec, disintegration time, 16 sec dispersion time and 95.5% drug release than the other formulation batch. The current study showed that the optimized formula A6 exhibited good disintegration time, drug release, and friability than marketed product X and other batches.

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (03) ◽  
pp. 28-38
Author(s):  
S. B. Baliga ◽  
B. P Manjula ◽  
M. Geetha ◽  

Sumatriptan succinate (SS) is a drug used in the treatment of migraine headaches, but suffers from low patient compliance due to its unpalatable bitter taste. The purpose of the present work was to prepare taste-masked oro dispersible tablets (ODTs) of SS by incorporating drug loaded microspheres into tablets for use in patients experiencing difficulty in swallowing. Microspheres loaded with SS were prepared by solvent evaporation technique. Eudragit EPO, a pH-sensitive aminoalkylmethacrylate copolymer, was used for coating the drug particles, acetone as solvent for the polymer and light liquid paraffin as an encapsulating medium. Drug : polymer ratio of 1:1 was considered to be optimized formulation with a yield of 99.96%, entrapment efficiency of 61.55%, particle size ranging from 30.32 – 90.96μm and in vitro drug release of 85.06% within an hour. FTIR studies suggested absence of drug-excipient interaction. Tablets prepared by direct compression containing microspheres and effervescent agents were evaluated for pre-compression and post-compression parameters. The wetting time, in vitro dispersion time and in vitro disintegration time of the tablets were found to be 39 sec, 35 sec and 32 sec, respectively. The drug release from the tablet was about 85.44% within an hour. The SEM of final ODTs revealed that the microspheres remained intact even after compression. Stability studies indicated that the selected formulation was stable. The results obtained suggested that effective taste-masking was achieved for SS using the technique of microencapsulation and ODTs of acceptable characteristics were obtained by adding effervescent agents followed by direct compression.


Author(s):  
RAJASEKHAR POONURU ◽  
ROHINI CHERUKU ◽  
PAVAN JULURI ◽  
KHADEERA JABEEN ◽  
SWETHA SREERAMULA ◽  
...  

Objective: The present study was designed to formulate and evaluate the orodispersible tablets of lamotrigine after enhancing its solubility. Methods: Lamotrigine was made into an inclusion complex with eudragit E 100 my kneading and mass extrusion method and later this mixture is compressed into orodispersible tablet using various super disintegrants and co-processed excipients to reduce the disintegration time for providing prompt action through rapid drug release. Results: Lamotrigine ODTs containing F-melt (F1-3%, F2-5%) dispersed in lesser time of (9±0.11) and (21±0.58) compared to formulations with polyplasdone XL-10 and primellose as super disintegrants respectively with F1 showing short wetting time. The water absorption was also was found to be more for formulation with 3% F-Melt. Conclusion: Lamotrigine orodispersible tablets were prepared by direct compression technique by using 3% and 5% of three super disintegrants (f-melt, primellose and polyplasdone XL-10). Disintegration time of F1 (3% f-melt) formulation was found to be least (7 sec).


Author(s):  
S. P. Hiremath ◽  
Chidambar Makanapur

Objective: The rationale of the current work was to formulate and evaluate orodispersible tablets by direct compression technique with a vision to augment patient compliance and rapid onset of action.Methods: Nine orodispersible formulations of propranolol were formulated by direct compression method using sodium starch glycolate, crospovidone and croscarmellose sodium as the super disintegrants. The prepared formulations were evaluated for wetting time, drug content, in vitro disintegration time, dispersion time, dissolution time and also projected to kinetic treatment to know the pattern of drug release. Further, the discovered promising formulation was subjected to stability studies.Results: Based on the results obtained, formulation F9 containing6 mg of croscarmellose sodium exhibited good wetting time, dispersion time, and disintegration time and drug release compared to orodispersible tablets prepared with other super disintegrants. The stability studies piloted as per International Conference on Harmonisation guidelines on the promising formulationF9disclosedno significant changes in the colour (white), drug content (94.87±0.141 mg), hardness (2.93±0.18 kg/cm2), disintegration time (17.11±0.089 s), and drug release after 4 w. After 60 s, the percentage drug release of F9 was found to be 98.52 % and 96.30 % after 1 and 4 w, respectively.Conclusion: Orodispersible tablets of propranolol hydrochloride were formulated successfully by employing direct compression technique. From the investigation, it can be reasonably concluded that F9 batch orodispersible tablets of propranolol with 6 mg of crospovidone exhibited maximum cumulative drug release in 60 s.


2020 ◽  
Vol 10 (3-s) ◽  
pp. 17-25
Author(s):  
Inder Kumar ◽  
Dipima Chaudhary ◽  
Bhumika Thakur ◽  
Vinay Pandit

Objective: In the present research work, fast dissolving tablets of Piroxicam were formulated by two different techniques i.e. direct compression method and sublimation method using different superdisintegrants. Methods: Twelve formulations were prepared (PXM1 to PXM12) in which first six formulation were prepared by direct compression technique and other six formulation were prepared by sublimation method by using camphor as a sublimating agent. Result and Discussion: All the formulations were subjected for precompression, post compression parameters, and shows all the data within the specific limits. Formulation PXM4 containing 5 % crospovidone showed 99.480 ± 0.291 % drug release in 20 min which was more than the drug release of rest of the formulations. The optimized formulation PXM4 was compared with the marketed formulation and it revealed that drug release of PXM4 was found to be 99.397 ± 0.751 % in 20 min, which was greater than the marketed formulation. Finally, results were statistically analysed by the application of one way ANOVA and t-test. The stability study of the optimized formulation PXM4 showed no significant changes in, drug content, disintegration time and in-vitro drug release. Conclusion: Piroxicam can be successfully prepared using direct compression technique and it will enhance the drug dissolution, which will further increase absorption and bioavailability of the drug. Keywords: Direct compression, fast dissolving tablets, sublimation, Piroxicam.


Author(s):  
Madhivardhana P ◽  
Rajalakshmi A N ◽  
Padmapriya S

The aim of this research work is to formulate and evaluate Levothroxine sodium immediate release tablets prepared by direct compression method . Five formulations were evaluated for different pre and post compression parameter and in vitro drug release studies.The results of pre compression parameters of formluation 1 to 5 were compared with prescribed limits. It showed that formulation 1 to 5 powder blend exhibit good flow property and compressibility property. The disintegration time of all formulation was found to be in the range 2mins 09 secsto 4mins 03 secs.Thus, based on evaluation of different parameters it was concluded that formulation of immediate release tablet Levothyroxine sodium was successfully done and F-5 showed almost 93% drug release at 45 mins in Alkaline borate buffer( pH 10). Keywords: Thyroid hormone (T4), Immediate release tablets, Direct compression, Dissolution.


2017 ◽  
Vol 9 (4) ◽  
pp. 92
Author(s):  
Hrishav Das Purkayastha ◽  
Bipul Nath

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant. 


Bio-Research ◽  
2020 ◽  
Vol 18 (1) ◽  
Author(s):  
BB Mohammed ◽  
EJ John ◽  
NK Ajuji

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.  


2021 ◽  
Vol 11 (5) ◽  
pp. 115-120
Author(s):  
Kritika Rai ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar

Orally disintegrating tablets (ODT) disintegrate quickly with saliva when administered into the oral cavity and taken without water or chewed. ODT are easy to take for children and the elderly, who may experience difficultly in taking ordinary oral preparations such as tablets, capsules, and powders.  The ODT threes substantial benefits for the patient (or elder) who cannot swallow (Dysphagia), or who is not permitted water intake due to disease. The reason of the current research was to prepare taste masking oral disintegrating tablets of poorly soluble lornoxicam (LXM) by direct compression technique using Kyron T-114 (cation exchange resin) as a taste masking agent. With in various ratios the Drug-resin of 1:4 was established to present best taste masking. The superdisintegrants used in formulation are croscarmellose sodium and cross povidone. Among these croscarmellose sodium demonstrated superior drug release. The tablets were evaluated for friability, weight variation, wetting time, hardness, disintegration time and uniformity of content. Optimized formulations were evaluated for in vitro dissolution test. Amongst all the formulations F-6 was found to be most successful tablets prepared by this technique had disintegration time of 30sec and % CDR 94.78 within 30min. Hence, this advance can be utilized for taste masking of bitter pharmaceutical ingredients leading to superior patient compliance. Keywords: Oral disintegration tablets, Lornoxicam, Kyron T-114, Superdisintegrants, Direct Compression.


Author(s):  
J. I. Ordu ◽  
I. E. Udenze

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.


2019 ◽  
Vol 9 (4) ◽  
pp. 574-578
Author(s):  
Mohammad Faizan Mohammad Gufran ◽  
Sailesh Kumar Ghatuary ◽  
Reena Shende ◽  
Prabhat Kumar Jain ◽  
Geeta Parkhe

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline. Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.


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