scholarly journals Formulation and Evaluation of Delayed Release Pellets of Ivabradine Hydrochloride

2021 ◽  
Vol 69 (1) ◽  
Author(s):  
Sanjesh G. Rathi ◽  
Shrenik K. Shah ◽  
Sohansinh S ◽  
Himanshu G. Parmar
Keyword(s):  
Drug Release ◽  
Process Parameters ◽  
Polymer Coating ◽  
Polymer Concentration ◽  
Research Work ◽  
Stability Study ◽  
Enteric Coating ◽  
Delayed Release ◽  
Extrusion Spheronization

The aim of preset research work is to formulate and evaluate delayed release pellets of Ivabradine HCl. Pellets are prepared using extrusion-spheronization process and the process parameters are optimized. Polymer coating done with Kollicoat SR 30 D as rate controlling polymer and finally enteric coating done with Eudragit L30D-55. Drug release in formulation F1-F9 studied and it found that the low polymer concentration (2 %) was unable to retard the drug release up to 12 hr so concentration increased batch by batch and finally 12 % coating batch gives desired results which retard the drug release up to 12 hr. also found that the drug release was very low after more % coating than the 12 %. Hence based on that the F5 batch was optimized batch and its found stable during stability study of 1 month.Delayed release pellets of Ivabradine HCl was successfully prepared using Kollicoat SR 30 D as rate controlling polymer.

scholarly journals Preparation and preclinical evaluation of aceclofenac loaded pectinate mucoadhesive microspheres

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Santanu Chakraborty ◽  
Priyanka Nayak ◽  
Bala Murali Krishna ◽  
Madhusmruti Khandai ◽  
Ashoke Kumar Ghosh
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Polymer Concentration ◽  
Research Work ◽  
In Vivo Studies ◽  
Systemic Absorption ◽  
Cross Linking ◽  
Significant Difference

The aim of the present research work was to fabricate aceclofenac loaded pectinate microspheres by ionic gelation method and evaluate the effect of different cross-linking agents and polymer concentration on particle size, encapsulation efficacy and drug release behavior. It was also investigated that whether this pectinate dosage form was able to target the drug release in intestinal region and prevent the different side effect associated with the drug in stomach or not. It was observed that particle size, encapsulation efficacy and in vitro drug release were largely depended on polymer concentration and cross-linking agents. It was also observed that pectinate microspheres showed excellent pH depended mucoadhesive properties and they were able to restrict the drug release in stomach. <em>In vitro</em> drug release study showed that alminium-pectinate microspheres have more sustaining property as compared to barium-pectinate microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t<sub>50%</sub> values among all the formulations with same cross-linking agent. In vivo studies revealed that the anti inflammatory and analgesic effects induced by pectinate microspheres were significantly high and prolonged as compared to pure drug. So, pectinate microspheres can be an excellent carrier for targeting the delivery of aceclofenac as well as help in improving the patient compliance by prolonging the systemic absorption.

scholarly journals Formulation, Optimization, and Characterization of Repaglinide Loaded Nanocrystal for Diabetes Therapy

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Gajanan Shinde ◽  
Mitesh Patel ◽  
Manan Mehta ◽  
Rajesh Kesarla ◽  
Ganesh Bangale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymer Concentration ◽  
Study Data ◽  
Stability Study ◽  
Diabetes Therapy ◽  
Peg 4000 ◽  
Number Of Cycles

The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy. Formulation was done by high pressure homogenization. HPH pressure and cycles range were screened by preliminary batches (T1 and T2). 5, 8, and 10 cycles and 500 to 1500 bar pressure range had kept for further investigation. Taguchi design was used to optimize type of polymer, % polymer concentration, number of cycles, and HPH pressure for nanocrystal formulation. Formulations were characterized for particle size, zeta potential, and in vitro drug release. Optimized formulation (NC 3) showed particle size of 187 nm, zeta potential of −29.4 mv, and % drug release of 80.58% and it was used for further study. Data analysis proved significant effects of factors on responses. Polydispersity index (PDI) Analysis of optimized formulation were found to be 0.248. SEM showed nanocrystal aggregation of drug, may be due to water removal process. DSC showed slight change in crystallinity, may be due to the presence of PEG 4000. Stability study was carried out for 3 months. It indicated no significant change in particle size and zeta potential. However, further studies in higher animals and human being need to be performed before this formulation can be commercially exploited.

scholarly journals IMPLEMENTATION OF QUALITY BY DESIGN (QBD) APPROACH IN FORMULATION AND DEVELOPMENT OF RITONAVIR PELLETS USING EXTRUSION SPHERONIZATION METHOD

2019 ◽  
pp. 139-146
Author(s):  
SATISH K. MANDLIK ◽  
PAYAL P. AGARWAL ◽  
HARSHAL P. DANDGAVHAL
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Factorial Design ◽  
Quality By Design ◽  
Research Work ◽  
Full Factorial Design ◽  
Extrusion Speed ◽  
Full Factorial ◽  
Extrusion Spheronization

Objective: Ritonavir is an antiretroviral drug used for HIV-AIDS treatment. The purpose of this research work was to implement the quality by design (QbD) approach in formulation of ritonavir sustained-release pellets by industrially applied extrusion spheronization technique. Methods: Pellets were prepared by extrusion spheronization method and evaluated for their physicochemical properties. Initially, on the basis of prior knowledge Quality Target Product Profile (QTTP) element was identified and further Critical Quality Attributes (CQA) elements were defined. Risk assessment (RA) was done by two tools as failure mode and effect analysis (FMEA) and fishbone diagram (Ishikawa plot). Placket Burman design was implemented as a screening design using seven high-risk factors (spheronization speed, spheronization time, extrusion speed, drying method, PVP K 30, cross povidone, and solvent). Optimization study was done by 23 full factorial design with three critical factors as (spheronization speed, extrusion speed and PVP K 30). The in vitro drug release was studied in both gastric and intestinal fluids for 12 h using USP Ι apparatus. Control space was established for the sustained release pellets. Results: Among all batches obtained in 23 full factorial design, batch R7 was found to be effective with carr’s index value of 5.281, percentage yield of 69.6%, time required to release 50% drug was 8 h and percent drug release after 12 h was found 83.132 %, R7 batch was selected as optimized batch. Statistical analysis showed model terms were significant. Conclusion: We can conclude that; sustained-release pellets of ritonavir were successfully designed using QbD approach.

scholarly journals FORMULATION OPTIMIZATION OF PROMETHAZINE THEOCLATE IMMEDIATE RELEASE PELLETS BY USING EXTRUSION-SPHERONIZATION TECHNIQUE

2018 ◽  
Vol 10 (1) ◽  
pp. 30
Author(s):  
Shelar Vishwas S. ◽  
Shirolkar Satish V. ◽  
Kale Rupali N.
Keyword(s):  
Drug Release ◽  
Motion Sickness ◽  
Dosage Form ◽  
Corn Starch ◽  
Research Work ◽  
Immediate Release ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Extrusion Spheronization ◽  
Pellet Formulation

Objective: Promethazine theoclate is a BCS Class II drug having anti-histaminic property and mainly used for the treatment of motion sickness and postoperative emesis. The main objective of the research work was to formulate and optimize immediate release pellets of promethazine theoclate by using the extrusion-spheronization technique to offer immediate release dosage form suitable for treatment of nausea and vomiting associated with motion sickness and post-operative conditions.Methods: Immediate release pellets of promethazine theoclate were prepared by using microcrystalline cellulose (MCC) and corn starch as filler and disintegrant respectively along with other excipients. Pellet formulation was further optimized for bulk density, disintegration time and percent drug release after 10 min. using 32 factorial design. Formulations were also characterized for drug-polymer interactions using Differential Scanning Calorimetry (DSC), surface morphology by Scanning Electron Microscopy (SEM) and other physicochemical properties.Results: Optimised pellet formulation contains 2.5:4.5:1 ratio of MCC: Corn Starch: Drug and spheronization time of 60 seconds showing highest percent yield of 78% and immediate drug release of 100.52±0.65% after 10 min.Conclusion: Promethazine theoclate pellets formulated in this study can serve as an alternative to tablet dosage form which can give immediate drug release for treatment of motion sickness and postoperative emesis.

scholarly journals Designing fabrication and evaluation of Oral fast Disintegrating tablet of Ranitidine HCL

2019 ◽  
Vol 9 (1) ◽  
pp. 95-102
Author(s):  
Afroza Akbar Patel ◽  
Siraj N Shaikh ◽  
Huzaifa Patel ◽  
Afzal Band ◽  
Ahmed Shaoor
Keyword(s):  
Drug Release ◽  
Optimization Technique ◽  
Research Work ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Compression Technique ◽  
Disintegration Time ◽  
Fenugreek Gum ◽  
Fast Disintegrating Tablets

The aim of this research work was to design develop & evaluate oral fast disintegrating tablets of Ranitidine HCL. The Orodispersible tablets of Ranitidine HCl were prepared by using direct Compression technique with a Synthetic Superdisintegrant such as Crosspovidone and a natural Superdisintegrant Fenugreek gum in different concentration. 32 factorial designs was applied to study the effect of independent variables,  concentration of Crosspovidone & Fenugreek gum on dependent variables like Cumulative % Drug release and Disintegration time by using design expert software. Prepared oral fast disintegrating tablets evaluated for Pre and Post-compression parameters. The prepared tablets exhibited satisfactory physico-chemical characterise especially fast disintegration & dissolution property. Full factorial design and optimization technique successfully used in the development oral fast disintegrating tablets. Comparing the all the formulations, formulation F9 was considered as optimized formulation which shows excellent fast disintegration, in vitro dissolution, and faster drug release within 6 min in comparison to other batches also stable in stability study. Keywords:  Fast disintegrating, Ranitidine, Crosspovidone, Gum, Optimizations, Water absorption ratio

scholarly journals FORMULATION AND EVALUATION OF GARLIC POWDER LOADED FLOATING MATRIX TABLET

2019 ◽  
pp. 17-21
Author(s):  
SHWETA PAWAR
Keyword(s):  
Drug Release ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Film Coating ◽  
Stability Study ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Peptic Ulcers ◽  
Garlic Powder ◽  
The Stability

Objective: The objective of the present work was to formulate and evaluate a stable, odour free garlic powder loaded floating matrix tablet for the treatment of peptic ulcers. Methods: A gastro-retentive floating matrix tablet (FMT) formulation of garlic powder (GP) was prepared using various concentrations of hydroxypropyl methylcellulose K4M (HPMC K4 M) and effervescent system (sodium bicarbonate and citric acid in 1:1 % w/w) to achieve desirable floating time (FT), floating lag time (FLT) and drug release. Wet granulation method was selected using ethanol as a binder for preparation of tablet. 32 full factorial designs were used for selection of suitable polymer concentration and effervescent system. Nonenteric film coating was applied to mask GP odour. Results: It was observed that FMT with optimum quantities of HPMC K4M and the effervescent system showed 97 % of drug release in 12 h with FT up to 10 h and minimum FLT of 3 min. There was no significant change in FLT, FT and drug content during the stability study of FMT. Conclusion: A stable, sustained release FMT of GP tablets using HPMC K4M and an effervescent system was successfully prepared. This formulation can overcome problems of taste and odour masking, gastric irritation, and loss of active constituents present in garlic.

scholarly journals MULTIPLE UNIT PELLET SYSTEM (MUPS) BASED FAST DISINTEGRATING DELAYED-RELEASE TABLETS FOR PANTOPRAZOLE DELIVERY

2018 ◽  
Vol 10 (1) ◽  
pp. 77
Author(s):  
Sandipkumar A. Patel ◽  
Nrupa G. Patel ◽  
Abhijeet B. Joshi
Keyword(s):  
Drug Release ◽  
Physical Properties ◽  
Microcrystalline Cellulose ◽  
Release Profile ◽  
Drug Release Profile ◽  
Delayed Release ◽  
Fluid Bed ◽  
Enteric Polymer ◽  
Multiple Unit ◽  
Extrusion Spheronization

Objective: The rationale for the study was to develop multiple unit pellet system (MUPS) of delayed release pantoprazole with desired physical properties and unaltered drug release profile from pellets even after compression into a fast disintegrating tablet.Methods: In the presented study, delayed release pellets of pantoprazole were developed by two methods, i.e. extrusion-spheronization and drug layering techniques, coated using enteric polymer and subsequently compressed in to tablet. In drug layering technique, pantoprazole was loaded on Celphere®102 (microcrystalline cellulose spheres) as well as on Suglet® (sugar spheres) in fluid bed processor. Acid resistant polymer Eudragit ND 30D was subsequently coated on each type of drug loaded pellets. Suitable tableting excipients were prepared such as soft pellets, Ceolus® (fibrous grade of microcrystalline cellulose) granules, Ludipress® (compressible lactose composition), Avicel® PH 200 and different combination of them. Various factors like property of pellets to be compressed, coating level, the composition of tableting excipient and ratio of drug-loaded pellets to tableting excipients were identified and optimized.Results: MUPS with delayed releasing pellets of pantoprazole proved to provide sufficient hardness, rapid disintegration property, and unaltered release profile after compression. Delayed release pantoprazole pellets prepared by drug layering on celphere® 102 followed by coating with Eudragit® NE 30D showed better compressibility to withstand the drug release properties. The combination of Ceolus® granules and Ludipress (in 1:1 ratio) was found to be suitable tableting excipient that helped compression of pellets without rupturing polymeric coat. Pellets to excipients ratio at 1:3 was found optimum.Conclusion: Compaction behaviour of pantoprazole delayed-release pellets without loss of original delayed release profile was achieved by formulating as MUPS based tablet of pantoprazole delayed release pellets using celephere® 102 was developed which was found suitable for desired release profile and physical properties.

scholarly journals ESTIMATION OF BACOSIDE-A IN BACOPA MONNIERI AERIAL PARTS USING TLC DENSITOMETRY

2019 ◽  
pp. 115
Author(s):  
RAJESH KUMAR ◽  
TEJPAL SINGH ◽  
DEEPAK KUMAR ◽  
MANDEEP SINGH ◽  
SANDEEP KAUR ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Film Coating ◽  
Stability Study ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Peptic Ulcers ◽  
Garlic Powder ◽  
The Stability

Objective: The objective of the present work was to formulate and evaluate a stable, odour free garlic powder loaded floating matrix tablet for the treatment of peptic ulcers. Methods: A gastro-retentive floating matrix tablet (FMT) formulation of garlic powder (GP) was prepared using various concentrations of hydroxypropyl methylcellulose K4M (HPMC K4 M) and effervescent system (sodium bicarbonate and citric acid in 1:1 % w/w) to achieve desirable floating time (FT), floating lag time (FLT) and drug release. Wet granulation method was selected using ethanol as a binder for preparation of tablet. 32 full factorial designs were used for selection of suitable polymer concentration and effervescent system. Nonenteric film coating was applied to mask GP odour. Results: It was observed that FMT with optimum quantities of HPMC K4M and the effervescent system showed 97 % of drug release in 12 h with FT up to 10 h and minimum FLT of 3 min. There was no significant change in FLT, FT and drug content during the stability study of FMT. Conclusion: A stable, sustained release FMT of GP tablets using HPMC K4M and an effervescent system was successfully prepared. This formulation can overcome problems of taste and odour masking, gastric irritation, and loss of active constituents present in garlic.

scholarly journals Formulation and Evaluation of Piroxicam Fast Dissolving Tablets Using Direct Compression and Sublimation Method

2020 ◽  
Vol 10 (3-s) ◽  
pp. 17-25
Author(s):  
Inder Kumar ◽  
Dipima Chaudhary ◽  
Bhumika Thakur ◽  
Vinay Pandit
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Stability Study ◽  
Drug Dissolution ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Sublimation Method ◽  
The Stability

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.

scholarly journals Development of Capecitabine Floating Tablet Dosage Forms for Treating Stomach Cancer

2020 ◽  
Vol 10 (3-s) ◽  
pp. 199-205
Author(s):  
Salma Shaik ◽  
Sudhir Maddela ◽  
Buchi N. Nalluri
Keyword(s):  
Calcium Carbonate ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Polymer Concentration ◽  
Research Work ◽  
Methyl Cellulose ◽  
Dosage Forms ◽  
Crystalline Cellulose ◽  
Scanning Calorimetry ◽  
Gastro Retentive

Objective: In the present research work, oral gastro retentive dosage forms (GRDFs) of capecitabine (CPC) were formulated using floating concept. Methods: GRDFs were formulated using hydroxypropyl methyl cellulose (HPMC K4M and K15M) as drug release retardant, sodium bicarbonate (NaHCO3) and calcium carbonate (CaCO3) as gas generating agents, and micro crystalline cellulose (MCC), dicalcium phosphate (DCP), spray dried lactose (SDL), and pre gelatinized starch (PGS) as fillers. The tablets were prepared by direct compression method and evaluated for various parameters. The GRDFs were also characterized by Fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). Results and Discussion: All the formulations were subjected for pre and post compression parameters, shows all the data within the limits. The lag times of GRDFs has decreased significantly for formulations containing calcium carbonate when compared to sodium bicarbonate as gas generating agent. In vitro drug release studies indicate that higher polymer concentration delayed the CPC release, and the sustaining effect was in the order K4M > K15M > LVCR 100. Addition of MCC, DCP, SDL, and PGS as fillers further affected the lag time and in turn the CPC release rates. Conclusion: The formulation (F9) containing 10%w/w HPMC K4M as the release retardant, microcrystalline cellulose as filler and 20%w/w CaCO3 as gas generating agent fulfilled regulatory requirements in terms of percent drug release at the end of 24h. Keywords: Capecitabine, Gastro retentive floating tablets, floating drug delivery systems, FTIR, DSC.

Sign in / Sign up

Export Citation Format

Share Document