Evaluation of the sustained release potential of a co-processed excipient in Ibuprofen tablet formulation

2020 ◽  
Vol 1 (4) ◽  
pp. 13-23
Author(s):  
B.B. Mohammed ◽  
◽  
T.J. Hayab ◽  
Z.S. Yahaya
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Dosage Form ◽  
Tablet Formulation ◽  
Angle Of Repose ◽  
Flow Properties ◽  
Disintegration Time ◽  
Duration Of Action ◽  
Two Component ◽  
Release Potential

Background: The oral route happens to be the most preferred route among the various routes of drug delivery. However, the conventional dosage form has few limitations which could be resolved by modifying the existing dosage form. Sustained and controlled drug delivery systems help to maintain constant plasma drug concentration and retarding the release rate of drug thereby extending the duration of action. Objectives: To develop by co-processing technique a two-component excipient and evaluate its sustained release potential in ibuprofen tablet formulation. Method: Maize starch (MS) was co-processed with polyvinylpyrrolidone (PVP), acacia powder (ACA) and hydroxypropyl methylcellulose (HPMC) respectively at a ratio of 60:40 using the co-fusion method. The granules so formed were analyzed for flow properties and compatibility tests based on; angle of repose, flow rate, bulk and tapped densities (BD/TD), Hausner ratio (HR) and Carr’s Index (CI), Differential Scanning Calorimetry (DSC) and Fourier Transform Infra-red (FTIR) spectroscopy. The tablets were evaluated after compression by direct compression. Results: The co-processed excipient (CE) had excellent flow properties as compared to the physical mix (PM). The DSC thermograms and FTIR spectra of CE when compared with their individual excipients and that of the drug, showed a similarity in their endothermic peaks respectively but for some slight difference showing compatibility and no new compound was found because of co-processing. The tablets had acceptable values for weight variation and disintegration time. Tablets of Batch XII B were of good quality regarding weight, hardness, disintegration time and friability by meeting the British Pharmacopoeia specifications. Conclusion: This study concluded that the two-component excipients developed improved the functionality of the single components. Conversely, the co-processed excipients did not exhibit good sustained release property but would be better employed as conventional tablets or prepared as a sustained release matrix formulation.

scholarly journals EVALUATION OF MUSA ACUMINATA FRUIT AS A NATURAL SUPERDISINTEGRANT FOR TABLET FORMULATION

2018 ◽  
Vol 11 (10) ◽  
pp. 167
Author(s):  
Gopinath E
Keyword(s):  
Nutritive Value ◽  
Low Cost ◽  
Cost Effective ◽  
Musa Acuminata ◽  
Tablet Formulation ◽  
Angle Of Repose ◽  
Average Weight ◽  
Disintegration Time ◽  
Solubility Study ◽  
Orodispersible Tablet

Objective: The objective of the present work was to develop and evaluate a new, low-cost effective superdisintegrant from Musa acuminata fruit for tablet formulation.Methods: The study involved collection of M. acuminata fruit powdered and evaluated for physicochemical properties. Propranolol Hcl was used as a model drug for tablet formulation. Different concentrations of M. acuminatea powder were used as superdisintegrant, and orodispersible tablet is prepared and evaluated. In the present study, sodium starch glycolate was used as synthetic superdisintegrant for comparative study.Result: The powder was dark brownish and did not change throughout the study. The percentage porosity of powder was found to be 42.88% and angle of repose of was found to be 33.69°. The solubility study shows that the powders are sparingly soluble in water and disperse into individual particles. Total ash and acid insoluble ash values of powder were found to be 2.61 and 2.11% w/w, respectively. The average weight of tablets was ranged from 101.42 to 103.52 mg and averaged hardness was found to be 3.4 kg/cm2. Moreover, the tablets exhibited acceptable friability. Disintegration time of all formulations was found to be in the range of 22–80 s and wetting time was found to be 07–18 s.Conclusion: From the study, it was concluded that M. acuminatea powder in the range of 2–12% can be used as superdisintegrant in orodispersible tablet formulation and shall be preferred as having nutritive value as well as cost profit in the development of orodispersible tablet than synthetic polymer.

Implementation of Quality by Design principles for the evolution of optimized sustained release drug delivery system

2021 ◽  
Vol 11 ◽  
Author(s):  
Lalit Singh ◽  
Vijay Sharma
Keyword(s):  
Mathematical Model ◽  
Drug Delivery ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Dosage Form ◽  
Quality By Design ◽  
Design Principles ◽  
Release Drug

Aim: Aim of the present work is implementation of Quality by Design principles for the evolution of optimized sustained release drug delivery system Background: Quality by Design (QbD) approach refers to an advance approach to develop a optimized dosage form.QbD has become a vital modern scientific approach to develop a quality dosage form.In modern era of science researcher can develop a optimized dosage form with least effort, money and manpower. Objectives: Objective of research work wasthe successful development of optimized floating bioadhesive tablets of glipizide using floating-bioadhesive potential of cellulosic polymer and carbomersusing quality by design (QbD) approach. Method: Quality Target Product Profile (QTPP) of drug delivery system was defined as well as critical quality attributes (CQAs) were identified. A face centered central composite design (CCD) was utilized in assessing the impact of individual critical material attribute (CMA) like Hydro Propyl Methyl Cellulose K4M(HPMC K4M)and Carbopol 934P (CP 934P) and their interactions, using least experimentation. Formulations were developed and quantitative impact on CQAs was determined using mathematical model. The optimized formulation was obtained and characterized for in-vitro as well as in-vivo parameters. Results: A Fishikawa diagram and Failure Mode and Effect Analysis (FMEA) were performed to identify potential failure modes associated with the dosage form. The optimum formulation was embarked upon using mathematical model developed yielding desired CQAs followed for confirmation of data. Sustained release drug delivery system was successfully developed by using QbD approach. In-vivo X-ray imaging in rabbit and γ-scintigraphic study in manconfirmed the buoyant nature of the mucoadhesive floating tablet for 8 h in the upper gastrointestinal tract. Conclusion: Optimized formulation shows phenomenal floating, bioadhesive properties and drug release retardation characteristics, utilizing a mixture of cost-effective polymers Hence, QbD approach may be regarded as an important tool in development of floating bioadhesive CR dosage forms.

scholarly journals Formulation and evaluation of fast dissolving tablets of amlodipine besylate by using Fenugreek seed mucilage and Ocimum basilicum gum

2012 ◽  
Vol 1 (9) ◽  
pp. 243-249 ◽  
Author(s):  
Sudheshnababu Sukhavasi ◽  
V. Sai Kishore
Keyword(s):  
Drug Delivery ◽  
Ocimum Basilicum ◽  
Angle Of Repose ◽  
Natural Polymers ◽  
Amlodipine Besylate ◽  
Disintegration Time ◽  
Fenugreek Seed ◽  
Wetting Time ◽  
Seed Mucilage

Fast dissolving/disintegrating tablets have received ever-increasing demand during the last decade, and the field has became a rapidly growing area in the pharmaceutical area. Particularly the fast dissolving drug delivery systems formulated with natural polymers have more demand because natural materials like gums and mucilages have been extensively used in the field of drug delivery for their easy availability, ease administration, non toxicity, non irritant nature etc. The main aim of the present study was to formulate the fast dissolving tablets of amlodipine besylate tablets using Fenugreek seed mucilage and Ocimum basilicum gum as a natural superdisintegrating agents to achieve quick onset of action, is to increase the water uptake with in shortest wetting time and there by decrease the disintegration time of the tablets by simple and cost effective direct compression technique. Pre-compression parameters like angle of repose and post-compression parameters like wetting time, water absorption ratio, in-vitro disintegration and in-vitro dispersion time were studied. The hardness, friability and drug content of all the formulations were found to be within the limits. The best formulations FFGK5 & FOB5 have shown good disintegration time, hardness and friability. The best formulations were also found to be stable. Optimized formulation was subjected to stability studies as per ICH guidelines and it insignificant change in hardness, disintegration time and in vitro drug release.DOI: http://dx.doi.org/10.3329/icpj.v1i9.11614 International Current Pharmaceutical Journal 2012, 1(9): 243-249 

scholarly journals Preparation and characterization of Gliclazide incorporated Cellulosic Microspheres: studies on drug release, compatibility and micromeritics

2015 ◽  
Vol 13 (2) ◽  
pp. 149-166 ◽  
Author(s):  
Navid Jubaer Ayon ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Sustained Release ◽  
Release Rate ◽  
Drug Loading ◽  
Angle Of Repose ◽  
Flow Properties ◽  
Dissolution Apparatus

Polymeric microspheres of gliclazide were prepared to provide sustained release delivery of gliclazide to aid in continuous therapy with high margin of safety. Gliclazide was microencapsulated with different polymers namely HPMC K100LV, Ethocel (20 cps) and HPMC K100M by emulsion solvent evaporation technique using acetone as internal phase and liquid paraffin as external phase. Seventeen formulations were prepared using different drug loading and polymeric ratio of which nine formulations were prepared by a 32 full factorial design. Each formulation was evaluated for flow properties, particle size, surface morphology, drug entrapment efficiency, drug release and compatibility. Yield (%) for every batch of microspheres was measured. Flow properties of the microspheres were examined by determining bulk density, tapped density, Carr’s compressibility index, Hausner ratio and angle of repose. Particle size distribution was examined by sieving and particle size analyzer. Surface morphology was determined by scanning electron microscopy (SEM). In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) for a period of 8 hours at 37°C using phosphate buffer ( pH 7.4). FTIR and DSC studies established compatibility of the drug with the polymers. Microspheres prepared with Ethocel (20 cps) and HPMC K100M were free flowing than those prepared only with HPMC K100LV. Entrapment efficiencies were within 75.88-99.69%. Microspheres prepared with Ethocel (20 cps) and HPMC K100M showed more sustained release when compared to microspheres prepared with HPMC K100LV only. Increase in drug loading resulted in increased drug release for the microspheres. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranging from diffusion controlled to anomalous type. Ethocel and HPMC K100M in a ratio of 1:3 exhibited better sustained release properties than 1:1 and 3:1 ratios. The release rate of gliclazide from microspheres prepared with Ethocel (20 cps) and HPMC K100M was less than the release rate of gliclazide from microspheres prepared with HPMC K100LV, demonstrating Ethocel and HPMC K100M as suitable polymeric blend for preparing the controlled release formulation for gliclazide whereas, HPMC K100LV was found not suitable candidate when used alone as a polymer. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21893 Dhaka Univ. J. Pharm. Sci. 13(2): 149-166, 2014 (December)

scholarly journals Physicochemical Characterization and Evaluation of the Binding Effect of Acacia etbaica Schweinf Gum in Granule and Tablet Formulations

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Kidan Haily Desta ◽  
Ebisa Tadese ◽  
Fantahun Molla
Keyword(s):  
Water Solubility ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Hot Water ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Flow Properties ◽  
Disintegration Time ◽  
Binding Effect ◽  
Tablet Formulations

This study is aimed at evaluating the binding effect of Acacia etbaica gum in granule and tablet formulations using paracetamol as a model drug. Some physicochemical properties of the purified gum such as pH, the presence of tannin and dextrin, solubility, viscosity, loss on drying, total ash value, water solubility index, swelling power, moisture sorption, and powder flow properties were investigated. Paracetamol granules were prepared using wet granulation method at 2%, 4%, 6%, and 8% w / w of the Acacia etbaica gum and compared with granules prepared with reference binders (PVP K-30 and Acacia BP) in similar concentrations. The granules were characterized for bulk and tapped densities, compressibility index and Hausner ratio, angle of repose, flow rate, and friability. Finally, the prepared granules were compressed into tablets and evaluated for different tablet characteristics: weight uniformity, thickness, diameter, crushing strength, tensile strength, friability, disintegration time, and in vitro release profile. The physicochemical characterization revealed that tannins and dextrin are absent in the gum, and the gum has acidic pH. Both the moisture content and total ash values were within the official limits. Furthermore, the gum was found to be soluble in cold and hot water but insoluble in organic solvent and exhibited a shear thickening viscosity profile and excellent flow properties with excellent compressibility. The granules prepared with the gum of Acacia etbaica and reference binders showed good particle size distribution and excellent flow and compressibility properties. All the prepared tablets passed pharmacopeial specifications with respect to their uniformity of weight, thickness, and disintegration time. Tablets formulated with Acacia etbaica gum and acacia BP meet the compendial specification for friability at binder concentrations more than 2%. Drug release properties of all the batches formulated with Acacia etbaica, PVP, and acacia BP complied with the pharmacopeial specification. It can be concluded that the gum of Acacia etbaica could be explored as an alternative excipient for its binder effect in granule and tablet formulations.

Formulation and Evaluation of Tramadol Hydrochloride Sustained Release Matrix Tablets

2018 ◽  
Vol 8 (3) ◽  
Author(s):  
B Sai Adithya ◽  
Gulshan Mohammad ◽  
Rama Rao Nadendla
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Patient Compliance ◽  
Oral Drug Delivery ◽  
The Body ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Tramadol Hydrochloride

The ultimate goal of any oral drug delivery system is the successful delivery of the drug, in which almost 90% of the drugs are administered to the body for the treatment of various disorders and diseases as it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. The aim of the present study is to formulate sustained release matrix tablets of a model drug (Tramadol hydrochloride) using HPMC 100 MCR, HPC and EC 7cps as rate retarding polymers, microcrystalline cellulose as bulking agent, magnesium stearate as lubricant and aerosil as glidant. Drug and polymer interactions were evaluated by using FTIR and DSC. The FTIR spectrum and DSC thermograms stated that drug and polymer are compatible to each other. Tablets were prepared by direct compression technique. The micromeritic properties of formulation mixtures of all the formulations were carried out and they were found to be as angle of repose (31.150- 40.100), bulk density (0.310g/ml-0.337g/ml), tapped density (0.355g/ml-0.59g/ml), Carr’s index (8.11%-15.3%), Hausner’s ratio (1.08-1.18) which are within the limits. The formulated tablets were physically acceptable and exhibited acceptable weight variation, friability. In vitro dissolution studies were carried out using USP type-II dissolution apparatus and of all the formulations F6 (containing HPMC and HPC in equal proportions) exhibited prolonged drug release for about 8 hrsas per the objective of the work. The percent drug content varied between 88% to 99%. It can be concluded from the study that the sustained release tablets can be better alternative over immediate release tablets by improving patient compliance and reducing frequency.

scholarly journals The DESIGN AND DEVELOPMENT OF CARVEDILOL GASTRORETENTIVE FLOATING DRUG DELIVERY SYSTEMS USING HYDROPHILIC POLYMERS AND IN VITRO CHARACTERIZATION

2020 ◽  
pp. 66-73
Author(s):  
PRASANTA KUMAR MOHAPATRA ◽  
C. H. SATYAVANI ◽  
SATYAJIT SAHOO
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Fourier Transforms ◽  
Magnesium Stearate ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Statistical Parameters ◽  
Compression Technique ◽  
Floating Tablets

Objective: The primary aim of the present examination was to create carvedilol phosphate floating tablets using factorial designs and for retention in the upper portion of the gastrointestinal (GI) tract to sustain the dissolution where the solubility of carvedilol phosphate is more in an acidic medium. Methods: The floating tablets of carvedilol phosphate were ready to employ different concentrations and a combination of these polymers of Na-alginate, Carbopol 934P, and sodium carboxymethyl cellulose (NaCMC) with lubricants magnesium stearate by direct compression technique. In the present experiment, involved sodium bicarbonate and citric acid as a gas-producing agent. Fifteen formulations structured and judged for pre-compression components like the angle of repose, bulk and tapped density, Hausner’s ratio, compressibility index, and post-compression factors are weight uniformity, hardness, drug content, friability, in vitro buoyancy, dissolution studies, and Fourier transforms infrared spectroscopy (FTIR). Results: The drug released 90.02% in 12 h by combining NaCMC (7.5 mg) and Na-alginate (7.5 mg) in the formulation F14 towards the achievement of sustained release. Batch F14 selected as optimized, as provided desired zero-order release profile as well as floating lag time 20 s and total floating time>12 h, and the mechanism of drug release observed (n = 1.098, super case-II transport). Conclusion: From the results fulfilled that all the preparation found to be within the pharmacopeia limits and was the best dosage form to treat moderate heart failure and hypertension. The in vitro dissolution profiles of all formulations placed into various kinetic models, the statistical parameters like slope, regression coefficient and intercept determined. The gastro-retentive dosage form to maintain the sustain drug delivery, which would improve the maximum therapeutic efficacy and patient compliance.

A Comprehensive Review on Pellets as a Dosage Form in Pharmaceuticals

2021 ◽  
Vol 22 ◽  
Author(s):  
Shailesh Thirumaleshwar ◽  
Maithri Shanbhogue H. ◽  
Gowrav Mysore Prakash ◽  
Hemanth Kumar Somareddy ◽  
Gangadharappa Hosahalli Veerabhadrappa
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Sustained Release ◽  
Patient Compliance ◽  
Single Unit ◽  
Dosage Form ◽  
Oral Route ◽  
Dosage Forms ◽  
Comprehensive Review ◽  
Pellet Formation

Abstract: Oral route of administration is widely accepted and desired because of its versatility, convenience, and most importantly patient compliance. Multiparticulate systems like granules and pellets are more advantageous when compared to single-unit dosage forms, as they are capable to distribute the drug more evenly in the gastrointestinal tract. The current paper focuses on pellets, the merits and demerits associated, various pelletization techniques, and its characterization. It also focuses on how pellets can be employed for drug delivery in controlled and sustained release formulations. It gives a com-plete emphasis on the drug and excipients that can be used in pellet formation, the marketed formulations, and the research pertaining to pellets.

scholarly journals Formulation and evaluation of orodispersible tablets of dimenhydrinate by using co-processed superdisintegrants

2018 ◽  
Vol 12 (1) ◽  
pp. 23-33
Author(s):  
A. Ankit ◽  
G.B. Kiran Kumar ◽  
B.K. Madhu
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Angle Of Repose ◽  
Flow Properties ◽  
Disintegration Time ◽  
Powder Mixtures ◽  
Orodispersible Tablets ◽  
Maximum Water ◽  
Wetting Time ◽  
High Degree

The main objective of this study was to formulate orodispersible tablets of Dimenhydrinate for quick relief of emesis. Orodispersible tablets were prepared by direct compression method using co-processed super-disintegrants. Co-processed super-disintegrants are the mixture of crospovidone and guar gum in different ratios. The powder mixtures and tablets were subjected to various pre-compression and post-compression evaluations. IR spectroscopy showed no interaction between drug and other excipients. Angle of repose and Carr’s index was found in the range of 23.89°-28.27° and 23.29-15.48 respectively. These results indicated that powder mixtures showed good to acceptable flow properties. All formulations containing co-processed super-disintegrant showed short disintegration time (38.23-17.67 s) and maximum water absorption ratio 73.39%-91.35% compared to control formulation (3.54 min wetting time). Among all formulation F7 containing crospovidone: guar gum in 1:3 ratio showed highest percentage of drug release (98.89%) in 30 min, which is due to high degree of swelling caused by guar gum along with rapid hydration of tablets by crospovidone. Formulation F7 was subjected for 3 months of stability studies; results reviled that the tablet formulation was stable throughout the study period. In conclusion the obtained results suggested that orodispersible tablets of Dimenhydrinate with rapid disintegration and fast drug release can be successfully formulated by employing co-processed super-disintegrants. Kathmandu University Journal of Science, Engineering and TechnologyVol. 12, No. I, June, 2016 Page: 23-33

scholarly journals “Success Depends on Your Backbone”—About the Use of Polymers as Essential Materials Forming Orodispersible Films

Materials ◽  
2021 ◽  
Vol 14 (17) ◽  
pp. 4872
Author(s):  
Katarzyna Olechno ◽  
Anna Basa ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Geriatric Patients ◽  
Drug Dosage ◽  
Synthetic Polymers ◽  
Disintegration Time ◽  
Orodispersible Films ◽  
Pharmaceutical Technology ◽  
Drug Dosage Form ◽  
Novel Drug

Polymers constitute a group of materials having a wide-ranging impact on modern pharmaceutical technology. Polymeric components provide the foundation for the advancement of novel drug delivery platforms, inter alia orodispersible films. Orodispersible films are thin, polymeric scraps intended to dissolve quickly when put on the tongue, allowing them to be easily swallowed without the necessity of drinking water, thus eliminating the risk of choking, which is of great importance in the case of pediatric and geriatric patients. Polymers are essential excipients in designing orodispersible films, as they constitute the backbone of these drug dosage form. The type of polymer is of significant importance in obtaining the formulation of the desired quality. The polymers employed to produce orodispersible films must meet particular requirements due to their oral administration and have to provide adequate surface texture, film thickness, mechanical attributes, tensile and folding strength as well as relevant disintegration time and drug release to obtain the final product characterized by optimal pharmaceutical features. A variety of natural and synthetic polymers currently utilized in manufacturing of orodispersible films might be used alone or in a blend. The goal of the present manuscript was to present a review about polymers utilized in designing oral-dissolving films.

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