Influence of Hydroxypropyl Methylcellulose on Flowing and Swelling Parameters in Biomucoadhesive Tablets with Miconazole Nitrate

2017 ◽  
Vol 68 (10) ◽  
pp. 2346-2349
Author(s):  
Magdalena Birsan ◽  
Nela Bibire ◽  
Madalina Vieriu ◽  
Alina Diana Panainte ◽  
Ileana Cojocaru
Keyword(s):  
Friction Coefficient ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Pharmaceutical Formulations ◽  
Direct Compression ◽  
Miconazole Nitrate ◽  
Proportionality Relationship ◽  
Formulation Variables

Original pharmaceutical formulations have been produced as oral biomucoadhesive tablets for antifungal medication. They have been obtained through direct compression using as matrix forming polymers various sorts of hydroxypropyl methylcellulose. The main goal of the study was determining the swelling index of the new mucobioadhesive formulations with miconazole nitrate in order to correctly evaluate the time of contact with mucosa, and the prolongation of drug release. For each formulation, the flowing parameters have been determined: flowing time, friction coefficient, repose angle, Haussner ratio, Carr index, and the swelling index for 6 formulations containing various sorts of hydroxypropyl methylcellulose as matrix molders, while the formulation variables studied were time and association ratio between those polymers. Though results analysis, we noticed that the values of the swelling index depended on the type and quantity of polymer, results that could also be explained by the proportionality relationship to flowing and compressibility parameters.

scholarly journals Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil

2019 ◽  
Vol 9 (4) ◽  
pp. 574-578
Author(s):  
Mohammad Faizan Mohammad Gufran ◽  
Sailesh Kumar Ghatuary ◽  
Reena Shende ◽  
Prabhat Kumar Jain ◽  
Geeta Parkhe
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Log P ◽  
Physical Parameters ◽  
Direct Compression ◽  
Formulation Development ◽  
Compression Technique

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.

IDENTIFICATION OF KEY VARIABLES AFFECTIN G DRUG RELEASE FROM LIPID MATRIX IN HYDROALCOHOLIC DISSOLUTION MEDIUM CONTAININ G HYDROXYPROPYL METHYLCELLULOSE

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (11) ◽  
pp. 72-76
Author(s):  
P. R Babariya ◽  
◽  
M. C Gohel ◽  
V. T. Thakkar ◽  
L. H. Baldaniya ◽  
...  
Keyword(s):  
Drug Release ◽  
Alcohol Intake ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Direct Compression ◽  
Dissolution Medium ◽  
Experimental Conditions ◽  
Dissolution Study ◽  
Key Variables ◽  
Compritol 888 Ato

The present research work was undertaken to formulate modified release tablets of lornoxicam using Compritol 888 ATO as a lipid matrixing agent and to evaluate the tablets for dissolution in hydro-alcoholic dissolution media to meet the requirement of regulators. The dissolution study was also conducted in aqueous medium containing alcohol and hydroxylpropyl methylcellulose to mimic the viscosity and pH after food and alcohol intake. The tablets were prepared by direct compression by adopting the concept of design of experiments and evaluated mainly for dissolution studies in aqueous dissolution media containing 10, 25 and 40% ethyl alcohol. The formulated tablets satisfied the USP requirements of drug release at 2, 6 and 10 hr. The drug release was insignificantly altered when the dissolution study was conducted in media containing increasing amount of alcohol probably due to higher solubility of the drug in alcohol. The drug release was suppressed when HPMC was used in the dissolution media. This may be due to rise in viscosity of the dissolution media. Dose dumping was not noticed under the experimental conditions.

Design of Floating HPMC Matrix Tablets: Effect of Formulation Variables on Floating Properties and Drug Release

2011 ◽  
Vol 311-313 ◽  
pp. 1140-1143
Author(s):  
Srisagul Sungthongjeen ◽  
Pornsak Sriamornsak ◽  
Satit Puttipipatkhachorn
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Hydraulic Press ◽  
Matrix Tablets ◽  
Compression Force ◽  
Lower Viscosity ◽  
Floating Tablet ◽  
Tablet Formulations ◽  
Model Drug ◽  
Formulation Variables

Floating matrix tablets were designed and evaluated. Theophylline was used as a model drug. The system was prepared by mixing drug, matrix-forming polymer (hydroxypropyl methylcellulose, HPMC) and fillers together. The blended powder was compressed by hydraulic press. The effect of formulation variables such as type of matrix forming polymer (HPMC K100LV, HPMC K4M, HPMC K100M), amount of effervescent agent (0, 20, 30, 40% w/w) and compression force (0.5, 1 ton) on floating properties and drug release of floating matrix tablets were investigated. The results demonstrated that type of polymer affected floating properties of the floating matrix tablets. The floating matrix tablets prepared from lower viscosity HPMC (HPMC K100LV) showed faster drug release than those prepared from higher viscosity HPMC (HPMC K4M, HPMC K100M). Increasing amount of effervescent agent decreased time to float and increased drug release from the floating matrix tablets. Higher compression force did not affect time to float but decreased drug release from the floating matrix tablets. According to these results, floating properties and drug release of the floating matrix tablets could be modified by formulation variables. Some floating tablet formulations developed in this study showed good floating properties (time to float less than 15 minutes, floating time more than 8 hours) with sustained release as required. The system is promising as a carrier for gastroretentive drug delivery systems.

scholarly journals Development of extended-release formulation of domperidone using a blend of Raphia hookeri gum and hydroxypropyl methylcellulose as tablet matrix

2017 ◽  
Vol 16 (10) ◽  
pp. 2341-2347
Author(s):  
Emmanuel O. Olorunsola ◽  
Stephen O. Majekodunmi
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Extended Release ◽  
Hydroxypropyl Methylcellulose ◽  
Direct Compression ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
Raphia Hookeri ◽  
The Matrix ◽  
The Individual

Purpose: To develop an extended-release formulation of domperidone using a blend of Raphia hookeri gum and hydroxypropyl methylcellulose as tablet matrix.Methods: Tablets (400 mg) containing 30 mg domperidone (DPD) were formulated using binary mixtures of hydroxypropyl methylcellulose (HPMC) and Raphia hookeri gum (RHG) as matrix former; and microcrystalline cellulose (MCC) as direct compression excipient. The proportions of the matrix formers (40 % of tablet weight) was varied as 100:0, 75:25, 50:50, 25:75 and 0:100. The composition of the matrix former was also kept constant (50:50) while MCC was varied as 40, 30, 20 and 10 %. The tablets were evaluated for compact density, tensile strength, friability and drug release over 24 h.Results: The tensile strength of tablets decreased while their friability increased with increase in the proportion of RHG. A similar trend was observed with decrease in the concentration of MCC. Tablets containing RHG alone as matrix former and 40 % MCC as direct compression excipient had tensile strength of 0.95 MNm-2, friability of 1.07 % and cumulative drug release of 83.2 % over a period of 24 h. Tablets containing equal proportions of HPMC and RHG as matrix former had the best release properties of 95.0 % over a period of 24 h.Conclusion: RHG is comparable with HPMC in terms of extending the release of  domperidone for a once daily administration. A suitable combination of the two  polymers for use as a matrix former is superior to either of the individual polymers.Keywords: Domperidone, Extended drug release, Hydroxypropyl methylcellulose, Raphia hookeri gum, Tablet properties

Evaluation of Curcuminoids Effervescent Floating Tablets

2014 ◽  
Vol 1060 ◽  
pp. 25-28
Author(s):  
Sakonjan Treesinchai ◽  
Satit Puttipipatkhachorn ◽  
Tasana Pitaksuteepong ◽  
Srisagul Sungthongjeen
Keyword(s):  
Drug Release ◽  
Sodium Lauryl Sulfate ◽  
Hydroxypropyl Methylcellulose ◽  
Protective Layer ◽  
Lauryl Sulfate ◽  
Floating Tablets ◽  
Floating Tablet ◽  
Core Tablet ◽  
Formulation Variables ◽  
Reduced Time

The objective of this study was to develop and evaluate curcuminoids effervescent floating tablet. The system consists of a curcuminoids-containing core tablet coated with a gas forming layer (tartaric acid layer and sodium bicarbonate layer divided by a protective layer (hydroxypropyl methylcellulose)) and a gas-entrapped membrane (Eudragit® RL 30D), respectively. The floating tablets using lactose as a filler showed higher drug release than those using microcrystalline cellulose (MCC) or MCC:lactose as a filler. However, type of core tablet fillers did not affect time to float of the floating tablets in 0.1 N HCl. Increasing amount of gas forming agent reduced time to float and increased drug release from the floating tablets. The floating tablets showed good floating properties in 0.1 N HCl, however, curcuminoids released was very slow. Addition of surfactant (1%w/v sodium lauryl sulfate (SLS)) in 0.1 N HCl could improve drug release of the floating tablets but it increased time to float and caused the floating tablet ruptured. The floating properties and drug release from curcuminoids effervescent floating tablets seemed to depend on formulation variables. The higher coating level or another type of gas-entrapped membrane may be need for further study.

scholarly journals Design and Development of Bi-layered Sustained Release Azithromycin Tablets

2017 ◽  
Vol 15 (2) ◽  
pp. 227-234
Author(s):  
Muhammad Rashedul Islam ◽  
Md Mizanur Rahman Moghal ◽  
FM Shah Noman Ul Bari ◽  
Elias Al Mamun
Keyword(s):  
Spectral Analysis ◽  
Drug Release ◽  
Sustained Release ◽  
Direct Compression ◽  
Design And Development ◽  
Bilayer Tablet ◽  
Formulation Variables

The objective of the current study was to develop a bilayer tablet of Azithromycin containing both immediate and sustained layer and evaluate the effect of formulation variables on drug release. Thirty different formulations (F-1 to F-30) were prepared by direct compression. When the fraction of polymer was increased from 5.55% to 10%, the rate of drug release was found to be slower. Maximum release of Azithromycin was from F-11 (within 8 hours), which contained 50 mg (5.55%) of HPMC 50 cps. Slowest release was observed from F-30 containing 90 mg (10%) of Carbopol 974 P. The IR spectral analysis revealed that all rate regarding agents and excipients used in this study are compatible with the active Azithromycin.Dhaka Univ. J. Pharm. Sci. 15(2): 227-234, 2016 (December)

scholarly journals APPLICATION OF QUALITY BY DESIGN APPROACH FOR THE OPTIMIZATION OF ORODISPERSIBLE FILM FORMULATION

2018 ◽  
Vol 11 (14) ◽  
pp. 8
Author(s):  
Ashutosh Gupta ◽  
Jatin Kumar ◽  
Surajpal Verma ◽  
Harmanpreet Singh
Keyword(s):  
Drug Release ◽  
Propylene Glycol ◽  
Quality By Design ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Dissolution ◽  
Polyethylene Glycol 400 ◽  
Disintegration Time ◽  
Peg 400 ◽  
Film Forming ◽  
Formulation Variables

Objective: The present study was done to understand the effect of formulation variables on the quality of orodispersible films using quality by design (QbD) approach as mentioned in ICH Q8 (R2) guideline.Methods: A definitive screening design of experiments (DoE) was used to identify and classify the critical formulation variables affecting critical quality attributes (CQA) using 2×2 factorial design. Based on prescreening study, the critical formulation variables, i.e. concentration of film-forming polymer and plasticizers (propylene glycol and polyethylene glycol 400 [PEG 400]) were kept in the range of 1.5–2.5% w/w and 0.5–1% v/v, respectively. A total of eight laboratory-scale formulations were prepared which were provided by DoE using solvent casting method. These batches were evaluated for CQA’s, i.e. mechanical properties such as folding endurance (FD) and disintegration time (DT). Data were analyzed for elucidating interactions between two variables and for providing a predictive model for the process. Finally, the drug was incorporated into optimized batches, and these were evaluated for in vitro dissolution study in simulated saliva (pH 6.8) as well as their mechanical properties.Results: The results suggested that the concentration of film-forming polymer and plasticizer was critical to manufacture orodispersible film with desired CQA, i.e. mechanical property (FD [>150 folds]) and DT (<60 s). The percent drug release, FD, and DT of optimized Formulation I (hydroxypropyl methylcellulose [HPMC] E5 (2%) and propylene glycol [0.15 mL]) were found to be 82.13%±0.260 (in 15 min), 164±2, and 49±1.5 s, respectively, and for optimized Formulation II (HPMC E5 [2%] and PEG 400 [0.15 mL]) was found to be 64.26%±2.026 (in 15 min) and 218±6 and 55±4 s, respectively.Conclusion: From the results, it has been found that the percentage drug release of naratriptan hydrochloride containing propylene glycol as a plasticizer was greater than the formulation containing PEG 400 as plasticizer. From this, we concluded that QbD is very much useful approach to get an optimized formulation in an economic and faster way in comparison to traditional method (hit and trail methods). The futuristic application of the film will involve the management of an acute migraine.

Influence of Formulation Variables and Processing Techniques on Drug Release from Carbopol-971 based Matrix Tablets of Cinnarizine and Nimodipine.

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Singh K. ◽  
Pandit K. ◽  
Mishra N.
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Weight Variation ◽  
Diffusion Controlled ◽  
The Matrix ◽  
Processing Techniques ◽  
Formulation Variables

The matrix tablets of cinnarizine and nimodipine were prepared with varying ratio of Carbopol- 971P and co-excipients of varying hydrophilicity (i.e. dicalcium phosphate and spray dried lactose) by direct compression and wet granulation using alcoholic mucilage. The prepared tablets were evaluated for weight variation, hardness and friability. The influence of concentration of the matrix forming material and co-excipients on the release rate of the drug was studied. The release rate of Cinnarizine (more soluble drug) from tablets followed diffusion controlled mechanism whereas for nimodipine (less soluble drug), the drug release followed case-II or super case- II transport mechanism based on Korsmeyer- Peppas equation. The results indicated that the drug release from matrix tablets was increases with increase in hydrophilicity of drug and co-excipients. The release of drug also increased with thermal treatment and decreasing polymer concentration.

Pharmaceutical Polymers - A Review

2019 ◽  
Vol 9 (01) ◽  
pp. 27-33
Author(s):  
Naveen Kumar ◽  
Sonia Pahuja ◽  
Ranjit Sharma
Keyword(s):  
Drug Release ◽  
Industrial Revolution ◽  
Pharmaceutical Formulations ◽  
Pharmaceutical Products ◽  
Water Soluble ◽  
Taste Masking ◽  
Natural Polymers ◽  
Pharmaceutical Dosage Forms ◽  
Pharmaceutical Applications ◽  
Pharmaceutical Industries

Humans have taken advantage of the adaptability of polymers for centuries in the form of resins, gums tars, and oils. However, it was not until the industrial revolution that the modern polymer industry began to develop. Polymers represent an important constituent of pharmaceutical dosage forms. Polymers have played vital roles in the formulation of pharmaceutical products. Polymers have been used as a major tool to manage the drug release rate from the formulations. Synthetic and natural-based polymers have found their way into the biomedical and pharmaceutical industries. Synthetic and Natural polymers can be produced with a broad range of strength, heat resistance, density, stiffness and even price. By constant research into the science and applications of polymers, they are playing an ever-increasing role in society. Diverse applications of polymers in the present pharmaceutical field are for controlled drug release. Based on solubility pharmaceutical polymers can be classified as water-soluble and water-insoluble. In general, the desirable polymer properties in pharmaceutical applications are film forming, adhesion, gelling, thickening, pH-dependent solubility and taste masking. General pharmaceutical applications of polymers in various pharmaceutical formulations are also discussed

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