3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Batch Size ◽  
Metoprolol Succinate ◽  
Zero Order Kinetics ◽  
Two Factors ◽  
Puffed Rice ◽  
Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

scholarly journals Formulation and investigation of crushed puffed rice-chitosan-HPMC based polymeric blends as carrier for sustained stomach specific drug delivery of piroxicam using 3(2) Taguchi mathematical design studies

2018 ◽  
Vol 6 (11) ◽  
pp. 61-80 ◽  
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Pharmaceutical Journal ◽  
Weight Variation ◽  
Zero Order Release ◽  
Puffed Rice

In the present experimental investigation an attempt has been made to assess the utility of Crushed Puffed Rice (CPR)-High Molecular Weight Chitosan (HMWCH)-Hydroxypropyl Methylcellulose K15M (HPMC K15M) as a polymeric carrier for the sustained stomach delivery of Piroxicam (PRX). A total of nine formulations were prepared by using 3 (2) Taguchi factorial design, physically blending drug and polymer(s) followed by encapsulation into hard gelatin capsules size 1. The prepared capsules were evaluated for various performance such as weight variation, drug contents, in vitro buoyancy and drug release in 0.1 M HCl. The effect of drug loading on in vitro performance of the formulations was also determined. Crushed puffed rice (CPR) remained buoyant for up to average time span of 06 hr as an unwetted irregular mass in 0.1 M HCl. However, when combined with HMWCH or HPMC K15M or HPMC K15M + HMWCH a low -density cylindrical raft type hydrogel was formed which remained buoyant for up to 12 hr and released up to 99% drug in a sustained manner from 8 to 12 hr following zero order release kinetics. It was also observed that drug release from drug + CPR matrices followed Fickian mechanism. Combination of CPR + HMWCH or HMWCH + HPMC K15M also follows Fickian mechanism. Obtained data from the research work suggests that CPR in combination with HMWCH or HPMC K15M or HPMC has sufficient potential to be used as a carrier for stomach specific delivery of gastric irritant drug like PRX.Soni et al., International Current Pharmaceutical Journal, April 2018, 6(11): 61-80http://www.icpjonline.com/documents/Vol6Issue11/01.pdf

scholarly journals Development and evaluation of miconazole mucoadhesive tablets for oropharyngeal candidiasis

2017 ◽  
Vol 16 (10) ◽  
pp. 2325-2330
Author(s):  
Qiong Jin ◽  
Wei Chen ◽  
Wan Wu
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Extended Period ◽  
Content Uniformity ◽  
Oropharyngeal Candidiasis ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Mucoadhesive Tablets

Purpose: To develop mucoadhesive tablets containing miconazole (MCZ) for the treatment of oropharyngeal candidiasis, using chitosan and hydroxypropyl methylcellulose (HPMC) as mucoadhesive polymers.Methods: Mucoadhesive tablets were formulated and optimized using a 23 factorial design and direct compression method. The independent variables were compression force and concentrations of chitosan and HPMC, while mucoadhesion time and in vitro drug release were dependent variables. Tablet characterization was carried out by evaluating hardness, thickness, tablet weight variation, content uniformity, friability and in vitro drug release at salivary pH (pH 6.8).Results: The tablets showed good mucoadhesion for an extended period (8 h), and their physical characteristics were within acceptable ranges. Drug release ranged from 60.5 % to 80.8 %.Conclusion: These results indicate that the mucoadhesive MCZ tablets formulated with chitosan and HPMC possess potential for the development of therapeutic preparations for management of oropharyngeal candidiasis.Keywords: Miconazole, Oropharyngeal candidiasis, Factorial design, Mucoadhesion, Chitosan, Drug release

Formulation and Evaluation of Gastro-Retentive Floating Extended Release Metoprolol Tablets using Sodium Alginate and HPMC K-100M Combination

2015 ◽  
Vol 8 (3) ◽  
pp. 2947-2954
Author(s):  
Ashok Thulluru ◽  
M. Mohan Varma ◽  
C M Setty ◽  
Pavan Kumar Chintamaneni ◽  
S. Sriharsha Vardhan
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Fickian Diffusion ◽  
Wet Granulation ◽  
Average Weight ◽  
Metoprolol Succinate ◽  
Floating Tablets ◽  
Zero Order Kinetics ◽  
Gastro Retentive

The present study was aimed to convert Metoprolol Succinate convert into Gastro Retentive Floating Tablet (GRFT). The gas generating floating tablets of Metoprolol Succinate were prepared to increase the gastric retention and to extend the drug release up to 12 hr. and thereby enhancing its bioavailability. The floating tablets were formulated using HPMCK 100M alone and with the combination of sodium alginate to the polymer of varying concentrations. The tablets were prepared by non-aqueous wet granulation method. The formulated granules were evaluated for pre-compression studies, after the compression of tablets they were subjected to various post-compression studies: Average weight, thickness, density, hardness, % friability, % drug content, (In vitro buoyancy studies: floating time, total floating time and matrix integrity up to 12 hr) and the In vitro drug release studies. The optimized formulation (F4) was found to follow a near perfect zero order kinetics (regression coefficient,      r2 = 0.978). Higuchi plot for formulation, F4, showed r2 value of 0.978, suggesting that the diffusion and erosion plays an important role in the controlled release of the drug. The data was fitted to the Korsemeyer-Peppa’s equation; and the value of the diffusion component (n=0.654), for the formulation F4, indicated that the drug release follows non-Fickian diffusion.  

scholarly journals IN VITRO DRUG RELEASE STUDY OF CHLORAMPHENICOL IN SITU GEL WITH BASES MIXTURE OF POLOXAMER 407 AND HPMC BY OPTIMIZATION WITH FACTORIAL DESIGN

2021 ◽  
pp. 116-123
Author(s):  
INSAN SUNAN KURNIAWANSYAH ◽  
TAOFIK RUSDIANA ◽  
HURIYATUS TSANIYAH ◽  
HANDRIAN RAMOKO ◽  
HABIBAH A. WAHAB ◽  
...  
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
In Situ Gel ◽  
Vitro Assay ◽  
Cumulative Amount

Objective: The objective of this study was to find the best base mixture composition (poloxamer 407 and HPMC) of chloramphenicol in situ gel formula based on in vitro property (Cumulative amount of drug release). Methods: The in vitro diffusion of chloramphenicol in situ gel study was carried out using franz diffusion cells to know the effect of the Critical Process Parameters (CPPs) as independent variables (poloxamer 407 and hydroxypropyl methylcellulose (HPMC)) on the Critical Quality Attribute (CQA) as dependent variable (cumulative amount of drug release) with 22 factorial design. Results: 22 factorial design of chloramphenicol in situ gel yielded 4 variations of poloxamer 407 and HPMC bases component in %w/v as follows, F1 (5:0.45), F2 (10:0.45) F3 (5:1) and F4 (10:1). The amount of drug release results from in vitro dissolution assay were 30.60% (F1), 45.64% (F2), 58.30% (F3), and 22.50%) (F4). Conclusion: Formula 3 (F3) was considered as the best formula component in terms of in vitro assay of chloramphenicol in situ gel with a desirability value of 0.58.

scholarly journals PREPARATION AND EVALUATION OF FAST DISSOLVING TABLETS OF PITAVASTATIN BY 32 FULL FACTORIAL DESIGN

2019 ◽  
pp. 108-114
Author(s):  
NIRMALA DASARI ◽  
VIDYAVATHI MARUVAJALA
Keyword(s):  
Drug Release ◽  
Water Absorption ◽  
Factorial Design ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Absorption Ratio ◽  
Conventional Film ◽  
Two Factors ◽  
The Stability

Objective: The objective of the present work was to prepare an optimized, fast dissolving tablet (FDT) of Pitavastatin to increase its dissolution by applying 32full factorial design. Methods: Nine formulations (PF1 to PF9) with all possible combinations according to 32full factorial design by selecting two factors i.e. concentration of super disintegrant, Indion414 (5-15%) (A) and sublimating agent, camphor (40-60%) (B) as independent variables at three levels of-1, 0 and 1. The effect of these two variables on three dependent parameters, water absorption ratio (Y1), disintegration time (Y2) and in vitro drug release (Y3) was studied. All the powder blends were evaluated for precompression parameters, and the tablets were prepared by direct compression method which were further evaluated for post-compression parameters. The effect of change in concentration of two selected factors on dependent parameters was studied through 3D surface response plots and polynomial equations using Design expert software version11. Optimized formula was obtained by desirability and overlay plots for which compatibility stability was assessed. Results: Precompression and post-compression parameters were satisfactorily within acceptable limits. Optimized formulation was prepared to prove the validity of the evolved mathematical model, which contained 6.75 mg of indion414(0.9) and 54 mg of camphor(0.9) with a disintegration time of 21 sec., water absorption ratio of 113 and 93% of drug release within 12 min. The compatibility between drugs and excipients was proved. The dissolution profiles of optimized formulation and commercially available conventional film-coated tablets of Pitavastatin were compared. Conclusion: The optimized formulation showed significantly (P>0.05) increased drug release compared to commercially available film-coated tablets. No changes in disintegration time, drug content and in in vitro drug release from optimized formulation on storage for 3months at 40 °C±2 °C/75% RH±5% RH were observed during stability studies which confirmed the stability of the optimized formulation.

scholarly journals Development and in vitro evaluation of sustained release multiparticulate tablet of freely water soluble drug

2010 ◽  
Vol 46 (3) ◽  
pp. 463-471 ◽  
Author(s):  
Ashlesha Pravin Pandit ◽  
Rajendra Dattatray Shinde
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Dispersion ◽  
Water Soluble ◽  
Coating Materials ◽  
Metoprolol Succinate ◽  
Water Soluble Drug ◽  
Zero Order Release

Blends of aqueous dispersion of a hydrophobic and hydrophilic polymer, namely Surelease®: hydroxypropyl methylcellulose (Surelease®: HPMC E15) were used as coating materials to control the drug release from coated pellets of the highly water soluble drug metoprolol succinate. Varying the polymer blends, ranges of drug release patterns were obtained at pH 6.8. The present study dealt with diffusion of drug through plasticized Surelease®/ hydroxypropyl methylcellulose (HPMC E15) films prepared by coating of drug and polymers onto non-pareil seeds using the solution layering technique. The release of metoprolol succinate from coated pellets was decreased with increased coating load of polymer. The optimized formulation was obtained by 3² full factorial design. The release profile revealed that the optimized formulation follows zero order release kinetics. The stability data showed no interaction for storage at 25ºC and 60% relative humidity.

scholarly journals Osmotic release tablets formulation and evaluationof ace inhibitor molecule

2021 ◽  
pp. 24-35
Author(s):  
Prachetha Kolli ◽  
Sudhakar Kancharla ◽  
Dr.K.Venkata Gopaiah
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Magnesium Stearate ◽  
Wet Granulation ◽  
Inhibitor Molecule ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Manufacturing Procedure ◽  
Release Data

In the present study the Suitable analytical methods were developed for the drug using UV – visible spectrophotometer. From the Preformulation study and thermal analysis (DSC), the interference was verified and found that the drug did not interfere with the excipient use.Core tablet was successfully prepared by wet granulation using Polyethylene oxide WSR N80, Mannitol 25C, silicon dioxide, magnesium stearate, Polyethylene WSR 303, sodium chloride, hydroxypropyl methylcellulose (HPMC E5), Iron oxide red. Isopropyl cellulose was found to be suitable granulating fluid for binder.Formulation of the drug coating was optimized by using 22 factorial design of experiment.The coated tablets were evaluated for various physicochemical parameter. About  79 to 95% of drug was released from the formulation A-E in 24 hr in 6.8 phosphate buffer.The in vitro drug release data were plotted in zero order kinetics and optimized batch were evaluated on the basis of regression coefficient.The in-vitro drug release from the optimized formulation in the dissertation was directly proportional to the concentration of plasticizer and concentration of cellulose acetate.The manufacturing procedure was standardized and reproducible

Preparation and Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets in Healthy Human Volunteers

2017 ◽  
Vol 10 (1) ◽  
pp. 3623-3630
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Haarika B ◽  
Jyothi Sri S ◽  
K Abbulu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Drug Bioavailability ◽  
Floating Tablets

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.   

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

Novel Herbal Topical Patch Containing Curcumin and Arnica montana for the Treatment of Osteoarthritis

2020 ◽  
Vol 16 (1) ◽  
pp. 43-60 ◽  
Author(s):  
Priyanka Kriplani ◽  
Kumar Guarve ◽  
Uttam Singh Baghel
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Analgesic Activity ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Methyl Cellulose ◽  
World Population ◽  
Jojoba Oil ◽  
Arnica Montana ◽  
Transdermal Patches

Background: Osteoarthritis (OA) ranks fifth among all forms of disability affecting 10% of the world population. Current treatments available are associated with multiple side effects and do not slow down the progression of the disease. Moreover, no such effective treatment is available to date in various systems of medicine to treat osteoarthritis. Curcumin and Arnica have shown evident clinical advances in the treatment of osteoarthritis. Objective: The aim of the present study was to design, optimize and characterize novel herbal transdermal patches of curcumin and Arnica montana using factorial design. Methods: A multiple factorial design was employed to investigate the effect of hydroxypropyl methyl cellulose, ethyl cellulose and jojoba oil on elongation and drug release. Transdermal patches were evaluated by FTIR, DSC, FESEM, ex vivo drug permeation, anti osteoarthritic activity and analgesic activity. Results: Independent variables exhibited a significant effect on the physicochemical properties of the prepared formulations. The higher values of drug release and elongation were observed with the higher concentration of hydroxypropyl methylcellulose and jojoba oil. Anti osteoarthritic activity was assessed by complete Freund's adjuvant arthritis model; using rats and analgesic activity by Eddy's hot plate method, using mice. Combination patch exhibited good anti osteoarthritic and analgesic activity as compare to individual drug patches. Conclusion: The design results revealed that the combination patch exhibited good physicochemical, anti osteoarthritic and analgesic activity for the treatment of osteoarthritis in animals. More plants and their combinations should be explored to get reliable, safe and effective formulations that can compete with synthetic drugs.

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