Effect of Hydroxypropyl Methylcellulose and Microcrystalline Cellulose in Design and Optimization of Nebivolol Hydrochloride Immediate Release Tablets by Response Surface Methodology

The goal of the research is to design and optimize Nebivolol Hydrochloride immediate-release tablet using response surface methodology. Nebivolol Hydrochloride immediate-release tablets used in the treatment of heart attacks, myocardial infarction. Response surface methodology calculations for this optimization study were performed utilizing Minitab 17. Different formulations of immediate-release were prepared by applying 2 factors 3 levels full factorial design using Minitab 17, which gave 9 formulations by using the wet granulation method. Independent variables like the amount of hydroxypropyl methylcellulose (X1), and microcrystalline cellulose (X2) and dependent variables like the per cent drug release at 45 minutes (Y1), disintegration (Y2) were selected for optimization. The prepared batches of Nebivolol Hydrochloride immediate-release tablets were evaluated for the pre-compression and post-compression parameters like weight variation, thickness, hardness, and friability, disintegration, and in-vitro drug release studies. All the Physico-chemical parameters were found satisfactory for prepared tablets. The optimized formulation F7 showed disintegrated in 83 sec, percentage dissolution release 97.85 at the end of 45th minute. The results shows that formulated immediate-release tablets of Nebivolol HCl were better to meet patient compliance with respect to effectiveness.

Download Full-text

Formulation, Optimization and in vitro Characterization of Stavudine Gastro Retentive Floating Matrix Tablets

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2016.080309 ◽

2016 ◽

Vol 8 (03) ◽

Author(s):

Mahendar Rupavath ◽

Kranthi G. ◽

Chinna Palem ◽

K. S. K. Patnaik

Keyword(s):

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Matrix Tablets ◽

Release Mechanism ◽

Wet Granulation ◽

Drug Bioavailability ◽

In Vitro Drug Release ◽

Weight Variation

The aim of the present investigation was to develop floating matrix tablets of stavudine to achieve prolong gastric residence time, leading to an increase in drug bioavailability and patient compliance. Floating tablets were prepared by wet granulation technique, using hydroxypropyl methylcellulose (HPMC K15M) as synthetic, pullulan gum as natural rate controlling polymers and optimum amounts of sodium-bicarbonate and citric acid as gas generating agents in suitable ratios to generate optimum buoyancy. Developed formulations were evaluated for weight variation, thickness, hardness, friability, drug content, in vitro drug release, floating lag time and floating buoyancy. All the formulations exhibited acceptable physical properties and the best formulation (F3) was selected based on in vitro characteristics. Further, the optimized formulation was evaluated for in vivo radiographic studies by incorporating BaSO4 as radio opaque substance. All the formulations were studied for in vitro drug release characteristics for 16 h. Optimized formulation showed controlled and prolonged drug release profiles while floating over the dissolution medium. Diffusion followed by erosion drug release mechanism was observed for the formulation, indicating that water diffusion and polymer erosion played an essential role in drug release. In vivo radiographic studies revealed that the tablets remained in the stomach for 8 ± 0.5 h in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered and desirable for absorption window drugs.

Download Full-text

FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF DONEPEZIL HYDROCHLORIDE

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2020v12i4.39049 ◽

2020 ◽

pp. 45-51

Author(s):

P. V. KAMALA KUMARI ◽

Y. SRINIVASA RAO

Keyword(s):

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Wet Granulation ◽

High Concentration ◽

Disintegration Time ◽

In Vitro Drug Release ◽

Orodispersible Tablets ◽

Weight Variation ◽

Donepezil Hydrochloride

Objective: The present study was aimed to develop the formulation and in vitro evaluation of Orodispersible tablets by wet granulation method using Donepezil HCl as a model drug to enhance patient compliance. Methods: In the wet granulation method, a mixture of microcrystalline cellulose and hydroxypropyl methylcellulose were used along with superdisintegrants, i.e., croscarmellose sodium and crospovidone. The prepared granules were subjected to both pre and post-compression evaluation parameters including; FTIR spectroscopy, micromeritics properties, tablet weight variation, hardness, friability, drug content, disintegration time and in vitro drug release. Results: FTIR studies indicated that there was nointeraction between the drug and the excipients used. The formulation containing high concentration of crospovidone and mixture as the best formulation F2 based on in vitro drug release characteristics of tablet formulation. Conclusion: The results of this work suggested that orodispersible tablets of Donepezil hydrochloride with rapid disintegration time, fast drug release and good hardness can be efficiently and successfully formulated by wet granulation method.

Download Full-text

DESIGN AND EVALUATION OF INTRAGASTRIC BUOYANT TABLETS OF VENLAFAXINE HYDROCHLORIDE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i5.16948 ◽

2017 ◽

Vol 10 (5) ◽

pp. 166

Author(s):

Parasuram Rajam Radhika ◽

Nishala N ◽

Kiruthika M ◽

Sree Iswarya S

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Xanthan Gum ◽

Hydroxypropyl Methylcellulose ◽

Methyl Cellulose ◽

In Vitro Drug Release ◽

Weight Variation ◽

Floating Drug Delivery ◽

Venlafaxine Hydrochloride

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate theintragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulationswere formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration ofdrug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitrobuoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimizedformulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMCK100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studiesand was found to be stable as no significant change was observed in various evaluated parameters of the formulation.Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach toincrease gastric residence time, thereby improving its bioavailability.Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P,Xanthan gum.

Download Full-text

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

International Current Pharmaceutical Journal ◽

10.3329/icpj.v6i11.36435 ◽

2018 ◽

Vol 6 (11) ◽

pp. 61-80 ◽

Cited By ~ 1

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

Download Full-text

Design, Development and Evaluation of Instant Release Oral Thin Films of Flunarizine

International Journal of Pharmaceutical Sciences Review and Research ◽

10.47583/ijpsrr.2021.v71i01.016 ◽

2021 ◽

Vol 71 (1) ◽

Author(s):

Asfiya Fatima ◽

Mamatha Tirunagari ◽

Divya Theja Chilekampalli

Keyword(s):

Thin Films ◽

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Rapid Onset ◽

In Vitro Dissolution ◽

Design Development ◽

Onset Of Action ◽

Weight Variation ◽

Accelerated Stability

The main objective of the present study was to prepare and evaluate the instant release oral thin films of Flunarizine, in order to enhance the bioavailability of the drug and to provide rapid onset of action thereby improving patient compliance. The instant release oral thin films of Flunarizine were prepared by solvent casting method using film forming polymer like Hydroxypropyl Methylcellulose E-15. The film was evaluated for various physicochemical parameters that include thickness, weight variation, folding endurance, tensile strength, drug content and in vitro drug release studies. No differences were observed in in vitro dissolution of drug from the formulated film F1-F9 as the film instantly gets wet by dissolution medium. The drug release for F5 formulations was about 98.1%. The accelerated stability studies for the optimized film formulations F5 were performed that indicates that the formulated instant release oral thin films were unaffected after initial and 3 months storage under accelerated conditions.

Download Full-text

Development and evaluation of miconazole mucoadhesive tablets for oropharyngeal candidiasis

Tropical Journal of Pharmaceutical Research ◽

10.4314/tjpr.v16i10.3 ◽

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

Download Full-text

Response Surface Optimization of Sustained Release Metformin-Hydrochloride Matrix Tablets: Influence of Some Hydrophillic Polymers on the Release

ISRN Pharmaceutics ◽

10.5402/2012/364261 ◽

2012 ◽

Vol 2012 ◽

pp. 1-10 ◽

Cited By ~ 1

Author(s):

Amitava Roy ◽

Kalpana Roy ◽

Sarbani Roy ◽

Jyotirmoy Deb ◽

Amitava Ghosh ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Hydroxypropyl Methylcellulose ◽

Dissolution Kinetics ◽

Matrix Tablets ◽

Metformin Hydrochloride ◽

Wet Granulation ◽

Matrix Tablet ◽

Response Surface Optimization

The aim of the present work was designed to develop a model-sustained release matrix tablet formulation for Metformin hydrochloride using wet granulation technique. In the present study the formulation design was employed to statistically optimize different parameters of Metformin hydrochloride tablets at different drug-to-polymer ratios employing polymers Hydroxypropyl methylcellulose of two grades K4M and K100M as two independent variables whereas the dependent variables studied were X60, X120, T50, T90, n, and b values obtained from dissolution kinetics data. The in vitro drug release studies were carried out at simulated intestinal fluids, and the release showed a non-Fickian anomalous transport mechanism. The drug release was found to reveal zero order kinetics. The granules and the tablets were tested for their normal physical, morphological, and analytical parameters and were found to be within the satisfactory levels. There were no significant drug-polymer interactions as revealed by infrared spectra. It has been found out that on an optimum increased Hydroxypropyl methylcellulose K100M concentration and decreased Hydroxypropyl methylcellulose K4M concentration the formulations were elegant in terms of their release profiles and were found to be statistically significant and generable.

Download Full-text

FORMULATION AND IN-VITRO EVALUATION OF THEOPHYLLINE HYDROCHLORIDE EFFERVESCENT FLOATING TABLETS: EFFECT OF POLYMER CONCENTRATION ON TABLET BUOYANCY

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2020v12i1.35055 ◽

2019 ◽

pp. 59-65

Author(s):

AKPABIO E. I. ◽

EFFIONG D. E. ◽

UWAH T. O. ◽

SUNDAY N. I.

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Polymer Concentration ◽

Hydroxypropyl Methylcellulose ◽

Controlled Drug Release ◽

Fickian Diffusion ◽

Wet Granulation ◽

Floating Tablets ◽

Swelling Characteristics

Objective: This study was undertaken to formulate a floating drug delivery system of theophylline hydrochloride using different concentrations of a chosen polymer and then investigate how polymer concentration affects buoyancy and drug release properties of the tablets. Methods: Hydroxypropyl methylcellulose (HPMC) at different concentration levels of 15% (F1), 20% (F2) and 30% (F3) was used to form the three formulation batches of floating tablets. Wet granulation method was used for the granule preparation while Sodium bicarbonate and citric acid were used as the gas generating agent. The physical properties of the granules and the floating tablets were evaluated. Also determined were the physicomechanical properties, buoyancy and swelling characteristics of the tablets. The in vitro drug release study was carried out according to the USP I (basket method) for 8h in 900 ml 0.1N HCl at 50 rpm. Samples withdrawn at the regular predetermined time were analyzed spectrophotometrically at a wavelength of 271 nm and data obtained statistically analyzed by one-way analysis of variance (ANOVA). The differences between means were considered significant at P<0.05. Results: The result showed that polymer (HPMC) concentration significantly (p>0.05) increased swelling index and improved floating lag time, it had no significant effect on the total floating time. Percentage drug release at the end of 8 h was 100%, 98.2% and 96.13% for formulation F1, F2 and F3, respectively. All three formulations followed the Higuchi drug release kinetics model and the mechanism of drug release was the non Fickian diffusion with exponents of 0.46, 0.51 and 0.56 for the respective batch. Conclusion: Batch F3 gave a better-controlled drug release and floating properties in comparison to batch F1 and F2 thus Polymer concentration influenced the onset of floating and controlled the release of Theophylline.

Download Full-text

Fexofenadine HCl Immediate Release Tablets: In vitro Characterization and Evaluation of Excipients

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v16i1.14483 ◽

2013 ◽

Vol 16 (1) ◽

pp. 1-9

Author(s):

Shahriar Ahmed ◽

Mehrina Nazmi ◽

Ikramul Hasan ◽

Sabiha Sultana ◽

Shimul Haldar ◽

...

Keyword(s):

Drug Release ◽

Immediate Release ◽

Pharmaceutical Journal ◽

In Vitro Dissolution ◽

Disintegration Time ◽

Sodium Starch Glycolate ◽

In Vitro Characterization ◽

Weight Variation ◽

Fexofenadine Hcl

Fexofenadine HCl immediate release tablets were designed to increase the dissolution rate by using superdisintegrants. Different formulations of Fexofenadine HCl were prepared by direct compression method. These formulations were evaluated for hardness, thickness, friability, weight variation, disintegration time, and in vitro dissolution study. The drug release from the formulations were studied according to USP specification (USP paddle method at 50 rpm for 60 minutes) maintaining the temperature to 37°C. Sodium starch glycolate, cross carmellose sodium, crospovidone (kollidon CL), ludiflash and xanthan gum were used in 3%, 6% and 8% concentrations as superdisintegrants. Thus, the ratio of superdisintegrants was changed whereas all the other excipients as well as the active drug (Fexofenadine HCl) remained same in every formulation. Here, 0.001N HCl was used as dissolution medium according to USP and absorbances were determined by using UV spectrophotometer at 217 nm. The F-3 and F-6 formulation prepared by 8% of Sodium starch glycolate and 8% of Cross carmellose sodium showed 99.99% drug release within 30 minutes and 45 minutes, respectively. The disintegration times of F-3 and F-6 formulation were within 9 seconds. The interactions between drug and excipients were characterized by FTIR spectroscopic study. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14483 Bangladesh Pharmaceutical Journal 16(1): 1-9, 2013

Download Full-text