Effect of various Polymers on Drug Release from Mucoadhesive Tablets of Cefixime Trihydrate

Cefixime trihydrate (CT) is a third-generation cephalosporin antibiotic and is used in the management of various infections caused by Gram +ve as well as Gram – ve bacteria. It has a plasma half-life of 3-4 h. It has poor oral bioavailability due to hepatic first pass metabolism. Hence, an attempt was made to develop CT mucoadhesive tablets for buccal delivery to avoid first-pass metabolism and improved oral delivery. CT mucoadhesive tablets developed using HPMC K4M, Na-CMC, guar gum and chitosan as rate controlling polymers and mucoadhesive agent, respectively and compressed by direct compression method. The prepared CT mucoadhesive tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, assay, mucoadhesive strength and in vitro release. From the results, all the evaluated parameters were within the pharmacopoeial limits. The in-vitro dissolution studies indicated that the CTmucoadhesive tablets formulation (F2) showed 99.7±1.4 % of drug release after 8 h and chose as the optimized formulation. The kinetic models suggest that the drug release follows Higuchi’s kinetics and tablets drug release was controlled by a diffusion mechanism.

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Formulation and Physicochemical Characterization of Buccal Mucoadhesive Films Containing Alfuzocin Hydrochloride

Journal of Advances in Medical and Pharmaceutical Sciences ◽

10.9734/jamps/2020/v22i230155 ◽

2020 ◽

pp. 9-20

Author(s):

Abikesh P. K. Mahapatra ◽

Sonia P. Nagvenkar ◽

Rajashree Gude

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Zero Order ◽

Content Uniformity ◽

Ideal System ◽

First Pass Metabolism ◽

Folding Endurance ◽

First Pass ◽

Pass Metabolism

The buccal region of oral cavity is a interesting target for the drug of choice administration. To increase prevent first pass metabolism and bioavailability, Alfuzocin Hydrochloride is embedded in buccal film for a sustained release over a period of 8 hours. The purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive films of Alfuzocin hydrochloride using the polymers HPMC K100M, Sodium Alginate and Chitosan. The films were provided with a backing layer of Eudragit RS100 so as to get an unidirectional release pattern. The films were evaluated for their physical characteristics like weight, thickness, content uniformity, folding endurance, bioadhesive strength, surface pH, in vitro drug release, ex vivo buccal permeation and XRD studies. The films, which were prepared by the solvent casting method, were smooth and elegant in appearance; uniform in thickness, weight, and drug content; and showed good folding endurance. The mechanical properties reveal that the formulations were found to be strong but not brittle. The in vitro release data were fit to different equations and kinetic models viz. zero order, first order, higuchi’s plot and peppas plot. The best mucoadhesive performance and matrix controlled release was exhibited by the formulation A7 (2% HPMC K100 M and 2% Chitosan). The correlation coefficient value (r) indicates, the kinetic of drug release was zero order. Stability study of optimized films was done and it was found that both drug and buccal films were stable. It can be concluded that the present buccal formulation can be an ideal system to improve the bioavailability of the drug by avoiding hepatic first-pass metabolism.

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Gastroretentive drug delivery system of a lipid lowering agent

International Current Pharmaceutical Journal ◽

10.3329/icpj.v2i9.16077 ◽

2013 ◽

Vol 2 (9) ◽

pp. 152-155

Author(s):

D. Krishnarajan ◽

N. Senthil Kumar ◽

Rajesh Yadav

Keyword(s):

Guar Gum ◽

Lipid Lowering ◽

In Vitro Dissolution ◽

Wet Granulation ◽

Natural Polymers ◽

First Pass Metabolism ◽

First Pass ◽

Mucoadhesive Tablets ◽

Pass Metabolism

The objective of this study was to develop mucoadhesive tablets of Simvastatin using natural polymers. Simvastatin has short biological half-life and high first pass metabolism hence which was designed to increase the gastric residence time which prolong the drug release. The tablets were prepared by wet granulation technique using Carbopol-934, guar gum, xanthine gum and chitosin as polymers. Formulations were evaluated for different parameters like hardness, friability, uniformity of weight, swelling characteristics, in vitro dissolution and kinetic studies. The dissolution was carried out for 12 hours in which the formulation with guar gum has shown highest dissolution release profile (F9). Thus the present study concludes that mucoadhesive tablets of simvastatin can be a good way to pass the extensive hepatic first pass metabolism and to improve the bioavailability of simvastatin.DOI: http://dx.doi.org/10.3329/icpj.v2i9.16077 International Current Pharmaceutical Journal, August 2013, 2(9): 152-155

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Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2016.9.3.8 ◽

1970 ◽

Vol 9 (3) ◽

pp. 3318-3329

Author(s):

Kranthi Kumar Kotta ◽

L. Srinivas

Keyword(s):

Controlled Release ◽

Drug Release ◽

Xanthan Gum ◽

Diffusion Mechanism ◽

Matrix Tablets ◽

Fickian Diffusion ◽

Content Uniformity ◽

In Vitro Drug Release ◽

Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

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Formulation and Characterization of Eplerenone Mucoadhesive Buccal Tablets

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00541 ◽

2021 ◽

pp. 3097-3103

Author(s):

Harini Amballa ◽

Navaneetha Kaluva ◽

Sree Giri Prasad Beri ◽

Krishna Mohan Chinnala ◽

Mayuri Konda

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Release System ◽

First Pass Metabolism ◽

First Pass ◽

Buccal Tablets ◽

Pass Metabolism

Mucoadhesive drug release system is a preferably unidirectional release system where mucosal epithelial exterior is enclosed by the mucus deposit that interacts with the bio-adhesive drug delivery system and swelling time of the buccal dosage form which is amplified by mucin molecules at the location of administration. Eplerenone is an Anti-hypertensive drug that undergoes hepatic first pass metabolism and shows 69% of bioavailability. In order to bypass the hepatic first pass metabolism the drug is designed to be delivered through buccal cavity to avoid the first pass metabolism. Eplerenone buccal tablets were formulated by using direct compression method with different polymers like HPMC K 100M, Carbopol 934P, Carbopol 974P, Xantham Gum, Eudragit L100 and NaCMC in various concentrations and compositions. Incompatibility complications were not observed from the FTIR spectrums. The formulated and prepared buccal solid dosage forms were evaluated for pre-compressions and post- compression parameters such as hardness, weight variation, thickness, friability, surface pH, swelling index, in-vitro dissolution studies, drug content uniformity, mucoadhesion strength and mucoadhesion time. Evaluation results of formulation F12 are proven to be the optimal formulation showing highest mucoadhesion time, mucoadhesion strength and in-vitro drug release for prolonged period of time about 8 hours. Eplerenone is best delivered through buccal drug delivery system to enhance its oral bioavailability and bypass the hepatic first pass metabolism.

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DESIGN AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PHENFORMIN HYDROCHLORIDE

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2017v9i6.23437 ◽

2017 ◽

Vol 9 (6) ◽

pp. 90

Author(s):

Pratik Swarup Das ◽

Puja Saha

Keyword(s):

Drug Release ◽

Diffusion Mechanism ◽

Skin Irritation ◽

In Vitro Release ◽

Chemical Properties ◽

In Vitro Dissolution ◽

Release Mechanism ◽

Transdermal Patches ◽

The Matrix

Objective: In present work was designed to develop suitable transdermal matrix patches of Phenformin hydrochloride using various hydrophilic (HPMC) and hydrophobic (EUDRAGID) polymers as matrix formers.Methods: Transdermal patches containing Phenformin hydrochloride were prepared by the solvent casting evaporation technique.Results: Revealed that prepared patches showed good physical characteristics, no drug-polymer interaction and no skin irritation was observed. The in vitro release study revealed that F3 formulation showed maximum release in 24 h. Formulation F3 was subjected for accelerated stability studies. The F3 formulation was found to be stable as there was no drastic change in the Physico-chemical properties of the patches, which was also confirmed by FTIR.Conclusion: Thus conclusion can be made that stable transdermal patches of Phenformin hydrochloride has been developed. F1, F2, F3, F4 formulations showed highest cumulative percentage drug release of 98.13%, 95.50%, 98.65%, 97.21% were obtained during in vitro drug release studies after 24 h. The release of Phenformin hydrochloride appears to be dependent on lipophilicity of the matrix. Moderately lipophillic matrices showed best release. The predominant release mechanism of drug through the fabricated matrices was believed to be by diffusion mechanism. Based upon the in vitro dissolution data the F3 formulation was concluded as optimized formulation.

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Formulation and Evaluation of Orodispersible Tablet of Atorvastatin Calcium by Using Hibiscus rosa sinesis Mucilage as Natural Superdisintegrant

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i6.3677 ◽

2019 ◽

Vol 9 (6) ◽

pp. 90-94

Author(s):

Ashish Gupta ◽

Juhi Bhadoria ◽

G.N. Darwhekar

Keyword(s):

Lipid Lowering ◽

Content Uniformity ◽

Atorvastatin Calcium ◽

Drug Content ◽

Orodispersible Tablets ◽

Orodispersible Tablet ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism

Orodispersible tablets (ODTs), also known as fast melt, quick melts, fast disintegrating have the unique property of disintegrating in the mouth in seconds without chewing and the need of water. Oral bioavailability of Atorvastatin Calcium is low (14%) and shows extensive intestinal clearance and first-pass metabolism, which is the main cause for the low systemic availability. In the present work, orodispersible tablets of Atorvastatin calcium were prepared by direct compression method using Hibiscus rosa sinesis mucilage as natural superdisintegrant with a view to enhance patient compliance and to avoid hepatic first pass metabolism and to improve its bioavailability. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water-absorption ratio and in-vitro dispersion time. Short-term stability studies on the promising formulation indicated that there are no significant changes in drug content and in vitro dispersion time. Keywords: Orodispersible tablet, Atorvastatin Calcium, lipid-lowering agent, Superdisintegrant, Hibiscus Rosa Sinensis, Bioavailability, solubility.

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FORMULATION, IN VITRO AND EX VIVO CHARACTERIZATION OF MUCOADHESIVE BUCCAL TABLETS FOR ANTIHYPERTENSIVE DRUG

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i8.26126 ◽

2018 ◽

Vol 11 (8) ◽

pp. 402 ◽

Cited By ~ 1

Author(s):

Himabindu Peddapalli ◽

Vasudha Bakshi ◽

Narender Boggula

Keyword(s):

Drug Release ◽

Ex Vivo ◽

Surface Ph ◽

Ex Vivo Permeation ◽

First Pass Metabolism ◽

First Pass ◽

Permeation Studies ◽

Buccal Tablets ◽

Pass Metabolism

Objective: Olmesartan belongs to a class of angiotensin II receptor blockers. It is used in the treatment of hypertension. However, it undergoes extensive hepatic first-pass metabolism, resulting in low oral bioavailability is about 26%. The aim of this study was to prepare and evaluate the mucoadhesive buccal tablets of olmesartan with a goal to increase the bioavailability and improve the patient compliance.Methods: Mucoadhesive buccal tablets were prepared by a direct compression technique using mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC K4M), sodium carboxymethylcellulose (SCMC), and Carbopol 934P. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, ex vivo mucoadhesive strength, ex vivo mucoadhesive time, and ex vivo permeation studies. The release kinetics was calculated to determine the drug release mechanism. Results: The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets F2, F7, and F11 showed satisfactory drug release rates with the diffusion controlled mechanism. Optimized buccal tablets developed for olmesartan possess reasonable mucoadhesive strength, mucoadhesive time, and surface pH was in an acceptable salivary pH 6.76±0.28–6.89±0.34. The ex vivo permeation studies for optimized tablets were shown satisfactory drug permeation and could meet the target flux 0.991 mg h−1cm−2.Conclusion: The obtained results could be used as a platform to develop the buccal delivery of this drug, which bypasses the first-pass metabolism and results in the improvement of bioavailability. Hence, the present study concludes that the olmesartan could be delivered through the buccal route.

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Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and mucoadhesive strength

Acta Pharmaceutica ◽

10.2478/acph-2019-0022 ◽

2019 ◽

Vol 69 (3) ◽

pp. 381-398

Author(s):

Amira A. Rashad ◽

Sara Nageeb El-Helaly ◽

Randa T. Abd El Rehim ◽

Omaima N. El-Gazayerly

Keyword(s):

In Vitro Release ◽

Aqueous Solubility ◽

Oral Route ◽

Wet Granulation ◽

Preparation Technique ◽

First Pass Metabolism ◽

First Pass ◽

Vitro Release ◽

Pass Metabolism

Abstract Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 33 factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and in vitro release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.

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Formulation and Evaluation of Buccoadhesive Tablets of Losartan Potassium

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.4.8 ◽

2015 ◽

Vol 8 (4) ◽

pp. 3045-3052

Author(s):

Sudarshan Singh ◽

S S Shyale ◽

A Jadhav

Keyword(s):

Drug Release ◽

Ex Vivo ◽

In Vitro Release ◽

Drug Dissolution ◽

Losartan Potassium ◽

Fickian Diffusion ◽

In Vitro Dissolution ◽

Content Uniformity ◽

Vitro Release

The present investigation is concerned with formulation and evaluation of buccoadhesive tablets containing antihypertensive drug, Losartan Potassium to avoid the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. The tablets were prepared by wet granulation method. Nine formulations were developed with varying concentrations of polymers like hydroxypropylmethyl cellulose K100 and Guar gum. The tablets were tested for hardness, friability, weight variation, content uniformity, surface pH, swelling index, ex vivo mucoadhesive strength, in vitro drug dissolution study and ex-vivo permeation study. FTIR and DSC studies showed no evidence on interactions between drug and excipients. The in vitro release of Losartan Potassium was performed under sink conditions. The mucoadhesive strength of formulation F9 was found to be 0.14307 N. The swelling index of formulation F9 was found to be 87%. The formulation F9, containing 25 mg of losartan potassium exhibited 6 h sustained drug release of 96% with desired therapeutic concentration. The in vitro release kinetics studies revealed that all formulations fits well with zero order kinetics followed by Korsemeyer-Peppas model and the mechanism of drug release is Non-Fickian diffusion. Based on the results of ex vivo mucoadhesive strength and swelling index studies formulation F9 was selected as optimized formulation and subjected for stability study. Short-term stability studies on the promising formulation indicated that there are no significant changes in drug content and in vitro dissolution characteristics.

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DESIGN AND CHARACTERIZATION OF ACECLOFENAC FAST DISSOLVING TABLETS USING SUPER DISINTEGRATING AGENTS

INDIAN DRUGS ◽

10.53879/id.51.01.p0034 ◽

2014 ◽

Vol 51 (01) ◽

pp. 34-40

Author(s):

V.L Narasaiah ◽

◽

Ch. Praneetha ◽

P Mallika ◽

K. Pullamma ◽

...

Keyword(s):

Drug Release ◽

In Vitro Release ◽

In Vitro Dissolution ◽

Wet Granulation ◽

Content Uniformity ◽

Disintegration Time ◽

First Order ◽

Drug Content ◽

Weight Variation

The aim of this project was to develop fast dissolving tablets (FDT) of aceclofenac by wet granulation using super disintegrating agents such as cross carmellose sodium (CCS), Crospovidone (CP) and sodium starch glycolate (SSG) were formulated and evaluated. The tablets evaluated for thickness, hardness, friability weight variation, drug content, water absorption ratio, wetting time, disintegration time and in vitro dissolution studies. The in vitro release studies were conducted in pH 7.4 phosphate buffer. Different release models like zero order, first order, Higuchi and Korsmeyer-Peppas were applied to in vitro drug release data in order to evaluate drug release mechanisms and kinetics. The formulation ‘F4’ showed satisfactory physico-chemical properties and drug content uniformity. The formulation ‘F4’ follows first order kinetics and the mechanism of drug release was governed by Higuchi. The ‘n’ value showed between <0.5, it was followed that Fickian transport. The FTIR studies were conducted and it shows that there is no interaction between drug and excipients.

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