Development of Mucoadhesive Buccal Films of Glipizide

1970 ◽  
Vol 1 (2) ◽  
pp. 177-183
Author(s):  
Mona Semalty ◽  
Ajay Semalty ◽  
Ganesh Kumar ◽  
Vijay Juyal
Keyword(s):  
Controlled Release ◽  
Residence Time ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Potential Candidate ◽  
Sodium Carboxymethylcellulose ◽  
Casting Technique ◽  
Buccal Films

For improving bioavailability in controlled release fashion and to circumvent the hepatic first pass effect of glipizide mucoadhesive buccal films of glipizide were prepared by solvent casting technique. Buccal films were prepared using hydroxy propylmethylcellulose, sodium carboxymethylcellulose, carbopol-934P and Eudragit RL-100. Films were evaluated for their weight, thickness, surface pH, swelling index,       in vitro residence time, folding endurance, in vitro release, ex vivo permeation studies and drug content uniformity. The films exhibited controlled release over more than 6 h. From the study it was concluded that the films containing 5 mg glipizide in 4.9 % w/v hydroxy propylmethylcellulose and 1.5 % w/v sodium carboxymethylcellulose exhibited satisfactory swelling, an optimum residence time and promising drug release thus proved to be potential candidate for the development of buccal films for therapeutic use.

Formulation and In vitro Evaluation of Mucoadhesive Buccal Patches of Ondansetron Hydrochloride

2010 ◽  
Vol 3 (1) ◽  
pp. 860-866
Author(s):  
Shayeda ◽  
Sathish Dharani
Keyword(s):  
Moisture Absorption ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Thickness Variation ◽  
Content Uniformity ◽  
Casting Technique ◽  
Weight Variation ◽  
Ondansetron Hydrochloride

The goal of the present investigation was to design and evaluate mucoadhesive buccal patches of Ondansetron Hydrochloride (OND) which is used for nausea and vomiting associated with cancer chemotherapy and radiotherapy. Permeation of OND was calculated ex vivo using porcine buccal membrane. Buccal films were developed by solvent-casting technique using Hydroxy Propyl Methyl Cellulose(HPMC E15) as mucoadhesive polymer. The patches were evaluated for weight variation, thickness variation, surface pH, moisture absorption, in vitro residence time, mechanical properties, in vitro release, ex vivo permeation studies and drug content uniformity. The formulation F3 was found to give the better results and obeys first order kinetics. 

scholarly journals DESIGN AND EVALUATION OF BUCCAL PATCHES CONTAINING COMBINATION OF HYDROCHLOROTHIAZIDE AND ATENOLOL

2018 ◽  
Vol 10 (2) ◽  
pp. 105
Author(s):  
Ashutosh Roda ◽  
Prabhakara Prabhu ◽  
Akhilesh Dubey
Keyword(s):  
Tensile Strength ◽  
Sustained Release ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Physicochemical Characteristics ◽  
Content Uniformity ◽  
Casting Technique ◽  
Weight Variation

Objective: Buccal patch is a non-dissolving thin matrix modified release dosage form which was developed to administer into the unconscious and less co-operative patients.Methods: The mucoadhesive buccal patches of hydrochlorothiazide (HCZ) and atenolol (ATN) were prepared by solvent casting technique using various concentrations of sodium alginate, hydroxyl propyl methyl cellulose, carbopol 934P and sodium carboxy methyl cellulose polymer and polyvinyl alcohol as a backing layer. The formulated patches were evaluated for their physicochemical parameters like thickness, weight variation, surface pH, content uniformity, folding endurance, swelling percentage studies and tensile strength, in vitro and ex vivo drug permeation. Results: The infra-red (IR) spectra showed no interaction between drug and polymer. Physicochemical characteristics of all the samples were found to be satisfactory and well within the range. Swelling of the films were increased with the increasing content of the polymers and it was found that swelling front erosion was comparably slower in the formulations with the carbopol 934 and HPMC. This is probably due to their marked viscous properties and therefore formulation provided sustained release of the drug. The percentage drug content of all the formulations were found to be in the range of 97-99 %. Among the patches, FC (Carbopol 934 and HPMC) patches were considered satisfactory for maintaining the in vitro residence in the oral cavity for almost 8h. Formulations FD (with CP and NaCMC) and FC showed high tensile strength and % E/B which is an indication of the strength and elasticity of the patch. The films were exhibited sustained release for more than 6 h which was confirmed by the in vitro release data and kinetic data reveals the combination of diffusion and erosion mechanism. The best mucoadhesive performance and matrix controlled release was exhibited by the formulation FC.Conclusion: The formulation of HCZ and ATN mucoadhesive buccal patch was found to be satisfactory and reasonable.

scholarly journals Characterization of bilayered matrix-type mucoadhesive buccal films containing tizanidine hydrochloride and piroxicam

2021 ◽  
Vol 20 (11) ◽  
pp. 2241-2248
Author(s):  
M. Yasmin Begum ◽  
Ali Alqahtani
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Residence Time ◽  
Ex Vivo ◽  
Drug Bioavailability ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Folding Endurance ◽  
Buccal Films

Purpose: To formulate and characterize tizanidine hydrochloride (TZN) and piroxicam (PRX)-loaded bilayer mucoadhesive buccal films with an intention to improve the bioavailability and patient compliance in pain management.Methods: Bilayer buccal films were prepared by solvent evaporation technique using hydroxypropyl methylcellulose (HPMC) 15cps and polyvinylpyrrolidone (PVP K30 as immediate release (IR) layer forming polymers and HPMC K15 M, PVP K 90 along with various muco adhesive polymers (Carbopol P934, sodium alginate, etc), as sustained release (SR) layer forming polymers. The prepared films werecharacterized for thickness, weight variation, folding endurance, surface pH, swelling index,mucoadhesive strength, in vitro residence time, in vitro drug release, ex vivo permeation and drug release kinetics.Results: The prepared films were of largely uniform thickness, weight and drug content. Moisture loss (%) and folding endurance were satisfactory. Surface pH was compatible with salivary fluid. Disintegration time was 85 s for F1 and 115 s for F2 of IR films. In vitro dissolution studies showed 99.12 ± 1.2 % (F1) and 90.36 ± 1.8 % (F2) were released in 45 min. Based on the above results, F1 was chosen as the optimum formulation to be combined with SR layer of TZN. Amongst the SR layers of TZN in vitro drug release. The findings show that of F2 was 98.38 ± 0.82 % and correlated with ex vivo release. Drug release followed zero order release kinetics and mechanism of drug release was non-Fickian type diffusion. In vitro residence time was greater than 5 h.Conclusion: The findings show that the bilayer buccal films demonstrate the dual impact of deliveringPRX instantly from the IR layer, with good controlled release and permeation of TZN from the SR layer, thus providing enhanced therapeutic efficacy, drug bioavailability and patient compliance.

scholarly journals Ondansetron Hydrochloride in Treating Patients with Cancer and Chronic Nausea Vomiting

2017 ◽  
Vol 1 (2) ◽  
pp. 01-04
Author(s):  
Hye jin
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Extended Period ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Ondansetron Hydrochloride ◽  
Backing Layer ◽  
Carbopol 934P

The objective of this study was to develop effective bioadhesive buccal bilayered tablets comprising of drug containing bioadhesive layer and drug free backing layer, expected to release the drug in unidirection for extended period of time. Tablets of ondansetron HCl were prepared by direct compression method using bioadhesive polymers like Carbopol 934P, Methocel K4M, Methocel K15M and Hydroxy propyl cellulose in different combinations and concentrations with backing layer of ethyl cellulose. Buccal tablets were evaluated by different parameters such as thickness, hardness, weight uniformity, content uniformity, swelling index, surface pH, ex vivo bioadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation, stability studies in human saliva, in vivo mucoadhesive performance studies and FTIR studies. The modified in vitro assembly was used to measure the bioadhesive strength of tablets with fresh porcine buccal mucosa as model tissue. Bioadhesion strength was increased with increase in the concentration of carbopol. The tablets were evaluated for in vitro release in pH 6.6 phosphate buffer for 8 hr in standard dissolution apparatus. In order to improve the permeation of the drug, tauroglycholate (permeation enhancer) added in the optimized formulation at 10mM concentration. In order to determine the mode of release, the data was subjected to Korsmeyer and Peppas diffusion model. The optimized formula followed non-fickian release mechanism with zero order kinetics. Carbopol 934P and HPC in the ratio of 3:1 could be used to design effective and stable buccoadhesive tablets of ondansetron HCl. The present study concludes that buccal delivery of ondansetron HCl tablets can be good way to bypass the first pass metabolism.

scholarly journals Development and radiographical evaluation of floating tablets with combination of Amoxicillin Trihydrate and Ranitidine Hydrochloride

2019 ◽  
Vol 10 (2) ◽  
pp. 1489-1499
Author(s):  
Parepalli Srikanth ◽  
Hemalatha S ◽  
Suggala Venkata Satyanarayana
Keyword(s):  
Residence Time ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Simultaneous Estimation ◽  
Content Uniformity ◽  
Floating Tablets ◽  
Ranitidine Hydrochloride ◽  
Amoxicillin Trihydrate

Stomach Specific Floating Tablets (SSFT) with a combination of Amoxicillin-Trihydrate (AT) and Ranitidine Hydrochloride (RH) were developed by using different grades of Hydroxypropylmethylcellulose (HPMCK) (i.e.HPMCK 100M, HPMCK4M and HPMCK15M), to treat patients with H. pylori-infected duodenal ulcer. Floating tablets were prepared by direct compression method, developed formulations were evaluated for different pre-compression and post-compression parameters like angle of repose, compressibility index, hardness, weight variation, floating lag time, content uniformity, and in-vitro drug release. In-Vitro release of two drugs (Amoxicillin-Trihydrate and Ranitidine hydrochloride) from the developed formulation was estimated by the Simultaneous Estimation method (Vierordt's Method). The optimized formulation was subjected to Radio graphical evaluation by incorporating the BaSO4, a radio-opaque substance by replacing a part of the drug from the optimized formulation of into the formulation and then it was administered to the healthy human volunteers to find out the in-vivo residence time. In-vivo X-ray studies were conducted both in fed condition, as well as fasted condition the optimized formulation showed a gastric residence time of more in fed state than that of fasting state. From these studies it was clearly observed that the floating tablets should be given to patients after a standard food and with frequent intake of water.

scholarly journals Development and Statistical Optimisation of Buspirone Hydrochloride Buccoadhesive Films

2014 ◽  
Vol 2014 ◽  
pp. 1-12
Author(s):  
Upendra Nagaich ◽  
Vandana Chaudhary ◽  
Jaya Nagaich
Keyword(s):  
Ex Vivo ◽  
Polyethylene Glycol 400 ◽  
Casting Technique ◽  
Buspirone Hydrochloride ◽  
Diffusion Studies ◽  
Predicted Values ◽  
The Stability ◽  
Eudragit Rl ◽  
Buccal Films

The aim of the present study was to prepare unidirectional buccal films of buspirone hydrochloride by solvent casting technique. Hydroxypropylmethylcellulose (HPMC K15M) and Eudragit RL-100 were used as polymers in different proportion. Polyethylene glycol 400 and sodium lauryl sulphate were used as plasticizer and permeation enhancer, respectively, in different concentration. In the formulation, total amount of polymer (X1) and percentage of HPMC K15M (X2) were kept as independent variables. Afterwards, statistically optimized process was carried out and two optimized formulations (OF1 and OF2) were developed. The observed results of optimized formulation were showed a greater degree of percentage of similarity with predicted values. The stability studies showed that there was no significant change found in physicochemical properties, in-vitro release, and ex-vivo diffusion studies.

Formulation and Evaluation of Buccoadhesive Tablets of Losartan Potassium

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.  

Bosentan Monohydrate Vesicles Loaded Transdermal Drug Delivery System: In Vitro In Vivo Evaluation

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Revathi M. ◽  
Indira Y.
Keyword(s):  
Controlled Release ◽  
Delivery System ◽  
Ex Vivo ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
In Vivo Evaluation ◽  
Vitro Release ◽  
Transdermal Route

This study elucidates the enhancement of the permeation of bosentan monohydrate through skin by encapsulating it in vesicles loaded transdermal delivery system. Niosomal vesicles were formulated by ether injection method. Formulation FN7 (span 60: cholesterol: poloxamer 401, 1.25:1:0.25) showed maximum entrapment efficiency of 96.7±0.037% and was optimized for loading in to transdermal system. Transdermal systems were formulated using both hydrophilic and hydrophobic polymers like HPMC, HEC and EC. Formulation F1 with HPMC was optimized based on in vitro release (99.21±1.45 %) and was further evaluated for ex-vivo permeation. The results indicate that the ex vivo release (98.13±1.65%) was as par with in vitro release and followed zero order super case- II transport mechanism. The in vivo studies were done on New Zealand male rabbits for oral and transdermal route. The results inferred no significant change in half-life of drug but a substantial difference in Tmax, AUC and MRT was observed in transdermal systems. A two fold increase in AUC was observed in transdermal route (18.609±7.251µg/ml/h) when compared to oral route (9.644±5.621µg/ml/h). A controlled release was attained up to 35h and reservoir effect was observed and this may be due to the barrier properties of skin. Drug encapsulated niosomes were released in to the skin by loosening the lipid layers and the surfactant acted as penetration enhancer. The study infers that niosomes loaded transdermal patches of bosentan monohydrate can enhance the bioavailability and provided controlled release for better therapeutic efficacy and safety of drug.

DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE BUCCAL PATCH OF TIMOLOL MALEATE

2018 ◽  
pp. 8-15
Author(s):  
Sharma K ◽  
Khan AD ◽  
Sachdeva M
Keyword(s):  
Controlled Release ◽  
Kinetic Models ◽  
Moisture Absorption ◽  
In Vitro Release ◽  
Lymphatic Drainage ◽  
Timolol Maleate ◽  
Casting Technique ◽  
Physiochemical Parameters ◽  
Vitro Release

The oral transmucosal Timolol maleate delivery bypasses liver and avoids presystemic elimination in the gastro intestinal tract andliver which enhance the bioavailability as well decreases the adverse effect. Objective: The present investigation highlights the formulation andevaluation of mucoadhesive buccal patch of Timolol maleate because Timolol maleate has biphasic solubility hence relatively permeated throughbuccal mucosa, which is well supplied with both vascular and lymphatic drainage. Material and Method: The mucoadhesive buccal patches ofTimolol maleate were prepared by solvent casting technique using polymers like Hydroxypropylmethyl cellulose-15cps and Polyvinylpyrrolidone. The formulated films were evaluated for their physiochemical parameters like surface pH, percentage moisture absorption, swellingpercentage, thickness, folding endurance and drug content. In vitro permeation and in vitro release studies were performed with pH 6.8 phosphatebuffer solution. Result and Discussion: The patches exhibited controlled release for more than 12 h. The in vitro release data were fit to differentequations and kinetic models to explain release profiles. The kinetic models used were zero order, first order higuchi’s and peppa’s. The bestmucoadhesive performance and matrix controlled release was exhibited by the formulation CK2 (3 % HPMC and 1 % PVP). Conclusion: Goodresults were obtained both in physico chemical characteristics and in vitro studies in formulation CK2. Hence the formulations of Timololmaleate bioadhesive buccal patch is a promising one as the controlled drug delivery with improved bioavailability.

scholarly journals Development of Tizanidine HCl transdermal patches: In-vitro and Ex-vivo characterization

2019 ◽  
Vol 9 (1-s) ◽  
pp. 295-300
Author(s):  
Dr. Shayeda ◽  
Nusrat Ayesha
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Transdermal Patches ◽  
Ex Vivo Permeation ◽  
Release Studies ◽  
Transdermal Drug Delivery Systems ◽  
Folding Endurance ◽  
Vitro Release

The purpose of this work was to design and evaluate matrix type transdermal patches of Tizanidine hydrochloride using Hypromellose (HPMC E15) as polymer, dibutyl phthalate as plasticizer and citral as permeation enhancer. The DSC and FTIR results showed the compatibility of the excipients with the drug. These transdermal drug delivery systems were characterized for their thickness, folding endurance, content uniformity, tensile strength and in-vitro release studies of the drug from the polymeric matrix. In-vitro release studies and ex-vivo permeation were carried out with modified Franz diffusion cell using pH 5.8 & pH 7.4 phosphate buffers as receptor medium and it showed controlled release of drug. The results suggest that the formulation of TIZ may be useful in the development of a therapeutic system to deliver TIZ across the skin for a prolonged period, i.e. 24 hr. Keywords: Tizanidine Hydrochloride, Transdermal patch, HPMC E15, in-vitro & ex-vivo.

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