Development and Evaluation of Trans Buccal Patches based on Natural and Synthetic Polymers Loaded with Rivastigmine using Solvent Casting Technique

2021 ◽  
pp. 5133-5140
Author(s):  
Prasanta Kumar Mohapatra ◽  
Boddu Pavan Kumar ◽  
Pankaj Singh Patel ◽  
Harish Chandra Verma ◽  
Satyajit Sahoo
Keyword(s):  
Drug Release ◽  
Kinetic Equations ◽  
Moisture Loss ◽  
Release Mechanism ◽  
Solvent Casting ◽  
Casting Technique ◽  
Weight Variation ◽  
Zero Order Release ◽  
Buccal Films

Mucoadhesive buccal films of rivastigmine were prepared by the solvent casting technique using HPMC K15M, sodium alginate, glycerine, and Eudragit RL100. Arranged films assessed for weight variation, thickness, % drug substance, % moisture loss, % moisture take-up, folding endurance, in-vitro medicament release, and Fourier transform Infrared spectroscopy (FTIR). The films showed a controlled release (CR) over 8 h. The preparation observed to be a worthy candidate for the development of buccal patches for therapeutic purposes. Drug-polymer compatibility considers FTIR demonstrated no contradiction between the medicament and the polymers. The optimized formulation found F7 indicated drug release 85% at the end of 8 h. Thinking about the correlation coefficient (R2) values got from the kinetic equations, the drug release from the formulations F1-F8 has discovered zero-order release mechanism. It can be concluded that oral buccal patches of rivastigmine, for treatment of Alzheimer’s and Parkinson’s disease, can be formulated. The study suggests that rivastigmine can be conveniently administered orally in the form of buccal patches, with the lesser occurrence of its side effects and improved bioavailability.

SYNTHESIS AND CHARACTERIZATION OF THIOLATED GUM KONDAGOGU AND EVALUATION AS MUCOADHESIVE POLYMER

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (01) ◽  
pp. 37-43
Author(s):  
Ashwin A. Patil ◽  
Ketan B. Patil ◽  
Laxmikant R. Zawar
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Matrix Tablet ◽  
Disintegration Time ◽  
Weight Variation ◽  
Zero Order Release ◽  
Gum Kondagogu ◽  
Ellman’S Method

Present work focused on thiolation for enhancing the mucoadhesive potential of Gum kondagogu (GK). Thiolation of GK was done by esterification process with 80 % thioglycolic acid in presence of 7N HCl. Thiolated Gum kondagogu (ThioGK) was determined to possess 1.59 ±0.04 mmol of thiol groups/g of the polymer by Ellman’s method. ThioGK was characterized by FTIR, NMR, DSC, XRD, and FE-SEM. The tablets were prepared by direct compression using 75 mg of ThioGK and GK. Tablets containing ThioGK (F1) and GK (F2) were subjected to evaluation of weight variation, hardness and friability and show enhanced disintegration time, swelling behavior, drug release and mucoadhesion. In vitro drug release of batch F1 exhibits complete release of drug in 24 hr with zero order release kinetics. Comparative mucoadhesive strength was studied using chicken ileum by texture analyzer and revealed higher mucoadhesion of tablet containing ThioGK. From the above study, ThioGK was suitability exploited as mucoadhesive sustained release matrix tablet.

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 Formulation and In Vitro Evaluation of Sustained Release Floating Matrix Tablet of Levofloxacin by Direct Compression Method

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Release ◽  
Acute Infection ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  

scholarly journals FABRICATION AND CHARACTERIZATION OF FAST DISSOLVING FILMS OF ECLIPTA PROSTRATE LEAVES EXTRACT TO TREAT MOUTH ULCERS

2021 ◽  
pp. 263-271
Author(s):  
MANIKIRAN S. S. ◽  
NAGAM SANTHI PRIYA ◽  
B. AUBINE MOLLY ◽  
LAKSHMI PRASANTHI NORI
Keyword(s):  
Drug Release ◽  
Moisture Loss ◽  
Disintegration Time ◽  
Weight Variation ◽  
Eclipta Prostrata ◽  
Release Studies ◽  
Study Results ◽  
The Stability ◽  
Oral Films

Objective: This research focused on the design of fast dissolving herbal film of Eclipta Prostrate leaves extract for mouth ulcers. Methods: The extract of Eclipta Prostrata leaves was formulated as films by solvent casting method using various polymers viz., HPMC E5, HPMC E15, sodium alginate and PVA. The films were designed by using propylene glycol as a plasticizer, SSG as super disintegrate and honey as a sweetener. Furthermore, the films were evaluated for thickness, folding endurance, weight variation, % elongation, surface pH, % moisture uptake, % moisture loss, disintegration and in vitro drug release study. Results: The revealed that all the films were good in appearance and had a smooth texture. Out of all ten formulations, F3 and F5 disintegrated rapidly with a disintegration time of 27 and 32 seconds. The drug release studies revealed that all the formulations had a good release profile, but the F3 formulation showed rapid release i.e. 83.57% in 4 min. The stability studies revealed that the formulations F3 and F5 were found good with non-tackiness, easily separable and disintegrated at 29 and 33 sec respectively with no appearance and drug release. Conclusion: The research revealed that Eclipta prostrate leaves extract can be formulated into oral films for the treatment of mouth ulcers with improved bioavailability and expected patient compliance.

DEVELOPMENT AND CHARACTERIZATION OF NOVEL GASTRORETENTIVE RAFT FORMING FLOATING FILM OF ATENOLOL

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (03) ◽  
pp. 15-23
Author(s):  
N Sharma ◽  
◽  
R. Awasthi
Keyword(s):  
Drug Release ◽  
Polymer Matrix ◽  
Processing Parameters ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Casting Technique ◽  
Floating Raft ◽  
Weight Variation ◽  
Folding Endurance

The aim of present work was to develop a gastroretentive floating raft forming film of atenolol using solvent casting technique. The films were characterized in terms of drug-excipient compatibility by FTIR, drug content, swelling, folding endurance, thermal behaviour by DSC, effect of processing parameters on drug state (amorphous or crystalline) by X-ray diffraction (XRD), and in vitro drug release profiles. The results confirm that there was no interaction between the drug-polymers and fusion of drug crystals within the polymer matrix. Results of XRD indicate partial dissolution of drug within the polymer matrix and suggested it was partly distributed in amorphous form throughout the film. The weight variation, thickness and folding endurance of films were in the range of 2.170 ± 0.05 to 2.444 ± 0.23 gm, 1.120 ± 0.032 to 1.125 ± 0.011 mm and 200 ± 5 to 400 ± 5, respectively. The pH values of the different films were between 6.8 to 7.21. After 24 h, the best selected film shows 75% and 90% of drug release in 0.1 N HCl (pH 1.2) and in phosphate buffer (pH 6.8), respectively. Based on these results it is suggested that the incorporation of drug into the hydrophilic floating film may be an appropriate strategy to improve the dissolution profile and oral bioavailability of the drug.

DESIGN AND IN VITRO EVALUATION OF MUCOADHESIVE BUCCAL FILMS OF LERCANIDIPINE HCL

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (07) ◽  
pp. 31-40
Author(s):  
H. Doddayya ◽  
◽  
S.S Patil ◽  
M Suman ◽  
P Kumar ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Zero Order Kinetics ◽  
Accelerated Stability ◽  
Buccal Films ◽  
Lercanidipine Hydrochloride

Lercanidipine hydrochloride, an anti hypertension drug, undergoes extensive first pass metabolism to inactive metabolites leading to very poor oral bioavailability. To overcome this problem, buccal films of Lercanidipine hydrochloride were prepared by solvent casting method, employing HPMC, HPC (alone and in combination with PVP) and PVP K30. The film thickness, weight, folding endurance, mucoadhesive strength and time were dependent on the nature and concentration of polymers used. The optimized film (F12, HPMC 3% and PVP 1.5%) showed: Swelling index (51.26 ± 1.90 %), ex vivo mucoadhesive strength (12.64 ± 0.83 grams) and time (3.6 ± 0.5hrs). In vitro drug release was inversely proportional to the polymeric concentration. Ex- vivo drug release studies carried out using goat buccal membrane was slower (42.90%, 6 hrs) compared to in vitro drug release (74.2%, 8hrs) for the same formulation (F12). The drug release mechanism for the optimized formulation followed zero order kinetics. FT-IR and DSC studies revealed the absence of any interaction between the formulation ingredients. The films remained stable during the accelerated stability conditions.

scholarly journals EFFECTIVE MANAGEMENT OF ODONTOGENIC INFECTIONS THROUGH CONTROLLED FASHION BY POLYMERIC DEVICE CONTAINING MOXYFLOXACIN

2017 ◽  
pp. 100-106
Author(s):  
Gorle A. P. ◽  
Mahale H. V. ◽  
Patil C. S.
Keyword(s):  
Drug Release ◽  
Bacterial Infections ◽  
Moisture Loss ◽  
Bacterial Invasion ◽  
Content Uniformity ◽  
Compatibility Study ◽  
Odontogenic Infections ◽  
Casting Technique ◽  
In Vitro Antibacterial Activity

Objective: Present work demonstrates the use of film that releases the drug at a pre-programmed manner. Several methods have been explored for management of moxifloxacin in dealing of Odontogenic infections which are mainly caused by necrotic pulp or by bacterial invasion from the periodontal tissue. These are usually mixed bacterial infections, and they penetrate mostly into the soft and bony oromaxillofacial tissues to produce submucosal infiltrates and abscesses.Methods: The films were developed with the intention to minimize the dose of a drug, to deliver definite concentration and to preserve dosage at its site for a longer period by this means gets a better patient compliance. Moxifloxacin films were prepared by solvent casting technique using gellan gum at different concentrations and PEG 400 as plasticizers. Compatibility study such as FT-IR and DSC also performed to check the interaction between drug and excipients used. The formulations were evaluated for their thickness, weight uniformity, folding endurance, content uniformity, surface pH, In vitro drug release. Optimized formulations were subjected to in vitro antibacterial activity and stability studies to assess the effectiveness of the formulations.Results: Formulations shown the good uniformity of drug content, there was no any kind of effect on moisture loss test. Weight and thickness of the films were found to be uniform. Plasticizer like PEG400 was found to influence their effect on drug release as well as characteristics of films.Conclusion: In vitro studies revealed that the formulations provide the best alternative to prolong drug release at the end of 10 h and formulations remained stable with intact at ambient conditions. 

scholarly journals Porous nanoparticles of metoprolol tartrate produced by spray-drying: development, characterization and in vitro evaluation

2012 ◽  
Vol 62 (3) ◽  
pp. 383-394 ◽  
Author(s):  
Mohammed S. Khan ◽  
Gowda D. Vishakante ◽  
H. G. Shivakumar
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Release Kinetics ◽  
Drug Loading ◽  
Release Mechanism ◽  
Metoprolol Tartrate ◽  
Pore Former ◽  
Porous Nanoparticles ◽  
Zero Order Release

The present investigation was undertaken to fabricate porous nanoparticles of metoprolol tartrate by spray-drying using ammonium carbonate as pore former. Prepared nanoparticles were coated with Eudragit S100 polymer in order to prevent the release of metoprolol tartrate in the upper GI tract. It was shown that nanoparticles with low size ranges can be obtained with a low feed inlet rate. Micromeritic studies confirmed that nanoparticle batches are discrete and free flowing. Effects of the pore former on drug loading, porosity and in vitro release were studied. It was found that there was an increase in drug loading and porosity with increasing the amount of pore former. In vitro drug release studies showed that an increase in pore former made drug release faster. Release kinetics proved that nanoparticles follow a zero-order release mechanism.

scholarly journals “FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING FILMS OF LAFUTIDINE”

2019 ◽  
Vol 7 (2) ◽  
Author(s):  
Hir. R. Mehta ◽  
Vijay K. Patel
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Stability Study ◽  
Formulation Development ◽  
Casting Technique ◽  
Drug Content ◽  
Peg 400 ◽  
Weight Variation ◽  
Folding Endurance

The present invention was aimed to formulate and evaluate Lafutidine gastro retentive films. The films were prepared by solvent casting technique using different film forming polymers like HPMC and Ethyl cellulose. PEG 400 used as a plastsizer. The prepared films were evaluated for number of parameters like Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, unfolding behavior, floating properties, drug content and In vitro drug release studies. From the trial batches the best release for gastroretentive film was shown by formulation T5 (Ethyl cellulose and PEG 400). Formulation T5 exhibited good appearance, better mechanical strength with acceptable flexibility. Also, formulation T5 was given more than 90 % drug released after 12 hr and 97.56 % Drug content.  For optimization of formulation, 32 factorial design was applied by taking Ethyl cellulose and PEG 400 as an independent variables. Drug release at 8 hour and folding endurance selected as dependent variables. Based on drug release study, L8 batch found most satisfactory in all formulation and the effect of Ethyl cellulose and PEG 400 found significant. L8 batch found stable during stability study. Key words: Lafutidine, Floating Films, Ethyl Cellulose.

scholarly journals FORMULATION AND EVALUATION OF CILNIDIPINE MUCOADHESIVE BUCCAL FILM BY SOLVENT CASTING TECHNIQUE FOR THE TREATMENT OF HYPERTENSION

2021 ◽  
pp. 34-43
Author(s):  
SHIFA SHAUKAT HAJU ◽  
SHEELA YADAV
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Calcium Channel ◽  
Content Uniformity ◽  
Solvent Casting ◽  
Casting Technique ◽  
Drug Content ◽  
Buccal Drug Delivery ◽  
Folding Endurance

Objective: Buccal drug delivery is the most suited route for local as well as systemic delivery of drugs. Cilnidipine is an L/N type dihydropyridine 4th generation calcium channel blocker (CCB), which decreases hypertension by blocking the N-type calcium channel to attenuate vascular sympathetic neurotransmission. It has high first-pass metabolism leading to low bioavailability. Hence the present research work was undertaken to formulate mucoadhesive buccal film of Cilnidipine with an objective to enhance therapeutic efficacy, bioavailability and was developed to administer into the unconscious and less-co-operative patients. Methods: Cilnidipine buccal films were prepared by a solvent-casting technique using various concentrations of mucoadhesive-polymers such as Hydroxyl propyl methylcellulose (HPMC) E15 and K4M and ethyl-cellulose as backing-layer, which acts like a patch providing unidirectional drug release. Prepared films were evaluated for their weight variation, thickness, surface-pH, swelling-index, drug content uniformity, in vitro residence time, folding endurance, tensile strength, in vitro release and permeability studies. Results: The infra-red (IR) spectra showed no interaction, and Physico-chemical characteristics were found within the limit. Swelling of the film increases with increasing concentration of polymers and %drug content of all formulations found to be in the range of 92.13%±0.94% to 97.92%±0.35%. The formulation F5, showed a promising tensile strength, folding endurance and in vitro drug release of about 95.18±0.03%, thus can be selected as an optimized formulation of mucoadhesive buccal film. Conclusion: The formulation of Cilnidipine mucoadhesive buccal film was found to be satisfactory and reasonable.

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