scholarly journals SOLID DISPERSION OF NEBIVOLOL HYDROCHLORIDE IMPREGNATED BUCCAL PATCH: FORMULATION AND CHARACTERIZATION

2021 ◽  
pp. 145-149
Author(s):  
CLINTON JOSE ◽  
SNEH PRIYA ◽  
DIVYA JYOTHI ◽  
HIMANSHU JOSHI ◽  
CYNTHIA LIZZIE LOBO ◽  
...  
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Exponential Model ◽  
Moisture Loss ◽  
Patient Noncompliance ◽  
Nebivolol Hydrochloride ◽  
Good Transparency

Objective: The objective of the present investigation was to design and characterize a mucoadhesive buccal patch of Nebivolol hydrochloride in order to administer a small dose of a drug to treat hypertension effectively and thereby avoiding disadvantages such as patient noncompliance and low bioavailability. Methods: The buccal patches were prepared by solvent casting method. The polymers used to formulate patches were HPMC K 15 M, PVP K 30, and propylene glycol was used as plasticizer and ethanol as the solvent. The drug-polymer compatibility studied was conducted by FTIR. Results: All the developed Patches had good transparency and stability. All formulated patches showed pH in the range of 6.49 to 7.22, and drug content was more than 90%. The folding endurance value showed that the patches are flexible and non-brittle. The in vitro residence time was found to more than 30 min. Thickness, % moisture absorption, and % moisture loss values were in a normal range. The drug release study was conducted for 8 h, and it was found drug release was decreased with the increase in polymer concentration. The in vitro release profiles of the drug from all the formulations appeared to follow Korsmeyer Peppa's exponential model, and release exponent (n) was found to be more than 0.45 so that the release can be characterized by Non–Fickian (anomalous) diffusion. Conclusion: From the results, it was concluded that drug released from formulated buccal patches follows sustained release pattern, Hence can be used for the treatment of the hypertensive patient.

scholarly journals IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM

2018 ◽  
Vol 10 (5) ◽  
pp. 76
Author(s):  
Methaq Hamad Sabar ◽  
Iman Sabah Jaafar ◽  
Masar Basim Mohsin Mohamed
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
High Viscosity ◽  
In Situ Gel ◽  
Alginate Concentration

Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).Conclusion: This study showed the formulation of Na alginate with GG and CaCO3, led to gain floating in situ gel and a sustained release of keto. 

COMPARATIVE EVALUATION OF POLYMER COMBINATION IN THE DESIGN OF BRIMONIDINE TARTRATE OCULAR INSERTS

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (07) ◽  
pp. 30-35
Author(s):  
P Goudanavar ◽  
◽  
N Ambhore ◽  
D. Hiremath ◽  
R Udupi
Keyword(s):  
Polymer Concentration ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Carboxymethyl Chitosan ◽  
Moisture Loss ◽  
In Vivo Release ◽  
Weight Variation ◽  
Brimonidine Tartrate

Brimonidine is an anti-glaucoma agent useful in treatment of intraocular pressure. In the present study an attempt was made to formulate ophthalmic inserts of brimonidine tartrate (BT) in combination with polymers like methylcellulose, carboxymethyl chitosan and HPMC. Prepared ocular films were evaluated for uniformity in thickness, weight variation, % moisture absorption, % moisture loss, in vitro and in vivo release studies. The physical characteristics of the films were found to be within acceptable limits. The study confirmed that brimonidine tartrate can be delivered through films made of methyl cellulose, carboxymethyl chitosan and HPMC combination matrix cast with ethyl cellulose (EC). In vitro release study revealed that increasing the proportion of polymer concentration decreased the rate of release of brimonidine tartrate. In vivo release profile of ocular inserts revealed controlled release of drug over a period of 24 h. Optimized formulation CH3 was evaluated for in vivo release characteristics using rabbits as animal model. The optimized formulation CH3 was found to be stable at accelerated storage condition of 40/75 % RH.

scholarly journals COMPARATIVE STUDY ON ANTI-INFLAMMATORY SYNERGISTIC ACTIVITY OF LORNOXICAM USING TURMERIC OIL IN TDDS

2018 ◽  
Vol 7 (4) ◽  
Author(s):  
Wasim Ahmed ◽  
Dipti Srivastava ◽  
Himani Awasthi ◽  
Bankim Chandra Nandy
Keyword(s):  
Moisture Absorption ◽  
Research Work ◽  
In Vitro Release ◽  
Penetration Enhancer ◽  
Moisture Loss ◽  
Synergistic Activity ◽  
Transdermal Patches ◽  
Rat Paw Edema ◽  
Anti Inflammatory

The present research work was an attempt to develop, evaluate matrix-type transdermal therapeutic system containing lornoxicam with hydrophilic polymer (HPMC E-5) and turmeric oil (leaf extract) by the solvent evaporation technique. The turmeric oil has been used for two reasons, one is to see whether it act as natural penetration enhancer (replacing chemical enhancers) and also to compare the anti-inflammatory synergism between the drug and the oil itself. The anti-inflammatory activity of turmeric oil has been well documented. The physicochemical compatibility of the drug, polymers and oil was studied by infrared spectroscopy. The results suggested no physicochemical incompatibility between them. Five  transdermal patch formulations (F1 to F5) consists of HPMC E5 (300 mg fixed) and turmeric oil in the concentrations 3%, 4%, 5%, 6% and 7% respectively were prepared. All formulations carried 10% w/v of Polyethylene glycol as plasticizer in dichloromethane and methanol (4:1) as solvent system. The prepared transdermal patches were evaluated for in vitro release, moisture absorption, moisture loss and mechanical properties. The diffusion studies were performed by using modified Franz diffusion cells. The formulation, F3 showed maximum release 97.56% as compared to patch without any penetration enhancer (58.83%).The synergistic activity has been determined by Carrageenan induced rat paw edema test and the results have confirmed the synergistic activity between the drug and turmeric oil. The developed transdermal patches may increase the efficacy of lornoxicam for the therapy of arthritis and other painful muscular conditions. Keywords: Transdermal system, HPMC, Turmeric oil, penetration enhancer, Synergistic activity.

Development of Mucoadhesive Patches for Buccal Administration of Prochlorperazine: Evaluation of In Vitro Release and Mechanical Properties

1970 ◽  
Vol 1 (1) ◽  
pp. 64-70
Author(s):  
Chandra Sekhar Kolli ◽  
Ramesh Gannu ◽  
Vamshi Vishnu Yamsani ◽  
Kishan V ◽  
Madhsudan Rao Yamsani
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Moisture Absorption ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Work Of Adhesion ◽  
Casting Technique ◽  
Vitro Release

The aim of this investigation was to develop and evaluate mucoadhesive buccal patches of prochlorperazine (PCPZ). Permeation of PCPZ was calculated in vitro using porcine buccal membrane. Buccal formulations were developed by solvent-casting technique using hydroxy propylmethyl cellulose (HPMC) as mucoadhesive polymer. The patches were evaluated for in vitro release, moisture absorption and mechanical properties. The optimized formulation, based on in vitro release and moisture absorption studies, was subjected for bioadhesion studies using porcine buccal membrane. In vitro flux of PCPZ was calculated to be 2.14 ± 0.01 µg. h–1.cm–2 and buccal absorption was also demonstrated in vivo in human volunteers.             In vitro drug release and moisture absorbed was governed by HPMC content. Increasing concentration of HPMC delayed the drug release. All formulations followed Zero order release kinetics whereas the release pattern was non-Fickian. The mechanical properties, tensile strength (10.28 ± 2.27 kg mm–2 for formulation P3) and elongation at break reveal that the formulations were found to be strong but not brittle. The peak detachment force and work of adhesion for formulation P3 were 0.68 ± 0.15 N and 0.14 ± 0.08 mJ, respectively. The results indicate that suitable bioadhesive buccal patches of PCPZ with desired permeability and suitable mechanical properties could be prepared

Pharmaceutical Development and Evaluation of Reservoirtype Ciprofloxacin Ocular Insert

2015 ◽  
Vol 8 (4) ◽  
pp. 3024-3030
Author(s):  
Jayesh K Jethva ◽  
Chintan H Trivedi ◽  
Sarita P Ratanpara ◽  
Geeta R Bathwar ◽  
Ramesh B Parmar
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Compartment Model ◽  
Moisture Loss ◽  
Physical Parameters ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Percent Moisture ◽  
Drug Reservoir

Ocular inserts of ciprofloxacin hydrochloride were prepared with the aim of achieving once a day administration. Drug reservoir was prepared using sodium CMC while rate controlling membrane was prepared using Eudragit RS100 and RL100. Ocular inserts were evaluated for their physicochemical parameters like thickness, weight uniformity, drug content, percent moisture loss, and percent moisture absorption. The in vitro drug release studies were carried out using Bi-chambered donor receiver compartment model.  In vitro drug release kinetic data was treated according to Zero, First, and Higuchi kinetics to access the mechanism of drug release. At the end of 24th hr, in-vitro percentage drug release was obtained for the formulations RF1 was% 46.02 and for RF5 was 98.23%. The drug release from the formulation RF5 (Eudragit RS and RL 100 (1:1)) was 98.23 % at the end of 24th hour which was available as controlled and prolonged. In Kors Meyer Peppas, n value in optimized batch (RF5) was observed 1.399 which indicated super case II transport occurs. All physical parameters evaluated were satisfactory. So formulation RF5 was selected as the best formulation.

Development of Promethazine Hydrochloride Mucoadhesive Patches for Buccal Delivery: In vitro, Ex vivo and In vivo Characterization

2012 ◽  
Vol 5 (2) ◽  
pp. 1697-1705
Author(s):  
Y. Madhusudan Rao ◽  
Chopparapu K S C ◽  
P. Chinna Reddy ◽  
Narender Doodipala
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Physicochemical Interaction ◽  
Surface Ph ◽  
Drug Permeation ◽  
Promethazine Hydrochloride

Promethazine hydrochloride (PMZ HCl), an antiemetic, undergoes extensive first-pass metabolism (bioavailability 25%). The purpose of the present investigation was to develop mucoadhesive patches for transbuccal delivery of PMZ HCl using solvent casting technique with Hydroxy ethyl cellulose (Natrosol 250 E) and hydroxylpropyl methyl cellulose as mucoadhesive polymers and propylene glycol as the plasticizer and evaluate their physicochemical characteristics, in vitro drug release, moisture absorption, surface pH, mechanical properties, in vitro bioadhesion, in vivo residence time, and ex vivo drug permeation through porcine buccal membranes from optimized buccal patch and stability studies. The physicochemical interaction between PMZ HCl and polymers was investigated by Fourier Transform Infrared Spectroscopy. Ex vivo drug permeation through porcine buccal membrane was performed and 83.7% of the drug permeated in 6 hours with flux 0.19 mg h–1cm–2. The optimized formulation AA4 showed maximum drug release (98%) in 6 hours in the Higuchi model release profile. Moisture absorption, surface pH, tensile strength, elongation at break, peak detachment force and work of adhesion values of the optimized formulation were found to be 68.1%, pH 6.7, 12.3 kg/mm2, 69.2 % mm2, 7.5 N and 2.73 mJ respectively. Formulation AA4 showed 77.6% of the drug permeated through porcine buccal membrane in 6 hours and flux calculated to be 0.45 mg h–1cm–2. FTIR studies showed no evidence of interaction between the drug and polymers. In vivo mucoadhesive behaviour of the optimized formulation was studied in healthy human volunteers and subjective parameters were evaluated. The stability of the optimized formulation was studied and no significant changes were detected in drug content, in vitro release and ex vivo permeation after 6 months.

scholarly journals FORMULATION AND EVALUATION OF IN-SITU GEL CONTAINING LINEZOLID IN THE TREATMENT OF PERIODONTITIS

2021 ◽  
pp. 79-86
Author(s):  
INAYATHULLA . ◽  
PRAKASH GOUDANAVAR ◽  
MOHAMMAD ALI ◽  
SHAHID UD DIN WANI ◽  
NAGARAJA SREEHARSHA
Keyword(s):  
Drug Release ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
In Situ Gel ◽  
Diffusion Controlled ◽  
Gelling Time ◽  
Carbopol 934P

Objective: The intent to prepare and evaluate Linezolid in-situ gel in the treatment of periodontitis. Methods: pH-sensitive in-situ gel was formed by the cold method using a varying concentration of the drug, carbopol 934P and hydroxypropyl methylcellulose (HPMC) and carbopol 934P and sodium carboxy methylcellulose (CMC) (1:1,1:1.5,1:2,1:2.5). An optimized batch was selected based on gelling time and gelling capacity. The prepared in-situ gels were evaluated for appearance, pH, gelling capacity, viscosity, in vitro release studies, rheological studies, and finally, was subjected to drug content estimation and antibacterial activity test. Results: FTIR study shows drug and physical mixture were compatible with each other. The rheology of formulated in-situ gel exhibited a pseudoplastic flow pattern. this may be because when polymer concentration was increased the prepared formulations become more viscous and in turn delayed the drug release and from the prepared formulation, LF4 and SF4 have polymer concentrations i. e, 0.9% carbopol and sodium CMC showed drug release up to 12 h. Conclusion: When carbopol is appropriately mixed with other suitable polymers it forms an in-situ gel-forming system that was substantiated by the property to transform into stiff gels when the pH is increased. The in-situ gel was prepared using a combination of carbopol-HPMC and carbopol-Na CMC The formulations LF1 to SF4 showed high linearity (R2 = 0.490-0.682), indicating that the drug was released from the prepared in-situ gel by the diffusion-controlled mechanism. Thus, the formulation of batches LF4 and SF4 containing carbopol: HPMC and carbopol: NaCMC in 1:2 ratios were considered as optimum formulation based on optimum viscosity, gelling capacity and to extend the in vitro drug release.

scholarly journals Formulation and Evaluation of Matrix Type Transdermal Patches of Glibenclamide

2009 ◽  
Vol 1 (01) ◽  
Author(s):  
J. R. D. Gupta ◽  
R. Irchhiaya ◽  
N. Garud ◽  
Priyanka Tripathi ◽  
Prashant Dubey ◽  
...  
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Skin Permeation ◽  
Moisture Loss ◽  
In Vitro Drug Release ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Weight Variation ◽  
Cumulative Amount

Matrix type transdermal patches containing Glibenclamide were prepared using three different polymers by solvent evaporation technique. Aluminium foil cup method was used as a substrate. Polyethylene glycol (PEG) 400 was used as plasticizer and Dimethyl sulfoxide (DMSO) was used as penetration enhancer. The physicochemical parameters like weight variation, thickness, folding endurance, drug content, % moisture absorption and % moisture loss were evaluated. In vitro drug release studies and skin permeation studies were carried out using Franz diffusion cell. Cumulative amount of drug released in 12 hours from the six formulations were 55.467, 52.633, 47.157, 53.394, 49.139 and 45.597 %, respectively. The corresponding values for cumulative amount of drug permeated for the said formulation were 43.013, 40.429, 37.793, 41.522, 37.450 and 34.656 %, respectively. On the basis of in vitro drug release and skin permeation performance, formulation HP-1 was found to be better than other formulations and it was selected as the optimized formulation.

scholarly journals EVALUATION OF OCULAR FILMS OF OFLOXACIN FOR ANTIBACTERIAL ACTIVITY

2018 ◽  
Vol 10 (6) ◽  
pp. 275 ◽  
Author(s):  
Arun Kumar ◽  
Brijesh Kumar Tiwari ◽  
Sokindra Kumar
Keyword(s):  
Antibacterial Activity ◽  
Drug Release ◽  
Moisture Absorption ◽  
Stability Study ◽  
Moisture Loss ◽  
Anhydrous Calcium Chloride ◽  
Ocular Infection ◽  
Surface Ph ◽  
Folding Endurance

Objective: The current study emphasizes on the treatment of ocular infection with objectives of reducing the frequency of administration, obtaining controlled release and greater therapeutic efficacy of the drug (ofloxacin) using ocular films.Methods: Ocular films were designed by solvent evaporation method containing a different combination of polymers. The folding endurance (mechanical strength) was determined by the number of folds at a specific single place required to break the film into two parts. Thickness was measured using screw gauze. The surface pH was done by pH paper. The percentage moisture absorption was carried out by placing the ocular films in a desiccator containing ammonium chloride. Percentage moisture loss was carried out by placing the ocular films in the desiccator containing anhydrous calcium chloride. in vitro drug release study were carried by using a modified version of franz diffusion cell. Stability study were carried using stability chambers as per ICH guidelines. The antibacterial activity was performed by using male albino rabbits.Results: The thickness and folding endurance of the films were in the range of 44±1.1 to 92±1.8 and 4.5±0.6 to 6.8±0.3, respectively for different formulations. Surface pH was evaluated in the range of 6.6 to 7.2. Percentage moisture absorption and percentage moisture loss were evaluated in the range of 1.17±1.1 to 6.72±1.5 and 0.58±0.9 to 1.23±0.9 respectively. Microbial growth was not observed in any formulation during sterility testing. The drug release for different batch codes PAH, PBE, PCP, PDC, PEEH, and PFEC was found to be 96.2, 56.9, 93.4, 94.5, 98.4 and 95.9 % respectively up to 12 h. Ocular films of batch code PEEH was optimized for maximum drug release (98.4%). The antibacterial effect was noted periodically (01 to 05 d) after administration of sterile formulation in the treated eyes vs. control eyes of each rabbit. The optimized batch PEEH of ocular films reduced the infection and redness completely within 3 d in a single dose.Conclusion: The optimized formulation would be able to offer benefits such as increased residence time, prolonged drug release, reduced frequency of administration and improved patient compliance with complete removal of inflammation and redness from the cul-de-sac.

scholarly journals In Vitro Drug Release Studies from a Novel Lyophilised Nasal Dosage Form

1970 ◽  
Vol 5 (1) ◽  
pp. 71-86 ◽  
Author(s):  
Panna Thapa ◽  
Howard NE Stevens ◽  
Alan J Baillie
Keyword(s):  
Drug Release ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Diffusion Cell ◽  
Nasal Drug Delivery ◽  
Donor Side ◽  
Receptor Compartment ◽  
The Difference

In vitro release of nicotine hydrogen tartrate (NHT) into phosphate buffer saline (PBS), pH 7.4 at 37°C was studied in a diffusion cell, which, with a minimal dissolution volume on the donor side, was intended to mimic the low hydration environment of the nasal mucosa. Lyophilisates prepared from different concentrations (0.25, 0.5, 1, 2 & 3% w/w) of Methocel K4MP solution and K100LVP, K15MP, K100MP solutions (1 & 2%) containing NHT were placed on the diffusion cell membrane which was maintained just in contact with the constantly agitated liquid phase of the receptor compartment. Samples were withdrawn at regular time intervals from the receptor compartment, replaced by fresh medium and analysed spectrophotometrically at 260nm after appropriate dilution. As controls, nicotine release profiles from NHT powder & aqueous solution, Methocel K solutions, and simple powder blends of K4MP were also measured. The nicotine release was dependent on the concentration of Methocel K polymer, whether the donor side of the cell was presented with a solution or lyophilisate of NHT in polymer. Nicotine release decreased with increasing polymer concentration (t50% = 25 min and 75 min for lyophilisate prepared from 1% and 3% w/w K4MP respectively). However at any polymer concentration, nicotine release was faster from solution than from lyophilisate. The difference in nicotine release between solution and lyophilisate became more prominent at higher polymer concentration. Interestingly, nicotine release was independent of Methocel K molecular weight. In vitro nicotine release took place by anomalous diffusion. Keywords: In vitro drug release; lyophilisation; nasal drug delivery; hydroxypropyl methylcellulose (HPMC), nicotine. DOI: 10.3126/kuset.v5i1.2848 Kathmandu University Journal of Science, Engineering and Technology Vol.5, No.1, January 2009, pp 71-86

Sign in / Sign up

Export Citation Format

Share Document