scholarly journals FORMULATION AND CHARACTERIZATION OF PERIODONTAL FILMS CONTAINING AZITHROMYCIN AND SERRATIOPEPTIDASE

Author(s):  
Soniya Rani ◽  
Nardev Singh

Objective: The objective of the present work was to formulate and evaluate periodontal film, which could be capable of delivering therapeutic concentration of azithromycin and serratiopeptidase for a prolonged period of time and could be easily placed into the periodontal pocket. Methods: The films were prepared by solvent casting method using combinations of ethyl cellulose, hydroxypropyl methylcellulose K4M, hydroxypropyl methylcellulose 50 cps, eudragit L-100, and Chitosan in different ratios using dibutyl phthalate as plasticizer. The periodontal films were evaluated for weight variation, thickness, percentage moisture absorption, percentage moisture loss, folding endurance, percentage swelling index, percentage elongation, and in vitro percentage cumulative drug-enzyme release profile. Results: Formulation F12 was found to be a good periodontal film. Hence, it was considered as an optimized formulation. In vitro drug-enzyme release rate studies using keshary-chien diffusion cell showed maximum drug release in F12 formulation (95.92% for azithromycin and 94.20% for serratiopeptidase at the end of 24 h) compared to other formulations. Conclusion: The optimized formulation F12 showed the best drug-enzyme release profile among the others for the preparation of periodontal film. There is a scope for the further study and development of the azithromycin and serratiopeptidase periodontal films.

Author(s):  
SHIKHA BAGHEL CHAUHAN ◽  
SUSHILA SAINI

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers. Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin. Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability. Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.


Author(s):  
Sanjay P ◽  
Vishal Gupta N ◽  
Gowda Dv ◽  
Praveen Sivadasu

Objective: The main objective of the study was to formulate the oral disintegrating films loaded with atenolol by solvent-casting method and to carry out its evaluation studies.Methods: The films were prepared using the film-forming hydrophilic polymer like hydroxypropyl methylcellulose (E-5) and super disintegrant like pectin in various proportions.The formulated oral films were characterized for Fourier transform infrared (FTIR) and morphological evaluations. Various physicochemical parameters such as weight variation, folding endurance, surface pH, in vitro disintegration, and in vitro dissolution studies were carried out.Results: FTIR studies revealed that there was no drug-polymer interaction. The morphological evaluation of films showed that all the films were homogenous and transparent. The folding endurance test ensured that the films had sufficient brittleness and by weight variation test, it was inferred that all the films were within the deviation. The surface pH study showed the pH of the films was around neutral pH. The drug was well distributed in all the films. The films disintegrated within 120 s and the fastest being disintegrated in 30 s. Based on all the evaluation parameters, F6 had shown optimal performance and remarkable increase in drug release of 94.38% in 2 min.Conclusion: Thus, formulated oral disintegrating films can be termed as an alternative approach to deliver atenolol.


Author(s):  
J. R. D. Gupta ◽  
R. Irchhiaya ◽  
N. Garud ◽  
Priyanka Tripathi ◽  
Prashant Dubey ◽  
...  

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.


2016 ◽  
Vol 19 (2) ◽  
pp. 133-146 ◽  
Author(s):  
Jayera Islam Urmi ◽  
Marzia Alam ◽  
Md Saiful Islam Pathan

Periodontitis is a local infection in the gingival crevices, which affects the structural organs surrounding the teeth like periodontal ligament, connective tissue and bone. Ornidazole is an antimicrobial drug widely used to treat periodontitis. The primary objective of this study was to design and evaluate periodontal films of ornidazole for placement into the periodontal pockets for targeted delivery of drug. Nine formulations (F1 to F9) were prepared by solvent casting method using polymer A, polymer B and plasticizer A. Chloroform and dichloromethane were used as solvent system. The API and dental films were then evaluated for various parameters including trinocular microscopic image, melting point, weight variation, thickness, folding endurance, surface pH, swelling index, percentage moisture loss, antimicrobial activity, content uniformity, in vitro drug release and release kinetics as well as RTIR and DSC. Formulation F1 showed the minimum weight and thickness and F9 showed the maximum. It was observed that weight and thickness of film were directly proportional to the total solid content of the film. RSDs of content uniformity test for all the batches were below 3.0%. Folding endurance and swelling index of films were inversely proportional to the amount of polymer in the film. The surface pH of all the batches were between 6-7. Formulation F1 revealed the maximum percentage of moisture loss (19.34%), while F8 showed the minimum (3.654%). Formulation F2 demonstrated data the highest zone of inhibition (21.91 mm).Bangladesh Pharmaceutical Journal 19(2): 133-146, 2016


Author(s):  
Zainab E Jassim ◽  
Mais F Mohammed ◽  
Zainab Ahmed Sadeq

Objective: The aim of the present work was to formulate and evaluate fast dissolving film containing lornoxicam.Materials and Methods: To prepare the film, hydroxypropyl methylcellulose E5 and polyvinyl alcohol (PVA) were used as film-forming polymers by solvent casting method. Glycerine was used as plasticizer, aspartame, and mannitol as sweetener. All prepared films were evaluated for its weight variation, disintegration time, thickness, drug content, pH, dissolution study, and folding endurance. The drug-excipients compatibility study was done using differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR).Results: Satisfactory results obtained when PVA was used as film-forming polymer, and the drug was dispersed in the polymer solution using poloxamer 407 as a solubilizing agent. Formulation F2 is considered as the optimized formulation as it showed good folding endurance (>300), faster disintegration rate (30 s), and maximum in vitro drug release (87%) within 5 min. DSC and FTIR studies showed no interaction between drug and the polymers.Conclusion: It can be concluded from the study that the fast dissolving film can be prepared for poorly water-soluble drug lornoxicam using PVA as a suitable film-forming polymer.


2018 ◽  
Vol 10 (6) ◽  
pp. 275 ◽  
Author(s):  
Arun Kumar ◽  
Brijesh Kumar Tiwari ◽  
Sokindra Kumar

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.


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (07) ◽  
pp. 53-58
Author(s):  
Sanjana A. ◽  
Mohammed Gulzar Ahmed ◽  
Jaswanth Gowda B. H. ◽  

The study was aimed to formulate a dental film containing linezolid, a broad spectrum antimicrobial agent which could be easily placed into the periodontal pocket and be capable of delivering therapeutic concentrations of drug for prolonged periods and also reducing the side effects. In the present investigation, chitosan strips containing linezolid in three different concentrations (10, 20, and 30 %w/w with respect to the weight of polymer) were prepared by the solvent casting method, by using 1 %V/V acetic acid solution. The prepared formulations were evaluated for various properties such as weight variation, thickness, folding endurance, moisture loss, tensile strength, in vitro release, release kinetic study and stability studies. The weight variation and thickness were found to be in the range of (0.99-1.58 mg) and (0.92-1.76 mm), the moisture content, folding endurance was found to be maximum for the plain film and minimum for the drug containing formulation. The tensile strength was found to be in the range of (2.44-1.43 kg/ mm2 ) for the formulation. The dissolution studies showed a burst release initially followed by a progressive fall in the release of the drug (91.15 - 95.87 %) and the release kinetics followed the zero-order pattern. The short term stability studies were conducted and there were no significant changes observed. Hence, low dose, site-specific linezolid film is a potential tool for the treatment of periodontitis.


Author(s):  
SHUBHAM BIYANI ◽  
SARANG MALGIRWAR ◽  
RAJESHWAR KSHIRSAGAR ◽  
SAGAR KOTHAWADE

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design. Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study. Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation. Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.


Processes ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 778
Author(s):  
Emőke-Margit Rédai ◽  
Paula Antonoaea ◽  
Nicoleta Todoran ◽  
Robert Alexandru Vlad ◽  
Magdalena Bîrsan ◽  
...  

The most used pharmaceutical formulations for children are syrups, suppositories, soft chewable capsules, and mini-tablets. Administrating them might create an administration discomfort. This study aimed to develop and evaluate orodispersible films (ODFs) for pediatric patients in which the fluoxetine (FX) is formulated in the polymeric matrix. Six FX fast dissolving films (10 mg FX/ODF), FX1, FX2, FX3, FX4, FX5, and FX6, were prepared by solvent casting technique. In the composition of the ODFs, the concentration of the hydroxypropyl methylcellulose and the concentration of the propylene glycol were varied. Each formulation of fluoxetine ODF was evaluated by determining the tensile strength, folding endurance, disintegration, behavior in the controlled humidity and temperature conditions, and adhesiveness. All the obtained results were compared with the results obtained for six ODFs prepared without FX. The disintegration time of the FX ODFs was of maximum 88 s for FX2. Via the in vitro releasing study of the FX from the ODFs it was noticed that FX1 and FX2 allow a better release of the drug 99.98 ± 3.81% and 97.67 ± 3.85% being released within 15 min. From the obtained results it was also confirmed that FX ODFs were found to follow first-order release kinetic.


Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S

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.


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