scholarly journals “FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF PREDNISOLONE”

Author(s):  
Chirayu. C ◽  
Nagaraja T.S ◽  
Vitthal K Vijapure

The purpose of this research work was to develop and evaluate transdermal patch of Prednisolone, using Xanthan gum, Guar gum and Polyacrylamide in different ratios prepared by the Glass Substrate Technique. The physicochemical compatibility of the polymers and the drug was evaluated by FTIR. The results suggested that no physicochemical incompatibility between the polymer and the drug. Drug free films were formulated and evaluated characteristics like flexibility and smoothness. Further drug loaded films were formulated and evaluated for thickness, weight uniformity, drug content, folding endurance and drug release. The XRD analysis confirmed the amorphous dispersion of the drug in the formulation. SEM analysis showed surface morphology of prepared formulations. Drug diffusion through cellophane membrane was carried out using Franz diffusion cell by in-vitro study. The film prepared with formulation PDS 9 showed maximum diffusion release at the end of 24 hours. It is shown that drug release follows order and non Fikinian mechanism of release diffusion. The PDS 9 formulation was found to be stable with respect to drug content as well as physical changes at 40 ºC and 75 % RH. Keywords: Transdermal drug delivery, Prednisolone, Xanthan gum, Guar gum, Polyacrylamide.

Author(s):  
MANJULA D ◽  
ABHISHEK RAJ ◽  
JOSEPHINE LENO JENITA J ◽  
SHANAZ BANU

Objective: The current research work has been carried out with the aim to develop a transdermal gel formulation of fenoprofen (a nonsteroidal anti-inflammatory drug used to treat pain associated in arthritis) which would overcome the gastrointestinal-related problems associated with oral administration of the drug. The present study aims at formulating transdermal gels using different concentrations of Carbopol, hydroxypropyl methylcellulose (HPMC), sodium alginate, and guar gum. Methods: The formulated gels were subjected for various evaluation tests such as clarity, homogeneity, viscosity, drug content, pH, spreadability, and in vitro permeation studies. Drug–polymer interaction was studied by Fourier transmission infrared (FTIR) and differential scanning calorimetry (DSC). The in vitro permeation studies were performed in phosphate buffer 7.4 using Franz diffusion cell. Results: The FT-IR and DSC studies showed no chemical interaction between drug and polymers used. All the formulated gels showed acceptable physical properties with respect to clarity, homogeneity, viscosity, drug content, pH, and spreadability. Among all the gel formulations, Carbopol gels containing fenoprofen showed good drug release compared to HPMC, sodium alginate, and guar gum. Optimized formulation was further subjected to kinetic studies which showed Higuchi model of drug release. The same formulation showed significant anti-inflammatory and analgesic activity, tested in Wistar albino rats. No signs of erythema, edema, flushing, and papules were observed when skin irritation test was performed. Stability studies under accelerated condition showed satisfactory results for the optimized formulation. Conclusions: Thus, it was concluded from the results that the optimized formulation showed controlled and slow drug delivery. Animal studies were significant at p<0.05 and 0.001. The selected formulation was stable at various ambient temperatures.


1970 ◽  
Vol 1 (3) ◽  
pp. 43-49 ◽  
Author(s):  
Jovita Kanoujia ◽  
Kanchan Sonker ◽  
Manisha Pandey ◽  
Koshy M Kymonil ◽  
Shubhini A Saraf

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49


Author(s):  
Anupriya Anand ◽  
Bharadhwaj Ramesh Iyer ◽  
Chandrasekar Ponnusamy ◽  
Rajesh Pandiyan ◽  
Abimanyu Sugumaran

Aim: The present research work discussed the preparation of lomustine loaded with chitosan nanoparticles (LNCp) by ionic gelation method with homogenization using the design on experiments by Box-Behnken design. Methods: The nanoparticles are evaluated by particle size, zeta potential, surface morphology, drug content, entrapment efficiency and in-vitro drug release. Results: The FT-IR results support that drug have no interaction with excipients, which are used in the preparation of nanoparticle. The particle size, drug content and encapsulation efficiency of the developed nanoparticles ranged from 190 to 255 nm, 80.88% to 94.02%, and 77.12 to 88.74%, respectively. The drug release rate is diffusion-controlled over 8 hours. The F-value for all of the responses shows that the models are significant. The p-value, less than 0.05 for all the responses reveals the significance of the models. Graphical optimisation is done by desirability plot and overlay plot, which contains optimal values of independent variables with the desirability of 1. Conclusion: In conclusion, the results suggested that the optimised lomustine loaded chitosan nanoparticles are useful for brain targeting hence hold the potential for further research and clinical application.


Author(s):  
SARIPILLI RAJESWARI ◽  
M. YERNI KUMARI

Objective: The main aim of the present research work was to formulate fast dissolving tablets of famotidine by direct compression method and to evaluate the effect of synthetic super disintegrating agent on drug release pattern. Methods: The fast dissolving tablets were prepared by using crospovidone, croscarmellose sodium, sodium starch glycolate as superdisintegrants (2, 4 and 6 %w/w), mannitol 20 % and microcrystalline cellulose (44, 46 and 48 % w/w) as a directly compressible vehicle. All the prepared tablets were evaluated for hardness, friability, drug content uniformity, weight variation, disintegrating time, wetting time and in vitro drug release studies. Results: All the prepared fast dissolving tablets formulations were within the Pharmacopoeial standards limits. Based on in vitro drug release studies (>90 % within 30 min), the optimised formulations were optimised tested for the short term stability (at 40 ˚C/75% RH for 3 mo) and drug excipient interaction (fourier transform infrared spectroscopy). Conclusion: Hence, formulation prepared with 6 % w/w of crosspovidine and 44 % w/w of microcrystalline cellulose as emerged as the overall best formulation (>90 % within 30 min) compared to marketed product (>70 % within 30 min). Short-term stability studies on the formulations indicated that there are no significant changes in drug content and in vitro drug release (p<0.05).


Author(s):  
Sanjesh Rathi ◽  
Sohansinh Vaghela ◽  
Raj Shah ◽  
Shrenik Shah

The present research work done with an objective of preparation and evaluation of floating tablets of Febuxostat drug with Hydroxypropylenemethyl cellulose (HPMC), Polyox N-60K, Carbopol 934 P and Guar gum polymers. Floating tablets were based on effervescent approach using sodium bicarbonate a gas releasing agent. Direct compression method was used in present study for preparation of tablets. Effect of polymers was evaluated by studying drug release and floating time. In-vitro drug release profile indicates that sustained nature increased by increasing the concentration of polymer. The formulation containing Polyox N-60K and Carbopol 934 P in combination was optimized as it showed drug release up to 12hrs. Optimized formulation F18 was found stable during stability condition up to 1 month.


Author(s):  
Mona Semalty ◽  
T Bisht ◽  
A Semalty

The aim of the present study was to develop sustained release, multilayered-matrix tablet of aceclofenac using natural polymers-guar gum (GG) and xanthan gum (XG) as carrier for core matrix and hydroxyl propylmethyl cellulose (HPMC K-15M), sodium carboxymethylcellulose (NaCMC) and ethyl cellulose (EC) and polyvinylpyrrolidone (PVP-K30) for preparing bottom and top layers. The formulated tablets were evaluated for uniformity of weight, drug content, friability, hardness, thickness, swelling index and in vitro drug release. The physicochemical properties of tablets were found within the limits. The physiochemical investigation showed that aceclofenac matrix tablet prepared with xanthan gum showed better dissolution profile as compared to that of guar gum. Matrix tablets of xanthan gum with 6% W/V xanthan gum (MTX1) showed the highest percent drug release (88.98%), while matrix tablets of guar gum with 6% W/V guar gum (MTG1) showed the highest percent drug release (73.89%) at the end of 8 hours in pH 6.8 phosphate buffer. Among the matrix tablet of xanthan gum MTX4 (with 24% W/V of xanthan) showed the lowest percent drug release (49.6%) and while among the guar gum tablets MTG4  (with 24% W/V of guar gum) showed the lowest percent drug release (48.65%) at the end of 8 hours. It was concluded that increasing the concentration of gum from 6% W/V to 24% W/V in the formulation decreased the amount of drug release from the tablet. The xanthan gum based matrix tablets of aceclofenac were found to be superior to that of guar gum matrix tablets for potential therapeutic uses. 


2020 ◽  
Vol 10 (01) ◽  
pp. 9-15
Author(s):  
Sabitri Bindhani ◽  
Utkalika Mohapatra ◽  
Snehamayee Mohapatra ◽  
Rajat K. Kar

Nifedipine is a dihydropyridine calci channel blocking agent belongs to biopharmaceutical classification system (BCS) class-II mainly applied in the treatment of hypertension and angina-pectoris. The objective of this work is to improve the solubility and dissolution rate of nifedipine by formulating into a solid-self micro emulsifying drug delivery system (solid smedds). Methods: Oil, Surfactant, and cosurfactant were selected by solubility screening study. For the determination of the best emulsion region, a pseudo ternary diagram was prepared. Based on solubility castor oil, tween 80 and polyethylene glycol (PEG) 400 was selected in which SCOSmix (a mixture of surfactant and cosurfactant) was 1:1. Thermodynamic stability study was performed for the determination of stable smedds formulation. These formulations were evaluated for self emulsification time, drug content analysis, robustness to dilution test, particle size analysis, and in vitro diffusion study. The optimized formulation was selected for formulating into solid-smedds by using aerosil 200 at a different ratio. SCF9L (0.65:1) was selected due to its good flow property. Then it was evaluated for particle size analysis, drug content study, differential scanning calorimetry (DSC), X-Ray Diffraction study (XRD), fourier transform infrared spectroscopy (FTIR) Scanning Electron Microscopy study (SEM) analysis, and in vitro dissolution study. Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM analysis, the texture of powder showed a uniform granular structure, and there was no incompatibility between drugs. Excipients was observed from ftir study. From the in vitro dissolution study, it improved the dissolution rate of nifedipine, which was 98.68% of drug release, where pure drug release only 6.75%.


Author(s):  
Pavani Chowdary ◽  
T Sravani ◽  
MD Basheeruddin

<p>The purpose of this research work was to formulate and evaluate the sustained release tablets of <em>Nateglinide</em> 500mg, an antidiabetic drug. <em>Nateglinide </em>is an oral hypoglycemic agent. The tablets are prepared by direct compression method. The formulations were optimized by incorporating varying composition of Xanthan gum and guar gum as polymers, lactose as flow aid and magnesium stearate as lubricant. All the excipients are tested for compatibility with drug, which revealed that there was no physical and chemical interaction occurred. The Preformulation parameters such as bulk density, tapped density, compressibility index and Hausner’s ratio were analyzed. The friability, drug content, loss on drying, bulk density and percentage yield was evaluated for tablets. The effect of these variables on drug release also studied. The In-Vitro drug release studied were Performed in the USP dissolution apparatus-II using pH 0.1N HCl as dissolution media at 75 rpm speed and temperature of 37<sup>o</sup>c ± 5<sup>o</sup>c. The sampling was done at periodic time intervals of 1,4,8,12,16,20 and 24 hours and was replaced by equal volume of dissolution media after each withdrawal. The cumulative amount of drug release at different intervals is estimated using UV method. Based on the evaluation result the formulations F-7 was selected as best formulation. The tablets were found to follow first order kinetics and Higguchi mechanism of drug release, ‘n’ value is less than 0.5 which confirms that the drug release through the matrix was fickian diffusion.  </p>


Author(s):  
Shubhrajit Mantry ◽  
Anna Balaji

Objective: The objective of this research work to design nasal microspheres of ropinirole hydrochloride (HCL) using different mucoadhesive polymers by adopting the suitable technique. To study the influence of formulation and process variables on microsphere formation and release characteristics. To perform the physicochemical characterization of the prepared microspheres. To carry out in vitro drug release studies and to explore the release behavior using various kinetic models.Methods: Experiments were performed with ropinirole HCL as a drug, chitosan, guar gum, carbopol 974P as a polymer. Span 80 and Tween 80 used light liquid paraffin, concentrated hydrochloric acid as solvent.Result: The in vitro drug release studies were conducted for all the formulations, that is, F1-F21 in 250 ml phosphate buffer pH 6.6 for 12 hrs. Among them, F15 showed 82.7±0.23% drug release and F21 showed 81.2% in 12 hrs in a sustained manner.Conclusion: Microspheres were formulated by emulsion solvent evaporation technique using different polymers. Apart from preventing nasal irritation, the microsphere possesses two major advantages over plain solutions, one is a high solubilization capacity for ropinirole HCL that exceeds their aqueous solubility and thus allows a reduction in the application volume. The results of this work indicate that intranasal microsphere of ropinirole may be beneficial for the treatment of Parkinson’s disease.


2018 ◽  
Vol 10 (6) ◽  
pp. 161
Author(s):  
Shan Mohanan ◽  
Nabeela Rasheed ◽  
Bimal Raj K S

Objective: The aim of the study was to design and develop a gel based drug delivery system containing combinational drugs (ketoconazole, neomycin sulphate and diclofenac) for the effective treatment of Paronychia.Methods: The drugs used are ketoconazole, neomycin sulphate and diclofenac. The first two drugs provide an antifungal and antibacterial action and the last drug with a pain relieving effect. Two formulations of gels F1 and F2 were prepared using polymers like carbopol 934 and xanthan gum respectively. The amounts of drugs and other ingredients were kept as constant in both formulations. The prepared formulations were then evaluated by visual examination, pH, drug content, spredability, extrudability, drug release study, in vitro antibacterial study, in vitro antifungal study, stability studies and in vivo antibacterial study.Results: The obtained results were analyzed and compared. All the test results were within the accepted limit. The physicochemical properties of the gels were assessed and it was found that the two formulations have enough gel consistency with good spreadability and extrudability. The drug content and drug release studies of the prepared gels were done and the results showed that the all the three drugs were properly loaded into the gel system, with good drug release profile. The antimicrobial activities of the formulated gels were proved by both in vitro antifungal and antibacterial studies. The in vivo antibacterial studies revealed a significant reduction in bacterial count in wistar rats treated with prepared gel when compared with standard drug solution. From among all the developed formulations, F1 formulation with carbopol 934 has got a slight superior property when compared with formulation F2 xanthan gum as gelling agent.Conclusion: On the basis of the evaluation studies it was concluded that the drugs (ketoconazole, neomycin sulphate and diclofenac) were successfully incorporated into the different topical gel preparations with good physicochemical properties and antimicrobial activity. Therefore, it was concluded that our formulae could be very promising topical alternative for the treatment of Paronychia.


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