scholarly journals Formulation development of oral controlled release tablets of hydralazine: Optimization of drug release and bioadhesive characteristics

2009 ◽  
Vol 59 (1) ◽  
pp. 1-13 ◽  
Author(s):  
Bhupinder Singh ◽  
Sonia Pahuja ◽  
Rishi Kapil ◽  
Naveen Ahuja
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Ex Vivo ◽  
Methyl Cellulose ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Optimization Study ◽  
Hydralazine Hydrochloride ◽  
Controlled Release Tablets

Formulation development of oral controlled release tablets of hydralazine: Optimization of drug release and bioadhesive characteristicsThe current study involves development of oral bioadhesive hydrophilic matrices of hydralazine hydrochloride, and optimization of theirin vitrodrug release profile andex vivobioadhesion against porcine gastric mucosa. A 32central composite design was employed to systematically optimize the drug delivery formulations containing two polymers,viz., carbomer and hydroxypropyl methyl cellulose. Response surface plots were drawn and optimum formulations were selected by brute force searches. Validation of the formulation optimization study indicated a very high degree of prognostic ability. The study successfully undertook the development of an optimized once-a-day formulation of hydralazine with excellent bioadhesive and controlled release characteristics.

DESIGN AND EVALUATION OF EUDRAGIT COATED LOSARTAN POTASSIUM CONTROLLED RELEASE PELLETS BY PAN COATING TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (10) ◽  
pp. 30-38
Author(s):  
S Vidyadhara ◽  
◽  
R. L. C. Sasidhar ◽  
P Thrilochani ◽  
L. K. Lavanya
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Methyl Cellulose ◽  
Losartan Potassium ◽  
Scanning Calorimetry ◽  
Coating Agent ◽  
Coating Technique ◽  
S 100 ◽  
Eudragit S 100

The present investigation was focused on the development and evaluation of controlled release pellets of losartan potassium with Eudragit S 100 and hydroxypropyl methyl cellulose phthalate (HPMCP) by employing pan coating technique. Eudragit S 100, a high viscosity grade controlled release polymer, was mainly used as coating agent for regulating the drug release from pellets. HPMCP, an enteric coating polymer was used in the present study to regulate the drug release at varied G.I. pH conditions. The prepared pellets were evaluated for particle size, drug content, friability and for in vitro drug release. The formulations were further characterized to identify any possible interactions by FTIR spectroscopy and differential scanning calorimetry. The surface morphology of the pellets was studied by scanning electron microscopy. From the results it was observed that due to increase in the concentration of Eudragit the drug release was extended up to 12 hours. The increase in the HPMCP polymeric concentration in formulations showed initial delay in drug release.

scholarly journals Preparation of Biodegradable Silk Fibroin/Alginate Blend Films for Controlled Release of Antimicrobial Drugs

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Yaowalak Srisuwan ◽  
Yodthong Baimark
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Silk Fibroin ◽  
Water Soluble ◽  
Drug Release Profile ◽  
Sem Images ◽  
Blend Ratio ◽  
Blend Films ◽  
Vis Spectroscopy

Silk fibroin (SF)/alginate blend films have been prepared for controlled release of tetracycline hydrochloride, an antimicrobial model drug. The blend films were analysed by Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and UV-vis spectroscopy. The functional groups of the SF/alginate blends were monitored from their FTIR spectra. The homogeneity of the blend films was observed from SEM images. The dissolution and film transparency of the blend films depended on the SF/alginate blend ratio. Thein vitrodrug release profile of the blend films was determined by plotting the cumulative drug release versus time. It was found that the drug release significantly decreased as the SF/alginate blend ratio increased. The results demonstrated that the SF/alginate blend films should be a useful controlled-release delivery system for water-soluble drugs.

Drug release profile and reduction in the in vitro burst release from pectin/HEMA hydrogel nanocomposites crosslinked with titania

RSC Advances ◽  
2016 ◽  
Vol 6 (23) ◽  
pp. 19060-19068 ◽  
Author(s):  
Elisangela P. da Silva ◽  
Marcos R. Guilherme ◽  
Francielle P. Garcia ◽  
Celso V. Nakamura ◽  
Lucio Cardozo-Filho ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Profile ◽  
Burst Release ◽  
Drug Release Profile ◽  
Initial Release ◽  
Hydrogel Nanocomposites

Hydrogel nanocomposites of pectin, HEMA and titania for Vit-B12 controlled release with reduced initial release burst were prepared. A reduction of up to ca. 60% was observed.

scholarly journals Vaginal Microbicide Gel for Delivery of IQP-0528, a Pyrimidinedione Analog with a Dual Mechanism of Action against HIV-1

2011 ◽  
Vol 55 (4) ◽  
pp. 1650-1660 ◽  
Author(s):  
Alamelu Mahalingam ◽  
Adam P. Simmons ◽  
Shweta R. Ugaonkar ◽  
Karen M. Watson ◽  
Charlene S. Dezzutti ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Mechanical Stability ◽  
Culture Media ◽  
Ex Vivo ◽  
Hydroxyethyl Cellulose ◽  
Therapeutic Window ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Hiv 1

ABSTRACTPyrimidinediones, a novel class of compounds, have previously been shown to possess antiviral activity at nanomolar concentrations. One member of this class of compounds, IQP-0528, was selected as the lead molecule for formulation development owing to its stability at physiologically relevant conditions, wide therapeutic window, and antiviral activity in the nanomolar range. Here, we report the development of two vaginal gels—3.0% hydroxyethyl cellulose (HEC) formulation and a 0.65% Carbopol formulation—for the sustained delivery of IQP-0528. Stability studies under accelerated conditions confirmed the chemical stability of IQP-0528 and mechanical stability of the gel formulation for 3 months.In vitrorelease studies revealed that diffusion-controlled release of IQP-0528 occurred over 6 h, with an initial lag time of approximately 1 h. Based on the drug release profile, the 3.0% HEC gel was selected as the lead formulation for safety and activity evaluations. Thein vitroandex vivosafety evaluations showed no significant loss in cell viability or significant inflammatory response after treatment with a 3.0% HEC gel containing 0.25% IQP-0528. In anin vitroHIV-1 entry inhibition assay, the lead formulation showed an 50% effective concentration of 0.14 μg/ml for gel in culture media, which corresponds to ∼0.001 μM IQP-0528. The antiviral activity was further confirmed by using polarized cervical explants, in which the formulation showed complete protection against HIV infection. In summary, these results are encouraging and warrant further evaluation of IQP-0528 gel formulations inin vivomodels, as well as the development of alternative formulations for the delivery of IQP-0528 as a microbicide.

scholarly journals Formulation development and evaluation of Luliconazole Topical Emulgel

2021 ◽  
pp. 79-87
Author(s):  
Naga sai divya K ◽  
T Malyadri ◽  
Ch.saibabu
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Formulation Development ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Diffusion Controlled ◽  
Carbopol 940 ◽  
Vitro Release

The purpose of the present study was to develop and optimize the emulgel system for Luliconazole using different types of gelling agents: HPMCK15M, Carbopol 940, and Xanthan Gum. The prepared emulgels were evaluated in terms of appearance, pH, spreadability, viscosity, drug content, and in-vitro drug release. In-vitro release study demonstrated diffusion-controlled release of Luliconazole from formulation up to 12 hours. The drug release profile exhibited zero-order kinetics. All the prepared emulgels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and higher drug release. In the case of all evaluation parameters, carbopol based formulation showed better properties so, as a general conclusion, it was suggested that the Luliconazole emulgel formulation prepared with carbopol (F6) was the formula of choice.

scholarly journals Formulation development and evaluation of voriconazole sustained release tablets

2013 ◽  
Vol 2 (10) ◽  
pp. 165-169 ◽  
Author(s):  
Manivannan Rangasamy ◽  
Venkata Krishna Reddy Palnati ◽  
Lakshmi Narayana Rao Bandaru
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Angle Of Repose ◽  
Type I ◽  
Dissolution Test ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Weight Variation ◽  
Sustained Release Tablets

The present study involves in the formulation and evaluation of sustained release tablets of Voriconazole (250mg). The objective of the present study was to formulate Voriconazole sustained release tablets by wet granulation method by using natural (Xanthan gum, Karaya gum) and semi synthetic polymers (HPMC K100M). Lactose was used as diluting agent, Magnesium stearate was used as a lubricant and Talc was used as a glident. These sustained release tablets can release the drug up to 12 hours in predetermined rate. The formulated powder blend was evaluated for bulk density, tapped density, compressibility index and angle of repose. The formulated tablets were evaluated for physical characteristics of sustained release tablets such as thickness, hardness, friability, weight variation and drug content. The results of the formulations found to be within the limits specified in official books. The tablets were evaluated for In-vitro drug release studies by using USP type I dissolution test apparatus. The dissolution test was performed in 0.1 N HCL for 2 hr and phosphate buffer pH 6.8 for 10hrs. The in-vitro cumulative drug release profile of all formulations F1-F10 at 12 hours showed 84.25% to 99.82% drug release, respectively. From the data it was clear that by increasing the amount of polymer in the formulation the amount of drug release was decreased. Hence, Formulation F9 was the most promising formulation as it gives satisfactory release (99.82%) for 12 hours and F9 found to be the best formulation.DOI: http://dx.doi.org/10.3329/icpj.v2i10.16410 International Current Pharmaceutical Journal, September 2013, 2(10): 165-169

scholarly journals ANTIEPILEPTIC RECTAL HYDROGEL LOADED WITH CARBAMAZEPINE – RICE BRAN WAX MICROSPHERES

2017 ◽  
Vol 10 (3) ◽  
pp. 264 ◽  
Author(s):  
Sreeja C Nair ◽  
Krishnapriya M ◽  
Karthika Ramesh
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Rice Bran ◽  
Ex Vivo ◽  
Rectal Mucosa ◽  
Natural Polymers ◽  
Rice Bran Wax ◽  
Release Pattern ◽  
Wide Range

ABSTRACTObjectives: The objective behind the study is to develop a mucoadhesive rectal hydrogel from carbamazepine (CBZ) – rice bran wax (RBW)microspheres for the purpose of controlled release for the treatment of epilepsy.Methods: The study was conducted to formulate controlled release rectal hydrogel loaded with CBZ – RBW microspheres in two different natural polymers,RBW and collagen which are prepared by modified cooling induced solidification method and gel preparation along with their evaluation studies.Results: A thorough analysis of the optimized gel revealed that all the evaluation parameters evaluated are within the acceptable limits. Further, theoptimized microsphere formulation (M5) was used to formulate it as rectal hydrogel using polymer collagen and was characterized. The mucoadhesiontime of 25% w/w collagen hydrogel (H4) was 565 minutes, allowing the loaded microspheres to be attached on rectal mucosa. In vitro drug releasefrom the mucoadhesive hydrogel formulations showed controlled drug release pattern with a maximum drug release of 96.45±0.35% for optimizedH4 formulation after 12 hr, followed zero order release pattern with diffusion mediated Higuchi model. Ex vivo permeation studies using bovine rectalmucosa revealed that H4 formulation showed greater permeability compared to control. Histopathological findings revealed that H4 formulation issafer for rectal administration without any signs of rectal irritancy. The stability studies of optimized formulation (H4) proved that hydrogel remainedstable over a wide range of temperature condition.Conclusion: Hence, the developed rectal hydrogel formulation seems to be a viable alternative to conventional drug delivery system for the effectivemanagement of epilepsy.Keywords: Carbamazepine, Rice bran wax, Rectal hydrogel, Sustainability.

Formulation Development of Aceclofenac Loaded Nanosupension by Three Square (32) Factorial Design

2012 ◽  
Vol 4 (4) ◽  
pp. 1575-1583
Author(s):  
Atul A Patak ◽  
Jorwekar, P ◽  
P D Chaudhari
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Factorial Design ◽  
In Vivo Studies ◽  
Differential Scanning Calorimetric ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Calorimetric Analysis ◽  
32 Factorial Design

In the present study, aceclofenac loaded polymeric nanosuspension were formulated and evaluated.  Aceclofenac is a potent analgesic under BCS Class II. Due to the need for its frequent dosing, aceclofenac is an ideal candidate for sustained or controlled drug delivery. For optimization of prepared formulation, the three square (32) factorial design was used.  Tween 80 (X1) and combination of Eudragit RL 100 and RS 100 (X2) were used as independent variables and particle size (Y1), entrapment efficiency (Y2), and Percent drug release (Y3) were taken as dependent variables. The formulations were evaluated for particle size, zeta potential and drug entrapment. The in vitro drug release profile supports nanosuspension form to be used as a sustained release vehicle for aceclofenac. The formulation was characterized by differential scanning calorimetric analysis, in vivo studies and stability testing.

FORMULATION DEVELOPMENT AND PHARMACODYNAMIC EVALUATION OF COLON TARGETED CONTROLLED RELEASE LORNOXICAM PELLETS FOR PAIN MANAGEMENT OF RHEUMATOID ARTHRITIS

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (08) ◽  
pp. 59-62
Author(s):  
M. U Paradkar ◽  
◽  
K. Hudda
Keyword(s):  
Rheumatoid Arthritis ◽  
Pain Management ◽  
Controlled Release ◽  
Drug Release ◽  
Physical Appearance ◽  
Screening Methods ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Eudragit S100

The aim of the present research work was to formulate and evaluate colon targeted pellets of lornoxicam for the pain management of rheumatoid arthritis. The product and process parameters were optimized by screening methods. Pellets were prepared by extrusion spheronization method using microcrystalline cellulose (MCC) as spheronizing aid and ethyl cellulose (EC) as controlled release polymer, in different ratios. Based on the physical appearance, sphericity and % in vitro drug release, batch B17 containing EC: MCC (6:4) was optimized for core pellets. The site specificity was obtained by screening Eudragit FS30D and Eudragit S100 as coating polymers and the core pellets were coated with Eudragit S100. The batch C4 (6%) showed appropriate physical appearance and % in vitro drug release upto 24 h, indicating controlled release property. The pharmacodynamic studies performed on rat model indicated the anti-inflammatory activity of pellet formulation. Thus, it is concluded that the coated pellets can be a good candidate for site specific delivery of lornoxicam to colon by decreasing the gastric irritation, reducing dose frequency and improving patient compliance.

scholarly journals APPLICATION OF NOVEL NATURAL POLYMER FOR CONTROLLING THE RELEASE OF FENOVERINE FROM CONTROLLED RELEASE MATRIX TABLETS

2017 ◽  
Vol 9 (2) ◽  
pp. 1 ◽  
Author(s):  
Ajit Kulkarni ◽  
Trushali Mandhare ◽  
Nagesh Aloorkar
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Natural Polymer ◽  
In Vitro Drug Release ◽  
Dissolution Studies ◽  
Drug Content

Objective: To explore a novel natural polymer, pullulan for controlling the release of fenoverine from matrix tablets and to elucidate the release kinetics of fenoverine from pullulan and HPMC matrices.Methods: In this study we formulated monolithic matrix tablets containing of fenoverine as controlled-release tablets by direct compression using pullulan, HPMC (Hydroxypropyl methyl cellulose) K4M and HPMC K100M polymers and evaluated for hardness, thickness, friability, weight variation drug content, in vitro drug release characteristics and FTIR (Fourier transform infrared spectroscopy) and DSC (Differential scanning calorimetry) study.Results: All the formulations showed compliance with pharmacopoeial standards. FTIR and DSC study indicated the absence of interaction between fenoverine and excipients. The formulation was optimized on the basis of acceptable tablet properties and in vitro drug release. The results of dissolution studies indicated that the formulation F5 [drug to polymer 1: 0.35] exhibited highest % cumulative drug release of 96.82±0.75 % at the end of 12 h. Optimised batch F5 showed super case II transport mechanism and followed zero order release kinetics. Short-term stability studies of the optimized formulation indicated that there were no significant changes observed in hardness, drug content and in vitro dissolution studies at the end of three months period. Similarity factor f2 was found to be 89, which indicated similar dissolution profiles before and after stability study.Conclusion: Based on above results we conclude that pullulan can be used as a polymer for retarding the release of drug from matrix formulations.Keywords: Pullulan, Fenoverine, Hydroxypropyl methyl cellulose, Controlled release, In vitro

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