scholarly journals Effect of Viscosity Imparting Agents on In vitro Drug Release from PEG Based Suppositories

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Md. Kamruzzaman Akanda ◽  
SM Ashraful Islam ◽  
Jakir Ahmed Chowdhury ◽  
Md. Selim Reza
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Phosphate Buffer ◽  
Xanthan Gum ◽  
Methyl Cellulose ◽  
Lag Time ◽  
Carboxy Methyl Cellulose ◽  
Dissolution Medium ◽  
Carboxy Methyl

Acetaminophen loaded suppositories were prepared and the effects of viscosity imparting agents on drug release were investigated. Suppositories containing 125 mg of acetaminophen were prepared by fusion method using PEG 4000 and PEG 1500 as hydrophilic base. In vitro dissolution studies were carried out by a thermal shaker with a shaking speed of 90 rpm at a temperature of 37 ± 0.50C in phosphate buffer of pH 6.8. The effect of viscosity imparting agents on the drug release into phosphate buffer were investigated by adding 0.1, 0.2 and 0.3% Xanthan gum, sodium carboxy methyl cellulose, acacia, hydroxyl propyl methyl cellulose 15 cps and 50 cps. The In vitro release data showed that drug release was linear in phosphate buffer. After incorporation of viscosity imparting agents in phosphate buffer a biphasic drug release profile i.e. initial lag phase followed by linear phase was observed. Lag time depends on nature and concentration of viscosity imparting agents. It is evident from the result that lag time increases with the increase in percentage of viscosity imparting agent. There is less or no effect of change of concentration of acacia on the lag time. After lag time drug release from the suppositories showed a linear fashion. It was found that the release rate decreases when dissolution medium contains high percentage of Xanthan gum and also sodium carboxy methyl cellulose. However in case of incorporation of HPMC into the dissolution medium, release rate decreased up to 0.2% HPMC, but with 0.3% HPMC the release rate increased. Inclusion of different percentage of acacia into the dissolution medium has not significantly changed the release of acetaminophen from suppositories. Key words: Suppositories, Acetaminophen, Viscosity imparting agent Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

scholarly journals DESIGN AND EVALUATION OF INTRAGASTRIC BUOYANT TABLETS OF VENLAFAXINE HYDROCHLORIDE

2017 ◽  
Vol 10 (5) ◽  
pp. 166
Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Xanthan Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Methyl Cellulose ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Floating Drug Delivery ◽  
Venlafaxine Hydrochloride

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.

scholarly journals Studying the Rheological Properties of Non-Newtonian Fluids Under the Addition of Different Chemical Additives

2020 ◽  
Vol 23 (1) ◽  
pp. 68-80
Author(s):  
Douaa Hussein Ali ◽  
Muhannad A.R. Mohammed
Keyword(s):  
Sodium Chloride ◽  
Polyvinyl Alcohol ◽  
Rheological Properties ◽  
Apparent Viscosity ◽  
Xanthan Gum ◽  
Methyl Cellulose ◽  
Carboxy Methyl Cellulose ◽  
Chemical Additives ◽  
Low Viscosity ◽  
Carboxy Methyl

This research study the rheological properties ( plastic viscosity, yield point and apparent viscosity) of non-Newtonian fluids under the addition of different chemical additives with different concentrations, such as (xanthan gum (xc-polymer) , carboxy methyl cellulose ( high and low viscosity ) ,polyacrylamide, polyvinyl alcohol, starch, quebracho, chrome lignosulfonate, and sodium chloride (NaCl). Fann viscometer model 800 with 8-speeds was used to measure the rheological properties of these samples, that have already been prepared. All samples were subjected to Bingham plastic model. It was concluded that the plastic viscosity, yield point and apparent viscosity should be increased with increasing the concentrations of (xanthan gum (xc-polymer) , carboxy methyl cellulose ( high and low viscosity ) ,polyacrylamide, polyvinyl alcohol, starch and sodium chloride (NaCl), while the opposite is true for quebracho, chrome lignosulfonate.

scholarly journals Preparation and In vitro Evaluation of Theophylline Loaded Gastroretentive Floating Tablets of METHOCEL K4M

1970 ◽  
Vol 7 (1) ◽  
pp. 65-70 ◽  
Author(s):  
Ferdous Khan ◽  
Md Shaikhul Millat Ibn Razzak ◽  
Md Ziaur Rahman Khan ◽  
Kazi Rashidul Azam ◽  
Sams Mohammad Anowar Sadat ◽  
...  
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Release Rate ◽  
Lag Time ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Floating Tablets ◽  
Time Required

This investigation describes the preparation and in vitro evaluation of gastroretentive floating tablets of theophylline. Hydrophilic polymer METHOCEL K4M was used for its gel forming and release controlling properties. Sodium bicarbonate and citric acid were incorporated as gas generating agents. The effects of soluble components (sodium bicarbonate and citric acid), gel forming agent (METHOCEL K4M) and dose variation on drug release profile and floating properties were investigated. It has been observed that in all cases increase of the amount of floating agent caused a decrease of the floating lag time. Increase of theophylline load showed an increase of the floating lag time, which was independent of floating agent content. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixon-Crowell equations. The release rate, extent and mechanisms were found to be governed by the content of polymer and floating agent. The content of active ingredient was also a vital factor in controlling drug release pattern. It was found that polymer content and amount of floating agent significantly affected the time required for 50% of drug release (T50%), percentage drug release after 8 hours, release rate constant, and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed that the drug release mechanism could range from diffusion controlled to case II transport, which was mainly dependent on presence of relative amount of theophylline, polymer and floating agent. Key words: Gastroretention, Floating tablet, Theophylline  DOI = 10.3329/dujps.v7i1.1220 Dhaka Univ. J. Pharm. Sci. 7(1): 65-70, 2008 (June)

scholarly journals Formulation and Evaluation of Floating Oral In Situ Gelling System of Amoxicillin

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Dasharath M. Patel ◽  
Divyesh K. Patel ◽  
Chhagan N. Patel
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Lag Time ◽  
Solution Viscosity ◽  
High Dose ◽  
In Situ Gelling

Purpose. Effective Helicobacter pylori eradication requires delivery of the antibiotic locally in the stomach. High dose of amoxicillin (750 to 1000 mg) is difficult to incorporate in floating tablets but can easily be given in liquid dosage form. Keeping the above facts in mind, we made an attempt to develop a new floating in situ gelling system of amoxicillin with increased residence time using sodium alginate as gelling polymer to eradicate H. pylori. Methods. Floating in situ gelling formulations were prepared using sodium alginate, calcium chloride, sodium citrate, hydroxypropyl methyl cellulose K100, and sodium bicarbonate. The prepared formulations were evaluated for solution viscosity, floating lag time, total floating time, and in vitro drug release. The formulation was optimized using a 32 full factorial design. Dissolution data were fitted to various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. Results. All formulations (F1–F9) showed floating within 30 s and had total floating time of more than 24 h. All the formulations showed good pourability. It was observed that concentration of sodium alginate and HPMC K100 had significant influence on floating lag time, cumulative percentage drug release in 6 h and 10 h. The batch F8 was considered optimum since it showed more similarity in drug release () to the theoretical release profile. Conclusion. Floating in situ gelling system of amoxicillin can be formulated using sodium alginate as a gelling polymer to sustain the drug release for 10 to 12 h with zero-order release kinetics.

scholarly journals Effect of Various Excipients on Theophylline-loaded Alginate Beads Prepared by Ionic Cross Linking Technique

1970 ◽  
Vol 9 (1) ◽  
pp. 15-22 ◽  
Author(s):  
Sheikh Tasnim Jahan ◽  
Sams Mohammad Anwar Sadat ◽  
Md Saiful Islam ◽  
Reza-ul Jalil ◽  
Jakir Ahmed Chowdhury
Keyword(s):  
Polyethylene Glycol ◽  
Drug Release ◽  
Sodium Alginate ◽  
Methyl Cellulose ◽  
Alginate Beads ◽  
Cross Linking ◽  
Carboxy Methyl Cellulose ◽  
Polyethylene Glycol 4000 ◽  
Sodium Starch Glycolate ◽  
Carboxy Methyl

Theophylline loaded sodium alginate beads were prepared by ionic cross linking technique using calcium chloride (CaCl2) as cross linking agents. The purpose of this work was to prepare sodium alginate beads as a device for the extended release of theophylline. Different excipients like sodium carboxy methyl cellulose, polyethylene glycol 4000, hydroxy propyl methyl cellulose, sodium starch glycolate, Eudragit L 100 and sodium lauryl sulphate were used to fabricate theophylline-alginate beads and their effect on drug release were investigated. In this study, the beads were characterized and evaluated in respect to their surface morphology, swelling index (SI) and in-vitro release characteristics. Beads were prepared by dropping a hot aqueous theophylline-alginate or theophylline-alginate-excipient solution into electrolyte solution. Alginate cross linked with electrolytes and beads were formed with entrapped drug. Beads were collected by decanting the solution and dried at room temperature. Surface of beads with various excipients revealed that smooth, dense and closely packed drug-polymer bonding was obtained when the excipients were changed. Beads in F 1 contain Eudragit L 100 that swelled highest at 3 hours with SI of 10.74 %. Sodium starch glycolate beads (F 4) swelled high up to 9.93 % at 2 hours. Dissolution studies were carried out in 900 ml of distilled water for 8 hours. Most of the formulations were fitted to Higuchi model. The drug release rate are shown in decreasing order: Eudragit L 100>Sodium carboxy methyl cellulose> Sodium lauryl sulphate> Sodium starch glycolate>Hydroxy propyl methylcellulose 5 cps>Polyethylene glycol 4000. The use of Eudragit L 100 was found to be promising because it released about 69 % of theophylline within 8 hours. It was found that among the hydrophilic polymers used, Sodium carboxy methyl cellulose showed 49 % theophylline release within 8 hours. The lowest amount of drug release was found with HPMC 5 cps and PEG 4000 which was about 26 % of drug release. Key words: Theophylline; ionic cross-linking technique; sodium alginate beads; swelling index; release kinetics. DOI: 10.3329/dujps.v9i1.7425 Dhaka Univ. J. Pharm. Sci. 9(1): 15-22 2010 (June)

scholarly journals Muco-adhesive buccal tablets of candesartan cilexetil for oral delivery: preparation, in-vitro and ex-vivo evaluation

2021 ◽  
Vol 11 (1-s) ◽  
pp. 35-42
Author(s):  
Kumara Swamy Samanthula ◽  
Agaiah Goud Bairi ◽  
CB Mahendra Kumar
Keyword(s):  
Candesartan Cilexetil ◽  
Ex Vivo ◽  
Methyl Cellulose ◽  
Carboxy Methyl Cellulose ◽  
First Pass Metabolism ◽  
First Pass ◽  
Buccal Tablets ◽  
Pass Metabolism ◽  
Carboxy Methyl

Candesartan cilexetil (CC) is an angiotensin II-receptor blocker (ARB). The antihypertensive effect of CC 4-16 mg/day was as great as that of other once-daily dosage regimens. Candesartan cilexetil has high first-pass metabolism and low oral bioavailability. The bioavailability of such drugs may be significantly improved if delivered through the buccal route; hence mucosal delivery is one of the alternative methods of systemic drug delivery. This study’s objective was to develop mucoadhesive buccal tablets of candesartan cilexetil using carbopol-934P, hydroxyl propyl methyl cellulose (HPMC), Eudragit RLPO, and sodium carboxy methyl cellulose (Na-CMC) as mucoadhesive polymers. Prepared CC buccal tablet formulations were evaluated for an optimized system based on physicochemical properties, ex-vivo residence time, in-vitro, and ex vivo permeation studies. The evaluation parameters of the tablets were within the acceptable Pharmacopoeial limits. However, the swelling and bio-adhesive time were increased with increasing polymer concentrations. The in-vitro release research shown that buccal tablets with sodium carboxy methyl cellulose (Na-CMC) exhibited a higher release than all other formulations and have been considered as optimized CC formulation. The release mechanism from kinetic methods suggests that the drug release follows zero-order kinetics with a diffusion mechanism. Further, in-vivo research in animal fashions is required to prove the bioavailability performance of the formulation. Keywords: Candesartan cilexetil, mucoadhesive buccal tablets, first-pass metabolism, bioavailability.

scholarly journals Development and Evaluation of Indomethacin Controlled Release Press Coated Tablets

2016 ◽  
Vol 14 (2) ◽  
pp. 187-192
Author(s):  
Muhammad Rashedul Islam ◽  
Md Elias Al Mamun ◽  
Md Mizanur Rahman Moghal ◽  
Md Habibur Rahman
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Chemical Properties ◽  
Methyl Cellulose ◽  
Compression Pressure ◽  
Physico Chemical ◽  
Compression Coating ◽  
Coating Formulation ◽  
Coating Formulations

In the present work, several batches of indomethacin press coated tablets were prepared with drug and Avicel PH 102 utilizing the press coating technology. The core tablet was compression coated with minimal compression pressure. The compression coating mixture was formulated using various amount of lactose and xanthan gum which was used as the release retarding agent. Three formulations (IX-1, IX-2 and IX-3) were designed to evaluate the release profile as function of xanthan gum load. In vitro drug release testing demonstrated that the drug release was inversely proportional to the amount of xanthan gum in the coating formulations. In addition, formulation IX-2 was modified by incorporating hydroxypropyl methyl cellulose (HPMC) 15 cps into the compression coating formulation to understand their effects on drug release. The formulation was evaluated for its properties and correlated with in vitro and kinetic release studies. Incorporation of HPMC caused the highest fraction of drug to be released in the dissolution fluid. The physico-chemical properties of the excipients can be held responsible for the discrepancy in release rate of indomethacin. From kinetic analysis drug release was found to follow Higuchi mechanism for all the formulations. Overall, the study concluded that excipients present in the coating formulations make a significant impact on drug release.Dhaka Univ. J. Pharm. Sci. 14(2): 187-192, 2015 (December)

Formulation and Evaluation of Galantamine Hydrobromide Floating Matrix Tablet

2018 ◽  
Vol 8 (2) ◽  
Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Vuppula Sruthi ◽  
Damineni Saritha
Keyword(s):  
Sodium Alginate ◽  
Xanthan Gum ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Compression Technique ◽  
Weight Variation ◽  
The Matrix

The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

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