Formulation of Oral Mucoadhesive Tablets using Mucilage Isolated from Buchanania lanzan spreng Seeds

2014 ◽  
Vol 7 (2) ◽  
pp. 2494-2503
Author(s):  
Sudarshan Singh ◽  
Ayaz Ahmad ◽  
Sunil Bothara B
Keyword(s):  
Drug Delivery ◽  
Guar Gum ◽  
Physical Property ◽  
Flow Property ◽  
Relative Effect ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Microbial Count

The present study was taken to formulate and evaluate mucilage obtained from Buchanania lanzan spreng seeds (BL) belonging to family anacardiacea for oral mucoadhesive drug delivery system containing losartan potassium. Physiochemical characteristics of mucilage, such as swelling index, microbial count, viscosity, hydration capacity, flow property, and pH were studied. The mucilage was evaluated for its mucoadhesive properties in compressed tablet, containing losartan potassium. Granules were prepared by wet granulation process using polyvinylpyrrolidone as binding agent. Mucilage was used in four different concentrations i.e., 21, 42 and 55% w/w. The tablet were prepared and evaluated for its physical property. Further, in vitro dissolution and swelling index was determined. The property of bioadhesive strength of isolated mucilage was compared with Guar gum and HPMC E5LV, which was used as standard mucoadhesive agent concentration. Bioadhesive strength of the tablet was measured on the modified physical balance. Result revealed that tablets had good physiochemical properties, and drug release was retarded as concentration of mucilage was increased. The force of adhesion was obtained 0.1238N, 0.2822N, 0.5175N, 0.8679N and 0.3983N respectively for F1, F2, F3, F4 and F5. Formulations were subjected for study the effect of agitation at different rpm. Formulation showed relative effect on release of drug from formulation. All the formulations were subjected to stability studies for three months, all formulations showed stability with respect to release pattern. In conclusions, these results indicate that the seed mucilage of BL can be a suitable excipient for oral mucoadhesive drug delivery systems.  

Development of Oral Mucoadhesive Tablets of Losartan Potassium using Natural Gum from Manilkara Zapota Seeds

2013 ◽  
Vol 6 (4) ◽  
pp. 2245-2254
Author(s):  
Sudarshan Singh ◽  
Sunil B Bothara
Keyword(s):  
Guar Gum ◽  
Physical Property ◽  
Flow Property ◽  
Relative Effect ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Microbial Count ◽  
Manilkara Zapota

The present investigation reports the isolation of mucilage from Manilkara zapota seeds as per AOAC guideline and evaluating it as mucoadhesive agent. Manilkara zapota (Linn.) P. Royen syn. a small tree belonging to family sapotaceae. Physiochemical characteristics of mucilage, such as swelling index, microbial count, viscosity, hydration capacity, flow property, and pH were studied. The mucilage was evaluated for its mucoadhesive properties in compressed tablet, using losartan potassium as model drug. Granules were prepared by wet granulation process using polyvinylpirrolidone as binding agent. Mucilage was used in four different concentrations i.e. 20, 40 and 60 % w/w. The tablet were prepared and evaluated for its physical property. Further in vitro dissolution and swelling index was determined. The property of bioadhesive strength of isolated mucilage was compared with guar gum and HPMC E5LV, which was used as standard mucoadhesive agent concentration. Bioadhesive strength of the tablet was measured on the modified physical balance. Result revealed that mucilage had good micromeritcs properties and prepared tablets showed good physical properties, further drug release was retarded as concentration of mucilage was increased. The force of adhesion was obtained 0.2337N, 0.4664N, 0.6210N, 0.8679N and 0.3983N respectively for F1, F2, F3, F4 and F5. Formulations were subjected for study of effect of intensity of agitation at different rpm and electrolyte, formulation showed relative effect on release of drug from formulation. All the formulations were subjected to stability studies for three months all formulation showed stability with respect to release pattern. It is concluded that the seed mucilage of Manilkara zapota can be used as a mucoadhesive excipient in oral mucoadhesive drug delivery systems.

Formulation Development of Oral Mucoadhesive Tablets of Losartan Potassium using Mucilage Isolated from Diospyros melonoxylon Roxb Seeds

2013 ◽  
Vol 6 (3) ◽  
pp. 2154-2163
Author(s):  
Sudarshan Singh ◽  
Sunil B Bothara
Keyword(s):  
Guar Gum ◽  
Flow Property ◽  
Relative Effect ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Microbial Count ◽  
Formulation Development ◽  
Weight Variation

Diospyros melonoxylon Roxb is a small tree with rather slender stem and smooth grey bark belonging to family Ebenaceae found widely in Chhattisgarh. The present investigation reports the isolation of mucilage from Diospyros melonoxylon seeds as per AOAC guideline and evaluating it as mucoadhesive agent. Physiochemical characteristics of mucilage, such as appearance, solubility, swelling index, microbial count, loss on drying, viscosity, hydration capacity, flow property, hausner ratio and pH were studied. The mucilage was evaluated for its mucoadhesive properties in compressed tablet, using Losartan Potassium as model drug. Granules were prepared by wet granulation process using polyvinylpirroli-done as binding agent. Mucilage was used in four different concentrations i.e. 20, 40 and 60 % w/w. The prepared granules were evaluated for micrometrics property. The tablet were prepared and evaluated for weight variation, thickness diameter, hardness, percent friability, in vitro dissolution and degree of swelling. The property of bioadhesive strength of isolated mucilage was compared with Guar Gum and HPMC E5LV, which was used as standard mucoadhesive agent concentration. Bioadhesive strength of the tablet was measured on the modified physical balance. The tablets had good physiochemical properties, and drug release was retarded as concentration of mucilage was increased. The force of adhesion was obtained 0.2063N, 0.3837N, 0.5175N, 0.8679N and 0.3983N respectively for F1, F2, F3, F4 and F5. Formulations were subjected for study of effect of intensity of agitation at different rpm (50 and 150) and electrolyte (NaCl and CaCl2), and formulation showed relative effect on release of drug from formulation. All the formulations were subjected to stability studies for three months all formulation showed stability with respect to release pattern.

Formulation and Evaluation of Microbially- triggered tablets of Valdecoxib

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Surender Verma ◽  
S. Singh ◽  
D. Mishra ◽  
Atul Gupta ◽  
Rakesh Sharma
Keyword(s):  
Phosphate Buffer ◽  
Guar Gum ◽  
Oral Route ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Dissolution Study ◽  
Caecal Content ◽  
Model Drug

The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher amount of drug which was also significantly higher than the dissolution media of same pH without caecal content (microflora) and it was concluded that guar gum can be used as a potential carrier for targeting drugs to colon.

scholarly journals Applicability of Gum Karaya in the Preparation and in Vitro Evaluation of Losartan Potassium as Chronotherapeutic Drug Delivery System

2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Tensile Strength ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
Gum Karaya

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 

scholarly journals Gastroretentive drug delivery system of a lipid lowering agent

2013 ◽  
Vol 2 (9) ◽  
pp. 152-155
Author(s):  
D. Krishnarajan ◽  
N. Senthil Kumar ◽  
Rajesh Yadav
Keyword(s):  
Guar Gum ◽  
Lipid Lowering ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Natural Polymers ◽  
First Pass Metabolism ◽  
First Pass ◽  
Mucoadhesive Tablets ◽  
Pass Metabolism

The objective of this study was to develop mucoadhesive tablets of Simvastatin using natural polymers. Simvastatin has short biological half-life and high first pass metabolism hence which was designed to increase the gastric residence time which prolong the drug release. The tablets were prepared by wet granulation technique using Carbopol-934, guar gum, xanthine gum and chitosin as polymers. Formulations were evaluated for different parameters like hardness, friability, uniformity of weight, swelling characteristics, in vitro dissolution and kinetic studies. The dissolution was carried out for 12 hours in which the formulation with guar gum has shown highest dissolution release profile (F9). Thus the present study concludes that mucoadhesive tablets of simvastatin can be a good way to pass the extensive hepatic first pass metabolism and to improve the bioavailability of simvastatin.DOI: http://dx.doi.org/10.3329/icpj.v2i9.16077 International Current Pharmaceutical Journal, August 2013, 2(9): 152-155

scholarly journals FORMULATION AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF LAFUTIDINE

2018 ◽  
Vol 8 (5) ◽  
pp. 393-399
Author(s):  
Ramdas T. Dolas ◽  
Shalindra Sharma ◽  
Madhuraj Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Active Agent ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Floating Tablets

The purpose of this research was to develop a novel gastroretentive drug delivery system based on wet granulation technique for sustained delivery of active agent. Quick GI transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to decreased efficacy of the administered dose and thus less patient compliance. Gastroretentive floating tablets, which was designed to provide the desired sustained and complete release of drug for prolonged period of time. Gastroretentive floating tablets of lafutidine were prepared by wet granulation technique using different concentrations of Gum Kondagagu, Gum olibanum and Locust bean Gum. The optimized formulation (LF14) exhibited 99.54% drug release in 12 hrs, while the buoyancy lag time was 33 sec. In-vitro drug release kinetics was found to follow both the Zero order and the possible mechanism of lafutidine release from the optimized formulation might be attributed to super case II transport mechanism. The Optimized formulation (LF14) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months. Keyword: Wet granulation, Floating lag Time, Gastroretentive, Lafutidine

scholarly journals DESIGN AND DEVELOPMENT OF LOSARTAN POTASSIUM FLOATING DRUG DELIVERY SYSTEMS

2018 ◽  
Vol 10 (6) ◽  
pp. 168
Author(s):  
Prasanta Kumar Mohapatra ◽  
Ch. Prathibha ◽  
Vivek Tomer ◽  
Mandeep Kumar Gupta ◽  
Satyajit Sahoo
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Angle Of Repose ◽  
Losartan Potassium ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Dissolution Studies

Objective: The current study was projected to prepare a losartan potassium gastroretentive drug delivery system (GRDDS) of floating tablets was planned to enhance the gastric residence time, thus prolong the drug release.Methods: Effervescent floating matrix tablets of losartan potassium were prepared by direct compression technique using polymers like HPMC k4m, guar gum, and gum karaya, with lubricants magnesium stearate and talc. In the present study, sodium bicarbonate was incorporated as a gas generating agent. Total nine formulations were designed and evaluated for pre-compression parameters known as the angle of repose, bulk density, tapped density, Hausner’s ratio, compressibility index, and post-compression parameters are uniformity of weight, hardness, and drug content percentage, variability, in vitro buoyancy, dissolution studies, and Fourier transform infrared spectroscopy (FTIR).Results: An in vitro dissolution study was carried out by using buffer pH 1.2. From in vitro dissolution studies, it has been found that an increase in polymer concentration diminishes the drug release profile. The in vitro drug release percentage from F4-F9 formulations ranged from 60.28%-98.66% at the closing of 12 h and buoyancy found over 12 h.Conclusion: The in vitro drug release from F1-F3 and F7-F9 followed zero-order, F4 followed Higuchi order, F5 and F6 followed Hixon-Crowell release kinetics. The drug release mechanism was set up to be F1-F8 non-Fickian (anomalous behavior) and F9 having Fickian diffusion type.

scholarly journals Formulation and In Vitro Evaluation of Compressed Coated Tablets of Simvastatin for Pulsatile Drug Delivery

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Kumari P.V. Kamala ◽  
Mounica V. ◽  
Rao Y. Srinivasa
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Guar Gum ◽  
Lag Time ◽  
Blood Cholesterol ◽  
In Vitro Dissolution ◽  
Pulsatile Drug Delivery

Pulsatile drug delivery system is one type of drug delivery system, where the delivery device is capable of releasing drugs after a predetermined time-delay (i.e. lag time). This system has a peculiar mechanism of delivering the drug rapidly and completely after a "lag time," i.e., a period of "no drug release." These systems are beneficial for drugs having high first-pass effect drugs administered for diseases that follow chrono pharmacological behavior such as drugs having specific absorption sites in GIT, targeting to colon; and cases where nighttime dosing is required. The objective of the present study was to formulate and evaluate a press coated pulsatile drug delivery system of simvastatin in order to attain a time controlled release to lower the blood cholesterol level by releasing the drug with a distinct predetermined lag time of five hrs. Simvastatin is a water insoluble drug and its absorption is dissolution rate limited. The core formulations were composed of simvastatin and disintegrants like lycoat, SSG, ludiflash in different ratios and was coated with xanthan gum, guar gum, HPMC K4M, HPMC K15M as a release modifier. Press coated tablets were evaluated for hardness, friability, drug content, and in vitro drug release. Result of in vitro dissolution study of the prepared tablet suggested that, the release of drug from press coated tablets match with chrono-biological requirement of disease.

scholarly journals Development and evaluation of sustained release matrix tablets of losartan potassium

2016 ◽  
Vol 1 (04) ◽  
pp. 127-132
Author(s):  
V. Viswanath ◽  
U. Chandrasekhar ◽  
B. Narasimha Rao ◽  
K. Gnana Prakash
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Wet Granulation ◽  
Natural Polymers ◽  
Hypertensive Drug

The objective of the present study was to develop a sustained release matrix tablets of Losartan potassium, an anti hypertensive drug. The sustained release tablets were prepared by wet granulation and formulated using different drug and polymer ratios. Hydrophilic natural polymers like xanthan Gum (XG), guar gum and cellulose were used. Compatibility of the drug with various excipients was studied. The compressed tablets were evaluated and showed compliance with Pharmacopoeial limits. Formulation was optimized (F2) on the basis of acceptable tablet properties and in vitro drug release. The resulting formulation produced matrix tablets with optimum hardness, consistent weight uniformity and friability. All tablets but one exhibited gradual and near completion sustained release for losartan potassium and 90.88% released at the end of 12h. The results of dissolution studies indicated that formulation F2 (drug to polymer 1:2) is the most successful of the study and exhibited drug release pattern very close to theoretical release profile. A decrease in release kinetics of the drug was observed on increasing polymer ratio. Applying exponential equation, all the formulation tablets (except F2) showed diffusion-dominated drug release. The mechanism of drug release from F2 was diffusion coupled with erosion.

Development and In‑Vitro Evaluation of Colon Specific Indomethacin Matrix Tablet for the Treatment of Inflammatory Bowel Disease

2021 ◽  
pp. 2391-2396
Author(s):  
Rohitas Deshmukh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Guar Gum ◽  
Fasting Blood Glucose ◽  
Chronic Inflammatory Disease ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Drug Release Profile ◽  
Weight Variation

IBD is a chronic inflammatory disease of the gastrointestinal tract, particularly small and large intestine consisting of ulcerative colitis (UC) and Crohn’s disease (CD). Oral route of drug delivery is considered as the most appropriate route of drug delivery of drugs. But this route has certain limitations of poor bioavailability due to gastric degradation and increase in dose size and frequency. Therefore, the present aim of the study is to prepare and evaluate Indomethacin loaded matrix tablet using guar gum, HPMC (release controlling polymer) and citric acid to facilitate the drug solubility in the colon. A total 8 different formulations were prepared by wet granulation method and coated with Eudragit S 100 polymer a pH dependent enteric coating polymer which dissolve at colonic pH (7.4) and specifically release the drug in the colon region in sustain release fashion. The granules evaluated for its micrometrics properties and tablets were evaluated for its hardness, thickness, friability, weight variation, drug content, and in‑vitro drug release studies. The % cumulative drug release profile of all tablets was little and insignificant at pH 1.2 and 6.8. In colonic pH the coating dissolves tablets starts to release drugs. Among all the formulation the formulation F3 having guar gum and HPMC ratio 3:1 shows a maximum release of drug of 80.41±6.5%. At 24 h. The study demonstrated that the prepared tablets can release the Indomethacin in sustained release manner and helps in management of IBD with reduced side effect of the therapy. The results of this study show that oral administration of aspartame (250mg/kg body weight) was correlated to a significant increase in the lipid profile, fasting blood glucose and some marker enzymes and this increase is time related.

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