Fabrication of Enteric Release Tablet without Coating Process by Using Bleached Shellac

2019 ◽  
Vol 819 ◽  
pp. 33-37
Author(s):  
Manee Luangtana-anan ◽  
Sontaya Limmatvapirat ◽  
Suthep Saengsod
Keyword(s):  
Gastrointestinal Tract ◽  
Wet Granulation ◽  
Coating Process ◽  
Binding Agent ◽  
Property A ◽  
Salt Form ◽  
Simple Method ◽  
Model Drug ◽  
Bleached Shellac ◽  
Release Tablet

The purpose of this study was to design an enteric release tablet by a simple method of tableting and avoiding the coating process. Polymers which had a protection ability against acid were required for tablet formulation. Bleached shellac was selected as an excipient due to colorless property, a protection ability against acid in upper gastrointestinal tract and release ability in lower gastrointestinal tract. Bleached shellacs in salt and acid forms were dissolved in 12 ml of 95% ethanol and used as a binding agent to get a concentration of 5, 7.5, 10, 12.5, 15, 17.5 and 20 %w/w of total formulation. 60% lactose, 30% Avicel pH 102 and 10% paracetamol (model drug) were mixed and tablets were prepared by wet granulation method with the weight of 550 mg and hardness of 8-10 kg. The tablets were evaluated for their disintegration and drug release at pH 1.2 and 6.8 and kept at 40 °C, 75%RH for 6 months. The findings showed that the disintegration and amount of release were dependent on type and concentration of bleached shellac. Only the bleached shellac in salt form could protect the release of drug at pH 1.2 for 2 h and could release completely at pH 6.8 but not in acid form. After 6 months of storage, 15% bleached shellac in salt form could still protect against acid and complete release at pH 6.8 for 4 h. Although the bleached shellac showed protection ability against acid, it could not comply with the required criteria of enteric release tablet. Further study is hence required. However, the stability test of tablets prepared with bleached shellacs in salt form could show protection against acid and complete release at pH 6.8 after 6 months of storage. Bleached shellacs in salt form as a binding agent showed a good approach for the fabrication of enteric release tablets without coating process by using a proper concentration of bleached shellac. Therefore, the attempt to design an enteric tablet by a simple method and avoiding the coating process is achieved.

Exploration of Neem Gum, Acrylamide Grafted Neem Gum and Carboxymethylated Neem Gum as Retardant in Tablet Formulation

2020 ◽  
Vol 16 (9) ◽  
pp. 1404-1410
Author(s):  
Rishabha Malviya
Keyword(s):  
Diclofenac Sodium ◽  
Tablet Formulation ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Binding Agent ◽  
Grafted Polymer ◽  
Model Drug ◽  
Tablet Dosage ◽  
Tapped Density ◽  
Derivatives Of

Background: In the previous study, investigators have synthesized acrylamide grafted and carboxymethylated derivatives of neem gum and evaluated their potential in the formulation of nanoparticles. In continuation of previous work, authors have evaluated neem gum polysaccharide (NGP), acrylamide grafted neem gum polysaccharide (NGP-g-Am) and carboxymethylated neem gum polysaccharide (CMNGP) as binding agent in the tablet dosage form. Methods: Diclofenac sodium was used as a model drug while microcrystalline cellulose and talc were used as excipient in the preparation of granules employing wet granulation technique. NGP, NGP-g-Am and CMNGP were utilized as binding agent in the preparation of granules. Prepared granules were characterized for various pre-compression and post-compression parameters. Results and Discussion: Binding agents were used in the concentration of 4-24%w/w. NGP incorporated granules showed more bulk density and lower values of tapped density, Carr’s index, bulkiness, Hausner’s ratio and angle of repose as compared to NGP-g-Am consisting granules. NGP-g-Am consisting tablets showed more hardness and zero friability as compared to NGP based tablets. Drug content was found lower for the tablets having grafted polymer in place of NGP. CMNGP were also utilized to prepare granules but granules were not be able to compress keeping all the compacting parameters same as used in the case of NGP and NGP-g-Am consisting granules. NGP and NGP-g-Am were able to sustain drug release up to 6 and 8 h, respectively. Conclusion: It can be concluded that NGP-g-Am induces better properties when used as a binder in the tablet formulation than native polymer, while CMNGP cannot be utilized as a binding agent in the preparation of a tablet.

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.

Preparation and Evaluation of a Gas Formation-based Multiple-Unit Gastro-Retentive Floating Delivery System of Dipyridamole

2012 ◽  
Vol 5 (1) ◽  
pp. 1607-1616
Author(s):  
Y. Madhusudan Rao ◽  
Katakam V V ◽  
S Reddy ◽  
J M Somagoni ◽  
P K Panakanti ◽  
...  
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Polymeric Membrane ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Gastric Residence Time ◽  
Gas Formation ◽  
Multiple Unit ◽  
Model Drug

The aim of this study was to prepare mini tablets to be filled into a capsule that is designed to float on the gastric contents based on gas formation technique. The drug-containing core mini-tablets were prepared by wet granulation method followed by a coating of the core units with seal coating, an effervescent layer and a gas-entrapping polymeric membrane (Eudragit RS30D, RL30D). Dipyridamole, which is predominantly absorbed in the upper part of GI tract and unabsorbed/insoluble at the lower intestine, was used as a model drug. The effect of the preparative parameters like amount of the effervescent agent layered onto the seal coated units, type and coating level of the gas-entrapping polymeric membrane, floating ability and drug release properties of the multiple-unit FDDS were evaluated. The formulations were evaluated for pharmacopoeial quality control tests. Physical parameters were found to be within the acceptable limits. The system using Eudragit® RL30D as a gas-entrapping polymeric membrane exhibited floating properties. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapping polymeric membrane decreased. The optimum system exhibited complete floating within 3 minutes and maintained that buoyancy over a period of 8 hours. The drug release was sustained and linear with the square root of time. Increasing the coating level of the gas-entrapping polymeric membrane decreased drug release. Both the rapid-floating and sustained-release properties were achieved in the multiple-unit floating delivery system developed in this study. The in vivo gastric residence time was examined by radiograms and it was found that the units remained in the stomach for about 6 hours. The analysis of the dissolution data after storage at 40°C and 75% RH for 6 months showed no significant change indicating good stability.

scholarly journals Extraction and Evaluation of Lepidium Sativum and Flax Seeds Mucilage as a Pharmaceutical Granulation Binder

2021 ◽  
Author(s):  
Nagla Algali Layas
Keyword(s):  
Physical Properties ◽  
Angle Of Repose ◽  
Lepidium Sativum ◽  
Wet Granulation ◽  
Binding Agent ◽  
Flax Seeds ◽  
Good Flow

The powders holdtogether by a binder to form granule. Some excipients of natural origins arecurrently available as an alternative over the synthetic ones in pharmaceuticalformulation. The aim of this study was to isolate the mucilage from differentplant seeds and compare them to evaluate the binding effects. In present studyan effort was made to investigate the efficacy of mucilage obtained from Lepidiumsativum and flax seeds as granules excipient. The mucilage   was extracted from selected seeds byconventional method by precipitation of soaked and blended seeds in acetone.The dried mucilages were subjected to several phytochemical and physicochemicalproperties. Granules were formulated by wet granulation method by usingextracted mucilage as a binding agent and comparison was made against thegranules prepared with standard binder as PVP. The granules evaluated byvarious physical properties such as (bulk and tapped densities, Hausner’sratio, Carr’s index, angle of repose and friability). The results showed thatthe granules prepared from extracted mucilage as a binder had good flow andmechanical properties, all evaluated parameters were within the permissiblelimits. Thus, mucilage could be used as an alternative binding agent in pharmaceuticalgranules.

Preparation and Evaluation of Ternary Polymeric Blends for Controlled Release Matrices Containing Weakly Basic Model Drug

2020 ◽  
Vol 17 ◽  
Author(s):  
Wasfy M. Obeidat ◽  
Shadi F. Gharaibeh ◽  
Abdolelah A. Jaradat ◽  
Osama Abualsuod
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Sodium Alginate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Sustained Drug Release ◽  
Basic Drug ◽  
Basic Model ◽  
Polymeric Compositions ◽  
Model Drug

Objective: The objective of this study was to evaluate the suitability of ternary mixture of smart polymers comprised of Eudragit®E100, Eudragit®L100, and sodium alginate to serve as a carrier for sustained drug release for weakly basic drugs. The model drug chosen in this part of the study is Metronidazole. Methods: Matrix tablets formulations were prepared by either direct compression or by wet granulation. Dissolution studies were conducted using USP XXΠ rotating paddle apparatus in three different consecutive stages (pH 1.2, 4.8 and 6.8). Tablets made of low to intermediate proportions of sodium alginate and an approximately equal proportions of Eudragit®E100 and Eudragit®L100 were found to have significant modification of drug release rates. Result: Thus, indicating a potential for controlling the drug release for 12 hours depending on polymers ratios in the formulation. The ratio of sodium alginate to total Eudragit® polymers and the ratio of Eudragit®E100 to Eudragit®L100 within the ternary polymeric composition were found critical in determining the controlled release performance. Conclusion: Results of swelling studies were in agreement with the dissolution behaviors of the tablets. The findings suggest the significance of the ternary polymeric compositions in controlling the release of weakly basic drug.

Nondestructive measurement of striation defect spacing using laser diffraction

2001 ◽  
Vol 16 (12) ◽  
pp. 3355-3360 ◽  
Author(s):  
Dylan E. Haas ◽  
Dunbar P. Birnie
Keyword(s):  
Spin Coating ◽  
Laser Light ◽  
Laser Diffraction ◽  
Thickness Variation ◽  
Coating Process ◽  
Defect Structures ◽  
Nondestructive Measurement ◽  
Simple Method ◽  
Striation Spacing ◽  
Diffraction Angle

A simple method is presented for measuring the characteristic spacing between striation defects that sometimes develop when coatings are deposited by the spin-coating process. Striation defects, because of their substantial regularity of thickness variation, are able to diffract laser light. By measuring the diffraction angle, it is possible to determine a characteristic spacing that corresponds to the most dominant spatial frequency for the striation defects that have formed. This diffraction technique is compared with other methods for determining the average striation spacing. This noncontact characterization technique may also be applicable to other regularly or quasi-regularly spaced defect structures that appear in coatings or other materials. The limits and accuracy of this technique are discussed in detail.

A New Approach for Study of pH- Solubility Profile of Bleached Shellac Film by Drop Shape Analysis

2014 ◽  
Vol 1060 ◽  
pp. 141-144 ◽  
Author(s):  
S. Saengsod ◽  
Manee Luangtana-Anan
Keyword(s):  
Contact Angle ◽  
Shape Analysis ◽  
Contact Line ◽  
Buffer Solution ◽  
Simple Method ◽  
Drop Shape ◽  
Solubility Profile ◽  
Angle Method ◽  
Bleached Shellac

The aim of this study was to apply contact angle method for the determination of the pH solubility profile of bleached shellac film. Various pH of buffer solution was dropped on the bleached shellac film and drop shape analysis was investigated. The changes in the contact angle and contact line were recorded during 10-min measurement. The graphs of change in slope –obtained from plot between contact angle and time-and % change in contact line were plotted against various pH. The results illustrated the slight change in slope and % change in contact line at low pH while the significant change was reported at high pH. The results were in agreement with % dissolved film at various pH. The bleached shellac film started to dissolve at pH 7. The higher % dissolved film was obtained at pH 8 and 9 and at pH 10 was completely dissolved. Therefore, the contact angle method by the drop shape analysis, a simple method and less solvent used, can be an indicator for determination of pH solubility profile of bleached shellac. The result obtained could then be applied to the other substances.

scholarly journals Mechanistic PBPK Modelling to Predict the Advantage of the Salt Form of a Drug When Dosed with Acid Reducing Agents

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1169
Author(s):  
Siri Kalyan Chirumamilla ◽  
Venkatesh Teja Banala ◽  
Masoud Jamei ◽  
David B. Turner
Keyword(s):  
Pbpk Model ◽  
Immediate Release ◽  
Reducing Agents ◽  
Free Base ◽  
Salt Form ◽  
Pbpk Modelling ◽  
Release Formulation ◽  
Drug Products ◽  
Model Drug ◽  
The Impact

Acid reducing agents (ARAs) reduce the dissolution rate of weakly basic drugs in the stomach potentially leading to lower bioavailability. Formulating the API as a rapidly dissolving salt is one strategy employed to reduce the impact of ARAs on dissolution of such drugs. In the present work, a model drug was selected with an immediate release formulation of the free base dosed in both the absence and presence of the ARA famotidine. In the latter case, bioavailability is restricted and several salt formulations were investigated. To simulate these drug products a mechanistic physiologically based pharmacokinetic (PBPK) model was built using the Simcyp Simulator, which illustrates the advantage of formulating an API as a salt compared to the free base form. The simulations use a mechanistic salt model utilising knowledge of the solubility product which was applied to predict the salt advantage. The developed PBPK model exemplifies that it can be critical to account for the surface pH and solubility when modelling the dissolution of low pKa bases and their salts in the gastric environment. In particular, the mechanistic salt model can be used to aid in screening and salt form selection where the aim is to mitigate effects of ARAs.

EVALUATION OF TRIBULUS TERRESTRIS MUCILAGE AS BINDER IN TABLET FORMULATIONS

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (07) ◽  
pp. 10-17
Author(s):  
V. A Arsul ◽  
◽  
S. Lahoti ◽  
P. K Sharma ◽  
B. Shrivastava
Keyword(s):  
Guar Gum ◽  
Chemical Interaction ◽  
Wet Granulation ◽  
Content Uniformity ◽  
Tribulus Terrestris ◽  
Stability Studies ◽  
Granulation Process ◽  
Ich Guidelines ◽  
Tablet Formulations ◽  
Model Drug

The aim of this study is to develop an economic and effective natural excipient that can be used as an alternative in formulation of tablets. Tribulus terrestris (Zygophyllaceae) is a herbaceous weed native throughout India and mucilage is derived from the freshly dried and coarsely powdered leaves. phytochemical and physiochemical characteristics of mucilage were studied. Mucilage was used in 5 different concentrations (10, 15, 20, 25, and 30% w/V). Metoprolol tartrate was used as model drug for formulation. The DSC and FTIR of drug and mucilage indicate no chemical interaction. The properties were compared with guar gum (GRAS excipient). The granules were prepared by wet granulation process and evaluated. Tablets were prepared and evaluated for disintegration, dissolution and content uniformity and was subjected to stability studies as per ICH guidelines. It was concluded that lower concentration of mucilage can be used as binder. The higher concentration shows sustained release and can be considered as alternative release retardant.

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