scholarly journals Carboxymethylation of Karaya gum: application in gastroretentive drug delivery for sustained release of model drug

2020 ◽  
pp. 300-306
Author(s):  
Amit Verma ◽  
Neetu Sachan ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Aqueous Solubility ◽  
Dosage Forms ◽  
Dissolution Medium ◽  
Propranolol Hcl ◽  
Model Drug ◽  
Karaya Gum ◽  
Ether Synthesis ◽  
Acidic Dissolution

Karaya gum (KG) is one of the least soluble of the gums. It does not dissolve in water to give a clear solution but instead absorbs water rapidly to form viscous colloidal sols. Carboxymethylation of Karaya gum is expected to improve its aqueous solubility and gelling behavior. Another objective of the research is to evaluate the potential of carboxymethylated Karaya gum (CMKG) as drug release modulator (in acidic dissolution medium) when combined with HPMC K15M based polymeric matrices bearing Propranolol HCl. In the present study, KG was carboxymethylated using Williamson Ether synthesis. FTIR spectroscopy confirmed the formation of CMKG. The prepared CMKG was used in conjunction with HPMC K15M as a polymer matrix in the formulation capsule dosage form, using Propranolol HCl as model drug. The filled capsules were then coated with Gelucire 43/01 to convert them into hydrodynamically balanced (HBS) capsule dosage form. Dextrose & fructose were also added to the drug-polymer mix as osmogen to facilitate the drug release. The degree of substitution of CMKG was found to be 0.87. HBS capsule dosage forms remained buoyant on 0.1 HCl for up to 6 hr, the buoyancy was attributed to the Gelucire 43/01 coating around the capsule shell. From the experimentation it was observed that CMKG, when mixed with HPMC K15M at 1:3 ratios, extended the release of model drug from HBS capsule dosage forms in 0.1 HCl. At CMKG: HPMC K15M ratio 2:1, release of Propranolol Hydrochloride from hydrodynamically balanced (HBS) capsules revealed fast drug release in 0.1 HCl. From the observations it is evident that KG is amenable to carboxymethylation to form CMKG. It is also evident that it is advantageous to combine CMKG with HPMC K15M as release modulator to retard the release of Propranolol HCl in acidic dissolution medium.

scholarly journals Embedded 3D Printing of Novel Bespoke Soft Dosage Form Concept for Pediatrics

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 630 ◽  
Author(s):  
Katarzyna Rycerz ◽  
Krzysztof Adam Stepien ◽  
Marta Czapiewska ◽  
Basel T. Arafat ◽  
Rober Habashy ◽  
...  
Keyword(s):  
Dosage Form ◽  
Drug Loading ◽  
Three Dimensional ◽  
Dosage Forms ◽  
Dose Titration ◽  
Step Method ◽  
Needle Size ◽  
Model Drug ◽  
Semi Solid ◽  
The Impact

Embedded three-dimensional printing (e-3DP) is an emerging method for additive manufacturing where semi-solid materials are extruded within a solidifying liquid matrix. Here, we present the first example of employing e-3DP in the pharmaceutical field and demonstrate the fabrication of bespoke chewable dosage forms with dual drug loading for potential use in pediatrics. LegoTM-like chewable bricks made of edible soft material (gelatin-based matrix) were produced by directly extruding novel printing patterns of model drug ink (embedded phase) into a liquid gelatin-based matrix (embedding phase) at an elevated temperature (70 °C) to then solidify at room temperature. Dose titration of the two model drugs (paracetamol and ibuprofen) was possible by using specially designed printing patterns of the embedded phase to produce varying doses. A linearity [R2 = 0.9804 (paracetamol) and 0.9976 (ibuprofen)] was achieved between percentage of completion of printing patterns and achieved doses using a multi-step method. The impact of embedded phase rheological behavior, the printing speed and the needle size of the embedded phase were examined. Owning to their appearance, modular nature, ease of personalizing dose and geometry, and tailoring and potential inclusion of various materials, this new dosage form concept holds a substantial promise for novel dosage forms in pediatrics.

scholarly journals Formulation, in vitro characterization and optimization of taste-masked orally disintegrating co-trimoxazole tablet by direct compression

PLoS ONE ◽  
2021 ◽  
Vol 16 (3) ◽  
pp. e0246648
Author(s):  
Chernet Tafere ◽  
Zewdu Yilma ◽  
Solomon Abrha ◽  
Adane Yehualaw
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Dosage Forms ◽  
Taste Masking ◽  
Direct Compression ◽  
Improve Patient Compliance ◽  
Preliminary Study ◽  
Improve Patient ◽  
Central Composite

Introduction Orally disintegrating tablet (ODT) is a dosage form that overcomes the problem of swallowing which is prevalent in about 35% of the general population. Co-trimoxazole (CTX) is given for patients with HIV for the prophylaxis of opportunistic infection (OI), commonly for pneumocystis carinii pneumonia. It was reported that CTX was associated with a 25–46% reduction in mortality among individuals infected with HIV in sub-Saharan Africa. Esophageal candidiasis which usually comes along with HIV/AIDS is one of AIDS defining illness affecting up to 1 in 5 of people with AIDS. This opportunistic illness is manifested by painful or difficulty of swallowing. In this respect, CTX ODT offer the advantages of both liquid dosage forms in terms of easy swallowing thereby improve patient compliance and solid dosage forms in terms of dose uniformity, stability, lower production, and transportation costs. The objective of this study was to formulate, characterize and optimize CTX ODT which could overcome swallowing problem and improve patient compliance. Co-trimoxazole ODTs were prepared by direct compression technique using a semi synthetic super disintegrant (crospovidone) along with other excipients. Two taste masking techniques were employed, addition of sweetening agent, and solid dispersion by using a pH sensitive polymer, Eudragit E-100 at different ratios (1:1, 1:2 and 1:3). Taste masking was determined by comparing taste threshold value and in vitro drug release. Preliminary study was used to investigate the effect of crospovidone, compression force (CF) and Hydroxypropyl cellulose (HPC) on disintegration time, friability and wetting time (WT). Factorial design was used as it enables simultaneous evaluation of formulation variables and their interaction effect. From the preliminary study, the factors that were found significant were further optimized using central composite design. Design-Expert 8.0.7.1 software was employed to carry out the experimental design. The bitterness threshold concentration of Trimethoprim was found to be 150 μg/ml and the in vitro drug release of the three batches of drug to polymer ratio (F1:1, 1:2 and 1:3) was 2.80±0.05, 2.77±0.00 and 2.63±0.00 respectively. From the optimization study, the optimal concentration for the superdisintegrant was 8.60% w/w and a CF of 11.25 KN which gave a rapid disintegration and WT of 13.79 and 23.19 seconds respectively and a friability of 0.666%. Conclusion In this study, co-trimoxazole ODT was formulated successfully. Central composite design was effectively used to model and optimize friability, DT and WT. The method was found effective for estimating the effect of independent variables on the dependent variables by using polynomial equation and surface plots. Optimization of the response variables was possible by using both numerical and graphical optimization and the predicted optimal conditions were confirmed experimentally and were found to be in good agreement within 5% of the predicted responses. The results of the study showed that CTX ODT had significantly rapid disintegration, less than 1% friability and enhanced dissolution profiles. The successful formulation of CTX ODT can solve difficulty of swallowing of conventional tablets for some group of patients which are unable to swallow solid oral dosage form.

scholarly journals DEVELOPMENT, CHARACTERIZATION AND EVALUATION OF SOFT ORAL EDIBLE GEL USING GELLAN GUM

2017 ◽  
Vol 9 (5) ◽  
pp. 73
Author(s):  
Vijayanand P ◽  
Deepa A. ◽  
Bhagavan Raju M.
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Sodium Citrate ◽  
Task Force ◽  
Research Work ◽  
Gelation Time ◽  
Gellan Gum ◽  
Gelling Agent ◽  
Model Drug ◽  
Dysphagic Patients

Objective: The objective of present research work was to formulate and evaluate a novel oral edible gel dosage form using gellan gum as gelling agent and carvedilol as a model drug to ease the administration to dysphagic and geriatric patients.Methods: Oral edible gels were prepared using gelling agent low acetylated gellan gum and sodium citrate in different concentrations. The prepared edible gel formulations were evaluated for gelation time, appearance, texture, viscosity, pH, syneresis, drug-excipient compatibility studies by fourier transform infrared FTIR and percentage of drug release from the gel formulation.Results: Formulation containing gellan gum (0.4 % w/v) and sodium citrate (0.3 % w/v)) was found to be “spoon thick” in consistency that is accepted for dysphagic patients as per national dysphagia diet task force. This formulation showed more than 95 % drug release within 12 min and found to be stable for 6 mo. All other parameters tested were optimal. Hence, this formulation was considered optimized.Conclusion: From this study, it can be concluded that the novel edible gel dosage form containing Carvedilol can be formulated and this dosage form may prove to be more efficacious in the treatment of hypertension in dysphagic patients.

scholarly journals Development of Film Dosage Form Containing Allopurinol for Prevention and Treatment of Oral Mucositis

2012 ◽  
Vol 2012 ◽  
pp. 1-5 ◽  
Author(s):  
Yoshifumi Murata ◽  
Kyoko Kofuji ◽  
Norihisa Nishida ◽  
Ryosei Kamaguchi
Keyword(s):  
Oral Cavity ◽  
Cancer Patients ◽  
Dosage Form ◽  
Physiological Saline ◽  
Dosage Forms ◽  
Release Profile ◽  
Water Soluble ◽  
Dissolution Medium ◽  
Casting Method ◽  
Prevention And Treatment

Film dosage forms (FDs) containing allopurinol (AP) were prepared using a casting method with water-soluble polysaccharides, such as sodium alginate (ALG), and the release profile of AP from FDs was investigated in limited dissolution medium. Some ALGs were able to form FDs incorporating AP, and the thickness was about 50 μm. All FDs were easy to handle, though the rheological properties varied with ALG species. AP was homogenously present throughout the FDs and was released with disintegration in 10 mL of physiological saline. These results confirmed that FDs are useful for preventing or treating localized problems in the oral cavity, such as mucositis. FDs are also useful for administering drugs to cancer patients receiving chemotherapy and/or radiotherapy.

scholarly journals Development, characterization and solubility enhancement of BCS class II drug phenytoin by solid phospholipid dispersion technique

2020 ◽  
Vol 11 (1) ◽  
pp. 403-410
Author(s):  
Veera Venkata Satyanarayana Reddy Karri ◽  
Sathish Ananthan ◽  
Lavanya Mude
Keyword(s):  
Freeze Drying ◽  
Dosage Form ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Oral Dosage ◽  
Bcs Class Ii ◽  
The Poor ◽  
Phospholipid Nanoparticles ◽  
Model Drug ◽  
Form Development

The poor aqueous solubility acts as a core challenge in oral dosage form development for BCS class II drugs. Phenytoin is taking as a model drug; the present study adopted an innovative solid phospholipid nanoparticle (SPLN) line of attack, and it is parallelly equated with the industrialized methods (freeze-drying) which are used for the boosting of solubility and dissolution of Phenytoin. Phenytoin was articulated along with phospholipid and mannitol at a diverse ratio of phenytoin, PL, mannitol, in which 1:12:18 was the correct ratio for ideal preparation. Freeze-drying helps to prepare SPLNs in orbicular shape, which is amorphous in nature with ≤ 1µm diameter on average. While the amorphous matrix-like structure of solid phospholipid dispersion with larger particle size is obtained by freeze-drying technique. Formulating the formulation from this method improved the dissolution rate in a remarkable way. Tris buffer with pH 7.4acts as an apparent solubility dissolved concentration of phenytoin. The poor aqueous solubility acts as a core challenge in oral dosage form development for BCS class II drugs. The decrease in the particle size or cumulating the drug surface area is the widely used practices to proliferate the solubility. The target of the present work was improvisation in solubility, dissolution of a poorly water-soluble drug, and its release by using solid phospholipid nanoparticles. Phenytoin is taking as a model drug. The solid phospholipid nanoparticles were primed by freeze-drying technique along with phospholipid and mannitol in diverse drug to excipients ratios (1:1, 1:2w: w). These preparations were assessed for compatibility study using FTIR, solubility enhancement study by XRD, entrapment efficiency, surface morphology by SEM, and in-vitro release study. As per the results, there is no influence of the excipients on the drug used. The solubility was increased by folds compared to in house prepared formulation. 

The Effect of Different Superdisintegrants and their Concentrations on the Dissolution of Topiramate Immediate Release Tablets

2009 ◽  
Vol 2 (2) ◽  
pp. 531-5366
Author(s):  
V A. Vamshi Priya ◽  
G. Chandra Sekhara Rao ◽  
D. Srinivas Reddy ◽  
V. Prabhakar Reddy
Keyword(s):  
Immediate Release ◽  
Drug Dissolution ◽  
Dissolution Profile ◽  
Dissolution Medium ◽  
Lactose Monohydrate ◽  
Sodium Starch Glycolate ◽  
Tablet Disintegration ◽  
Croscarmellose Sodium ◽  
Model Drug ◽  
Usp Apparatus

The purpose of this study was to investigate the efficiency of superdisintegrants: sodium starch glycolate, croscarmellose sodium and crospovidone in promoting tablet disintegration and drug dissolution of Topiramate immediate release tablets. The efficiency of superdisintegrants was tested, by considering four concentrations, viz., like 2%, 3%, 4% and 5% in the formulations. The dissolution was carried out in USP apparatus II at 50 rpm with distilled water as a dissolution medium. The dissolution rate of the model drug topiramate was found highly dependent on the tablet disintegration, on the particle size of the superdisintegrant, on the solubility of the drug and also on the type of superdisintegrant in the dissolution medium. There was no effect of the diluent (Lactose monohydrate) on the disintegration of different concentrations of superdisintegrants. These results suggest that, as determined by the f2 metric (similarity factor), the dissolution profile of the formulation containing 4% sodium starch glycolate and lactose monohydrate as a diluent was similar to that of a marketed product.

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.

Spectrophotometric Determination of Alendronate Sodium by using Sodium-1,2-Naphthoquinone-4-Sulphonate

2012 ◽  
Vol 4 (4) ◽  
pp. 1563-1568
Author(s):  
Sagar Suman Panda ◽  
Ravi Kumar B V V ◽  
D Patanaik
Keyword(s):  
Spectrophotometric Method ◽  
Absorption Maximum ◽  
Dosage Form ◽  
Dosage Forms ◽  
Alendronate Sodium ◽  
Colored Complex ◽  
Pharmaceutical Dosage Forms ◽  
Recovery Study ◽  
Assay Conditions

A simple, precise and accurate spectrophotometric method was developed for analysis of the osteoporesis drug alendronate sodium (ALS). The method is based on reaction of the drug with sodium-1,2-naphthoquinone-4-sulphonate (NQS) in presence of alkali to form a brown colored complex giving absorption maximum at 525 nm. The drug obeyed Beer’s law in the range of 5-70 µg/ml with a correlation coefficient of 0.999. The LOD and LOQ values are 1.7 µg/ml and 5.0 µg/ml, respectively. The average recoveries for recovery study were found to be in the range of 99.37%-100.46%. The R.S.D. values for intraday and inter-day precision were found to be 0.48 and 0.62, respectively. The optimized assay conditions were applied successfully for determination of ALS in pharmaceutical dosage forms. No interference was observed from the excipients present in the dosage form. The method is statistically validated as per the ICH requirements.  

Development of Innovative Orally Fast Disintegrating Film Dosage Forms: A Review

2012 ◽  
Vol 5 (2) ◽  
pp. 1666-1674 ◽  
Author(s):  
Bibhu Prasad Panda ◽  
N.S Dey ◽  
M.E.B. Rao
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Dosage Form ◽  
Geriatric Patients ◽  
Dosage Forms ◽  
Delivery Systems ◽  
Design And Development ◽  
Innovative Drug ◽  
Potential Benefits ◽  
Pharmaceutical Industries

Over the past few decades, there has been an increased interest for innovative drug delivery systems to improve safety, efficacy and patient compliance, thereby increasing the product patent life cycle. The discovery and development of new chemical entities is not only an expensive but also time consuming affair. Hence the pharmaceutical industries are focusing on the design and development of innovative drug delivery systems for existing drugs. One such delivery system is the fast disintegrating oral film, which has gained popularity among pediatric and geriatric patients. This fast disintegrating film with many potential benefits of a fast disintegrating tablet but devoid of friability and risk of choking is more acceptable to pediatric and geriatric patients. Formulation of fast disintegrating film can be achieved by various techniques, but common methods of preparation include spraying and casting. These film forming techniques use hydrophilic film former in combination with suitable excipients, which allow the film to disintegrate or dissolve quickly in the mouth within a few seconds without the administration of water. In view of the advantages of the fast disintegrating films over the fast disintegrating tablets and other dosage forms, it has the potential for commercial exploitation. The oral film dosage form not only has certain advantages of other fast disintegrating systems but also satisfies the unmet needs of the market. The present review emphasizes on the potential benefits, design and development of robust, stable, and innovative orally fast- disintegrating films and their future scenarios on a global market as a pharmaceutical dosage form.  

An Overview of Excipients Classification and Their Use in Pharmaceuticals

2020 ◽  
Vol 16 ◽  
Author(s):  
Cansel Kose Ozkan ◽  
Ozgur Esim ◽  
Ayhan Savaser ◽  
Yalcin Ozkan
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Dosage Form ◽  
Dosage Forms ◽  
Design Development ◽  
Pharmaceutical Dosage Form ◽  
Pharmaceutical Dosage Forms ◽  
Product Identification ◽  
Direct Administration ◽  
Active Substances

: The content and the application of pharmaceutical dosage forms must meet several basic requirements to ensure and maintain efficiency, safety and quality. A large number of active substances have limited ability to direct administration. Excipients are generally used to overcome the limitation of direct administration of these active substances. However, the function, behavior and composition of the excipients need to be well known in the design, development and production of pharmaceutical dosage forms. In this review, excipients used to assist in any pharmaceutical dosage form production processes of drugs, to preserve, promote or increase stability, bioavailability and patient compliance, to assist in product identification / separation, or to enhance overall safety and effectiveness of the drug delivery system during storage or use are explained. Moreover, the use of these excipients in drug delivery systems are identified. Excipient toxicity, which is an issue discussed in the light of current studies, also discussed in this review.

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