scholarly journals Application of Eudragit RS 30D as a Potential Drug Release Retardant of Acetaminophen and Caffeine for Prolonged Duration of Comfort

2019 ◽  
Vol 2019 ◽  
pp. 1-7
Author(s):  
Lailoona Jaweed ◽  
Huma Dilshad ◽  
Ghulam Sarwar
Keyword(s):  
Dosage Form ◽  
Water Soluble ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Potential Drug ◽  
Eudragit Rs ◽  
Prolonged Duration ◽  
Water Soluble Drugs ◽  
Eudragit Rs 30D ◽  
Percentage Release

The objective of the study is to formulate an extended release matrix tablet dosage form containing acetaminophen and caffeine by applying polymer technology which will relieve all kinds of pain for about 12 hours. Considering the fact that there is no such formulation available in the pharmaceutical market, it is expected that this drug could be an effective introduction. Hydrophobic polymers have a great application in pharmaceutical sciences as they retard the release of water-soluble drugs and give prolonged effect. Eudragit RS 30D was used to prepare 3 formulations (EF1, EF2, and EF3) containing varying concentrations of polymer, through the wet granulation method. Each tablet contained 1000 mg of acetaminophen and 130 mg of caffeine including other suitable excipients. All pharmacopeial and nonpharmacopeial tests were conducted to determine the quality of dosage form and to identify optimized formulation among EF1-EF3. Dissolution was conducted on similar gastric conditions through which different kinetic models were applied using DDSolver. For 12 hrs of dissolution, caffeine was released from EF1, EF2, and EF3 with the percentage release in the range from 99.85% to 100.65%, 99.32% to 100.28%, and 98.09% to 100.77%, respectively. For acetaminophen, the percent release was from 99.81% to 100.91%, 100.24% to 100.91%, and 86.81% to 95.73% for EF1-EF3, respectively. Results concluded that EF2 is the most optimized drug having all physicochemical quality control tests within the specified limits. On applying different models like zero-order, Hixson-Crowell, Higuchi, and Korsmeyer-Peppas upon use, it is concluded that the formulation follows Korsmeyer-Peppas as it was the best-fitted model with the r2 value closest to 0.999. EF2 is considered as a potential drug to be manufactured that will give prolonged relief against pain and will decrease compliance issues related to dosing frequency.

Improved Dissolution Properties of Ketoconazole through Application of Liquisolid Techniques

2015 ◽  
Vol 8 (4) ◽  
pp. 3053-3059
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
H G Sandip
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Water Soluble ◽  
Wet Granulation ◽  
Wetting Properties ◽  
Enhanced Dissolution ◽  
Water Soluble Drug ◽  
Drug Concentrations ◽  
Water Soluble Drugs ◽  
Liquisolid Compacts

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Ketoconazole. The liquisolid tablets were formulated with liquid medications, namely Propylene Glycol (PG) drug concentrations, 60% w/w, 70% w/w and 80% w/w. Avicel pH102 was used as a carrier material, Aerosil 200 as a coating material and Sodium starch glycollate as a super-disintegrant. Quality control tests, such as uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate prepared tablets. For further confirmation of results the liquisolid compacts were evaluated by XRD and FTIR studies to prove that, solubility of Ketoconazole has been increased by liquisolid compact technique. From the results obtained, it was be speculated that such systems exhibit enhanced drug release profiles due to increased wetting properties and surface of drug available for dissolution. As liquisolid compacts demonstrated significantly higher drug release rates, in PG as compared to directly compressible tablets and conventional wet granulation, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.  

REVIEW ON FAST DISSOLVING TABLET BY SOLID DISPERSION APPROACH

2021 ◽  
pp. 2840-2845
Author(s):  
V. Namitha
Keyword(s):  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
And Performance ◽  
High Level ◽  
Determining Factor ◽  
Mouth Dissolving Tablet

Tablet is found to be the most popular dosage form among all existing dosage form. However, in certain occurrences as a result of the huge size of dosage forms, and in the uncooperative, pediatric and dysphasia patients, it might make a few problems, to avoid this issues, another type of dosage form is created, which is known as fast dissolving tablet or mouth dissolving tablet. These are the high level dosage form which breaks down within seconds when placed on the toungue. Mouth dissolving tablets have become impressive consideration as a better option in contrast to others because of better convenience to patients. This review discusses the method of preparation, properties, mechanisms; capsules to be incorporated inside the mouth dissolving pill and evaluation of the drugs are emphasized. The solid dispersion is one of the established solubilization techniques for poorly water-soluble drugs. It is basically the interaction between drug and polymer, and hence it is found to be the determining factor in its design and performance. This review additionally summarizes our knowledge on solid dispersions both in the solid as well as liquid state.

scholarly journals DEVELOPMENT OF DISINTEGRATION CONTROL MATRIX TABLETS OF FEBUXOSTAT

2018 ◽  
Vol 6 (4) ◽  
pp. 12-20
Author(s):  
Kanke Pralhad
Keyword(s):  
Gastrointestinal Transit ◽  
Water Soluble ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
New Approach ◽  
Water Soluble Drugs ◽  
Control Matrix ◽  
Wax Coating

Disintegration control matrix tablet (DCMT) is a new approach for poorly water soluble drugs which successfully sustain the release up to 24hrs by controlling the disintegration rate of tablet. DCMT mainly forms the granules containing drug febuxostat and disintegrant sodium alginate which controls the release of febuxostat by controlling the rate of disintegration in wax coating plays an important role. The sustained release of drug is maintained by increasing the wax coating or decreasing the amount of disintegrant. The release of drug from tablet is uniform throughout till all the drug releases from tablet and it is justified by in-vitro dissolution studies. DCMT increases the solubility of drug and improves the bioavailability without disturbing gastrointestinal transit.

scholarly journals THE DEVELOPMENT OF GLIBENCLAMIDE-SACCHARIN COCRYSTAL TABLET FORMULATIONS TO INCREASE THE DISSOLUTION RATE OF THE DRUG

2019 ◽  
pp. 359-364 ◽  
Author(s):  
ARIF BUDIMAN ◽  
PATIHUL HUSNI ◽  
SHAFIRA ◽  
Tazyinul Q. Alfauziah
Keyword(s):  
Dissolution Rate ◽  
Dosage Form ◽  
Water Soluble ◽  
Crystal Habit ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Grinding Method ◽  
Water Soluble Drugs ◽  
Rate Test ◽  
Tablet Dosage

Objective: Cocrystallisation is a promising method in order to increase the solubility and dissolution of poorly water-soluble drugs. The aim of this study was to prepare, formulate and evaluate glibenclamide (GCM) cocrystal in direct compress tablet dosage form using saccharin (SAC) as the coformer. Methods: GCM cocrystal with various stoichiometric ratios were prepared by the solvent drop grinding method. The co-crystal was characterized by a saturated solubility test and dissolution rate test, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-Ray Diffraction (PXRD). The tablet dosage form of GCM was formulated and evaluated compare with the conventional dosage form. Results: The solubility and disso­lution rate of GCM-SAC cocrystals increased significantly compared with pure GCM, especially for 1:2 of ratio. The dissolution rate of cocrystal with ratio 1:2 increased by almost 91.9% compared with pure GCM. Based on the FTIR analysis, it showed the shifting of characteristic bands of GCM in the spectrum and there was no chemical reaction in GCM cocrystal. In PXRD measurement, the new crystalline peak was detected in the crystal habit of cocrystal compared with pure GCM and coformer. The new single melting of GCM-SAC cocrystal also was detected in DSC measurement. The tablets of GCM-SAC cocrystal were successfully prepared by direct compression method which rapidly disintegrated (1 min) and has higher dissolution compared with its pure form (32.36% greater than glibenclamide after 45 min). Conclusion: The tablet dosage form of GCM cocrystal with SAC as coformer was successfully prepared, formulated and improved its solubility and dissolution rate.

scholarly journals Formulation and evaluation of sustain released matrix tablet of atenolol

2019 ◽  
Vol 9 (1) ◽  
pp. 183-189 ◽  
Author(s):  
Sonal Sahu ◽  
Rohit Dangi ◽  
Rohit Patidar ◽  
, Rukhsaar ◽  
Jagdish Rathi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Oral Route ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Natural Polymer ◽  
Flexible Design ◽  
Weight Variation

Oral route is one of the most popular routes of drug delivery due to its ease of administration, patient compliance, least sterility constraints and flexible design of dosage form. The aim of present investigation was to develop matrix tablets of atenolol using different polymers. Atenolol matrix tablets were prepared by direct compression and wet granulation method using different polymers. All the formulations were evaluated for weight variation, thickness, hardness, friability and dissolution. Tablets of atenolol were prepared utilizing natural polymer chitosan. The formulation F-2 contained chitosan which might have sustained the release since it is also known for its polymeric sustaining effect. The formulation F-2 gave 89.57±0.24% of the drug release in 12 hrs of study. Keywords: Atenolol, Sustained release Matrix tablets, Direct compression, Wet granulation method.

scholarly journals Physicochemical characterisation and in vitro evaluation of modified release matrix tablets: The role of different grades of hydroxypropylmethyl cellulose

2018 ◽  
Vol 63 (02) ◽  
pp. 37-47
Author(s):  
Vesna Petrovska Jovanovska ◽  
Ljupco Pejov ◽  
Aleksandra Petrovska ◽  
Sonja Ugarkovic ◽  
Maja Simonoska Crcarevska ◽  
...  
Keyword(s):  
Water Soluble ◽  
Matrix Tablets ◽  
Polymer Chains ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Prolonged Release ◽  
Matrix Tablet ◽  
Hydroxypropylmethyl Cellulose ◽  
Release Data

The purpose of this work was to formulate prolonged release matrix tablets with water soluble opioid drug (API) using different types of hydroxypropylmethyl cellulose (Methocel) as controlled release polymers. Methocel K100M was incorporated as intra-granular polymer (sample 1) along with Methocel K4M (sample 2) or Methocel K15M (sample 3) as extra-granular polymers. The final blends and tablets prepared by wet granulation process were fully characterized. Results showed that the polymer used extra-granularly significantly affects the tablet properties. By incorporation of Methocel extra granularly (samples 2 and 3), the hardness and tensile strength of the tablets increased and the total tablet porosity decreased. Sample 1, containing only Methocel K100M (intra granularly) has the lowest index of swelling and the fastest release of API probably due to the cross-linking of the polymer chains during the process of wet granulation. Also, the type of Methocel used extra-granularly (with different viscosity grade) was found to significantly affect the swelling ratio of the designed matrix systems and the drug release behavior. Sample 2 containing Methocel K4M extra-granularly has a lower index of swelling and faster release of API compared to sample 3. Considering the release mechanism, release data showed best fitting to the heuristic model proposed by Korsmeyer-Peppas. Two additional approaches were used for mathematical modeling of the release data in order to make them directly applicable for our experimental results. Keywords: matrix tablet, water soluble opioid drug, prolonged release, HPMC (Methocel)

scholarly journals Preparation and In Vitro Evaluation of Ethylcellulose and Polymethacrylate Resins Loaded Microparticles Containing Hydrophilic Drug

2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Satish Pandav ◽  
Jitendra Naik
Keyword(s):  
Encapsulation Efficiency ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Propranolol Hydrochloride ◽  
Eudragit Rs ◽  
Internal Phase ◽  
Water Soluble Drugs ◽  
Percentage Yield ◽  
Emulsification Solvent Evaporation

Objective. The purpose of the recent study was to prepare and estimate sustained release of Ethylcellulose (300 cps) and Eudragit (RS 100 and RL 100) microparticles containing Propranolol hydrochloride used as a treatment of cardiovascular system, especially hypertension. Method. Propranolol hydrochloride was microencapsulated with different polymers (Ethylcellulose, Eudragit RS, and Eudragit RL) using modified hydrophobic (O/O) solvent evaporation method using 1 : 1 combination of acetone and isopropanol as the internal phase. Obtained microparticles were showing higher batch yield with higher encapsulation efficiency. Microparticles were prepared with different ratios of 1 : 1, 1 : 3, 1 : 5, and 1 : 7 (%, wt/wt) using span 80 (%, v/v) as a surfactant. Results. The influence of formulation factors like drug: polymer ratio, internal phase, and type of polymers on obtained microparticles was characterized with respect to particle size distribution, encapsulation efficiency, percentage yield, FTIR, and FE-SEM. Higher encapsulation efficiencies were obtained with various polymers like Ethylcellulose (96.63 ± 0.5) compared to Eudragit RS 100 (83.70 ± 0.6) and RL 100 (89.62 ± 0.6). The in vitro release study was characterized by initial burst. Conclusion. The result of study displays that Ethylcellulose and Eudragit loaded microparticles of Propranolol hydrochloride can be effectively prepared using modified hydrophobic emulsification solvent evaporation technique. Therefore, the modified hydrophobic emulsion technique can also be applied to the preparation of microparticles for low molecular weight and highly water soluble drugs.

scholarly journals A COMPREHENSIVE REVIEW ON SUSTAINED RELEASE MATRIX TABLETS: A PROMISING DOSAGE FORM

2019 ◽  
Author(s):  
Agarwal Prakhar ◽  
Akhtar Semimul
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Extended Release ◽  
Evaluation Studies ◽  
Porous Matrix ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Hydrophobic Polymers

Oral ingestion is most convenient and commonly employed route of drug delivery due to its ease of administration, least aseptic and flexibility in the design of dosage form. The objective of the study was to explore the necessity, advantages and various techniques of extended release matrix tablet to get a constant drug delivery rate and reproducible kinetics for advance delivery. Different types of extended release matrix tablet have been explained briefly along with the various formulation which mainly by wet granulation or direct compression method or by dispersion of solid particle within a porous matrix formed by using different polymers. Matrix controls the free rate of drug. Matrix tablets can be formulated by either direct compression or wet granulation method by using a variety of hydrophilic or hydrophobic polymers. The extended release matrix tablets can assure better patient compliance through reduction in total dose and dosage regimen, which can be great help to treat chronic diseases. This review highlights the types of matrices, mechanisms involved and evaluation studies.

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