Preparation and Evaluation of Rapidly Disintegrating Glimepiride Tablets

2011 ◽  
Vol 3 (4) ◽  
pp. 1220-1229
Author(s):  
Adel M Aly ◽  
Bassam I Amro ◽  
Feras D El Hajji
Keyword(s):  
Fasting Blood Glucose ◽  
Diabetic Patients ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Glucose Levels ◽  
Orally Disintegrating Tablets ◽  
Accelerated Stability ◽  
The Stability

The objective of this work was to prepare Glimepiride (1 mg) rapidly disintegrating tablets (RDT) by direct compression, and also, to evaluate Pharmaburst™ as a newly introduced diluent for this type of tablets, either alone or in combination with other well known tablet excipients. Another goal was to study the stability, as well as, the in vivo effects of selected formulations. Orange flavor was the most preferred flavor for the prepared rapidly disintegrating tablets containing Pharmaburst™ as a single diluent. Pharmaburst™ alone is sufficient to produce rapidly (orally) disintegrating tablets of Glimepiride with good physical characteristics, better compactability and shorter in-vivo and in-vitro disintegration time. The prepared Glimepiride RDT were found to have faster onset of action than the conventional Glimepiride tablets. Also, they were effective in lowering fasting blood glucose levels (FBG) in rabbits. Glimepiride RDT containing Pharmaburst™ alone were found to be stable when subjected to accelerated stability conditions (40 °C / 75 % relative humidity) for at least 3 months. Packaging the prepared Glimepiride  RDT in 40 CC high density polyethylene (HDPE) bottles with 2 grams silica gel desiccant canisters and rayon had provided sufficient protection for the tablets. The used packaging system is believed to be very practical and convenient for elderly diabetic patients. It is also assumed to be preferred by the manufacturers.

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

scholarly journals DEVELOPMENT, FORMULATION AND EVALUATION OF MECLOFENAMATE FAST DISSOLVING TABLETS

2021 ◽  
Vol 10 (1) ◽  
pp. 59-67
Author(s):  
Mahipal Shakkarwal ◽  
Dr. Mukesh Sharma ◽  
Dr. Ram Garg ◽  
Shankar Lal Soni ◽  
Gopal Kumar Paswan ◽  
...  
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation ◽  
Suitable Treatment ◽  
The Stability

The demands for fast dissolving tablets have received ever increasing day by day during the last 10-15 years for the onset of action. In the present study, the effect of superdisintegrant was compared with synthetic super disintegrants and other conventional super disintegrants in the of fast dissolving tablet formulation of Meclofenamate. Meclofenamate is an antihypertensive drug and in case of hypertension immediate treatment is required so the proposed investigation is totally based to provide the suitable treatment for hypertension. In the present work 9 formulations of Fast dissolving tablets of Cilnidipine were prepared by using Synthesized Co-proceed was evaluated and compiles with the official standards, parameters and specifications. Various formulations were prepared using four different superdisintegrant namely- kyron T-304, sodium starch glycolate, cross carmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose , bulk density , tapped density , and then tablet  evaluated post-compression parameters like thickness , drug content , hardness , weight variation  , wetting time , friability , disintegration time , dissolution time, drug release study. Formulation A8 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation A8 showed 98.64% drug release at the end of 3 minutes. The best formulations were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline and standards.

Formulation and Evaluation of Oro Dispersible Tablets of Ondansetron Hydrochloride by Direct Compression using Superdisintegrants

1970 ◽  
Vol 1 (1) ◽  
pp. 106-111
Author(s):  
Avani R. Gosai ◽  
Sanjay B. Patil ◽  
Krutika K. Sawant
Keyword(s):  
Mechanical Strength ◽  
Direct Compression ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation ◽  
Ondansetron Hydrochloride ◽  
Dispersible Tablets ◽  
In Vitro Disintegration

The objective of the present investigation was to prepare oro dispersible tablets of ondansetron hydrochloride, because of its application in emesis condition, fast onset of action and avoidance of water is highly desirable. Tablets were prepared by direct compression using sodium starch glycolate and croscarmellose as superdisintegrants, as the combination of these two agents gives better disintegration of the tablet. Microcrystalline cellulose was used as diluent and mannitol, mint flavor, sodium saccharine to enhance the organoleptic properties of tablets. The tablets were evaluated for weight variation, mechanical strength, in vitro disintegration time, in vivo disintegration time, wetting time, and drug release characteristics. Hardness and friability data indicated good mechanical strength of tablets.  The results of in vitro disintegration time and in vivo disintegration time indicated that the tablets dispersed rapidly in mouth within 3 to 5 seconds. Dissolution study revealed faster release rate of ondansetron hydrochloride from the tablets as compared to pure drug and marketed conventional tablet formulation of ondansetron hydrochloride. It was concluded that superdisintegrants addition technique is a useful method for preparing oro dispersible tablets by direct compression method

Formulation and Characterization of Fast Dissolving films of Etoricoxib

2021 ◽  
Vol 3 (2) ◽  
Author(s):  
Km. Roshani ◽  
Mangla Nand Singh ◽  
D. Sasmal ◽  
P. D. Panda ◽  
Jai Narayan Mishra ◽  
...  
Keyword(s):  
Uv Spectroscopy ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Presystemic Metabolism ◽  
The Stability ◽  
Preformulation Studies ◽  
Oral Films

Etoricoxib belongs to a class of drugs called non-steroidal anti-inflammatory drugs (NSAIDs). Etoricoxib acts by reducing the pain and swelling (inflammation) in the joints and muscles of people older than 16 years of age and older patients with osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and gout. The present study was aimed to formulate fast dissolving oral films to enhance bioavailability, avoid presystemic metabolism and fast onset of action. The Preformulation studies such as Micromeritics, melting point, partition coefficients, UV spectroscopy, thin layer chromatography, loss on drying were carried out. The fast dissolving oral film was successfully fabricated by solvent casting method. Oral film was fabricated using PVA and PVP polymer. The prepared films were evaluated for Organoleptic evaluations, film weight, thickness, folding endurance, tensile strength, drug content uniformity of films, surface pH, disintegration time and in-vitro dissolution studies and SEM study. The formulation F8 has shown disintegration time of 22±1 seconds and is more promising, showed drug release in phosphate buffer 6.8 pH 86.33% in 10 min. Hence formulation F8 was selected as best formulation. In the stability testing all films stored at elevated temperature showed slight change in pH, other parameters were found to be unchanged.

scholarly journals OPTIMIZATION AND EVALUATION OF CHLORPHENIRAMINE MALEATE ORAL STRIP FOR PEDIATRIC USE

2018 ◽  
Vol 11 (12) ◽  
pp. 548 ◽  
Author(s):  
Sura Zuhair Mahmood ◽  
Hiba Sabah Sabry ◽  
Nora Zawar Yousif ◽  
Zeina D Salman
Keyword(s):  
Pediatric Population ◽  
Hydroxypropyl Methylcellulose ◽  
Chlorpheniramine Maleate ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Casting Technique ◽  
Fast Onset ◽  
Pediatric Use

Objective: The goal of performing this study is to prepare an oral strip, especially designed for pediatric use that provides fast onset of action with ease of swallowing particularly for young individuals who suffer from difficulty of swallowing, in addition provides maximum therapeutic effectiveness by reducing the first pass effect.Materials and Methods: The oral strip was prepared by solvent casting technique through using different sole polymers (hydroxypropyl methylcellulose [HPMC] 15cp, HPMC 50cp, polyvinyl alcohol, and sodium carboxymethyl cellulose). Maltodextrin (MD) was added as the secondary polymer in different ratios to optimize the release parameters, and disintegration time (DT), three different plasticizers were employed (propylene glycol, dibutyl phthalate, and glycerin) to boost the film forming polymer characteristics.Results: From this study, it is obvious that F10 which composed of HPMC as a main polymer and MD as a secondary polymer in ratio 2:1, respectively, provides adequate physicochemical characteristics, in vivo/in vitro DT (40/36 s), respectively, nevertheless a satisfactory release parameters as (59.9%) released at 2 min and 80% of drug released at 14.8 min.Conclusion: The optimized formula is pretty encouraging to originate an oral strip that provides ease of administration, fast onset of action with wide acceptance for the pediatric population.

scholarly journals In Vitro and In Vivo Effects of Norathyriol and Mangiferin on α-Glucosidase

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Zhi-Long Shi ◽  
Yi-Dan Liu ◽  
Yun-Yun Yuan ◽  
Da Song ◽  
Mei-Feng Qi ◽  
...  
Keyword(s):  
Blood Glucose ◽  
Glucose Tolerance Test ◽  
Fasting Blood Glucose ◽  
Tolerance Test ◽  
Glucose Levels ◽  
Blood Glucose Levels ◽  
In Vivo Effects ◽  
Antidiabetic Effects

Norathyriol is a metabolite of mangiferin. Mangiferin has been reported to inhibit α-glucosidase. To the best of our knowledge, no study has been conducted to determine or compare those two compounds on inhibiting α-glucosidase in vitro and in vivo by far. In this study, we determined the inhibitory activity of norathyriol and mangiferin on α-glucosidase in vitro and evaluated their antidiabetic effect in diabetic mice. The results showed that norathyriol inhibited α-glucosidase in a noncompetitive manner with an IC50 value of 3.12 μM, which is more potent than mangiferin (IC50 = 358.54 μM) and positive drug acarbose (IC50 = 479.2 μM) in the zymological experiment. Both of norathyriol and mangiferin caused significant (p<0.05) reduction in fasting blood glucose and the blood glucose levels at two hours after carbohydrate loading and it was interesting that mangiferin and norathyriol can make the decline of the blood glucose earlier than other groups ever including normal group in the starch tolerance test. However, norathyriol and mangiferin did not significantly influence carbohydrate absorption in the glucose tolerance test. Therefore, the antidiabetic effects of norathyriol and mangiferin might be associated with α-glucosidase, and norathyriol was more potent than mangiferin.

scholarly journals Antidiabetic potential of Gaultheria trichophylla in mice

2017 ◽  
Vol 12 (3) ◽  
pp. 292
Author(s):  
Fiaz Alam ◽  
Qazi Najam us Saqib
Keyword(s):  
Fasting Blood Glucose ◽  
Video Clip ◽  
Diabetic Control ◽  
Control Group ◽  
Standard Drug ◽  
Glucose Levels ◽  
Full Screen ◽  
The Difference

<p>This study evaluated <em>Gaultheria trichophylla</em> for its <em>in vitro</em> and <em>in vivo</em> anti-diabetic activity and its effect on biochemical parameters. The extract inhibited α-glucosidase with IC<sub>50 </sub>= 17.5 ± 0.1 μg/mL). The difference of body weight of the extract-treated diabetic groups and diabetic control was significant (p&lt;0.05). The extract-treated and the standard-treated groups showed significant (p&lt;0.001) decrease in the fasting blood glucose levels compared to diabetic control. The extract-treated groups after 15 days of treatment showed a significance (p&lt;0.001 and p&lt;0.05) decrease of the urea and creatinine levels respectively. The extract and standard-treated diabetic groups showed a significant decreased in the serum level of cholesterol, LDL, and triglycerides compared to the diabetic control group (p&lt;0.001). The extract and standard drug showed a significance improvement of HDL level in diabetic mice compared to the diabetic control (p&lt;0.001).</p><p><strong>Video Clip of Methodology</strong>:</p><p>2 min 49 sec:   <a href="https://www.youtube.com/v/l8cU2wT953w">Full Screen</a>   <a href="https://www.youtube.com/watch?v=l8cU2wT953w">Alternate</a></p>

Tobramycin Collagen Fast Dissolving Ocular Films for Corneal Tissue Engineering of Keratoconus

2019 ◽  
Vol 9 (6) ◽  
pp. 804-809
Author(s):  
Jing Qin ◽  
Ni Yin
Keyword(s):  
Pharmaceutical Research ◽  
Immediate Release ◽  
Ease Of Use ◽  
Corneal Tissue ◽  
Disintegration Time ◽  
Weight Variation ◽  
Orally Disintegrating Tablets ◽  
Drug Polymer Interaction

Fast dissolving films are a one of novel dosage form in pharmaceutical research. They have convenience and ease of use over other dosage forms such as orally disintegrating tablets and immediate release tablets. In the present research, rapidly dissolving films of Tobramycin were developed using Polyvinyl acetate (PVA) and polyvinyl pyrollidone (PVP) as film forming polymers by solvent casting method. The prepared films were evaluated for drug content, weight variation, thickness and in vitro in vivo disintegration time. The in vitroand in vivodissolving time of the optimized formulation was found to be below 15–40 seconds respectively. The prepared films exhibited good integrity and thickness. In vitro dissolution studies were performed as per the FDA dissolution guidelines for about 3 minutes, the optimum formulation released complete drug within 3 minutes. Statistical analysis showed no drug polymer interaction.

Formation and Structure of Casein Micelles in Lactating Mammary Tissue

1970 ◽  
Vol 28 ◽  
pp. 150-151
Author(s):  
Robert J. Carroll ◽  
Marvin P. Thompson ◽  
Harold M. Farrell
Keyword(s):  
Size Distribution ◽  
G Protein ◽  
Milk Proteins ◽  
Mammary Tissue ◽  
Colloidal System ◽  
Casein Micelles ◽  
The Stability

Milk is an unusually stable colloidal system; the stability of this system is due primarily to the formation of micelles by the major milk proteins, the caseins. Numerous models for the structure of casein micelles have been proposed; these models have been formulated on the basis of in vitro studies. Synthetic casein micelles (i.e., those formed by mixing the purified αsl- and k-caseins with Ca2+ in appropriate ratios) are dissimilar to those from freshly-drawn milks in (i) size distribution, (ii) ratio of Ca/P, and (iii) solvation (g. water/g. protein). Evidently, in vivo organization of the caseins into the micellar form occurs in-a manner which is not identical to the in vitro mode of formation.

Kinetics of Various 99mTc-Sn-Pyrophosphate Compounds in the Rat

1977 ◽  
Vol 16 (04) ◽  
pp. 157-162 ◽  
Author(s):  
C. Schümichen ◽  
B. Mackenbrock ◽  
G. Hoffmann
Keyword(s):  
Normal Saline ◽  
Half Life ◽  
Compound A ◽  
Short Half Life ◽  
Low Concentrations ◽  
The Stability ◽  
Kinetics Of ◽  
In Vitro Stability

SummaryThe bone-seeking 99mTc-Sn-pyrophosphate compound (compound A) was diluted both in vitro and in vivo and proved to be unstable both in vitro and in vivo. However, stability was much better in vivo than in vitro and thus the in vitro stability of compound A after dilution in various mediums could be followed up by a consecutive evaluation of the in vivo distribution in the rat. After dilution in neutral normal saline compound A is metastable and after a short half-life it is transformed into the other 99mTc-Sn-pyrophosphate compound A is metastable and after a short half-life in bone but in the kidneys. After dilution in normal saline of low pH and in buffering solutions the stability of compound A is increased. In human plasma compound A is relatively stable but not in plasma water. When compound B is formed in a buffering solution, uptake in the kidneys and excretion in urine is lowered and blood concentration increased.It is assumed that the association of protons to compound A will increase its stability at low concentrations while that to compound B will lead to a strong protein bond in plasma. It is concluded that compound A will not be stable in vivo because of a lack of stability in the extravascular space, and that the protein bond in plasma will be a measure of its in vivo stability.

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