Formulation and evaluation of Diclofenac sodium mucoadhesive buccal tablets by using natural polymers

2018 ◽  
Vol 9 (1) ◽  
pp. 236 ◽  
Author(s):  
Venkatalakshmi Raganathan ◽  
Muhammad Zulfahmi Bin Abd Majid ◽  
Prasanthi Sri ◽  
Sasikala Chinnappan
Keyword(s):  
Ex Vivo ◽  
Diclofenac Sodium ◽  
Systemic Circulation ◽  
In Vitro Dissolution ◽  
In Vitro Tests ◽  
Dissolution Profile ◽  
Natural Polymers ◽  
Weight Variation ◽  
Buccal Tablets

Diclofenac sodium is a common and widely-used drug for the treatment of pain, inflammation and also migraine. Unfortunately, it undergoes extensive first-pass hepatic metabolism when administered through the oral systemic route. Thus, this study will be about the formulation of mucoadhesive buccal tablets of diclofenac sodium that can prevent the extensive metabolism of the drug, which in turn increases its bioavailability inside the systemic circulation. This formulation might also reduce the dosing frequency, which can lead to a better patient compliance to the medication. The formulations would be using natural polymers such as acacia gum and chitosan as the mucoadhesive polymers. Ethylcellulose (EC) was included as the backing layer of the buccal tablets, along with other excipients. In total, four different formulations were prepared with the varying concentration of the natural polymers. The formulated buccal tablets have been evaluated for their general appearance, thickness, hardness, weight variation, friability, ex-vivo mucoadhesion time and other in-vitro tests such as swelling and dissolution studies. The finding of this study confirmed that Formulation 3 (F3) had the best properties of mucoadhesive buccal tablets as it displayed the highest in-vitro swelling index and in-vitro dissolution profile, also with the longest ex-vivo mucoadhesion time.

Fabrication and Evaluation of Mouth Dissolving Strips of Metoclopramide Hydrochloride by Using Novel Film Former

2021 ◽  
pp. 5515-5520
Author(s):  
Hemant A. Deokule ◽  
Smita S. Pimple ◽  
Praveen D. Chaudhari ◽  
Ajit S. Kulkarni
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Systemic Circulation ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Visual Appearance ◽  
Dsc Studies ◽  
Weight Variation ◽  
Metoclopramide Hydrochloride

Fast dissolving strips are used as novel approaches, as it dissolves rapidly in mouth and directly reaches the systemic circulation. In present research work, an attempt has been made to prepare mouth dissolving strips of Metoclopramide hydrochloride by using a novel film former Pullulan by solvent casting method. A33 full factorial design was utilized for the optimization of the effect of independent variables such as the amount of Pullulan, amount of PEF 400, amount of SSG on mechanical properties, and % drug release of strips. The drug compatibility studies using FTIR and DSC studies formulated strips were characterized for their physicochemical parameter like weight variation, visual appearance, folding endurance, thickness, disintegration time, drug content, and in vitro dissolution studies. FTIR and DSC studies revealed that the polymer is compatible with the drug. It was found that the optimum levels of the responses for a fast release strip could be obtained at low levels of Pullulan, PEG400, and SSG. The prepared strip was clear transparent and had a smooth surface. The surface pH was found 4.8 to 5.2 be in the range of to which is close to salivary pH, which indicates that strips may have less potential to irritate the oral mucosa, thereby they are comfortable. The drug release was found to be between 90.94 to 100.5% in 2 min. The in-vitro disintegration time of strips prepared with Pullulan was in the range of 19 to 57 sec. As the concentration of SSG increases the decrease in the disintegration time of strips a decrease. The dissolution rate increased with an increase in the concentration of SSG. Hence, it can be inferred that the fast dissolving oral strips of Metoclopramide hydrochloride may produce rapid action thereby improving bioavailability and enhance the absorption by avoiding the first-pass effect.

scholarly journals Eight enteric-coated 50 mg diclofenac sodium tablet formulations marketed in Saudi Arabia: in vitro quality evaluation

2020 ◽  
Vol 13 (1) ◽  
Author(s):  
Muhammad M. Hammami ◽  
Rajaa F. Hussein ◽  
Reem AlSwayeh ◽  
Syed N. Alvi
Keyword(s):  
Quality Evaluation ◽  
Diclofenac Sodium ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
United States Pharmacopoeia ◽  
Weight Variation ◽  
Tablet Formulations ◽  
Enteric Coated

Abstract Objective To evaluate in vitro quality of enteric-coated 50 mg diclofenac sodium tablet formulations on Saudi market. Results A reference and seven generic (G1-7) formulations were commercially available in December 2019/January 2020 and were assessed within 25–75% of manufacture-expiration period. Weight variation (range as% difference from mean, n = 20), active substance content (ASC, mean (SD) as% difference from label, n = 20), hardness (mean (SD), n = 10), and friability (% weight loss, n = 20) were 97–103%, 102.0% (3.4%), 15.4 (1.1) kg, and 0.24%, respectively, for the reference. For G2-7, they were ≤ ±5%, 98.6% (4.0%) to 109.9% (1.8%), 11.9 (0.9) to 18.3 (0.8) kg, and ≤ 0.00 to 0.75%, respectively. G1 ASC, hardness, and friability were 111.3% (1.7%), 20.1 (1.7) kg, and 1.10%, respectively. Disintegration time (n = 6) and dissolution profile (n = 8) were also determined. No formulation disintegrated or released ˃ 0.1% of label ASC in 0.1 N HCl for 2 h. The reference disintegrated in 15:00 min:seconds and released a mean (range) of 100% (99–103%) of label ASC by 45 min in phosphate buffer (pH = 6.8). G1-7 disintegrated in 8:53 to 20:37 min:seconds and released 81% (69–90%) (G1) to 109%. Except for borderline performance of G1, all formulations passed in vitro quality tests according to United States Pharmacopoeia.

scholarly journals A Comparative Study on In-vitro Quality Control Parameters of Different Brands of Loratadine Tablets Commercially Available in Bangladesh

2021 ◽  
pp. 50-58
Author(s):  
Rosy Fatema ◽  
Sumaiya Khan ◽  
A. S. M. Roknuzzaman ◽  
Ramisa Anjum ◽  
Nishat Jahan
Keyword(s):  
Research Work ◽  
Drug Market ◽  
Quality Standard ◽  
In Vitro Dissolution ◽  
Active Principle ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Weight Variation ◽  
Local Companies

Loratadine, a second generation H1-receptor antagonist, works by blocking the action of histamine and is widely prescribed for itching, runny nose, watery eyes, and sneezing from "hay fever" and other allergic conditions. To ensure quality the main requirements for a medicinal product are safety, potency, efficacy and stability. This research work aimed to compare and assess the quality levels of different local brands of loratadine tablets available in the drug market of Bangladesh. Six different brands of loratadine 10 mg tablet manufactured by the local companies were used for the analysis. The evaluation was performed through the determination of weight variation, hardness, friability, percent potency, disintegration time, and dissolution profile in accordance with USP-NF specifications. All brands showed acceptable weight variation and % friability. The percent potency for tested samples by UV method ranges from 97.02%-108%, showing none of the brands contains less than 90% of the active principle as per the specification. The result of the physical and chemical studies, such as in-vitro dissolution, disintegration, hardness, etc., has been found to differ but lie within the specified limit. After analyzing the data obtained from the tests, it can be claimed that loratadine 10 mg tablets manufactured and marketed by several local companies in Bangladesh meet the quality standard required to achieve the desired therapeutic outcomes.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING ORAL FILM OF ANTI-ALLERGIC DRUG

2018 ◽  
Vol 6 (3) ◽  
pp. 5-16 ◽  
Author(s):  
ABRAHAM LINKU ◽  
JOSEPH SIJIMOL
Keyword(s):  
Ex Vivo ◽  
Methyl Cellulose ◽  
Moisture Loss ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Permeation Study ◽  
Weight Variation

The aim of present work was the development of fast dissolving oral film of Loratadine to overcome the limitations of current routes of administration, to provide immediate action and increase the patient compliance. To improve the bioavailability of the drug, fast dissolving oral film were formulated using different grades of Hydroxy Propyl Methyl Cellulose(HPMC) and various plasticizers like Polyethylene Glycol(PEG) 400, glycerol, Propylene glycol(PG) by solvent casting method. The formulated films were evaluated for film thickness, surface pH, folding endurance, weight variation, % moisture loss, exvivo permeation study, tensile strength, % elongation, drug content uniformity, in vitro dissolution studies,in vitro disintegration test and in vivo study. The optimized formulation (F9) containing HPMC E5 and glycerol showed minimum disintegration time (10.5 s), highest in vitrodissolution (92.5%) and satisfactory stability. Ex vivo permeation study of optimized formulation showed a drug release of 80.6% within 10 min. The milk induced leucocytosis inrat proved that fast dissolving oral films of Loratadine produced a faster onset of action compared to the conventional tablets. These findings suggest that fast dissolving oral film of Loratadine could be potentially useful for treatment of allergy where quick onset of action is required.

scholarly journals Formulation and Evaluation of Loperamide HCl Oro Dispersible Tablets

2020 ◽  
Vol 13 (5) ◽  
pp. 100
Author(s):  
Blasco Alejandro ◽  
Torrado Guillermo ◽  
Peña M Ángeles
Keyword(s):  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Biomedical Sciences ◽  
Disintegration Time ◽  
Weight Variation ◽  
Orally Disintegrating Tablets ◽  
Wetting Time ◽  
Percentage Of Water Absorption ◽  
Hostile Environments

This work proposes the design of novel oral disintegrating tablets (ODTs) of loperamide HCl with special emphasis on disintegration and dissolution studies. The main goal was augmenting the adherence to treatment of diseases which happen with diarrhea in soldiers who are exposed to diverse kinds of hostile environments. Optimized orally disintegrating tablets were prepared by the direct compression method from galenic development to the industrial scale technique, thanks to strategic and support actions between the Spanish Army Force Lab and the Department of Biomedical Sciences (UAH). The results show that loperamide HCl ODT offers a rapid beginning of action and improvement in the bioavailability of poorly absorbed drugs. The manufactured ODTs complied with the pharmacopeia guidelines regarding hardness, weight variation, thickness, friability, drug content, wetting time, percentage of water absorption, disintegration time, and in vitro dissolution profile. Drug compatibility with excipients was checked by DSC, FTIR, and SEM studies.

Theoritical Uses of Pramipexole dihydrochloride in Parkinson's Resistance Depression

2017 ◽  
Vol 1 (2) ◽  
pp. 01-03
Author(s):  
Samuel Langhorne
Keyword(s):  
Drug Release ◽  
Dopamine D2 Receptor ◽  
In Vitro Dissolution ◽  
Molecular Formula ◽  
Dissolution Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Pramipexole Dihydrochloride

Pramipexole dihydrochloride monohydrate is an antiparkinson’s agent which is known as dopamine D2 receptor agonist. It is structurally different from the ergot-derived drugs, e.g. bromocriptine or pergolide. Pramipexole is designated chemically as (S)-2-Amino-4, 5, 6, and 7-tetrahydro-6-(propylamino) benzothiazole and has the molecular formula C10H17N3S. It comes under class I of Biopharmaceutical Classification System. The purpose of this study was to develop and evaluate pramipexole dihydrochloride monohydrate extended release tablets by wet granulation method using different proportions of polymers and binder. Pre-formulation studies were done initially and the results were found to be within the limits. All the mentioned batches were prepared and granules were evaluated for pre-compression parameters such as loss on drying, bulk density, tapped density and compressibility index. Tablets were evaluated for weight variation, thickness, hardness, friability; disintegration time and assay were found to be within the limits. In vitro dissolutions were performed with 0.05M 6.8 PH phosphate buffer and effect of various polymers were explored. Final selection of formulation was based on dissolution profile, from dissolution studies formulation 9 showed 80% drug release within 20 hours, so it will be compared with innovator. Similarity and difference factors which revealed that formulation (F 9) containing HPMC K 200, Eudragit L100 and binder are most successful as it exhibited in vitro drug release that matched with innovator product. In vitro drug release profile reveals that with increased concentration of Eudragit L 100. Accelerated stability studies were performed for the optimized batch which indicated that there were no changes in drug content and in vitro dissolution.

scholarly journals DESIGN AND COMPARATIVE EVALUATION OF CLARITHROMYCIN GASTRIC BIOADHESIVE TABLETS BY EX VIVO AND IN VIVO METHODS

2018 ◽  
Vol 11 (4) ◽  
pp. 248
Author(s):  
Nishad Km ◽  
Arul B ◽  
Rajasekaran S
Keyword(s):  
Controlled Release ◽  
Imaging Technique ◽  
Ex Vivo ◽  
In Vitro Dissolution ◽  
Natural Polymers ◽  
Drug Bioavailability ◽  
X Ray ◽  
X Ray Imaging

 Objective: The present investigation was to formulate controlled release of mucoadhesive clarithromycin tablets using natural polymers.Methods: Tamarind seed polysaccharide obtained from Tamarindus indica and chitosan act as natural polymers. The formulated tablets of the combined form of thrombospondin (TSP) and chitosan were analyzed by in vitro dissolution method. The optimized formulations were selected for ex vivo and in vivo studies and compared with hydroxypropyl methylcellulose K100 polymer by evaluating gastric retention period by X-ray imaging technique, and drug bioavailability by a pharmacokinetic method from blood samples was determined by high-performance liquid chromatography-mass spectrometry method.Results: The gastric mucoadhesive tablets were prepared using chito-TSP polymers. The in vitro drug release showed good release character for 24 h. The ex vivo studies of tablets showed good adhesive property for a long time. The X-ray imaging technique also proved the adhesive character of tablets. From blood serum sample of rabbits, bioavailability of the drug is in according to the controlled release mechanism.Conclusion: The selected formulations were subjected to stability studies. The study concluded that combination of chitosan and TSP is best natural polymer for mucoadhesion by the advantages of controlled release and biodegradation.

scholarly journals CINNARIZINE LIQUID SOLID COMPACTS: PREPARATION EVALUATION

2019 ◽  
Vol 11 (1) ◽  
pp. 150
Author(s):  
Sreenivas Patro Sisinthy ◽  
Shubbaneswarei Selladurai
Keyword(s):  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Dsc Studies ◽  
Weight Variation ◽  
Drug Concentrations ◽  
R Value

Objective: The objective of this research was to formulate cinnarizine tablets using the liquid-solid compact technique to enhance its solubility and dissolution rate.Methods: Cinnarizine liquid-solid compacts were formulated using propylene glycol as the non-volatile solvent, Neusilin US2 as the carrier material, Aerosil 200 as the coating material and croscarmellose sodium as the disintegrant. The interaction between drug and excipients were characterized by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies. Different batches of liquid, solid compacts were prepared by using varying carrier-coating excipient ratio and different concentration of liquid medication. Flow parameters such as bulk density, tapped density, Carr’s Index, Hausner’s Ratio as well as an angle of repose were used to test the flowability of the powder blend. The liquid-solid compacts were produced by direct compression method and were evaluated for tests such as weight variation, drug content, hardness, thickness, friability, wetting time, disintegration time as well as the in vitro dissolution studies.Results: The results of the preformulation studies of liquisolid compacts showed acceptable flow properties. The results of FTIR and DSC studies showed that there is no drug-excipient interactions. The different R values and concentrations were found to have a marked effect on the dissolution profile. Formulations with higher carrier: coating ratio (R-value) and lower drug concentrations displayed a better dissolution profile. The percentage of drug release of F3 with an R-value of 20 and a drug concentration of 10% was found to be 88.11% when compared to the conventional marketed tablet which released only 44.07% at the end of 2 h.Conclusion: From this research, it is inferred that liquid-solid technique is a promising and effective approach that can be used to enhance the dissolution rate of cinnarizine.

scholarly journals BIOEQUIVALENCE STUDY OF ANTIDIABETIC ACTIVITY BETWEEN TWO MARKETED FORMULATIONS OF METFORMIN ON GLUCOCORTICOID-INDUCED HYPERGLYCEMIA IN RABBIT

2017 ◽  
Vol 9 (4) ◽  
pp. 47
Author(s):  
Debanga Das ◽  
Jashabir Chakraborty ◽  
Suvakanta Dash
Keyword(s):  
Blood Glucose ◽  
Normal Saline ◽  
Bioequivalence Study ◽  
In Vitro Dissolution ◽  
Antidiabetic Activity ◽  
Control Group ◽  
In Vitro Tests ◽  
Weight Variation

Objective: Bioequivalence studies are the commonly accepted methods displaying therapeutic equivalence between two products. This study was conducted to evaluate the bioequivalence study of anti-diabetic activity between two formulations of metformin tablets which were marketed in India.Methods: In in vitro study five essential in vitro tests including disintegration, weight variation, hardness, friability and a comparative in vitro dissolution study were performed.Results: For in vivo study adult male rabbits were divided into three groups of two each. The first group is regarded as control group received 3 ml of normal saline daily by using the gastric tube for 15 d and the second and third group received (0.35 mg/Kg B.W. single dosage) of dexamethasone tablets which were powdered, dissolved in 3 ml of normal saline daily for 15 d. After 15 d the blood glucose of second and third group was estimated and after that received formulation X and formulation Y, dissolved in 3 ml of normal saline daily for 15 d at the dose of 0.5 gm/kg body weight orally. After 15 d again blood glucose of second and third group was estimated and compare the results of both the group. This shows the favourable response of metformin against glucocorticoid-induced renal damage and hyperglycemia.Conclusion: Results of this study showed that the extent, rate of absorption and anti-diabetic activity of two different formulations of metformin tablets are bioequivalent to each other.

scholarly journals The In-vitro studies and evaluation of telmisartan marketed tablets

2019 ◽  
Vol 9 (1) ◽  
pp. 74-78
Author(s):  
Jayendra Singh Bayas ◽  
Rameshwar Sanjabrao Cheke ◽  
Prachi Lokhande ◽  
Santosh Waghmare ◽  
Shivshankar Gunjegaonkar ◽  
...  
Keyword(s):  
Effective Means ◽  
Systemic Circulation ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Local Market ◽  
Dissolution Test ◽  
Disintegration Time ◽  
Weight Variation ◽  
Tablet Properties

Tablets or capsules taken orally remain one of the most effective means of treatment available. The effectiveness of such dosage forms relies on the drug dissolving in the fluids of the gastrointestinal tract prior to absorption into the systemic circulation. The present study reveals the evaluation of four marketed sample of Telmisartan tablets. The main aim of the study is to conduct dissolution test on the tablets to determine the compliance with a given official monograph. Four different marketed samples of Telmisartan were purchased from local market. The Telmisartan tablets were evaluated for the various in-vitro tablet properties such as thickness, hardness, friability, weight variation, drug content, disintegration time and dissolution rate. In-vitro dissolution test is conducted on four different brands of telmisartan tablets to assess their equivalency. All the four marketed samples of Telmisartan have shown good tablet properties and comply with the pharmacopoeial specification. The in- vitro dissolution showed the 80% drug release within one hour from all the four brands which complies with the specification of pharmacopoeia.

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