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Preparation and Evaluation of Telmisartan Solid Dispersion as Sublingual Tablets: تحضيير وتقييم حبوب التلميسارتان سريعة التفكك تحت اللسان
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Background: Telmisartan is an antihypertensive angiotensin II receptor antagonist drug commonly used to treat hypertension and renal disease. Based on the Biopharmaceutical Classification System.  It’s a Class II poorly soluble drug.

Objective: To prepare a sublingual tablet by increasing the dissolution and solubility of Telmisartan utilizing the solid dispersion method.

Methods: Three methods were obtained to prepare the solid dispersion of telmisartan: solvent evaporation, Kneading, and microwave method. Each method uses surplus as a hydrophilic carrier in different ratios of 1%, 2%, and 3%. Preparation of ternary solid dispersion by adding potassium carbonate salt to the binary solid dispersion. After that preparing the sublingual tablets by applying a direct compression method, using different types and ratios of superdisintegrants such as crospovidone, croscarmellose and sodium starch glycolate in 5% and 10%.

Study the evaluation tests of sublingual tablets, such as friability, hardness, disintegration time and dissolution time.

Results: The solid dispersion showed an improvement in solubility over the pure medication. The best result was obtained with the formula (Telmisartan, soluplus and k2co3 salt at 1:1:0.3 ratio) prepared by microwave method, in this method and the high ratio of soluplus, the solubility increased more than the solvent evaporation and kneading method. The selected tablet is prepared using crospovidone 10% as a superdisintegrant that appears disintegration time in 5 seconds and releases in 1 min in dissolution media.

Conclusion: The solubility and dissolution of Telmisartan were improved by microwave-based ternary solid dispersion using hydrophilic carriers and salt in a ratio of 1:1:0.3 (drug: carrier: salt). The analysis exerts the increases in wettability, enhanced solubility, and dissolution due to conversion from crystal to amorphous state.

Received May. 2023

Accepted Aug. 2023

Published Jan. 2024

 

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Publication Date
Wed Jul 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Fast Dissolving Tablets of Taste-Masked Ondansetron Hydrochloride by Solid Dispersion
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Ondansetron hydrochloride (ONH) is a very bitter, potent antiemetic drug used for the treatment and/or prophylaxis of chemotherapy or radiotherapy or postoperative induced emesis. The objective of this study is to formulate and evaluate of taste masked fast dissolving tablet (FDTs) of ONH to increase patient compliance.

 ONH taste masked granules were prepared by solid dispersion technique using Eudragit E100 polymer as an inert carrier. Solvent evaporation and fusion melting methods were used for such preparation.

Completely taste masking with zero release of drug in phosphate buffer pH 6.8was obtained from granules prepared by solvent evaporation method using drug: polymer ratio of 1:2, from which four formulas pas

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Publication Date
Sun Jun 02 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Preparation and Evaluation of Solid Dispersion-Based Bilastine Effervescent Granules
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Background: Bilastine (BLA) is a second-generation H1 antihistamine used to treat allergic rhinoconjunctivitis. Because of its limited solubility, it falls under class II of the Biopharmaceutics Classification System (BSC). The solid dispersion (SD) approach significantly improves the solubility and dissolution rate of insoluble medicines. Objective: To improve BLA solubility and dissolution rate by formulating a solid dispersion in the form of effervescent granules. Methods: To create BLA SDs, polyvinylpyrrolidone (PVP K30) and poloxamer 188 (PLX188) were mixed in various ratios (1:5, 1:10, and 1:15) using the kneading technique. All formulations were evaluated based on percent yield, drug content, and saturation solubility. The fo

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Publication Date
Fri Jun 01 2007
Journal Name
Journal Of The College Of Languages (jcl)
David Hare's Teeth 'n' Smiles: A Drama of Disintegration
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David Hare (b.1947) is one of the most critically acclaimed, contemporary British dramatists. A playwright, director and filmmaker, he has written more than thirty plays for the stage and seven original screen plays for cinema and TV (Susan Emerling, p.1). He began his dramatic career in the late sixties. Along with such dramatists as Howard Brenton and Trevor Griffiths, he writes in the aftermath of the "Angry Young Men" tradition of John Osborne. It is a well-known fact that the element of anger continued in the drama of the 1960s and became even more radicalized after the social, cultural and political unrests of 1968 by the dramatists of the "second wave" to whom Hare belongs (John Russell Taylor, p.14). Setting his plays in a variet

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Publication Date
Tue Dec 05 2023
Journal Name
Baghdad Science Journal
Synthesis and Antibacterial Evaluation for Some New Schiff-bases Derived from P-aminoacetanilide
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Derivatives of Schiff-bases possess a great importance in pharmaceutical chemistry. They can be used for synthesizing different types of bioactive compounds. In this paper, derivatives of new Schiff bases have been synthesized from several serial steps. The acid (I) was synthesized from the reaction of dichloroethanoic acid with 2 moles of p-aminoacetanilide. New acid (I) converted to its ester (II) via the reaction of (I) with dimethyl sulphate in the present of anhydrous of sodium carbonate and dry acetone. Acid hydrazide (III) has been synthesized by adding 80% of hydrazine hydrate  to the new ester using ethanol as a solvent. The last step included the preparation of new Schiff-bases (IV-VIII) by the reaction of acid hydrazide with

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Publication Date
Thu Jan 31 2019
Journal Name
Journal Of The College Of Education For Women
Appearances of family Disintegration for Delinquency females
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Family social institution mission in the community, if and repaired Magistrate society and often lead that institution a positive role in the socialization, but a variety of factors ailing infect system family Vtfkdh role effective and influential in society and stands at the forefront of those factors disintegration family, whether caused by the death of one or both parents, divorce or separation, or whether the result of domestic weakness and poor family behavioral practices. And gaining the study of great importance and that the scarcity of studies that address the problem of delinquency female, is no secret that stand on the fact the role of disintegration family in the events of that problem will help and a large degree in the devel

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Publication Date
Tue Mar 30 2021
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Biological Activity Evaluation of Some Pyrazoles, Thiazoles and Oxazoles Derived from 2-Mercaptoaniline
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    Synthesis of 2-mercaptobenzothiazole (A1) is performed from the reaction of  o-aminothiophenol and carbon disulfide CS2 in ethanol under basic condition. Compound (A1)  is reacted with chloro acetyl chloride to give compound (A2). Hydrazide acid compound (A3) is obtained from the reaction of compound (A2) with  hydrazine hydrate in ethanol under reflux in the presence of glacial acetic acid .The reaction of hydrazide acid compound (A3) with ethyl acetoacetate gives pyrazole compound (A4). The new hydrazone  compound (A5) was prepared from the reaction of compound (A3) with  benzaldehyde. Reaction of compound

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Publication Date
Mon Jan 02 2012
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Disease modifying effects of simvastatin &/or telmisartan on pulmonary function in patients with mild to moderate chronic obstructive pulmonary disease(COPD)
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Background: chronic obstructive pulmonary disease (COPD) is characterized by chronic airflow limitation and a range of pathological changes in the lung.

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Publication Date
Thu Nov 30 2023
Journal Name
Research Journal Of Pharmacy And Technology
Preparation and Evaluation of Aceclofenac Solid Dispersion by Fusion Technique and Effervescent Assisted Fusion Technique: Comparative Study
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Solid dispersion (SD) is one of the most widely used methods to resolve issues accompanied by poorly soluble drugs. The present study was carried out to enhance the solubility and dissolution rate of Aceclofenac (ACE), a BCS class II drug with pH-dependent solubility, by the SD method. Effervescent assisted fusion technique (EFSD) using different hydrophilic carriers (mannitol, urea, Soluplus®, poloxamer 188, and poloxamer 407) in the presence of an effervescent base (sodium bicarbonate and citric acid) in different drug: carrier: effervescent base ratio and the conventional fusion technique (FSD) were used to prepare ACE SD. Solubility, dissolution rate, Fourier transformation infrared spectroscopy (FTIR), PowderX-ray diffraction

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Publication Date
Wed May 10 2023
Journal Name
Journal Of Planner And Development
Analysis and evaluation of related factors affecting community Participation as a policy to upgrade residential slums area
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have suffered from deteriorating residential neighborhoods, poor economic, social and urban living conditions of the population and deteriorating the infrastructural and superior services. These problems were the secretions of these cities' rapid urbanization. Based on the principles of sustainable urban planning and in order to achieve adequate opportunities for the lives of the population and provide them with sustainable livelihoods, policies have emerged to upgrade along the lines of community participation and programmes to reform and develop those neighbourhoods, raise their efficiency and make them livable. Thus, the problem of research was identified "The absence of a comprehensive cognitive perception of the most prominent facto

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Publication Date
Mon Jan 01 2024
Journal Name
Journal Of Research In Pharmacy
Formulation and Evaluation of Immediate-Release Tablet Containing Atorvastatin Phospholipid Solid Dispersion
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Oral tablets containing solubilized drug in the presence of appropriate excipients may give us an immediate release of the drug. Phospholipid solid dispersion (PSD) is a branch of solid dispersion in which phospholipid acts as a hydrophilic polymer in the presence of a suitable adsorbent to enhance the solubility of poorly soluble drugs. The anti-hyperlipidemic drug Atorvastatin (ATR) is an example of such drug, as it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Phosphatidylcholine in combination with magnesium aluminum silicate as an adsorbent in a ratio of ATR: PC: MAS 1:3:4 was used to prepare ATR PSD by the solvent evaporation method, the

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