Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen

Daravath, Bhaskar; Tadikonda, Rama Rao; Vemula, Sateesh Kumar

doi:10.3109/03639045.2014.940963

Cited by 20 publications

(15 citation statements)

References 14 publications

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“…tions that are achieved with normal therapeutic doses (11)(12)(13)(14). In contrast, the usual therapeutic plasma levels of acetaminophen are lower than the concentration at which inhibition of bacterial growth has been shown (15).…”

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confidence: 87%

Antimicrobial Effects of Antipyretics

Zimmermann

Curtis

2017

Antimicrob Agents Chemother

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Antipyretics are some of the most commonly used drugs. Since they are often coadministered with antimicrobial therapy, it is important to understand the interactions between these two classes of drugs. Our review is the first to summarize the antimicrobial effects of antipyretic drugs and the underlying mechanisms involved. Antipyretics can inhibit virus replication, inhibit or promote bacterial or fungal growth, alter the expression of virulence factors, change the surface hydrophobicity of microbes, influence biofilm production, affect the motility, adherence, and metabolism of pathogens, interact with the transport and release of antibiotics by leukocytes, modify the susceptibility of bacteria to antibiotics, and induce or reduce the frequency of mutations leading to antimicrobial resistance. While antipyretics may compromise the efficacy of antimicrobial therapy, they can also be beneficial, for example, in the management of biofilm-associated infections, in reducing virulence factors, in therapy of resistant pathogens, and in inducing synergistic effects. In an era where it is becoming increasingly difficult to find new antimicrobial drugs, targeting virulence factors, enhancing the efficacy of antimicrobial therapy, and reducing resistance may be important strategies.

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confidence: 87%

Antimicrobial Effects of Antipyretics

Zimmermann

Curtis

2017

Antimicrob Agents Chemother

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“…Dissolution of griseofulvin from the SD was 11-times greater than that of the pure drug at a ratio of griseofulvin: PVP (1:20). This method has been used to improve solubility of many drugs such as azithromycin [91], tectorigenin [92], flurbiprofen [93], cilostazol [94], ticagrelor [95], piroxicam [96], indomethacin [97], loratadine [98], diclofenac [68], abietic acid [99], efavirenz [100], and repaglinide [101] (Table 1). An SD of tectorigenin, PVP, and PEG 4000 at a weight ratio of 7:54:9 was prepared using solvent evaporation to increase dissolution and BA [92].…”

Section: Solid Dispersionsmentioning

confidence: 99%

Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs

et al. 2019

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Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic anticancer drugs) based on effectiveness and safety profile. Biologic drugs are administered by intravenous (IV) injection due to their large molecular weight, while small molecule drugs are preferentially administered by gastrointestinal route. Even though IV injection is the fastest route of administration and ensures complete bioavailability, this route of administration causes patient inconvenience to visit a hospital for anticancer treatments. In addition, IV administration can cause several side effects such as severe hypersensitivity, myelosuppression, neutropenia, and neurotoxicity. Oral administration is the preferred route for drug delivery due to several advantages such as low cost, pain avoidance, and safety. The main problem of NCEs is a limited aqueous solubility, resulting in poor absorption and low bioavailability. Therefore, improving oral bioavailability of poorly water-soluble drugs is a great challenge in the development of pharmaceutical dosage forms. Several methods such as solid dispersion, complexation, lipid-based systems, micronization, nanonization, and co-crystals were developed to improve the solubility of hydrophobic drugs. Recently, solid dispersion is one of the most widely used and successful techniques in formulation development. This review mainly discusses classification, methods for preparation of solid dispersions, and use of solid dispersion for improving solubility of poorly soluble anticancer drugs.

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“…Development of oral solid dosage forms using insoluble drugs with the help of different methods is not only to enhance the solubility and dissolution rate of poor soluble drugs but also to improve the therapeutic efficacy (Chaitanya et al, 2014;Vemula and Katkum, 2014). Development of fast dissolving tablets can be achieved by various conventional methods like direct compression, wet granulation, spray drying, freeze drying, and sublimation (Seager, 1998;Hirani et al, 2009;Daravath Among the different methods, use of superdisintegrants is one of the easiest and successful methods to enhance the dissolution rate. Formulation of fast dissolving tablets by integrating superdisintegrants is a user friendly, convenient and industry feasible method (Neduri 2013).…”

Section: Introductionmentioning

confidence: 99%

Effect of Combination of Superdisintegrants on the Dissolution Rate: Meclizine Hydrochloride Fast Dissolving Tablets

Vemula¹,

Paulos²,

Kebamo³

2015

Sci. Technol. Arts Res. J.

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The aim of the present research is to develop the fast dissolving tablets and to study the effect of combination of superdisintegrants on the dissolution rate by using meclizine hydrochloride as a model drug. Development of oral fast dissolving tablets is achieve the following objectives; they are to give fast onset of action and to overcome difficulty in swallowing tablets and capsules that resulting in non tablets were characterized for hardness, weight variation, friabi absorption ratio, and disintegration time. using USP XXIV Type II dissolution apparatus in 0.1 N HCl. From the formulation F3 (3% crosscarmellose and 3% about 99.34% in 15 min, and disintegration time 39 sec when compared with others. The percent drug release in 15 min (Q15) and initial dissolution rate for formulation F3 was 99.34±0.56%, 6.54%/min. These were ve (36.48±0.82%, 2.43%/min). The dissolution efficiency was found to be increased by 3.5 fold with F3 formulation compared to control tablet. From the stability studies, the similarity index was found to be above 50 that indicates the stability of tablets. In conclusion, development of meclizine hydrochloride fast dissolving tablets using combination of superdisintegrants is showed improved results rather than the tablets with individual superdisintegrants. Further the efficacy of the developed formulations has to be assessed by pharmacokinetic studies. Copyright@2015 STAR Journal

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Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen

Abstract: From the above results, it is concluded that the formulation of gelucire 44/14 solid dispersions is able to improve the solubility, dissolution rate as well as the absorption rate of flurbiprofen than pure form of drug.

Cited by 20 publications

References 14 publications

Antimicrobial Effects of Antipyretics

Antimicrobial Effects of Antipyretics

Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs

Effect of Combination of Superdisintegrants on the Dissolution Rate: Meclizine Hydrochloride Fast Dissolving Tablets

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