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Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
ISSN
1330-0075
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

Volume 63 (2013): Edizione 3 (September 2013)

Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
ISSN
1330-0075
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

10 Articoli
Accesso libero

Drug interactions with statins

Pubblicato online: 22 Oct 2013
Pagine: 277 - 293

Astratto

Abstract

The 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) are generally well tolerated as monotherapy. Statins are associated with two important adverse effects, asymptomatic elevation in liver enzymes and myopathy. Myopathy is most likely to occur when statins are administered with other drugs. Statins are substrates of multiple drug transporters (including OAT- -P1B1, BCRP and MDR1) and several cytochrome P450 (CYP) enzymes (including CYP3A4, CYP2C8, CYP2C19, and CYP2C9). Possible adverse effects of statins can occur due to interactions in concomitant use of drugs that substantially inhibit or induce their methabolic pathway. This review summarizes the most important interactions of statins.

Parole chiave

  • statins
  • drug interactions
  • cytochrome P450 (CYP) enzymes
  • drug transporters
  • adverse effects
Accesso libero

Nanofibers and their biomedical use

Pubblicato online: 22 Oct 2013
Pagine: 295 - 304

Astratto

Abstract

The idea of creating replacement for damaged or diseased tissue, which will mimic the physiological conditions and simultaneously promote regeneration by patients’ own cells, has been a major challenge in the biomedicine for more than a decade. Therefore, nanofibers are a promising solution to address these challenges. These are solid polymer fibers with nanosized diameter, which show improved properties compared to the materials of larger dimensions or forms and therefore cause different biological responses. On the nanometric level, nanofibers provide a biomimetic environment, on the micrometric scale three-dimensional architecture with the desired surface properties regarding the intended application within the body, while on the macrometric scale mechanical strength and physiological acceptability. In the review, the development of nanofibers as tissue scaffolds, modern wound dressings for chronic wound therapy and drug delivery systems is highlighted. Research substantiates the effectiveness of nanofibers for enhanced tissue regeneration, but ascertains that evidences from clinical studies are currently lacking. Nevertheless, due to the development of nano- and bio-sciences, products on the market can be expected in the near future.

Parole chiave

  • nanofibers
  • tissue engineering
  • wound dressings
  • drug delivery systems
  • analogues of ECM
Accesso libero

Methods of amorphization and investigation of the amorphous state

Pubblicato online: 22 Oct 2013
Pagine: 305 - 334

Astratto

Abstract

The amorphous form of pharmaceutical materials represents the most energetic solid state of a material. It provides advantages in terms of dissolution rate and bioavailability. This review presents the methods of solid- -state amorphization described in literature (supercooling of liquids, milling, lyophilization, spray drying, dehydration of crystalline hydrates), with the emphasis on milling. Furthermore, we describe how amorphous state of pharmaceuticals differ depending on the method of preparation and how these differences can be screened by a variety of spectroscopic (X-ray powder diffraction, solid state nuclear magnetic resonance, atomic pairwise distribution, infrared spectroscopy, terahertz spectroscopy) and calorimetry methods.

Parole chiave

  • amorphous solid preparation
  • crystallinity
  • spectroscopy
  • calorimetry
Accesso libero

Cyclodextrin based nanosponges for pharmaceutical use: A review

Pubblicato online: 22 Oct 2013
Pagine: 335 - 358

Astratto

Abstract

Nanosponges are a novel class of hyper-crosslinked polymer based colloidal structures consisting of solid nanoparticles with colloidal sizes and nanosized cavities. These nano-sized colloidal carriers have been recently developed and proposed for drug delivery, since their use can solubilize poorly water-soluble drugs and provide prolonged release as well as improve a drug’s bioavailability by modifying the pharmacokinetic parameters of actives. Development of nanosponges as drug delivery systems, with special reference to cyclodextrin based nanosponges, is presented in this article. In the current review, attempts have been made to illustrate the features of cyclodextrin based nanosponges and their applications in pharmaceutical formulations. Special emphasis has been placed on discussing the methods of preparation, characterization techniques and applications of these novel drug delivery carriers for therapeutic purposes. Nanosponges can be referred to as solid porous particles having a capacity to load drugs and other actives into their nanocavity; they can be formulated as oral, parenteral, topical or inhalation dosage forms. Nanosponges offer high drug loading compared to other nanocarriers and are thus suitable for solving issues related to stability, solubility and delayed release of actives. Controlled release of the loaded actives and solubility enhancement of poorly water-soluble drugs are major advantages of nanosponge drug delivery systems.

Parole chiave

  • nanosponges
  • solubility enhancement
  • cyclodextrin
Accesso libero

Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

Pubblicato online: 22 Oct 2013
Pagine: 359 - 372

Astratto

Abstract

The aim of the present investigation was to prepare and evaluate novel bioadhesive vaginal tablets containing clotrimazole loaded microspheres in order to provide long-term therapeutic activity at the site of infection. Tablets were prepared by incorporating drug loaded microspheres and using bioadhesive polymers hydroxypropylmethylcellulose, sodium carboxymethylcellulose and Carbopol. Microspheres were prepared by the spray drying technique using Eudragit RS-100 and Eudragit RL-100. Microspheres were characterized by SEM, DSC, FTIR, particle size analysis and evaluated for percentage yield, drug loading, encapsulation efficiency and in vitro drug release. To achieve bioadhesion to the mucosal tissue, optimized microspheres were incorporated into bioadhesive tablets and were evaluated for in vitro drug release, in vitro and in vivo mucoadhesion. FTIR and DSC studies showed that no chemical interaction occurred between the drug and polymers. The sphericity factor indicated that the prepared microspheres were spherical. Formulation Mt6 indicated a controlled in vitro drug release and good bioadhesive strength. The in vivo images confirmed the bioadhesion and retention property of tablets up to 24 h. The results indicated that this drug delivery system can be explored for controlled intravaginal drug release.

Parole chiave

  • clotrimazole
  • microspheres
  • bioadhesive vaginal tablet
Accesso libero

Quantification of ascorbic acid and sodium ascorbate in powder blends for tableting and in vitamin C chewable tablets by NIR-chemometry

Pubblicato online: 22 Oct 2013
Pagine: 373 - 384

Astratto

Abstract

The paper proposes a near infrared method able to directly and simultaneously quantify ascorbic acid and sodium ascorbate in powder blends for tableting and in vitamin C chewable tablets without any sample preparation. In the first step, calibration models for the quantification of ascorbic acid and sodium ascorbate in powder blends for tableting and subsequently in chewable vitamin C tablets (corresponding to 80-120 % active substance) were developed according to an experimental design with 2 variables and 5 levels. Then, using the best calibration models, the methods were fully validated in terms of recovery, precision and accuracy for both powder blends and vitamin C chewable tablets. The validated concentration range was 15.14-18.51 % for ascorbic acid and 12.06-14.49 % for sodium ascorbate in powder blends and 91.85-111.03 mg per tablet for ascorbic acid and 71.01-84.50 mg per tablet for sodium ascorbate in tablets. Validation results showed good precision and accuracy.

Parole chiave

  • NIR spectroscopy
  • chemometrics
  • ascorbic acid
  • sodium ascorbate
  • validation
  • powder blends
Accesso libero

Synthesis of the impurities during the manufacture of bulk drug midazolam and separation of these impurities by HPLC

Pubblicato online: 22 Oct 2013
Pagine: 385 - 396

Astratto

Abstract

During the manufacture of bulk drug midazolam various impurities arised that can be the related products or degradation products. Structures of eight impurities that can arise during the manufacture of bulk drug midazolam were proposed. In the present work, synthesis of these impurities and their characterization by different spectroscopic techniques have been done. HPLC method was developed for the separation of impurities from the bulk drug. The developed method separates midazolam from its eight impurities/degradation products within a run time of 45 min.

Parole chiave

  • midazolam
  • impurities
  • degradation products
  • HPLC method
Accesso libero

Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones

Pubblicato online: 22 Oct 2013
Pagine: 397 - 408

Astratto

Abstract

A series of novel 5-alkyl/aryl thiadiazole substituted thiazolidin-4-ones were synthesized by a two-step process. In the first step, 5-alkyl/aryl substituted 2-aminothiadiazoles were synthesized, which on reaction with substituted aromatic aldehydes and thioglycolic acid in the presence of dicyclohexylcarbodiimide afforded thiazolidin- 4-ones. All the compounds were synthesized in fairly good yields and their structures were confirmed by spectral and physical data. The title compounds were screened for in vitro anti-proliferative activity on human breast adenocarcinoma cells (MCF-7) by MTT assay. Most of the derivatives showed an IC50 less than 150 μmol L-1. Among the compounds tested, 2-(2-nitrophenyl)- 3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3f), 2-(3-fluorophenyl)-3-(5-methyl-1,3,4-thiadiazol-2- -yl)-thiazolidin-4-one (3b), and 2-(4-chlorophenyl)-3- -(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3c) were found to be the most active derivatives with IC50 values of 46.34, 66.84, and 60.71 μmol L-1, respectively. Antioxidant studies of all the synthesized compounds were carried out by diphenylpicrylhydrazyl (DPPH) assay. Among the compounds tested, 2-phenyl-3-(5-styryl- -1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3s) elicited superior antioxidant activity with IC50 of 161.93 μmol L-1.

Parole chiave

  • thiadiazole
  • thiazolidin-4-ones
  • anticancer
  • antioxidant
Accesso libero

A convenient synthesis of new NSAID esters containing amino acid, urea and amide moieties

Pubblicato online: 22 Oct 2013
Pagine: 409 - 418

Astratto

Abstract

A convenient synthetic method for the preparation of novel NSAID twin esters 6a-i containing amino acid residue, urea and amide moieties has been developed. The synthetic pathway applied for the preparation of target compounds and key intermediates 1-benzotriazolecarboxylic acid chloride (1), NSAID benzotriazolides 2a-c and N-(1-benzotriazolecarbonyl)-amino acids 3a-d involved benzotriazole as a synthetic auxiliary. The final preparation step of esters 6a-i included the solvent-free reaction of compounds 2a-c with amino acid derivatives 5a-g, bearing two hydroxyl groups, one at each terminal, beside urea and amide functionalities.

Parole chiave

  • NSAID
  • ester
  • amino acid
  • benzotriazole
  • urea
  • amide
Accesso libero

Development and validation of RP HPLC method for determination of betamethasone dipropionate in gingival crevicular fluid

Pubblicato online: 22 Oct 2013
Pagine: 419 - 426

Astratto

Abstract

A simple RP HPLC method for quantification of betamethasone dipropionate (BDP) in gingival crevicular fluid (GCF) has been developed and validated. GCF represents a valuable matrix for therapeutic monitoring of drugs used in the treatment of periodontal disease. The proposed method involves single step extraction for sample preparation. The calibration curve for BDP was linear over the concentration range of 0.10-2.00 μg mL-1 (R2 = 0.9971). RSD values of intra- and inter-day precision ranged 2.2-4.5 and 1.6-5.7 %, while accuracy values were higher than 96.6 and 97.0 %, respectively. The described method can be successfully applied for determination of betamethasone concentrations in GCF obtained from patients with chronic periodontitis after local treatment with BDP cream 0.5 mg g-1.

Parole chiave

  • betamethasone dipropionate
  • gingival crevicular fluid
  • HPLC
  • periodontal disease
10 Articoli
Accesso libero

Drug interactions with statins

Pubblicato online: 22 Oct 2013
Pagine: 277 - 293

Astratto

Abstract

The 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) are generally well tolerated as monotherapy. Statins are associated with two important adverse effects, asymptomatic elevation in liver enzymes and myopathy. Myopathy is most likely to occur when statins are administered with other drugs. Statins are substrates of multiple drug transporters (including OAT- -P1B1, BCRP and MDR1) and several cytochrome P450 (CYP) enzymes (including CYP3A4, CYP2C8, CYP2C19, and CYP2C9). Possible adverse effects of statins can occur due to interactions in concomitant use of drugs that substantially inhibit or induce their methabolic pathway. This review summarizes the most important interactions of statins.

Parole chiave

  • statins
  • drug interactions
  • cytochrome P450 (CYP) enzymes
  • drug transporters
  • adverse effects
Accesso libero

Nanofibers and their biomedical use

Pubblicato online: 22 Oct 2013
Pagine: 295 - 304

Astratto

Abstract

The idea of creating replacement for damaged or diseased tissue, which will mimic the physiological conditions and simultaneously promote regeneration by patients’ own cells, has been a major challenge in the biomedicine for more than a decade. Therefore, nanofibers are a promising solution to address these challenges. These are solid polymer fibers with nanosized diameter, which show improved properties compared to the materials of larger dimensions or forms and therefore cause different biological responses. On the nanometric level, nanofibers provide a biomimetic environment, on the micrometric scale three-dimensional architecture with the desired surface properties regarding the intended application within the body, while on the macrometric scale mechanical strength and physiological acceptability. In the review, the development of nanofibers as tissue scaffolds, modern wound dressings for chronic wound therapy and drug delivery systems is highlighted. Research substantiates the effectiveness of nanofibers for enhanced tissue regeneration, but ascertains that evidences from clinical studies are currently lacking. Nevertheless, due to the development of nano- and bio-sciences, products on the market can be expected in the near future.

Parole chiave

  • nanofibers
  • tissue engineering
  • wound dressings
  • drug delivery systems
  • analogues of ECM
Accesso libero

Methods of amorphization and investigation of the amorphous state

Pubblicato online: 22 Oct 2013
Pagine: 305 - 334

Astratto

Abstract

The amorphous form of pharmaceutical materials represents the most energetic solid state of a material. It provides advantages in terms of dissolution rate and bioavailability. This review presents the methods of solid- -state amorphization described in literature (supercooling of liquids, milling, lyophilization, spray drying, dehydration of crystalline hydrates), with the emphasis on milling. Furthermore, we describe how amorphous state of pharmaceuticals differ depending on the method of preparation and how these differences can be screened by a variety of spectroscopic (X-ray powder diffraction, solid state nuclear magnetic resonance, atomic pairwise distribution, infrared spectroscopy, terahertz spectroscopy) and calorimetry methods.

Parole chiave

  • amorphous solid preparation
  • crystallinity
  • spectroscopy
  • calorimetry
Accesso libero

Cyclodextrin based nanosponges for pharmaceutical use: A review

Pubblicato online: 22 Oct 2013
Pagine: 335 - 358

Astratto

Abstract

Nanosponges are a novel class of hyper-crosslinked polymer based colloidal structures consisting of solid nanoparticles with colloidal sizes and nanosized cavities. These nano-sized colloidal carriers have been recently developed and proposed for drug delivery, since their use can solubilize poorly water-soluble drugs and provide prolonged release as well as improve a drug’s bioavailability by modifying the pharmacokinetic parameters of actives. Development of nanosponges as drug delivery systems, with special reference to cyclodextrin based nanosponges, is presented in this article. In the current review, attempts have been made to illustrate the features of cyclodextrin based nanosponges and their applications in pharmaceutical formulations. Special emphasis has been placed on discussing the methods of preparation, characterization techniques and applications of these novel drug delivery carriers for therapeutic purposes. Nanosponges can be referred to as solid porous particles having a capacity to load drugs and other actives into their nanocavity; they can be formulated as oral, parenteral, topical or inhalation dosage forms. Nanosponges offer high drug loading compared to other nanocarriers and are thus suitable for solving issues related to stability, solubility and delayed release of actives. Controlled release of the loaded actives and solubility enhancement of poorly water-soluble drugs are major advantages of nanosponge drug delivery systems.

Parole chiave

  • nanosponges
  • solubility enhancement
  • cyclodextrin
Accesso libero

Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

Pubblicato online: 22 Oct 2013
Pagine: 359 - 372

Astratto

Abstract

The aim of the present investigation was to prepare and evaluate novel bioadhesive vaginal tablets containing clotrimazole loaded microspheres in order to provide long-term therapeutic activity at the site of infection. Tablets were prepared by incorporating drug loaded microspheres and using bioadhesive polymers hydroxypropylmethylcellulose, sodium carboxymethylcellulose and Carbopol. Microspheres were prepared by the spray drying technique using Eudragit RS-100 and Eudragit RL-100. Microspheres were characterized by SEM, DSC, FTIR, particle size analysis and evaluated for percentage yield, drug loading, encapsulation efficiency and in vitro drug release. To achieve bioadhesion to the mucosal tissue, optimized microspheres were incorporated into bioadhesive tablets and were evaluated for in vitro drug release, in vitro and in vivo mucoadhesion. FTIR and DSC studies showed that no chemical interaction occurred between the drug and polymers. The sphericity factor indicated that the prepared microspheres were spherical. Formulation Mt6 indicated a controlled in vitro drug release and good bioadhesive strength. The in vivo images confirmed the bioadhesion and retention property of tablets up to 24 h. The results indicated that this drug delivery system can be explored for controlled intravaginal drug release.

Parole chiave

  • clotrimazole
  • microspheres
  • bioadhesive vaginal tablet
Accesso libero

Quantification of ascorbic acid and sodium ascorbate in powder blends for tableting and in vitamin C chewable tablets by NIR-chemometry

Pubblicato online: 22 Oct 2013
Pagine: 373 - 384

Astratto

Abstract

The paper proposes a near infrared method able to directly and simultaneously quantify ascorbic acid and sodium ascorbate in powder blends for tableting and in vitamin C chewable tablets without any sample preparation. In the first step, calibration models for the quantification of ascorbic acid and sodium ascorbate in powder blends for tableting and subsequently in chewable vitamin C tablets (corresponding to 80-120 % active substance) were developed according to an experimental design with 2 variables and 5 levels. Then, using the best calibration models, the methods were fully validated in terms of recovery, precision and accuracy for both powder blends and vitamin C chewable tablets. The validated concentration range was 15.14-18.51 % for ascorbic acid and 12.06-14.49 % for sodium ascorbate in powder blends and 91.85-111.03 mg per tablet for ascorbic acid and 71.01-84.50 mg per tablet for sodium ascorbate in tablets. Validation results showed good precision and accuracy.

Parole chiave

  • NIR spectroscopy
  • chemometrics
  • ascorbic acid
  • sodium ascorbate
  • validation
  • powder blends
Accesso libero

Synthesis of the impurities during the manufacture of bulk drug midazolam and separation of these impurities by HPLC

Pubblicato online: 22 Oct 2013
Pagine: 385 - 396

Astratto

Abstract

During the manufacture of bulk drug midazolam various impurities arised that can be the related products or degradation products. Structures of eight impurities that can arise during the manufacture of bulk drug midazolam were proposed. In the present work, synthesis of these impurities and their characterization by different spectroscopic techniques have been done. HPLC method was developed for the separation of impurities from the bulk drug. The developed method separates midazolam from its eight impurities/degradation products within a run time of 45 min.

Parole chiave

  • midazolam
  • impurities
  • degradation products
  • HPLC method
Accesso libero

Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones

Pubblicato online: 22 Oct 2013
Pagine: 397 - 408

Astratto

Abstract

A series of novel 5-alkyl/aryl thiadiazole substituted thiazolidin-4-ones were synthesized by a two-step process. In the first step, 5-alkyl/aryl substituted 2-aminothiadiazoles were synthesized, which on reaction with substituted aromatic aldehydes and thioglycolic acid in the presence of dicyclohexylcarbodiimide afforded thiazolidin- 4-ones. All the compounds were synthesized in fairly good yields and their structures were confirmed by spectral and physical data. The title compounds were screened for in vitro anti-proliferative activity on human breast adenocarcinoma cells (MCF-7) by MTT assay. Most of the derivatives showed an IC50 less than 150 μmol L-1. Among the compounds tested, 2-(2-nitrophenyl)- 3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3f), 2-(3-fluorophenyl)-3-(5-methyl-1,3,4-thiadiazol-2- -yl)-thiazolidin-4-one (3b), and 2-(4-chlorophenyl)-3- -(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3c) were found to be the most active derivatives with IC50 values of 46.34, 66.84, and 60.71 μmol L-1, respectively. Antioxidant studies of all the synthesized compounds were carried out by diphenylpicrylhydrazyl (DPPH) assay. Among the compounds tested, 2-phenyl-3-(5-styryl- -1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3s) elicited superior antioxidant activity with IC50 of 161.93 μmol L-1.

Parole chiave

  • thiadiazole
  • thiazolidin-4-ones
  • anticancer
  • antioxidant
Accesso libero

A convenient synthesis of new NSAID esters containing amino acid, urea and amide moieties

Pubblicato online: 22 Oct 2013
Pagine: 409 - 418

Astratto

Abstract

A convenient synthetic method for the preparation of novel NSAID twin esters 6a-i containing amino acid residue, urea and amide moieties has been developed. The synthetic pathway applied for the preparation of target compounds and key intermediates 1-benzotriazolecarboxylic acid chloride (1), NSAID benzotriazolides 2a-c and N-(1-benzotriazolecarbonyl)-amino acids 3a-d involved benzotriazole as a synthetic auxiliary. The final preparation step of esters 6a-i included the solvent-free reaction of compounds 2a-c with amino acid derivatives 5a-g, bearing two hydroxyl groups, one at each terminal, beside urea and amide functionalities.

Parole chiave

  • NSAID
  • ester
  • amino acid
  • benzotriazole
  • urea
  • amide
Accesso libero

Development and validation of RP HPLC method for determination of betamethasone dipropionate in gingival crevicular fluid

Pubblicato online: 22 Oct 2013
Pagine: 419 - 426

Astratto

Abstract

A simple RP HPLC method for quantification of betamethasone dipropionate (BDP) in gingival crevicular fluid (GCF) has been developed and validated. GCF represents a valuable matrix for therapeutic monitoring of drugs used in the treatment of periodontal disease. The proposed method involves single step extraction for sample preparation. The calibration curve for BDP was linear over the concentration range of 0.10-2.00 μg mL-1 (R2 = 0.9971). RSD values of intra- and inter-day precision ranged 2.2-4.5 and 1.6-5.7 %, while accuracy values were higher than 96.6 and 97.0 %, respectively. The described method can be successfully applied for determination of betamethasone concentrations in GCF obtained from patients with chronic periodontitis after local treatment with BDP cream 0.5 mg g-1.

Parole chiave

  • betamethasone dipropionate
  • gingival crevicular fluid
  • HPLC
  • periodontal disease

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