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Journal Details
Format
Journal
eISSN
1846-9558
ISSN
1330-0075
First Published
28 Feb 2007
Publication timeframe
4 times per year
Languages
English

Search

Volume 61 (2011): Issue 2 (June 2011)

Journal Details
Format
Journal
eISSN
1846-9558
ISSN
1330-0075
First Published
28 Feb 2007
Publication timeframe
4 times per year
Languages
English

Search

10 Articles
Open Access

The technologies used for developing orally disintegrating tablets: A review

Published Online: 17 Jun 2011
Page range: 117 - 139

Abstract

The technologies used for developing orally disintegrating tablets: A review

Orally disintegrating tablets (ODTs), also known as fast melts, quick melts, fast disintegrating and orodispersible systems, have the unique property of disintegrating in the mouth in seconds without chewing and the need of water and are thus assumed to improve patient compliance. Conventional methods like direct compression, wet granulation, moulding, spray-drying, freeze-drying and sublimation were used to prepare ODTs. New advanced technologies like Orasolv®, Durasolv®, Wowtab®, Flashtab®, Zydis®, Flashdose®, Oraquick®, Lyoc®, Advatab®, Frosta®, Quick-Disc® and Nanomelt® have been introduced by some pharmaceutical companies for the production of ODTs. The main objective of this review is to give a comprehensive insight into conventional and recent technologies used for the preparation of ODTs.

Keywords

  • orally disintegrating tablet
  • orodispersible tablet
  • superdisintegrant
  • drug delivery
  • fast disintegrating tablet
Open Access

Design and development of paclitaxel-loaded bovine serum albumin nanoparticles for brain targeting

Published Online: 17 Jun 2011
Page range: 141 - 156

Abstract

Design and development of paclitaxel-loaded bovine serum albumin nanoparticles for brain targeting

Bovine serum albumin (BSA) nanoparticles loaded with paclitaxel (PTX) were prepared using a desolvation technique. A 32 full factorial design (FFD) was employed to formulate nanoparticles. Nanoparticles were characterized for particle size by photon correlation spectroscopy and surface morphology by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Encapsulation efficiency, zeta potential and particle yield were also determined. Response surface linear modelling (RSLM) was used to predict the optimal formulation. Various models were applied to determine the release mechanism from PTX nanoparticles. The effect of drug-polymer ratio on the release profile of formulations was observed and was applied to determine the suitability of the predicted optimal formulation. A preliminary study to determine the feasibility of targeting the prepared nanoparticles to brain was also carried out using mice as in vivo models.

Keywords

  • paclitaxel
  • bovine serum albumin
  • nanoparticles
  • desolvation
  • brain targeting
  • factorial design
Open Access

Development and characterization of mucoadhesive patches of salbutamol sulfate for unidirectional buccal drug delivery

Published Online: 17 Jun 2011
Page range: 157 - 170

Abstract

Development and characterization of mucoadhesive patches of salbutamol sulfate for unidirectional buccal drug delivery

Buccal patches of salbutamol sulfate were prepared using five different water soluble polymers in various proportions and combinations using PEG-400/PG as plasticizers. A 32 full factorial design was used to design the experiments for each polymer combination. Patches were laminated on one side with a water impermeable backing layer for unidirectional drug release. The thickness of medicated patches ranged between 0.2 and 0.4 mm and showed an increase in mass whenever PEG-400 was used as plasticizer. The surface pH of all patches approached neutral. Eight formulations which had shown high folding endurance (> 300) were selected for evaluation. Patches prepared with PEG-400 showed a high swelling index. The residence time of the tested patches ranged between 105 and 130 min. Formulations A10, A32, B10 and B32 fitted the Higuchi model best, whereas formulations A19 and B19 showed super case II transport drug release. Stability studies indicated that there was no change in the chemical and physical characteristics during the test period of 6 months.

Keywords

  • salbutamol sulfate
  • mucoadhesive patches
  • buccal drug delivery
  • 3 full factorial design
Open Access

Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivatives

Published Online: 17 Jun 2011
Page range: 171 - 185

Abstract

Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivatives

A series of 6-aryl-5-cyano-2-thiouracil derivatives (1a-d) was synthesized by the reaction of ethyl cyanoacetate with thiourea and aldehydes. These products were used as intermediate compounds for the synthesis of a number of thiouracil derivatives (2a-d to 10a-d). All compounds were screened for antibacterial and antifungal activities. Some of the prepared compounds, 6-(4-fluorophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2a), 4-oxo-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2d), 6-(4-fluorophenyl)-4-hydrazino-2-thioxo-1,2-dihydropyrimidine-5-cabonitrile (7a) and 4-hydrazino-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrimidine-5-carbonitrile (7d) revealed promising antimicrobial activity.

Keywords

  • 6-aryl-5-cyano-2-thiouracil
  • antibacterial activity
  • antifungal activity
Open Access

Synthesis, antibacterial and potential anti-HIV activity of some novel imidazole analogs

Published Online: 17 Jun 2011
Page range: 187 - 201

Abstract

Synthesis, antibacterial and potential anti-HIV activity of some novel imidazole analogs

A series of 1-(2-methyl-4-nitro-imidazol-1-yl)-3-arylaminopropan-2-ones (2a-e), 2-methyl-5-nitro-1-{2-[arylmethoxy] ethyl}-1H-imidazoles (5a-d), and N-(3-hydroxyphenyl)-2-(substituted imidazol-1-yl)alkanamides (8a-e) were synthesized with the aim to develop novel imidazole analogs with broad-spectrum chemotherapeutic properties. Title compounds were evaluated for their anti-HIV and antibacterial activities.

Keywords

  • imidazole
  • reverse transcriptase
  • non-nucleoside reverse transcriptase
  • anti-HIV
  • antibacterial
Open Access

Formulation and evaluation of mucoadhesive glipizide films

Published Online: 17 Jun 2011
Page range: 203 - 216

Abstract

Formulation and evaluation of mucoadhesive glipizide films

Glipizide is mainly absorbed in the proximal areas of the gastrointestinal tract. The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach for prolonged intervals. Polymeric films were designed with various compositions of hydroxypropyl cellulose and polyethylene glycol 400 (PEG 400). Properties of the mucoadhesive film such as tensile strength, percentage elongation, swelling index, moisture content, pH and viscosity of polymeric dispersion, film thickness, content uniformity and mucoadhesion in a simulated gastric environment were characterized. In addition, percentage drug retained in stomach mucosa was estimated using a simulated dynamic stomach system as a function of time. Increase in hydroxypropyl cellulose concentration resulted in a higher tensile strength and elongation at break, while increase in concentration of PEG 400 was reflected in a decrease in tensile strength and increase of elongation at break. Glipizide/hydroxypropyl cellulose/PEG 400 (2.5:1:0.5) (GF5) was found to be the optimal composition for a novel mucoadhesive stomach formulation that showed good peelability, relatively high swelling index, moderate tensile strength, and stayed on rat stomach mucosa up to 8 h. In vivo testing of the mucoadhesive films with glipizide demonstrated a potential hypoglycemic effect.

Keywords

  • glipizide
  • mucoadhesive film
  • factorial design
  • desirability function
  • hypoglycemic effect
Open Access

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

Published Online: 17 Jun 2011
Page range: 217 - 226

Abstract

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h.

Keywords

  • tizanidine hydrochloride
  • gastroretentive drug delivery system
  • floating tablets
  • release kinetics
Open Access

Synthesis, antispasmodic and antidiarrheal activities of some 1-substituted imidazole derivatives

Published Online: 17 Jun 2011
Page range: 227 - 236

Abstract

Synthesis, antispasmodic and antidiarrheal activities of some 1-substituted imidazole derivatives

A series of 1-substituted imidazoles 1a-d and 2a-d were synthesized and screened for antispasmodic and antidiarrheal activities. Antispasmodic activity was tested at various concentrations on isolated tissue preparations; concentration-response curves were plotted and compared with atropine. All compounds were found to inhibit contraction of the guinea pig ileum. Castor oil-induced diarrhea model in rats was used for evaluation of antidiarrheal activity. Parameters such as intestinal transit and volume of intestinal fluid were measured for antidiarrheal activity at 40 mg kg-1 dose and compared with the standard drug loperamide at 6 mg kg-1 dose. Defecation frequency in the test group was found to be significantly lower (p < 0.01) compared to the control group and comparable with that of the standard. The present study reveals that the compounds exert antidiarrheal activity through possible inhibition of intestinal movement and reduction of capillary permeability in the abdominal cavity.

Keywords

  • 1-substituted imidazoles
  • antispasmodic
  • antidiarrheal
  • gastro-intestinal transit
Open Access

Compatibility studies of nateglinide with excipients in immediate release tablets

Published Online: 17 Jun 2011
Page range: 237 - 247

Abstract

Compatibility studies of nateglinide with excipients in immediate release tablets

Experiments were done to assess the compatibility of nateglinide with selected excipients in the development of immediate release tablets of nateglinide by thermal and isothermal stress testing (IST) techniques. To evaluate the drug-excipient compatibility, different techniques such as differential scanning calorimetric (DSC) study, infra-red (IR) spectrophotometric study and isothermal stress testing were adopted. The results of DSC study showed that magnesium stearate exhibited some interaction with nateglinide. However, the results of IR, and IST studies showed that all the excipients used in the formula were compatible with nateglinide. Optimized formulations developed using the compatible excipients were found to be stable over 3 months of accelerated stability studies (40 ± 2°C and 75 ± 5% RH). Overall, compatibility of excipients with nateglinide was successfully evaluated using a combination of thermal and IST methods and the formulations developed using the compatible excipients were found to be stable.

Keywords

  • nateglinide
  • immediate release tablet
  • drug-excipient interaction
Open Access

Application of artificial neural networks in optimizing the fatty alcohol concentration in the formulation of an O/W emulsion

Published Online: 17 Jun 2011
Page range: 249 - 256

Abstract

Application of artificial neural networks in optimizing the fatty alcohol concentration in the formulation of an O/W emulsion

The purpose of this study was to optimize the concentration of a fatty alcohol, in addition to internal phase, for formulating a stable O/W emulsion, by using artificial neural networks (ANNs). Predictions from ANNs are accurate and allow quantification of the relative importance of the inputs. Furthermore, by varying the network topology and parameters it was possible to obtain output values that were close to experimental values. The ANN model's predictive results and the actual output values were compared. R2 values depict the percentage of response variability for the model; R2 value of 0.84 for the model suggested adequate modeling, which is supported by the correlation coefficient value of 0.9445.

Keywords

  • O/W emulsion
  • emulsifier
  • fatty alcohol
  • back propagation network
  • optimization
  • stability
10 Articles
Open Access

The technologies used for developing orally disintegrating tablets: A review

Published Online: 17 Jun 2011
Page range: 117 - 139

Abstract

The technologies used for developing orally disintegrating tablets: A review

Orally disintegrating tablets (ODTs), also known as fast melts, quick melts, fast disintegrating and orodispersible systems, have the unique property of disintegrating in the mouth in seconds without chewing and the need of water and are thus assumed to improve patient compliance. Conventional methods like direct compression, wet granulation, moulding, spray-drying, freeze-drying and sublimation were used to prepare ODTs. New advanced technologies like Orasolv®, Durasolv®, Wowtab®, Flashtab®, Zydis®, Flashdose®, Oraquick®, Lyoc®, Advatab®, Frosta®, Quick-Disc® and Nanomelt® have been introduced by some pharmaceutical companies for the production of ODTs. The main objective of this review is to give a comprehensive insight into conventional and recent technologies used for the preparation of ODTs.

Keywords

  • orally disintegrating tablet
  • orodispersible tablet
  • superdisintegrant
  • drug delivery
  • fast disintegrating tablet
Open Access

Design and development of paclitaxel-loaded bovine serum albumin nanoparticles for brain targeting

Published Online: 17 Jun 2011
Page range: 141 - 156

Abstract

Design and development of paclitaxel-loaded bovine serum albumin nanoparticles for brain targeting

Bovine serum albumin (BSA) nanoparticles loaded with paclitaxel (PTX) were prepared using a desolvation technique. A 32 full factorial design (FFD) was employed to formulate nanoparticles. Nanoparticles were characterized for particle size by photon correlation spectroscopy and surface morphology by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Encapsulation efficiency, zeta potential and particle yield were also determined. Response surface linear modelling (RSLM) was used to predict the optimal formulation. Various models were applied to determine the release mechanism from PTX nanoparticles. The effect of drug-polymer ratio on the release profile of formulations was observed and was applied to determine the suitability of the predicted optimal formulation. A preliminary study to determine the feasibility of targeting the prepared nanoparticles to brain was also carried out using mice as in vivo models.

Keywords

  • paclitaxel
  • bovine serum albumin
  • nanoparticles
  • desolvation
  • brain targeting
  • factorial design
Open Access

Development and characterization of mucoadhesive patches of salbutamol sulfate for unidirectional buccal drug delivery

Published Online: 17 Jun 2011
Page range: 157 - 170

Abstract

Development and characterization of mucoadhesive patches of salbutamol sulfate for unidirectional buccal drug delivery

Buccal patches of salbutamol sulfate were prepared using five different water soluble polymers in various proportions and combinations using PEG-400/PG as plasticizers. A 32 full factorial design was used to design the experiments for each polymer combination. Patches were laminated on one side with a water impermeable backing layer for unidirectional drug release. The thickness of medicated patches ranged between 0.2 and 0.4 mm and showed an increase in mass whenever PEG-400 was used as plasticizer. The surface pH of all patches approached neutral. Eight formulations which had shown high folding endurance (> 300) were selected for evaluation. Patches prepared with PEG-400 showed a high swelling index. The residence time of the tested patches ranged between 105 and 130 min. Formulations A10, A32, B10 and B32 fitted the Higuchi model best, whereas formulations A19 and B19 showed super case II transport drug release. Stability studies indicated that there was no change in the chemical and physical characteristics during the test period of 6 months.

Keywords

  • salbutamol sulfate
  • mucoadhesive patches
  • buccal drug delivery
  • 3 full factorial design
Open Access

Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivatives

Published Online: 17 Jun 2011
Page range: 171 - 185

Abstract

Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivatives

A series of 6-aryl-5-cyano-2-thiouracil derivatives (1a-d) was synthesized by the reaction of ethyl cyanoacetate with thiourea and aldehydes. These products were used as intermediate compounds for the synthesis of a number of thiouracil derivatives (2a-d to 10a-d). All compounds were screened for antibacterial and antifungal activities. Some of the prepared compounds, 6-(4-fluorophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2a), 4-oxo-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2d), 6-(4-fluorophenyl)-4-hydrazino-2-thioxo-1,2-dihydropyrimidine-5-cabonitrile (7a) and 4-hydrazino-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrimidine-5-carbonitrile (7d) revealed promising antimicrobial activity.

Keywords

  • 6-aryl-5-cyano-2-thiouracil
  • antibacterial activity
  • antifungal activity
Open Access

Synthesis, antibacterial and potential anti-HIV activity of some novel imidazole analogs

Published Online: 17 Jun 2011
Page range: 187 - 201

Abstract

Synthesis, antibacterial and potential anti-HIV activity of some novel imidazole analogs

A series of 1-(2-methyl-4-nitro-imidazol-1-yl)-3-arylaminopropan-2-ones (2a-e), 2-methyl-5-nitro-1-{2-[arylmethoxy] ethyl}-1H-imidazoles (5a-d), and N-(3-hydroxyphenyl)-2-(substituted imidazol-1-yl)alkanamides (8a-e) were synthesized with the aim to develop novel imidazole analogs with broad-spectrum chemotherapeutic properties. Title compounds were evaluated for their anti-HIV and antibacterial activities.

Keywords

  • imidazole
  • reverse transcriptase
  • non-nucleoside reverse transcriptase
  • anti-HIV
  • antibacterial
Open Access

Formulation and evaluation of mucoadhesive glipizide films

Published Online: 17 Jun 2011
Page range: 203 - 216

Abstract

Formulation and evaluation of mucoadhesive glipizide films

Glipizide is mainly absorbed in the proximal areas of the gastrointestinal tract. The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach for prolonged intervals. Polymeric films were designed with various compositions of hydroxypropyl cellulose and polyethylene glycol 400 (PEG 400). Properties of the mucoadhesive film such as tensile strength, percentage elongation, swelling index, moisture content, pH and viscosity of polymeric dispersion, film thickness, content uniformity and mucoadhesion in a simulated gastric environment were characterized. In addition, percentage drug retained in stomach mucosa was estimated using a simulated dynamic stomach system as a function of time. Increase in hydroxypropyl cellulose concentration resulted in a higher tensile strength and elongation at break, while increase in concentration of PEG 400 was reflected in a decrease in tensile strength and increase of elongation at break. Glipizide/hydroxypropyl cellulose/PEG 400 (2.5:1:0.5) (GF5) was found to be the optimal composition for a novel mucoadhesive stomach formulation that showed good peelability, relatively high swelling index, moderate tensile strength, and stayed on rat stomach mucosa up to 8 h. In vivo testing of the mucoadhesive films with glipizide demonstrated a potential hypoglycemic effect.

Keywords

  • glipizide
  • mucoadhesive film
  • factorial design
  • desirability function
  • hypoglycemic effect
Open Access

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

Published Online: 17 Jun 2011
Page range: 217 - 226

Abstract

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h.

Keywords

  • tizanidine hydrochloride
  • gastroretentive drug delivery system
  • floating tablets
  • release kinetics
Open Access

Synthesis, antispasmodic and antidiarrheal activities of some 1-substituted imidazole derivatives

Published Online: 17 Jun 2011
Page range: 227 - 236

Abstract

Synthesis, antispasmodic and antidiarrheal activities of some 1-substituted imidazole derivatives

A series of 1-substituted imidazoles 1a-d and 2a-d were synthesized and screened for antispasmodic and antidiarrheal activities. Antispasmodic activity was tested at various concentrations on isolated tissue preparations; concentration-response curves were plotted and compared with atropine. All compounds were found to inhibit contraction of the guinea pig ileum. Castor oil-induced diarrhea model in rats was used for evaluation of antidiarrheal activity. Parameters such as intestinal transit and volume of intestinal fluid were measured for antidiarrheal activity at 40 mg kg-1 dose and compared with the standard drug loperamide at 6 mg kg-1 dose. Defecation frequency in the test group was found to be significantly lower (p < 0.01) compared to the control group and comparable with that of the standard. The present study reveals that the compounds exert antidiarrheal activity through possible inhibition of intestinal movement and reduction of capillary permeability in the abdominal cavity.

Keywords

  • 1-substituted imidazoles
  • antispasmodic
  • antidiarrheal
  • gastro-intestinal transit
Open Access

Compatibility studies of nateglinide with excipients in immediate release tablets

Published Online: 17 Jun 2011
Page range: 237 - 247

Abstract

Compatibility studies of nateglinide with excipients in immediate release tablets

Experiments were done to assess the compatibility of nateglinide with selected excipients in the development of immediate release tablets of nateglinide by thermal and isothermal stress testing (IST) techniques. To evaluate the drug-excipient compatibility, different techniques such as differential scanning calorimetric (DSC) study, infra-red (IR) spectrophotometric study and isothermal stress testing were adopted. The results of DSC study showed that magnesium stearate exhibited some interaction with nateglinide. However, the results of IR, and IST studies showed that all the excipients used in the formula were compatible with nateglinide. Optimized formulations developed using the compatible excipients were found to be stable over 3 months of accelerated stability studies (40 ± 2°C and 75 ± 5% RH). Overall, compatibility of excipients with nateglinide was successfully evaluated using a combination of thermal and IST methods and the formulations developed using the compatible excipients were found to be stable.

Keywords

  • nateglinide
  • immediate release tablet
  • drug-excipient interaction
Open Access

Application of artificial neural networks in optimizing the fatty alcohol concentration in the formulation of an O/W emulsion

Published Online: 17 Jun 2011
Page range: 249 - 256

Abstract

Application of artificial neural networks in optimizing the fatty alcohol concentration in the formulation of an O/W emulsion

The purpose of this study was to optimize the concentration of a fatty alcohol, in addition to internal phase, for formulating a stable O/W emulsion, by using artificial neural networks (ANNs). Predictions from ANNs are accurate and allow quantification of the relative importance of the inputs. Furthermore, by varying the network topology and parameters it was possible to obtain output values that were close to experimental values. The ANN model's predictive results and the actual output values were compared. R2 values depict the percentage of response variability for the model; R2 value of 0.84 for the model suggested adequate modeling, which is supported by the correlation coefficient value of 0.9445.

Keywords

  • O/W emulsion
  • emulsifier
  • fatty alcohol
  • back propagation network
  • optimization
  • stability

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