Papers by Faisal Al-akayleh
he combined properties of SepineoP 600 (S600), a self-gelling dispersion and SepineoSE 68
(M68), ... more he combined properties of SepineoP 600 (S600), a self-gelling dispersion and SepineoSE 68
(M68), a natural liquid crystal forming surfactant, were utilized in the development of emulgel
base for topical application. The emulgels were prepared in water alone or combined with
propylene glycol (PG), polyethylene glycol 400 (PEG400) and glycerol (G) as cosolvents.
Emulgels were characterized for their optical and flow behavior. Two model drugs: caffeine (CF)
and methylparaben (MP) were used in the evaluation of drug permeation across the stratum
corneum (SC). The results showed that emulgel prepared using 70% PG:water (1:1) and 30%
S600 has the best flow behavior compared to other cosolvents. Also the permeability
coefficient of CF was found to be higher than that of MP and the addition of 3% M68 improved
the physical stability of the emulgel, but it did not affect the drug diffusion profile.
A simple, economical, precise, accurate, and rapid HPLC method has been developed and validated f... more A simple, economical, precise, accurate, and rapid HPLC method has been developed and validated for assay determination of ca
and imidapril simultaneously in their raw material and tablet dosage forms. The chromatographic
acetonitrile and phosphate buffer (25:75 v/v) ratio. The detection of Prills drugs was carried out at 210 nm with a flow rate
retention times for lisinopril, captopril and imidapril were 3.6, 4.4,
by recovery studies. The proposed method was successfully employed for the estimatio
ABSTRACT
Directly compressed matrices were produced using a binary mixture of different chitosan ... more ABSTRACT
Directly compressed matrices were produced using a binary mixture of different chitosan (CH) and xanthan gum
(XG) ratios. These hydrophilic excipients were used to control the release of ambroxol HCl. CH and XG were
investigated at three ratios of 1:1, 1:4 and 4:1. Mucosolvan LA® was used as a commercially available reference
product. The optimal CH to XG ratio was 1:1 and the optimal drug to polymer ratio was 1:3. Matrix erosion,
hydration and drug release studies were carried out using a dissolution apparatus (basket method). The release
mechanism is also discussed.
Abstract: The performance of the novel chitin metal silicate (CMS) co-precipitates as a
single mu... more Abstract: The performance of the novel chitin metal silicate (CMS) co-precipitates as a
single multifunctional excipient in tablet formulation using direct compression and wet
granulation methods is evaluated. The neutral, acidic, and basic drugs Spironolactone
(SPL), ibuprofen (IBU) and metronidazole (MET), respectively, were used as model drugs.
Commercial Aldactone®, Fleximex® and Dumazole® tablets containing SPL, IBU and
MET, respectively, and tablets made using Avicel® 200, were used in the study for
comparison purposes. Tablets of acceptable crushing strength (>40 N) were obtained using
CMS. The friability values for all tablets were well below the maximum 1% USP tolerance
limit. CMS produced superdisintegrating tablets (disintegration time < 1 min) with the
three model drugs. Regarding the dissolution rate, the sequence was as follow:
CMS > Fleximex® > Avicel® 200, CMS > Avicel® 200 > Dumazole® and Aldactone® >
Avicel® 200 > CMS for IBU, MET and SPL, respectively. Compressional properties of
formulations were analyzed using density measurements and the compression Kawakita
equation as assessment parameters. On the basis of DSC results, CMS co precipitates were
found to be compatible with the tested drugs. Conclusively, the CMS co-precipitates have
This study investigates co-processing lactose with synthetic amorphous magnesium silicate with th... more This study investigates co-processing lactose with synthetic amorphous magnesium silicate with the aim of
expanding the use of directly compressible excipients based on native lactose. The co-processing was
performed using roller compaction. The co-processed excipient was characterized using particle size analysis
and compression properties (Kawakita equation). The co-processed excipient demonstrated plastic behavior
upon compression, good flowability and crushing strength and a shorter disintegration time. Compatibility
between the different ingredients of the co-processed excipient, as well as, between the co-processed excipient
and model drugs was tested using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared
spectroscopy (FTIR). The interaction between lactose and magnesium silicate proved to be of a physical
nature. Formulating this co-processed excipient with Mebeverine HCl and Losartan Potassium as model
drugs, indicated its suitability as a single multi-functional excipient. Co-processed lactose with magnesium
silicate could be used as a single direct compression excipient for tablet manufacturing.
ABSTRACT
An oral controlled release (CR) matrix system of Ambroxol hydrochloride was developed us... more ABSTRACT
An oral controlled release (CR) matrix system of Ambroxol hydrochloride was developed using a binary
hydrophilic polymer mixture of chitosan (CH) and xanthan gum (XG) (1:1 w/w ratio). Two test tablet
formulations were prepared using drug to polymer mixture ratios (D:P) of 1:1 and 1:3 (w/w), designated as
T1 and T2, respectively. The in vitro drug release data was best fitted to the Higuchi equation. The 1:1 ratio
(T1) demonstrated in vitro dissolution similarity with the commercial product, Mucosolvan LA. A preliminary
in vivo study was performed using six volunteers. The study was designed to include open, randomized, singledose,
three-treatment, six-sequence, crossover (Williams design) under fasting conditions. The data showed
that T1 was bioequivalent to Mucosolvan LA ® after the administration of a single 75mg oral dose. Two in
vivo, in vitro correlations (IVIVC) were established between Cmax versus the fraction of drug dissolved (FRD)
after 4 hours, and AUC versus the ratio of fraction of drug dissolved (FRD) after 10 hours where a multiple
point level C correlation of IVIVC was obtained.
While determining cefaclor in biological fluid, it could be degraded due to oxidation hydrolysis
... more While determining cefaclor in biological fluid, it could be degraded due to oxidation hydrolysis
and racemisation. Furthermore, such degradation process can be accelerated depending on pH, temperature,
carbon dioxide, oxygen, light, humidity and storage. Thus such measures are crucial in cefaclor
determination in biological fluids and reducing or inhibiting the degradation process while assaying is
mandatory. In the developed method, samples were assayed without pretreatment or with perchloric acid
and protein precipitation treatment. Sulphamethoxazole as an internal standard was used. Chromatographic
separation was carried out on with lichrospher RP-18 column using mobile phase 80:20 v/v
(potassium dihydrogen phosphate buffer (0.067M): methanol, pH 4.5), hexane-1-sulphonic acid sodium
salt (0.002 M) was used as an ion pair and the flow rate was 1.3 mL/min. Cefaclor was monitored using
UV detector at λ 265 nm. Pre-sample treatment with perchloric acid as acidifying agent and plasma protein
precipitant was found to enhance stability of cefaclor. The calibration curve was demonstrated to be
linear in the range of 0.25-20 μg/mL (r2 = 0.999) and the limit of quantitation was estimated at 0.25 μg/mL.
In conclusion, a stability-indicating, accurate, precise, simple, and highly sensitive reversed phase HPLC
method for the determination of cefaclor in biological fluids was developed and can be successfully used in
bioequivalence study and other pharmacokinetic evaluation
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Papers by Faisal Al-akayleh
(M68), a natural liquid crystal forming surfactant, were utilized in the development of emulgel
base for topical application. The emulgels were prepared in water alone or combined with
propylene glycol (PG), polyethylene glycol 400 (PEG400) and glycerol (G) as cosolvents.
Emulgels were characterized for their optical and flow behavior. Two model drugs: caffeine (CF)
and methylparaben (MP) were used in the evaluation of drug permeation across the stratum
corneum (SC). The results showed that emulgel prepared using 70% PG:water (1:1) and 30%
S600 has the best flow behavior compared to other cosolvents. Also the permeability
coefficient of CF was found to be higher than that of MP and the addition of 3% M68 improved
the physical stability of the emulgel, but it did not affect the drug diffusion profile.
and imidapril simultaneously in their raw material and tablet dosage forms. The chromatographic
acetonitrile and phosphate buffer (25:75 v/v) ratio. The detection of Prills drugs was carried out at 210 nm with a flow rate
retention times for lisinopril, captopril and imidapril were 3.6, 4.4,
by recovery studies. The proposed method was successfully employed for the estimatio
Directly compressed matrices were produced using a binary mixture of different chitosan (CH) and xanthan gum
(XG) ratios. These hydrophilic excipients were used to control the release of ambroxol HCl. CH and XG were
investigated at three ratios of 1:1, 1:4 and 4:1. Mucosolvan LA® was used as a commercially available reference
product. The optimal CH to XG ratio was 1:1 and the optimal drug to polymer ratio was 1:3. Matrix erosion,
hydration and drug release studies were carried out using a dissolution apparatus (basket method). The release
mechanism is also discussed.
single multifunctional excipient in tablet formulation using direct compression and wet
granulation methods is evaluated. The neutral, acidic, and basic drugs Spironolactone
(SPL), ibuprofen (IBU) and metronidazole (MET), respectively, were used as model drugs.
Commercial Aldactone®, Fleximex® and Dumazole® tablets containing SPL, IBU and
MET, respectively, and tablets made using Avicel® 200, were used in the study for
comparison purposes. Tablets of acceptable crushing strength (>40 N) were obtained using
CMS. The friability values for all tablets were well below the maximum 1% USP tolerance
limit. CMS produced superdisintegrating tablets (disintegration time < 1 min) with the
three model drugs. Regarding the dissolution rate, the sequence was as follow:
CMS > Fleximex® > Avicel® 200, CMS > Avicel® 200 > Dumazole® and Aldactone® >
Avicel® 200 > CMS for IBU, MET and SPL, respectively. Compressional properties of
formulations were analyzed using density measurements and the compression Kawakita
equation as assessment parameters. On the basis of DSC results, CMS co precipitates were
found to be compatible with the tested drugs. Conclusively, the CMS co-precipitates have
expanding the use of directly compressible excipients based on native lactose. The co-processing was
performed using roller compaction. The co-processed excipient was characterized using particle size analysis
and compression properties (Kawakita equation). The co-processed excipient demonstrated plastic behavior
upon compression, good flowability and crushing strength and a shorter disintegration time. Compatibility
between the different ingredients of the co-processed excipient, as well as, between the co-processed excipient
and model drugs was tested using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared
spectroscopy (FTIR). The interaction between lactose and magnesium silicate proved to be of a physical
nature. Formulating this co-processed excipient with Mebeverine HCl and Losartan Potassium as model
drugs, indicated its suitability as a single multi-functional excipient. Co-processed lactose with magnesium
silicate could be used as a single direct compression excipient for tablet manufacturing.
An oral controlled release (CR) matrix system of Ambroxol hydrochloride was developed using a binary
hydrophilic polymer mixture of chitosan (CH) and xanthan gum (XG) (1:1 w/w ratio). Two test tablet
formulations were prepared using drug to polymer mixture ratios (D:P) of 1:1 and 1:3 (w/w), designated as
T1 and T2, respectively. The in vitro drug release data was best fitted to the Higuchi equation. The 1:1 ratio
(T1) demonstrated in vitro dissolution similarity with the commercial product, Mucosolvan LA. A preliminary
in vivo study was performed using six volunteers. The study was designed to include open, randomized, singledose,
three-treatment, six-sequence, crossover (Williams design) under fasting conditions. The data showed
that T1 was bioequivalent to Mucosolvan LA ® after the administration of a single 75mg oral dose. Two in
vivo, in vitro correlations (IVIVC) were established between Cmax versus the fraction of drug dissolved (FRD)
after 4 hours, and AUC versus the ratio of fraction of drug dissolved (FRD) after 10 hours where a multiple
point level C correlation of IVIVC was obtained.
and racemisation. Furthermore, such degradation process can be accelerated depending on pH, temperature,
carbon dioxide, oxygen, light, humidity and storage. Thus such measures are crucial in cefaclor
determination in biological fluids and reducing or inhibiting the degradation process while assaying is
mandatory. In the developed method, samples were assayed without pretreatment or with perchloric acid
and protein precipitation treatment. Sulphamethoxazole as an internal standard was used. Chromatographic
separation was carried out on with lichrospher RP-18 column using mobile phase 80:20 v/v
(potassium dihydrogen phosphate buffer (0.067M): methanol, pH 4.5), hexane-1-sulphonic acid sodium
salt (0.002 M) was used as an ion pair and the flow rate was 1.3 mL/min. Cefaclor was monitored using
UV detector at λ 265 nm. Pre-sample treatment with perchloric acid as acidifying agent and plasma protein
precipitant was found to enhance stability of cefaclor. The calibration curve was demonstrated to be
linear in the range of 0.25-20 μg/mL (r2 = 0.999) and the limit of quantitation was estimated at 0.25 μg/mL.
In conclusion, a stability-indicating, accurate, precise, simple, and highly sensitive reversed phase HPLC
method for the determination of cefaclor in biological fluids was developed and can be successfully used in
bioequivalence study and other pharmacokinetic evaluation
(M68), a natural liquid crystal forming surfactant, were utilized in the development of emulgel
base for topical application. The emulgels were prepared in water alone or combined with
propylene glycol (PG), polyethylene glycol 400 (PEG400) and glycerol (G) as cosolvents.
Emulgels were characterized for their optical and flow behavior. Two model drugs: caffeine (CF)
and methylparaben (MP) were used in the evaluation of drug permeation across the stratum
corneum (SC). The results showed that emulgel prepared using 70% PG:water (1:1) and 30%
S600 has the best flow behavior compared to other cosolvents. Also the permeability
coefficient of CF was found to be higher than that of MP and the addition of 3% M68 improved
the physical stability of the emulgel, but it did not affect the drug diffusion profile.
and imidapril simultaneously in their raw material and tablet dosage forms. The chromatographic
acetonitrile and phosphate buffer (25:75 v/v) ratio. The detection of Prills drugs was carried out at 210 nm with a flow rate
retention times for lisinopril, captopril and imidapril were 3.6, 4.4,
by recovery studies. The proposed method was successfully employed for the estimatio
Directly compressed matrices were produced using a binary mixture of different chitosan (CH) and xanthan gum
(XG) ratios. These hydrophilic excipients were used to control the release of ambroxol HCl. CH and XG were
investigated at three ratios of 1:1, 1:4 and 4:1. Mucosolvan LA® was used as a commercially available reference
product. The optimal CH to XG ratio was 1:1 and the optimal drug to polymer ratio was 1:3. Matrix erosion,
hydration and drug release studies were carried out using a dissolution apparatus (basket method). The release
mechanism is also discussed.
single multifunctional excipient in tablet formulation using direct compression and wet
granulation methods is evaluated. The neutral, acidic, and basic drugs Spironolactone
(SPL), ibuprofen (IBU) and metronidazole (MET), respectively, were used as model drugs.
Commercial Aldactone®, Fleximex® and Dumazole® tablets containing SPL, IBU and
MET, respectively, and tablets made using Avicel® 200, were used in the study for
comparison purposes. Tablets of acceptable crushing strength (>40 N) were obtained using
CMS. The friability values for all tablets were well below the maximum 1% USP tolerance
limit. CMS produced superdisintegrating tablets (disintegration time < 1 min) with the
three model drugs. Regarding the dissolution rate, the sequence was as follow:
CMS > Fleximex® > Avicel® 200, CMS > Avicel® 200 > Dumazole® and Aldactone® >
Avicel® 200 > CMS for IBU, MET and SPL, respectively. Compressional properties of
formulations were analyzed using density measurements and the compression Kawakita
equation as assessment parameters. On the basis of DSC results, CMS co precipitates were
found to be compatible with the tested drugs. Conclusively, the CMS co-precipitates have
expanding the use of directly compressible excipients based on native lactose. The co-processing was
performed using roller compaction. The co-processed excipient was characterized using particle size analysis
and compression properties (Kawakita equation). The co-processed excipient demonstrated plastic behavior
upon compression, good flowability and crushing strength and a shorter disintegration time. Compatibility
between the different ingredients of the co-processed excipient, as well as, between the co-processed excipient
and model drugs was tested using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared
spectroscopy (FTIR). The interaction between lactose and magnesium silicate proved to be of a physical
nature. Formulating this co-processed excipient with Mebeverine HCl and Losartan Potassium as model
drugs, indicated its suitability as a single multi-functional excipient. Co-processed lactose with magnesium
silicate could be used as a single direct compression excipient for tablet manufacturing.
An oral controlled release (CR) matrix system of Ambroxol hydrochloride was developed using a binary
hydrophilic polymer mixture of chitosan (CH) and xanthan gum (XG) (1:1 w/w ratio). Two test tablet
formulations were prepared using drug to polymer mixture ratios (D:P) of 1:1 and 1:3 (w/w), designated as
T1 and T2, respectively. The in vitro drug release data was best fitted to the Higuchi equation. The 1:1 ratio
(T1) demonstrated in vitro dissolution similarity with the commercial product, Mucosolvan LA. A preliminary
in vivo study was performed using six volunteers. The study was designed to include open, randomized, singledose,
three-treatment, six-sequence, crossover (Williams design) under fasting conditions. The data showed
that T1 was bioequivalent to Mucosolvan LA ® after the administration of a single 75mg oral dose. Two in
vivo, in vitro correlations (IVIVC) were established between Cmax versus the fraction of drug dissolved (FRD)
after 4 hours, and AUC versus the ratio of fraction of drug dissolved (FRD) after 10 hours where a multiple
point level C correlation of IVIVC was obtained.
and racemisation. Furthermore, such degradation process can be accelerated depending on pH, temperature,
carbon dioxide, oxygen, light, humidity and storage. Thus such measures are crucial in cefaclor
determination in biological fluids and reducing or inhibiting the degradation process while assaying is
mandatory. In the developed method, samples were assayed without pretreatment or with perchloric acid
and protein precipitation treatment. Sulphamethoxazole as an internal standard was used. Chromatographic
separation was carried out on with lichrospher RP-18 column using mobile phase 80:20 v/v
(potassium dihydrogen phosphate buffer (0.067M): methanol, pH 4.5), hexane-1-sulphonic acid sodium
salt (0.002 M) was used as an ion pair and the flow rate was 1.3 mL/min. Cefaclor was monitored using
UV detector at λ 265 nm. Pre-sample treatment with perchloric acid as acidifying agent and plasma protein
precipitant was found to enhance stability of cefaclor. The calibration curve was demonstrated to be
linear in the range of 0.25-20 μg/mL (r2 = 0.999) and the limit of quantitation was estimated at 0.25 μg/mL.
In conclusion, a stability-indicating, accurate, precise, simple, and highly sensitive reversed phase HPLC
method for the determination of cefaclor in biological fluids was developed and can be successfully used in
bioequivalence study and other pharmacokinetic evaluation