Papers by Durgesh R Parakh
Application of Factorial Design Approach in Development and Evaluation of Self Microemulsifying Drug Delivery System (SMEDDS) of Mebendazole
Self microemulsifying drug delivery systems (SMEDDS) are defined as isotropic mixtures ofnatural ... more Self microemulsifying drug delivery systems (SMEDDS) are defined as isotropic mixtures ofnatural or synthetic oils, surfactants and co-solvents/co-surfactants. Upon mild agitation followedby dilution in aqueous media, such as GI fluids, these systems can form fine oil in water o/wmicroemulsion. The purpose of this study was to formulate SMEDDS containing mebendazole. Labrafil M2125 CS (an oil), Tween20 (a surfactant), and Maisine 35-1 (a cosurfactant) were used to formulate SMEDDS. Effect ofconcentrations of oil and surfactant on emulsification process and in-vitro drug release (percentcumulative drug release) was studied using 32 factorial design. Multiple regression analysis dataand response surfaces obtained showed that viscosity increased significantly with increasingamount of co-surfactant. Whereas, decrease in emulsification time, it may decreases averagedroplet size of resultant microemulsion and rapid drug release. The drug release from theformulation increased with increasing amount of surfactant concentration increases solubility of drug in system. Prepared SMEDDS produced acceptable properties of immediate-releasedosage forms. The L5 formulation was found to be optimized on basis of high percent cumulative drug release. And it is evaluated by globule size and zeta potential indicates globule size is in micrometer range and good stable formulation. Itmay expect to increase the bioavailability of mebendazole as solubility enhances.
Formulation and Evaluation of Solid Self Micro-Emulsifying Drug Delivery System (S-SMEDDS) of Chlorthalidone by Spray Drying Technology
The main objective of this study was to prepare a solid self micro-emulsifying drug delivery syst... more The main objective of this study was to prepare a solid self micro-emulsifying drug delivery system (S-SMEDDS) by spray drying liquid SMEDDS with an inert solid carrier Aerosil 200 to improve the dissolution rate and permeability of Chlorthalidone (CTD). The liquid SMEDDS was composed of CTD, oleic Acid, Tween 20, PEG 200. Preliminary screening was carried out to select proper components combination. Solubility of Chlorthalidone was determined in various vehicles. Ternary phase diagram for four series were constructed to delineate the boundaries of the nanoemulsion domain. Optimized S-SMEDDS (S3) was evaluated for dispersibility test (13.30 ± 0.95), percentage transmittance (99.50 ± 0.002), turbidity (260.43 ± 1.02), percent drug content (97.86 ± 0.56), droplet size (159.4), polydispersity index (0.30) and zeta potential (-12.4). Solid state characterization was done by SEM, DSC, XRD and FT-IR. The XRD analysis confirmed that there was no crystalline CTD in the S-SMEDDS. SEM study revealed adsorption of liquid SMEDDS on Aerosil 200. In-vitro drug release study was performed using water and 0.1 N HCl as dissolution medium and compared with plain drug and marketed tablet Thaiklor TM 12.5 and marked increase in rate and extent of dissolution of S-SMEDDS was observed. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain drug. The solid SMEDDS formulation was stable. In conclusion, the S-SMEDDS might be an encouraging strategy to improve the oral absorption of CTD.
A new simple and sensitive RP-HPLC method was developed and validated for quantification of Meben... more A new simple and sensitive RP-HPLC method was developed and validated for quantification of Mebendazole in Active Pharmaceutical Ingredient (API) and pharmaceutical formulation. The gradient RP-HPLC method was developed on Agilent (India) C18 250 × 4.6 mm, 5 μ column using mobile phase as acetonitrile: water pH 3.0 with orthophosphoric acid (90:10 v/v) at a flow rate of 1 mL/min and detection was carried out at 234 nm using UV-Visible detector (UV 3000 M). The method was validated linearity, limit of detection, limit of quantification, precision, ruggedness, robustness, accuracy and specificity were found to be satisfactory. The method was found to be linear in the concentration range of 20-100 μ/mL with correlation coefficient of 0.999. The method was validated according to the ICH guidelines and was proved to be specific, linear, accurate, precise and economical for the analysis of Mebendazole.
The development of oral controlled release system has been a challenge to formulation scientist d... more The development of oral controlled release system has been a challenge to formulation scientist due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. Various physical and chemical approaches have been applied to produce a well characterized dosage form that controls drug input into the body within the specifications of the desired release profile. This is generally accomplished by attempting to obtain " zero-order " release from the dosage form, i.e., the rate of drug release is independent of the drug concentration. Controlled porosity osmotic pump tablet; which is an extension of elementary osmotic tablet, utilizes the principle of osmotic pressure for the delivery of drugs and avoids the expensive laser drilling for creation of delivery orifice on the tablet coat. They do not have any aperture to release the drugs; drug release is achieved through the pores, which are formed in the semi permeable wall in situ during the operation. The advantages of controlled porosity osmotic pump tablet are mainly driven by the capacity to deliver drugs in a sustained manner, independent of the drug chemical properties, patient's physiological factors or concomitant food intake. However, access to this technology has been restricted by the crowded patent landscape and manufacturing challenges. The present review highlights the principle of osmosis, formulation variables, factors affecting drug release, recent researches, marketed products and the evaluation parameters of controlled porosity osmotic pump tablet.
Development of Self Microemulsifying Drug Delivery System of Mebendazole by Spray Drying Technology: Characterization, in-Vitro and in-Vivo evaluation
In this study, a novel liquid self micro emulsifying drug delivery system (SMEDDS) containing meb... more In this study, a novel liquid self micro emulsifying drug delivery system (SMEDDS) containing mebendazole was formulated and further developed into a solid form by a spray drying method using Aerosil 200 as the solid carrier. The optimum liquid SMEDDS consisted of Labrafil 2125 CS, Tween 20 and Maisine 35-1 as the oil phase, the surfactant and the co-surfactant respectively. The formulated SMEDDS was completely emulsified or dispersed within a minute. All formulations were dissolved within 1 hr. using 0.1 N HCl as dissolution medium whereas, pure drug was less significantly dissolved in this time period. The droplet size was found to be within 250 nm for solid forms of SMEDDS. Solid state characterization was performed by scanning electron micrograph (SEM), differential scanning calorimetry (DSC), and X-Ray powder diffraction (XRD). After oral administration to Wistar rats, mebendazole in the solid SMEDDS resulted in significant improvement in bioavailability compared with that of pure drug analyzed by RP-HPLC. The optimized formulation showed 24.87 folds increase in bioavailability as compared to pure drug and 8.39 folds increase in bioavailability in comparison to marketed tablet of mebendazole. The optimized batch has found to be 3.1726 years of shelf life. In conclusion, the solid SMEDDS is a promising solid dosage form for poorly water soluble and low bioavailability drugs.
Spray Dried Solid Self-Emulsifying Delivery System of Ketoprofen: Development and Its Characterization
Drying Technology
Ketoprofen is classified as BCS class II drug having low aqueous solubility, short half
life (2-... more Ketoprofen is classified as BCS class II drug having low aqueous solubility, short half
life (2-2.5 hrs) low oral bioavailability and also causes gastric irritation. The systems
intended for oral administration were prepared by using soyabean oil, Cremophor EL and
Maisine 35-1 and its adsorption on Aerosil 200. The spray dried product demonstrated
high process yield (52.2-68.3%) with good loading capacity (83.13-93.69%) and
significant drug release as compare to pure drug. The smooth spherical particles produced
had no interaction with the excipients as demonstrated by SEM and FTIR respectively.
The DSC indicated the complete miscibility of drug with excipients while XRD
demonstrated the transformation from crystalline to amorphous form.
World Journal of Pharmaceutical Research, Jul 8, 2015
Human skin acts as one of the key sites for non-invasive delivery of
therapeutic agents into the... more Human skin acts as one of the key sites for non-invasive delivery of
therapeutic agents into the body and it has verious numerous
advantages over oral drug delivery system.but the molecule or
compound with high molecular weight(500 Da) can not cross the skin.
For that compound reqires some novel techniques, methods to transfer
these compound across the skin easily without any side effects.
Vesicular system is one of the systems which have potential to transfer
high molecular weight compound (hydrophilic as well as lipophilic)
across the skin in control manner. But the major drawback of this
system is their stability issue, and hence it can not prepare in large
quantity both in laboratory scale and in industrial scale, it required
some specific condition when formulation is concerned. Proniosomal
is advanced concept over niosome and liposome, which have ability to overcome the problem
associated with farmal vesicular drug delivery system. Basically, proniosomal gel is a
compact semi-solid liquid crystaline (gel) product of non-ionic surfactants easily formed on
dissolving the surfactant in minimal amount of acceptable solvent and the least amount of
aqueous phase. This compact liquid crystalline gel can be readily converted into niosomes on
hydration. This review provides an important overview of preparation, formulation,
evaluation and application of proniosome gel as a drug carrier.
Inventi Rapid NDDS, Jun 24, 2015
The aim of the present investigation was to formulate and evaluate stable ketoconazole organogel ... more The aim of the present investigation was to formulate and evaluate stable ketoconazole organogel preparation to
increase the solubility of ketoconazole and release the drug for prolonged period of time. Ketoconazole was dissolved in clove
oil. The required amount of the tween 80 and PEG 400 was added to the clove oil containing propyl paraben. Subsequently,
water containing methyl paraben was added drop-by-drop to the organogelator solution with constant stirring on magnetic
stirrer until there was a formation of clear microemulsion. Carbopol 934 was used as a gelling phase, slowly mixed with
microemulsion in 1:1 ratio with constant and uniform stirring to get milky white homogeneous organogel. Formulated
organogels were evaluated for their physical appearance, pH, viscosity, globule size, drug content, spreadability, extrudability,
in-vitro and ex-vivo drug release, antifungal activity and stability. Organogel carrying ketoconazole showed good physical
appearance, acceptable skin pH (6 - 6.8), non-newtonian pseudoplastic system, drug content (99.68±0.19), globule size (572
nm), spreadability (21.67±0.034 gm.cm/sec), good extrudability, in-vitro release (98.75±0.32 %), ex-vivo release (73.45±0.86 %)
for optimized batch. Skin irritation study did not showed any irritation reaction and possess a good anti-fungal activity. The
optimized batch OG3 showed better drug release as compared to marketed cream. Similarly ex-vivo release of formulation
showed better drug release through mice skin as compared with marketed cream (KT CURE). The formulations followed zero
order kinetic model followed by higuchi mechanism. Thus, results of the current study clearly indicated a promising potential of
the ketoconazole organogel as an alternative to the conventional dosage form.
An International Journal of Advances in Pharmaceutical Sciences, Jul 1, 2014
In this study, comparison methods for in vitro dissolution profiles of conventional marketed dicy... more In this study, comparison methods for in vitro dissolution profiles of conventional marketed dicyclomine as performed. Dissolution
testing was conducted using the USP monograph for Dicyclomine hydrochloride tablet. The comparison of in vitro dissolution profile
was based upon model dependent methods and model independent models. The model dependent methods includes kinetic
modeling and model independent method includes difference factor, f1 and similarity factor, f2. The f1 factor seems to be easy to
apply and interpret; only one value is obtained to describe closeness of the two dissolution profiles. Here dissolution profile follows
Higuchi and Hixson – Crowell model while the f1 and f2 value were obtained in the range.
INTERNATIONAL JOURNAL OF INSTITUTIONAL PHARMACY AND LIFE SCIENCES, Jul 12, 2015
Self Micro-emulsifying drug delivery systems (SMEDDS) are usually used to improve the bioavailabi... more Self Micro-emulsifying drug delivery systems (SMEDDS) are usually used to improve the bioavailability of hydrophobic drugs. Approximately 60-70% of new chemical entities exhibit poor aqueous solubility and present a major challenge to modern drug delivery system, because of their low bioavailability. SMEDDS is isotropic (one phase system) mixture of oil or modified oils, surfactants and co-surfactants, which form the fine oil-in-water microemulsion when introduced into aqueous phase under condition of gentle agitation. The digestive motility of the stomach and intestine provide the agitation necessary for self-microemulsion in-vivo. Triglyceride is the one of the component of SMEDDS, which helps in the absorption of drugs from the GI tract. SMEDDS enhance the bioavailability enabling reduction in dose of the drug. SMEDDS is evaluated by various methods like visual assessment, droplet polarity and droplet size, size of emulsion droplet, dissolution test, charge of oil droplets, viscosity determination, in-vitro diffusion study. This article gives an overview of improvement in the rate and extent of oral absorption of drugs by SMEDDS approach. The characterization of SMEDDS and application of SMEDDS is also introduced, with particular emphasis being placed on the developments of Solid self micro-emulsifying delivery system and dosage form of SMEDDS.
World Journal of Pharmaceutical Research, Jun 30, 2015
A new simple and sensitive spectrophotometric method in UV region
has been developed for the det... more A new simple and sensitive spectrophotometric method in UV region
has been developed for the determination of Mebendazole in bulk and
in pharmaceutical formulations. Mebendazole exhibits absorption
maxima at 234 nm. The method obeys the Beer’s law in the
concentration range of 1-10 μg/mL. The method is accurate, precise
and economical. The percent recovery is near to 100%. This shows that
the method was free from the interference of excipients. The results of
validation study were analyzed with respect to accuracy, limit of
detection, linearity, limit of quantification, precision, ruggedness,
robustness and specificity were found to be satisfactory. The proposed
method has been applied successfully of drug in bulk and
pharmaceutical formulation.
Uploads
Papers by Durgesh R Parakh
life (2-2.5 hrs) low oral bioavailability and also causes gastric irritation. The systems
intended for oral administration were prepared by using soyabean oil, Cremophor EL and
Maisine 35-1 and its adsorption on Aerosil 200. The spray dried product demonstrated
high process yield (52.2-68.3%) with good loading capacity (83.13-93.69%) and
significant drug release as compare to pure drug. The smooth spherical particles produced
had no interaction with the excipients as demonstrated by SEM and FTIR respectively.
The DSC indicated the complete miscibility of drug with excipients while XRD
demonstrated the transformation from crystalline to amorphous form.
therapeutic agents into the body and it has verious numerous
advantages over oral drug delivery system.but the molecule or
compound with high molecular weight(500 Da) can not cross the skin.
For that compound reqires some novel techniques, methods to transfer
these compound across the skin easily without any side effects.
Vesicular system is one of the systems which have potential to transfer
high molecular weight compound (hydrophilic as well as lipophilic)
across the skin in control manner. But the major drawback of this
system is their stability issue, and hence it can not prepare in large
quantity both in laboratory scale and in industrial scale, it required
some specific condition when formulation is concerned. Proniosomal
is advanced concept over niosome and liposome, which have ability to overcome the problem
associated with farmal vesicular drug delivery system. Basically, proniosomal gel is a
compact semi-solid liquid crystaline (gel) product of non-ionic surfactants easily formed on
dissolving the surfactant in minimal amount of acceptable solvent and the least amount of
aqueous phase. This compact liquid crystalline gel can be readily converted into niosomes on
hydration. This review provides an important overview of preparation, formulation,
evaluation and application of proniosome gel as a drug carrier.
increase the solubility of ketoconazole and release the drug for prolonged period of time. Ketoconazole was dissolved in clove
oil. The required amount of the tween 80 and PEG 400 was added to the clove oil containing propyl paraben. Subsequently,
water containing methyl paraben was added drop-by-drop to the organogelator solution with constant stirring on magnetic
stirrer until there was a formation of clear microemulsion. Carbopol 934 was used as a gelling phase, slowly mixed with
microemulsion in 1:1 ratio with constant and uniform stirring to get milky white homogeneous organogel. Formulated
organogels were evaluated for their physical appearance, pH, viscosity, globule size, drug content, spreadability, extrudability,
in-vitro and ex-vivo drug release, antifungal activity and stability. Organogel carrying ketoconazole showed good physical
appearance, acceptable skin pH (6 - 6.8), non-newtonian pseudoplastic system, drug content (99.68±0.19), globule size (572
nm), spreadability (21.67±0.034 gm.cm/sec), good extrudability, in-vitro release (98.75±0.32 %), ex-vivo release (73.45±0.86 %)
for optimized batch. Skin irritation study did not showed any irritation reaction and possess a good anti-fungal activity. The
optimized batch OG3 showed better drug release as compared to marketed cream. Similarly ex-vivo release of formulation
showed better drug release through mice skin as compared with marketed cream (KT CURE). The formulations followed zero
order kinetic model followed by higuchi mechanism. Thus, results of the current study clearly indicated a promising potential of
the ketoconazole organogel as an alternative to the conventional dosage form.
testing was conducted using the USP monograph for Dicyclomine hydrochloride tablet. The comparison of in vitro dissolution profile
was based upon model dependent methods and model independent models. The model dependent methods includes kinetic
modeling and model independent method includes difference factor, f1 and similarity factor, f2. The f1 factor seems to be easy to
apply and interpret; only one value is obtained to describe closeness of the two dissolution profiles. Here dissolution profile follows
Higuchi and Hixson – Crowell model while the f1 and f2 value were obtained in the range.
has been developed for the determination of Mebendazole in bulk and
in pharmaceutical formulations. Mebendazole exhibits absorption
maxima at 234 nm. The method obeys the Beer’s law in the
concentration range of 1-10 μg/mL. The method is accurate, precise
and economical. The percent recovery is near to 100%. This shows that
the method was free from the interference of excipients. The results of
validation study were analyzed with respect to accuracy, limit of
detection, linearity, limit of quantification, precision, ruggedness,
robustness and specificity were found to be satisfactory. The proposed
method has been applied successfully of drug in bulk and
pharmaceutical formulation.
life (2-2.5 hrs) low oral bioavailability and also causes gastric irritation. The systems
intended for oral administration were prepared by using soyabean oil, Cremophor EL and
Maisine 35-1 and its adsorption on Aerosil 200. The spray dried product demonstrated
high process yield (52.2-68.3%) with good loading capacity (83.13-93.69%) and
significant drug release as compare to pure drug. The smooth spherical particles produced
had no interaction with the excipients as demonstrated by SEM and FTIR respectively.
The DSC indicated the complete miscibility of drug with excipients while XRD
demonstrated the transformation from crystalline to amorphous form.
therapeutic agents into the body and it has verious numerous
advantages over oral drug delivery system.but the molecule or
compound with high molecular weight(500 Da) can not cross the skin.
For that compound reqires some novel techniques, methods to transfer
these compound across the skin easily without any side effects.
Vesicular system is one of the systems which have potential to transfer
high molecular weight compound (hydrophilic as well as lipophilic)
across the skin in control manner. But the major drawback of this
system is their stability issue, and hence it can not prepare in large
quantity both in laboratory scale and in industrial scale, it required
some specific condition when formulation is concerned. Proniosomal
is advanced concept over niosome and liposome, which have ability to overcome the problem
associated with farmal vesicular drug delivery system. Basically, proniosomal gel is a
compact semi-solid liquid crystaline (gel) product of non-ionic surfactants easily formed on
dissolving the surfactant in minimal amount of acceptable solvent and the least amount of
aqueous phase. This compact liquid crystalline gel can be readily converted into niosomes on
hydration. This review provides an important overview of preparation, formulation,
evaluation and application of proniosome gel as a drug carrier.
increase the solubility of ketoconazole and release the drug for prolonged period of time. Ketoconazole was dissolved in clove
oil. The required amount of the tween 80 and PEG 400 was added to the clove oil containing propyl paraben. Subsequently,
water containing methyl paraben was added drop-by-drop to the organogelator solution with constant stirring on magnetic
stirrer until there was a formation of clear microemulsion. Carbopol 934 was used as a gelling phase, slowly mixed with
microemulsion in 1:1 ratio with constant and uniform stirring to get milky white homogeneous organogel. Formulated
organogels were evaluated for their physical appearance, pH, viscosity, globule size, drug content, spreadability, extrudability,
in-vitro and ex-vivo drug release, antifungal activity and stability. Organogel carrying ketoconazole showed good physical
appearance, acceptable skin pH (6 - 6.8), non-newtonian pseudoplastic system, drug content (99.68±0.19), globule size (572
nm), spreadability (21.67±0.034 gm.cm/sec), good extrudability, in-vitro release (98.75±0.32 %), ex-vivo release (73.45±0.86 %)
for optimized batch. Skin irritation study did not showed any irritation reaction and possess a good anti-fungal activity. The
optimized batch OG3 showed better drug release as compared to marketed cream. Similarly ex-vivo release of formulation
showed better drug release through mice skin as compared with marketed cream (KT CURE). The formulations followed zero
order kinetic model followed by higuchi mechanism. Thus, results of the current study clearly indicated a promising potential of
the ketoconazole organogel as an alternative to the conventional dosage form.
testing was conducted using the USP monograph for Dicyclomine hydrochloride tablet. The comparison of in vitro dissolution profile
was based upon model dependent methods and model independent models. The model dependent methods includes kinetic
modeling and model independent method includes difference factor, f1 and similarity factor, f2. The f1 factor seems to be easy to
apply and interpret; only one value is obtained to describe closeness of the two dissolution profiles. Here dissolution profile follows
Higuchi and Hixson – Crowell model while the f1 and f2 value were obtained in the range.
has been developed for the determination of Mebendazole in bulk and
in pharmaceutical formulations. Mebendazole exhibits absorption
maxima at 234 nm. The method obeys the Beer’s law in the
concentration range of 1-10 μg/mL. The method is accurate, precise
and economical. The percent recovery is near to 100%. This shows that
the method was free from the interference of excipients. The results of
validation study were analyzed with respect to accuracy, limit of
detection, linearity, limit of quantification, precision, ruggedness,
robustness and specificity were found to be satisfactory. The proposed
method has been applied successfully of drug in bulk and
pharmaceutical formulation.