Mohammed Habibuddin - Academia.edu (original) (raw)

Papers by Mohammed Habibuddin

International journal of pharmaceutical investigation, 2013

Turkish journal of pharmaceutical sciences, 2015

Curcumin, an ayurvedic natural product has many pharmacological properties including liver protec... more Curcumin, an ayurvedic natural product has many pharmacological properties including liver protection. The objective of this study was to investigate parenteral nanosuspensions of curcumin for enhancing the solubility, Cmax and liver protection and achieve sustained parenteral drug release after intravenous administration. Curcumin nanosuspensions were prepared using solvent-antisolvent precipitation method. The formulations were characterized using techniques such as powder x-ray diffractometry (XRPD), scanning electron microscopy, saturation solubility, in-vitro dissolution, pharmacokinetics and liver protection in rats. Nanosuspensions of curcumin were successfully prepared using solvent-antisolvent precipitation. The size of the particles was below 600 nm. XRPD studies indicated transformation of curcumin from crystalline to amorphous form upon fabrication into nanosuspensions. Saturation solubility and dissolution rate were higher for nanosuspensions when compared to pure drug. The optimum formulation sustained the drug release for 8 days in vivo. Cmax and liver protection of curcumin in the form of intravenous nanosuspensions was significantly higher than that of intravenously administered pure drug in the solution form. Therefore, in this study a parenteral sustained release curcumin nanosuspension formulation intended for sustained systemic release of the drug, enhanced Cmax and enhanced liver protection/targeting was successfully developed. The formulation can be successfully used in liver fibrosis/cirrhosis.

Pharmacy and Pharmacology Communications, Nov 1, 1999

The activity of four new GABA derivatives, N-valproyl GABA (V-GABA), N-phthaloyl GABA (P-GABA), N... more The activity of four new GABA derivatives, N-valproyl GABA (V-GABA), N-phthaloyl GABA (P-GABA), N-octanoyl GABA (O-GABA) and g-phthalamido-N-amyl butyramide (PGA) on GABA, glutamic acid decarboxylase (GAD) and GABA-transaminase (GABA-T) levels in the mouse brain were studied. All the GABA derivatives significantly increased both GABA and GAD levels. P-GABA and PGA inhibited GABA-T activity, while V-GABA and O-GABA had no significant effect. The GABA derivatives probably act by stimulating the enzyme GAD. The GABA formed reacts with the particular receptor subtype to elicit a definite pharmacological action.

Social Science Research Network, May 1, 2001

$Research paper thumbnail of Hepatoprotective activity of extracted anthocyanins fraction of red radish (<i>Raphanus sativus</i> L) on albino rats$

Journal of Experimental and Integrative Medicine, 2013

Objective: We investigated hepatoprotective and antioxidant activity of extracted anthocyanins fr... more Objective: We investigated hepatoprotective and antioxidant activity of extracted anthocyanins fraction of red radish for the first time. Methods: Anthocyanins fraction of red radish (Raphanus sativus; AFRS) was selectively extracted by employment of polymeric ion-exchange resin. AFRS was evaluated for antioxidant and hepatoprotective activity against carbon tetrachloride (CCl4)-induced hepatotoxicity in rats. The animals were divided into seven groups of six animals each. Group I (control) received vehicle. Group II (drug control) received AFRS. Group III (toxicant) received CCl4. Group IV, V and VI received AFRS at doses of 50, 100 and 150 mg/kg po, respectively. Group VII (standard) received silymarin. Various biochemical parameters like alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), total bilirubin (TB) and direct bilirubin (DB) levels in serum as well as the glutathione (GSH) and malondialdehyde (MDA) levels in the liver were determined. Histopathological changes in the liver were also studied. The activity of AFRS was compared with the reference drug silymarin. Results: The yield of AFRS was found to be 0.084% (w/w). AFRS treated group did not show any significant change in the activity of serum ALT, AST, ALP, TB, DB, MDA and GSH level compared to control group. CCl4 significantly raised the serum level of all biochemical parameters (except GSH) in the toxicant group. The pre-treatment of AFRS for seven days had reversed the alteration of biochemical parameters towards normal, and the effects were comparable to standard drug (silymarin 100 mg/kg). The animals received pre-treatment of AFRS showed amelioration in necrotic zones and hepatocellular degeneration. Conclusion: This study demonstrates the antioxidant and hepatoprotective activity of anthocyanins fraction isolated from Raphanus sativus and thus scientifically supports the usage of it as food colorant and also justifies the use of the crude extracts of radish to treat various liver ailments in Indian folk medicine.

International Scholarly Research Notices, Oct 30, 2014

A simple, rapid, and precise RP-HPLC method for simultaneous analysis of atorvastatin calcium, me... more A simple, rapid, and precise RP-HPLC method for simultaneous analysis of atorvastatin calcium, metformin hydrochloride, and glimepiride in bulk and its pharmaceutical formulations has been developed and validated. These drugs were separated by using Grace Smart Altima C-8 column (250 × 4.6 mm, 5-m) with a mobile phase consisting of acetonitrile : phosphate buffer (60 : 40 (v/v), pH 3.0) at a flow rate of 1 mL/min, injection volume 25 L, and detection at 235 nm. Metformin, atorvastatin, and glimepiride were eluted with retention times of 2.57 min, 7.06 min, and 9.39 min, respectively. The method was validated for accuracy, precision, linearity, specificity, and sensitivity in accordance with ICH (Q2B) guidelines. The results of all the validation parameters were found to be within the acceptable limits. The calibration plots were linear over the concentration ranges from 10 to 150 g/mL, 20 to 200 g/mL, and 10 to 150 g/mL for atorvastatin, metformin, and glimepiride, respectively. The accuracy and precision were found to be between 98.2%-105% and ≤2% for three drugs. Developed method was successfully applied for the determination of the drugs in tablet dosage form and recovery was found to be >98% for three drugs. The degradation products produced as a result of stress studies did not interfere with drug peaks.

Indian drugs, Feb 26, 2014

The objective of this study was to investigate nanosuspensions, hydroxypropyl-β-cyclodextrin (HPβ... more The objective of this study was to investigate nanosuspensions, hydroxypropyl-β-cyclodextrin (HPβCD) complexes and SLS powders for enhancing the solubility and dissolution rate of Prasugrel HCl (PHCl) so as to reduce the fluctuations in its oral bioavailability. PHCl nanosuspensions were prepared using evaporative precipitation method. HPβCD inclusion complexes of PHCl were prepared using physical mixture, co-evaporation and kneading methods. Powders of the pure drug with different SLS amounts were prepared. The formulations were characterized using techniques such as powder x-ray diffractometry, scanning electron microscopy, in vitro dissolution and in vivo absorption in rats. To further aid in the betterment of development of nevirapine nanosuspension, in vitro in vivo correlation (IVIVC) was established using deconvolution technique. Nanosuspensions and HPβCD inclusion complexes of PHCl were successfully prepared. The dissolution rate and oral absorption of PHCl in the form of nanosuspensions was significantly higher than that of HPβCD complexes, SLS powders as well as pure drug. All the techniques investigated in this study can be used to enhance dissolution rate and oral absorption of prasugrel HCl and thus can reduce the fluctuations in its oral bioavailability. Nanosuspensions demonstrated to be better and superior technique when compared to other techniques investigated in enhancing oral bioavailability of PHCl. IVIVC that could aid in further formulation development of PHCl nanosuspension was successfully developed using a deconvolution approach.

PubMed, Mar 1, 1994

Out of fourteen compounds reported here only four [N-valproyl GABA (V.GABA), N-phthaloyl GABA (P.... more Out of fourteen compounds reported here only four [N-valproyl GABA (V.GABA), N-phthaloyl GABA (P.GABA), gamma-phthalimido N-amyl butyramide (PGA) and gamma-phthalimido N-phenyl butyramide (PGP)] gave significant protection to all the four components of maximal electroshock-induced seizures (MES) in mice. It appeared that substitution of either amino or carboxylic or both groups of gamma-aminobutyric acid (GABA) with bulkier groups like aliphatic or aromatic carbons usually produced effective anticonvulsant GABA derivatives. V.GABA and P.GABA were the most effective anticonvulsant GABA derivatives in protecting all the components of MES-induced seizures. They were 2.3 and 1.5 times potent than sodium valproate in molar ratio, but P.GABA has low therapeutic index when compared to V.GABA. The observed anticonvulsant activity may be due to enhanced GABA concentration in the CNS. Probably, the active compound (V.GABA) crossed the blood brain barrier and hydrolysed to GABA and valproic acid to bring about its anticonvulsant action.

International Journal of Pharmacy and Pharmaceutical Sciences, Oct 1, 2018

Objective: The present investigation demonstrates a simple, sensitive and accurate high pressure ... more Objective: The present investigation demonstrates a simple, sensitive and accurate high pressure liquid chromatographic (HPLC) method for the determination of alvimopan (AMP) in rat plasma. Methods: The chromatographic separation was achieved within 10 min by using acetonitrile: potassium dihydrogen phosphate buffer pH 3.0 adjusted with orthophosphoric acid (50:50) as mobile phase on Altima Grace Smart C-18 column (5μ; 250 × 4.6 mm) at a flow rate of 1.0 ml/min with injection volume 50 µl. The drug was extracted from plasma by liquid-liquid extraction using a mixture of methanol: acetonitrile (50:50) as a solvent. The retention times of drug and internal standard were found to be 5.17 and 6.74 min, respectively. This method was validated as per the United States Food and Drug Administration (US-FDA) guidelines. Results: The results of the validation parameters were found to be within the acceptance limits. The method was linear in the concentration range from 5-1000 ng/ml (r 2 = 0.9998), and the extraction recovery was found to be 78.71±3.86% for AMP. The lower limit of quantification was found to be 5ng/ml, and the stability of recovered samples at different conditions was found to be more than 95%. Conclusion: The developed method possess good selectivity, specificity, there was no interference found in the plasma blanks at retention times of AMP and Internal Standard (IS). We found a good correlation between the peak area and concentration of the drug under prescribed conditions. Furthermore, the method can also be used to estimate the pharmacokinetic parameters of AMP.

Current Pharmaceutical Analysis, Jul 1, 2012

Indian Journal of Pharmaceutical Sciences, 2016

Curcumin, a hydrophobic polyphenol called diferuloyl methane, which is extracted from the rhizome... more Curcumin, a hydrophobic polyphenol called diferuloyl methane, which is extracted from the rhizome of Curcuma longa (turmeric) belongs to zingiberaceae family [1]. Curcumin has been associated with many pharmacological activities which include antiproliferative, anticancer, antiangiogenic, antidiabetic, antioxidant and antiinflammatory activities. The major limitations of curcumin is rapid systemic elimination, degradation at alkaline pH, limited oral bioavailability [2,3]. To overcome the limitations of curcumin several novel drug delivery carriers has been tagged to curcumin. These delivery systems increased its aqueous solubility, stability, oral bioavailability and achieved controlled and targeted delivery. For instance, Jithan et al., developed curcumin albumin nanoparticles and investigated its application in breast cancer [4]. The results of the study indicated that the solubility of curcumin in aqueous dissolution medium was increased with the nanoformulation compared to its pure solid form and the formulation can be

International Journal of Current Pharmaceutical Research, Sep 21, 2017

Objective: The objective of the present study is to develop and validate a simple, rapid, sensiti... more Objective: The objective of the present study is to develop and validate a simple, rapid, sensitive reverse phase HPLC method for the determination of Armodafinil present in bulk and its pharmaceutical formulations. Methods: The chromatographic separation was achieved by using Hypersil ODS C-18 (150 x 4.6 mm, 5µ) in an isocratic mode with mobile phase methanol: phosphate buffer 3.0 (60:40 %v/v) was used. The flow rate was 1 ml/min and effluent was monitored at 225 nm. The method was validated for validation parameters i.e. linearity, accuracy, precision and robustness according to ICH guidelines. Results: The retention time of Armodafinil was 4.2 min and the linearity range of the method was 500-20000ng/ml with regression (r 2 Conclusion: The developed method possess good selectivity, specificity, there is no interference found in the blank at a retention time of ARM and good correlation between the peak area and concentration of the drugs under prescribed conditions. Hence, the method can be applied for routine analysis of Armodafinil.) coefficient 0.9998. The method was validated for precision, accuracy, robustness and which were found to be within the acceptable limits according to the ICH guidelines. Also, the method was successfully applied for the estimation of Armodafinil in the marketed formulation of Nuvigil and the recovery was found to be>98%.

Pharmacognosy Research, 2018

Background: Several factors contribute to the increased use of herbal products: namely, easy acce... more Background: Several factors contribute to the increased use of herbal products: namely, easy accessibility, perception of herbs as safe alternate treatment, desire for self-medication, and lesser cost. With expanding utilization of home-grown medications, there have been concerns with respect to the security of these items, specifically the potential communication of these medications with regular medications. Certain natural enhancements can cause conceivably perilous symptoms when taken with physician recommended drugs. Objective: To inspect the pharmacodynamic interaction of allicin and gliclazide in animal models and to understand the safety and adequacy. Methods: Single and multiple dose treatments in normal rats, diabetes triggered rats and rabbits to assess the impact of allicin on the gliclazide movement. Blood tests from the examination of animals were utilized for the estimation insulin and glucose levels by utilizing radioimmunoassay technique and science analyzer (computerized) separately. Homeostasis evaluation utilized for assurance of β-cell work. Results: Gliclazide produces huge lessening in blood glucose levels in diabetic animals. In the combination, gliclazide in mix with allicin demonstrated more noticeable diminishment in blood glucose fixation in animals with diabetes. Conclusion: Coadministration of allicin and gliclazide did enhance the antidiabetic activity compared with individual drugs.

Saudi journal of obesity, 2014

Obesity is defined as an excess fat deposition due to long term change in the energy balance resu... more Obesity is defined as an excess fat deposition due to long term change in the energy balance resulting in increasing energy input, lowering physical activity and decreases in energy output, or both. There are many factors governing obesity such as, sedentary movement, unhealthy diet and eating habits, family lifestyle , pregnancy, lack of sleep, certain medications, age, social and economic issues, medical problems and genetics. [1] Some of these factors are corrected by exercise, changing diet and a change of lifestyle. The factors that are not able to be corrected are subjected to pharmacological interventions. Therapeutic agents can help the weight loss with decreasing the consumption of foods or inhibiting absorption of food or increasing energy expenditure. Over the last 10 years, there has been a rapid explosion in our knowledge of the mechanisms involved in regulating feeding behavior and cellular mechanisms involved in

Journal of The Saudi Pharmaceutical Society, 2016

We studied the application of Taguchi orthogonal array (TOA) design during the development of an ... more We studied the application of Taguchi orthogonal array (TOA) design during the development of an isocratic stability indicating HPLC method for glimepiride as per TOA design; twenty-seven experiments were conducted by varying six chromatographic factors. Percentage of organic phase was the most significant (p < 0.001) on retention time, while buffer pH had the most significant (p < 0.001) effect on tailing factor and theoretical plates. TOA design has shortcoming, which identifies the only linear effect, while ignoring the quadratic and interaction effects. Hence, a response surface model for each response was created including the linear, quadratic and interaction terms. The developed models for each response found to be well predictive bearing an acceptable adjusted correlation coefficient (0.9152 for retention time, 0.8985 for tailing factor and 0.8679 for theoretical plates). The models were found to be significant (p < 0.001) having a high F value for each response (15.76 for retention time, 13.12 for tailing factor and 9.99 for theoretical plates). The optimal chromatographic condition uses acetonitrile-potassium dihydrogen phosphate (pH 4.0; 30 mM) (50:50, v/v) as the mobile phase. The temperature, flow rate and injection volume were

Behavioural Pharmacology, May 1, 1995

Asian Journal of Pharmaceutical and Clinical Research, Apr 1, 2018

Objective: The objective of this study was to prepare and evaluate itraconazole (ITZ) nanosuspens... more Objective: The objective of this study was to prepare and evaluate itraconazole (ITZ) nanosuspensionsusing polymer Eudragit RL-100 and stabilizer Tween-80 by nanoprecipitation method. Materials and Methods: Itraconazole is a potent broad-spectrum Biopharmaceutical Classification System Class II triazole antifungal drug. Nanosuspensions were prepared using solvent displacement/nanoprecipitation method with the help of Eudragit RL-100 as rate-controlled polymer in different ratios and using Tween-80 as stabilizer. The nanosuspension preparation was optimized for particle size by investigating two factors that are solvent:anti-solvent ratio and surfactant concentration, at three levels. The prepared nanosuspensions were evaluated and characterized for particle size, drug excipient compatibility, percentage yield, drug entrapment efficiency, surface morphology, zeta potential, saturation solubility, solid state, and in vitro drug release studies. Results: The nanosuspensions of itraconazole were successfully prepared using solvent displacement/nanoprecipitation method. The two factors solvent: anti-solvent ratio and surfactant concentration influenced the particle size of the nanosuspensions prepared. The Fourier-transform infrared spectroscopy studies confirmed that drug and excipients are compatible, and the X-ray powdered diffraction and differential scanning calorimetry results indicated that the nanoprecipitation method led to the amorphization of itraconazole. Itraconazolenanosuspensions increased the saturation solubility to an extent of 4 times. Itraconazole nanosuspensions completely dissolved in the dissolution medium within 10 s and 72% drug release within 5 min, while the pure drug was dissolved only up to 20% in 15 min and nanosuspensions showed increased dissolution rate of 3 folds, the active drug. Conclusions: Stable itraconazole nanosuspensions were successfully prepared and these nanosuspensions demonstrated dramatic improvement in dissolution rate of the active drug.

International journal of pharmaceutical investigation, Jul 16, 2021

Background: Acyclovir (ACV) a 21-deoxy guanosine analogue effective against Herpes Simplex Virus ... more Background: Acyclovir (ACV) a 21-deoxy guanosine analogue effective against Herpes Simplex Virus (both type 1 and 2) and other viral diseases, mainly acts by inhibiting the viral DNA polymerase. The limited oral bioavailability of ACV (5-10%) requires higher dosage (400-800 mg), results in neurotoxicity and renal failure. Topically, the lower efficacy of ACV is attributed to inadequate drug permeation across the stratum corneum (SC). Methods: In present research, ACV containing proliposomes formulated using various ratios of lipid mixtures (Phosphotidyl choline and Cholesterol) by co acervation phase separation method. Results: The formulated vesicles are having the acceptable particle size range (385-616 nm). Other characters like morphological behaviour, zeta potential, polydispersity index and entrapment efficiency were evaluated. In vitro release studies reveal the controlled delivery of ACV from formed liposomes. Significant higher permeation parameter values [flux (Jss), permeability coefficient (Kp) and enhancement ratio (ER)] evaluated from all the formulations by performing ex vivo permeation studies using male wistar rats. 3.24 fold increment was observed in bioavailability of optimized formulation than control (oral suspension). The formulated ACV proliposomal gels were more stable when stored at 4°C. Conclusion: Improved bioavailability of ACV incorporated proliposomal gels than control reveals its potential in releasing of drug applied through transdermal route.

$Research paper thumbnail of Anthocyanins fraction of red radish (Raphanus sativus L) protects hepatic damage induced by carbon tetrachloride in albino rats$

We investigated hepatoprotective and antioxidant activity of extracted anthocyanins fraction of r... more We investigated hepatoprotective and antioxidant activity of extracted anthocyanins fraction of red radish for the first time. Methods: Anthocyanins fraction of red radish (Raphanus sativus; AFRS) was selectively extracted by employment of polymeric ion-exchange resin. AFRS was evaluated for antioxidant and hepatoprotective activity against carbon tetrachloride (CCl4)-induced hepatotoxicity in rats. The animals were divided into seven groups of six animals each. Group I (control) received vehicle. Group II (drug control) received AFRS. Group III (toxicant) received CCl4. Group IV, V and VI received AFRS at doses of 50, 100 and 150 mg/kg po, respectively. Group VII (standard) received silymarin. Various biochemical parameters like alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), total bilirubin (TB) and direct bilirubin (DB) levels in serum as well as the glutathione (GSH) and malondialdehyde (MDA) levels in the liver were determined. Histopathological changes in the liver were also studied. The activity of AFRS was compared with the reference drug silymarin. Results: The yield of AFRS was found to be 0.084% (w/w). AFRS treated group did not show any significant change in the activity of serum ALT, AST, ALP, TB, DB, MDA and GSH level compared to control group. CCl4 significantly raised the serum level of all biochemical parameters (except GSH) in the toxicant group. The pre-treatment of AFRS for seven days had reversed the alteration of biochemical parameters towards normal, and the effects were comparable to standard drug (silymarin 100 mg/kg). The animals received pre-treatment of AFRS showed amelioration in necrotic zones and hepatocellular degeneration. Conclusion: This study demonstrates the antioxidant and hepatoprotective activity of anthocyanins fraction isolated from Raphanus sativus and thus scientifically supports the usage of it as food colorant and also justifies the use of the crude extracts of radish to treat various liver ailments in Indian folk medicine.

Journal of Drug Delivery Science and Technology, Aug 1, 2015

The objective of this study was to prepare a solid supersaturatable self-nanoemulsifying drug del... more The objective of this study was to prepare a solid supersaturatable self-nanoemulsifying drug delivery system (solid S-SNEDDS) to improve the dissolution, absorption and pharmacodynamic effects of a poorly water-soluble drug: glipizide. The liquid supersaturatable formulation (liquid S-SNEDDS) was prepared by adding a polymeric precipitation inhibitor (HPMC-E5 at 5% w/w) to a liquid SNEDDS. Dilution of the liquid S-SNEDDS generated a nanoemulsion with a mean droplet size of 28.0 nm. The liquid S-SNEDDS was transformed into a free-flowing powder (solid S-SNEDDS) by adsorption onto calcium carbonate and talc. The solid S-SNEDDS generated a higher glipizide concentration in comparison with the solid SNEDDS (without HPMC-E5) during an in-vitro supersaturation test. Moreover, glipizide precipitated in an amorphous form from the solid S-SNEDDS. SEM studies of solid S-SNEDDS indicated the existence of molecularly dissolved glipizide. The solid S-SNEDDS was found to be stable during accelerated stability studies. In-vivo pharmacokinetic studies showed a significant (p < 0.001) increase in C max (3.4-fold) and AUC 0e12h (2.7-fold) of glipizide from solid S-SNEDDS as compared with the pure drug. Solid S-SNEDDS showed a significant (p < 0.001) decrease in the plasma glucose level by 1.3, 1.3, and 2.9-fold as compared with solid SNEDDS, the commercially available drug product and the pure drug, respectively.