Dr. Kinjal Solanki | Gujarat Technological University (original) (raw)
Papers by Dr. Kinjal Solanki
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions ... more The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac. The present work describes the formulation and evaluation of an ophthalmic delivery system of an anti-bacterial agent-Norfloxacin, based on the concept of pH-triggered in situ gelation. Polyacrylic acid (Carbopol-934) was used as the gelling agent in combination with HPMC K4 M which acted as a viscosity enhancing agent. The developed formulation was therapeutically efficacious, stable, non-irritant and provided sustained release of the drug over a period of 8-hours. The developed system is thus a viable alternative to conventional eye drops.
Nanotechnology is the science that deals with the processes tha t occur at molecular level and of... more Nanotechnology is the science that deals with the processes tha t occur at molecular level and of nanolength scale size. There are numerous examples from nature like DNA, water molecules, virus, red blood corpuscles (RBC) etc., which are of nanodimensions. Recent developments in nanotechnology offer researchers opportunities to significantly transform various therapeutics. This technology has enabled the manipulation of the biological and physicochemical properties of nanomaterial to facilitate more efficient drug targeting and delivery. The size of nanomaterial is similar to that of most biological molecules and structures; therefore, nanomaterial can be useful for both in vivo and in vitro biomedical research and applications. Clinical investigations suggest that therapeutic nanoparticles can enhance efficacy and reduced side effects c ompared with conventional therapeutic drugs. Nanotechnology is on its way to make a big impact in Biotech, Pharmaceutical and Medical diagnostics s...
Fluoroquinolones is major antibacterial group comprising antimicrobial agent with wide antibacter... more Fluoroquinolones is major antibacterial group comprising antimicrobial agent with wide antibacterial spectrum though differences exist between compounds in their potency against Gram positive and Gram Negative bacteria. Present study was carried out in order to find out current status regarding resistance to seven fluoroquinolones by E.coli, Klebsiella spp. Pseudomonas aeruginosa and Proteus spp. ,recovered from hospitalized patients. The overall result showed resistance to Levofloxacin(75.29%),Gatifloxacin(48.23%),Lomefloxacin(80%),Sparfloxacin(92.94%), Ciprofloxacin (72.94%), Norfloxacin(72.94%), and Ofloxacin(76.47%).
Pyrrolopyrimidines are well known scaffold which play a critical role as anticancer agents so it ... more Pyrrolopyrimidines are well known scaffold which play a critical role as anticancer agents so it was thought of interest to synthesize series of novel substituted pyrrolo[2,3-d]pyrimidines having diverse groups at position C4 and N7 of the pyrrolo[2,3-d]pyrimidine core and performed in vitro screening against MDA-MB-468 (breast cancer cell line) cell line. The details of the synthetic methods and characterization data of the synthesized compounds have been presented in this study. Compounds 08h, 09j, 09m, 09n, 09o showed excellent anticancer activity compared to standard doxorubicin IC 50 value on MDA-MB-468 (breast cancer cell line) which was non-toxic to normal vero cell line. N CN NH 2
Thiazole, a unique heterocycle containing sulphur and nitrogen atoms, occupies an important place... more Thiazole, a unique heterocycle containing sulphur and nitrogen atoms, occupies an important place in medicinal chemistry. It is an essential core scaffold present in many natural (Vitamin B1-Thiamine) and synthetic medicinally important compounds. The versatility of thiazole nucleus demonstrated by the fact that it is an essential part of penicillin nucleus and some of its derivatives which have shown antimicrobial (sulfazole), antiretroviral (ritonavir), antifungal (abafungin), antihistaminic and antithyroid activities. Present review describes biological importance of thiazoline derivatives with an emphasis on recent developments.
Oromucosal delivery of drugs promotes rapid absorption and high bioavailability, with faster onse... more Oromucosal delivery of drugs promotes rapid absorption and high bioavailability, with faster onset of pharmacological effect. However, many oromucosal delivery systems are compromised by the possibility of the patient swallowing the active substance before it has been released and absorbed locally into the systemic circulation. The present work introduces a new tablet system for sublingual administration in which the tablet is based on interactive mixtures of components, consisting of carrier particles partially covered by fine dry particles of the drug, in this case rabeprazole sodium. In the interests of increasing retention of the drug at the site of absorption in the oral cavity, a bioadhesive component was also added to the carrier particles. With this approach, it is possible to obtain rapid dissolution in combination with bioadhesive retention of the drug in the oral cavity. Rabeprazole sodium is an anti-ulcer drug having oral bioavailability 52% due to hepatic first pass metabolism. This work aims to avoid degradation of drug in acidic environment of stomach. In this study, rabeprazole sodium sublingual tablets were prepared by direct compression method using different bioadhesive polymers such as HPMC K4M and chitosan and sodium starch glycolate as a superdisintegrant. The effect of different concentration of polymers and super-disintegrating agents was measured by applying Box-Behnken design. The prepared tablets were evaluated for thickness, weight variation, hardness, friability, disintegration time, wetting time, bioadhesive strength, surface pH, drug content and in vitro drug release. FT-IR spectroscopy study revealed that there was no possible interaction between drug and polymers. Our results show that optimized formulation showed bioadhesive strength 12.34 ± 0.695 gm along with disintegration time 48.45 ± 0.230 seconds and in vitro drug release 95.98% in 10 min.
The objective of present study was to develop chitosan based sustained release Itopride Hydrochlo... more The objective of present study was to develop chitosan based sustained release Itopride Hydrochloride microspheres to reduce the dosing frequency. The Itopride Hydrochloride loaded chitosan microspheres were formulated by Emulsion cross linking method. Drug excipients compatibility study by FTIR showed no interaction between drug and excipients. The percentage Entrapment efficiency was found to be 56.26 ± 1.78 % to 77.85 ± 1.97 % and mean particle size range 77.67 ± 2.15 µm-142.02 ± 2.18 µm. The Batch R9 showed that 26.35 ± 1.22 % and 100.08 ± 1.34% drug release at 1 h and 24 h respectively. From all Parameter, it was concluded that drug release rate decreased with an increase the drug: polymer ratio and volume of glutaraldehyde. The in vitro release kinetics revealed korsmeyer-peppas model is followed and drug release is by fickian diffusion. From the SEM study observed that microspheres were spherical and fairly smooth surface.
Improvement of patient's compliance has always a challenge towards the development of oral drug d... more Improvement of patient's compliance has always a challenge towards the development of oral drug delivery system. Recent advances in Novel Drug Delivery Systems (NDDS) aim was to manufacture and administrate patients convenient dosage form. It was said to be a best alternative to conventional dosage to the patients having swallowing problems, psychic, paediatrics, geriatric and bedridden , unconscious patients. FDTs are solid with liquid unit dosage forms, which disintegrate or dissolve rapidly(within or less than 60 min) in the mouth without chewing and water. In particular, this review describes in detail on FDT mechanisms, Properties of FDT, advantages and disadvantages, ingredients used in dosage, evaluation, FDT technologies (based on lyophilization, molding, sublimation, and compaction, spray drying), rescent trends on FDT and case study on FDT.
Oral administration is one of the most convenient forms for the intake of drug due to ease of adm... more Oral administration is one of the most convenient forms for the intake of drug due to ease of administration, painless, versatility, and paramount patient compliance. The demand of fast disintegrating tablets has been growing, during the last decades especially for geriatric and pediatric patients due to dysphasia. Despite of tremendous innovations in drug delivery, the oral route remains the preferred route for administration of therapeutic agents because of accurate dosage, low cost therapy, self-medication, non-invasive method and ease of administration which ultimately lead to high level of patient compliance. Peroral administration of drug has disadvantages such as Hepatic first pass metabolism and enzymatic degradation within the GI tract that limits oral administration of certain classes of drug like peptides and proteins. So, other absorptive mucosa is considered as potential sites for drug administration. Trans-mucosal routes of drug delivery (i.e. the mucosal linings of the nasal, rectal, vaginal, ocular, and oral cavity) offer several advantages over peroral administration for systemic delivery.
Meloxicam, a preferential COX-2 inhibitor was found to be potential chemopreventive agents of col... more Meloxicam, a preferential COX-2 inhibitor was found to be potential chemopreventive agents of colorectal cancer. Hence, the local targeting of Meloxicam in colon was proved to be effective tools for the treatment of colorectal cancer. In the light of this information, the objective of the present study was to develop a colon targeted meloxicam tablet to achieve site-specific and instant drug release in the colon for potential application in the treatment of colorectal cancer. Meloxicam is an extremely poorly soluble acidic drug, having a pH-dependent solubility. Thus, in order to achieve pH-independent drug release of meloxicam, buffering agents (Magnesium Hydroxide) were used. Meloxicam Core tablet was prepared by direct compression method and coated with a polymeric solution of 2.5% w/v Eudragit S 100 using Acetone: Isopropyl alcohol (60:40) as a solvent by pan coating technique to achieve different total percentage weight gain. The coated tablets were evaluated in-vitro for their suitability as colon specific drug delivery systems. Meloxicam tablet containing 4% Crospovidone and 2% Croscarmellose sodium with 10% weight gain (F12) retained their physical integrity up to 5 hours corresponding to the colonic arrival time and showed instant drug release after reached in colon. The drug content was found to be 96.96% and within the USP standard. This study demonstrated that colon targeted meloxicam tablet exhibited promising targeting and hence can be used for treatment of colorectal cancer.
A novel, Simple, specific, safe and economical method of spectrophotometric estimation in UV regi... more A novel, Simple, specific, safe and economical method of spectrophotometric estimation in UV region has been developed and validated by using Methanol as a solvent for the quantitative determination of Tadalafil and Dapoxetine HCl in tablet dosage form. Simultaneous equation method was described for the simultaneous estimation of Tadalafil and Dapoxetine HCl in tablet. The absorption maxima were found to be at 284 nm (λ max of Tadalafil) and 290 nm (λ max of Dapoxetine HCl) in Methanol and these wavelengths were selected for the analysis. The proposed method follows Beer's linearity in the range of 3-15 μg/ml for Tadalafil and 10-50 μg/ml for Dapoxetine HCl with correlation coefficient values(R 2) 0.999 for Tadalafil and Dapoxetine HCl. According to ICH guidelines the parameters linearity, precision, accuracy, LOD and LOQ were studied, the results of analysis were validated statistically and by recovery studies. The proposed methods were simple, cost effective and were successfully applied to the estimation of these drugs in quality control of combined pharmaceutical dosage.
A simple, accurate, rapid, specific, accurate, economical, precise, reproducible and sensitive RP... more A simple, accurate, rapid, specific, accurate, economical, precise, reproducible and sensitive RP-HPLC method was developed for determination of Tadalafil and Dapoxetine Hydrochloride in tablet dosage form. The chromatographic was performed on Kromasil C18 column (250 mm X 4.6 mm, 5 µm), with a mobile phase comprising of a mixture of ACN: buffer (10:90 v/v, pH 5.5 adjusted with ortho phosphoric acid and diethyl ether), at a flow rate was 1.0 mL/min. Detection was carried out at 290 nm. The Retention time of TDF and DAPO were found to be 2.806 min and 5.965 min, respectively. As per ICH guidelines, the method was validated for linearity, precision, solution stability, accuracy, robustness, system suitability, limit of detection and limit of quantification. Linearity was found to be in the range 1-5 μg/ml for TDF and 3-15 μg/ml for DAPO. The low % RSD values indicate the method to be accurate and precise. The LOD and LOQ for TDF were found to be 0.010 μg/ml and 0.030 μg/ml, respectively. The LOD and LOQ for DAPO were found to be 0.020 μg/ml and 0.062 μg/ml, respectively. The % recovery of tablets found to be in range of 99-100%. Developed and validated HPLC method can be applied successfully for routine analysis of TDF and DAPO in tablets.
Dissolution rate of inclusion complex of Atorvastatin calcium (AT) (10.23mg equivalent to 10mg of... more Dissolution rate of inclusion complex of Atorvastatin calcium (AT) (10.23mg equivalent to 10mg of Atorvastatin), Fenofibrate (FE) (160mg) and Ezetimibe (EZ) (10mg) with β-cyclodextrin (β-CD) were investigated. The phase solubility profiles of AT, FE and EZ with β-CD were classified as AL-type, which indicated the formation of 1:1 stoichiometry inclusion complexes. Stability constants with 1:1 molar ratio obtained from the phase solubility diagrams were 550.60 M-1 , 2020.61 M-1 and 1604.05 M-1 for AT, FE and EZ respectively. Quaternary systems of AT, FE and EZ with β-CD prepared by kneading and co-evaporation method were characterized by Differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRD). The dissolution profiles of inclusion complexes were determined and compared with those of AT, FE and EZ and physical mixtures with β-CD. The dissolution rate of AT, FE and EZ were increased by β-CD inclusion complexation. Highest dissolution rate was obtained by co-evaporation method followed by kneading method. However, the dissolution rate were increased significantly (p < 0.05) by co-evaporation method compared to kneading method.
Objectives: Nicorandil is a potassium channel opener and used in treatment of angina. It has a sh... more Objectives: Nicorandil is a potassium channel opener and used in treatment of angina. It has a short half life of 1 hrs, so it requires frequent administration. The objective of present study was to develop sustained release Nicorandil microspheres. Method: The microspheres for sustained delivery of Nicorandil were formulated using ethyl cellulose polymer by non aqueous solvent evaporation method and study the effect different variables such as drug: polymer ratio and heavy: light liquid paraffin ratio on % Yield, % Entrapment efficiency, particle size and In vitro drug release. Results: The Entrapment efficiency was found to be 85.33% to 88.65% and In-vitro release study showed release of drug 98.25 % up to 12 hours. Conclusions: It was found that increases the concentration of Heavy liquid paraffin resulted in decrease the particle size and increase the release rate. Drug: Polymer ratio had significant effect on % Yield, % Entrapment efficiency, and particle size and release rate.
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions ... more The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac. The present work describes the formulation and evaluation of an ophthalmic delivery system of an anti-bacterial agent-Norfloxacin, based on the concept of an ion activated in situ gelation. Sodium alginate was used as the gelling agent in combination with Hydroxy Propyl Methyl Cellulose (HPMC K4M) which acted as a viscosity enhancing agent. The prepared formulations were characterized for clarity, pH, drug content, viscosity, gelling capacity, in vitro drug release, antimicrobial efficacy, ocular irritation and stability. The clarity, pH viscosity and drug content of the developed formulation were found to be satisfactory. The developed formulation was therapeutically efficacious, stable, non-irritant, and provided sustained drug release over an 8-h period. The developed formulation is a viable alternative to conventional eye drops by virtue of its ability to enhance bioavailability through its longer precorneal residence time and ability to produce sustained drug release. Also important factor is the ease of instillation and the reduced frequency of instillation resulting in better patient acceptance. Key words: In situ gelling, sodium alginate, norfloxacin, antimicrobial efficacy. W WO OR RL LD D J JO OU UR RN NA AL L O OF F P PH HA AR RM MA AC CY Y A AN ND D P PH HA AR RM MA AC CE EU UT TI IC CA AL L S SC CI IE EN NC CE ES S V Vo ol lu um me e 2 2, , I Is ss su ue e 6 6, , 5 58 88 88 8-5 58 89 97 7.. R Re es se ea ar rc ch h A Ar rt ti ic cl le e I
Tramadol HCl was microencapsulated with Ethylcellulose using multiple emulsion solvent evaporatio... more Tramadol HCl was microencapsulated with Ethylcellulose using multiple emulsion solvent evaporation method. A 3 2 factorial design employed to study the effect of drug: polymer ratio and volume of External phase (1% PVA) on % yield, % encapsulation efficiency, particle size, % drug release rate. The drug: polymer ratio and volume of continuous phase were significant effect on % yield, % entrapment efficiency, particle size, % drug release rate. % drug release was Biphasic system first initially bursting effect and finally sustained. Higher Percentage yield (77.4%) and Higher Percentage Encapsulation Efficiency(31.1%) were observed in Batch EC3. All the microspheres were spherical in nature its surface was smooth observed in SEM report.
Transdermal drug delivery is one of the most promising methods for drug application. The administ... more Transdermal drug delivery is one of the most promising methods for drug application. The administration of drugs by transdermal route offers the advantage of being relatively painless. Drug delivery with Transdermal patch systems exhibit slow, controlled drug release and absorption. Controlled drug delivery can be achieved by transdermal drug delivery system which can deliver the drug through skin to the systemic circulation at a predetermine rate over a prolonged period of time. Skin penetration enhancement technique have been developed to improve the bioavailability and increase the range of drug for which the transdermal and topical route is viable option. Characterization of transdermal patch is use to check it's quality, size, time of onset & duration, adhesive property, thickness, weight of patch, moisture of content, uniformity & cutaneous toxicological studies. The market for transdermal products has been in a significant upward trend that is likely to continue for the foreseeable future.
Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems ... more Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. From the formulation and technological point of view, the floating drug delivery system is comparatively easy and logical approach. The present review addresses briefly about the floating drug delivery systems. It also summarizes methods of evaluation of various floating dosage forms and applications of these systems. KEYWORDS: Floating drug delivery system, evaluation and applications. INTRODUCTION [1,2,3] The oral route is considered as the most promising route of drug delivery. Conventional drug delivery system achieves as well as maintains the drug concentration within the therapeutically effective range needed for treatment, only when taken several times a day. This results in a significant fluctuation in drug levels. Recently, several technical advancements have led to the development of several novel drug delivery systems (NDDS) that could revolutionize method of medication and provide a number of therapeutic benefits. The most important objectives of these new drug delivery systems are: First, it would be single dose, which releases the active ingredient over an extended period of time. Second, it should deliver the active entity directly to the site of action, thus minimizing or eliminating side effects. To overcome the limitations of conventional drug delivery system, oral controlled drug delivery system came into existence.
Objectives: Nicorandil is a potassium channel opener and used in treatment of angina. It has a sh... more Objectives: Nicorandil is a potassium channel opener and used in treatment of angina. It has a short half life of 1 hrs, so it requires frequent administration. The objective of present study was to develop sustained release Nicorandil microspheres. Method: The microspheres for sustained delivery of Nicorandil were formulated using ethyl cellulose polymer by non aqueous solvent evaporation method and study the effect different variables such as drug: polymer ratio and heavy: light liquid paraffin ratio on % Yield, % Entrapment efficiency, particle size and In vitro drug release. Results: The Entrapment efficiency was found to be 85.33% to 88.65% and In-vitro release study showed release of drug 98.25 % up to 12 hours. Conclusions: It was found that increases the concentration of Heavy liquid paraffin resulted in decrease the particle size and increase the release rate. Drug: Polymer ratio had significant effect on % Yield, % Entrapment efficiency, and particle size and release rate.
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions ... more The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac. Norfloxacin ophthalmic solution has been shown to be effective ocular infections and may be used in patients with chronic conjunctivitis or ocular irritation. Norfloxacin in-situ gel was prepared using various concentrations of polymers such as Carbopol-934 and HPMC K4M by pH triggered gelling system with objectives of increasing contact time, achieving controlled release, reduction in frequency of administration and greater therapeutic efficacy of drug. The prepared in-situ gels were then evaluated for their visual appearance, clarity, pH, drug content analysis, in-vitro gelation (Gelling capacity), rheological studies, sterility testing and in-vitro drug release studies. It is evident from these studies that, formed polymeric in-situ gels had transparent, clear possessing satisfactory gelling capacity. The developed formulation was light yellow in colour, therapeutically efficacious, stable, non-irritant with sustained release of drug. INTRODUCTION: Extensive research has been carried in designing of polymeric drug delivery systems. The development of in situ gel systems has received considerable attention over the past few years. The in situ gelling polymers undergo sol-to-gel phase transition on exposure to the physiological conditions present in the eye. Insitu gels are viscous polymer-based liquids that exhibit sol-to-gel phase transition on the ocular surface due to change in a specific physico-chemical parameter (ionic strength, temperature or pH) 1 .
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions ... more The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac. The present work describes the formulation and evaluation of an ophthalmic delivery system of an anti-bacterial agent-Norfloxacin, based on the concept of pH-triggered in situ gelation. Polyacrylic acid (Carbopol-934) was used as the gelling agent in combination with HPMC K4 M which acted as a viscosity enhancing agent. The developed formulation was therapeutically efficacious, stable, non-irritant and provided sustained release of the drug over a period of 8-hours. The developed system is thus a viable alternative to conventional eye drops.
Nanotechnology is the science that deals with the processes tha t occur at molecular level and of... more Nanotechnology is the science that deals with the processes tha t occur at molecular level and of nanolength scale size. There are numerous examples from nature like DNA, water molecules, virus, red blood corpuscles (RBC) etc., which are of nanodimensions. Recent developments in nanotechnology offer researchers opportunities to significantly transform various therapeutics. This technology has enabled the manipulation of the biological and physicochemical properties of nanomaterial to facilitate more efficient drug targeting and delivery. The size of nanomaterial is similar to that of most biological molecules and structures; therefore, nanomaterial can be useful for both in vivo and in vitro biomedical research and applications. Clinical investigations suggest that therapeutic nanoparticles can enhance efficacy and reduced side effects c ompared with conventional therapeutic drugs. Nanotechnology is on its way to make a big impact in Biotech, Pharmaceutical and Medical diagnostics s...
Fluoroquinolones is major antibacterial group comprising antimicrobial agent with wide antibacter... more Fluoroquinolones is major antibacterial group comprising antimicrobial agent with wide antibacterial spectrum though differences exist between compounds in their potency against Gram positive and Gram Negative bacteria. Present study was carried out in order to find out current status regarding resistance to seven fluoroquinolones by E.coli, Klebsiella spp. Pseudomonas aeruginosa and Proteus spp. ,recovered from hospitalized patients. The overall result showed resistance to Levofloxacin(75.29%),Gatifloxacin(48.23%),Lomefloxacin(80%),Sparfloxacin(92.94%), Ciprofloxacin (72.94%), Norfloxacin(72.94%), and Ofloxacin(76.47%).
Pyrrolopyrimidines are well known scaffold which play a critical role as anticancer agents so it ... more Pyrrolopyrimidines are well known scaffold which play a critical role as anticancer agents so it was thought of interest to synthesize series of novel substituted pyrrolo[2,3-d]pyrimidines having diverse groups at position C4 and N7 of the pyrrolo[2,3-d]pyrimidine core and performed in vitro screening against MDA-MB-468 (breast cancer cell line) cell line. The details of the synthetic methods and characterization data of the synthesized compounds have been presented in this study. Compounds 08h, 09j, 09m, 09n, 09o showed excellent anticancer activity compared to standard doxorubicin IC 50 value on MDA-MB-468 (breast cancer cell line) which was non-toxic to normal vero cell line. N CN NH 2
Thiazole, a unique heterocycle containing sulphur and nitrogen atoms, occupies an important place... more Thiazole, a unique heterocycle containing sulphur and nitrogen atoms, occupies an important place in medicinal chemistry. It is an essential core scaffold present in many natural (Vitamin B1-Thiamine) and synthetic medicinally important compounds. The versatility of thiazole nucleus demonstrated by the fact that it is an essential part of penicillin nucleus and some of its derivatives which have shown antimicrobial (sulfazole), antiretroviral (ritonavir), antifungal (abafungin), antihistaminic and antithyroid activities. Present review describes biological importance of thiazoline derivatives with an emphasis on recent developments.
Oromucosal delivery of drugs promotes rapid absorption and high bioavailability, with faster onse... more Oromucosal delivery of drugs promotes rapid absorption and high bioavailability, with faster onset of pharmacological effect. However, many oromucosal delivery systems are compromised by the possibility of the patient swallowing the active substance before it has been released and absorbed locally into the systemic circulation. The present work introduces a new tablet system for sublingual administration in which the tablet is based on interactive mixtures of components, consisting of carrier particles partially covered by fine dry particles of the drug, in this case rabeprazole sodium. In the interests of increasing retention of the drug at the site of absorption in the oral cavity, a bioadhesive component was also added to the carrier particles. With this approach, it is possible to obtain rapid dissolution in combination with bioadhesive retention of the drug in the oral cavity. Rabeprazole sodium is an anti-ulcer drug having oral bioavailability 52% due to hepatic first pass metabolism. This work aims to avoid degradation of drug in acidic environment of stomach. In this study, rabeprazole sodium sublingual tablets were prepared by direct compression method using different bioadhesive polymers such as HPMC K4M and chitosan and sodium starch glycolate as a superdisintegrant. The effect of different concentration of polymers and super-disintegrating agents was measured by applying Box-Behnken design. The prepared tablets were evaluated for thickness, weight variation, hardness, friability, disintegration time, wetting time, bioadhesive strength, surface pH, drug content and in vitro drug release. FT-IR spectroscopy study revealed that there was no possible interaction between drug and polymers. Our results show that optimized formulation showed bioadhesive strength 12.34 ± 0.695 gm along with disintegration time 48.45 ± 0.230 seconds and in vitro drug release 95.98% in 10 min.
The objective of present study was to develop chitosan based sustained release Itopride Hydrochlo... more The objective of present study was to develop chitosan based sustained release Itopride Hydrochloride microspheres to reduce the dosing frequency. The Itopride Hydrochloride loaded chitosan microspheres were formulated by Emulsion cross linking method. Drug excipients compatibility study by FTIR showed no interaction between drug and excipients. The percentage Entrapment efficiency was found to be 56.26 ± 1.78 % to 77.85 ± 1.97 % and mean particle size range 77.67 ± 2.15 µm-142.02 ± 2.18 µm. The Batch R9 showed that 26.35 ± 1.22 % and 100.08 ± 1.34% drug release at 1 h and 24 h respectively. From all Parameter, it was concluded that drug release rate decreased with an increase the drug: polymer ratio and volume of glutaraldehyde. The in vitro release kinetics revealed korsmeyer-peppas model is followed and drug release is by fickian diffusion. From the SEM study observed that microspheres were spherical and fairly smooth surface.
Improvement of patient's compliance has always a challenge towards the development of oral drug d... more Improvement of patient's compliance has always a challenge towards the development of oral drug delivery system. Recent advances in Novel Drug Delivery Systems (NDDS) aim was to manufacture and administrate patients convenient dosage form. It was said to be a best alternative to conventional dosage to the patients having swallowing problems, psychic, paediatrics, geriatric and bedridden , unconscious patients. FDTs are solid with liquid unit dosage forms, which disintegrate or dissolve rapidly(within or less than 60 min) in the mouth without chewing and water. In particular, this review describes in detail on FDT mechanisms, Properties of FDT, advantages and disadvantages, ingredients used in dosage, evaluation, FDT technologies (based on lyophilization, molding, sublimation, and compaction, spray drying), rescent trends on FDT and case study on FDT.
Oral administration is one of the most convenient forms for the intake of drug due to ease of adm... more Oral administration is one of the most convenient forms for the intake of drug due to ease of administration, painless, versatility, and paramount patient compliance. The demand of fast disintegrating tablets has been growing, during the last decades especially for geriatric and pediatric patients due to dysphasia. Despite of tremendous innovations in drug delivery, the oral route remains the preferred route for administration of therapeutic agents because of accurate dosage, low cost therapy, self-medication, non-invasive method and ease of administration which ultimately lead to high level of patient compliance. Peroral administration of drug has disadvantages such as Hepatic first pass metabolism and enzymatic degradation within the GI tract that limits oral administration of certain classes of drug like peptides and proteins. So, other absorptive mucosa is considered as potential sites for drug administration. Trans-mucosal routes of drug delivery (i.e. the mucosal linings of the nasal, rectal, vaginal, ocular, and oral cavity) offer several advantages over peroral administration for systemic delivery.
Meloxicam, a preferential COX-2 inhibitor was found to be potential chemopreventive agents of col... more Meloxicam, a preferential COX-2 inhibitor was found to be potential chemopreventive agents of colorectal cancer. Hence, the local targeting of Meloxicam in colon was proved to be effective tools for the treatment of colorectal cancer. In the light of this information, the objective of the present study was to develop a colon targeted meloxicam tablet to achieve site-specific and instant drug release in the colon for potential application in the treatment of colorectal cancer. Meloxicam is an extremely poorly soluble acidic drug, having a pH-dependent solubility. Thus, in order to achieve pH-independent drug release of meloxicam, buffering agents (Magnesium Hydroxide) were used. Meloxicam Core tablet was prepared by direct compression method and coated with a polymeric solution of 2.5% w/v Eudragit S 100 using Acetone: Isopropyl alcohol (60:40) as a solvent by pan coating technique to achieve different total percentage weight gain. The coated tablets were evaluated in-vitro for their suitability as colon specific drug delivery systems. Meloxicam tablet containing 4% Crospovidone and 2% Croscarmellose sodium with 10% weight gain (F12) retained their physical integrity up to 5 hours corresponding to the colonic arrival time and showed instant drug release after reached in colon. The drug content was found to be 96.96% and within the USP standard. This study demonstrated that colon targeted meloxicam tablet exhibited promising targeting and hence can be used for treatment of colorectal cancer.
A novel, Simple, specific, safe and economical method of spectrophotometric estimation in UV regi... more A novel, Simple, specific, safe and economical method of spectrophotometric estimation in UV region has been developed and validated by using Methanol as a solvent for the quantitative determination of Tadalafil and Dapoxetine HCl in tablet dosage form. Simultaneous equation method was described for the simultaneous estimation of Tadalafil and Dapoxetine HCl in tablet. The absorption maxima were found to be at 284 nm (λ max of Tadalafil) and 290 nm (λ max of Dapoxetine HCl) in Methanol and these wavelengths were selected for the analysis. The proposed method follows Beer's linearity in the range of 3-15 μg/ml for Tadalafil and 10-50 μg/ml for Dapoxetine HCl with correlation coefficient values(R 2) 0.999 for Tadalafil and Dapoxetine HCl. According to ICH guidelines the parameters linearity, precision, accuracy, LOD and LOQ were studied, the results of analysis were validated statistically and by recovery studies. The proposed methods were simple, cost effective and were successfully applied to the estimation of these drugs in quality control of combined pharmaceutical dosage.
A simple, accurate, rapid, specific, accurate, economical, precise, reproducible and sensitive RP... more A simple, accurate, rapid, specific, accurate, economical, precise, reproducible and sensitive RP-HPLC method was developed for determination of Tadalafil and Dapoxetine Hydrochloride in tablet dosage form. The chromatographic was performed on Kromasil C18 column (250 mm X 4.6 mm, 5 µm), with a mobile phase comprising of a mixture of ACN: buffer (10:90 v/v, pH 5.5 adjusted with ortho phosphoric acid and diethyl ether), at a flow rate was 1.0 mL/min. Detection was carried out at 290 nm. The Retention time of TDF and DAPO were found to be 2.806 min and 5.965 min, respectively. As per ICH guidelines, the method was validated for linearity, precision, solution stability, accuracy, robustness, system suitability, limit of detection and limit of quantification. Linearity was found to be in the range 1-5 μg/ml for TDF and 3-15 μg/ml for DAPO. The low % RSD values indicate the method to be accurate and precise. The LOD and LOQ for TDF were found to be 0.010 μg/ml and 0.030 μg/ml, respectively. The LOD and LOQ for DAPO were found to be 0.020 μg/ml and 0.062 μg/ml, respectively. The % recovery of tablets found to be in range of 99-100%. Developed and validated HPLC method can be applied successfully for routine analysis of TDF and DAPO in tablets.
Dissolution rate of inclusion complex of Atorvastatin calcium (AT) (10.23mg equivalent to 10mg of... more Dissolution rate of inclusion complex of Atorvastatin calcium (AT) (10.23mg equivalent to 10mg of Atorvastatin), Fenofibrate (FE) (160mg) and Ezetimibe (EZ) (10mg) with β-cyclodextrin (β-CD) were investigated. The phase solubility profiles of AT, FE and EZ with β-CD were classified as AL-type, which indicated the formation of 1:1 stoichiometry inclusion complexes. Stability constants with 1:1 molar ratio obtained from the phase solubility diagrams were 550.60 M-1 , 2020.61 M-1 and 1604.05 M-1 for AT, FE and EZ respectively. Quaternary systems of AT, FE and EZ with β-CD prepared by kneading and co-evaporation method were characterized by Differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRD). The dissolution profiles of inclusion complexes were determined and compared with those of AT, FE and EZ and physical mixtures with β-CD. The dissolution rate of AT, FE and EZ were increased by β-CD inclusion complexation. Highest dissolution rate was obtained by co-evaporation method followed by kneading method. However, the dissolution rate were increased significantly (p < 0.05) by co-evaporation method compared to kneading method.
Objectives: Nicorandil is a potassium channel opener and used in treatment of angina. It has a sh... more Objectives: Nicorandil is a potassium channel opener and used in treatment of angina. It has a short half life of 1 hrs, so it requires frequent administration. The objective of present study was to develop sustained release Nicorandil microspheres. Method: The microspheres for sustained delivery of Nicorandil were formulated using ethyl cellulose polymer by non aqueous solvent evaporation method and study the effect different variables such as drug: polymer ratio and heavy: light liquid paraffin ratio on % Yield, % Entrapment efficiency, particle size and In vitro drug release. Results: The Entrapment efficiency was found to be 85.33% to 88.65% and In-vitro release study showed release of drug 98.25 % up to 12 hours. Conclusions: It was found that increases the concentration of Heavy liquid paraffin resulted in decrease the particle size and increase the release rate. Drug: Polymer ratio had significant effect on % Yield, % Entrapment efficiency, and particle size and release rate.
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions ... more The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac. The present work describes the formulation and evaluation of an ophthalmic delivery system of an anti-bacterial agent-Norfloxacin, based on the concept of an ion activated in situ gelation. Sodium alginate was used as the gelling agent in combination with Hydroxy Propyl Methyl Cellulose (HPMC K4M) which acted as a viscosity enhancing agent. The prepared formulations were characterized for clarity, pH, drug content, viscosity, gelling capacity, in vitro drug release, antimicrobial efficacy, ocular irritation and stability. The clarity, pH viscosity and drug content of the developed formulation were found to be satisfactory. The developed formulation was therapeutically efficacious, stable, non-irritant, and provided sustained drug release over an 8-h period. The developed formulation is a viable alternative to conventional eye drops by virtue of its ability to enhance bioavailability through its longer precorneal residence time and ability to produce sustained drug release. Also important factor is the ease of instillation and the reduced frequency of instillation resulting in better patient acceptance. Key words: In situ gelling, sodium alginate, norfloxacin, antimicrobial efficacy. W WO OR RL LD D J JO OU UR RN NA AL L O OF F P PH HA AR RM MA AC CY Y A AN ND D P PH HA AR RM MA AC CE EU UT TI IC CA AL L S SC CI IE EN NC CE ES S V Vo ol lu um me e 2 2, , I Is ss su ue e 6 6, , 5 58 88 88 8-5 58 89 97 7.. R Re es se ea ar rc ch h A Ar rt ti ic cl le e I
Tramadol HCl was microencapsulated with Ethylcellulose using multiple emulsion solvent evaporatio... more Tramadol HCl was microencapsulated with Ethylcellulose using multiple emulsion solvent evaporation method. A 3 2 factorial design employed to study the effect of drug: polymer ratio and volume of External phase (1% PVA) on % yield, % encapsulation efficiency, particle size, % drug release rate. The drug: polymer ratio and volume of continuous phase were significant effect on % yield, % entrapment efficiency, particle size, % drug release rate. % drug release was Biphasic system first initially bursting effect and finally sustained. Higher Percentage yield (77.4%) and Higher Percentage Encapsulation Efficiency(31.1%) were observed in Batch EC3. All the microspheres were spherical in nature its surface was smooth observed in SEM report.
Transdermal drug delivery is one of the most promising methods for drug application. The administ... more Transdermal drug delivery is one of the most promising methods for drug application. The administration of drugs by transdermal route offers the advantage of being relatively painless. Drug delivery with Transdermal patch systems exhibit slow, controlled drug release and absorption. Controlled drug delivery can be achieved by transdermal drug delivery system which can deliver the drug through skin to the systemic circulation at a predetermine rate over a prolonged period of time. Skin penetration enhancement technique have been developed to improve the bioavailability and increase the range of drug for which the transdermal and topical route is viable option. Characterization of transdermal patch is use to check it's quality, size, time of onset & duration, adhesive property, thickness, weight of patch, moisture of content, uniformity & cutaneous toxicological studies. The market for transdermal products has been in a significant upward trend that is likely to continue for the foreseeable future.
Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems ... more Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. From the formulation and technological point of view, the floating drug delivery system is comparatively easy and logical approach. The present review addresses briefly about the floating drug delivery systems. It also summarizes methods of evaluation of various floating dosage forms and applications of these systems. KEYWORDS: Floating drug delivery system, evaluation and applications. INTRODUCTION [1,2,3] The oral route is considered as the most promising route of drug delivery. Conventional drug delivery system achieves as well as maintains the drug concentration within the therapeutically effective range needed for treatment, only when taken several times a day. This results in a significant fluctuation in drug levels. Recently, several technical advancements have led to the development of several novel drug delivery systems (NDDS) that could revolutionize method of medication and provide a number of therapeutic benefits. The most important objectives of these new drug delivery systems are: First, it would be single dose, which releases the active ingredient over an extended period of time. Second, it should deliver the active entity directly to the site of action, thus minimizing or eliminating side effects. To overcome the limitations of conventional drug delivery system, oral controlled drug delivery system came into existence.
Objectives: Nicorandil is a potassium channel opener and used in treatment of angina. It has a sh... more Objectives: Nicorandil is a potassium channel opener and used in treatment of angina. It has a short half life of 1 hrs, so it requires frequent administration. The objective of present study was to develop sustained release Nicorandil microspheres. Method: The microspheres for sustained delivery of Nicorandil were formulated using ethyl cellulose polymer by non aqueous solvent evaporation method and study the effect different variables such as drug: polymer ratio and heavy: light liquid paraffin ratio on % Yield, % Entrapment efficiency, particle size and In vitro drug release. Results: The Entrapment efficiency was found to be 85.33% to 88.65% and In-vitro release study showed release of drug 98.25 % up to 12 hours. Conclusions: It was found that increases the concentration of Heavy liquid paraffin resulted in decrease the particle size and increase the release rate. Drug: Polymer ratio had significant effect on % Yield, % Entrapment efficiency, and particle size and release rate.
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions ... more The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac. Norfloxacin ophthalmic solution has been shown to be effective ocular infections and may be used in patients with chronic conjunctivitis or ocular irritation. Norfloxacin in-situ gel was prepared using various concentrations of polymers such as Carbopol-934 and HPMC K4M by pH triggered gelling system with objectives of increasing contact time, achieving controlled release, reduction in frequency of administration and greater therapeutic efficacy of drug. The prepared in-situ gels were then evaluated for their visual appearance, clarity, pH, drug content analysis, in-vitro gelation (Gelling capacity), rheological studies, sterility testing and in-vitro drug release studies. It is evident from these studies that, formed polymeric in-situ gels had transparent, clear possessing satisfactory gelling capacity. The developed formulation was light yellow in colour, therapeutically efficacious, stable, non-irritant with sustained release of drug. INTRODUCTION: Extensive research has been carried in designing of polymeric drug delivery systems. The development of in situ gel systems has received considerable attention over the past few years. The in situ gelling polymers undergo sol-to-gel phase transition on exposure to the physiological conditions present in the eye. Insitu gels are viscous polymer-based liquids that exhibit sol-to-gel phase transition on the ocular surface due to change in a specific physico-chemical parameter (ionic strength, temperature or pH) 1 .