Journal of Pharmaceutical Technology, Research and Management, 2014
The poor bioavailability of cefotaxime and limitation of conventional system limits the delivery ... more The poor bioavailability of cefotaxime and limitation of conventional system limits the delivery of antibacterial drug cefotaxime for bone infection treatment. In the current study in situ chitosan implant containing cefotaxime was developed. Injectable implantable drug delivery system containing Cefotaxime was prepared by physically mixing β-glycerophosphate with chitosan in different concentrations. The objective of this study was to standardize the concentrations of the ingredients so as to develop formulation that remains liquid when stored at 4ºC but forms a gel, in minimum time, when injected or when its temperature is raised to 37oC. Injectable in-situ implant before injection was clear and transparent. Gelation temperature significantly increase from 32.6°C ±0.1 to 48.43°C ±0.1 of all formulation. Percentage drug content of all formulation were found in the range of 82.42±1.93 to 99.43±0.55. The syringeability of the final solutions greatly decreased with the increase of chi...
Generic products are the chemical, pharmaceutical, and biological equivalents of the innovator pr... more Generic products are the chemical, pharmaceutical, and biological equivalents of the innovator product that is already registered and currently in use in one or more countries. During development, generic products are subjected to a battery of stability tests to guide the choice of excipients, packaging material and processing conditions, and help establish shelf-life, storage conditions, hold time, and transportation environmental control. This chapter discusses key aspects of stability testing through the life cycle of a generic product.
Stability studies ensuring the maintenance of product quality, safety and efficacy throughout the... more Stability studies ensuring the maintenance of product quality, safety and efficacy throughout the shelf life are considered as prerequisite for the acceptance and approval of any pharmaceutical product. These studies are required to be conducted in a planned way following the guidelines issued by ICH, WHO and or other agencies. Importance of various methods followed for stability testing of pharmaceutical products, guidelines issued for stability testing and other aspects related to stability of pharmaceutical products have been presented in a concise manner in the present review
In the present study, the relationship between the Zagreb topochemical index M 1 c and the cortic... more In the present study, the relationship between the Zagreb topochemical index M 1 c and the corticotropin releasing factor receptor antagonizing activity of N-phenylphenylglycine analogs has been investigated. The values of Zagreb topochemical index M 1 c of all the analogs involved in the data set were calculated using an in-house computer program. The resulting data was analyzed and a suitable model was developed after identification of the active range. Subsequently, a biological activity was assigned to each of the compounds involved in the dataset which was then compared with the reported biological activity. Accuracy of prediction was found to be 82.3% using the said model. High predictability of the model offers vast potential for providing lead structures for development of potent CRF receptor antagonist.
Frequent failure of drug candidates during development stages remains the major deterrent for an ... more Frequent failure of drug candidates during development stages remains the major deterrent for an early introduction of new drug molecules. The drug toxicity is the major cause of expensive late-stage development failures. An early identification/optimization of the most favorable molecule will naturally save considerable cost, time, human efforts and minimize animal sacrifice. (Quantitative) Structure Activity Relationships [(Q)SARs] represent statistically derived predictive models correlating biological activity (including desirable therapeutic effect and undesirable side effects) of chemicals (drugs/toxicants/environmental pollutants) with molecular descriptors and/or properties. (Q)SAR models which categorize the available data into two or more groups/classes are known as classification models. Numerous techniques of diverse nature are being presently employed for development of classification models. Though there is an increasing use of classification models for prediction of either biological activity or toxicity, the future trend will naturally be towards the development of classification models capable of simultaneous prediction of biological activity, toxicity, and pharmacokinetic parameters so as to accelerate development of bioavailable safe drug molecules.
A modification of Wiener's index, termed as Wiener's topochemical index... more A modification of Wiener's index, termed as Wiener's topochemical index (Wc), has been conceptualized. This topochemical index is not only sensitive to the presence of heteroatoms but also exhibits far less degeneracy when compared to Wiener's index. The relationship of the Wiener's topochemical index and Wiener's index with the anti-HIV activity of phenethylthiazolethiourea (PETT) compounds was investigated. The values of
A novel highly discriminating adjacency‐cum‐distance based topochemical descriptor, termed as Sup... more A novel highly discriminating adjacency‐cum‐distance based topochemical descriptor, termed as Superadjacency topochemical index, has been derived and its discriminating power investigated with regard to activation of Carbonic anhydrase (CA) isozyme‐I by tri‐/tetrasubstituted‐pyridinium‐azole compounds. The new index is not only sensitive to the presence of heteroatoms but also overcomes the problem of degeneracy of many topological descriptors. The discriminating power of Superadjacency topochemical index was found to be far superior when compared with that of distance based Wiener's index and adjacency based Molecular connectivity index. The values of Wiener's index, path‐one Molecular connectivity index and Superadjacency topochemical index of each of the 42 substituted‐pyridinium‐azole compounds comprising the dataset were computed. Resultant data was analyzed and suitable models developed after identification of the active ranges. Subsequently, a biological activity was ...
Relationship between topochemical indices and anti-HIV activity of 4-Benzyl pyridinone derivative... more Relationship between topochemical indices and anti-HIV activity of 4-Benzyl pyridinone derivatives has been investigated. The values of molecular connectivity topochemical index (an adjacency based topochemical descriptor) Wiener's topochemical index (a distance based topochemical descriptor) and superadjacency topochemical index (an adjacency cum distance based topochemical descriptor) were calculated for each of the 32 compounds comprising the data set using an in-house computer program. The resultant data was analyzed and suitable models were developed after identification of the active ranges. Subsequently, a biological activity was assigned using these models to each of the compounds involved in the dataset which was then compared with the reported anti-HIV activity. Exceptionally high accuracy of prediction was observed using these models. These models offer vast potential for providing lead structures for the development of potent anti-HIV agents.
Over the past decade, use of microwave energy, to heat chemical reactants on a laboratory scale, ... more Over the past decade, use of microwave energy, to heat chemical reactants on a laboratory scale, has evolved as a well-demonstrated alternative to traditional heating. Clean chemistry, reduction in reaction times, improved yields, and applicability to wide range of reactions, greatly improved efficiency with better quality, safety and tremendous scope for automation are some of the benefits of this emerging technology. Association of biological activity with heterocyclic motifs is well known and is important from drug discovery viewpoint. This article gives an account of the recent applications of microwaves in the synthesis of biologically active heterocyclic compounds with synthesis schemes and/or comprehensive review of reaction conditions and biological importance of over 50 such applications.
... To teach a man how he may learn to grow independently, and for himself, is perhaps the great... more ... To teach a man how he may learn to grow independently, and for himself, is perhaps the greatest service that one man can do for another. - Benjamin Jowett. I wish to express my sincere gratitude to my revered teacher, counselor and co-supervisor Prof. AK Madan, for ...
Relationship between topochemical indices and anti-HIV-1 (HTLV-III) inhibitory activity of 1-alko... more Relationship between topochemical indices and anti-HIV-1 (HTLV-III) inhibitory activity of 1-alkoxy-5-alkyl-6-(arylthio)uracils has been studied. Superadjacency, an adjacency-cum-distance-based, topochemical index and Wiener’s, a distance-based, topochemical index were calculated for a set of 36 1-alkoxy-5-alkyl-6-(arylthio)uracils. Resulting data were analyzed and suitable models were developed after identification of the active ranges. Subsequently, a biological activity was assigned to each of the compounds using these models and compared with the reported anti-HIV-1 activity. High accuracy of prediction was observed using these models. Statistical analysis revealed significance of the proposed models as well as a lack of correlation between the topochemical indices employed for the chosen data set.
The relationship between the superadjacency topochemical index and the anti-HIV activity of HEPT ... more The relationship between the superadjacency topochemical index and the anti-HIV activity of HEPT analogs has been investigated in the present study. The values of superadjacency topochemical index of all the analogs involved in the data set were calculated using an in-house computer program. Resulting data were analyzed and a suitable model was developed after identification of the active range. Subsequently, a computed biological activity was assigned to each of the compounds involved in the dataset, which was then compared with the reported anti-HIV activity. Accuracy of prediction was found to be 88% using the said model. The predictive ability of the model indicates that this model can be used for predicting the anti-HIV activity of the compounds prior to synthesis and may prove to be highly beneficial for providing lead structures for development of potent anti-HIV agents.
Journal of Pharmaceutical Technology, Research and Management, 2014
The poor bioavailability of cefotaxime and limitation of conventional system limits the delivery ... more The poor bioavailability of cefotaxime and limitation of conventional system limits the delivery of antibacterial drug cefotaxime for bone infection treatment. In the current study in situ chitosan implant containing cefotaxime was developed. Injectable implantable drug delivery system containing Cefotaxime was prepared by physically mixing β-glycerophosphate with chitosan in different concentrations. The objective of this study was to standardize the concentrations of the ingredients so as to develop formulation that remains liquid when stored at 4ºC but forms a gel, in minimum time, when injected or when its temperature is raised to 37oC. Injectable in-situ implant before injection was clear and transparent. Gelation temperature significantly increase from 32.6°C ±0.1 to 48.43°C ±0.1 of all formulation. Percentage drug content of all formulation were found in the range of 82.42±1.93 to 99.43±0.55. The syringeability of the final solutions greatly decreased with the increase of chi...
Generic products are the chemical, pharmaceutical, and biological equivalents of the innovator pr... more Generic products are the chemical, pharmaceutical, and biological equivalents of the innovator product that is already registered and currently in use in one or more countries. During development, generic products are subjected to a battery of stability tests to guide the choice of excipients, packaging material and processing conditions, and help establish shelf-life, storage conditions, hold time, and transportation environmental control. This chapter discusses key aspects of stability testing through the life cycle of a generic product.
Stability studies ensuring the maintenance of product quality, safety and efficacy throughout the... more Stability studies ensuring the maintenance of product quality, safety and efficacy throughout the shelf life are considered as prerequisite for the acceptance and approval of any pharmaceutical product. These studies are required to be conducted in a planned way following the guidelines issued by ICH, WHO and or other agencies. Importance of various methods followed for stability testing of pharmaceutical products, guidelines issued for stability testing and other aspects related to stability of pharmaceutical products have been presented in a concise manner in the present review
In the present study, the relationship between the Zagreb topochemical index M 1 c and the cortic... more In the present study, the relationship between the Zagreb topochemical index M 1 c and the corticotropin releasing factor receptor antagonizing activity of N-phenylphenylglycine analogs has been investigated. The values of Zagreb topochemical index M 1 c of all the analogs involved in the data set were calculated using an in-house computer program. The resulting data was analyzed and a suitable model was developed after identification of the active range. Subsequently, a biological activity was assigned to each of the compounds involved in the dataset which was then compared with the reported biological activity. Accuracy of prediction was found to be 82.3% using the said model. High predictability of the model offers vast potential for providing lead structures for development of potent CRF receptor antagonist.
Frequent failure of drug candidates during development stages remains the major deterrent for an ... more Frequent failure of drug candidates during development stages remains the major deterrent for an early introduction of new drug molecules. The drug toxicity is the major cause of expensive late-stage development failures. An early identification/optimization of the most favorable molecule will naturally save considerable cost, time, human efforts and minimize animal sacrifice. (Quantitative) Structure Activity Relationships [(Q)SARs] represent statistically derived predictive models correlating biological activity (including desirable therapeutic effect and undesirable side effects) of chemicals (drugs/toxicants/environmental pollutants) with molecular descriptors and/or properties. (Q)SAR models which categorize the available data into two or more groups/classes are known as classification models. Numerous techniques of diverse nature are being presently employed for development of classification models. Though there is an increasing use of classification models for prediction of either biological activity or toxicity, the future trend will naturally be towards the development of classification models capable of simultaneous prediction of biological activity, toxicity, and pharmacokinetic parameters so as to accelerate development of bioavailable safe drug molecules.
A modification of Wiener's index, termed as Wiener's topochemical index... more A modification of Wiener's index, termed as Wiener's topochemical index (Wc), has been conceptualized. This topochemical index is not only sensitive to the presence of heteroatoms but also exhibits far less degeneracy when compared to Wiener's index. The relationship of the Wiener's topochemical index and Wiener's index with the anti-HIV activity of phenethylthiazolethiourea (PETT) compounds was investigated. The values of
A novel highly discriminating adjacency‐cum‐distance based topochemical descriptor, termed as Sup... more A novel highly discriminating adjacency‐cum‐distance based topochemical descriptor, termed as Superadjacency topochemical index, has been derived and its discriminating power investigated with regard to activation of Carbonic anhydrase (CA) isozyme‐I by tri‐/tetrasubstituted‐pyridinium‐azole compounds. The new index is not only sensitive to the presence of heteroatoms but also overcomes the problem of degeneracy of many topological descriptors. The discriminating power of Superadjacency topochemical index was found to be far superior when compared with that of distance based Wiener's index and adjacency based Molecular connectivity index. The values of Wiener's index, path‐one Molecular connectivity index and Superadjacency topochemical index of each of the 42 substituted‐pyridinium‐azole compounds comprising the dataset were computed. Resultant data was analyzed and suitable models developed after identification of the active ranges. Subsequently, a biological activity was ...
Relationship between topochemical indices and anti-HIV activity of 4-Benzyl pyridinone derivative... more Relationship between topochemical indices and anti-HIV activity of 4-Benzyl pyridinone derivatives has been investigated. The values of molecular connectivity topochemical index (an adjacency based topochemical descriptor) Wiener's topochemical index (a distance based topochemical descriptor) and superadjacency topochemical index (an adjacency cum distance based topochemical descriptor) were calculated for each of the 32 compounds comprising the data set using an in-house computer program. The resultant data was analyzed and suitable models were developed after identification of the active ranges. Subsequently, a biological activity was assigned using these models to each of the compounds involved in the dataset which was then compared with the reported anti-HIV activity. Exceptionally high accuracy of prediction was observed using these models. These models offer vast potential for providing lead structures for the development of potent anti-HIV agents.
Over the past decade, use of microwave energy, to heat chemical reactants on a laboratory scale, ... more Over the past decade, use of microwave energy, to heat chemical reactants on a laboratory scale, has evolved as a well-demonstrated alternative to traditional heating. Clean chemistry, reduction in reaction times, improved yields, and applicability to wide range of reactions, greatly improved efficiency with better quality, safety and tremendous scope for automation are some of the benefits of this emerging technology. Association of biological activity with heterocyclic motifs is well known and is important from drug discovery viewpoint. This article gives an account of the recent applications of microwaves in the synthesis of biologically active heterocyclic compounds with synthesis schemes and/or comprehensive review of reaction conditions and biological importance of over 50 such applications.
... To teach a man how he may learn to grow independently, and for himself, is perhaps the great... more ... To teach a man how he may learn to grow independently, and for himself, is perhaps the greatest service that one man can do for another. - Benjamin Jowett. I wish to express my sincere gratitude to my revered teacher, counselor and co-supervisor Prof. AK Madan, for ...
Relationship between topochemical indices and anti-HIV-1 (HTLV-III) inhibitory activity of 1-alko... more Relationship between topochemical indices and anti-HIV-1 (HTLV-III) inhibitory activity of 1-alkoxy-5-alkyl-6-(arylthio)uracils has been studied. Superadjacency, an adjacency-cum-distance-based, topochemical index and Wiener’s, a distance-based, topochemical index were calculated for a set of 36 1-alkoxy-5-alkyl-6-(arylthio)uracils. Resulting data were analyzed and suitable models were developed after identification of the active ranges. Subsequently, a biological activity was assigned to each of the compounds using these models and compared with the reported anti-HIV-1 activity. High accuracy of prediction was observed using these models. Statistical analysis revealed significance of the proposed models as well as a lack of correlation between the topochemical indices employed for the chosen data set.
The relationship between the superadjacency topochemical index and the anti-HIV activity of HEPT ... more The relationship between the superadjacency topochemical index and the anti-HIV activity of HEPT analogs has been investigated in the present study. The values of superadjacency topochemical index of all the analogs involved in the data set were calculated using an in-house computer program. Resulting data were analyzed and a suitable model was developed after identification of the active range. Subsequently, a computed biological activity was assigned to each of the compounds involved in the dataset, which was then compared with the reported anti-HIV activity. Accuracy of prediction was found to be 88% using the said model. The predictive ability of the model indicates that this model can be used for predicting the anti-HIV activity of the compounds prior to synthesis and may prove to be highly beneficial for providing lead structures for development of potent anti-HIV agents.
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