Volume 5, Issue 2
Pages no. 131-206
Available online on 01 March 2015
ISSN 2277-3681
J Pharm Sci Bioscientific Res. 2015; 5(2):131-206.
Copyright © 2014 JPSBR Publications
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ABSTRACT:
There are vast number of pharmacologically active heterocyclic compounds known, many of which are in regular chemical use. Among
these N and S containing heterocycles are of great importance. 5-Aminothiabendazole, known for its synthetic utility and broad spectrum
of pharmacological activity, is one among such heterocyclic compounds. Several of its derivatives showed pharmacological activity. These
are used as therapeutic agents and are thus interesting for the synthesis of biologically active compounds. The benzimidiazole framework
and many of its derivative exhibit variety of biological action. They are used as antibacterial, antiviral, anticancer and antifungal agents. 5-
Aminothiabedazole is a well known Anthelmintic agent which is non-toxic to humans. It has also application as a fungicide in agriculture.
Because of a structural similarity to chelating agents, such as 2, 2'-bipyridine and 1-10 phenanthroline, we were promoted to design and
synthesize metal complexes of it.
KEY WORDS: 5-Aminothiabendazole, Cobalt complexes of 5-Aminothiabendazole, Anthelmintic agent, heterocyclic compounds, Cobalt
complexes
There are vast number of pharmacologically active heterocyclic compounds known, many of which are in regular chemical use. Among
these N and S containing heterocycles are of great importance. 5-Aminothiabendazole, known for its synthetic utility and broad spectrum
of pharmacological activity, is one among such heterocyclic compounds. Several of its derivatives showed pharmacological activity. These
are used as therapeutic agents and are thus interesting for the synthesis of biologically active compounds. The benzimidiazole framework
and many of its derivative exhibit variety of biological action. They are used as antibacterial, antiviral, anticancer and antifungal agents. 5-
Aminothiabedazole is a well known Anthelmintic agent which is non-toxic to humans. It has also application as a fungicide in agriculture.
Because of a structural similarity to chelating agents, such as 2, 2'-bipyridine and 1-10 phenanthroline, we were promoted to design and
synthesize metal complexes of it.
KEY WORDS: 5-Aminothiabendazole, Cobalt complexes of 5-Aminothiabendazole, Anthelmintic agent, heterocyclic compounds, Cobalt
complexes
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ABSTRACT:
Multifunctional dendritic polymer (also known as dendrimer) mediated drug delivery system is aimed at providing effective drug delivery at the
target site. This system exhibits low toxicity, high solubility of drugs, high loading capacity and stability in biological environment. Cell specificity
is achieved by functionalizing the surface of dendritic polymer by targeting ligands. The multi-valent property of this drug delivery system
increases the binding strength of the polymer with the corresponding cell. The article reviews the advantages of Multifunctional Dendrimers in
Drug Delivery system, also briefs formulations of drugs using dendrimers.
KEYWORDS: Dendrimers, Dendritic polymers, Multifunctional polymers, Dendrimeric drug delivery, Branched polymers.
Multifunctional dendritic polymer (also known as dendrimer) mediated drug delivery system is aimed at providing effective drug delivery at the
target site. This system exhibits low toxicity, high solubility of drugs, high loading capacity and stability in biological environment. Cell specificity
is achieved by functionalizing the surface of dendritic polymer by targeting ligands. The multi-valent property of this drug delivery system
increases the binding strength of the polymer with the corresponding cell. The article reviews the advantages of Multifunctional Dendrimers in
Drug Delivery system, also briefs formulations of drugs using dendrimers.
KEYWORDS: Dendrimers, Dendritic polymers, Multifunctional polymers, Dendrimeric drug delivery, Branched polymers.
ABSTRACT:
The purpose of this research study was to develop and optimize an accurate and precise Gas Chromatography method for the determination
of Residual solvents (Methanol, Ethanol, Isopropyl alcohol, Acetonitrile, Dichloromethane, Ethyl acetate, Tetrahydrofuran, Benzene, Toluene) in
Danazol using the BP-624, 30 m x 0.53mm ID, 3.0 ?mcolumn as stationary phase. The injection volume of samples taken is 1.2 ml with
splitless injection. The temperature maintained at the injector and detector was to be 200ºC and 220ºC respectively. Nitrogen gas with flow 2.0
ml/minute used as mobile phase and the detection was by FID. The flow of hydrogen and Air was maintained at 30ml/min and 300ml/min
respectively. The diluent used is Dimethyl Sulfoxide and water. All solvents were well resolved each other with diluents peak. Total run time is
24.3 min. The RTs observed for the Residual solvents Methanol, Ethanol, Isopropyl Alcohol, Acetonitrile, Dichl- -oromethane, Ethyl acetate,
Tetrahydrofuran, Benzene and Toluene are 6.12, 9.40, 7.84, 9.68, 10.34, 15.78, 16.41, 17.43 & 19.80 respectively. The method was validated
as meets all the regulations of System suitability, Specificity, Method Precision, Linearity, LOD & LOQ, Precision of LOQ and
Accuracy/Recovery under ICH specifications.
KEY WORDS: Gas Chromatography, Residual solvents, Danazol, BP-624 stationary phase.
The purpose of this research study was to develop and optimize an accurate and precise Gas Chromatography method for the determination
of Residual solvents (Methanol, Ethanol, Isopropyl alcohol, Acetonitrile, Dichloromethane, Ethyl acetate, Tetrahydrofuran, Benzene, Toluene) in
Danazol using the BP-624, 30 m x 0.53mm ID, 3.0 ?mcolumn as stationary phase. The injection volume of samples taken is 1.2 ml with
splitless injection. The temperature maintained at the injector and detector was to be 200ºC and 220ºC respectively. Nitrogen gas with flow 2.0
ml/minute used as mobile phase and the detection was by FID. The flow of hydrogen and Air was maintained at 30ml/min and 300ml/min
respectively. The diluent used is Dimethyl Sulfoxide and water. All solvents were well resolved each other with diluents peak. Total run time is
24.3 min. The RTs observed for the Residual solvents Methanol, Ethanol, Isopropyl Alcohol, Acetonitrile, Dichl- -oromethane, Ethyl acetate,
Tetrahydrofuran, Benzene and Toluene are 6.12, 9.40, 7.84, 9.68, 10.34, 15.78, 16.41, 17.43 & 19.80 respectively. The method was validated
as meets all the regulations of System suitability, Specificity, Method Precision, Linearity, LOD & LOQ, Precision of LOQ and
Accuracy/Recovery under ICH specifications.
KEY WORDS: Gas Chromatography, Residual solvents, Danazol, BP-624 stationary phase.
ABSTRACT:
The present research describes a validated and novel RP-HPLC method for the quantitative analysis of (3-fluoro-4-morpholin-4-yl-phenyl)-
carbamic acid methyl ester and its two related substances in KSM (Key Starting material). The chromatographic separation was achieved on a
C18 stationary phase with a gradient mobile phase prepared from methanol and phosphate buffer. The quantification was carried out by UV
detection at 250 nm. The developed RP-LC method was validated according to ICH guidelines. The percent recovery for individual substances
at 25, 50, 100 and 150% of specification concentrations were found to be between 95 to 105% Indicating the accuracy of the method. The
%RSD for system precision was found to be less than 2.0. The %R.S.D for repeatability and intermediate precision for the process-related
impurities in (3-fluoro-4-morpholin-4-yl-phenyl)-carbamic acid methyl ester were found to be less than 1.0. The correlation coefficient of (3-
fluoro-4-morpholin-4-yl-phenyl)-carbamic acid methyl ester and its two related substances was found to be greater than 0.99. The developed
LC method can be used for the quantitative determination of (3-fluoro-4-morpholin-4-yl-phenyl)-carbamic acid methyl ester and its two related
substances in KSM.
KEY WORDS: (3-fluoro-4-morpholin-4-yl-phenyl)-carbamic acid methyl ester, ICH guidelines, Validation, RP-HPLC, KSM
The present research describes a validated and novel RP-HPLC method for the quantitative analysis of (3-fluoro-4-morpholin-4-yl-phenyl)-
carbamic acid methyl ester and its two related substances in KSM (Key Starting material). The chromatographic separation was achieved on a
C18 stationary phase with a gradient mobile phase prepared from methanol and phosphate buffer. The quantification was carried out by UV
detection at 250 nm. The developed RP-LC method was validated according to ICH guidelines. The percent recovery for individual substances
at 25, 50, 100 and 150% of specification concentrations were found to be between 95 to 105% Indicating the accuracy of the method. The
%RSD for system precision was found to be less than 2.0. The %R.S.D for repeatability and intermediate precision for the process-related
impurities in (3-fluoro-4-morpholin-4-yl-phenyl)-carbamic acid methyl ester were found to be less than 1.0. The correlation coefficient of (3-
fluoro-4-morpholin-4-yl-phenyl)-carbamic acid methyl ester and its two related substances was found to be greater than 0.99. The developed
LC method can be used for the quantitative determination of (3-fluoro-4-morpholin-4-yl-phenyl)-carbamic acid methyl ester and its two related
substances in KSM.
KEY WORDS: (3-fluoro-4-morpholin-4-yl-phenyl)-carbamic acid methyl ester, ICH guidelines, Validation, RP-HPLC, KSM
ABSTRACT:
The population growth of past several years in India was due to difference in the number of birth rate and number of death rate. To control the
birth rate, fertility control is required. There are many methods for fertility regulation available but the oral contraception method is most popular
method for contraception. The traditional medicines are being popular in the current time because of having fewer side effects as compare to
synthetic allopathic drugs. There are many herbal drugs having fertility regulating activity but they are not as effective as compare to Synthetic
allopathic drugs. As per market survey, doctors opinion that ayurvedic abortion drugs are not effective in the process of abortion. While in current
market ayurvedic abortion drugs are more used than the allopathic abortion drugs by patients. Hence scientifically designed research on
ayurvedic abortifacients for its effectiveness in the abortion process to compare with standard allopathic drug like Mifepristone is highly required
to save the public health. In this study it is confirmed that there is a no abortifacient activity seen in Polyherbal formulations in comparison of
standard Mifepristone drug sold in today's market.
KEY WORDS: abortion, abortifacient, Mifepristone, Poly-herbal formulation, Contraceptive
The population growth of past several years in India was due to difference in the number of birth rate and number of death rate. To control the
birth rate, fertility control is required. There are many methods for fertility regulation available but the oral contraception method is most popular
method for contraception. The traditional medicines are being popular in the current time because of having fewer side effects as compare to
synthetic allopathic drugs. There are many herbal drugs having fertility regulating activity but they are not as effective as compare to Synthetic
allopathic drugs. As per market survey, doctors opinion that ayurvedic abortion drugs are not effective in the process of abortion. While in current
market ayurvedic abortion drugs are more used than the allopathic abortion drugs by patients. Hence scientifically designed research on
ayurvedic abortifacients for its effectiveness in the abortion process to compare with standard allopathic drug like Mifepristone is highly required
to save the public health. In this study it is confirmed that there is a no abortifacient activity seen in Polyherbal formulations in comparison of
standard Mifepristone drug sold in today's market.
KEY WORDS: abortion, abortifacient, Mifepristone, Poly-herbal formulation, Contraceptive
ABSTRACT:
Acne is a cutaneous pleomorphic disorder of the pilosebaceous unit involving abnormalities in sebum production and is characterized by both
inflammatory (papules, pustules and nodules) and no inflammatory (comedones, open and closed) lesions. Propionibacterium acnes and
Staphylococcus epidermidis are common pus-forming microbes responsible for the development of various forms of, acne vulgaris. Common
therapies that are used for the treatment of acne include topical, systemic, hormonal, herbal and combination therapy. It is the sequelae of the
disease that are the distinguishing characteristics of acne in skin of color, namely postinflammatory hyperpigmentation and keloidal or
hypertrophic scarring. Although the medical and surgical treatment options are the same, it is these features that should be kept in mind when
designing a treatment regimen for acne.This review focuses on the treatment of acne using various drug delivery systems. Many herbal drugs
are used for the treatment of acne vulgaris. Though they have very few number of clinical trials, many successful results have been recorded.
There are many types of herbal drugs which act against acne vulgaris and some of those are:- Aloe Vera , Amaranth, Arnica, Asparagus,
Barberry, Basil, Birch, Bittersweet nightshade, Brewer's yeast, Burdock, Calendula, Celandine, Chaste tree, Chaste berry, Coriander, Cur
cumin, Green Tea, Guggul, Jojoba oil, Kali bromatum, Labrador tea, Lavender, Liquorice, Mint, Neem, Orange peel, Pine, Poplan, Rhubarb,
Rose, Saw palmuto, Soapwart,Stinging nettle, Tea tree oil, Thyme, Turmeric, Usnea Barbara, Viola, Walnut, Willow bark.
KEY WORDS: Herbal Drugs, Acne Vulgeris, Propionibacterium acnes, Staphylococcus epidermidis, Staphylococcus aureus, stages of acne,
causes of acne.
Acne is a cutaneous pleomorphic disorder of the pilosebaceous unit involving abnormalities in sebum production and is characterized by both
inflammatory (papules, pustules and nodules) and no inflammatory (comedones, open and closed) lesions. Propionibacterium acnes and
Staphylococcus epidermidis are common pus-forming microbes responsible for the development of various forms of, acne vulgaris. Common
therapies that are used for the treatment of acne include topical, systemic, hormonal, herbal and combination therapy. It is the sequelae of the
disease that are the distinguishing characteristics of acne in skin of color, namely postinflammatory hyperpigmentation and keloidal or
hypertrophic scarring. Although the medical and surgical treatment options are the same, it is these features that should be kept in mind when
designing a treatment regimen for acne.This review focuses on the treatment of acne using various drug delivery systems. Many herbal drugs
are used for the treatment of acne vulgaris. Though they have very few number of clinical trials, many successful results have been recorded.
There are many types of herbal drugs which act against acne vulgaris and some of those are:- Aloe Vera , Amaranth, Arnica, Asparagus,
Barberry, Basil, Birch, Bittersweet nightshade, Brewer's yeast, Burdock, Calendula, Celandine, Chaste tree, Chaste berry, Coriander, Cur
cumin, Green Tea, Guggul, Jojoba oil, Kali bromatum, Labrador tea, Lavender, Liquorice, Mint, Neem, Orange peel, Pine, Poplan, Rhubarb,
Rose, Saw palmuto, Soapwart,Stinging nettle, Tea tree oil, Thyme, Turmeric, Usnea Barbara, Viola, Walnut, Willow bark.
KEY WORDS: Herbal Drugs, Acne Vulgeris, Propionibacterium acnes, Staphylococcus epidermidis, Staphylococcus aureus, stages of acne,
causes of acne.
ABSTRACT:
The oral delivery of drugs with a narrow absorption window in the gastrointestinal tract (GIT) is often limited by poor bioavailability with
conventional dosage forms due to incomplete drug release and short residence time at the site of absorption. In-situ gel provides the best way to
overcome problems of immediate release and short gastrointestinal residence of liquids. The in situ gel dosage form is a liquid before
administration and after it comes in contact with gastric contents due to one or more mechanisms gets converted to gel which floats on gastric
contents. This achieves increased residence as well as sustained release. This approach is useful for systemic as well as local effect of drugs
administered. In the presence of gastric acid, alginates precipitate, forming a gel.Alginate-based raft-forming formulations usually contain sodium
or potassium bicarbonate; in thepresence of gastric acid, the bicarbonate is converted to carbon dioxide which becomes entrapped within the gel
precipitate, converting it into a foam which floats on the surface of the gastric contents, much like a raft on water. Alginate-based rafts can entrap
carbon dioxide, as well as antacid components contained in some formulations, thus providing a relatively pH-neutral barrier, they also act as
physical barrier to reduce the episode of reflux disorders. This review gives the information about alginate raft gel alone and/ or along with
different type of antacids( H2 receptors & proton pump inhibitors) can be efficiently used to treat peptic ulcers as well as reflux disorders.
KEY WORDS: oral, in-situ, alginate forming raft, pH-neutral barrier, reflux disorders
The oral delivery of drugs with a narrow absorption window in the gastrointestinal tract (GIT) is often limited by poor bioavailability with
conventional dosage forms due to incomplete drug release and short residence time at the site of absorption. In-situ gel provides the best way to
overcome problems of immediate release and short gastrointestinal residence of liquids. The in situ gel dosage form is a liquid before
administration and after it comes in contact with gastric contents due to one or more mechanisms gets converted to gel which floats on gastric
contents. This achieves increased residence as well as sustained release. This approach is useful for systemic as well as local effect of drugs
administered. In the presence of gastric acid, alginates precipitate, forming a gel.Alginate-based raft-forming formulations usually contain sodium
or potassium bicarbonate; in thepresence of gastric acid, the bicarbonate is converted to carbon dioxide which becomes entrapped within the gel
precipitate, converting it into a foam which floats on the surface of the gastric contents, much like a raft on water. Alginate-based rafts can entrap
carbon dioxide, as well as antacid components contained in some formulations, thus providing a relatively pH-neutral barrier, they also act as
physical barrier to reduce the episode of reflux disorders. This review gives the information about alginate raft gel alone and/ or along with
different type of antacids( H2 receptors & proton pump inhibitors) can be efficiently used to treat peptic ulcers as well as reflux disorders.
KEY WORDS: oral, in-situ, alginate forming raft, pH-neutral barrier, reflux disorders
ABSTRACT:
A newer, simple, rapid, accurate, precise and sensitive Absorbance ratio and Area under curve methods are developed for the simultaneous
estimation of Cetirizine Hydrochloride (CTZ HCl) and Phenylephrine Hydrochloride (PHE HCl) in combined dosage form. The methods employed
were I) absorbance ratio and II) area under curve (AUC) method. Beer's law was obeyed in concentration range of 5-25 µg/ml for both drugs and
for both proposed methods. The first developed method makes use absorbance ratio method using wavelength at 219 nm (isoabsorptive point)
and 230 nm (?max of CTZ HCl). The second method is area under curve method in which Sampling wavelengths range selected are 225-235 nm
and 268-278 nm with linearity for CTZ HCl and PHE HCl respectively. The results of the analysis were analyzed and validated statistically and
recovery studies were carried out as per ICH guidelines. It can be used for routine analysis of both drugs in bulk as well as in pharmaceutical
formulations.
KEY WORDS: Cetirizine Hydrochloride (CTZ HCl), Phenylephrine Hydrochloride (PHE HCl), Absorbance ratio method (Q-ratio), Area under curve
method (AUC)
A newer, simple, rapid, accurate, precise and sensitive Absorbance ratio and Area under curve methods are developed for the simultaneous
estimation of Cetirizine Hydrochloride (CTZ HCl) and Phenylephrine Hydrochloride (PHE HCl) in combined dosage form. The methods employed
were I) absorbance ratio and II) area under curve (AUC) method. Beer's law was obeyed in concentration range of 5-25 µg/ml for both drugs and
for both proposed methods. The first developed method makes use absorbance ratio method using wavelength at 219 nm (isoabsorptive point)
and 230 nm (?max of CTZ HCl). The second method is area under curve method in which Sampling wavelengths range selected are 225-235 nm
and 268-278 nm with linearity for CTZ HCl and PHE HCl respectively. The results of the analysis were analyzed and validated statistically and
recovery studies were carried out as per ICH guidelines. It can be used for routine analysis of both drugs in bulk as well as in pharmaceutical
formulations.
KEY WORDS: Cetirizine Hydrochloride (CTZ HCl), Phenylephrine Hydrochloride (PHE HCl), Absorbance ratio method (Q-ratio), Area under curve
method (AUC)
ABSTRACT:
Oral route has always been the favorite route of drug administration in many diseases and till today it is the first way investigated in the
development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor
aqueous solubility, thereby pretense problems in their formulation. More than 40% of potential drug products suffer from poor water solubility. For
the therapeutic delivery of lipophilic active moieties (BCS class II and IV drugs), lipid based formulations are inviting increasing attention.
Currently a number of technologies are available to deal with the poor solubility, dissolution rate and bioavailability of insoluble drugs such as
micronization, solid dispersions or cyclodextrin complex formation and different technologies of drug delivery systems. One of the promising
techniques is Self?Micro Emulsifying Drug Delivery Systems (SMEDDS). Self emulsifying drug delivery system has gained more attention due to
enhanced oral bio-availability, enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug toward
specific absorption window in GIT, and protection of drug from the unreceptive environment in gut. This article gives a complete overview of
SMEDDS as a promising approach to effectively deal with the problem of poorly soluble molecules.
KEY WORDS: SMEDDS, surfactant, oil, co-surfactant, bioavailability
Oral route has always been the favorite route of drug administration in many diseases and till today it is the first way investigated in the
development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor
aqueous solubility, thereby pretense problems in their formulation. More than 40% of potential drug products suffer from poor water solubility. For
the therapeutic delivery of lipophilic active moieties (BCS class II and IV drugs), lipid based formulations are inviting increasing attention.
Currently a number of technologies are available to deal with the poor solubility, dissolution rate and bioavailability of insoluble drugs such as
micronization, solid dispersions or cyclodextrin complex formation and different technologies of drug delivery systems. One of the promising
techniques is Self?Micro Emulsifying Drug Delivery Systems (SMEDDS). Self emulsifying drug delivery system has gained more attention due to
enhanced oral bio-availability, enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug toward
specific absorption window in GIT, and protection of drug from the unreceptive environment in gut. This article gives a complete overview of
SMEDDS as a promising approach to effectively deal with the problem of poorly soluble molecules.
KEY WORDS: SMEDDS, surfactant, oil, co-surfactant, bioavailability
ABSTRACT:
Sickle cell anemia is a hemoglobin disorder which is affecting relatively under privileged population like a tribal population who is belonging to
economically poor background so might be lack of education and awareness about current health facility provided by the government and other
helping organizations. While on the other hand the medical and para medical people too found difficulty in understanding about the sickle cell
anemia and handling patients of it. No doubt so much work already done on understanding the pathophysiology of the disease and newer
treatment for this lifelong disease. The current review is an initiative attempt to highlight the basic what kind of changes pathophysiologically
occurs in sickle cell anemia and what kind of effect can be occur on various body organ systems are studied. This review can be helpful to the all
health care provider and it might be helpful even to the general population to be aware about the disease and its complication.
KEY WORDS: Sickle cell anemia, hemoglobin disorder, Adhesion, Reperfusion, Vasoocclusion.
Sickle cell anemia is a hemoglobin disorder which is affecting relatively under privileged population like a tribal population who is belonging to
economically poor background so might be lack of education and awareness about current health facility provided by the government and other
helping organizations. While on the other hand the medical and para medical people too found difficulty in understanding about the sickle cell
anemia and handling patients of it. No doubt so much work already done on understanding the pathophysiology of the disease and newer
treatment for this lifelong disease. The current review is an initiative attempt to highlight the basic what kind of changes pathophysiologically
occurs in sickle cell anemia and what kind of effect can be occur on various body organ systems are studied. This review can be helpful to the all
health care provider and it might be helpful even to the general population to be aware about the disease and its complication.
KEY WORDS: Sickle cell anemia, hemoglobin disorder, Adhesion, Reperfusion, Vasoocclusion.
