IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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JULY 2019
1

A REVIEW ON QUALITY BY DESIGN APPROACHES TO ANALYTICAL METHOD DEVELOPMENT

Rajendra Phadke1*, Dr. Amit Gosar2, Rupali Mali2, Deepesh Patil2
1J.J.T University, Churu, Jhunjhunu Road, Rajasthan -333001.
2Indoco Remedies Limited, Analytical Research & Development Department, Navi Mumbai, 400701, Maharashtra, India.

Quality by Design (QbD) refers to a holistic approach towards the drug development. In pharmaceutical industries drug development is important and critical to achieve the best quality. New drug development we should follow Quality by Design approach. Most of regulatory agency and or FDA are reviewing the drug development data. To answer such agencies and FDA we have to go towards a more scientific, risk based, holistic and proactive approach. Industrial concepts are to understand the product and manufacturing process, starting with product development, basically building quality in, not testing it. Under this concept of QbD during designing and development of a product, Now-a-days the concept of QbD can be extended to analytical techniques. Under this concept of QbD throughout designing and development of a product, it is essential to define desire product performance profile, Target product Profile (TPP), Target Product Quality Profile (TPQP)] and identify critical quality attributed (CQA). This paper gives idea about the Pharmaceutical QbD and describes use of Quality by Design to ensure quality of Pharmaceuticals. Recently the concept has been also appreciated by different regulatory, especially by EMA (Europe Medicines Agency) and other ICH countries authorities over the globe. They are very popularly accepted as AQbD (Analytical Quality by Design) concepts by the industry. 


 


2

MICROSPONGES – A COMPREHENSIVE REVIEW: SUCCESS AND CHALLENGES

G. Ravi, Valluru Ravi*, P. Subhash Chandra Bose, Damineni Saritha
Department of Pharmaceutics, MNR College of Pharmacy, Sangareddy-502294, TS, India.
Department of Pharmaceutics, Sultan-Ul-Uloom College of Pharmacy, Hyderabad, TS, India.

Microsponges are polymeric delivery systems composed of porous microspheres. They are tiny sponge-like spherical particles with a large porous surface. Moreover, they may enhance stability, reduce side effects and modify drug release favorably. Microsponge is current novel technique for control release and target specific drug delivery system. Microsponge technology has been introduced in topical drug products to facilitate the controlled active drug release into the skin in order to decrease the systemic exposure and minimize local cutaneous reactions to active drugs. This review focus on a microsponge’s delivery system discussing the preparation methods, evaluation methods, mechanism of drug release and Physical characterization of microsponges. Microsponge delivery system technology is being used at present in skin care, sunscreens, cosmetics, over-the-counter (OTC) and prescription products. One of the most excellent features of the microsponge is it is self-sterilizing. 



3

FORMULATION AND EVALUATION OF RANITIDINE SEMISOLID MATRIX CAPSULE BY LIQUID FILLING TECHNOLOGY

Kadam Sagar*1, Dr. Kshirsagar Sandip2, Shinde Vaishali2
1Hon.Shri. Babanrao Pachpute Vichardhara Trust’s, Group of Institutions, College of Pharmacy, Kashti, Ahmednagar, Maharashtra, India
2Kasturi Shikshan Sanstha, College of Pharmacy, Shikrapur, Pune, Maharashtra, India.

The aim of the present study was formulation and development of Ranitidine capsules by liquid filling technology in order to improve its dissolution properties and thereby its bioavailability. Ranitidine falls under histamine H2-receptor antagonist, a drug used to block the action of histamine on parietal cells in the stomach, decreasing acid production by these cells. Antagonists at Histamine H2-receptor are used in the treatment of dyspepsia; however their use has waned since the advent of the more effective proton pump inhibitors. Similar to the H1-antihistamines, the H2 antagonists are inverse agonists rather than true receptor antagonists. Excipients like polyethylene glycol 400 (PEG 400), propylene glycol (PG), polyvinylpyrrolidone (PVP K-30), antioxidants, ethanol, and purified water were used for formulation. These prepared formulations were evaluated for appearance, pH, viscosity, drug content percentage, stability, and in vitro dissolution studies. The compatibility between the drug and excipients in formulations was confirmed by FTIR spectra. The drug contents were in the range of 99.62-99.63 and the viscosity was in the range of 60.9–591.7 cps with all the formulations developed. 


 


4

“SYNTHESIS, SPECTRAL AND MICROBIAL STUDIES OF QUINAZOLIN-4-ONE BASED SOME NEW CHALCONES DERIVATIVES.”

Komal Savaliya and Pankaj S. Patel
Department of Chemistry, Sheth L.H. Science College, MANSA-382845, Gujarat, India.

Chalcones and their analogs have been an area of great interest in recent years. Therefore it is very important to develop the latest strategies in the synthesis of chalcone. Therefore in present research study, a series of 6, 8-dibromo-3-{4-[3-(substitutedphenyl)prop-2-enoyl]phenyl}-2-phenylquinazolin-4-one have been synthesized by the condensation of 3-(4-acetylphenyl)-6,8-dibromo-2-phenylquinazolin-4-one with various aldehydes in presence of ethanol. The intermediate 3-(4-acetylphenyl)-6,8-dibromo-2-phenylquinazolin-4-one synthesized by fusion of 6,8-dibromo-2-phenyl-3,1-benzoxazin-4-one with 1-(4-aminophenyl) ethanone. These newly synthesized compounds are screened for antibacterial and antifungal activity by Agar Cup method .The structure of the synthesized compounds are characterized by the IR ,1H-NMR and elemental analysis. 


 


5

DESIGN, DEVELOPMENT AND EVALUATION OF BUCCAL MUCOADHESIVE PATCH OF DEXAMETHASONE SODIUM PHOSPHATE FOR THE MANAGEMENT OF ORAL SUBMUCOUS FIBROSIS, ULCERATION AND LICHEN PLANUS

Satish Polshettiwar2, Saroj Valvi1, Akshay Baheti2, B. S. Kuchekar2
1MAEERS, Maharashtra Institute of Pharmacy, MIT Campus, Kothrud, Pune-411038, Maharashtra, India.
2Dr Vishwanath Karad MITWPU, School of Pharmacy, Pune-411038.

The objective of the present study was to develop mucoadhesive buccal patch of Dexamethasone for the treatment of oral submucous fibrosis. In formulation, chitosan is used as a polymer and PEG 400 as a plasticizer. Backing membrane was prepared by using ethyl cellulose and isopropyl alcohol. The solvent casting method was used for the preparation of mucoadhesive buccal patch as it is cost effective and efficient method. Preformulation studies of Dexamethasone were carried out. FTIR studies implied that there were no interactions between drug and polymers. The prepared batches were evaluated for visual appearance, thickness, folding endurance, weight variation, swelling index, surface pH, mucoadhesive time, % drug content, in-vitro diffusion and ex-vivo permeation study. Total nine batches of Dexamethasone mucoadhesive buccal patch were prepared successfully using chitosan as a polymer and PEG 400 as a plasticizer by solvent casting method. Based on results batch F2 was selected as optimized formulation. From invitro release of batches, F2 was found best, showing release of drug 64.53% in 4 hours. A clinical examination of the oral cavity was carried out under artificial light which includes extra oral examination and intra oral examination. The results of the present study of mucoadhesive semi-solid drug design for the treatment of OSMF will be useful for drug industry for the benefit of patients suffering from OSMF. The most important advantage of the Mucoadhesive buccal films is that it contains a lower drug dose, adequate for therapeutic effect as it is placed directly on the site of the inflammation, when compared to conventional administration. Moreover, this Mucoadhesive buccal patch is very convenient because it is non-irritant and self-administration is possible. Given promising therapeutic effects, the buccal film developed here could become a local drug delivery device for management of oral submucous fibrosis, ulceration and lichen planus. 


 


6

A VALIDATED CHIRAL HPLC METHOD FOR THE ENANTIOMERIC PURITY OF ANAGLIPTIN

K. Durga Malleswar1, B. Venugopala Rao*1, S.Shylaja2.
1Stereokem Private Limited. Plot No-36/A, IDA, Uppal, Hyderabad, Telangana, India.
2Chaitanya Bharathi Institute of Technology ,Gandipet, Hyderabad, Telangana, India.

An isocratic chiral phase high-performance liquid chromatographic method has been developed and validated to quantitation the (R)-isomer in Anagliptin. Separation was achieved in a Lux Cellulose-3 (250×4.6mm, 5?m) column. The ratio of hexane, ethanol and diethyl amine in the mobile phase were optimized to obtain the best separation. UV detection was performed at 254 nm. The described method is linear over a range of LOQ – 1.4 ?g/mL of (R)-isomer. The mean recovery of (R)-isomer was found to be in the range of 100–102%. The method is simple, accurate, selective and precise. The method can be used in the quality control of bulk manufacturing. 


 


7

ANTIMICROBIAL POTENTIAL OF A NOVEL SIDDHA METALLO-MINERAL FORMULATION “KAALAMEGA NARAYANA CHENDHOORAM” AS MENTIONED IN “ATHMARAKSHA MIRTHAM ENNUM VAITHIYA SAARA SANGERAHAM” AGAINST A GRAM NEGATIVE ORGANISM E.Coli IN IN-VITRO STUDIES.

Dr. R. Abinaya, Dr. R. Vijaya Nirmala, Dr. R. Karolin Daisy Rani, Dr. M. D. Saravana Devi.
Government Siddha Medical College, Arumbakkam,Chennai, Tamil Nadu, India.

AIM AND OBJECTIVE: The aim of this present study is to validate the Anti microbial potentials of a novel siddha metallo-mineral formulation Kaalamega Narayana Chendhooram as mentioned in Athmaraksha Mirtham Ennum Vaithiya Saara Sangeraham against a Gram negative organism Escherichia coli in in-vitro Studies. METHODS: Siddha system of medicine was a fruitful gift offered by the siddhars. It contains plants, metals, minerals and animal products in their medicinal preparations. It involved in treating various acute and chronic diseases. Siddha system of medicine had a history of antimicrobial medicine before the prehistoric era of antibiotics. Due to the lack of proper validations of medicine, it was not accepted by the scientific world. Thus an attempt was made in this paper to screen the efficacy of anti microbial potentials of Kaalamega Narayana Chendhooram as mentioned in Athmaraksha Mirtham Ennum Vaithiya Saara Sangeraham, a novel siddha metallo-mineral formulation against a Gram negative organism Escherichia coli in In-vitro Studies of Muller Hinton Agar Medium with streptomycin as a standard drug and test drug with the different concentration of the drug as 250?g/ml, 500?g/ml, 1000 ?g/ml were added and zone of inhibitions were measured in mm. RESULTS: At the end of this research study, that the trail drug of a novel siddha metallo-mineral formulation Kaalamega Narayana Chendhooram as mentioned in Athmaraksha Mirtham Ennum Vaithiya Saara Sangeraham through Muller Hinton Agar Medium with streptomycin as standard drug. The gram negative organism showed the zone of inhibition in following concentration of Escherichia coli 250?g/ml, 500?g/ml, 1000 ?g/ml as 15mm,16mm, 19mm .On increasing the concentration of the drug there is a gradual increase in the zone of inhibition of micro organisms. CONCLUSION: The present in-vitro study of a potent siddha metallo-mineral formulation Kaalamega Narayana Chendhooram as mentioned in Athmaraksha Mirtham Ennum Vaithiya Saara Sangeraham through a Muller Hinton Agar Medium with streptomycin as a standard drug was found to be a potent anti-microbial medicine. 


 


8

FUTURE ASPECT OF NANOMEDICINE

Dhanashree B. Midgule, Sutaja L. Ingale, Sayali C. Dudhal, Geetanjali S. Mehetre
Department of Pharmaceutical Chemistry ,KasturiShikshanSanstha College of Pharmacy, Shikrapur, Pune-412208.
Department of Pharmaceutics, Kasturi Shikshan Sanstha College of Pharmacy, Shikrapur, Pune-412208.

Nanotechnology is science which focused on the design, synthesis, characterization and application of materials on the nanoscale. The nanotechnologies nowadays are present in many areas of our life, and they will have much impact on the fields of medicine and health care. The world of medicine is very complex, so all of the benefits from nanoscience and nanotechnology to medicine will take time to become evident; however, other benefits will come immediately. Nanomedicine is the improvement and preservation of human health using molecular tools and molecular knowledge of the human body. Nanomedicines future applications will be based on the ability to repair specific diseased cells, functioning in a similar way to antibodies in our natural healing processes. Human health has always been determined on the nanometer scale; this is where the structure and properties of the machines of life work in every one of thecells in every living thing. 


 


9

MOLECULAR DOCKING STUDIES OF SOME NOVEL N’-ARYLSUBSTITUTED PYRROLE ANALOGS

Shrinivas D. Joshi* S. R. Prem Kumar, and Venkatrao H. Kulkarni
Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical Chemistry, S. E. T’s College of Pharmacy, Sangolli Rayanna Nagar, Dharwad 580 002, Karnataka, India.

In present work, Surflex docking has been carried out on a series (23 compounds bearing N’-arylsubstituted pyrrole heterocyclic molecules) of M. tuberculosis inhibitors. SYBYL-X 2.0 package (Tripos Inc., St. Louis, USA) was used for the study. Surflex-docking shown that the peptide connection between the aryl substitution and pyrroly moiety was significant to exhibit receptor and molecular interactions, and it was also found that the pattern of binding of established compounds is same as that of the ligand 1-cyclohexyl-N-(3,5-dichlorophenyl)-5-oxopyrrolidine-3-carboxamide, which gives an idea in understanding the specific activity of compounds towards the receptor. 


 


10

CO-CRYSTALLIZATION: A NOVEL APPROACH TO ENHANCE THE DISSOLUTION OF POORLY SOLUBLE DRUGS

S. J. Shankar1*, Jaswanth Gowda B. H.1, Akshatha R. S.2, Basavaraj Metikurki1
1Vivekananda College of Pharmacy, Dr. Rajkumar Road, Rajajinagar 2nd Stage, Bengaluru – 560 055.
2PES College of Pharmacy, 50 feet Road, Hanumanth nagar, Srinagara, Bengaluru – 560 050.

Approximately 40% of newly synthesized drugs are not able to enter market due to biopharmaceutical issues like poor solubility and poor permeability. Most number of drugs marketed is administered orally hence solubility enhancement plays a major role. There are different techniques to upgrade the dissolvability of inefficiently soluble drugs including pro-drug approach, salt formation, particle size reduction, complexation and solid dispersion. Out of all other techniques, salt formation is one of majorly used technique to improve physicochemical characteristics of drugs which includes formation of ionic bond. But nowadays development of co-crystals has evolved as a suitable technique towards improving the dissolvability and bioavailability of ineffectively soluble drugs that includes non-ionic bond formation. In this paper a brief and accurate precis of pharmaceutical co-crystals is stated with specific spotlight on co-crystal preparation methodologies, mechanism of co-crystal formation, characterization methods and some of the examples of pharmaceutical co-crystals are additionally outlined. The difference between salts and co-crystals, regulatory facet and also the future prospective of co-crystallization is being discussed. 


 


11

FORMULATION AND EVALUATION OF HYDROXYAPATITE MICROSPHERES OF AN ANTIMICROBIAL DRUG FOR THE TREATMENT OF OSTEOMYELITIS

S. J. Shankar*, Jaswanth Gowda B. H., Nimitha A.G., Basavaraj Metikurki
Vivekananda College of Pharmacy, Dr. Rajkumar Road, Rajajinagar 2nd Stage, Bengaluru – 560 055.

This study was intended to formulate, characterize, evaluate in-vitro formulation release and dissolution studies of hydroxyapatite included microspheres of an antimicrobial drug for the disease osteomyelitis. Levofloxacin stacked hydroxyapatite microspheres were set up by inotropic gelation strategy by varing the measure of polymer and carrier. The microspheres of levofloxacin which was formulated were exposed to different physico-chemical parameters like size distribution, solubility studies, FT-IR, drug content, in-vitro dissolution studies, DSC and crystal morphology by SEM. FT-IR results has identified no traces of chemical interaction between the polymer and drug. SEM studies determined that the microspheres were framed in spherical and round shape. DSC curve demonstrated that the melting point of the polymer isn't influencing the melting point of the drug and affirmed that no chemical change among drug and polymer. Anti-microbial activity of formulated microspheres shown a substantial zone of inhibition and inhibition of bacterial growth observed. The in-vitro levofloxacin release from optimized microspheres was initially slow and sustained over the period of time and the cumulative release was 97% in SF-2 and 91% in CF-3 formulation. The drug release pattern was co-related well with Korsmeyer-Peppas model and was followed by case II non fickian release mechanism. 


 


12

FORMULATION AND EVALUATION OF COLON TARGETED MATRIX TABLET OF AZATHIOPRINE

Kadam Sagar*, Abnave Dattatray, Landge Dhananjay
Hon. Shri. Babanrao Pachpute Vichardhara Trust’s, Group of Institutions, College of Pharmacy, Kashti, Ahmednagar, Maharashtra, India.

 The aim of the current work was to formulate as well as evaluate colon targeted matrix tablet using Azathioprine. Excipients include Eudragit S100, Microcrystalline cellulose, Lactose, Talc, Magnesium stearate. Quantities of the excipients were chosen by carrying out FT-IR method. Preformulation studies were performed so as to study the nature as well as compatibility of Active Pharmaceutical Ingredient with that of the excipients by physical observations along with FT-IR studies. The tablets were processed by direct compression method making use of the selected excipient quantities. Pre-compression parameters like tapped density, bulk density, Hauser’s ratio, compressibility index, and compressibility index. The formulated Azathioprine matrix tablets were coated using pan coating method with enteric polymer Eudragit S 100. The final tablets were evaluated for weight variation, thickness, hardness, and drug content, friability and disintegration time and in-vitro dissolution studies. Cumulative percentage drug release found to be 64.24 % (lowest) for F1 to 97.66 (highest) for F9 up to 8 hr. as the sustained release is main aim, formulation F1 was selected a optimized formulation. Formulation F1 containing enteric coated matrix tablet of Azathioprine would be a promising formulation that will aid in achieving the purpose of treating inflammatory bowel diseases (ulcerative colitis) without any gastric irritation or ulcers, which is useful for patients having prehistory of ulcerative colitis.