NOVEL TECHNOLOGY USED IN THE PREFORMULATION STUDY: A REVIEW
Abstract
Preformulation is a study which deals which provides the framework for drug’s combination with pharmaceutical ingredients in the fabrication of dosage form. Preformulation study is to develop the elegant dosage form by the establishing kinetic rate profile, compatibility with the other ingredients, establish physicochemical parameter and polymorphism of the new drug. Among these properties the preformulation also provide the information regarding degradation process, adverse condition relevant to the drug, bioavailability, pharmacokinetics, toxicity, drug stability, partition coefficient, dissolution rate, and polymorphic forms. Preformulation studies strengthen the scientific foundation of the guidance, provide regulatory relief and conserve resources in the drug development and evaluation process, improve public safety standards, enhance product quality, facilitate the implementation of new technologies. According to ICH, all technical requirements for the application of drug approval were homonized in CTD format which are scientifically more elaborate by USFDA in QoS-QbR format. QbR is based on the principle of Quality by Design (QbD) which increased efficiently in the FDA review process.
Keywords:
Preformulation, Physiochemical properties, Polymorphism, Quality by design (QbD), ICH guideline.
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References
[1] Vilegave kailsah, Vidyasagar Gali, “Preformulation Studies of Pharmaceutical New Drug Molecule and Products; An Overview†.2013; 1(3): 2321-3647.
[2] Lachman Leon, Lieberman Herbert A. and Kanig Joseph L. “The Theory and Pharmaceutical of Industrial Pharmacyâ€. Varghese publishing house, third edition, 171-196.
[3] Gopinath R., Naidu R.A.S., “Pharmaceutical Reformulation Studies-Current Review†International Journal of Pharmaceutical and Biological Archives, 2011; 2(5):1391-1400.
[4] Sahitya G., Krishna moorthy B., Muthukumaran M., “Importance of Preformulation Studies in Designing Formulations for Sustained Release Dosage Formâ€, ISSN-975-766X.
[5] Ajay, Bemis, G.W. and Murcko, M.A. “Designing libraries with CNS activityâ€. J Med. Chem., 1999; 42: 4942–51.
[6] Tushar Lathiya, Akhilesh D., Prabhakara.P, J.V. Kamath “Preformulation Studies of Controlled/Sustained Release Formulation: An Overviewâ€. ISRJP, 2012; 3(5): ISSN 2230-8407.
[7] J. Walter, Jr Weber, Chin Yu-Ping, “Determination of Partition Coefficient And Aqueous Solubility by Reverse Phase Chromatography-1â€, WAT Res., 1986; 20(11): 1422-1442.
[8] Qin-Wei Tong, “Pharmaceutical Preformulation:Integrated Drug Product Development Processâ€. University of Utah. July 2006.
[9] Keseru, G.M., Molnar, L. And Greiner, I. “A Neural Network Based Virtual High Throughput Screening Test for the Prediction of CNS Activityâ€. Comb. Chem. High Throughput Screen, 2000; 3: 535–40.
[10] Gibson Mark, “Pharmaceutical Guide from Candidate Drug Selection To Commercial Dosage Formâ€, 21-88.
[11] Pathare Beebe, Tambe Vrushali, Patel Vandana, “A Review on Various Analytical Methods Used In Determination of Dissociation Constantâ€, International Journal of Pharmacy and Pharmaceutical Science, 2014; 6(8): ISSN-0975-1491.
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[13] Marjamaki Marko, Keskinen Jorma, “Technologies for Measuring Paticulatesâ€, 248-256.
[14] Carr, R.L. “evaluating flow properties of solid†Chem.Eng., 1965; 72: 163-168
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[16] Mitchell, T. 2006. Personal communication: Cambridge, UK.
[17] Paul Kippax Dr, “Measuring Particle Size Using Modern Laser Diffraction Techniquesâ€, Chem-Europe.Com,UK, WR14 1*2
[18] Tushar Lathiya, Akhilesh D., prabhakara P., J.V Kamath, “Preformulation Studies of Controlled/Sustained Release Formulations: An Overviewâ€, IRJP, 2012; 3(5).
[19] Weissing volkmar, pettinger K Tacy, and Murdock Nicole, “Nanopharmaceuticals Products On The Marketâ€. Internation Journal of Nanomedicine.
[20] Savjani Ketan T., Gajjar Anuradha K., Savjani Jigana K., “Drug Solubility: Importance And Enhancement Techniqueâ€, ISRN Pharm., 2012; 195727.
[21] Gibson Mark, “Pharmaceutical Preformulation and Formulation,†second edition, 188-246.
[22] Gupta M, Patel G, Nimesh S, Madhulika K. “Enhancement of Dissolution Rate of Ibuprofen By Preparing Solid Dispersion Using Different Methodsâ€. Int J Pharm and Pharm Sci, 2011; 3(3): 204-06
[23] Rutkowska Ewelina, Pajak Karolina & Jozwiak “Kryzsztof. Lipophilicity- Methods of Determination and Its Role In Medical Chemistryâ€. Aata Polniae Pharmaceutical Drug Research, 2013; 70(1): 3-18.
[24] SourceURL:http://chemwiki.ucdavis.edu/Physical_Chemistry/Acids_and_Bases/Solubilty/Common_Ion_Effect
[25] Patel, Niraja, "Development and Characterization of Ternary Solid Dispersion Granules of Poorly Water Soluble Drugs: Diflunisal And Mefenamic Acid". Thesis and Dissertations. (2011) Paper 672
[26] Manallack David T, “The Pka Determination of Drug Discovery, Perspective Medicinal Chemistryâ€. 2007; 1 : 25-38.
[27] Bulk Density and Tapped density of powders, document QAS/11. 450 March 2012.
[28] Babic Sandra, Horvath J.M Alka, Pavlovic Mtavdzic Dragana, Macan-Kastelan Marija, “Determination of Pka Values of Active Pharmaceutical Ingredients, Trends In Analytical Chemistryâ€. 2007; 26(11).
[29] Sahid Mahanand Naji, Darwis Yusrida, Khiong Peh Kok, “Aerodynamic Characterization of Marketed Inhaler Dosage Forms: High Performance Liquid Chromatography Assay Method for the Determination Buclesonideâ€. 2010; 4(12): 878-884.
[30] Reijega jetse, Hoof van Arno, Loon van Antonie, Teunissen Bram, “Development of Methods of Determination of Pka Values, Analytical Chemistry Insightsâ€. 2013; 8: 53-71.
[31] Lumay G., Baschini F., Traina K., Bontempi S., Remy J.C., “Powder Technologyâ€, Measuring the flowing properties of powders and grainsâ€. 2012; 224: 19-27.
[32] Partition and Distribution coefficients, RSC Advancing the chemical science, Reckitt Benckiser.
[33] Pratap Surya Singh, Vivek Kushwah, Rathore Puneet, Jain Pritam, Jaiswal Satish. “Determination of Partition Coefficient of Salicylic Acid between N-Octanol and Distilled Waterâ€. 3 (2): 2145-2150.
[34] Chawla Garima, Gupta Piyush, Thilagavathi R., “Characterization of Solid-State Forms Of Celecoxibâ€. European Journal of Pharmaceutical Sciences, 2003; 20: 305-317.
[35] Fairhurst David, Weiner Bruce, “A Guide To Determination of Particle Size- Making An Effective And Reliable Measurement: Brookhaven Instrumentsâ€. A Nova Instrument Company.
[36] Patel Niraja, ‘Development and Characterization of Ternary Solid Dispersion Granules of Poorly Water Soluble Drugs: Diflunisal and Mefenamic Acidâ€. 2011; Thesis and dis.
[37] Bajaj Sanjay, Sakhuja Neha, “Stability testing of pharmaceutical productsâ€. Journal of Applied Pharmaceutical Science, 2012; 02(03): 129-138.
[38] Leo Albert, Hansch Corwin and Elkine David, “Partition coefficient and their usesâ€. 1971; 71.
[39] Larsson Jesper, “Methods For Measurement Of Solubility And Dissolution Rate Of Sparingly Soluble Drugsâ€. 2010.
[40] Horiba scientific, “A Guidebook to Particle Size Analysis
[41] Estime Nicolas, Teychene Sebastein, Autret Jean-Marie, “Influence of pH, Temperature and Impurities on the Solubility of an Active Pharmaceutical Ingredientâ€. API, DOI: 1542-6580.2099.
[42] Tagalpallewar V.R, Ughade M.A., Indurwade Dr. N.H., “Enhancement Of Solubility Of Poorly Water Solunle Drug By Solid Dispersion Techniqueâ€. 2015; 6(2).
[43] Gruner Klaus-Dieter, “Principle of Non-Contact Temperature Measurementâ€.
[44] Takacs Krisztina, “Solubility-Ph Profile Dugs. Experience and Surprise in Logs Measurementâ€.
[45] Nagendra kumar Dr. D., Keshavshetti G Ganesh, Ambarish Shardor, Kulkarni Pooja, “Enhancing Dissolution Rate of Naproxen Using Modern Techniqueâ€. 4(5): 929-939.
[46] Gopinath R., Naidu R.A.S., ‘Pharmaceutical Preformulation Studies-Current Reviewâ€. 2001; 2(5): 1391-1400.
[47] Niazi Sarfaraz K., “Handbook of Preformulation: Chemical, Biological, and Botanical Drugs RSâ€. 2006; 199. F67N53.
[48] Vyas J, Patel J, Jain D. “Preparation and Characterization of Solid Dispersion of Modafinil for Improvement of Dissolution Profileâ€. Int J Pharm and Pharmaceutical Sci, 2012; 14(5): 348-352.
[49] Natarajan R, Komala G, Ramcy TR, Swathi P, Mohan S. “Dissolution Enhancement Of Aceclofenacsolid Dispersion Prepared With Hydrophilic Carriers By Solvent Evaporation Methodsâ€. IJRPC, 2014; 4(1): 83-89.
[50] Bromberg L. “Cross Linked Polyethylene Glycol Networks as Reservoirs For Protein Deliveryâ€. J Apply Poly Sci , 1996; 59: 459-466.
[51] Verma PRP, Iyer SS. “Transdermal Delivery of Propranolol Using Mixedgrades of Eudragit: Design And In Vitro And In Vivo Evaluationâ€. Drug Dev. Ind Pharm, 2000; 26: 471-476.
[52] Martin, A., Swarbrick.J, and Cammarata, “A.Physical Pharmacy: Phisical Chemical Principles In The Pharmaceutical Sciencesâ€.3rd ed. Lea and Febiger, Philadelphia, 1983.
[53] Bemis, G.W. and Murcko, M.A. “Properties of known drugs. 2. Side chainsâ€. J Med. Chem., 1999; 42: 5095–5099.
[54] Ajay, A., Walters, W.P. and Murcko, M.A. “Can We Learn To Distinguish Between “Drug-Like†And “Nondrug-Like†Molecules†J Med. Chem., 1999; 41: 3314–3324.
[55] Comer, J. and Tam, K. “Lipophilicity Profile Les. Pharmacokinetic Optimization in Drug Research: Biological, Physicochemical and Computational Strategiesâ€. Wiley: Zurich. 2001; 275–304.
[56] Clark, D.E. and Pickett, S.D. “Computational Methods for the Prediction of ‘Drug-Likenessâ€. Drug Discov. Today, 2000; 5: 49–58.
[57] Clark, D.E. “Computational Prediction Of Blood-Brain Barrier Permeation. Annual Reports In Medicinal Chemistryâ€. Elsevier San Diego, 2005; 403–15.
[58] Wells, J.I “Pharmaceutical Preformulationâ€. Ells Hoowood Ltd. London, 1998; 25.
[59] WDI the World Drug Index is available from Derwent Informatin, London, U.K. www.derwent.com.
[2] Lachman Leon, Lieberman Herbert A. and Kanig Joseph L. “The Theory and Pharmaceutical of Industrial Pharmacyâ€. Varghese publishing house, third edition, 171-196.
[3] Gopinath R., Naidu R.A.S., “Pharmaceutical Reformulation Studies-Current Review†International Journal of Pharmaceutical and Biological Archives, 2011; 2(5):1391-1400.
[4] Sahitya G., Krishna moorthy B., Muthukumaran M., “Importance of Preformulation Studies in Designing Formulations for Sustained Release Dosage Formâ€, ISSN-975-766X.
[5] Ajay, Bemis, G.W. and Murcko, M.A. “Designing libraries with CNS activityâ€. J Med. Chem., 1999; 42: 4942–51.
[6] Tushar Lathiya, Akhilesh D., Prabhakara.P, J.V. Kamath “Preformulation Studies of Controlled/Sustained Release Formulation: An Overviewâ€. ISRJP, 2012; 3(5): ISSN 2230-8407.
[7] J. Walter, Jr Weber, Chin Yu-Ping, “Determination of Partition Coefficient And Aqueous Solubility by Reverse Phase Chromatography-1â€, WAT Res., 1986; 20(11): 1422-1442.
[8] Qin-Wei Tong, “Pharmaceutical Preformulation:Integrated Drug Product Development Processâ€. University of Utah. July 2006.
[9] Keseru, G.M., Molnar, L. And Greiner, I. “A Neural Network Based Virtual High Throughput Screening Test for the Prediction of CNS Activityâ€. Comb. Chem. High Throughput Screen, 2000; 3: 535–40.
[10] Gibson Mark, “Pharmaceutical Guide from Candidate Drug Selection To Commercial Dosage Formâ€, 21-88.
[11] Pathare Beebe, Tambe Vrushali, Patel Vandana, “A Review on Various Analytical Methods Used In Determination of Dissociation Constantâ€, International Journal of Pharmacy and Pharmaceutical Science, 2014; 6(8): ISSN-0975-1491.
[12] Nicklaus, M.C., Milne, G.W. and Zaharevitz, D., “Chem-X and Cambridge:Comparison of Computer Generated Chemical Structures With X-Ray Crystallographic Dataâ€. J Chem. Inf. Compute. Sci., 1993; 33: 639–46.
[13] Marjamaki Marko, Keskinen Jorma, “Technologies for Measuring Paticulatesâ€, 248-256.
[14] Carr, R.L. “evaluating flow properties of solid†Chem.Eng., 1965; 72: 163-168
[15] Sadowski, J. And Kubinyi, H. “A Scoring Scheme for Discriminating Between Drugs and Nondrugsâ€. J Med. Chem., 1998; 41: 3325–3329.
[16] Mitchell, T. 2006. Personal communication: Cambridge, UK.
[17] Paul Kippax Dr, “Measuring Particle Size Using Modern Laser Diffraction Techniquesâ€, Chem-Europe.Com,UK, WR14 1*2
[18] Tushar Lathiya, Akhilesh D., prabhakara P., J.V Kamath, “Preformulation Studies of Controlled/Sustained Release Formulations: An Overviewâ€, IRJP, 2012; 3(5).
[19] Weissing volkmar, pettinger K Tacy, and Murdock Nicole, “Nanopharmaceuticals Products On The Marketâ€. Internation Journal of Nanomedicine.
[20] Savjani Ketan T., Gajjar Anuradha K., Savjani Jigana K., “Drug Solubility: Importance And Enhancement Techniqueâ€, ISRN Pharm., 2012; 195727.
[21] Gibson Mark, “Pharmaceutical Preformulation and Formulation,†second edition, 188-246.
[22] Gupta M, Patel G, Nimesh S, Madhulika K. “Enhancement of Dissolution Rate of Ibuprofen By Preparing Solid Dispersion Using Different Methodsâ€. Int J Pharm and Pharm Sci, 2011; 3(3): 204-06
[23] Rutkowska Ewelina, Pajak Karolina & Jozwiak “Kryzsztof. Lipophilicity- Methods of Determination and Its Role In Medical Chemistryâ€. Aata Polniae Pharmaceutical Drug Research, 2013; 70(1): 3-18.
[24] SourceURL:http://chemwiki.ucdavis.edu/Physical_Chemistry/Acids_and_Bases/Solubilty/Common_Ion_Effect
[25] Patel, Niraja, "Development and Characterization of Ternary Solid Dispersion Granules of Poorly Water Soluble Drugs: Diflunisal And Mefenamic Acid". Thesis and Dissertations. (2011) Paper 672
[26] Manallack David T, “The Pka Determination of Drug Discovery, Perspective Medicinal Chemistryâ€. 2007; 1 : 25-38.
[27] Bulk Density and Tapped density of powders, document QAS/11. 450 March 2012.
[28] Babic Sandra, Horvath J.M Alka, Pavlovic Mtavdzic Dragana, Macan-Kastelan Marija, “Determination of Pka Values of Active Pharmaceutical Ingredients, Trends In Analytical Chemistryâ€. 2007; 26(11).
[29] Sahid Mahanand Naji, Darwis Yusrida, Khiong Peh Kok, “Aerodynamic Characterization of Marketed Inhaler Dosage Forms: High Performance Liquid Chromatography Assay Method for the Determination Buclesonideâ€. 2010; 4(12): 878-884.
[30] Reijega jetse, Hoof van Arno, Loon van Antonie, Teunissen Bram, “Development of Methods of Determination of Pka Values, Analytical Chemistry Insightsâ€. 2013; 8: 53-71.
[31] Lumay G., Baschini F., Traina K., Bontempi S., Remy J.C., “Powder Technologyâ€, Measuring the flowing properties of powders and grainsâ€. 2012; 224: 19-27.
[32] Partition and Distribution coefficients, RSC Advancing the chemical science, Reckitt Benckiser.
[33] Pratap Surya Singh, Vivek Kushwah, Rathore Puneet, Jain Pritam, Jaiswal Satish. “Determination of Partition Coefficient of Salicylic Acid between N-Octanol and Distilled Waterâ€. 3 (2): 2145-2150.
[34] Chawla Garima, Gupta Piyush, Thilagavathi R., “Characterization of Solid-State Forms Of Celecoxibâ€. European Journal of Pharmaceutical Sciences, 2003; 20: 305-317.
[35] Fairhurst David, Weiner Bruce, “A Guide To Determination of Particle Size- Making An Effective And Reliable Measurement: Brookhaven Instrumentsâ€. A Nova Instrument Company.
[36] Patel Niraja, ‘Development and Characterization of Ternary Solid Dispersion Granules of Poorly Water Soluble Drugs: Diflunisal and Mefenamic Acidâ€. 2011; Thesis and dis.
[37] Bajaj Sanjay, Sakhuja Neha, “Stability testing of pharmaceutical productsâ€. Journal of Applied Pharmaceutical Science, 2012; 02(03): 129-138.
[38] Leo Albert, Hansch Corwin and Elkine David, “Partition coefficient and their usesâ€. 1971; 71.
[39] Larsson Jesper, “Methods For Measurement Of Solubility And Dissolution Rate Of Sparingly Soluble Drugsâ€. 2010.
[40] Horiba scientific, “A Guidebook to Particle Size Analysis
[41] Estime Nicolas, Teychene Sebastein, Autret Jean-Marie, “Influence of pH, Temperature and Impurities on the Solubility of an Active Pharmaceutical Ingredientâ€. API, DOI: 1542-6580.2099.
[42] Tagalpallewar V.R, Ughade M.A., Indurwade Dr. N.H., “Enhancement Of Solubility Of Poorly Water Solunle Drug By Solid Dispersion Techniqueâ€. 2015; 6(2).
[43] Gruner Klaus-Dieter, “Principle of Non-Contact Temperature Measurementâ€.
[44] Takacs Krisztina, “Solubility-Ph Profile Dugs. Experience and Surprise in Logs Measurementâ€.
[45] Nagendra kumar Dr. D., Keshavshetti G Ganesh, Ambarish Shardor, Kulkarni Pooja, “Enhancing Dissolution Rate of Naproxen Using Modern Techniqueâ€. 4(5): 929-939.
[46] Gopinath R., Naidu R.A.S., ‘Pharmaceutical Preformulation Studies-Current Reviewâ€. 2001; 2(5): 1391-1400.
[47] Niazi Sarfaraz K., “Handbook of Preformulation: Chemical, Biological, and Botanical Drugs RSâ€. 2006; 199. F67N53.
[48] Vyas J, Patel J, Jain D. “Preparation and Characterization of Solid Dispersion of Modafinil for Improvement of Dissolution Profileâ€. Int J Pharm and Pharmaceutical Sci, 2012; 14(5): 348-352.
[49] Natarajan R, Komala G, Ramcy TR, Swathi P, Mohan S. “Dissolution Enhancement Of Aceclofenacsolid Dispersion Prepared With Hydrophilic Carriers By Solvent Evaporation Methodsâ€. IJRPC, 2014; 4(1): 83-89.
[50] Bromberg L. “Cross Linked Polyethylene Glycol Networks as Reservoirs For Protein Deliveryâ€. J Apply Poly Sci , 1996; 59: 459-466.
[51] Verma PRP, Iyer SS. “Transdermal Delivery of Propranolol Using Mixedgrades of Eudragit: Design And In Vitro And In Vivo Evaluationâ€. Drug Dev. Ind Pharm, 2000; 26: 471-476.
[52] Martin, A., Swarbrick.J, and Cammarata, “A.Physical Pharmacy: Phisical Chemical Principles In The Pharmaceutical Sciencesâ€.3rd ed. Lea and Febiger, Philadelphia, 1983.
[53] Bemis, G.W. and Murcko, M.A. “Properties of known drugs. 2. Side chainsâ€. J Med. Chem., 1999; 42: 5095–5099.
[54] Ajay, A., Walters, W.P. and Murcko, M.A. “Can We Learn To Distinguish Between “Drug-Like†And “Nondrug-Like†Molecules†J Med. Chem., 1999; 41: 3314–3324.
[55] Comer, J. and Tam, K. “Lipophilicity Profile Les. Pharmacokinetic Optimization in Drug Research: Biological, Physicochemical and Computational Strategiesâ€. Wiley: Zurich. 2001; 275–304.
[56] Clark, D.E. and Pickett, S.D. “Computational Methods for the Prediction of ‘Drug-Likenessâ€. Drug Discov. Today, 2000; 5: 49–58.
[57] Clark, D.E. “Computational Prediction Of Blood-Brain Barrier Permeation. Annual Reports In Medicinal Chemistryâ€. Elsevier San Diego, 2005; 403–15.
[58] Wells, J.I “Pharmaceutical Preformulationâ€. Ells Hoowood Ltd. London, 1998; 25.
[59] WDI the World Drug Index is available from Derwent Informatin, London, U.K. www.derwent.com.
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Kesharwani R, Ansari M S, Patel DK. NOVEL TECHNOLOGY USED IN THE PREFORMULATION STUDY: A REVIEW. JDDT [Internet]. 15Jul.2017 [cited 2Mar.2021];7(4):20-3. Available from: http://jddtonline.info/index.php/jddt/article/view/1487
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