Abstract View

Author(s): Rohit Patil*1, Sachinkumar Patil2, Sachin Mali.3

Email(s): 1rdpatil2000rp@gmail.com

Address:

    1Ashokrao Mane College of Pharmacy, Peth Vadgaon
    416112, (M.S.) India

Published In:   Volume - 3,      Issue - 4,     Year - 2024

DOI: Not Available

 View HTML        View PDF

Please allow Pop-Up for this website to view PDF file.

ABSTRACT:
The abstract provides an overview of solubility in pharmaceuticals, emphasizing its significance and challenges. It discusses the importance of drug solubility in dosage frequency and bioavailability, highlighting the prevalence of solubility issues in marketed drugs. The framework for classifying biopharmaceuticals (BCS) categorizes medicines determined by solubility and permeability, guiding formulation strategies. Cocrystals offer a promising approach to address solubility challenges, providing a rational means to modify drug properties. The abstract explores the definition and potential of cocrystals in various applications, with a focus on pharmaceuticals. It examines the mechanisms of cocrystal formation and their impact on drug solubility enhancement. Various cocrystallization techniques, including solution-based and solid-state methods, are discussed, along with analytical techniques for characterization. Case studies on AZL-NA and lopinavir-menthol cocrystals highlight the efficacy of cocrystal technology in improving drug properties. Future prospects for cocrystal engineering involve overcoming commercialization challenges and scaling up production. Computer-assisted techniques and continuous processes offer promising avenues for advancing cocrystal technology. Overall, cocrystal engineering presents a viable strategy for enhancing drug solubility and bioavailability, potentially leading to the development of novel and improved pharmaceutical formulations.

Cite this article:
Rohit Patil, Sachinkumar Patil, Sachin Mali. Unlocking Potential: Cocrystals as catalyst for heightened solubility and dissolution of low solubility pharmaceuticals. IJRPAS, July – Aug 2024; 3(4): 73-88.



1.                  Gaikwad SS, Mhalaskar RS, Mahale YD, Jain NP. Review on: solubility enhancement of poorlywater-soluble drug. Indo Am J Pharm Res. 2014;4(11):5530-41.

2.                  Patel R, Patel N, Patel NM, Patel M. A novel approach for dissolution enhancement of Ibuprofen by preparing floating granules. Int. J. Res. Pharm. Sci. 2010;1(1):57-64.

3.                  Nash RA. Suspensions,‖ in Encyclopedia of Pharmaceutical Technology, J. Swarbrick and JC Boylan, Eds., vol. 3.

4.                  Chowdary KP, Madhavi BL. Novel drug delivery technologies for insoluble drugs. Indiandrugs-bombay. 2005;42(9):557.

5.                  Humberstone AJ, Charman WN. Lipid-based vehicles for the oral delivery of poorly water- soluble drugs. Advanced drug delivery reviews. 1997;25(1):103-28.

6.                  Spireas S, inventor; HYGROSOL PHARMACEUTICAL CORP, assignee. Liquisolid systems and methods of preparing same. United States patent US 6,423,339. 2002 Jul 23.

7.                  Steed JW. The role of co-crystals in pharmaceutical design. Trends in pharmacological science. 2013 Mar 1;34(3):185-93.

8.                  Jones JT, Hasell T, Wu X, Bacsa J, Jelfs KE, Schmidtmann M, Chong SY, Adams DJ, Trewin A, Schiffman F, Cora F. Modular and predictable assembly of porous organic molecular crystals. Nature. 2011 Jun 16;474(7351):367-71.

9.                  Tayi AS, Shveyd AK, Sue AC, Szarko JM, Rolczynski BS, Cao D, Kennedy TJ, Sarjeant AA, Stern CL, Paxton WF, Wu W. Room-temperature ferroelectricity in supramolecular networks of charge-transfer complexes. Nature. 2012 Aug 23;488(7412):485-9.

10.              Huang KS, Britton D, Byrn SR. A novel class of phenol–pyridine co-crystals for second harmonic generation. Journal of Materials Chemistry. 1997;7(5):713-20.

11.              Etter MC, Reutzel SM. Hydrogen bond directed cocrystallization and molecular recognition properties of acyclic imides. Journal of the American Chemical Society. 1991 Mar;113(7):2586-98.

12.              Etter MC, Urbanczyk-Lipkowska Z, Zia-Ebrahimi M, Panunto TW. Hydrogen bond-directed cocrystallization and molecular recognition properties of diarylureas. Journal of the American Chemical Society. 1990 Nov;112(23):8415-26.

13.              Brittain HG. Cocrystal systems of pharmaceutical interest: 2010. Crystal growth & design. 2012 Feb 1;12(2):1046-54.

14.              Shan N, Zaworotko MJ. The role of cocrystals in pharmaceutical science. Drug discovery today. 2008 May 1;13(9-10):440-6.

15.              Jones W, Motherwell WS, Trask AV. Pharmaceutical cocrystals: An emerging approach to physical property enhancement. MRS bulletin. 2006 Nov;31(11):875-9.

16.              Blagden N, Berry DJ, Parkin A, Javed H, Ibrahim A, Gavan PT, De Matos LL, Seaton CC. Current directions in co-crystal growth. New Journal of Chemistry. 2008;32(10):1659-72.

17.              Good DJ, Rodríguez-Hornedo N. Solubility advantage of pharmaceutical cocrystals. Crystal Growth and Design. 2009 May 6;9(5):2252-64.

18.              Wouters J, Quéré L, editors. Pharmaceutical salts and co-crystals. Royal Society of Chemistry; 2011 Nov 4.

19.              Barbour LJ, Das D, Jacobs T, Lloyd GO, Smith VJ. Concepts and nomenclature in chemical crystallography. Supramolecular Chemistry: From Molecules to Nanomaterials. 2012 Mar 15.

20.              Friscic T, Jones W. Recent advances in understanding the mechanism of cocrystal formation via grinding. Crystal Growth and Design. 2009 Mar 4;9(3):1621-37.

21.              Dunitz JD. Crystal and co-crystal: a second opinion. CrystEngComm. 2003;5(91):506.

22.              Bis JA, Vishweshwar P, Weyna D, Zaworotko MJ. Hierarchy of Supramolecular Synthons: Persistent Hydroxyl Pyridine Hydrogen Bonds in Cocrystals That Contain a Cyano Acceptor. Molecular Pharmaceutics. 2007 Jun 4;4(3):401-16.

23.               Almarsson Ö, Zaworotko MJ. Crystal engineering of the composition of pharmaceutical phases. Do pharmaceutical co-crystals represent a new path to improved medicines?. Chemical communications. 2004(17):1889-96.

24.              Trask AV. An overview of pharmaceutical cocrystals as intellectual property. Molecular pharmaceutics. 2007 Jun 4;4(3):301-9.

25.              Aakeröy CB, Forbes S, Desper J. Using cocrystals to systematically modulate aqueous solubility and melting behavior of an anticancer drug. Journal of the American Chemical Society. 2009 Dec 2;131(47):17048-9.

26.              Griesser UJ. The importance of solvates. Polymorphism: In the pharmaceutical industry. 2006 Feb 6:211-33.

27.              Almarsson O, Zaworotko MJ. Crystal engineering of the composition of pharmaceutical phases: Do pharmaceutical co-crystals represent a new path to improved medicines. Chem Commun. 2004;35(17):1889-96.

28.              Khan M, Enkelmann V, Brunklaus G. Crystal engineering of pharmaceutical co-crystals: application of methylparaben as molecular hook. J Am Chem Soc. 2010;132(14):5254-63.

29.              Karki S, Friscic T, Jones W. Control and interconversion of cocrystal stoichometry in grinding: stepwise mechanism for the formation of a hydrogen-bonded cocrystal. Crysteng Comm. 2009;11(3):470-81.

30.              He GW, Jacob C, Guo LF, Chow PS, Tan RBH. Screening for cocrystallization tendency: The role of intermolecular interaction. J Phys Chem B. 2008;112(32):9890-5.

31.              Bis JA, Vishweshwar P, Weyna D, Zaworotko MJ. Hierarchy of supramolecular synthons: Persistent hydroxyl pyridine hydrogen bonds in cocrystals that contain a cyano acceptor. Mol Pharmaceutics. 2007;4(3):401-16.

32.              Vishweshwar P, McMahon JA, Bis JA, Zaworotko MA. Pharmaceutical cocrystals. J Pharm Sci. 2006;95:499-516

33.              Jones W, Motherwell WDS, Trask AV. Pharmaceutical co-crystals: An Emerging approach to physical property enhancement. MRS Bull. 2006;31(11):875-9.

34.              Guidance D. Regulatory Classification of Pharmaceutical Co-Crystals Guidance for Industry. US Dept. of Health and Human Services FDA Center for Drug Evaluation and Research (CDER). Rev. 2016 Aug;1.

35.              Cerreia VP, Chierotti MR, Gobetto R. Pharmaceutical aspects of salt and cocrystal forms of APIs and characterization challenges. Adv Drug Deliv Rev. 2017;117:86-110.

36.              Serajuddin AT. Salt formation to improve drug solubility. Advanced drug delivery reviews. 2007 Jul 30;59(7):603-16.

37.              Good DJ, Rodríguez-Hornedo N. Solubility Advantage of Pharmaceutical Cocrystals. Cryst Growth Des. 2009;9(5):2252-64.

38.              Liu R. Water-insoluble drug formulation. CRC press; 2000 Sep 30.

39.              Yalkowsky SH. Solubility and Solubilization in Aqueous Media. American Chemical Society. New York: Oxford University Press: 1999. J Am Chem Soc. 2000;122(40):9882.

40.              Bak A, Gore A, Yanez E, Stanton M, Tufekcic S, Syed R, et al. The co-crystal approach to improve the exposure of a water-insoluble compound: AMG 517 sorbic acid co-crystal characterization and pharmacokinetics. J Pharm Sci. 2008;97(9):3942-56

41.              Trask AV, Motherwell WDS, Jones W. Physical stability enhancement of theophylline via cocrystallization. Int J Pharm. 2006;320(1-2):114-23

42.              Kuminek G, Cao F, Bahia de Oliveira da Rocha A, Gonc¸alves Cardoso S, Rodrıguez-Hornedo N. Cocrystals to facilitate delivery of poorly soluble compounds beyond-rule-of-5. Adv Drug Deliv Rev 2016;101:143-66.

43.              Weyna DR, Shattock T, Vishweshwar P, Zaworotko MJ. Synthesis and structural characterization of cocrystals and pharmaceutical cocrystals: mechanochemistry vs slow evaporation from solution. Cryst Growth Des 2009;9:1106-23.

44.              Mullin JW. Crystallization. Elsevier; 2001 May 9.

45.              ZQ, Chow PS, Tan RBH. Operating regions in cooling cocrystallization of caffeine and glutaric acid in acetonitrile. Cryst Growth Des 2010;10:2382-7.

46.              Rodrıguez-Hornedo N, Nehm SJ, Seefeldt KF, Pagan-Torres Y, Falkiewicz CJ. Reaction crystallization of pharmaceutical molecular complexes. Mol Pharm 2006;3:362-7.

47.              3. Huang Y, Zhou L, Yang W, Li Y, Yin Q. Preparation of theophylline-benzoic acid cocrystal and on-line monitoring of cocrystallization process in solution by Raman spectroscopy. Crystals 2019;9:329-44.

48.              Dai XL, Yao J, Wu C, Deng JH, Mo YH, Lu TB, et al. Solubility and permeability improvement of allopurinol by cocrystallization. Cryst Growth Des 2020;20:5160-8.

49.              Nagapudi K, Umanzor EY, Masui C. High-throughput screening and scale-up of cocrystals using resonant acoustic mixing. Int J Pharm 2017;521:337-45.

50.              Michalchuk AAL, Hope KS, Kennedy SR, Blanco MV, Boldyreva EV, Pulham CR. Ball-free mechanochemistry: in situ real-time monitoring of pharmaceutical co-crystal formation by resonant acoustic mixing. Chem Comm 2018;54:4033-6.

51.              am Ende DJ, Anderson SR, Salan JS. Development and scale-up of cocrystals using resonant acoustic mixing. Org Process Res Dev 2014;18:331-41

52.              Guo M, Sun X, Chen J, Cai T. Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications. Acta Pharmaceutica Sinica B. 2021 Aug 1;11(8):2537-64.

53.              Kaupp G. Solid-state molecular syntheses: complete reactions without auxiliaries based on the new solid-state mechanism. Cryst Eng Comm 2003;5:117-33.

54.              Chadwick K, Davey R, Cross W. How does grinding produce cocrystals? Insights from the case of benzophenone and diphenylamine. Cryst Eng Comm 2007;9:732-4.

55.              Lien Nguyen K, Friscic T, Day GM, Gladden LF, Jones W. Terahertz time-domain spectroscopy and the quantitative monitoring of mechanochemical cocrystal formation. Nat Mater 2007;6:206-9.

56.              Macfhionnghaile P, Crowley CM, Mcardle P, Erxleben A. Spontaneous solid-state co-crystallization of caffeine and urea. Cryst Growth Des 2020;20:736-45.

57.              Fischer F, Scholz G, Benemann S, Rademann K, Emmerling F. Evaluation of the formation pathways of cocrystal polymorphs in liquid-assisted syntheses. Cryst Eng Comm 2014;16:8272-8.

58.              Lapidus SH, Stephens PW, Arora KK, Shattock TR, Zaworotko MJ. A comparison of cocrystal structure solutions from powder and single crystal techniques. Cryst Growth Des 2010;10(10):4630-7.

59.              Kumar S, Nanda A. Pharmaceutical cocrystals: an overview. Indian J Pharm Sci 2017;79(6):858-71.

60.              Patole T, Deshpande A. Co-crystallization-a technique for solubility enhancement. Int J Pharm Sci Res 2014;5(9):3566- 76.

61.              Xiao Y, Jin T, Geng X, Zhu X. Azilsartan-nicotinamide cocrystal: Preparation, characterization and in vitro/vivo evaluation. European Journal of Pharmaceutical Sciences. 2022 1;176:106241.

62.              Fayed ND, Arafa MF, Essa EA, El Maghraby GM. Lopinavir-menthol co-crystals for enhanced dissolution rate and intestinal absorption. Journal of Drug Delivery Science and Technology. 2022 1;74:103587.

63.              Vogt FG, Clawson JS, Strohmeier M, Edwards AJ, Pham TN, Watson SA. Solid-state NMR analysis of organic cocrystals and complexes. Cryst Growth Des 2009;9(2):921-37.

64.              Kotak U, Prajapati VD, Solanki HK, Jani GK, Jha P. Cocrystallization technique its rationale and recent progress World J Pharm Pharm Sci 2015;4(4):1484-508.

Related Images:



Recent Images



RPHPLC Method for Concurrent Determination of Haloperidol and Trihexyphenidyl in API and Combined Tablet Formulations
A review on HPLC Methods for Estimation of Travoprost  in Combined and Single Pharmaceutical formulation and Bulk
To Study number and types of refund Medicines from different Wards of Hospital to the In-Patient Pharmacies
A Novel RP-HPLC Analytical Method Development and Validation of Berberine In Bulk and Polyherbal Formulation
Formulation and Evaluation of A Polyherbal Cough Syrup with Potential Anti-Obesity Effects
Formulation and evaluation of Herbal Face Cream
Formulation and In-vitro Evaluation of Cold Cream
Prevalence study of Diabetes Mellitus
Design and Optimization of Extended-Release Mini-Tablets of Metoprolol Succinate Using Okra Stalk Powder and HPMC K100 M as Release Modifiers
Comprehensive review on Alfuzosin quantification: Analytical techniques and the evolution of AQbD in method development

Tags


Recomonded Articles:

Author(s): Hasanen Pinjari; Rehan Deshmukh; Khan Faizan; Dr. Gulam Javed.

DOI:         Access: Open Access Read More

Author(s): Shaikh Aminoddin Raisoddin; Shifa Maniya; Sayeeda Begum; Naziya Shaikh.

DOI:         Access: Open Access Read More

Author(s): Girisha Chaudhari;Sofiya Morris; Dr. Ashish Jain

DOI:         Access: Open Access Read More

Author(s): Devadatta Pandurang Hatim; Sachinkumar V. Patil; Sachin Mali

DOI:         Access: Open Access Read More

Author(s): Magendran Rajendiran1*, Muruganand R2, Abhisek Kumar Sinha2, Mohamed Raashith M S2, Jasitha Begam M2, Usharani G2, Dhivyari D2, Deepika T2

DOI: https://doi.org/10.71431/IJRPAS.2025.4413         Access: Open Access Read More

Author(s): Mohammad Zaid*; Prof. Imran Kalam; Dr. Quazi Majaz

DOI:         Access: Open Access Read More

Author(s): Venkatesh; Chaithra N; Parthasarathi K Kulkarni; Siddartha H N; Hanumanthachar Joshi K

DOI:         Access: Open Access Read More

Author(s): Apurva Arabhavi; Manisha Mane; Neha Desap Sachin Mali; Akanksha Sawant.

DOI:         Access: Open Access Read More

Author(s): Mr. Shrinivas Kapale; Mr. Gopal Lohiya; Dr.Kranti Satpute

DOI:         Access: Open Access Read More

Author(s): Quazi Kamil Hafiz Anees Ahemad; Dr. Majaz Quazi; Quazi Wasil; Dr. G. J. Khan

DOI:         Access: Open Access Read More

Author(s): Swetha Yoganandan1, Gururaj S Kulkarni1, Padmaa M Paarakh2, Surinder Kaur1, A. Muthukumar3

DOI:         Access: Open Access Read More

Author(s): Vaibhav S. Jadhav; Vishwajeet G. Thorat; Priyanka V. Gawali; Dr. Balmukund R. Rathi

DOI:         Access: Open Access Read More

Author(s): Mansoori Safwan Salim; Prof. Rehan Deshmuhk; Dr. G.J. Khan; Shaikh Amaan; Sayyed Ahamad Sayyed Kaleem; Hamza Iliyas Amliwala

DOI:         Access: Open Access Read More

Author(s): S. Sathya, Karthiga. D, Lokesh. S, Sabari Manikandan, V. R. Rajeswari

DOI: https://doi.org/10.71431/IJRPAS.2025.4105         Access: Open Access Read More

Author(s): Mansuri Jahid; Rehan Deshmukh; Khan Ramiz.V; Sayyed Anas Ali

DOI:         Access: Open Access Read More

Author(s): Nilesh R. Suryawanshi; Karan. A. Patil; Nikhil. J. Rajput; H. P. Suryawanshi; R. A. Ahirrao; J. I. Pinjari

DOI:         Access: Open Access Read More

Author(s): Shaikh Aklakh Gafar1*; Dr. M.H.G Dehghan1;Khan Juber Kadir2

DOI:         Access: Open Access Read More

Author(s): Baburao Mohite; Manisha Mane; Sarika Suryavanshi; Shrirang Kharmate; Pranali Patil; Anand Gadad.

DOI:         Access: Open Access Read More

Author(s): Museb shaikh Mukhtar; Khalifa Mahmadasif Y; Pathan Ayyaj Magbul; Shaikh Faisal; Shaikh Aman; MD Moiz, Shaikh Arbaj.

DOI:         Access: Open Access Read More