STUDIES ON REFINED LIQUISOLID SYSTEM FOR SIMULTANEOUS IMPROVEMENT OF CONTENT UNIFORMITY AND DISSOLUTION PROFILE OF GLIMEPIRIDE
DOI:
https://doi.org/10.22159/ijap.2019v11i4.33025Keywords:
BCS, Glimepiride, Conventional solid dispersion, Surface solid dispersion, Content uniformity, Refined liquisolid systemAbstract
Objective: To improve and compare dissolution contour of poorly soluble BCS Class II drug Glimepiride (GLD) by altering it to conventional solid dispersion (CSD), surface solid dispersion (SSD) and refined liquisolid system (RLS).
Methods: The three formulations of GLD namely CSD, SSD and RLS were fabricated using the conventional methods by employing the suitable polymer and solvent system. These formulations were optimized on the basis of powder flow properties, FTIR, DSC and XRD analysis. All the optimized formulations were compared to the marketed formulation for content uniformity and dissolution rate.
Results: The characteristic analysis of all the optimized formulations was obtained in the standard range. The average content uniformity (% age) of Marketed formulation, CSD, SSD and RLS found to be 88.28±0.721, 92.91±0.789, 95.98±0.478, 99.32±0.744 respectively. The in vitro dissolution rate (%age at 30 min time interval) fall in the range 59.78±0.036, 75.78±0.013, 93.11±0.019, 93.99±0.062 and 98.55±0.043 for pure drug, Marketed formulation, CSD, SSD and RLS respectively. All the analytical studies exhibited improved homogeneity/distribution of the drug in RLS.
Conclusion: The RLS formulation presented sheer expansion in the content uniformity and dissolution contour of GLD at a minimal cost.
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Berner GM, Stevens CW. Pharmacology, drugs for diabetes mellitus. In: Saunders. 3rd ed. Philadelphia, Pennsylvania: Elsevier; 2010. p. 388-99.
Rosenkranz B, Profozic V, Metelko Z, Mrzljak V, Lange C, Malerczyk V. Pharmacokinetics and safety of glimepiride at clinically effective doses in diabetic patients with renal impairment. Diabetologia 1996;39:1617-24.
Ahmed I, Goldstein B. Diabetes mellitus. Clin Dermatol 2006;24:237-46.
Tripathi KD. Oral hypoglycaemic drugs. Essentials of medical pharmacology. 6th ed: New Delhi: Jaypee Brothers Medical Publishers (P) Ltd; 2008. p. 266-8.
Draeger E. Clinical profile of glimepiride. Diabetes Res Clin Pract 1995;28:139-46.
Lestari M LAD, Indrayanto G. Glimepiride; profiles of drug substances, excipients and related. Methodology 2011;36:169-204.
Mascarello A, Frederico MJ, Castro AJ, Mendes CP, Dutra MF, Woehl VM, et al. Novel sulfonyl (thio) urea derivatives act efficiently both as insulin secretagogues and as insulinomimetic compounds. Eur J Med Chem 2014;86:491-501.
Bhandare PS, Gharge VG. Formulation and evaluation of microencapsulated Glimepiride produced by the emulsion-solvent evaporation method. Pharma Tutor 2018;6:2-30.
Rajpurohit VS, Rakha P, Goyal S, Dureja H, Arora G, Nagpal M. Formulation and characterization of solid dispersions of glimepiride through factorial design. Iran J Pharm Sci 2011;7:7-16.
Singh SK, Prakash D, Sirinivasan KK, Kuppusamy G. Liquisolid compacts of glimepiride: an approach to enhance the dissolution of poorly water-soluble drugs. J Pharm Res 2011;4:2263-8.
Kiran T, Shastri N, Sistla R, Sadanandam M. Surface solid dispersion of glimepiride for enhancement of dissolution rate. Int J Pharm Res 2009;1:822-31.
Rajpurohita VS, Rakha P, Goyal S, Dureja H, Arora G, Nagpal M. Formulation and characterization of solid dispersions of glimepiride through factorial design. Iran J Pharm Sci 2011;7:7-16.
Patil SK, Wagh KS, Parik VB, Akarte AM, Baviskar DT. Strategies for solubility enhancement of poorly soluble drugs. Int J Pharm Sci Rev Res 2011;8:75-80.
Choudhary A, Rana CA, Aggarwal G, Kumar V, Zakir F. Development and characterization of an atorvastatin solid dispersion formulation using skimmed milk for improved oral bioavailability. Acta Pharm Sinica B 2012;2:421-8.
Chau VLN, Chulhun P, Beom Jin L. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm 2013;85:799-13.
Chiou WL, Riegelman S. Preparation and dissolution characteristics of several fast release solid dispersion of griseofulvin. J Pharm Sci 1969;58:1505-10.
Kurmi R, Mishra DK, Jain DK. Solid dispersion: a novel means of solubility enhancement. J Crit Rev 2016;3:1-8.
Arunachalam A, Karthikeyan M, Kishore K, Pottabathula PH, Sethuraman S. Solid dispersions: a review. Curr Pharma Res 2010;1:82-90.
Fazil, Shamsuddin M, Ansari HS, Ali J. Development and evaluation of solid dispersion of spironolactone using fusion method. Int J Pharm Investig 2016;6:63-8.
Huanga Y, Wei Guo D. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharm Sinica B 2014;4:18-25.
Kim KT, Lee JY, Lee MY, Song CK, Choi J, Kim D. Solid dispersions as a drug delivery system. J Pharm Invest 2011;41:125-42.
Marano S, Barker AS, Raimi Abraham TB, Missaghi S, Rajabi Siahboomi A, Craig DQM. Development of micro-fibrous solid dispersions of poorly water-soluble drugs in sucrose using temperature-controlled centrifugal spinning. Eur J Pharm Biopharm 2016;103:84-94.
Surampalli G, Kumar S, Nanjwade B, Patil PA. Amorphous solid dispersion method for improving oral bioavailability of poorly water-soluble drugs. J Pharm Res 2013;6:476–80.
Bary A Abd-El, Louis D, Sayed S. Olmesartan medoxomil surface solid dispersion-based orodispersible tablets: formulation and in vitro characterization. J Drug Delivery Sci Technol 2014; 24:665-72.
Bhagavanth GR, Madhusudhan A, Ramakrishna D. Development, evaluation and characterization of surface solid dispersion for solubility and dispersion enhancement of irbesartan. J Pharm Res 2013;7:472-47.
Fazil, Shamsuddin M, Ansari HS, Ali J. Development and evaluation of solid dispersion of spironolactone using fusion method. Int J Pharm Investig 2016;6:63-8.
Dixit RP, Nagarsenkar MS. In vitro and in vivo advantage of Celecoxib surface solid dispersion and dosage form development. Ind J Pharm Sci 2007;69:370-7.
Sisinthy SP, Selladurai S. Cinnarizine liquid solid compacts: preparation evaluation. Int J Appl Pharm 2019;11:150-7.
Rokade M, Khandagale P, Phadtare D. Liquisolid compact techniques: a review. Int J Curr Pharm Res 2018;10:1-5.
Vajir S. Enhancement of dissolution rate of poorly water soluble diclofenac sod. by liquisolid technique. Int J Pharm Chem Sci 2012;3:989-1008.
Hentzschel CM, Alnaief M, Smirnova I. Enhancement of griseofulvin release from liquisolid compacts. Eur J Pharm Biopharm 2012;80:130-5.
Sirisha VNL, Sruthi B, Namrata M, Harika IB, Kirankumar, Rao KK, et al. A review on liquid-solid compacts. Int J Pharm Phytopharmacol Res 2012;2:116-21.
Lindenberg M, Kopp S, Dressman JB. Classification of orally administered drugs on the world health organization model list of essential medicines according to the biopharmaceutics classification system. Eur J Pharm Biopharm 2004;58:265-78.
Nainar S, Rajiah K, Angamuthu S, Prabakaran D, Kasibhatta R. Biopharmaceutical classification system in in vitro/in vivo correlation: concept and development strategies in drug delivery. Trop J Pharm Res 2012;11:319-29.
Burkalow AV. Angle of repose and angle of sliding friction: an experimental study. GSA Bull 1945;56:669-707.
Denver Procedure for determining the angle of basic friction (static) uses a tilting table test. Materials Engineering and Research Laboratory, code 86-68180, Technical Service Center Designation USBR 6258-09; 1976.
Khatry S, Sood N, Arora S. Surface solid dispersion: a review. Int J Pharm Sci 2013;1:1915-24.
Rao M, Mandage Y, Thanki K, Bhise. Dissolution improvement of simvastatin by surface solid dispersion technology. Dissolution Technol 2010;6:27-34.
Anil A, Thomas L, Sudheer P. Liquisolid compacts: an innovative approach for dissolution enhancement. Int J Pharm Sci 2018;10:1-7.
Kapoor D, Lad C, Vyas R, Patel M. Formulation development, optimization and in vitro characterization of liquisolid compacts of oxicam derivative. J Drug Delivery Ther 2016;6:64-70.
Dias RJ, Mali KK, Ghorpade VS, Havaldar VD, Mohite VR. Formulation and evaluation of carbamazepine liquid-solid compact using novel carriers. Indian J Pharm Edu Res 2017;51(2S):69-77.
Bergum JS, Li H. Acceptance limits for the new ICH USP 29 content uniformity test. Pharm Tech 2007;31:91-6.
Mohanty SS, Biswal S, Biswal S, Sahoo J, Mahapatra AK, Murthy PN. Enhancement of dissolution rate of glimepiride using solid dispersions with polyvinylpyrrolidone k 90. Indian J Pharm Edu Res 2010;44:71-7.
Ibrahim EH, El-Faham TH, Mohammed FA, El-Eraky NS. Enhancement of solubility and dissolution rate of domperidone by utilizing different techniques. Bull Pharm Sci 2011; 34:105-20.
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