Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride

Isaiah Boyapati; Rajendra Awasthi; Giriraj T. Kulkarni

Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride

Abstract

Multiple unit particulate system (MUPS) is more recent, challenging, effective and attractive option for the pharmaceutical industries that gives an efficient way to deliver drugs in modified pattern. This study aimed to improve the release profile of venlafaxine hydrochloride by developing modified release MUPS using polyvinyl pyrrolidone K-30, ethyl cellulose 20 cps and Hypromellose E 5LV. Preliminary trials were carried out to select the inert carrier, binder, and viscosity grade of rate controlling polymers. Further, optimization of binder concentration and extended-release coating was carried out. The formulation development of MUPS was divided into two categories as (i) drug layering on inert carrier, i.e., sugar spheres and (ii) extended-release coating. Comparative multimedia dissolution study of venlafaxine hydrochloride extended-release capsules was carried out and compared with the marketed formulation to ascertain the in vitro drug release behavior. XRD study indicated conversion of monohydrate form of venlafaxine hydrochloride and remained unaffected during storage. SEM images confirmed smooth surface of MUPS without any pores. The coated spheres had more dense surface compared to the uncoated pellets. Hypromellose E 5 LV showed better binding properties. Ethyl cellulose (20 cps) showed sustained release profile. The blend containing ER – I spheres (10% coating) and ER – II spheres (11% coating) at 60: 40 ratio showed dissolution profile similar to that of the innovator product. The formulated venlafaxine hydrochloride loaded MUPS filled in hard gelatin capsule can open a new avenue for the delivery of therapeutics with improved potential.

Keywords

References

[1] Awasthi R, Kulkarni GT, Ramana MV, Pinto TJA, Kikuchi IS, Ghisleni DDM, Braga MS, Bank PD, Dua K. Dual crosslinked pectin–alginate network as sustained release hydrophilic matrix for repaglinide. Int J Biol Macromol. 2017; 97: 721-732. [CrossRef]
[2] Bhatt P, Patel D, Patel A, Patel A, Nagarsheth A. Oral controlled release systems: current strategies and challenges. In: Misra A, Shahiwala A, editors. Novel drug delivery technologies. Singapore: Springer Nature; 2019, p. 73-120. [CrossRef]
[3] Wheless JW, Phelps SJ. A clinician's guide to oral extended-release drug delivery systems in epilepsy. J Pediatr Pharmacol Ther. 2018: 23(4): 277-292. [CrossRef]
[4] Hoffman A. Pharmacodynamic aspects of sustained release preparations. Adv Drug Deliv Rev. 1998; 33(3): 185-199. [CrossRef]
[5] Ranade VV. Drug delivery systems 5A. Oral drug delivery. J Clin Pharmacol. 1991; 31(1): 2-16. [CrossRef]
[6] Leucuta SE. Drug delivery systems with modified release for systemic and biophase bioavailability. Curr Clin Pharmacol. 2012; 7(4): 282-317. [CrossRef]
[7] Qiu Y. Lee PI. Rational design of oral modified-release drug delivery systems. In: Qiu Y, Chen Y, Zhang G, Yu L, Mantri RV, editor. Developing solid oral dosage forms; United States: Academic Press; 2017, p. 519-554. [CrossRef]
[8] Fu Y, Kao WJ. Drug release kinetics and transport mechanisms of non-degradable and degradable polymeric delivery systems. Expert Opin Drug Deliv. 2010; 7(4): 429-444. [CrossRef]

[9] Al-Hashimi N, Begg N, Alany RG, Hassanin H, Elshaer A. Oral modified release multiple-unit particulate systems: Compressed pellets, microparticles and nanoparticles. Pharmaceutics. 2018; 10(4): 176. [CrossRef]
[10] Patel S, Patel N, Misra M, Joshi A. Controlled-release domperidone pellets compressed into fast disintegrating tablets forming a multiple-unit pellet system (MUPS). J Drug Deliv Sci Technol. 2018; 45: 220-229. [CrossRef]
[11] Abdul S, Chandewar AV, Jaiswal SB. A flexible technology for modified-release drugs: multiple-unit pellet system (MUPS). J Control Release. 2010; 147(1): 2-16. [CrossRef]
[12] Bhattacharya S, Kshirsagar R, Joshi M, Pandita S. Extended release formulation of venlafaxine hydrochloride. U.S. Patent 7,807,195, October 5, 2010.
[13] Sanghavi BJ, Wolfbeis OS, Hirsch T, Swami NS. Nanomaterial-based electrochemical sensing of neurological drugs and neurotransmitters. Microchimica Acta. 2015; 182(1-2): 1-41. [CrossRef]
[14] Sherman DM, Clark JC, Lamer JU, A Steven. White. Extended release formulation of venlafaxine hydrochloride. United States Patent US6419958B2. 18.07.2002.
[15] Magalhães P, Alves G, Llerena A, Falcão A. Venlafaxine pharmacokinetics focused on drug metabolism and potential biomarkers. Drug Metabol Drug Interact. 2014; 29(3): 129-141. [CrossRef]
[16] Ali KA, Han J, Lee YJ, inventors; Wyeth LLC, assignee. Crystalline polymorph of venlafaxine hydrochloride and methods for the preparation thereof. United States patent US 7,030,164. 2006 Apr 18.
[17] Roy S, Aitipamula S, Nangia A. Thermochemical analysis of venlafaxine hydrochloride polymorphs 1− 5. Cryst Growth Des. 2005; 5(6): 2268-2276. [CrossRef]
[18] Madan JR, Patil K, Awasthi R, Dua K. Formulation and evaluation of solid self-microemulsifying drug delivery system for azilsartan medoxomil. Int J Polym Mater. 2021; 70(2): 100-116. [CrossRef]
[19] Murdande SB, Pikal MJ, Shanker RM, Bogner RH. Aqueous solubility of crystalline and amorphous drugs: Challenges in measurement. Pharm Dev Technol. 2011; 16: 187-200. [CrossRef]
[20] Awasthi R, Kulkarni GT. Development of novel gastroretentive floating particulate drug delivery system of gliclazide. Curr Drug Deliv. 2012; 9(5): 437-451. [CrossRef]
[21] Rahman Z, Siddiqui A, Bykadi S, Khan MA. Determination of tacrolimus crystalline fraction in the commercial immediate release amorphous solid dispersion products by a standardized X-ray powder diffraction method with chemometrics. Int J Pharm. 2014; 475(1-2): 462-470. [CrossRef]
[22] Tan DCT, Chin WW, Tan EH, Hong S, Gu W, Gokhale R. Effect of binders on the release rates of direct molded verapamil tablets using twin-screw extruder in melt granulation. Int J Pharm. 2014; 463(1): 89-97. [CrossRef]

Details

Primary Language

English

Subjects

Pharmaceutical Sciences

Journal Section

Research Article

Authors

Isaiah Boyapati This is me
India

Rajendra Awasthi ^*
India

Giriraj T. Kulkarni ^* This is me
India

Publication Date

June 28, 2025

Submission Date

October 3, 2021

Acceptance Date

November 18, 2021

Published in Issue

Year 2022 Volume: 26 Number: 1

IZ

https://izlik.org/JA27CS35TG

Cite

RIS / Bibtex

APA

Boyapati, I., Awasthi, R., & Kulkarni, G. T. (2025). Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride. Journal of Research in Pharmacy, 26(1), 75-87. https://izlik.org/JA27CS35TG

AMA

1.Boyapati I, Awasthi R, Kulkarni GT. Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride. J. Res. Pharm. 2025;26(1):75-87. https://izlik.org/JA27CS35TG

Chicago

Boyapati, Isaiah, Rajendra Awasthi, and Giriraj T. Kulkarni. 2025. “Formulation, Characterization, and in Vitro Release Studies of Modified Release Multiple Unit Particulate System (MUPS) of Venlafaxine Hydrochloride”. Journal of Research in Pharmacy 26 (1): 75-87. https://izlik.org/JA27CS35TG.

EndNote

Boyapati I, Awasthi R, Kulkarni GT (June 1, 2025) Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride. Journal of Research in Pharmacy 26 1 75–87.

IEEE

[1]I. Boyapati, R. Awasthi, and G. T. Kulkarni, “Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride”, J. Res. Pharm., vol. 26, no. 1, pp. 75–87, June 2025, [Online]. Available: https://izlik.org/JA27CS35TG

ISNAD

Boyapati, Isaiah - Awasthi, Rajendra - Kulkarni, Giriraj T. “Formulation, Characterization, and in Vitro Release Studies of Modified Release Multiple Unit Particulate System (MUPS) of Venlafaxine Hydrochloride”. Journal of Research in Pharmacy 26/1 (June 1, 2025): 75-87. https://izlik.org/JA27CS35TG.

JAMA

1.Boyapati I, Awasthi R, Kulkarni GT. Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride. J. Res. Pharm. 2025;26:75–87.

MLA

Boyapati, Isaiah, et al. “Formulation, Characterization, and in Vitro Release Studies of Modified Release Multiple Unit Particulate System (MUPS) of Venlafaxine Hydrochloride”. Journal of Research in Pharmacy, vol. 26, no. 1, June 2025, pp. 75-87, https://izlik.org/JA27CS35TG.

Vancouver

1.Isaiah Boyapati, Rajendra Awasthi, Giriraj T. Kulkarni. Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride. J. Res. Pharm. [Internet]. 2025 Jun. 1;26(1):75-87. Available from: https://izlik.org/JA27CS35TG