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Venlafaksin Hidroklorürün Uzatılmış Salım Yapan Tablet Formülasyonlarının Geliştirilmesi ve Değerlendirilmesi

Year 2022, Volume: 12 Issue: 1, 28 - 35, 14.01.2022
https://doi.org/10.33631/sabd.1055227

Abstract

Amaç: Depresyon, 250 milyondan fazla insanı yaştan bağımsız olarak etkileyen mental bozukluktur. Venlafaksin, antidepresan bir ilaçtır ve eski antidepresan ilaçlara göre daha az yan etki ile panik atak ve anksiyete tedavisinde kullanılır. Bununla birlikte, venlafaksin hidroklorür (VH), yeterli plazma-ilaç konsantrasyonunu sağlamak için günde üç kez dozlama gerektiren kısa yarı ömre sahiptir. Bu çalışmanın amacı, günde bir kez verilecek uzun süreli salım yapan VH tabletleri geliştirmektir.
Gereç ve Yöntemler: Kontrollü salım ajanı olarak polietilen oksit, sodyum aljinat, hidroksipropil metil selüloz, guar zamkı ve poliakrilik asit kullanıldı. Tabletler doğrudan basım yöntemi ile hazırlandı. Toz (yığın açısı, akış hızı, Carr indeksi ve Hausner oranı) ve tablet (ağırlık homojenliği, sertlik, friabilite) karakterizasyonları değerlendirildi. 24 saat boyunca in vitro salım çalışmaları yapıldı ve ilaç salım kinetikleri farklı modeller kullanılarak değerlendirildi.
Bulgular: Guar zamkı ile hazırlanan formülasyon dışında tüm formülasyonlar uygun Carr indeksi ve Hausner oranı gösterdi. Doğrudan basım yöntemi ile üretilen tabletler, ticari tablet ile karşılaştırıldı. Tüm formülasyonlar için uzun süreli VH salımı gözlendi. In vitro salım hızı test sonuçlarına göre, HPMC ve Carbopol polimerlerini içeren F1 formülasyonundan ilaç salımı, ticari tabletlere kıyasla benzer bulunmuştur.
Sonuç: Doğrudan basılmış VH tabletler, hasta uyumu ve diğer üretim yöntemlerine kıyasla daha az üretim aşaması ile ticari tabletlere tercih edilebilir bir alternatif olabilir.

References

  • Burcusa SL, Iacono WG. Risk for recurrence in depression. Clin Psychol Rev. 2007; 27(8): 959-85.
  • Olchanski N, McInnis Myers M, Halseth M, Cyr PL, Bockstedt L, Goss TF, et al. The economic burden of treatment-resistant depression. Clin Ther. 2013; 35(4): 512-22.
  • Katon W, Schulberg H. Epidemiology of depression in primary care. Gen Hosp Psychiatry. 1992; 14(4): 237-47.
  • Sifneos PE. Comprehensive textbook of psychiatry. Psychosom Med. 1967; 29(5): 552-3.
  • Thase ME, Shelton RC, Khan A. Treatment with venlafaxine extended release after ssrı nonresponse or ıntolerance. J Clin Psychopharmacol. 2006; 26(3): 250-8.
  • Montgomery SA, Entsuah R, Hackett D, Kunz NR, Rudolph RL. Venlafaxine versus placebo in the preventive treatment of recurrent major depression. J Clin Psychiatry. 2004; 65(3): 328-36.
  • Aranaz I, Panos I, Peniche C, Heras A, Acosta N. Chitosan spray-dried microparticles for controlled delivery of venlafaxine hydrochloride. Molecules. 2017; 26(11): 1980. 8. Peng Y, Li J, Li J, Fei Y, Dong J, Pan W. Optimization of thermosensitive chitosan hydrogels for the sustained delivery of venlafaxine hydrochloride. Int J Pharm. 2013; 441(1-2): 482-90.
  • Aboelwafa AA, Basalious, EB. Optimization and in vivo pharmacokinetic study of a novel controlled release venlafaxine hydrochloride three-layer tablet. AAPS PharmSciTech. 2010; 11(3): 1026-37.
  • Pathan IB, Shingare PR, Kurumkar P. Formulation design and optimization of novel mouth dissolving tablets for venlafaxine hydrochloride using sublimation technique. J Pharm Res. 2013; 6(6): 593-8.
  • Haque S, Md S, Fazil M, Kumar M, Sahni JK, Ali J. Venlafaxine loaded chitosan NPs for brain targeting: Pharmacokinetic and pharmacodynamic evaluation. Carbohydr Polym. 2012; 89(1): 72-9.
  • Sun J, Liu Y, Sun Y, Zhao N, Sun M, He Z. Preparation and in vitro/in vivo evaluation of sustained-release venlafaxine hydrochloride pellets. Int J Pharm. 2012; 426(1–2): 21-8.
  • Segale L, Giovannelli L, Foglio Bonda A, Pattarino F, Rinaldi M. Effect of self-emulsifying phase composition on the characteristics of venlafaxine loaded alginate beads. J Drug Deliv Sci Technol. 2020; 55: 101483.
  • Gil-Chávez J, Padhi SSP, Leopold CS, Smirnova, I. Application of aquasolv lignin in ibuprofen-loaded pharmaceutical formulations obtained via direct compression and wet granulation. Int J Biol Macromol, 2021; 174: 229-39.
  • Bhosale AV, Hardikar SR, Patil N, Patel U, Sumbe Y, Jagtap R. Formulation and in-vitro evaluation of microbially triggered ibuprofen delivery for colon targetting. Int J PharmTech Res. 2009; 1(2): 328-33.
  • Wan LSC, Heng PWS, Wong LF. Relationship between swelling and drug release in a hydrophilic matrix. Drug Dev Ind Pharm. 1993; 19(10): 1201-10.
  • Tuǧcu-Demiröz F, Acartürk F, Takka S, Konuş-Boyunaǧa Ö. Evaluation of alginate based mesalazine tablets for intestinal drug delivery. Eur J Pharm Biopharm. 2007; 67(2): 491-7.
  • Tuǧcu-Demiröz F, Acartürk F, Takka S, Konuş-Boyunaǧa Ö. In-vitro and in-vivo evaluation of mesalazine-guar gum matrix tablets for colonic drug delivery. J Drug Target. 2004; 12(2): 105-12.
  • Zhang X, Gu X, Wang X, Wang H, Mao S. Tunable and sustained-release characteristics of venlafaxine hydrochloride from chitosan–carbomer matrix tablets based on in situ formed polyelectrolyte complex film coating. Asian J Pharm Sci. 2018; 13(6): 566-74.
  • Pawar HA, Dhavale R. Development and evaluation of gastroretentive floating tablets of an antidepressant drug by thermoplastic granulation technique. Beni-Suef Univ J Basic Appl Sci. 2014; 3(2): 122-32.
  • Haeusler JMC. Change in formulation and its potential clinical and pharmacoeconomic value: example of extended release venlafaxine. Current Med Res Opin, 2009; 25(5): 1089-94.
  • Hiremath SP, Saha RN. Design and study of rifampicin oral controlled release formulations. Drug Deliv. 2004; 11(5): 311-7.
  • Taylor MK, Ginsburg J, Hickey AJ, Gheyas F. Composite method to quantify powder flow as a screening method in early tablet or capsule formulation development. AAPS PharmSciTech. 2000; 1: 20-30.
  • Osei-Yeboah F, Sun CC. Validation and applications of an expedited tablet friability method. Int J Pharm. 2015; 484(1-2): 146-55.
  • Zhang Y, Huo M, Zhou J, Zou A, Li W, Yao C, et al. DDSolver: An add-in program for modeling and comparison of drug dissolution profiles. AAPS J. 2010; 12(3): 263-71.
  • Noreen M, Farooq MA, Ghayas S, Bushra R, Yaqoob N, Abrar MA. Formulation and in vitro characterization of sustained release tablets of lornoxicam. Lat Am J Pharm. 2019; 38(4): 701-11.
  • Khairnar MVA, Bakliwal SR, Rane BR, Pawar SP. A Novel on “Formulation and Evaluation of Sustained Release Matrix Tablet of Anti-Hypertensive Drug.” Drugs. 2016; 2(6): 1-10.
  • Anisuzzman M, Islam S, Arif Ur Rashid AHM, Alam MN, Acharzo AK. Formulation development and evaluation of bio-adhesive carbopol 974P nf polymer matrix based sustained release gliclazide tablet. Int Res J Pharm. 2017; 8(4): 28-34.
  • Yang L, Venkatesh G, Fassihi R. Characterization of compressibility and compactibility of poly(ethylene oxide) polymers for modified release application by compaction simulator. J Pharm Sci. 1996; 85(10): 1085-90.
  • Reddy BV. Formulation and characterization of extended release matrix tablets of venlafaxine hydrochloride. Journal of Global Trends in Pharmaceutical Sciences. 2015; 6(1): 2423-8.
  • Ma L, Deng L, Chen J. Applications of poly(ethylene oxide) in controlled release tablet systems: a review. Drug Dev Ind Pharm. 2014; 40(7): 845-51.
  • Körner A, Larsson A, Andersson Å, Piculell L. Swelling and polymer erosion for poly(ethylene oxide) tablets of different molecular weights polydispersities. J Pharm Sci. 2010; 99(3): 1225-38.
  • Ford JL, Rubinstein MH, Hogan JE. Formulation of sustained release promethazine hydrochloride tablets using hydroxypropyl-methylcellulose matrices. Int J Pharm. 1985; 24(2–3): 327-38.
  • Sahadevan JT, Prabhakaran R, Vijay J, Mehra Gilhotra R. Formulation and evaluation of cephalexin extended-release matrix tablets using hydroxy propyl methyl cellulose as rate-controlling polymer. J Young Pharm. 2012; 4(1): 3-12.
  • Acharya S, Patra S, Pani NR. Optimization of HPMC and carbopol concentrations in non-effervescent floating tablet through factorial design. Carbohydr Polym. 2014; 102: 360-8.
  • Kiss D, Süvegh K, Zelkó R. The effect of storage and active ingredient properties on the drug release profile of poly(ethylene oxide) matrix tablets. Carbohydr Polym. 2008; 74(4): 930-3.
  • Cappello B, Derosa G, Gıannını L, Larotonda M, Mensıtıerı G, Mıro A, et al. Cyclodextrin-containing poly(ethyleneoxide) tablets for the delivery of poorly soluble drugs: Potential as buccal delivery system. Int J Pharm. 2006; 319(1–2): 63-70.
  • Petrovic J, Jockovic J, Ibric S, Duric Z. Modelling of diclofenac sodium diffusion from swellable and water-soluble polyethylene oxide matrices. J Pharm Pharmacol. 2009; 61(11): 1449-56.
  • Li H, Hardy RJ, Gu X. Effect of drug solubility on polymer hydration and drug dissolution from polyethylene oxide (peo) matrix tablets. AAPS PharmSciTech. 2008; 9(2): 437-43.
  • Prasad YVR, Krishnaiah YS., Satyanarayana S. In vitro evaluation of guar gum as a carrier for colon-specific drug delivery. J Control Release. 1998; 51(2–3): 281-7.
  • Rajendra K, Vishnu Patel HP. Comparative evaluation study of matrix properties of natural gums and semi-synthetic polymer. J Pharm Res. 2008; 1(2): 208-14.
  • Khan MS, Vishakante GD, Bathool A. Preparation and evaluation of sodium alginate porous dosage form as carriers for low dosed active pharmaceutical ingredients. Turkish J Pharm Sci. 2012; 9(2): 183-98.
  • Liew CV, Chan LW, Ching AL, Heng PWS. Evaluation of sodium alginate as drug release modifier in matrix tablets. Int J Pharm. 2006; 309(1–2): 25-37.
  • Mandal S, Ray R, Basu SK, Sa B. Evaluation of a matrix tablet prepared with polyacrylamide-g-sodium alginate co-polymers and their partially hydrolyzed co-polymers for sustained release of diltiazem hydrochloride. J Biomater Sci Polym Ed. 2010; 21(13): 1799-814.
  • Omprakash B, Ajay S, Santosh G, Amin P. Formulation development of venlafaxine hydrochloride extended release tablet and invitro characterizations. Int J PharmTech Res. 2012; 4(4): 1777-84.
  • Zuo J, Gao Y, Bou-Chacra N, Löbenberg R. Evaluation of the DDSolver software applications. Biomed Res Int. 2014; 2014: 1-9.

Development and Evaluation of Sustained Release Tablet Formulations of Venlafaxine Hydrochloride

Year 2022, Volume: 12 Issue: 1, 28 - 35, 14.01.2022
https://doi.org/10.33631/sabd.1055227

Abstract

References

  • Burcusa SL, Iacono WG. Risk for recurrence in depression. Clin Psychol Rev. 2007; 27(8): 959-85.
  • Olchanski N, McInnis Myers M, Halseth M, Cyr PL, Bockstedt L, Goss TF, et al. The economic burden of treatment-resistant depression. Clin Ther. 2013; 35(4): 512-22.
  • Katon W, Schulberg H. Epidemiology of depression in primary care. Gen Hosp Psychiatry. 1992; 14(4): 237-47.
  • Sifneos PE. Comprehensive textbook of psychiatry. Psychosom Med. 1967; 29(5): 552-3.
  • Thase ME, Shelton RC, Khan A. Treatment with venlafaxine extended release after ssrı nonresponse or ıntolerance. J Clin Psychopharmacol. 2006; 26(3): 250-8.
  • Montgomery SA, Entsuah R, Hackett D, Kunz NR, Rudolph RL. Venlafaxine versus placebo in the preventive treatment of recurrent major depression. J Clin Psychiatry. 2004; 65(3): 328-36.
  • Aranaz I, Panos I, Peniche C, Heras A, Acosta N. Chitosan spray-dried microparticles for controlled delivery of venlafaxine hydrochloride. Molecules. 2017; 26(11): 1980. 8. Peng Y, Li J, Li J, Fei Y, Dong J, Pan W. Optimization of thermosensitive chitosan hydrogels for the sustained delivery of venlafaxine hydrochloride. Int J Pharm. 2013; 441(1-2): 482-90.
  • Aboelwafa AA, Basalious, EB. Optimization and in vivo pharmacokinetic study of a novel controlled release venlafaxine hydrochloride three-layer tablet. AAPS PharmSciTech. 2010; 11(3): 1026-37.
  • Pathan IB, Shingare PR, Kurumkar P. Formulation design and optimization of novel mouth dissolving tablets for venlafaxine hydrochloride using sublimation technique. J Pharm Res. 2013; 6(6): 593-8.
  • Haque S, Md S, Fazil M, Kumar M, Sahni JK, Ali J. Venlafaxine loaded chitosan NPs for brain targeting: Pharmacokinetic and pharmacodynamic evaluation. Carbohydr Polym. 2012; 89(1): 72-9.
  • Sun J, Liu Y, Sun Y, Zhao N, Sun M, He Z. Preparation and in vitro/in vivo evaluation of sustained-release venlafaxine hydrochloride pellets. Int J Pharm. 2012; 426(1–2): 21-8.
  • Segale L, Giovannelli L, Foglio Bonda A, Pattarino F, Rinaldi M. Effect of self-emulsifying phase composition on the characteristics of venlafaxine loaded alginate beads. J Drug Deliv Sci Technol. 2020; 55: 101483.
  • Gil-Chávez J, Padhi SSP, Leopold CS, Smirnova, I. Application of aquasolv lignin in ibuprofen-loaded pharmaceutical formulations obtained via direct compression and wet granulation. Int J Biol Macromol, 2021; 174: 229-39.
  • Bhosale AV, Hardikar SR, Patil N, Patel U, Sumbe Y, Jagtap R. Formulation and in-vitro evaluation of microbially triggered ibuprofen delivery for colon targetting. Int J PharmTech Res. 2009; 1(2): 328-33.
  • Wan LSC, Heng PWS, Wong LF. Relationship between swelling and drug release in a hydrophilic matrix. Drug Dev Ind Pharm. 1993; 19(10): 1201-10.
  • Tuǧcu-Demiröz F, Acartürk F, Takka S, Konuş-Boyunaǧa Ö. Evaluation of alginate based mesalazine tablets for intestinal drug delivery. Eur J Pharm Biopharm. 2007; 67(2): 491-7.
  • Tuǧcu-Demiröz F, Acartürk F, Takka S, Konuş-Boyunaǧa Ö. In-vitro and in-vivo evaluation of mesalazine-guar gum matrix tablets for colonic drug delivery. J Drug Target. 2004; 12(2): 105-12.
  • Zhang X, Gu X, Wang X, Wang H, Mao S. Tunable and sustained-release characteristics of venlafaxine hydrochloride from chitosan–carbomer matrix tablets based on in situ formed polyelectrolyte complex film coating. Asian J Pharm Sci. 2018; 13(6): 566-74.
  • Pawar HA, Dhavale R. Development and evaluation of gastroretentive floating tablets of an antidepressant drug by thermoplastic granulation technique. Beni-Suef Univ J Basic Appl Sci. 2014; 3(2): 122-32.
  • Haeusler JMC. Change in formulation and its potential clinical and pharmacoeconomic value: example of extended release venlafaxine. Current Med Res Opin, 2009; 25(5): 1089-94.
  • Hiremath SP, Saha RN. Design and study of rifampicin oral controlled release formulations. Drug Deliv. 2004; 11(5): 311-7.
  • Taylor MK, Ginsburg J, Hickey AJ, Gheyas F. Composite method to quantify powder flow as a screening method in early tablet or capsule formulation development. AAPS PharmSciTech. 2000; 1: 20-30.
  • Osei-Yeboah F, Sun CC. Validation and applications of an expedited tablet friability method. Int J Pharm. 2015; 484(1-2): 146-55.
  • Zhang Y, Huo M, Zhou J, Zou A, Li W, Yao C, et al. DDSolver: An add-in program for modeling and comparison of drug dissolution profiles. AAPS J. 2010; 12(3): 263-71.
  • Noreen M, Farooq MA, Ghayas S, Bushra R, Yaqoob N, Abrar MA. Formulation and in vitro characterization of sustained release tablets of lornoxicam. Lat Am J Pharm. 2019; 38(4): 701-11.
  • Khairnar MVA, Bakliwal SR, Rane BR, Pawar SP. A Novel on “Formulation and Evaluation of Sustained Release Matrix Tablet of Anti-Hypertensive Drug.” Drugs. 2016; 2(6): 1-10.
  • Anisuzzman M, Islam S, Arif Ur Rashid AHM, Alam MN, Acharzo AK. Formulation development and evaluation of bio-adhesive carbopol 974P nf polymer matrix based sustained release gliclazide tablet. Int Res J Pharm. 2017; 8(4): 28-34.
  • Yang L, Venkatesh G, Fassihi R. Characterization of compressibility and compactibility of poly(ethylene oxide) polymers for modified release application by compaction simulator. J Pharm Sci. 1996; 85(10): 1085-90.
  • Reddy BV. Formulation and characterization of extended release matrix tablets of venlafaxine hydrochloride. Journal of Global Trends in Pharmaceutical Sciences. 2015; 6(1): 2423-8.
  • Ma L, Deng L, Chen J. Applications of poly(ethylene oxide) in controlled release tablet systems: a review. Drug Dev Ind Pharm. 2014; 40(7): 845-51.
  • Körner A, Larsson A, Andersson Å, Piculell L. Swelling and polymer erosion for poly(ethylene oxide) tablets of different molecular weights polydispersities. J Pharm Sci. 2010; 99(3): 1225-38.
  • Ford JL, Rubinstein MH, Hogan JE. Formulation of sustained release promethazine hydrochloride tablets using hydroxypropyl-methylcellulose matrices. Int J Pharm. 1985; 24(2–3): 327-38.
  • Sahadevan JT, Prabhakaran R, Vijay J, Mehra Gilhotra R. Formulation and evaluation of cephalexin extended-release matrix tablets using hydroxy propyl methyl cellulose as rate-controlling polymer. J Young Pharm. 2012; 4(1): 3-12.
  • Acharya S, Patra S, Pani NR. Optimization of HPMC and carbopol concentrations in non-effervescent floating tablet through factorial design. Carbohydr Polym. 2014; 102: 360-8.
  • Kiss D, Süvegh K, Zelkó R. The effect of storage and active ingredient properties on the drug release profile of poly(ethylene oxide) matrix tablets. Carbohydr Polym. 2008; 74(4): 930-3.
  • Cappello B, Derosa G, Gıannını L, Larotonda M, Mensıtıerı G, Mıro A, et al. Cyclodextrin-containing poly(ethyleneoxide) tablets for the delivery of poorly soluble drugs: Potential as buccal delivery system. Int J Pharm. 2006; 319(1–2): 63-70.
  • Petrovic J, Jockovic J, Ibric S, Duric Z. Modelling of diclofenac sodium diffusion from swellable and water-soluble polyethylene oxide matrices. J Pharm Pharmacol. 2009; 61(11): 1449-56.
  • Li H, Hardy RJ, Gu X. Effect of drug solubility on polymer hydration and drug dissolution from polyethylene oxide (peo) matrix tablets. AAPS PharmSciTech. 2008; 9(2): 437-43.
  • Prasad YVR, Krishnaiah YS., Satyanarayana S. In vitro evaluation of guar gum as a carrier for colon-specific drug delivery. J Control Release. 1998; 51(2–3): 281-7.
  • Rajendra K, Vishnu Patel HP. Comparative evaluation study of matrix properties of natural gums and semi-synthetic polymer. J Pharm Res. 2008; 1(2): 208-14.
  • Khan MS, Vishakante GD, Bathool A. Preparation and evaluation of sodium alginate porous dosage form as carriers for low dosed active pharmaceutical ingredients. Turkish J Pharm Sci. 2012; 9(2): 183-98.
  • Liew CV, Chan LW, Ching AL, Heng PWS. Evaluation of sodium alginate as drug release modifier in matrix tablets. Int J Pharm. 2006; 309(1–2): 25-37.
  • Mandal S, Ray R, Basu SK, Sa B. Evaluation of a matrix tablet prepared with polyacrylamide-g-sodium alginate co-polymers and their partially hydrolyzed co-polymers for sustained release of diltiazem hydrochloride. J Biomater Sci Polym Ed. 2010; 21(13): 1799-814.
  • Omprakash B, Ajay S, Santosh G, Amin P. Formulation development of venlafaxine hydrochloride extended release tablet and invitro characterizations. Int J PharmTech Res. 2012; 4(4): 1777-84.
  • Zuo J, Gao Y, Bou-Chacra N, Löbenberg R. Evaluation of the DDSolver software applications. Biomed Res Int. 2014; 2014: 1-9.
There are 45 citations in total.

Details

Primary Language Turkish
Subjects Pharmacology and Pharmaceutical Sciences
Journal Section Research Articles
Authors

Serdar Tort This is me 0000-0003-4945-5420

Esra Kodan Akça This is me 0000-0002-0011-6025

Seval Olğaç This is me 0000-0001-8876-9268

Sinem Saar This is me 0000-0001-6892-5497

Ayşegül Yıldız This is me 0000-0002-3435-0530

İlay Sema Ünal This is me 0000-0001-5054-9606

Zeliha Duygu Özdal This is me 0000-0001-5273-3407

Fatmanur Tuğcu Demiröz This is me 0000-0002-9468-3329

Publication Date January 14, 2022
Submission Date January 6, 2021
Published in Issue Year 2022 Volume: 12 Issue: 1

Cite

Vancouver Tort S, Kodan Akça E, Olğaç S, Saar S, Yıldız A, Ünal İS, Özdal ZD, Tuğcu Demiröz F. Venlafaksin Hidroklorürün Uzatılmış Salım Yapan Tablet Formülasyonlarının Geliştirilmesi ve Değerlendirilmesi. VHS. 2022;12(1):28-35.