Stabilisasi Tablet yang Mengandung Zat Aktif Bersifat Higroskopis

Fitri Nurjanah, Sriwidodo Sriwidodo, Bambang Nurhadi

Abstrak

Rute pemberian obat secara oral banyak disukai masyarakat karena mudah digunakan. Salah satu bentuk sediaan oral yang paling disukai adalah tablet. Tablet adalah bentuk sediaan padat yang mengandung bahan aktif dengan atau tanpa eksipien. Dalam formulasi tablet, kandungan air zat obat dan eksipien padat merupakan parameter penting yang harus dipantau selama proses pengembangan produk obat. Pada sediaan padat, senyawa yang bersifat higroskopis dapat menimbulkan masalah yang dapat mempengaruhi aliran serbuk, kompresibilitas, dan kekerasan tablet. Pada review artikel ini akan di bahas mengenai pengaruh kelembapan terhadap karakteristik fisika tablet dan upaya menjaga stabilitas zat aktif yang sensitif terhadap kelembapan. Review ini menyimpulkan bahwa pemilihan eksipien, penyalutan tablet dan kemasan yang tepat dapat menjaga kestabilan tablet dari pengaruh kelembapan.

Kata Kunci

Tablet, zat aktif, stabilisasi, higroskopis

Teks Lengkap:

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Referensi

. Bibi, R., Naqvi, B.S., Shoaib, M.H. and Rahim, N. Design and evaluation of a new formulation of enalapril maleate tablet. Pak J Pharm Sci. 2011. 24, pp.211-215.

. Pawar R, Jaimini M, Chauhan BS, Sharma SK. Compression coated tablets as drug delivery system (tablet in tablet): a review. International Journal of Pharmaceutical Research and Development. 2014 Mar;6(1):21-33.

. Gaikwad VD, Yadav VD, Gaikwad MD. Novel sustained release and swellable gastroretentive dosage form for ciprofloxacin hydrochloride. International journal of pharmaceutical investigation. 2014 Apr;4(2):88-92.

. Jin P, Madieh S, Augsburger LL. Selected physical and chemical properties of feverfew (Tanacetum parthenium) extracts important for formulated product quality and performance. AAPS PharmSciTech. 2008 Mar 1;9(1):22-30.

. Anbarasan A, Nataraj J, Shanmukhan N, Radhakrishnan A. Effect of hygroscopicity on pharmaceutical ingredients, methods to determine and overcome: an overview. Journal of Chemical and Pharmaceutical Research. 2018;10(3):61-7.

. Dely A, Lodin U, Nangia A, inventors; Andrx Labs LLC, assignee. Formulations including hygroscopic compounds. United States patent application US 11/391,739. 2007 Oct 4.

. Singh S. Increase In The Rate Of Moisture Gain By Hygroscopic Drugs In The Presence Of Non-Hygroscopic Water-Soluble Substances: Study Of The Generalization Of This Hitherto Unknown Phenomenon, Explanation To Its Occurrence And Implications In Formulation Developm. Asian Journal Of Pharmaceutics (Ajp): Free Full Text Articles From Asian J Pharm. 2016 Sep 9;1(1):69-76

. Roy S, et al. A systemic approach on understanding the role of moisture in pharmaceutical product degradation and its prevention: challenges and perspectives. Biomedical Research 2018; 29 (17): 3336-3343

. Nokhodchi A, Javadzadeh Y. The effect of storage conditions on the physical stability of tablets. Pharmaceutical Technology Europe. 2007 Jan 1;19(1):20.

.Tomar M, Kumar SA, Raj SA. Effect of moisture content of exicipient (microcrystalline cellulose) on direct compressible solid dosage forms. International Journal of Pharmaceutical Sciences and Research. 2017;8(1):282.

. Lei J, Sha P, Jin R, Shi Y, Shen X, inventors; Shanghai Anbison Laboratory Co., Ltd., assignee. Preparation method of the solid formulation of Clopidogrel bisulfate. United States patent US 9,144,550. 2015 Sep 29.

. Badawi AA, Hegazy MM, Louis D, Eldegwy MA. Solving manufacturing problems for L-carnitine-L-tartrate to improve the likelihood of successful product scale-up. Acta Pharmaceutica. 2017 Dec 20;67(4):511-25.

Riyanti, K.M.P. and Rohmani, S., Pengaruh Variasi Konsentrasi Avicel PH 102 dengan Dikalsium Fosfat Anhidrat sebagai Fillerbinder terhadap Sifat Fisik Tablet Vitamin C. In Prosiding APC (Annual Pharmacy Conference) (Vol. 3, No. 1).

. Gallo L, Ramírez-Rigo MV, Piña J, Palma S, Allemandi D, BucalÁ V. Valeriana officinalis dry plant extract for direct compression: preparation and characterization. Scientia pharmaceutica. 2012 Dec;80(4):1013-26.

. Damayanti D, Sari IP, Sulaiman TS, Bestari AN, Setiawan IM. The Formulation of Pacing (Costus speciosus) Extract Tablet by Using Avicel® Ph 200 As Filler-Binder and Amylum As Disintegration Agent. Indonesian Journal of Pharmacy. 2018 Jan 2;29(1):29.

. Autamashih M, Isah AB, Allagh TS, Ibrahim MA. Use of avicel® ph-103 and selected binders in the tablet formulation of the del-iquescent crude leaves extract of Vernonia galamensis (Asteraceae). International Journal of Research in Pharmaceutical Sciences. 2011 Apr 25;2(2):295-300.

. Wendemagegn Sm. Formulation Of Cassia Didymobotrya Leaf Laxative Tablets (Doctoral Dissertation, University Of Nairobi). 2016

. Islam SA, Hossain MA, Kabir AH, Kabir S, Hossain MK. Study of moisture absorption by ranitidine hydrochloride: effect of% RH, excipients, dosage forms and packing materials. Dhaka University Journal of Pharmaceutical Sciences. 2008;7(1):59-64.

. Nishimura M, et al. Effects of intravenous L-carnitine on myocardial fatty acid imaging in hemodialysis patients: responders or non-responders to L-carnitine. SpringerPlus. 2015 Dec 1;4(1):353.

.Guy A. Cellulose, Microcrystalline, dalam Rowe, R.C., Sheskey, P.J., dan Quinn, M.E., (Eds.), Handbook of Pharmaceutical Excipients, 6 th Ed., 129-131, London: Pharmaceutical Press;2009

Rahman MS, Al-Rizeiqi MH, Guizani N, Al-Ruzaiqi MS, Al-Aamri AH, Zainab S. Stability of vitamin C in fresh and freeze-dried capsicum stored at different temperatures. Journal of food science and technology. 2015 Mar 1;52(3):1691-7.

. Hadisoewignyo L, Teny Gracesya Florensya, dkk Pengaruh bahan pengisi padat Ibu Profen dengan metode cetak langsung, Majalah farmasi Indonesia (22). 2011; hal. 279-285.

. Tong HH, Wong SY, Law MW, Chu KK, Chow AH. Anti-hygroscopic effect of dextrans in herbal formulations. International journal of pharmaceutics. 2008 Nov 3;363(1-2):99-105.

. Sari IP, Nurrochmad A, Rahayu S. Evaluation of Anti-Fertility Effect of Aqueous Extract of Costus speciosus (Koen.) JE Smith Rhizome in Mice. Int J Pharm Chem Res. 2016;8:440-.

Allagh TS, Ameh GO, Okafor IS. Formulation and evaluation of the physicochemical properties of Ageratum conyzoides (Fam asteraceae) granules and tablets. Niger J Pharm Sci. 2009 Oct;8:18-25.

. Choudhari Y, Hoefer H, Libanati C, Monsuur F, McCarthy W. Mesoporous silica drug delivery systems. InAmorphous Solid Dispersions 2014 (pp. 665-693). Springer, New York, NY.

Rajabi-Siahboomi AR, Levina M, Upadhye SB, Teckoe J. Excipient Selection in Oral Solid Dosage Formulations Containing Moisture Sensitive Drugs. InExcipient Applications in Formulation Design and Drug Delivery 2015 (pp. 385-421). Springer, Cham.

Pahwa R, Sharma S, Kumar V, Kohli K. Ranitidine hydrochloride: An update on analytical, clinical and pharmacological aspects. J Chem Pharm Res. 2016;8(7):70-80.

Silverstein: Excipient quality and selectionPharmaceutical technology Europe 2016; 28 (2): 16-20.

Waterman, K.C.,Adami, R.C..Accelerated aging: prediction Of chemical stability of pharmaceuticals.Int.J.Pharm. 2016; 293 (1-2): 101–125.

Hockerfelt, M.H., Alderborn, G.,. The crystallinity of cellulose controls The physical distribution of sorbed water and the capacity to present water for chemical degradation of a solid drug. Int.J. Pharm. 2014;477 (1-2): 326–333.

Accupril (Quinapril Hydrochloride) Product Monograph. Canada: Parke Davis and Company Pfizer Inc. [di unduh 30 Juni 2020] Tersedia dari: https://www.pfizer.ca/sites/default/files/201710/accupril_pm_200979_e_14mar2017_clean.pdf.

Shwetha margret jl, & madhavi blr. Study of direct compression method for the preparation of quinapril hydrochloride tablets. Asian journal of pharmaceutical and clinical research. 2019; 13 (1): 202–211.

. Alsabbagh, M., Abdel, W., Khalyl, A. Assesment of the Impact of Formulation and Packaging on the Stability of Cabergoline Tablets. International Journal of Pharmacy and Pharmaceutical Science. 2012; 4 (5), 511-518

Monika Tomar, Ajay Kumar Singh and Amit Raj Sinha. Physicochemical parameter of microcrystalline cellulose and the most acceptability in pharmaceutical Industries. Journal of Innovations in Pharaceuticals and biological Sciences. 2015; 2(4):570-578.

Richardson, P.H., Balchem Corp. Stable hygroscopic compositions and methods for stabilizing hygroscopic ingredients. U.S. Patent. 2006; 6: 797, 291

Akhavan-Mahdavi, S., S. M. Jafari, E. Assadpoor and D. Dehnad. Microencapsulation optimization of natural anthocyanins with maltodextrin, gum Arabic and gelatin. Int. J. Biol. Macromol. 2016; 85: 379-385

Joshi, S. and Petereit, H.U. Film coatings for taste masking and moisture protection. International journal of pharmaceutics. 2013; 457(2): 395-406.

Snyder, H.E dan Lechuga-Ballesteros, D. Spray drying: theory and Pharmaceutical applications. In: Pharmaceutical Dosage Forms: (Tablets L.L. Augsburger and S.W. Hoag). New York: Informa Health Care; 2008

Thoorens G, Krier F, Leclercq B, Carlin B, Evrard B. Microcrystalline cellulose, a direct compression binder in a quality by design environment.. Int J Pharm. 2015; 473(1-2) :64-72.

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