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Ijpbs-2010-01-03

Int J Pharm Biomed Sci 2010, 1(1), 12-15 Research Drops
PharmaInterScience Publishers

Formulation and in vitro
evaluation of floating drug delivery system
for salbutamol sulphate


The purpose of this research work is to formulate the salbutamol sulphate as a floating matrix tablets and control the drug release up to 24 h for administration as once daily dose. Salbutamol Sulphate is a short acting bronchodilators which have short biological half life about 2 - 4 h. Floating matrix tablets were formulated by Department of Pharmaceutics, Gokula using swelling polymer like Methylcellulose, Hydroxy propyl methyl cellulose Krishna College of Pharmacy, Sullurpet 524 121, Nellore district, Andhra (K100M, K4M) with different concentration 25, 50, 75 % w/w of the polymer were used for the preparation of the floating matrix tablets. The formulation variables like hardness, polymer concentrations, and shape of the tablets were optimized to *Correspondence:
Mr. V. Narayan
achieve the floating nature of the tablet in stomach for 24 h. In addition stearic acid is included in this formulation to evaluate their release characteristics. From this the hydrophilic floating matrix control the release up to 12 h with HPMC K100M at 75 % w/w of the polymer concentration. The formulations, which have stearic acid retards the drug release by controlling the water penetrations in to the floating matrix tablets, sustained their drug release above 12 h. The floating matrix tablets with minimum hardness of 5 kg/cm2 and round shaped tablets exhibited better buoyancy. Key words: Salbutamol sulphate, Floating matrix tablets, Methylcellulose, HPMC K100M, HPMC K4M Received: 15 May 2010 / Revised: 26 May 2010 / Accepted: 30 May 2010 / Online publication: 14 Jun 2010 1. INTRODUCTION
Urinary studies indicate elimination half life of approximately 4 h. Salbutamol sulphate is given by mouth The floating drug delivery systems can be retained in in a dose of 2 to 4 mg three to four times a day [9]. the stomach prolongs overall gastrointestinal transit time Salbutamol sulphate requires multiple daily drug dosage in and improves the oral bioavailability of the drugs that are order to maintain adequate plasma concentrations. having site-specific absorption from the stomach or upper Therefore, salbutamol sulphate has all the characteristics part of the small intestine. These systems help in suitable for developing floating dosage form which would continuously releasing the drug before it reaches the increase its oral bioavailability. The floating drug delivery absorption window, thus ensuring optimal bioavailability systems can be retained in the stomach and assist in [1]. Therefore different approaches have been proposed to improving the oral sustained delivery of drugs that have an retain the dosage form in the stomach including bioadhesive absorption window in a particular region of the systems [2], swelling and expanding systems [3,4], floating gastrointestinal tract. These systems help in continuously systems [5,6] and delayed gastric emptying devices [7]. The releasing the drug before it reaches the absorption window, principle of buoyant preparation offers a simple and thus ensuring optimal bioavailability. High solubility of practical approach to achieve increased gastric residence salbutamol sulphate was a major challenge in designing its time for the dosage form and sustained drug release. controlled drug delivery system. In this study, methyl Salbutamol sulphate is a sympathomimetic amine which cellulose, methocel K4M and K100M were used as is used as a bronchodilator in the treatment of reversible buoyancy agents as well as a release-retarding polymer. In bronchospasm. It is almost exclusively metabolised by order to develop the floating matrix tablet of salbutamol conjugation to a 4’-o-sulphate ester in the intestinal wall and sulphate it is necessary to optimize both the residence time liver. Salbutamol sulphate is freely soluble in water and has of the system in the gastro intestinal tract and release rate of site-specific absorption in stomach and upper part of small intestine [8]. The maximum plasma concentration occurs In context of the above principles, a strong need was within 2.5 h and plasma half life ranges from 2.7-7.0 h. recognized for the development of a dosage form to deliver 2010 PharmaInterScience Publishers. All rights reserved. www.pharmainterscience.com Sarath Chandiran et al., Int J Pharm Biomed Sci 2010, 1(1), 12-15 Formulation of salbutamol floating matrix tablets 4.8% 4.8% 4.8% 4.8% 4.8% 4.8% 4.8% 4.8% 4.8% 4.8% 4.8% 4.8% stearate 1.5% 1.5% 1.5% 1.5% 1.5% 1.5% 1.5% 1.5% 1.5% 1.5% 1.5% 1.5% alcohol q.s q.s q.s q.s q.s q.s q.s q.s q.s q.s q.s q.s Total weight of tablet-150mg, Hardness-5 kg/cm2 (F1 to F12) Hardness – 10 kg/cm2 (F1, F2, F3) Physical parameters and floating behaviour of salbutamol floating matrix tablets Fig.1. Effect of hardness and stearic acid on floating behaviour of salbutamol matrix tablets in simulated gastric fluid pH 1.2 c) F10, F11 and F12 of hardness 5 kg/m2 and with different stearic acid concentrations 2010 PharmaInterScience Publishers. All rights reserved. www.pharmainterscience.com Sarath Chandiran et al., Int J Pharm Biomed Sci 2010, 1(1), 12-15 salbutamol sulphate in the stomach and to increase the 2.5. In vitro drug release profile efficiency of the drug, providing controlled release action. The present investigation applied a systematic balance The drug release was studied using USP Paddle between floating lag time, floating duration, and in vitro dissolution apparatus in 900 mL of 0.1HCl (stimulated drug release for the development of floating dosage forms of gastric fluid) at 37 ± 0.5ºC at 50 rpm [11,12]. The 5 mL of salbutamol sulphate suitable for a once-daily formulation the sample were withdrawn at 0.25, 0.5, 0.75, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, up to 12 h. The samples were replaced by an equivalent volume of dissolution medium. The absorbance 2. MATERIALS AND METHODS
of the sample was measured by UV-Spectrophotometrically at 276 nm [13]. 3. RESULTS AND DISCUSSION
Salbutamol sulphate obtained as gift sample from Cipla Private Ltd and Methylcellulose, HPMC K100M, HPMC The physical parameter (hardness, shape) and floating K4M, PVP K30, Microcrystalline cellulose were as gift time of all fabricated tablets depicts in Table 2, Fig.1. The in samples from Micro Laboratory Limited, Bangalore. All vitro releases of the drug from various floating matrix tablets other ingredients were of analytical grades and were used as were shown in Fig.2. In this F1, F2, F3, formulation were made at two different hardness and shapes and evaluated their floating behavior in artificial stimulated gastric fluid 2.2. Formulation of floating matrix tablets from that the tablet which have minimum hardness of about 5 kg/cm2 and round shaped tablet were shows better Floating matrix tablet were prepared by non- buoyancy as compared with highest hardness and oval effervescent and wet granulation methods using shaped tablet (Table 2 and Fig.1). The weight variation test hydrocolloids (Methylcellulose, HPMC K100M, HPMC of all fabricated batches complies with the IP limits. From K4M) as buoyancy agents [10]. The composition of the that above result the other formulation were made with formulation is given in Table 1. The concentration of the hardness of about 5 kg/cm2 and round shape tablet. polymer for floating matrix tablet was optimized under experimental formula and condition of the preparation to float in the stomach up to 24 h. The ingredient except glidants and lubricant were thoroughly mixed and passed through sieve no.60. Granulation was done with a solution calculated quantity of PVP K30 (4.8%) in sufficient isopropyl alcohol. The wet mass passed through the sieve no. 10 and dried at 45-55ºC for 2 h. The dried granules were sized by sieve no.22 and mixed with magnesium stearate and talc. The granules were compressed into tablet on a 10- station Rotary Remerick tablet punching machine using 7 mm punch. The tablets were compressed at two different The prepared floating matrix tablets were evaluated for hardness, weight variation, buoyancy characteristics. Pfizer hardness tester measured hardness. Floating time were determined using USP dissolution Fig.2. Invitro release profile of salbutamol from different hydrophilic apparatus at 100 rpm, using 900 mL of 0.1N HCl (stimulated gastric fluid) pH 1.2 and temperature of the medium maintained at 37 ± 0.5ºC throughout the study [10]. The duration of the floating time is the tablet float in the It shows hardness and shape also will interfere in dissolution medium (including buoyancy lag time). floating behaviors. The all-hydrophilic matrix tablet (F1, F2, 2010 PharmaInterScience Publishers. All rights reserved. www.pharmainterscience.com Sarath Chandiran et al., Int J Pharm Biomed Sci 2010, 1(1), 12-15 F3, F4, F5, and F7, F8, F9) shows their invitro drug release REFERENCES
less than 12 h. The formulation (F6) is control the drug release up to 12 h (HPMC K100M [1] Singh BN, Kim, KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release included in formulation F10, F11, and F12 with an intention to retard the drug release from the hydrophilic matrix by [2] Santus G, Lazzarini G, Bottoni G, Sandefer EP, Page RC. An in vitro- in vivo investigation of oral bioadhesive controlled release furosemide reducing the penetration of water into the floating matrix formulations. Eur J Pharm Biopharm 1997, 44, 39. tablet. It will control the drug release up to 24 h. Hence we [3] Deshpande AA, Rhodes CT, Shah NH, Malick AW. Controlled- concluded that the hydrophilic floating matrix tablet without release drug delivery systems for prolonged gastric residence: an overview. Drug Dev Ind Pharm. 1996, 22, 531. stearic acid could not control the drug release above 12 h. [4] Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of a The incorporation of stearic acid into the hydrophilic matrix novel controlled-release system for gastric retention. Pharm Res 1997, tablets prepared by using HPMC K100 (F11, F12) shows [5] Menon A, Ritschel WA, Sakr A. Development and evaluation of a well-controlled and sustained release more than 12 h. monolithic floating dosage form for furosemide. J Pharm Sci 1994, 83, 239. 4. CONCLUSIONS
[6] Whitehead L, Fell JT, Collett JH, Sharma HL, Smith AM. Floating dosage forms: an in vivo study demonstrating prolonged gastric retention. J Control Release 1998, 55, 3. In conclusion, the result of this study based on invitro A means to address regional variability in performance, the drug release delays which suggest that intestinal drug absorption. Pharm Technol 2003, 27, 50. sustain release floating matrix tablet can be prepared by non [8] Swarbrick J, Boylon J.C, Encyclopedia of Pharmaceutical Technology, effervescent method (HPMC K100M at 50% and [9] Lipworth BJ, Clark RA, Dhillon DP, Charter MK, Palmer JBD, incorporation of stearic acid 25%). The formulations, which McDevitt DG. Single dose and steady-state pharmacokinetics of 4 mg have stearic acid retards the drug release by controlling the and 8 mg oral salbutamol controlled-release in patients with bronchial asthma. Eur J Clin Pharmaco 1989, 37, 49. water penetrations in to the floating matrix tablets, sustained [10] Basak SC, Nageswara Rao K, Manavalan R. Development and in-vitro their drug release above 12 h. The floating matrix tablets evaluation of an oral floating matrix tablets formulation of with minimum hardness of 5 kg/cm2 and round shaped ciprofloxacin. Indian J Pharm Sci 2004, 66, 313. [11] Goole J, Vanderbist F, Amighi K. Development of new multiple unit levodopa sustained release floating dosage form. Int J Pharm 2004, 334, 35. ACKNOWLEDGEMENTS
[12] Patel VF, Patel NM. Statistical evaluation of influence of viscosity of polymer and type of filler on dipridamole release form floating matrix tablets. Ind J Pharm Sci 2007, 69, 51. The authors are sincerely thankful to our Secretary Sri [13] Srinivasan K, Shirwasikar A, Joesph A. Simultaneous estimation for C. Srinivasa Baba, Gokula Krishna College of Pharmacy, the analysis of salbutamol sulphate and ambroxal hydrochloride in solid dosage forms by ultraviolet spectroscopy. Indian Drugs 2005, 42, Sullurpet, Nellore district, Andhra Pradesh, India. 2010 PharmaInterScience Publishers. All rights reserved. www.pharmainterscience.com

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