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ORIGINAL/BRIEF
Year : 2012  |  Volume : 4  |  Issue : 5  |  Page : 84-85  

Preparation, optimization and characterization of multiple unit microspheres containing kollidone SR


Nootan Pharmacy College, Visnagar, Gujarat, India

Date of Web Publication21-Mar-2012

Correspondence Address:
Marvin I Patel
Nootan Pharmacy College, Visnagar, Gujarat
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0975-7406.94149

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   Abstract 

The present investigation described the influence of viscosity and drug: Polymer ratio on Hydrochlorothiazide release. Floating microspheres loaded with hydrochlorothiazide were prepared by Emulsion solvent evaporation method. The prepared microspheres were evaluated by micromeritics properties, in vitro drug release, floating ability and drug entrapment efficiency.

Keywords: Hydrochlorthiazide, multiple unit microspheres, kollidone


How to cite this article:
Patel MI, Patel RR, Patel JK. Preparation, optimization and characterization of multiple unit microspheres containing kollidone SR. J Pharm Bioall Sci 2012;4, Suppl S1:84-5

How to cite this URL:
Patel MI, Patel RR, Patel JK. Preparation, optimization and characterization of multiple unit microspheres containing kollidone SR. J Pharm Bioall Sci [serial online] 2012 [cited 2020 Sep 24];4, Suppl S1:84-5. Available from: http://www.jpbsonline.org/text.asp?2012/4/5/84/94149

Floating microspheres have a bulk density less than gastric fluid and so remain buoyant in the stomach for a prolonged period of time. While the system floats over gastric contents, the drug is released slowly at the desired rate from the system, therefore improving bioavailability of drug and better control over the fluctuations in plasma drug concentration. Thus it not only reduces dosing frequency but also reduces side effects like gastric irritation and major problem like dose dumping thereby greatly increasing patient compliance. [1]

Hydrochlorothiazide is a thiazide diuretic commonly prescribed for treatment of hypertension, congestive heart failure and edema. It is mostly absorbed from the duodenum and the first part of the jejunum. [2]

Bioavailability of hydrochlorothiazide was enhanced when given with food through delaying of gastric emptying in both cases. Bioavailability was lower from SR formulation such as pellets compared to an IR tablet, because the SR formulation passed the drug absorption sites before from completed the drug release. These studies support the absorption window theory for hydrochlorothiazide and therefore a higher bioavailability of the drug in a GRD can be expected if there is a prolonged gastric residence time. [2]


   Materials and Methods Top


Floating microspheres loaded with hydrochlorothiazide were prepared by Emulsion solvent evaporation method. [3] Formulations were prepared using different polymers Kollidone SR, cellulose acetate, Acrycoat S 100, Methocel K4M, Methocel K15M, Methocel K100M. Drug and polymer in proportion 1:2, (drug:Polymer) were dissolved in organic solvent (Ethanol and Acetone). This clear solution was poured slowly as a thin stream in oil phase; about 100 ml of liquid paraffin solution with continuous stirring at a speed of 500 rpm using mechanical stirrer at room temperature until complete evaporation of solvent took place. The floating microspheres were collected by decantation, while the non floating microspheres were discarded along with any polymer precipitates. The microspheres were then dried overnight at 40 0 C. The microspheres were weighed and stored in desiccators until further analysis.


   Results and Discussion Top


Several preformulation trials were undertaken for various proportions of drug and polymer by variation of the ethyl acetate-acetone ratio and dichloromethane-ethanol ratio. Kollidone SR, Acrycoat S 100 and Cellulose acetate were selected as matrixing agent considering its widespread applicability and excellent gelling activity in sustain release formulations and also having the pH-independent and reproducible drug release profile. It was found that Kollidone SR microspheres show desirable high drug content, yield, floatation and adequate release characteristics and hence was suitable for development of a controlled release system.

In the present study, in vitro release studies of the floating microspheres were carried out in 0.1 N hydrochloric acid at 37°C for a maximum period of 12 hours. At different time intervals, samples were withdrawn and cumulative % drug release was calculated. The percentage drug release of all the formulations is presented in [Figure 1]. Out of 9 formulations tried, the formulation K 1 was found to be satisfactory; since it showed prolonged and complete release with 94.75% at end of 12 h.
Figure 1: % Drug release of all nine formulations

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   Conclusion Top


Multi unit gastroretentive drug delivery system has additional advantage of absence of dose dumping as in single unit drug delivery. The present investigation described the influence of the drug: Polymer ratio on Hydrochlorothiazide release. The release and drug entrapment efficiency of the microspheres were affected by the different polymers. It was found that the Kollidone SR had a dominant role in the drug release from microspheres rather than Acrycoat S 100 and Cellulose acetate. And it can be given in hard gelatin capsule form. Therefore, it may be concluded that drug loaded floating microspheres in combination with Kollidone SR are a suitable drug delivery system for Hydrochlorothiazide.

 
   References Top

1.Arora S, Ali J, Ahuja A, Khar RK, Baboota S. AAPS Pharma Sci 2005;6:47.  Back to cited text no. 1
    
2.Herman J, Remon JP, Lefebvre R, Bogaert M, Klinger GH. The dissolution rate and bioavailability of hydrochlorothiazide in pellet formulations. J Pharm Pharmacol 1988;40:157-60.  Back to cited text no. 2
    
3.Kale R, Rao BS, Sharma S, Ramanmurthy KV. Int J Pharm Excp 2001;:64-5.  Back to cited text no. 3
    


    Figures

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