Research Journal of Pharmaceutical Dosage Form and Technology

S. Shanmugam ¹, K. M. Sandhiya ¹, T. Ayyappan ¹, K. Sundaramoorthy ¹, T. Vetrichelvan ¹

Affiliations
1 Department of Pharmaceutics. Adhiparasakthi College of Pharmacy, Melmarvathur-603 319, Tamilnadu, IN

Abstract

In the present investigation, an attempt was made to formulate the oral sustained release matrix tablets of Ambroxol HCl in order to improve efficacy, reduce the frequency of administration, and better patient compliance. Ambroxol Hydrochloride is a potent mucolytic agent capable of inducing bronchial secretions used in the treatment of respiratory disorders. Differential scanning calorimetric analysis confirmed the absence of any drug polymer interaction. Matrix tablets of Ambroxol Hydrochloride were formulated employing hydrophilic polymers HPMC K100M, Carbopol 934P and hydrophobic polymer Ethyl cellulose as release retardant polymers. The powder blend was evaluated for micromeritic properties. The sustained release matrix tablets were prepared by direct compression technique. The tablets were evaluated for thickness, diameter, weight variation test, hardness, friability, and drug content. The in vitro drug release characteristics were studied in simulated gastric fluid (2 hours) and intestinal fluid for a period of 6hours using USP type II dissolution apparatus (total 8hours). The results of dissolution studies indicated that formulation F3 (drug to polymer 1:1.06), the most successful of the study and exhibited satisfactory drug release in the initial hours and the total release was very close to the theoretical release profile. Matrix tablet containing HPMC K 100M (F3) formulation were found to show good initial release (14.8% in 2 hrs) and extended the release (90% in 11 hrs). The n value for F3 obtained from Korsmeyer - peppas model confirmed that the drug release was anomalous diffusion mechanism.

Keywords

Ambroxol HCl, Hydroxypropyl Methylcellulose, Carbopol 934P, Ethyl Cellulose.

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S. Shanmugam ¹, T. R. Ramvignesh ², K. Sundaramoorthy ², T. Ayyappan ², T. Vetrichelvan ³

Affiliations
1 Adhiparasakthi College of Pharmacy, Melmaruvathur – 603 319, Tamilnadu, IN
2 Adhiparasakthi College of Pharmacy, Melmaruvathur – 603 319 Tamil Nadu, IN
3 Adhiparasakthi College of Pharmacy, Melmaruvathur – 603 319, Tamil Nadu, IN

Abstract

Aciclovir, an antiviral is effective against human Herpes Simplex viruses, commercially available as a 3 % w/w eye ointment to be applied 5 times a day in the eye. The poor therapeutic response exhibited by conventional ophthalmic ointments due to rapid precorneal elimination of the drug may be overcome by the use of an ocusert inserted in the cul-de-sac of lower eye lid. Inserts containing Aciclovir were prepared by using solvent casting method. Drug reservoir and rate controlling membrane were prepared using different hydrophilic and hydrophobic polymers respectively with Poly Ethylene Glycol 400 as the plasticizer. DSC and IR spectral studies were performed to confirm the interaction of drug and polymers in formulation. The ocuserts were evaluated for their physico chemical properties, mechanical properties and in-vitro release characteristics. A zero order release formulation VI was subjected to UV irradiation for sterilization. The developed formulation was stable, sterile and non-irritant.

Keywords

Aciclovir, Ocusert, Diffusion, Polymers.

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S. Sandhya Raj ¹, K. Sundramoorthy ¹, T. Vetrichelvan ¹

Affiliations
1 Department of Pharmaceutics, Adhiparasakthi College of Pharmacy, Melmaruvathur, Kanchipuram Dst.-603391, Tamilnadu, IN

Abstract

Sustained release alginate microcapsules of valsartan were prepared by orifice-ionic gelation method using Hydroxy Propyl Methyl Cellulose, (viz, 50 cps, K4M) as mucoadhesive polymer. Microcapsules were discrete spherical and free flowing. Encapsulation efficiency varied from 68.42% to 85.46%. Microcapsules were evaluated for % yield, drug content uniformity, particle size distribution, surface morphology(scanning electron microscopy), percentage moisture loss, in vitro drug release profile, and mucoadhesion study by in vitro wash off test, short term stability ,and drug excipients interactions (DSC and IR spectroscopy). The formulation prepared by using alginate - Hydroxy propyl methyl cellulose (K4M) in the ratio of 5:1 along with magnesium stearate, emerged as the overall best formulation based upon their drug release characteristics (in phosphate buffer 6.8). This formulation showed slow release up to 12 hrs. In vitro drug release followed first order kinetics, fickian diffusion mechanism (n<0.5) and the results had proven the release of the best formulation had extended up to 12 hrs according to t50%, t70% and t90% and the values. All the microcapsules exhibited good mucoadhesive property in the in -vitro wash off test. Accelerated stability studies were carried out for short term studies of formulations according to ICH and Q 1 A (R2) guidelines. These mucoadhesive microcapsules are thus suitable for oral controlled release of valsartan.

Keywords

Valsartan, Mucoadhesive Microcapsules, Orifice Ionic Gelation Method, Hydroxy Propyl Methyl Cellulose (50 Cps, K4M).

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S. Shanmugam ¹, S. Banthala Rajan ¹, T. Ayyappan ¹, K. Sundaramoorthy ¹, T. Vetrichelvan ¹

Affiliations
1 Adhiparasakthi College of Pharmacy, Melmaruvathur-603 319, Tamilnadu, IN

Abstract

In the present investigation, an attempt was made to formulate the oral sustained release matrix tablets of zidovudine in order to improve efficacy, reduce the frequency of administration, and better patient compliance. Differential scanning calorimetric analysis confirmed the absence of drug polymer interaction. The sustained release tablets were prepared by wet granulation method using different polymers viz, hydroxypropyl methylcellulose, xanthan gum, and ethyl cellulose as release retardant polymers, alcoholic solution of polyvinylpyrrolidone were used as granulating agent. In- vitro release studies were carried out at pH1.2 for first 2 hrs followed by phosphate buffer at pH7.4 over a period of 8hrs using USP dissolution apparatus. The formulated granules showed satisfactory flow properties. All the tablets formulation showed acceptable pharmaco technical properties and complied with pharmacopoeial standards. The in-vitro release profiles from tablets of drug and different polymer ratio were applied on various kinetic models. Based on t90% values the formulation F9 was found to show good initial release (12% in 2 hrs) and may extend the release (90% in 10 hrs) and can overcome the disadvantages of conventional tablets of Zidovudine. The n value obtained from korsmeyer - peppas model confirmed that the drug release was non- fickian diffusion mechanism.

Keywords

Zidovudine, Matrix Tablets, Hydroxypropylmethylcellulose, xanthan Gum, Ethyl Cellulose.

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B. N. Kumar Darapu ¹, K. Sundaramoorthy ², T. Vetrichelvan ²

Affiliations
1 Department of Pharmaceutics, Adhiparasakthi College of Pharmacy, Melmarvathur-603 319, Tamilnadu, IN
2 Adhiparasakthi College of Pharmacy, Melmaruvathur- 603 319, Tamilnadu, IN

Abstract

The present study involves preparation of floating microspheres of Ranitidine Hydrochloride with HPMC K 100, Xanthan gum and Eudragit S‐100 and in various ratios of 1: 1, 1: 2, and 1: 3. Floating microspheres were aimed to achieve an extended retention in the upper gastrointestinal tract, which may result in enhanced absorption and thereby improved bioavailability. The formulations were evaluated for FTIR, drug loading, % entrapment, particle size, SEM, buoyancy, dissolution study and the drug release kinetics. The enhanced floatability of the formulation and its retention in GIT may attribute for the increased bioavailability and decrease in frequency of administration. Comparison of three polymers revealed HPMC to be a suitable candidate for sustained release.

Keywords

Ranitidine Hcl, HPMC K 100, Eudragit S 100, Xanthan Gum.

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