International Journal of PharmTech Research Vol.3, …

1 International Journal of PharmTech ResearchCODEN (USA): IJPRIF ISSN : 0974-4304 , ,pp 1737-1749, July-Sept 2011 Solubility and Dissolution EnhancementProfile of Telmisartan using , , ,Anusha rupenagunta4, *School of Pharmaceutical sciences, Pharmaceutics, Vels University,Pallavaram,Chennai,Tamilnadu, India.*Corres. Author: is Angiotensin II Receptor Antagonist, which is used in the prevention and treatment belongs to class II drug in BCS classification low solubility and high of the major problems with this drug is its low solubility in biological fluids, which results into poorbioavailability after oral to improve the aqueous solubility and dissolution rate of thetelmisartan solid dispersions of drug using different methods were prepared and investigated.

2 Enhancement ofsolubility of Telmisartan was observed with solid dispersion of drug using carriers such as Poly vinyl pyrrolidone-k30, Poly ethylene glycol-4000 and eta -Cyclodextrin. The observed results showed the solid dispersion of drugalmost three times greater than the pure :Telmisartan, Solid dispersion, Aqueous solubility,Bioavailability, IntroductionTelmisartan is Angiotensin II Receptor Antagonist,which is used in the prevention and treatment belongs to class II drug inBCS classification low solubility and of the major problems with this drugis its low solubility in biological fluids.

3 Which resultsinto poor bioavailability after oral of Telmisartan in aqueous medium was verylow mg/ml in bioavailabilityof theTelmisartan was 42-58% and biological half-lifeis only 24 hours that results into poor bioavailabilityafter oral administration. Poor solubility ofTelmisartan leads to poor dissolution and hencevariation in bioavailability. Thus increasing aqueoussolubility and dissolution of Telmisartan is oftherapeutic many number of approaches have been developed toimprove the drug solubility and dissolution solid dispersion is a technique to achievethis goal particularly the poor aqueous soluble drugsin which the drug is incorporated in to water solublepolymeric matrix.

4 In this Research the solubility and bioavailability oftelmisartan in conjugation with various carriers byusing various methods were thissolubility and dissolution study, the various evaluationmethods were carried out to determine the physicochemical properties of physical mixture and soliddispersions in comparison to pure et al PharmTech ,3(3)17382. Materials and MethodsMaterialsTelmisartan was obtained from Orchid health , Methol,Sodium lauryl sulphate,Hydrochloric acid, Poly vinyl pyrrolidone-k30, Polyethylene glycol-4000, and Beta-cyclodextrin wereobtained from fine chemical ltd.

5 , Mumbai. All theother materials used in study were of analytical gradeMethods8-14 Preparation of physical mixturesAccurately weighed quantities of drug andcarrier were weighed taken in a glass mortar weremixed thoroughly. The resultant mixture was passedthrough sieve number 100 # and was stored indesiccators for the complete removal of moisture andwas tested for the content uniformity. Drug: polymerratios of 1:1, 1:2 and 1:4 were Evaporation TechniqueIn this method the drug and carriers are usedin different ratios [1:1, 1:2, 1:4]. The respectiveamount of carrier was dissolved in methanol (20ml)and Telmisartan was added in parts with continuousstirring.

6 The solvent was then removed byevaporation. The prepared dispersions werepulverized and sifted through 100 # and stored indesiccator for further Method7,21-23In this method the drug and carriers are usedin different ratios [1:1, 1:2, 1:4]. Both drug andcarrier was triturated by using a small volume ofethanol and water(1:1) to give a thick paste, whichwas kneaded upto 60 minutes and then kept for air the dried mass was scratched and pulverized andsifted through 100# and stored in desiccator for no: 1 Formula for Telmisartan Physical Batch codeCompositionRatio(Drug:Carrier)1P1 Telmisartan+PVP-K301:12P2 Telmisartan+ PVP-K301:23P3 Telmisartan+PVP-K301:44P4 Telmisartan+PEG-40001:15P5 Telmisartan+ PEG-40001:26P6 Telmisartan+PEG-40001:4 Table no 2.

7 Formula for Telmisartan solid dispersions using SolventEvaporation Batch codeCompositionRatio(Drug:Carrier)1S1 Telmisartan+PVP-K301:12S2 Telmisartan+ PEG-40001:13S3 Telmisartan+PVP-K301:24S4 Telmisartan+PEG-40001:25S5 Telmisartan+ PVP-K301:46S6 Telmisartan+PEG-40001:4 Table no 3: Formula forTelmisartan solid dispersions using Kneading Batch codeCompositionRatio(Drug:Carrier)1D1 Telmisartan+PVP-K301:12D2 Telmisartan+ PEG-40001:13D3 Telmisartan+PVP-K301:24D4 Telmisartan+PEG-40001:25D5 Telmisartan+ PVP-K301:46D6 Telmisartan+PEG-40001 et al PharmTech ,3(3)1739 Preparation Of Beta Cyclodextrin InclusionComplexes and Physical Mixtures OfTelmisartan15,23,26 There are several carriers, which have been reportedfor the preparation of Inclusion complexes by usingvarious methods of preparation described earlier.

8 Thefollowing carriers were selected depending uponsuitability of carriers like Beta Cyclodextrin. It wasselected for their efficiency in increasing thedissolution rate of of physical mixturesAccurately weighed quantities of drug andcarrier were weighed taken in a glass mortar weremixed thoroughly. The resultant mixture was passedthrough sieve number 100 # and was stored indesiccators for the complete removal of moisture andwas tested for the content uniformity. Drug: polymerratios of 1:1, 1:2 and 1:4 were of inclusion evaporation Evaporation Technique In this methodthe drug and carriers are used in different ratios[1:1, 1:2, 1:4].

9 The respective amount of carrierwas dissolved in methanol (20ml) and Telmisartanwas added in parts with continuous stirring. Thesolvent was then removed by evaporation. Theprepared dispersions were pulverized and siftedthrough 100 # and stored in desiccators for MethodIn this method the drug and carriers are usedin different ratios [1:1, 1:2, 1:4] Both drug and carrierwas triturated by using a small volume of ethanol andwater(1:1) to give a thick paste, which was kneadedupto 60 minutes and then kept for air dry. Then thedried mass was scratched and pulverized and siftedthrough 100# and stored in desiccators for no:4 Formula for Telmisartan Physical codeCompositionRatio(Drug:Carrier)1P7 Telmisartan+ -cyclodextrin1:12P8 Telmisartan+ -cyclodextrin1:23P9 Telmisartan+ -cyclodextrin1:4 Table no 5: Formula for Telmisartan Inclusion Complexes using Solvent codeCompositionRatio(Drug:Carrier)1C1 Telmisartan+ -cyclodextrin1:12C2 Telmisartan+ -cyclodextrin1:23C3 Telmisartan+ -cyclodextrin1:4 Table no 6 : Formula for Telmisartan Inclusion Complexes using Kneading codeCompositionRatio(Drug.)

10 Carrier)1C4 Telmisartan+ -cyclodextrin1:12C5 Telmisartan+ -cyclodextrin1:23C6 Telmisartan+ -cyclodextrin1 et al PharmTech ,3(3)17403. Results and Preformulation Organoleptic propertiesTable No: Micromeritic Properties of Telmisartan and ExcipientsTable No: Table No:9 Data for calibration curve of : calibration curve of TelmisartanTests SpecificationObservationColorWhite colored powder White TELMISARTAN PVP-K30 PEG-4000 -CYCLODEXTRIN1 BulkDensity(gm/ml) (gm/ml) (%) s of repose ( ) 48 54 16 25 54.