Abstract

FORMULATION, CHARACTERIZATION and OPTIMIZATION OF CAPTOPRIL FAST-DISSOLVING ORAL FILMS USING HPMC WITH OTHER POLYMERS

Dr. Ch. Saibabu*, Dr. K. Thejomoorthy and P. Bhargavi

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Abstract

Captopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Captopril may be used in the treatment of hypertension. Captopril, a widely prescribed anti-hypertensive drug belongs to class I under BCS classification and exhibit High solubility and permeability. This oral films enjoys some distinct advantages over other oral formulations such as availability of larger surface area that leads to rapid disintegrating and dissolution in the oral cavity. Oral mucosal delivery via Buccal, sublingual, and mucosal route by use of OTFs could become a preferential delivery method for therapies in which rapid absorption is desired, including those used to manage pain, allergies, sleep difficulties, and central nervous system disorders. Captopril were prepared by solvent casting method using super disintegrants such as, crospovidone and MCC. Captopril is soluble in water but its bioavailability is limited. The dispersion time of films were reduced by super disintegrants like crospovidone and MCC were tried to control the dissolution rate of captopril in its oral films formulation development. The objective of the study is to prepare oral films formulation. There are Eighteen formulations[1] employing selected combinations of the Gelatin, PVA, HPMC, Crospovidone, MCC, PEG 400, citric acid, Sucrose and Trusil mixed flavour RSV were formulated. The oral films were prepared by casting technique and were evaluated. The physical parameters[2] of the Captopril oral films evaluated and Physical appearance is translucent white and surface texture of patch is very smooth, Weight uniformity of films measured without the disintegrating agents with 4% Gelatin, 3% PVA and 4% HPMC were about 63.92 + 0.12, 51.02 + 0.24 and 64.01 + 0.08 mg respectively, Thickness of films measured without the disintegrating agents with 4% Gelatin, 3% PVA and 4%HPMC were about 0.135 + 0.010, 0.125 + 0.005 and 0.130 + 0.010 mm respectively. Folding endurance of films of films prepared without the disintegrating agents with 4% Gelatin, 3% PVA and 4%HPMC were about 272 + 1.674, 265 + 1.205 and 275 + 1.453 respectively, Surface pH of films was determined by the films were allowed in contact with 1ml of distilled water. The surface pH was noted by bringing a combined glass electrode or pH Paper near the surface of films and allowing equilibrate for 1 min and surface pH of the films prepared without the disintegrants from 4% Gelatin, 3% PVA and 4% HPMC were about 6.67 + 0.154, 6.89 + 0.122 and 6.65 + 0.111 respectively, In vitro disintegration time of films limit of 30 s or less for orally disintegrating tablets described in CDER guidance can be applied to fast dissolving oral strips and pharmacopoeial disintegrating test apparatus may be used for this study. Typical disintegration time for films is 5– 30 s, Drug content uniformity study of films was observed average drug content was calculated, the drug was dispersed in the range of 95.00 ± 1.056 to 98.86 ± 1.175%. Suggesting that drug was uniformly dispersed throughout all films. Captopril films are not official in any pharmacopoeia; In vitro dissolution study was tested in SLS solution which is normally recommended for drugs having poor solubility. Drug release was found to be maximum in 0.5% w/v SLS. The in vitro drug release study of mouth dissolving tablets from each batch (Fg, Fp, Fh F1to F18) was carried out in 0.5% w/v SLS solution for 30 mins. From results, formulations showed maximum dissolution rate in 4% crospovidone is 98.35% with 4% Gelatin, 99.27% with 3% PVA and 97.42% with 4% HPMC in 30 min. and with 10% MCC is 95.56% with 4% Gelatin, 96.49% with 3% PVA and 94.64% with 4% HPMC respectively in 30 min.

Keywords: Caprtopril, Gelatin, PVA, HPMC, Crospovidone, MCC, PEG 400, citric acid, Sucrose and Trusil mixed flavour RSV, Oral films.