Orlistat Pellets

The drug acts systemically & prevents breakdown of complex fats in to simple one by tagging to Enzyme Lipase. Since it is a systemically acting drug, in vitro dissolution profile plays a crucial role in governing the pharmacological activities.

The formula employed is non- infringing but has a time dissolution profile of the innovators [Xenical® from Roche]. This assures an optimal pharmacological index.

Orlistat Pellets 50% w/w

Orlistat   is   a tetrahydrolipstatin  designed  to  treat  obesity  by  preventing  the  absorption  of  fats  from  the  human  diet,  thereby reducing  caloric  intake. Orlistat is (S)-2-formylamino-4-methyl-pentanoic acid (S)-1-[[(2S, 3S)-3-hexyl-4-oxo-2-oxetanyl] methyl]-dodecyl ester. Its empirical formula is C₂₉H₅₃NO₅, and its molecular weight is 495.7. It is a single diastereomeric molecule that contains four chiral centers, with a negative optical rotation in ethanol at 529 nm.

Orlistat is a white to off-white crystalline powder. Orlistat is practically insoluble in water, freely soluble in chloroform, and very soluble in methanol and ethanol. Orlistat has no pK within the physiological pH range.

The Innovator

XENICAL is available for oral administration as a turquoise hard-gelatin capsule. The capsule is imprinted with black. Each capsule contains a pellet formulation consisting of 120 mg of the active ingredient, orlistat, as well as the inactive ingredients microcrystalline cellulose, sodium starch glycolate, sodium lauryl sulfate, povidone, and talc. The capsule shell contains gelatin, titanium dioxide, and FD&C Blue No. 2 with black printing ink containing pharmaceutical grade shellac, propylene glycol, strong ammonium solution, potassium hydroxide and black iron oxide.

XENICAL is indicated for obesity management including weight loss and weight maintenance when used in conjunction with a reduced-calorie diet. XENICAL is also indicated to reduce the risk for weight regain after prior weight loss.

MKPPL has developed Orlistat pellets equivalent to innovator product (Xenical) using aqueous technology.

The strength of the pellets is, 50.0% w/w for dose of 60 mg and 120 mg with average capsule fill weight 120 mg and 240 mg in size 3 and 1 capsule.

Orlistat pellets were formulated using the technique of Extrusion and Spheronization. Extrusion eliminates dust during formulation and yields high quality pellets. In the formulation of orlistat pellets PVPK-30, Sodium lauryl sulfate, Micro Crystalline Cellulose etc, are used in different concentrations.  With respect to description the pellets are same like Innovator pellets. The pellets are cylindrical to semispherical in shape. We have developed this product customer specific also with high bulk density of same strength to fit in customer requirement of capsule fill weight. Multimedia Dissolution Profile is compared with Marketed Product i.e. Xenical and similarity results were within the limits in all medias.