|Title of Invention||
NOVEL STOMACH-SPECIFIC ORAL LIPOSOMAL FORMULATIONS BY MODIFIED METHOD
|Abstract||The invention relates to a method of oral formulation of irinotecan in alginate coated liposomes for stomach specific release. Thus site specific oral formulations of CPT-11 can improve the safety and convenience by keeping in lactone form.|
FORM - 2
THE PATENTS ACT, 1970
(39 of 1970)
THE PATENTS RULES, 2003
(See section 10 and rule 13)
1. Title of the invention:
Novel stomach-specific oral liposomal formulations by modified method
(a) NAME: Shende Pravin Keshaorao, Gaud R.S.
(b) NATIONALITY: INDIAN
(c) ADDRESS: School of Pharmacy and Technology Management,
SVKM's NMIMS University, V M Mehta Road, Vile Parle (W), Mumbai-400056 (India).
3. PREAMBLE TO THE DESCRIPTION
CPT-11 has shown a broad spectrum of antitumor activity in various disease types including colorectal, lung, cervical, and ovarian cancer. CPT-11 is a prodrug under the class of topoisomerase I inhibitors which, upon administration, is converted to 7-ethyl-10-hydroxycarnptothecin (SN-38), by hydrolysis in the liver. Presystemic metabolism of irinotecan is observed when administered either as a solution with CranGrape juice, as powder-filled capsules, or as semisolid matrix capsules. In order to develop stomach-specific oral formulations of CPT-11 by modified method (microencapsulation) that would overcome the inconvenience and the discomfort of the patient associated with parenteral administration; improve efficacy by reducing side effects and protect its photo degradation.
The invention relates to a method of oral formulation of irinotecan in alginate coated liposomes for stomach specific release. Thus site specific oral formulations of CPT-11 can improve the safety and convenience by keeping in lactone form.
THE FOLLOWING SPECIFICATION PARTICULARLY DESCRIBES THE INVENTION AND THE MANNER IN WHICH IT IS TO BE PERFORMED.
CPT-11-HCI (Irinotecan hydrochloride) is semisynthetic, water-soluble derivative of camptothecin, an alkaloid isolated from Camptotheca acuminate. Although CPT-11 has a potent antitumor activity, preventing DNA synthesis by inhibiting topoisomerase I. It has lethal side effects such as myelosupression and gastrointestinal disorders, with dehydration and electrolyte disorder to maintain serious diarrhea. In the liver, CPT-11 is enzymatically hydrolyzed by carbonylesterase to the active metabolite, SN-38. To overcome the inconvenience and the discomfort of the patient associated with parenteral administration, improve efficacy by reducing side effects and protect from photo degradation, alginate coated liposomes of CPT-11 for stomach specific release is invented. The invention relates to a method of oral formulation of irinotecan in alginate coated liposomes for stomach specific release. Thus stomach specific oral formulations of CPT-11 can improve the safety and convenience by keeping in lactone form.
Liposomes were prepared by microencapsulation vesicle method using sealed type homogenizer and chlorofornVethanol solvent system with alpha tocopherol as antioxidant. The liposomes were coated with sodium alginate solution in absence and presence of calcium carbonate (gas forming agent) and cross linked with calcium chloride solution under agitation with a magnetic stirrer at 800 rpm at ambient temperature. Different batches with different levels of cholesterol, phosphatidylcholine, calcium chloride were prepared and evaluated for particle size, surface morphology, entrapment efficiency, physicochemical interaction between drug and excipients, zeta potential and release studies. Accelerated stability studies were carried out for three months.
|Indian Patent Application Number||1981/MUM/2008|
|PG Journal Number||07/2013|
|Date of Filing||18-Sep-2008|
|Name of Patentee||SHENDE PRAVIN KESHAORAO|
|Applicant Address||SCHOOL OF PHARMACY AND TECHNOLOGY MANAGEMENT, SVKM'S NMIMS UNIVERSITY, V.M. MEHTA ROAD, VILE PARLE (W), MUMBAI,|
|PCT International Classification Number||A61K9/127; A61K31/436; A61K31/685|
|PCT International Application Number||N/A|
|PCT International Filing date|