# US 8,772,292 B2 · Process for the preparation of a medicament comprising vardenafil hydrochloride trihydrate > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,772,292 B2 - Document ID: US8772292B2 - Status: Granted - Kind: B2 - Application number: 12/600,446 - Filed: 2008-06-12 - Published: 2010-06-24 - Granted: 2014-07-08 - Earliest claimed: 2007-06-12 - Assignees: ratiopharm GmbH - Applicants: Yogesh S. Deshpande; Sandra Brueck; Julia Schulze Nahrup; Birgit Schnitter; Ganesh Gat; Javed Hussain - Inventors: Yogesh S. Deshpande; Sandra Brueck; Julia Schulze Nahrup; Birgit Schnitter; Ganesh Gat; Javed Hussain - Web page: https://patentgrep.com/patent/US8772292B2 ## CPC - A61K 9/2095: {Tabletting processes} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 31/53: having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine (melarsoprol A61K31/555 {; with four nitrogen atoms A61K31/495}) - A61P 15/10: for impotence - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present invention relates to a process for the preparation of a medicament containing vardenafil hydrochloride trihydrate in solid form, in which vardenafil hydrochloride trihydrate is processed with suitable pharmaceutical auxiliaries at a temperature of from approx. 20° C. to approx. 45° C. ## Claims ### Claim 1 A process for the preparation of a medicament containing vardenafil hydrochloride trihydrate in solid form, characterized in that vardenafil hydrochloride trihydrate is processed with suitable pharmaceutical auxiliaries at a temperature of from approx. 20° C. to approx. 45° C., the relative humidity of the processing atmosphere is approx. 30% to approx. 90%, and the processed medicament is coated with a film in a further step at a temperature of from approx. 40° C. to approx. 55° C., the entire process being carried out without a rehydration step, whereby vardenafil hydrochloride trihydrate is processed to the medicament in solid form without loss of hydrate during the entire process. ### Claim 2 (depends on 1) The process as claimed in claim 1, characterized in that the processing temperature is approx. 23° C. and the processing atmosphere is at approx. 33% to approx. 35% relative humidity. ### Claim 3 (depends on 1) The process as claimed in claim 1, characterized in that the vardenafil hydrochloride trihydrate is mixed with suitable pharmaceutical auxiliaries in a first step, the mixture is then pressed and the tablets are coated with a film. ### Claim 4 (depends on 1) The process as claimed in claim 1, comprising the following steps: (a) precompacting of the active compound vardenafil hydrochloride trihydrate in the presence of suitable pharmaceutical auxiliaries, (b) subsequent mixing with further suitable pharmaceutical auxiliaries, (c) pressing and (d) coating. ### Claim 5 (depends on 4) The process as claimed in claim 4, characterized in that according to step (a) the precompacting is carried out in the presence of at least one binder. ### Claim 6 (depends on 4) The process as claimed in claim 4, characterized in that according to step (b) the subsequent mixing is carried out with at least one flow regulator and at least one lubricant. ### Claim 7 (depends on 4) The process as claimed in claim 4, characterized in that according to step (d) the coating is carried out with at least one film-forming agent. ### Claim 8 (depends on 1) The process as claimed in claim 1, characterized in that the suitable pharmaceutical auxiliaries are chosen from binders, flow regulators and/or lubricants and optionally also from fillers and/or disintegrating agents (dissociating agents) and optionally a film-forming agent. ### Claim 9 (depends on 8) The process as claimed in claim 8, characterized in that the binder is chosen from cellulose, cellulose polyvinylpyrrolidone, or starch. ### Claim 10 (depends on 8) The process as claimed in claim 8, characterized in that the flow regulator is chosen from silicon dioxide and/or a glycerol fatty acid ester. ### Claim 11 (depends on 8) The process as claimed in claim 8, characterized in that the lubricant is chosen from magnesium stearate, calcium stearate, fumaric acid, sodium stearyl fumarate, stearic acid, talc, starch, and/or solid polyethylene glycols. ### Claim 12 (depends on 8) The process as claimed in claim 8, characterized in that the disintegrating agent is chosen from crosslinked polyvinylpyrrolidone, starch, sodium carboxymethylstarch, carboxymethylcellulose, alginic acid, calcium alginate, pectic acid, formaldehyde-gelatins, and/or amylose. ### Claim 13 (depends on 8) The process as claimed in claim 8, characterized in that the filler is chosen from microcrystalline cellulose, starch, mono- and disaccharides, sugar alcohols, and/or calcium carbonate. ### Claim 14 (depends on 8) The process as claimed in claim 8, characterized in that the film-forming agent is chosen from water-soluble cellulose derivatives, water-insoluble cellulose derivatives, polyacrylates, polymethacrylates, polyvinylpyrrolidone, polyvinyl acetate phthalate, polyvinyl acetate, polyvinyl alcohols, polyethylene glycol, or fats and sugar syrup. ### Claim 15 (depends on 8) The process as claimed in claim 8, characterized in that the flow regulator is colloidal silicon dioxide or precipitated silicon dioxide, the disintegrating agent is crosslinked carboxymethylcellulose (croscarmellose), crosslinked sodium carboxymethylcellulose (croscarmellose sodium), or maize starch, the filler is modified starch or the film-forming agent is based on HPMC (hydroxypropylmethylcellulose) or based on PVA (polyvinyl alcohol). ### Claim 16 (depends on 3) The process as claimed in claim 3, characterized in that the process comprises no precompacting of the active compound vardenafil hydrochloride trihydrate. ### Claim 17 (depends on 3) The process as claimed in claim 3, characterized in that the film contains one or more pigments. ### Claim 18 (depends on 17) The process as claimed in claim 17, characterized in that the pigment is chosen from iron oxide, aluminum oxide and/or titanium dioxide. ### Claim 19 (depends on 1) The process as claimed in claim 1, wherein said temperature of from approx. 20° C. to approx. 45° C. is approx. 23° C. ### Claim 20 (depends on 1) The process as claimed in claim 1, wherein said relative humidity of the processing atmosphere is approx. 33% to approx. 35%. ### Claim 21 (depends on 1) The process as claimed in claim 1, wherein said temperature of from approx. 40° C. to approx. 55° C. is approx. 45° C.