Patent
Sublingual pharmaceutical composition containing an antihistamine agent and method for the preparation thereof
| العنوان: | Sublingual pharmaceutical composition containing an antihistamine agent and method for the preparation thereof |
|---|---|
| Patent Number: | 9,675,551 |
| تاريخ النشر: | June 13, 2017 |
| Appl. No: | 14/353074 |
| Application Filed: | October 25, 2011 |
| مستخلص: | The present invention relates to a stable pharmaceutical composition for sublingual administration comprising a therapeutically effective quantity of an antihistamine agent, in particular Dimenhydnnate and a process for the preparation thereof. |
| Inventors: | Karavas, Evangelos (Pallini Attikis, GR); Koutris, Efthimios (Pallini Attikis, GR); Samara, Vicky (Pallini Attikis, GR); Diakidou, Amalia (Pallini Attikis, GR); Karatzas, Aggelos (Pallini Attikis, GR) |
| Assignees: | EXPERMED S.A. (Kifisia Attikis, GR) |
| Claim: | 1. A pharmaceutical composition in a form of a tablet for sublingual administration comprising Dimenhydrinate or a pharmaceutical acceptable salt thereof, an extragranular disintegrant and an effective amount of pH dependent excipient as a taste masking agent to reduce the numbness of the mucosa, wherein said excipient is insoluble in acidic environment and soluble in neutral or alkaline conditions; wherein the taste-masking agent that reduces the numbness of the mucosa is Poly(methacrylic acid-co-methyl methacrylate) 1:1; wherein the extragranular disintegrant is sodium starch glycolate; and wherein the taste-masking agent that reduces the numbness of the mucosa is from about 5 to about 50 wt % of the total weight of the composition. |
| Claim: | 2. The pharmaceutical composition according to claim 1 , further comprising at least one pharmaceutically acceptable excipient selected from diluents, flavour enhancers, glidants, and lubricants. |
| Claim: | 3. The pharmaceutical composition according to claim 1 , further comprising microcrystalline cellulose, spray-dried mannitol, sodium starch glycolate, vanilla flavour, saccharin acid, silica colloidal anhydrous, magnesium stearate, menthol and talc. |
| Claim: | 4. A process for the preparation of a tablet for sublingual administration comprising Dimenhydrinate or a pharmaceutical acceptable salt thereof, as the active ingredient, and an effective amount of a pH dependent excipient as a taste masking agent, to reduce the numbness of the mucosa, wherein said excipient is insoluble in acidic environment and soluble in neutral or alkaline conditions, and an extragranular disintegrant, wherein said process comprises: Blending the active ingredient with the pH dependent excipient and at least one pharmaceutically acceptable excipient selected from diluents, glidants, and flavour enhancers until complete homogeneity; Kneading the above mixture with ethanol and mixing until uniformity; Drying the wetted mass; Sieving the dried mass and adding to the sieved mixture, the extragranular disintegrant and mixing until uniform; Adding to the obtained mixture, at least one pharmaceutically acceptable excipient selected from glidants and lubricants and mixing until uniformity is achieved; Compressing the resulted mixture into a sublingual tablet dosage form; Optionally, applying a coating; wherein the taste-masking agent that reduces the numbness of the mucosa is Poly(methacrylic acid-co-methyl methacrylate) 1:1; wherein the extragranular disintegrant is sodium starch glycolate; and wherein the taste-masking agent that reduces the numbness of the mucosa is from about 5 to about 50 wt % of the total weight of the composition. |
| Patent References Cited: | 6127385 October 2000 Midha 6372253 April 2002 Daggy 7229980 June 2007 Lee et al. 2007/0092553 April 2007 Tengler 2008/0305166 December 2008 Durig 2009/0004254 January 2009 Maibach 2010/0215730 August 2010 Guy 2010/0240631 September 2010 Bellorini WO9515155 June 1995 WO2011024029 March 2011 WO 95/15155 June 1995 WO 2009078034 June 2009 |
| Other References: | Patel et al. (Int.J. PharmTech Res.2009,1(3); 783-789). cited by examiner Scavone et al. (Biopharmaceutics & Drug Disposition, vol. 11, 185-189 (1990)). cited by examiner Joseph M. Scavone et al. Diphenhydramine kinetics following intravenous, oral and sublingual dimenhydrinate administration Biopharmaceutics&Drug Disposition, vol. 11, No. 3, Apr. 1, 1990 pp. 185-189. cited by applicant |
| Primary Examiner: | Gembeh, Shirley V |
| Attorney, Agent or Firm: | AKC PATENTS, LLC Collins, Aliki K. |
| رقم الانضمام: | edspgr.09675551 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |