Soft capsule of butylphthalide and a process for preparing the same

Abstract

The present invention discloses a novel soft capsule of butylphthalide and a process for preparing the same. The soft capsule of butylphthalide is composed of a capsule wall material and a drug-containing oil, wherein the drug-containing oil is essentially composed of butylphthalide and a vegetable oil as the diluent in a weight ratio of about 1:0˜10. The capsule wall material is composed of a capsule wall matrix, a plasticizer and water in a weight ratio of 1:0.2˜0.4:0.8˜1.3. The soft capsule of butylphthalide described in the present invention can mask the strong and special flavour of butylphthalide, and overcome the difficulties associated with formulating oily active ingredient into other oral formulation. The disintegration time of the soft capsule satisfies the requirement of Pharmacopoeia of P.R. China.

1 . A soft capsule comprising butylphthalide, characterized in that it is comprised of a capsule wall material and a drug-containing oil, wherein the drug-containing oil comprises butylphthalide and a vegetable oil in a weight ratio in the range of 1:0 to 1:10.  
   
   
       2 . A soft capsule comprising butylphthalide, characterized in that it is comprised of a capsule wall material and a drug-containing oil, wherein the drug-containing oil consists essentially of butylphthalide and a vegetable oil in a weight ratio in the range of 1:0 to 1:10.  
   
   
       3 . The soft capsule of  claim 1 , wherein the weight ratio of butylphthalide to vegetable oil is in the range of 1:1 to 1:8.  
   
   
       4 . The soft capsule of  claim 3 , wherein the weight ratio of butylphthalide to the vegetable oil is in the range of 1:2 to 1:5.  
   
   
       5 . The soft capsule of  claim 4 , wherein the weight ratio of butylphthalide to the vegetable oil is 1:3.5.  
   
   
       6 . The soft capsule of  claim 1 , wherein the vegetable oil is selected from the group consisting of sesame oil, corn oil, peanut oil, soybean oil, almond oil, peach kernel oil, cotton seed oil, sunflower seed oil, olive oil and mixtures thereof.  
   
   
       7 . The soft capsule of  claim 1 , wherein the butylphthalide is selected from the group consisting of racemic butylphthalide, levo-butylphthalide and dextro-butylphthalide.  
   
   
       8 . The soft capsule of  claim 1 , wherein the drug-containing oil further comprises 0-0.2% of dibutylcarboxyl toluene as an antioxidant relative to the weight of drug-containing oil.  
   
   
       9 . The soft capsule of  claim 1 , wherein the capsule wall material comprises a capsule wall matrix, a plasticizer and water in a weight ratio of 1:0.2-0.4:0.8-1.3.  
   
   
       10 . The soft capsule of  claim 1 , wherein the capsule wall material consists essentially of a capsule wall matrix, a plasticizer and water in a weight ratio of 1:0.2-0.4:0.8-1.3.  
   
   
       11 . The soft capsule of  claim 9 , wherein the capsule wall matrix is selected from the group consisting of gelatin, Arabic gum, and a mixture of gelatin and Arabic gum.  
   
   
       12 . The soft capsule of  claim 9 , wherein the plasticizer is selected from the group consisting of glycerol, sorbitol, and a mixture of glycerol and sorbitol.  
   
   
       13 . The soft capsule of  claim 9 , wherein the capsule wall material further comprises a preservative.