Abstract
Orphenadrine is an anticholinergic ,antimuscarinic , centrally acting skeletal muscle relaxant .It presents in the form of citrate and HCl salts which are used in treatment of the symptoms of mild Parkinson's disease and also it is used as adjuvant with other drugs in the therapy .
 Many trials were made to formulate Orphenadrine citrate as a plain tablet using wet granulation or direct compression technique in order to get a satisfactory formula through studying the effect of various factors such as binders , diluents and disintegrants types .
 The best formula was obtained by using Poly Vinyl Pyrolidine (PVP) as a binder also the results indicated that starch and mannitol gave acceptable physical properties to the tablets when they were used as diluents . At the same time , the results showed that Avicel which was used as a disintegrant gave an acceptable disintegration and dissolution time in comparison with the reference tablet DISIPAL Ò. In addition , the selected formula was used to study the effect of method of incorporation of disintegrant on the physical properties of tablets .It was found that the intragranular incorporation resulted in a shorter disintegration and dissolution times .The stability of Orphenadrine citrate prepared tablets was also studied upon storage at 50°C, 60°C and 70°C for four months .The drug was fairly stable and the expiration date for the prepared tablet was considered to be equal for 5 years .On the other hand , the results of clinical study on patients suffering from Parkinson's disease indicated that patients with tremor (regular rhythmic oscillation of extremities especially hand and finger ) and mild symptoms of Parkinson's disease showed a good response to the prepared tablets , but it had no effect on patients of dystonia ( fixed upward gaze , neck twisting ,clenching jaws ) and akinesia ( slow down of movement of voluntary muscle and difficulty of initiation of movement ).
 The overall results of this study indicate that the drug can be prepared as tablets , which fit the requirements of British Pharmacopoeia since the prepared tablets gave satisfactory results .
Highlights
The skeletal muscle relaxants are group of compounds used to relieve spasticity & abnormally high muscle tone (1,2 ) .They produce their effects by action on central nervous system (CNS), their mechanism of action not yet understood .There are many theories, which explain the mechanism of action or the clinical uses of muscle relaxants .One of these theories is that they reduce skeletal muscle spasm, possibly through an atropine like central action on cerebral motor centers or on the medulla but they do not have analgesic activity that contribute to their effects in patients with skeletal muscle spasm (3)
Different formulas (1,3,8 and 9 ) were prepared to study the effect of binder type on the hardness, friability, disintegration and dissolution times as shown in table (2) and fig
For example, formula 1 in which Poly Vinyl Pyrolidine (PVP) was used as a binder, showed a good hardness (8.25kg), friability (0.5%),disintegration time (5 mins.) and dissolution time up to 100% (20 mins. ) in comparison with the reference tablet DISPAL .This may be due to the use of PVP in ethanol which has the same viscosity as
Summary
The skeletal muscle relaxants are group of compounds used to relieve spasticity & abnormally high muscle tone (1,2 ) .They produce their effects by action on central nervous system (CNS) , , their mechanism of action not yet understood .There are many theories , which explain the mechanism of action or the clinical uses of muscle relaxants .One of these theories is that they reduce skeletal muscle spasm , possibly through an atropine like central action on cerebral motor centers or on the medulla but they do not have analgesic activity that contribute to their effects in patients with skeletal muscle spasm (3). Different formulas (1,3,8 and 9 ) were prepared to study the effect of binder type on the hardness , friability , disintegration and dissolution times as shown in table (2) and fig
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Schedule a callMore From: Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
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